ANTIBIOTICS

Antibiotics are the substances produced by microorganisms (bacteria, fungi, actinomycetes) which
suppress the growth of or kill other microorganisms without affecting the host tissue at very low
concentration.
An antibiotic is a drug used in the treatment and prevention of bacterial infections. They may either kill
or inhibit the growth of bacteria.
Note: Antibiotics acts against bacteria, fungus, and yeast but not against the viruses.
Antimicrobial agents: The drugs which are used to kill or inhibit the growth of the microbes.
Therapeutics: Therapeutics is the branch of pharmacology which deals with the application of drugs for
the treatment and prevention of diseases.
Historical developments of antibiotics
Sir Alexander Fleming discovered penicillin from a fungus named Penicillium notatum in 1928.
Benzyl penicillin (Penicillin G) is a narrow spectrum penicillin/antibiotic which is effective against
Gram+ve organisms. The use of penicillin is wider in the veterinary practice.
Howard Florey and Ernst Chain in 1945 shared with Sir Alexander Fleming for awarding Nobel Prize.
Professor Waxman discovered Streptomycin from fungus Streptomycis griseus in 1944 which is effective
against Tuberculus organism.
Chloramphenicol was discovered from fungus Streptomycis venezuelae in 1947 that is effective against
Typhoid organism.
Chlortetracycline broad spectrum antibiotic was discovered by Subbarow and Duggar and
Oxytetracycline by Woodard in 1948.
Semi-synthetic penicillin was discovered in 1958.
Some bacteria can produce enzyme –Penicillinase, as a result penicillin can’t work against the respective
organisms.
Cephalosporin’s was invented in 1960 by Giuseppe Brotzu.
Fluroquinolones, a broad spectrum antibiotic was invented by George Lesher and co-workers in 1980
which is effective against bacteria, fungus & yeast.

Classification of antibiotics
On the basis of spectrum antibiotics are
• Broad spectrum antibiotics
• Narrow spectrum antibiotics
Broad spectrum antibiotics: these antibiotics prevent the growth & multiplication of the wide range of
microorganisms such as Gram+ve & Gram-ve bacteria, possibly Rickettsiae. E.g.-Chloramphenicol,
Tetracycline etc
Narrow spectrum antibiotics: these antibiotics prevent the growth & multiplication at narrow range of
microorganisms. e.g. - Penicillin is mainly effective against Gram+ve bacteria, Polymyxin-B are active
only against Gram –ve organisms.
On the basis of types of action, antibiotics are-
• Bacteriostatic agents: they inhibit the growth & multiplication of bacteria.
E.g. - Sulphonamide, Tetracycline, Chloramphenicol etc.
• Bactericidal agents: they destroy or kill the bacteria.
E.g.-Penicillin including Semi-synthetic, Cephalosporin, Streptomycin etc

Bacteriostatic activity (ETDSC3)

Sulphonamides, Oxytetracycline, Chlortetracycline, Doxycycline, Baquiloprim, Chloramphenicol,
Erythromycin, Novomycin, Lincomycin, Tiamulin, Trimethoprim Clindamycin.
Bactericidal activity:
Benzyl penicillin (Penicillin –G)
Penicillin, Cloxacillin, Flucloxacillin, Dicloxacillin, Nafcillin, Oxacillin, Amoxycillin, Ampicillin
(Amoxycillin+Clavulanic acid), Pivampicllin, Bacampicillin, Carbenicillin, Ticarcillin, Cefaloridin,
Cefalotin, Rifampicin, Rifamycin, Cefazolin, Cefacetril, Cefamandol, Cefuroxim, Cefoxitin, Ceforanide,
Cefradine, Cefaclor, Flumequine, Enrofloxacin, Ciprofloxacin, Norfloxacin, Pipermidic acid, Nalidixic
acid, Danofloxacin, Spectinomycin, Colistin sulphate, Aminoglycosides (e.g.- Streptomycin,
gentamycin)
Macrolides: (Erythromycin, Tylosin, Spiramycin, Nitrofurazon, Furazolide, Furaltadone) are
Bacteriostatic in action but in high concentration they are bactericidal.
Combination of antibiotics:
When there is mixed infection combination treatment with antibiotics are required to increase synergistic
action. Examples:
• Bactericidal + Bactericidal drug→ synergism action, e.g.- Gentamycin+ Carbenicillin
• Bacteriostatic + Bacteriostatic drug→ Simple additives, e.g.- Sulphomethazole + Trimethoprim
• Bacteriostatic + Bactericidal→ may be antagonistic, which is not used or required in the field or
practice

On the basis of their structure antibiotics may be classified as-

1. Penicillin: they are again classified into the followings-
a) Natural penicillin: it may be-
➢ Short acting→ Benzyl penicillin (Penicillin-G)
➢ Medium acting→ Procaine penicillin
➢ Long acting→ Benzathine penicillin
b) Semi-synthetic penicillins→ Amoxicillin, Cloxacillin, Ampicillin, Carbenicillin etc
c) Acid resistance penicillin → Phenoxymethyl penicillin, Cloxacillin, Ampicillin etc
d) Penicillinase resistant penicillins→ Cloxacillin, Oxacillin etc
e) Beta lactamase resistant penicillin→ Cloxacillin, Nafcillin etc
2. Cephalosporins→ cefradine, cephalexin, cefapirin etc
3. Macrolides→ Erythromycin, Tylosin, Spiramycin, Azithromycin etc
4. Aminoglycosides→ Gentamycin, Kenamycin, Streptomycin etc
5. Tetracycline→ Chlortetracycline, Oxytetracycline, Doxycycline etc
6. Chloramphenicol→ Chloramphenicol
7. Miscellaneous antibiotics→ Clindamycin.
 Sources of antibiotics
Antibiotics are obtain from-
➢ Fungi→ penicillin, cephalosporin, griseofulvin etc
➢ Bacteria→ Polymyxin-B, Colistin, Bacitracin etc
➢ Actinomycetes→ Aminoglycosides, Tetracycline, Macrolides etc

According to the molecular mechanism of action of drugs antibiotics are classified as follows:
a) Inhibition of bacterial cell wall synthesis→ penicillin, Cephalosporins, Bacitracin etc.(PCB)
b) Impairment of cell membrane functions by increasing permeability→ Polymyxin, Colistin,
amphotericin, nystatin etc
c) Interference with microtubules & microfilaments→ Griseofulvin, Colchicine etc
d) Inhibition of protein synthesis:
➢ By binding with 50S ribosome subunit→ Chloramphenicol, Macrolides, Lincosamides
etc. (LMC)
➢ By binding with 30S ribosome subunit→ Aminoglycosides, tetracycline, spectinomycin
etc.(TAS)
➢ By inhibiting transcription→ Rifamycin, Rifampicin & Rifampin etc
➢ By inhibiting binding of aminoacyl tRNA to the ribosomal A site→ Fusidic acid &
erythromycin etc
➢ Premature termination of peptide chain→ Puromycin
e) Inhibition of nucleic acid synthesis:
➢ Interference in the synthesis of nucleotides→ Fluorouracil, mercaptopurine etc
➢ Alteration of base pairing property of template→ Acridines (Acriflavin, proflavine),
Antiviral drugs etc
➢ Inhibition of DNA & RNA polymerases: RNA polymerases are inhibited by Rifampin &
Rifamycin & DNA polymerases by Acyclovir & Cytarabine
➢ Direct effects on DNA →Alkylating agents
f) Inhibition of bacterial folic acid synthesis by competitive inhibition mechanism→ Sulfa drugs,
Sulfones & paramino salicylic acid or by sequential blockade, Trimethoprim & Sulfa drug
combination

Properties of an ideal antibiotic

➢ Antibiotics should have selective & effective anti-bacterial activity against the wide range of
microorganisms
➢ Antibiotics should have bactericidal activity rather than Bacteriostatic activity
➢ Antibiotics should have characteristics absorption, distribution, fate &excretion
➢ Bacteria should not develop resistance to the drug
➢ Its anti-microbial efficacy should not be reduced by body fluids, exudates, plasma proteins or tissue
enzymes
➢ It should be excreted in urine in bactericidal concentration especially in urinary tract infection. E.g.-
Comparatively tetracycline is an ideal antibiotic
Why antibiotics are not harmful on the animal cell?
Antibiotics are not harmful on the animal cells because of the following reasons-
➢ Antibiotic like penicillin do not act against animal cell because of the absence of cell wall in
animal cell
➢ Antibiotic like Sulfonamide do not act against animal cell because the animal cell do not use
PABA in the synthesis of DNA &RNA like bacteria
➢ Difference in the constitutional & enzyme actions in the animal & bacterial cell that permit the
antibiotic to destroy the bacteria but not the animal cell.

Factors influencing clinical use of antibiotics

a) Combined therapy
b) Route of administration
c) Reaction with blood & tissue fluid, e.g. - Tetracycline reacts with calcium to form bond. The
animal fed calcium rich food should not be given tetracycline. Since tetracycline would not work
as it binds with calcium & remains unabsorbed.
d) Physiological barrier: some antibiotic cannot pass the barrier in the body like
➢ Blood brain barrier: antibiotic cannot pass the blood brain barrier as a result cannot reach
the cerebrospinal fluid. If there is meningitis antibiotics are directly injected to the
cerebrospinal fluid.
➢ Placental barrier: normally the placental membrane resists the passage of antibiotics.
Oxytetracycline should not be administered to the pregnant animal as it inhibits the
calcium, animal might die due to heart failure.
➢ Intestinal barrier: some antibiotic can’t pass the intestinal wall. If administered orally it
will not enter the system. E.g. Gut active sulphonamide and streptomycin work in the
intestinal lumen and mucosa of the intestinal wall only.
➢ Serous membrane: some antibiotics cannot reach the pleura, peritoneum. However some
can reach. E.g.-Streptomycin cannot reach the pleura, peritoneum but Oxytetracycline can
reach there.
➢ Milk barrier: usually penicillin/ Streptomycin can not reach the milk. However, some
higher broad spectrum antibiotics can reach the milk. During mastitis antibiotic is given
directly into the udder through the teat along with systemic antibiotics.
e) Effect on intestinal flora in herbivores: Oxytetracycline damages/ kills rumen flora as a result there
is digestive disturbance. Severe colic occurs in horse while Oxytetracycline is administered orally.
f) Antibiotic & immunity: sometimes there occurs mild infection & antibiotics are not required for
treatment. Normal immunity of the body can prevent the infection to get cure. If we use antibiotics
immunoglobulin will not be produced against the infective agent.
 Penicillin (Benzyl penicillin)
Penicillin was the first antibiotic discovered by Sir Alexander Fleming in 1928 from the mould,
Penicillium notatum
Source:
Penicillin, originally made on a small scale from surface broth culture of the mould is now
manufactured on a vast scale by dup vat culture method using various “medium supplements” & various
species & strains of penicillium moulds.
Stability of penicillin:
➢ Penicillin is relatively unstable. It depends on the followings-
➢ Moisture: penicillin is hygroscopic & deterioration by hydrolysis is rapid. In dry condition, it will
keep for 2 or 3 years, but when in un-buffered aqueous solution the salt lose about 16% activity
at 4°c & 78% at 24°c in 7 days
➢ PH: acid or alkalis cause rapid deterioration in the potency of penicillin solutions. Penicillin is
most stable when it is kept within a range of pH 6-6.5
➢ Temperature: deterioration rate increases with temperature. E.g.- 100°c temperature destroy the
activity of penicillin
➢ Oxidizing & reducing agent: these agents rapidly destroy penicillin
➢ Enzymes: contamination with penicillin –resistant organisms or the enzyme penilllinase produced
by the organisms rapidly destroys the penicillin
➢ Other factors: Cu, Hg, Fe, & Zn etc markedly affect the action of penicillin
Routes of administration of penicillin:
✓ Parenteral route: penicillin should be given subcutaneously & intra muscularly, where former is
better & it should not be given intravenously because of thrombophlebitis
✓ Oral route: inorganic procaine penicillin should not be given orally, because these compounds are
largely destroyed by gastric acidity& bacterial action. The acid resistant penicillin such as
Oxacillin, Cloxacillin, Dicloxacillin & Nafcillin can given orally
✓ Topical route: penicillin can be applied topically or locally as a powder solution or ointment
✓ Intramammary infusion: it can be given intramammary for systemically in the treatment of bovine
mastitis
Toxicity:
There is no toxicity problem in veterinary medicine with penicillin but occasionally allergic skin
reaction may occur in small animals following previous treatment. Some lab animals, but particularly
Guinea pig, show a particular sensitivity to penicillin. Animals showing allergy should be treated with
antihistamines or corticosteroids locally & systemically.
Antibacterial spectrum:
Penicillin-G is a narrow spectrum antibiotic activity is limited primarily to Gram+ve bacteria &
few others. E.g.-Streptococci species, Bacillus anthracis, Actinomyces israelli is sensitive to that
antibiotics.
 Mode of action of penicillin (Benzyl penicillin)
The antibiotics are active when bacteria are multiplying & interfere with the formation of cell wall of
Gram+ve bacteria. Bacteria have a rigid cell wall which protects the protoplasmic membrane from
osmotic & mechanical damage. The rigidity of the cell wall comes from a peptidoglycon (mucopeptide)
network which is consists of N-acetyl glucose amine & N-acetyl muramic acid.
Penicillin inhibits the enzyme transpeptidase which is necessary for the synthesis of mucopeptide. As a
results bacterial cell wall become weak resulting high internal osmotic pressure swelling of bacterial cell
leading to rupture & death.

Why penicillin antibiotics are not generally administered intravenously?

Penicillin are not administered intravenously because of the following reasons-
i. To avoid hypersensitivity reaction & thrombophlebitis
ii. It is advisable in systemic infections to use Parenteral administration of sodium Benzyl penicillin,
intramuscularly, because of penicillin intramuscularly/ intramuscular injection promotes
therapeutic blood ( vessel) level at a rate only very slightly below that of intravenous injections
iii. A depot injection in the form of Procaine penicillin aqueous suspension would be given intra
muscularly. So further antibiotic need be given for about 24 hrs when the intramuscular dose
would be repeated.
iv. The blood level are maintained for getting effective activity of penicillin by continuous slow
absorption from “depot’s” or less (should) soluble & slowly diffusible antibiotic forms

Why penicillin is inactive against Gram-ve bacteria?

Because-
The cell wall of Gram-ve bacteria consists of mucopeptide & endotoxin (lipopolysaccharide). The
extra layer in Gram –ve cell wall, lipopolysaccharide layer, which Benzyl penicillin can’t penetrate

Contraindication, side effect & precaution of penicillin:

1. Allergy (hypersensitivity reaction) to penicillin is the only contraindication, although it is limited
in animal practices.
2. The use of penicillin in pregnancy should be reserved for case consideration essential by the
clinician because safety for use in pregnancy has not been established.
3. Appropriate treatment for systemic reactions should be kept ready in hand to meet the situation
N.B: penicillin & Aminoglycosides must never be mixed in the same bottle because penicillin
inactivates Aminoglycosides.
Clinical application of penicillin:
Bovine mastitis, Anthrax, Erysipelothrix infection, Strangles (Streptococcus equi), Tetanus infection,
Black leg, Pyelonephritis, Actinomycosis/ lumpy jaw (Actinomyces bovis), Actinobacillosis / woody
tongue (Actinobacillus lignieresi), Streptococcal infection in puppies, Leptospirosis, Salmonellosis,
Malignannt edema, Bacillary hemoglobinuria (Clostridium haemolyticum), Syphilis (Treponema
pallidum), Gonorrhoea, Meningitis etc

Dosages of penicillin:
• Parenteral route: 8000 to 20000 units (5-12mg)/kg body wt every 6 hours, if a soluble salt in
water is used; every 12 hours, if a soluble salt in oil with stearate or wax & every 24 hours if
Procaine penicillin is used in an oil suspension. (1600unit=1mg).
• Oral route: cattle, sheep, goat- 20-30 mg/kg body wt 3 times daily
Pigs & poultry-80-100mg/kg body wt twice daily

Trade name of penicillin:

Name Dosage
Pronapen® 40 lac (each vial dissolved with 1ml/10kg bwt i/m daily for 5-7 days
10ml distilled water)
Pronacillin® 40 lac (dissolved in 10ml 1ml/10kg bwt i/m daily for 5-7 days
distilled water)
Penbacillin®inj.(dissolved in 10ml distilled Large animal→1ml/10kg bwt
water) Small animal→0.5-1ml/1kg bwt i/m daily for 5-7 days
 Broad spectrum penicillins (Smisynthetic)
Amino penicillin (Ampicillin, Amoxicillin)
Ampicillin is one of the most interesting & one of the valuable of the semi-synthetic penicillin because
it has (true) broad spectrum antimicrobial activity. i.e active against Gram+ve & Gram-ve bacteria.
Toxicity
It is less toxic, very high doses may be given over a prolong period without producing any toxic
reactions, with the exception of Rabbits, Guinea pig etc.
Antimicrobial activity
Ampicillin is bactericidal in action & is a true broad spectrum antibiotic, both in vivo & in vitro
& is active against a large number of Gram+ve & Gram –ve organisms. But destroyed by β-lactamase.
Ampicillin is not destroyed by gastric juice, so oral administration may be done. Better administration
may be done in empty stomach. It is more useful in respiratory & urinary tract infection, meningitis,
Typhoid fever (Salmonella), bacillary dysentery (Shigella), Listeria infection etc. E.g. - Streptococci,
Staphylococci, Corynebacterium, Clostridium, E.coli, Klebsiella, Shigella, Salmonella, Proteus, Brucella
& Pasteurella etc.
Resistance:
This drug is destroyed by Penicillinase (β-lactamase), producing by Staphylococci & some Gram-
ve strains
Action & uses:
Clinical traits have demonstrated that Ampicillin is of considerable value in the treatment of the following
clinical enteritis in farm & small animals.
1. Cattle: Calf scours& pneumonia, calf enteritis & septicemia due to Salmonella infections, Foul of
the foot, Mastitis due to E. coli infections, Metritis & retained placenta, Pyelonephritis
2. Pig: Enteritis & pneumonia associated with E.coli infections, Erysipeals, Metritis
3. Sheep: Contagious foot rot, Mastitis, Metritis, Pneumonia, Foot abscess
4. Horses: Enteritis & pneumonia in the new born & young foal, Metritis, Respiratory infection,
particularly in association with Equine influenza
5. Poultry: Enteritis due to E. coli infection & clostridial infection
6. Dog: secondary infection associated with dermatitis, Enteritis, ear infection, Pharyngitis &
tonsillitis, post operative wounds, respiratory infections, urogenital infections
7. Cat: secondary infections associated with respiratory viruses
Dosage:
Oral: 4-10 mg/kg bwt
Parenteral: 2-7 mg/kg bwt
Normally given at 24hrs intervals but in very acute cases dose may be given twice daily
In young animals and in acute infection the upper dose level is recommended.
Preparation: Ampicillin is available in powder, tablet, cream, intra mammary & parenteral infection
forms
Trade name:
➢ Ampicillin→20% inj
➢ Acipillin inj
 Amoxicillin
Amoxicillin has a close chemical & pharmacological relation to Ampicillin. Amoxicillin
Differs from Ampicillin in that it is better absorbed when given by mouth in animals, as a result, the
antibiotic levels reached in the food & urine are considerably higher than those obtained with Ampicillin.
Induction of diarrhea is less.
Toxicity: very high doses may be given over a prolonged period without producing toxic reaction/ effect
Action & uses: same as Ampicillin
Dose:
Orally → 10mg/kg bwt twice daily
Parenterally → 7-15mg/kg bwt twice daily.
Amoxivet inj → 8-15 mg/kg bwt for 3-5 days
Chloramphenicol
✓ Isolated from a fungus Actinomyces venezuelae
✓ It is the first antibiotic to be synthesized commercially
✓ A broad spectrum antibiotic effective against both Gram +ve & Gram-ve bacteria & also some
rickettsiae
E.g.- Staphylococci, Salmonella, Pasteurella, Bordetella, Haemophilus, coliform
organisms, Chlamydia, Corynebacterium spp
✓ It is the 2nd drug of choice for anaerobic bacterial infection. Deep infection of the eye (eye ointment)
& infection of the CNS (encephalitis, meningitis) is possible because it crosses blood brain barrier.
✓ It is used especially for the treatment of typhoid.
Mode of action:
It is a bacteriostatic antibiotic that interferes with protein synthesis at the 50S ribosomal subunit.
It also inhibits mitochondrial protein synthesis in mammalian bone marrow cells.
Toxicity:
➢ Circulatory collapse (grey syndrome)
➢ Bone marrow toxicity resulting in fatal aplastic anemia & a reversible depression of
hematopoiesis when given at high doses
Dosage:
Oral administration as capsules or a palmitate suspension
Calves & foals→0.5gm, 2/3times daily
Piglet & lambs→0.25gm 2/3 times daily
Dogs→ up to 165mg/kg bwt daily in 3 equal doses
Cats→ 0.25gm once or twice daily
I/m administration employs Chloramphenicol Sodium Succinate as a 40% solution.
For i/v injection, it is usual to use the Succinate as a 10% solution
Large animal →2-4mg/kg bwt
Sheep, goat, pig, foal& calves→4-10mg/kg bwt.

Side effects/toxicity: Chloramphenicol is quite toxic and causes serious side effects. The most common
side effect is a temporary or permanent depression of bone marrow function that results in cessation of
formation of blood cells.
 This antibiotic has been found to prevent incorporation of hemoglobin by the blood cells leading
to aplastic anaemia. It also causes thrombocytopenia and leucopenia. Other side effects are allergic
responses or neurotoxic reactions. Thus Chloramphenicol is now used in life-threatening situations when
other suitable drugs are inadequate.

Containdication: Chloramphenicol enters into milk; discontinue the drug or do not milkfeed.
 Aminoglycosides
Aminoglycosides are protein in nature, broad spectrum in activity, inhibit protein synthesis of bacteria.
They are bactericidal antibiotics. E.g.-Streptomycin, Neomycin, Gentamycin, Kenamycin, Tobramycin,
Framycetin
Mode of action:
Aminoglycosides

Binding to the 30s subunit of bacterial Interfere with the initiation of DNA replication
ribosome
Interfere with several mechanisms in the mRNA translation process

Responsible for bactericidal effects.

Clinical uses
Aminoglycosides are the drugs of choice for the treatment of serious Gram-ve infection in animals.
However, not all aminoglycosides are equal in the ability to combat these serious infections.
Side effects of amino glycosides antibiotics:
➢ Ototoxicity: vestibular & auditory dysfunction
➢ Nephrotoxicity
➢ Symptoms: low contracting activity, proteinuria, hypokalemia, acute renal acidosis.
➢ Neuromuscular: reduced prejunctional release of acetylcholine which may leads to muscular
paralysis.
➢ Others: enlargement of blind spot, optic neuritis

Streptomycin
➢ Isolated from a fungus Streptomyces griseus in 1943
➢ Streptomycin is relatively more stable than penicillin
➢ Oral formulation of Streptomycin, frequently combined with Sulfonamide drugs & other
compounds are used in the treatment of enteritis
Toxicity & side effects:
➢ Acute toxicity: anaphylactic reaction, nausea, vomiting, rapid collapse & loss of consciousness.
➢ Chronic toxicity: vertigo, irreversible loss of balance (vestibulo toxicity)
Streptomycin has got some side effect due to that reason the structure was being changed & Dihydro
streptomycin was prepared. However, it is also neurotoxic. The side effects are headache & hearing
problem due to toxic effect on 8th cranial nerve. (8th cranial nerve→ auditory→ vestibular & cochlear
nerve)
Antibacterial action: usually bactericidal. It is active against Gram-ve organisms specially against
Mycobaterium spp but some Gram+ve bacteria & the Leptospira are also affected.
Clinical application/uses: Actinomycosis (Lumpy jaw), transit fever, calf & pig scours, mastitis, metritis,
Vibrionic abortion in cattle, Leptospirosis, Enteritis, Cystitis, Septicemia, Brucellosis, Glanders,
Pasteurellosis.
Dose:
➢ Parenterally→5-10mg/kg bwt i/m
➢ orally→20mg/kg bwt
➢ intra mammary→100mg/quarter in lactating cow & 500mg/quarter in dry cow
❖ Used in combination with procaine penicillin for the treatment of Gram+ve & Gram-ve organism,
synergistic effect
Intravenous injection of Streptomycin can produce anaphylactic shock

Neomycin
Isolated from a fungus Streptomyces fradidae
In market, it is available as Neomycin Sulphate which is white or yellow crystal, hygroscopic, odorless,
and highly soluble. It is effective against Streptomycin resistant Gram-ve & acid fast organisms.
Trade name→ Neomycin Sulphate B or Neomycin Sulphate C
About 3% absorption in oral route.
Side effect:
Causes loss of hearing (deafness) due to irreversible damage of the auditory, division of the 8th
cranial nerve, causes kidney damage.
Antibacterial action:
Neomycin is bactericidal, it is a broad spectrum antibiotic with a wide activity against Gram-ve
organism and some Gram+ve organism. Highly effective for the treatment of enteric infection due to
Gram-ve organisms, Effective against Salmonella, E. coli, Klebsiella, Proteus, Enterobacter
Clinical use:
✓ urinary infection due to coliform & skin, eye & ear infection
✓ scour in calves & piglets
✓ mastitis-along with penicillin
✓ solution for dressing wounds & eyes
✓ ointment for superficial conditions like otitis, corneal ulcers, conjunctivitis, keratitis, abscess &
dermatitis
All respond favorably to neomycin treatment, especially where other antibiotics fail
Routes of administration:
✓ Parenterally
✓ Orally
✓ Intramammary: intramammary application neomycin is combined with penicillin to counteract
penicillin resistance & to give a broader spectrum
✓ Topical: topical application usually contain 5mg neomycin Sulphate per ml or per gm in either
aqueous solution or ointment form
Dosage:
✓ 10mg/kg bwt orally
✓ 2.5mg/kg bwt parenterally
These are daily dose & should be divided into 2 or 4 equal doses given at regular interval.

Gentamycin
It is isolated from Micromonospora purpurea
Antibacterial action:
The action on bacteria is bactericidal & effective against Gram-ve as well as some Gram+ve
bacteria like Staphylococcus & certain Mycoplasma.
OR,
It covers many aerobic Gram-ve organisms including Pseudomonas spp, E. coli & some Gram+ve
organism like Staphylococcus spp & certain Mycoplasma. It also effective against Salmonella, Shigella,
Klebsiella, Proteus, Neisseria
Toxicity:
The main effect is Ototoxicity with vestibular function being most often damaged kidney damage
at high dose, respiratory paralysis (rare case) due to neuromuscular blockage which can be treated by
parenteral calcium or by anti-cholinesterase agents such as Neostigmine.
Clinical use:
✓ Urinary tract, respiratory tract & soft tissue infection
✓ Otitis, metritis, eye infection
Usually it is used as skin ointment, ointment in mastitis treatment to avoid toxical
Dosage:
Small animal → 2-4mg/kg bwt
8 hourly i/m or i/v
Large animal → 3.5-5mg/kg bwt
Routes of administration:
✓ Parenterally
✓ Topical application: are widely used in some countries for the treatment of eye & ear condition.
The lower dose is suitable for kidney & urinary tract infection
Best use→ topical ≥ oral ≥ parenteral
Contra indication & side effects:
✓ Gentamycin injection should not be used in pregnancy except in life threatening situations
✓ Do not use in animals known to have auditory or equilibrium dysfunction or malfunction of the
kidney
✓ Withdrawal period: Meat → 12 days
Milk → 3 days
 Kenamycin
− Antibacterial activity similar to that of Neomycin, use for similar purpose
− Topical preparation for ear infection & oral preparation for enteric infection
− Antibacterial activity against E. coli, Salmonella, Klebsiella
Toxicity:
Parenteral administration may cause permanent damage to the cochlear & vestibular portions of
th
the 8 cranial nerve
Clinical use:
Necrotic enteritis, pneumonia, diarrhea, hemorrhagic dysentery & atrophic rhinitis in swine, E.
coli, Streptococcus fecalis, Staphylococcus aureus & Proteus infection in dog, Colibacillosis in chickens,
Bovine mastitis
Dose: 15mg/kg bwt/day in 3 divided doses i/m

Tobramycin
Tobramycin, like Gentamycin, is active against Pseudomonas spp & it is expensive.
 Tetracycline
Commonly used tetracyclines are
1. Chlortetracycline
2. Tetracycline
3. Oxytetracycline
4. Doxycycline
5. Minocycline
Tetracycline is Bacteriostatic but in higher dose it is bactericidal
Antibacterial action/ Spectrum
Tetracyclines are broad spectrum antibiotics & are highly effective against Gram+ve but less
effective against Gram –ve bacteria, Rickettsia, Chlamydia, Anaplasma etc. It does not acts against
Pseudomonas & Proteus species.
Mode of action
Tetracycline inhibits protein synthesis to 30S ribosomal subunit in susceptible organism & prevent
the access of aminoacyl tRNA to the acceptor site on the mRNA ribosome complex. As a result, the
peptide chain fails to grow & thereby inhibit protein synthesis.
Field use/ therapeutic indication:
a) Enteric infection→ bacteria used only
b) Respiratory infection→ Mycoplasma
c) Hemorrhagic septicemia(H.S)
d) Transit fever
e) Pasteurellosis
f) Poultry diseases (Colibacillosis, E.coli, Infectious coryza by Hemophilus gallinarum)
g) Chronic Respiratory disease(CRD) by Mycoplasma gallinarum
h) Air saculitis by Mycoplasma synovae
i) Clostridial dermatitis by Clostridium septicum
j) Necrotic enteritis by Clostridium perfringens
k) Pullorum disease by Salmonella Pullorum (drug can be given with feed & water)
l) Mastitis
m) Foot rot
n) Anaplasmosis
o) Theileriasis
p) Early ehrlichia a tick borne disease
q) Ehrlichia canis
In addition, tetracycline are also employed as feed additive for promoting growth
Forms of tetracycline are Tablet, Capsule, Ointment, and Spray
Dose: (Oxytetracycline is an irritant injection)
− Orally: 10-20mg/kg bwt
− In poultry: the dose required high due to high metabolic rate of poultry
10-60gm/100kg feed orally
0.1-0.3gm/liter water
− I/M route: 20mg/kg bwt
In Doxycap the dose is repeated every 12hours
Toxicity
− Though tetracyclines are relatively nontoxic, yet produce some adverse effect.
− Supra-infection (due to gastrointestinal disturbances), irritation, Photo-toxicity, Hepato &
Nephro-toxicity, Hypersensitivity, Effect on cardiovascular system.
− In small animal→ Nausea, Vomition, Diarrhea, Abdominal pain may occur
Tetracycline should not be given to the horses due to producing enteritis.

Contraindication and side effects

✓ Chlortetracycline is slightly more irritant than the other tetracycline when administrated
✓ Oxytetracycline is contraindicated in case of chronic renal failure & presence of hepatic
dysfunction
✓ Tetracycline are deposited in developing bones & teeth & may produce staining and enamel
hypoplasia and therefore, they should not be prescribed in pregnant, milch and newborn animals
✓ Treated animals should not be slaughtered for human consumption within 21days after treatment
✓ Milk from treated animals should not be delivered for human consumption for a 7 days period.

Trade name:
Name Dose
Renamycin Animal Formula Tablet 1 tab/100 kg b wt.
Inj. Renamycin 1ml/10 kg b wt in large animals
Inj. Renamycin 100 1ml/20 kg b wt in large animals
Inj. Renamycin LA 1ml/10 kg b wt in large animals

Erythromycin
Erythromycin belongs to a group of drugs called macrolide antibiotics. Macrolide antibiotics slow
the growth of, or sometimes kill, sensitive bacteria by reducing the production of important proteins
needed by the bacteria to survive.
Uses: Erythromycin is used to treat a wide variety of bacterial infections.
Mechanism of action:
Erythromycin displays bacteriostatic activity or inhibits growth of bacteria, especially at higher
concentrations. By binding to the 50s subunit of the bacterial rRNA complex, protein synthesis and
subsequent structure and function processes critical for life or replication are inhibited.

Erythromycin may cause side effects:

✓ upset stomach
✓ diarrhea
✓ vomiting
✓ stomach pain
✓ loss of appetite
Some side effects can be serious:
• rash
• itching
• hives
• difficulty breathing or swallowing
• wheezing
• yellowing of the skin or eyes
• dark urine
• pale stools
• unusual tiredness
• pain in the upper right part of the stomach
• seizures
• fast, pounding, or irregular heartbea
Dosage:
− 5-10 mg/kg b.wt. orally
− 1-5 mg/kg b.wt. parenterally

Trade name:

Name Dose
Erom vet (Kemiko Pharmaceuticals) 1gm/litre drinking water for 5-7 days
Eryxel vet (SKF) 1gm/litre drinking water for 5-7 days
Combination of erythromycin, sulpphadiazine and trimethoprim
Micronid (Renata Ltd) 0.5-1gm/litre drinking water for 5-7 days
EST vet powder (Eon 0.5-1gm/litre drinking water for 5-7 days
Pharmaceuticals)
Eraprim vet (Acme Laboratories 0.5-1gm/litre drinking water for 5-7 days
Ltd)
Eryvet (ACI Limited). 0.5-1gm/litre drinking water for 5-7 days
 Cephalosporins
Definition: These are a group of semi synthetic antibiotics derived from cephalosporin-C obtained from
a fungus Acremonium (cephalosporium). They are chemically related to penicillins: the nucleus consists
of a -lactum ring fused to a dihydrothiazine ring (7-aminocephalosporanic acid). By addition of different
side chains at position 7- of -lactum ring (altering spectrum of activity) and position 3 of dihydrothiazine
ring, a large number of semi synthetic compounds have been produced. These have been conventionally
divided into four generations. This division has chronological sequences of development but more
importantly, takes into consideration the overall antibacterial spectrum as well as potency.

Classification of cephalosporins:
First generation: Moderate -lactamase stability.
• Parenteral:-
i. Cephalothin
ii. Cephaloridine
iii. Cefazolin
• Oral:
i. Cephalexin
ii. Cephradine
iii. Cefadroxil
Second generation: Greater stability to -lactamase.
• Parenteral:-
i. Cefuroxime
ii. Cefoxitin
• Oral:
i. Cefaclor
ii. Cefuroxime axetil.
Third generation: Considerable -lactamase stability and occasionally active against Pseudomonas.
• Parenteral:-
i. Cefotaxime
ii. Ceftizoxime
iii. Ceftriaxone
iv. Ceftazidime
v. Cefoperazone
• Oral:
Cefixime
Fourth generation: Highly resistant to -lactamase.
• Parenteral:-
i. Cefepine
ii. Cefpirome
Fifth generation: Specifically, it's active against multidrug-resistant infections like MRSA (methicillin-
resistant S. aureus) and VRSA (vancomycin-resistant S. aureus). This drug is also injectable and
prescribed to fight community-acquired pneumonia and serious skin and soft tissue infections.
• Parenteral:-
i. Ceftaroline
ii. Cefto bipirole

Intramammary cephalosporins:
i. Cephapirin
ii. Cephalonium
iii. Cephoxazole
iv. Cephacectril

Mode of action of cephalosporins

All the cephalosporins are bactericidal and have the same mechanism of action as penicillin. i.e.
inhibition of bacterial cell wall synthesis.
OR
The cephalosporins resemble the penicillins in that they interfere with cell wall formation
particularly with transpeptidation. They are thus bactericidal and are active largely against growing
organism. They are broad spectrum, being effective against both gram-positive and gram-negative
organisms.
Side effects of cephalosporins: Minor gastrointestinal effects such as vomiting and diarrhea may occur
following oral admission of cephalosporins. Fever, skin rash, eosinophilia, hemolytic anemia and
anaphylaxis.
Adverse effects of cephalosporins: Pain after i/m injection, diarrhea, bleeding, hypersensitivity
reactions, nephrotoxicity, neutropenia and thrombocytopenia.
Toxicity of cephalosporins: Toxicities include neutropenia, thrombocytopenia, agranulocytosis,
glomerular and intestinal nephritis, tubular necrosis, hepatitis and neurotoxicity. All these effects are
associated with very high doses and prolonged use of cephalosporins. Nephrotoxicity and enter colitis
may occur.
Contraindications of cephalosporins: Allergy (hypersensitivity reactions) is the only contraindications,
although it is limited in animal practices. The use of cephalosporin in pregnancy should be reserved for
cases considered essential by the clinician because safety for use in pregnancy has not been established.
Appropriate treatment for systemic reactions (adrenaline, antihistamine and hydrocortisone
injections) should be kept ready in hand to meet the situation.
 First generation cephalosporins
These were developed in the 1960s, have high activity against gram positive but weaker against
gram negative bacteria.
Cephalothin
Cephalothin is highly resistant to Staphylococcal -lactamase treatment of Penicillinase producing
Staphylococcal infection is its main indication.
It is not absorbed orally; i/m injection is very painful, only i/v route is used.
Dose: 1-2 gm/6 hourly.
It is partly metabolized in the liver and rapidly excreted by glomerular filtration as well as tubular
secretion.
Cephazolin
It is more active against Klebsiella and Escherichia coli but quite susceptible to Staphylococcal -
lactamase. It can be given i/m or i/v. It is the preferred parenteral first generation ephalosporins, especially
for surgically prophylaxis.
Dose: 0.25gm 8 hourly in mild cases i/m or i/v.
1gm 6 hoursly in mild cases i/m or i/v.
Cephaloridine
It has high activity against gram positive but weaker against gram negative bacteria, but is the most
nephrotoxic cephalosporins less popular, even withdrawn in some countries.
Dose: 11gm/kg body weight twice daily.
Toxicity: Large dose may cause kidney damage
Cephalexin
It is an orally effective first generation cephalosporin. It has high activity against gram positive but weaker
against gram negative bacteria, but less active Penicillinase producing Staphylococci and against
Haemophilus influenza. It is little bound to plasma protein, attains high concentration in bile and is
excreted unchanged in urine.
Dose: Adult: 0.25-1gm/6- 8 hourly.
Children: 25-100mg/kg/day/6-8 hourly.
Cephradine
Another orally active drug, almost identical to cephalexin, but less active against some organisms. Oral
administration causes diarrhea as side effects. It is available for parenteral use also.
Dose: 0.25gm-1gm/ 6-8 hourly oral or i/m or i/v.
Cephadroxil
A close congener of cephalexin has good tissue penetration exerts more sustained action at the site of
infection.
Dose: 0.25gm-1gm twice in a day.
 Second generation cephalosporin’s
These were developed subsequently to the first generation compounds and are more active against gram
negative organisms, with some members active against anaerobes.
Cefoxitin
It is a cephamycin produced by Actinomycetes. The main value of cefoxitin is in the treatment of anaerobic
and mixed obstetric or surgical infection, lung abscess.
Dose: 1-2gm / every 6-8 hours i/m or i/v.
Cefuroxime
It is resistant to gram negative -lactamase has high activity against organisms producing these enzymes.
The most important use is meningitis caused Haemophilus influenza, meningococci, pneumococci and
for single dose i/m therapy of gonorrhea due to PPNG.
Dose: Adult: 0.75-1.5gm/8 hourly i/m or i/v
Children: 30-100mg/kg/day
Cefuroxime axetil
This ester of cefuroxime is effective orally, though absorption in incomplete. The activity depends on in
vivo hydrolysis and release of cefuroxime.
Dose: Adult: 250-500 mg twice in a day.
Children: half dose.
Cefaclor
It retains significant activity by the oral route and is more active than the first generation compounds
Haemophilus influenza, Escherichia coli.
Dose: 250 mg, 125 and 500 mg cap.

Third generation cephalosporins

These compounds introduced in the 1980s have highly augmented activity against gram negative
Enterobacteriaceae; some inhibit pseudomonas as well. All are highly resistant to -lactamase from gram
negative bacteria.
Cefotaxime
It is protype of the third generation cephalosporins; exert potent action on aerobic gram negative as well
as some gram positive bacteria, but is not so active on anaerobes.
Dose: Adult: 1-2gm/6-12 hourly i/m or i/v.
Children: 50-100mg/kg/day.
Ceftizoxime
It is similar in antibacterial activity and indications to potent action on aerobic gram negative as well as
some gram positive bacteria, but is not so active on anaerobes, but is not metabolized excreted by the
kidney at a slower rate.
Dose: Adult: 0.5-1gm/ 8-12 hourly i/m or i/v.
 Ceftriaxone
The distinguishing feature of these cephalosporins is its longer duration of action (t ½ 8 hours) permitting
once or at the most twice daily dosing. It has good CSF penetration and is eliminated equally in urine and
bile.
Dose: Adult: 4gm following by 2gm i/v.
Children: 75-100mg/kg body weight once daily for 7-10 days.
Ceftazidime
The most prominent feature of this third generation cephalosporins is its high activity against
pseudomonas. It has been specifically used in febrile neutropenic patients with hematological
malignancies, burn etc.
Dose: Adult: 0.5-2gm every 8 hours i/m or i/v.
Children: 30mg/kg/ day.
Cefoperazone
Like Ceftazidime it differs from other third generation compounds in having stronger activity on
pseudomonas and weaker activity on other organisms. It is good for S. typhi and B. fragilis also, but more
susceptible to -lactamase.
Dose: 1-2gm /12 hourly i/m or i/v.
Cefixime
It is an orally active third generation cephalosporins highly active against Enterobacteriaceae,
Haemophilus influenza, Streptococcus pneumonia and is resistant to many -lactamases.
Dose: 200-400 mg twice daily for respiratory, urinary and biliary infections.

Fourth generation cephalosporins

Cefepine
Developed in 1990s this 4th generation cephalosporin has antibacterial spectrum similar to third
generation compounds, but is highly resistant to -lactamase, hence active against many bacteria resistant
to the earlier drug.
Uses of cephalosporins
Cephalosporins are now extensively used antibiotics.
• As alternative to penicillins G in patients developing rashes or other allergic reactions with
penicillin G.
• Respiratory, urinary and soft tissue infections caused by gram negative organisms, especially
Klebsiella, Proteus, Enterobacter, Serratin etc.
• Penicillinase producing Staphylococcal infections; Cephalothin is the preferred drug.
• Septicemia caused by gram negative organisms.
• Meningitis caused by Haemophilus influenza specially used cefuroxime + gentamycin is most
effective drugs.
• Gonorrhea caused by Penicillinase producing organisms.
• Typhoid as alternative to Fluoroquinolones.
It is used in upper respiratory tract, urinary tract, skin and soft tissue infections by sensitive gram positive
and gram negative bacteria and life threatening infections before specific organism identified.

Trade name:

Name Dosage
Tab. Axet (125, 250 and 500 mg) 250 mg tab in adult 12 hoursly for 5-7 days
Inj. Axet (250, 500 mg) 250-750 i/v in adult 8 hoursly for 5-7 days
Inj. Rencef (1 gm, 2gm) IM 1gm/100 kg b wt i/m in large animals for 5-7 days if
needed i/v it should be diluted with dist. water.
Inj. Ceftron (1 and 2) 1gm/100 kg b wt i/m in large animals for 5-7 days if
needed i/v it should be diluted with dist. water.

MD. SODOR UDDIN

DVM 24TH BATCH, SAU
 Sulphonamides and other antibacterial
Definition of Sulphonamides: Sulphonamides are a group of complex synthetic organic chemical
compounds with chemotherapeutic activity. They have a common chemical nucleus which is essential for
antibacterial activity. The chemical structure and bond is same between PABA (Para amino benzoic acid)
and sulphonamides. But one carbon is replaced by sulfur in case of sulphonamide. ‘Sulpha’ part of the
name such as sulphanilamide and sulphadiazine. Hydrogen atom of the –So2.NH2 group of the basic
compound, sulphanilamide. Sulphonamide was first synthesized in 1908 by Gelmo.
Classification of sulphonamide
The sulphonamides can be divided into two main sections according to the site of therapeutic action or
on the basis of their absorption pattern:-
1. The systemic sulphonamides: These are absorbed well from the intestines. The most important
of these are:-
i. Sulphanilamide
ii. Sulphacetamide
iii. Sulphapyridine
iv. Sulphadimidine
v. Sulphathiazole
vi. Sulphafurazole
vii. Sulphamerazine
viii. Sulphadiazine
ix. Sulphamethazine
x. Sulphaquinoxaline (used only in case of poultry).
2. The gut active Sulphonamides: These are absorbed poorly from the intestines and exert their
effect only on the intestinal flora and possibly microorganisms situated in the superficial cells of
the mucosa. The most important of these are:-
i. Sulphaguanidine
ii. Succinylsulphathiazole
iii. Phthalylsulphathiazole
iv. Phthalylsulphacetamide.
3. Topical sulphonamide- Sulphacetamide sodium (used as a topical treatment for ophthalmic
infection).

Mode of action of sulphonamides

The sulphonamides in very concentrations stimulate cell growth, but in low therapeutic
concentrations they are bacteriostatic and in high therapeutic concentrations may be bactericidal. They
are normally used as bacteriostats.
The sulphonamides act against bacteria by substituting and replacing essential vitamins upon
which the susceptible bacteria are actually dependent. Sulphonamides interfere with the synthesis of folic
acid of bacteria from Para amino benzoic acid, because the structures of PABA and the nucleus of
sulphonamides are similar. Bacteria take the sulphonamide instead of PABA. Within the bacteria
sulphonamides inhibit the conversion of PABA to dihydrofolic acid and heterocyclic pyridine and thiazole
derivatives disrupt nicotinamide metabolism and the working of coenzymes I and II, synthesis of various
amino acids (methionine, a precursor of choline) may also be interrupted. As a result, bacteria cannot
synthesize nucleic acid and ultimately death occurs.
Antibacterial spectrum: The sulphonamides are as a group active mainly against Gram positive
organisms but there is also some activity against Gram negative organisms, a few rickettsiae and some
protozoa.
1. Sulphanilamide, sulphaguanidine and sulphacetamide are active against Streptococci and
Escherichia coli. Sulphacetamides are slightly more active than the other two.
2. Sulphapyridine and sulphadimidine are active in higher degree against Streptococci and
Escherichia coli but less active against Staphylococci, Salmonella and Pasteurella.
Sulphadimidine is also active against some Rickettsiae and protozoa.
3. Sulphamerazine and sulphafurazole are more active against Escherichia coli, Pasteurella and
Staphylococci.
4. Sulphadiazine and sulphathiazole are active against Streptococci, Staphylococci, Escherichia coli
and Pasteurella.
Therapeutic principles in using sulphonamides
The following therapeutic principles are followed in using sulphonamides:-
1. The effect of a sulphonamide decreases with the increasing number of organisms. Therefore, the
indicated sulphonamide should be given as early as possible in the course of the disease. For the
same reason, the more severe the infection, the larger should be the dose.
2. Maximum blood levels are achieved in one or two hours with the most soluble Sulphonamides.
So, in the critical cases treatment should be indicated by parenteral injection of a monosodium or
disodium salt.
3. Because of the low solubility and relatively slow absorption rate, the initial dose should be larger
which will be maintained by regularly repeated smaller doses.
4. Sulphonamides are not easily soluble in acid urine and crystallization may occur. So, during
sulphonamide therapy available water should be supplied and urinary alkalizer should be given to
the animal.
5. To avoid systemic toxicity dose sizes should be cut by a half after the initial period.
6. Though Sulphonamides are bacteriostatic in action dosing should be continued for about 48 hours
after the disappearance of clinical symptoms otherwise reinfection may occur.
Dosage of sulphonamides:
1. Systemic sulphonamides
Sulphonamides Initial dose (g/kg Maintenance dose
body weight)
Sulphadiazine 0.2 Half of the initial dose twice daily.
Sulphamerazine 0.2 Half of the initial dose once daily.
Sulphadimidine 0.2 Half of the initial dose once daily except dog (one third
initial dose twice daily).
Sulphapyridine 0.15 Half of the initial dose twice daily.
Sulphathiazole 0.2 Half of the initial dose every 6 hours.
Sulphafurazole 0.2 Half of the initial dose every 12 hours.
Sulphanilamide 0.2 (small spp. One third initial dose 3 times daily or half of the initial
0.15) dose twice daily.
Sulphacetamide 0.15-0.2 Initial dose repeated daily.
Sulphaquinoxaline 0.05% and 0.04% 0.05% in feed and 0.04% in drinking water.
 2. Gut active sulphonamides
Sulphonamides Initial dose (g/kg Maintenance dose
body weight)
Sulphaguanidine 0.10-0.30 Half of the initial dose twice daily.
Phthalylsulphathiazole and 0.10-0.15 In two doses per day.
Succinylsulphathiazole
Phthalylsulphacetamide 0.35-0.57 In two doses per day.

Routes of administration of sulphonamides

1. Orally- Continue oral use in cattle causes enteritis with scouring.
2. Topically
3. Monosodium salts- intravenously
4. Disodium salts- i/v, s/c, i/m.
5. Solutions of sodium salts- i/p
6. Pessaries as intrauterine.
Excretion of sulphonamides
Sulphonamides are excreted mainly via the urine. Fecal excretion is relatively high, as much as
10% of a single dose of sulphonamides, more of other sulphonamides remains unabsorbed in the
intestines.
Clinical application of sulphonamides
1. Colibacillosis (Escherichia coli)
2. Respiratory infection (Pasteurella spp.)
3. Foot rot disease (Fusobacterium necrophorus)
4. Coccidiosis in poultry and large animals
5. Pasteurellosis (H.S)
6. Actinobacillosis (Wooden tongue).
Doses: 50-300 mg/kg body weight orally, i/m, s/c, i/v.
Toxicity and side effects of sulphonamides
Toxicity may arise in two forms- acute and chronic.
1. Acute toxicity: - mostly occurs in man and the symptoms include nausea, temporary blindness,
giddiness etc. Skin rashes, hematuria, hemoglobinuria, photosensitization, hemolytic anemia and
agranulocytosis have also been reported following previous course of treatment with
sulphonamides. In dog, if large dosage given there will be salivation, vomition, diarrhoea,
hyperpnoea, excitement, muscular weakness and ataxia.
2. Chronic toxicity: - is more important and is use of two types. One associated with depression of
intestinal flora and interference with vitamin B complex metabolism or synthesis. Continual use
of sulphonamide in ruminant cause diarrhoea, dehydration, loss of appetite and decreased milk
yield. In other species sulphonamide cause depression, loss of appetite, nausea and vomiting.
Crystaluria more frequently in man than animals which causes reduced urine production with pain
and casts of albumin being seen in urine. In poultry, it causes decreased egg production and
thinning of egg shell.
 PHT-302

Anthelmintics
Definition of anthelmintics: Anthelmintics are drugs or agents that eliminate worms from
gastrointestinal tract. Drugs which are classified as anthelmintics are intended to act against parasites
which inhabit the alimentary tract, its associated organs as the liver, lungs and blood circulatory
system.
Most parasites of the intestinal tract and associated structures such as bile ducts are classified as
trematodes (flukes), nematodes (round worms) and cestodes (tape worms).

Vermicides: When the anthelmintics kill the worms they are called vermicides.

Vermifuges: When the anthelmintics remove the worms from gastrointestinal tract by temporary
paralyzing them they are called vermifuges. In this case, purgation is essential for eliminating the
worms.

Effects of parasites on their host

Parasites can cause damage in various ways:

1. They can absorb the host’s food. e.g. tape worms.

2. They can continually suck blood. e.g. hook worms.
3. They can feed on the host’s tissue. e.g. red worm in horses.
4. They can cause mechanical obstructions of-
a. the gut – ascarids
b. blood vessels – filaroids
c. the heart – heart worm
d. the liver – liver fluke.
5. They can cause tissue damage which can lead to infection. e.g. Black disease caused by
Clostridium oedimatins in liver fluke infection.
6. They can lead to tissue reactions. e.g. the nodules produced by lung worms.

Characteristics or properties of an ideal anthelmintic

Ideal anthelmintics would have the following properties:-

1. The widest possible therapeutic index. A therapeutic index is narrower than 1:4 is not
considered safe. TI = Median lethal dose/ Median effective dose or LD50/ED50.

2. A wide spectrum of activity.

3. Effective against both mature and immature stages of the worm.

4. Ease of administration – It should be easily administered. Most of the anthelmintics are

administered orally in empty stomach. e.g. Albendazole, levamisole etc. However, some of
the anthelmintics are administered parenterally. e.g. Ivermectin. It would be acceptable to the
animal so that administration causes no trouble and would be simple to administer.

1
 PHT-302

5. An ideal anthelmintic would not cause any interruption in the normal life of the animal or
cause any check in its development.

6. It would be economically cheap.

7. Residue – It should be eliminated from the body without any residual problems. The
anthelmintics possessing a long withdrawal time will create human health hazards after
consumption of milk, meat and other animals produce. The anthelmintics having a short
withdrawal time are much safer.

8. Efficacy – The efficacy is said to be good if it removes 95% of a gastrointestinal nematodes

from ruminant species. If it is removes only 70% of the worm burden it is considered as a
poor anthelmintic. It should have effect on both adult and larval stages of worms. 100%
removal of the worm load also eliminates the source of antigenic stimulation and animal
looses the acquired resistance to parasites.

Anthelmintic need

It has been observed that parasitic infestation in animals makes them anemic and weak. They can
interfere with the growth of young ones. Parasitic infestation in lactating animals generally
decreases milk yield. As a whole, the parasitic load in animals make them debilitated and bad
looking. If an animal with worm load is seen, its skin and hair texture is not charming.

Classification of anthelmintics

A. According to chemical structure anthelmintics are classified as follows :–

1. Benzimidazoles- Thiabendazole, albendazole, fenbendazole, mebendazole, cambendazole,

triclabendazole, oxfendazole, oxibendazole, parbendazole and thiophanate etc.
2. Imidazothiazoles- Levamisole, tetramisole etc.
3. Tetrahydropyrimidines- Morantel, pyrantel etc.
4. Organophosphorus compounds- Coumaphos, dichlorphos, trichlorphos and haloxon etc.
5. Piperazine- Piperazine citrate, piperazine adepate etc.
6. Avermectins (Semi synthetic analogue is ivermectin).
7. Unrelated individual entities- Dichlorphen, niclosamide, oxyclozanide, praziquantel,
rafoxanide, nitroxynil, phenothiazine, hexachloroethane, diethylcarbamazine, carbon
tetrachloride, bunamidine and bephenium etc.

B. According to the types of worms on which anthelmintics act:-

1. Antinematodal drugs- Which acts against nematodes. e.g. Thiabendazole, mebendazole,

piperazine and thiophenate etc.

2
 PHT-302

2. Antitrematodal drugs- Which acts against trematodes. e.g. Nitroxynil, praziquantel,

triclabendazole, dichlorphen, hexachlorophene, rafoxanide, closantel and oxyclosanide
etc.
3. Anticestodal drugs- Which acts against cestodes. e.g. Oxfendazole and niclosamide etc.

General mode of action of anthelmintics

1. Neuromuscular blockers- Some of the anthelmintics have action on the neuromuscular

system. e.g. Piperazine causes paralysis of the worms especially Ascariasis. The
paralysis of the worms is due to hyper polarization of the muscle membranes.

2. Cholinomimetics- e.g. Levamisole, morantel, pyrantel etc. The above cited drugs affect
neuromuscular system of the worms acting like cholinomimetics. These agents possess
functional groups similar to acetylcholine and bind to receptors from which the
acetylcholine binds. It causes a continuous stimulatory effect. However, these are not
inactivated by acetylcholine esterase.

3. Inhibitors of glucose transport- Some anthelmintic agents like dithiazanine which is

given for canine whip worm, inhibits glucose uptake. Thus, by reducing glucose content
causes death of the worms.

4. Disruptors of glycogen metabolism- Schistosomicidal drug (niridazole) reduces

phosphorylase phosphatase activity and increases the breakdown of glycogen reserve in
worms. The death of the worms is due to starvation.

5. Inhibitors of glycolysis- Arsenicals (thiacetarsamide), antimonials (potassium antimony

tartarate), stibophen etc. are organic trivalent heavy metals and bind with sulfhydryl (-
SH) group. By binding with –SH they change the tertiary structure of proteins and the
active site of enzymes.

6. Inhibitors of mitochondrial reactions- Benzimidazoles and thiophanate work in this

way. For muscle contraction in works, high energy (ATP) is required which is provided
after reduction of fumerate to succinate in mitochondria. The above drugs exert their
action by inhibiting fumerate reductase which is required for convertion of fumerate to
succinate.

7. Uncouplers electron transport- Niclosamide, oxyclozanide, rafoxanide, dinitrophenol,

hexachlorophene, niclofolam, nitroxynil etc. are uncouplers of electron transport. These
drugs interfere with electron transport associated with phosphorylation process which is
an important biochemical process for generation of ATP. As ATP is an important
source of chemical energy to parasites, the worms lack this energy and die.

3
 PHT-302

Benzimidazole

The Benzimidazoles have been used since 1960 to till date. Due to their poor solubility
benzimidazoles generally dosed orally as suspensions or paste or boluses or as powder; granules and
pellets in order to mix with the diet.

All the benzimidazoles have good activity against nematodes, their larvae and eggs. The more recent
analogues have some tape worm activity such as mebendazole is highly effective against larval tape
worm and albendazole is also effective against adult liver flukes. The triclabendazole is the most
recent derivatives and is highly effective against all stages of liver fluke but not effective against
round worm.

Thiabendazole

Thiabendazole is a stable white crystalline compound with no appreciable taste. It is practically

insoluble in water, with low solubility in alcohol, chloroform and ether.

Mode of action of benzimidazole and thiabendazole

The benzimidazole and thiabendazole act on nematodes by inhibiting the fumerate reductase system
in the mitochondria, ultimately inhibiting the uptake of glucose and uncoupling of oxidative
phosphorylation. The lack of absorbed glucose causes a depletion of the worm glycogen reserve and
leaves it unable to produce the ATP necessary for survival. Ultimately death of the parasites occurs.

Anthelmintic spectrum: It is highly effective against Haemonchus, Trichostrongylus, Bunostomum,

Oesophagostomum and Chabertia. Although less effective against Ostertagia, Cooperia and
Nematodirus, however, an increased dose will give satisfactory results.

Dosage: Thiabendazole is given orally and the recommended doses are as follows-
Cattle, horses, sheep and goats: - 50-100 mg/kg body weight.
Pigs: - 50 mg/kg body weight.

Safety and toxicity: It has 20 times safety margin and safety margin without producing side effects.
Under experimental condition the toxic effect appears to be associated with anorexia and nausea.
When given at the dose of 100 mg/kg in piglets, it can reduce glycogen level, RNA, ascorbic acid and
increase succinate dehydrogenase activity.

Albendazole

Available in Bangladesh including in human practices

Action and use: Albendazole is active against all important nematodes and their larvae, including
hypo biotic or inhibited forms. It is also effective against tape worms and adult flukes.

Dosage:
Cattle: - 7.5 mg/kg (10 mg/kg for flukes) orally.

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 PHT-302

Horse and sheep: - 5 mg/kg (7.5 mg/kg for flukes) orally.

Safety and toxicity: The safety index has been reported to be 7.5-20 times the recommended dose.
High dose may be embryo toxic (Teratogenicity). Albendazole are the cause of some toxic effect to
the embryo of pregnant mother. Their use in early stages of pregnancy causes developmental
anomalies.

Contraindications: The drug should not be used in pregnancy.

Trade name: Tab. Helmex, Endokill, Ralnex.

Cambendazole

Action and use: Cambendazole is effective against round worms and some of the tape worms.

Dosage:
Cattle, sheep, horse and pigs: - 20 mg/kg body weight orally.

Safety and toxicity: Cambendazole is a fairly toxic benzimidazole. It may be lethal to cattle at 2-3
times the recommended dose, but sheep tolerate 10 times the dose. The drug may be embryo toxic if
dosed to pregnant animals. Cambendazole are the cause of some toxic effect to the embryo of
pregnant mother. Their use in early stages of pregnancy causes developmental anomalies.

Contraindications: The drug should not be used in pregnancy.

Fenbendazole

Available in Bangladesh

Action and use: Fenbendazole is effective against all important nematodes including hypo biotic or
inhibited forms. It has got some activity against tape worms.

Dosage:
Cattle: - 7.5 mg/kg body weight orally
Horse, sheep and pigs: - 5 mg/kg body weight orally.

Safety and toxicity: Fenbendazole is extremely safe with a safety factor in excess of 100 times the
recommended dose. Cattle with heavy lung worm infections may suffer an allergic response to
treatment as a result of killing worms in situ. It is not embryo toxic. Fenbendazole is widely used
with medicated urea-molasses-block (MUMB 5%).

Trade name: Peraclear (Techno) (1 bolus/50 kg body weight; 5 mg/kg body weight orally.
Pancur bolus.

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 PHT-302

Mebendazole

Available in Bangladesh.

Mode of action: It inhibits irreversibly the uptake of glucose and worms die due to starvation.

Action and use: It is effective against round worms and tape worms.

Anthelmintic spectrum: It possesses broad spectrum activity and mainly used in equine against
Ascariasis, Strongyloids, Trichonema, Oesophagostomum and Oxyuris species. In poultry it is used
against Syngamus trachea.

Dosage:
Horse, Dogs and Cats: - 10 mg/kg body weight orally.

Safety and toxicity: Mebendazole is well tolerated with a safety index in excess of 20 times the
recommended dose. The drug is not embryo toxic in target species.

Contraindications: The drugs should not be used in pregnancy.

Oxfendazole

Action and use: Effective against round worms and tape worms.

Dosage:
Horses: - 10 mg/kg body weight orally
Cattle, sheep and pig: - 5 mg/kg body weight orally.

Safety and toxicity: The safety index is greater than 10 times the recommended dose but high dose
levels may be embryo toxic to pregnant ewes. Oxfendazole are the cause of some toxic effect to the
embryo of pregnant mother. Their use in early stages of pregnancy causes developmental anomalies.

Contraindications: The drugs should not be used in pregnancy.

Triclabendazole

Action and use: Triclabendazole is very potent against liver fluke (Fasciola gigantica) from one day
old to adult. It is poorly effective against Dicrocoelium and has no antinematode activity.

Dosage:
Cattle: - 12 mg/kg body weight orally
Sheep and goats: - 10 mg/kg body weight orally.

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 PHT-302

Thiophanate

Available in Bangladesh.

Action and use: Thiophanate is effective against most nematodes of farm animals.

Dosage: 50 mg/kg body weight orally.

Safety and toxicity: Thiophanate is very safe compound. 1 gm/kg is being non toxic to ruminants.

Imidathiazoles

The major drug used in this group is levamisole, which was developed following the introduction of
tetramisole in 1966. Their withdrawal period is short 3 days. They are not teratogenic.

Levamisole

It is a potent water soluble round worm remedy which may be administered orally or parenterally.

Mode of action: Levamisole is a cholinergic (ganglion stimulant) agent which causes muscular
paralysis of the worms. It also interferes with carbohydrate metabolism specially inhibit the enzyme
fumerate reductase and succinate dehydrogenase.

Action and use: Levamisole is a broad spectrum anthelmintic and is effective against adult and larval
stages of Haemonchus, Ostertagia, Trichostrongylus, Cooperia, Nematodirus, Bunostomum,
Oesophagostomum, Metastrongylus, Ascaris, Hyostrongylus, Trichuris and against the lung worm
Dictyocaulus, both orally and parenterally. It has got a very rapid action on parasites; most nematodes
are expelled within 24 hours.

Dosage:
Cattle, sheep, pig: - 7.5 mg/kg body weight orally
Poultry: - 18-36 mg/kg body weight orally.
The dose for s/c injection is 2 ml/50 kg body weight of 18.2% solution.

Safety and toxicity: The chemotherapeutic index of levamisole is 5-6 times the recommended dose.
It is neither embryo toxic nor teratogenic.

Trade name: Levavet bolus: - 7.5 mg/kg body weight orally

Ralnex: - 7.5 mg/kg body weight orally.

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 PHT-302

Tetramisole

It is a potent water soluble round worm remedy which may be administered orally or parenterally.

Mode of action: Tetramisole is a cholinergic (ganglion stimulant) agent which causes muscular
paralysis of the worms. It also interferes with carbohydrate metabolism specially inhibit the enzyme
fumerate reductase and succinate dehydrogenase.

Action and use: Tetramisole is a broad spectrum anthelmintic and is effective against adult and
larval stages of Haemonchus, Ostertagia, Trichostrongylus, Cooperia, Nematodirus, Bunostomum,
Oesophagostomum, Metastrongylus, Ascaris, Hyostrongylus, Trichuris and against the lung worm
Dictyocaulus, both orally and parenterally. It has got a very rapid action on parasites; most nematodes
are expelled within 24 hours.

Dosage:
Cattle, sheep, pig: - 7.5 mg/kg body weight orally
Poultry: - 18-36 mg/kg body weight orally.
The dose for s/c injection is 2 ml/50 kg body weight of 18.2% solution.

Safety and toxicity: The chemotherapeutic index of tetramisole is 5-6 times the recommended dose.
It is neither embryo toxic nor teratogenic.

Tetrahydropyrimidines

There are three tetrahydropyrimidines currently used for the treatment of nematodes in animals.
Morantel, pyrantel and oxantel.

Mode of action: The primary mode of action of tetrahydropyrimidines is to affect the worms
neuromuscular system leading to paralysis and death. In vitro, they also show inhibition of the
enzyme fumerate reductase.

Morantel tartrate, citrate

Available in our country. Morantel is a pale yellow crystalline solid of uniform appearance. It is
soluble in water and insoluble in ethyl acetate or benzene.

Mode of action: Morantel acts by depolarization of the myoneural junction, leading to inhibition of
cholinesterase and spastic paralysis of the worm occur.

Action and use: Morantel is a broad spectrum anthelmintics with activity against many adult and
immature gastrointestinal worms in sheep and cattle including Haemonchus, Ostertagia,
Trichostrongylus, Cooperia, Nematodirus, Chabertia and Oesophagostomum.

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 PHT-302

Dosage: Cattle, sheep: - 10 mg/kg body weight orally.

Safety and toxicity: Morantel is a safe drug and up to 7 times safety margin. The withdrawal period
is 14 days.

Pyrantel embonate

It is a pale yellow, odorless, non-staining, amorphous powder.

Mode of action: The pharmacological action of pyrantel is similar to that of levamisole. They act by
mimicking the effect of excessive amount of acetylcholine and finally by paralyzing the
neuromuscular sites.

Action and use: It is a broad spectrum anthelmintic and is used in the horse for the control and
treatment of Strongylus vulgaris, small strongylus, Oxyuris equi and Parascaris equorum.

Dosage: Horse: - 19 mg/kg body weight orally.

Safety and toxicity: Pyrantel embonate is a very safe anthelmintic and it has got 20 times safety
margin.

Oxantel

Available in market. Oxantel is a whip worm remedy.

Activity: Oxantel is only effective against whip worms (Trichuris spp) and is usually used as the
pamoate salt in combination with pyrantel.

Dosage: Horse: - 55 mg/kg body weight orally.

Toxicity: Being poorly absorbed oxantel shows little toxicity.

Organophosphate

Mode of action: They inhibit the enzyme acetyl cholinesterase of worms leading to paralysis and
death.

Action and use: A number of organophosphorus compounds such as coumaphos, dichlorphos,

trichlorphos and haloxon are effective against both insects and nematodes.

Dosage:
Coumaphos
Cattle: - 15 mg/kg body weight orally
Sheep: - 8 mg/kg body weight orally
Dichlorphos
Cattle, horse: - 31-41 mg/kg body weight orally

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 PHT-302

Sheep: - 11-22 mg/kg body weight orally

Dog, cat: - 27-34 mg/kg body weight orally
Trichlorphos
Cattle: - 60 mg/kg body weight orally
Sheep: - 55 mg/kg body weight orally
Haloxon
Cattle: - 44 mg/kg body weight orally
Sheep: - 35-40 mg/kg body weight orally.

Safety and toxicity: There may be poisoning in animals in higher doses.

Piperazine

Salts of piperazine:
i) Piperazine adepate
ii) Piperazine citrate
iii) Piperazine phosphate
iv) Piperazine sulfate
v) Piperazine tartarate
vi) Piperazine hydrochloride etc.

Mode of action: It produces neuromuscular block in susceptible worms. In addition to the above
action, it inhibits succinic acid production in worms. Due to narcotic and paralytic effects produced
by piperazine, worms loose their ability to maintain their position in gastrointestinal tract and are
eliminated due to peristaltic movement and possibly augmented by a laxative or purgative Or
Piperazine compounds block the response to acetylcholine and cause reversible paralysis of the
worm which can then be removed from the intestinal normal peristalsis, possibly augmented by a
laxative or purgative.

Action and use: Piperazine used mainly against ascarid and oxyurid infections of calves, pigs,
horses, pets and man. Piperazine is effective against the ascarid and nodular worms of all species of
domestic animals and poultry birds orally or with feed or in drinking water.

Dosage and administration:

Horse: - 110-250 mg/kg body weight
Dog and cat: - 45-65 mg/kg body weight
Poultry: - 32 mg/kg body weight.

It is convenient to give tablets of piperazine in dogs and cats. In poultry, the powder or suspension is
given with feed or drinking water orally. In other animals, it is given in bran mashes.

Safety and toxicity: Piperazine is very safe to use, the only occasional side effects are emesis and
softening of the faeces. It may be administered to pregnant animals and also to animals suffering
from gastrointestinal disorders. Young animals can also be treated. Large dose may produce
vomiting, diarrhea, in coordination and head pressing in dogs and cats. Doses four times more than
therapeutic dose can produce transitory diarrhea, tympany and anorexia in calves.

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 PHT-302

Contraindications: Animals suffering from hepatic and renal disorders should not be treated.

Ivermectin

Ivermectin is the latest anthelmintic. It is highly effective at very low concentration against a range of
both internal and external parasites when given either orally or parenterally. The drug is now
available commercially and technical reports indicate highly effective against cattle, sheep and dogs.
Avermectins are produced by fermentation of an actinomycete known as Streptomyces avermitilis.
Avermectins are complex of eight components that are a group of macro cyclic lactones derivatives.
These complexes are A1a, A2a, B1a and B2a, A1b, A2b, B1b and B2b. Each of the components has
anthelmintic activity. These are not antibacterial or fungicidal as the macrolide or polyene
derivatives. Ivermectin is the combination of B1a and B1b in ratio of 80% and 20% respectively.

Mode of action: Avermectins inhibit the motility and thereby causes paralysis of worms - amino
butyric acid (GABA) release is increased due to B1a from synaptosomes of the nervous system.
Increased release of GABA causes hyperpolarization of post synaptic cells and inhibits contraction of
muscle. Thus, worms are expelled due to peristaltic movement and possibly augmented by a laxative
or purgative or
It increases the permeability of parasite membranes to chloride ions (Cl-) by inhibiting neuromuscular
transmission of parasite by stimulating release of neurotransmitter - amino butyric acid. {The
ivermectin resistant strains of Haemonchus contortus, exit in South Africa so far}.

Actions and use: For the treatment of gastrointestinal nematodes, lung worms, warbles, mange and
sucking lice in beef and non lactating dairy cattle the dosage used is 200 µg/kg body weight.
Ivermectin is effective against the following parasites:-
1. Nematodirus- Gastrointestinal worms (adults and fourth stage larvae), Ostertagia ostertagi,
Haemonchus placei, Trichostrongylus axei, Trichostrongylus colubriformis, Cooperia spp.,
Oesophagostomum radiatum and lung worms.
2. External parasites- Warbles (Parasite stages), Hypoderma bovis, Hypoderma lineatum, Lice-
Linognathus vituli and Haematopinus eurysternus, Mites- Psoroptes bovis, Sarcoptes scabei
var bovis.

Dosage:
Cattle: - 0.2 mg/kg body weight s/c.
Horse: - 0.2 mg/kg body weight orally or i/m.
Sheep: - 0.2 mg/kg body weight orally
Swine: - 0.3 mg/kg body weight s/c or
100-200 µg/kg body weight orally, 25-100 µg/kg body weight parenterally.

Safety and toxicity: It produces mydriasis after a 10 fold oral dose in dogs. Horses show an
impaired vision after two consecutive oral dosing. The acute toxicity symptoms include CNS
depression, listness, ataxia, recumbency. Death in horses has been reported after i/m administration of
60 times of therapeutic dose. It is safer to pregnant animals.

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 PHT-302

Precautions:
1. Cattle must not be treated within 21 days of slaughter.
2. Ivermectin must not be used in milk producing animals or in dairy cows for 28 days prior to
calving.

Diethylcarbamazine

Activity: Diethylcarbamazine citrate is effective against various round worms and ruminant lung
worm but its principal value or use in the control of canine heart worm disease caused by (Dirofilaria
immitis).

Mode of action: The mode of action of diethylcarbamazine against heart worm larvae is unknown,
although it has been suggested that it opsonizes microfilaria for destruction by the hosts immune
system. Recent studies have shown that it disrupts microtubules and inhibits microtubule
polymerization.

Dosage: Dog: - 5.5 mg/kg body weight/day.

Safety and toxicity: Diethylcarbamazine is safe to use in pregnant and young animals but may cause
vomiting in fasting days.
Dichlorophen

Dichlorophen is a safe, narrow spectrum tape worm remedy.

Action and use: Dichlorophen has moderate and somewhat erratic activity against Taenia and
Dipylidium in dog. It is ineffective against Echinococcus.

Dosage:
Dogs and cats: - 200 mg/kg body weight orally.

Toxicity: Apart from occasionally causing vomiting and diarrhea, dichlorophen is extremely well
tolerated.
Closantel

Closantel is an oral and injectable fasciolicide. It is the most recent analogue of the group (modern
drug).

Actions and use: Closantel is effective against adult and juvenile (6-10 weeks old) flukes, blood
sucking nematodes. Parasitic larvae of flies and has some effect against the tape worms, mites and
ticks.

Mode of action: Closantel affect the phosphorylase link in energy metabolism and may also inhibit
fumerate reductase. These drug are not water soluble, nevertheless, solutions have been formulated
that enable rafoxanide and closantel administered parenterally.

Dosage:

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 PHT-302

Cattle and sheep: - 5 mg/kg body weight s/c

Goats: - 10 mg/kg body weight orally.

Toxicity: Closantel has a six fold safely margin is not carcinogenic, teratogenic or embryogenic.

Niclosamide or Mansonil

Niclosamide is an oral tape worm remedy.

Mode of action: Niclosamide affect the phosphorylase link in energy metabolism and may also
inhibit fumerate reductase. The drug appears to act by inhibiting oxidative phosphorylation in
mitochondria and interfering with anaerobic generation of ATP by the tape worm. Injured by
niclosamide, the tape worms are partly digested in the intestine. It blocks the Krebs cycle which
causes accumulation of lactic acid and thus results in death of tape worm.

Action and use: Niclosamide is effective against the tape worms Echinococcus, Taenia and
Dipylidium in dogs and cats. It is less effective against Dipylidium. It is also effective against rumen
fluke- Paramphistomum in ruminants.

Dosage:
Dogs and cats: - 150 mg/kg body weight orally.

Safety and toxicity: Niclosamide has a 5-7 fold safety margin despite the high dose. The doses
higher than the recommended one causes damage to liver and kidney.

Oxyclosanide

Oxyclosanide is an oral fasciolicide.

Actions and use: Oxyclosanide is effective against adult liver fluke only.

Mode of action: Oxyclosanide affect the phosphorylase link in energy metabolism and may also
inhibit fumerate reductase. These drug are not water soluble, nevertheless, solutions have been
formulated that enable rafoxanide and closantel administered parenterally.

Dosage:
Cattle and sheep: 10-15 mg/kg body weight orally.

Toxicity: Toxic symptoms may appear at four times the recommended dose.

Rafoxanide

Rafoxanide is a fasciolicide that may be given orally or parenterally.

Actions and use: Rafoxanide is effective against adult and young (6-10 weeks old) fluke. It is also
effective against blood sucking nematodes and tissue invading fly maggots.

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 PHT-302

Dosage:
Cattle and sheep: 7.5 mg/kg body weight orally, 3 mg/kg body weight s/c.

Safety and toxicity: Rafoxanide has a safety index of 6 times the recommended dose. However, in
appetence and diarrhea may occur in cattle after a high dose of rafoxanide. It may produce blindness
and optic nerve degeneration in some animals.

Contraindications: Lactating animals should not be treated with rafoxanide whose milk and milk
products are consumed by human within 28 days.

Nitroxynil

Nitroxynil is a fasciolicide which is only effective by injection.

Actions and use: Nitroxynil is effective against adult flukes and also effective against fly larvae
(Oestrus ovis) and blood sucking nematodes.

Mode of action: It inhibits the oxidase phosphorylation in the cell mitochondria of fluke and
consequently blocks the energy producing system.

Dosage:
Cattle and sheep: - 10 mg/kg body weight s/c, double dose for immature flukes.

Toxicity: The maximum tolerated dose of nitroxynil is only four times the therapeutic dose.

Praziquantel

Actions and use: Praziquantel is effective against all adult tape worms, many of the larval forms (but
not hydatid cysts) and against lung worms, gastrointestinal worms, blood sucking parasites and liver
flukes. The drug may be administered orally or parenterally.

Mode of action: It is rapidly taken up by the susceptible worms and appears to act by causing
leakage of intracellular calcium from the membranes contracture and paralysis. The tape worms lose
gip of the intestinal mucosa and are expelled. Flukes are also dislodged. Praziquantel is active against
adult as well as juvenile and larval stages of tape worms. At relatively higher concentrations, it
causes vacuolization of the tegument and release of the contents of the worms and flukes followed by
their destruction by the host. This action appears to be more important in the cases of Schistosomes
and flukes.

Dosage:
Dogs and cats: - 5 mg/kg body weight orally or 5.5 µg/kg body weight s/c or i/v.

Toxicity: At 40 times the therapeutic dose, the only toxic symptoms develop in dogs is occasional
vomiting. The injectable formulation may cause transient pain and irritation.

14
 Endocrine pharmacology

Hormones: Hormones are commonly defined as chemical messengers for controlling and
coordinating the functions of those organs and tissues of the body which are equipped to
interact with them.

Hormone as a chemical substance produced by living cells in an endocrine

gland and carried by the circulatory system to another part of the body where it produces
a specific effect.

Hormones are chemicals that

1). are secreted in minute amounts directly into the blood stream classically from
“ductless” glands
2). are transported by the vascular system, some of them tightly bound to specific plasma
proteins.
3). act at remote loci on specific target cells producing a specific effect.
4).act together with the neural system, as physiologic regulators of the metabolism of the
whole body and either in a positive or negative sense, physiologic integrators of
metabolism, usually in concert with one or more other hormones.

Hormone is a substance produced by a gland that acts on a remote tissue

(target tissue) to bring about a change in the target tissue. These changes may involve
alterations in metabolism, synthetic activity and secretory activity. Extremely small
quantities of a hormone can cause dramatic physiologic responses. Hormone act at blood
levels ranging from nanograms (10-9) to picograms (10-12) per ml of blood.

Origin of hormones: - Hormones originate from endocrine glands or nerves. They enter
the blood and cause cells in target tissues containing specific receptors to produce new
products or new hormones. The original hormones and the products of their action are
necessary for successful reproduction.

Classification of hormones:-

A). Protein or peptide hormones are produced by the following organs:-

1. Hypothalamus.
2. Anterior pituitary (Adenohypophysis).
3. Posterior pituitary (Neurohypophysis).
4. Thyroid.
5. Parathyroid.
6. Pancreas (Islets of Langher Hans) and
7. The hormone produced by GIT (Stomach and intestine).

B). Steroid hormones produced by following organs:-

1. Adrenal gland.
2. Gonads (Testes and ovary).

1
 C). Fatty acids having compounds:-
1. Prostaglandin hormones.

Classification of hormones on the basis of secretion:-

A). Pure endocrine gland:-

1. Pituitary gland.
2. Thyroid gland.
3. Parathyroid gland.
4. Adrenal gland.
5. Uterus.

B). Mixed gland:-

1. Pancreas (Islets of Langer Hans).
2. Testes.
3. Ovary.
4. Placenta.

Classification of reproductive hormones:-

Reproductive hormones can be classified according to

A. Their source of origin.
B. Their primary mode of action.
C. Their biochemical properties.

A). Glandular origin constitutes one method of hormonal classification:-

1. Hypothalamic hormones
- Gonadotropin releasing hormone (GnRH).

2. Pituitary hormones
- Follicle stimulating hormone (FSH).
- Luteinizing hormone (LH).
- Prolactin
- Oxytocin.

3. Gonadal hormones:-
In female the ovary produces
- Estrogens
- Progestogens
- Inhibin
- Some testosterone
- Oxytocin and
- Relaxin.

2
 In male, the testes produce
- Testosterone and other androgens
- Inhibin and
- Some estrogens.

4. Uterine hormones:-
- Prostaglandin F2 (PG F2).

5. Placental hormones:-
- Progesterone
- Estrogen
- Equine chorionic gonadotropin (ECG).
- Human chorionic gonadotropin (HCG).

B).Classification of hormones according to their mode of action:-

1. Neurohormones: - Neurohormones are synthesized by neurons and are

released directly into the blood so that they can cause a response in target tissues
elsewhere in the body.eg. Oxytocin.

2. Releasing hormones: - Releasing hormones are synthesized by neurons in

the hypothalamus and cause release of other hormones from the anterior pituitary. e.g.
Gonadotropin releasing hormone (GnRH) which controls the release of FSH and LH
from the anterior pituitary.

3. Gonadotropins: - Gonadotropins are hormones released by the

gonadotroph cells of the anterior pituitary and they stimulate the gonads. e.g. FSH,
LH.etc.

4. Sexual promoters:-
- Estrogen
- Progesterone
- Testosterone.

5. Stimulation of the maternal ovary:-

- Human chorionic gonadotropin (HCG)
- Equine chorionic gonadotropin (ECG).

6. Pregnancy maintenance hormones:-

- Progesterone

7. General metabolic hormones:-

- Thyroxin
- Adrenal corticoids
- Growth hormones (Somatotropin).

3
 - These general metabolic hormones are all necessary for optimum
reproduction. However, they considered to exert an indirect rather than a direct effect on
reproductive hormones.

8. Luteolytic hormones:-
- PG F2.

C). Classification of hormones according to their biochemical properties:-

1. Peptide hormones: - Protein hormones act via plasma membrane

receptors and exert effects in the cytoplasm of the cell.

2. Glycoprotein and

3. Steroid hormones: - Steroid hormones act through nuclear receptors and

cause transcription and translation that result in the production of new proteins.

Endocrine glands, hormones, and their functions and chemical structure:

Gland Hormones Major functions Chemical

structure
1. Thyrotropin releasing 1. Stimulates secretion of 1. Peptide.
hormone (TRH). TSH and prolactin.
2. Corticotropin 2. Causes release of ACTH. 2. Peptide.
releasing hormone
(CRH).
3. Growth hormone 3. Causes release of growth 3. Peptide.
Hypothalamus releasing hormone hormone.
(GHRH).
4. Growth hormone 4. Inhibits release of growth 4. Peptide.
inhibitory hormone hormone.
(GHIH) or
Somatostatin.
5. Gonadotropin 5. Causes release of LH and 5. Peptide.
releasing hormone FSH.
(GnRH).
6. Dopamine or 6. Inhibits release of 6. Amine.
Prolactin inhibiting prolactin.
factor (PIF).
1. Growth hormone. 1. Stimulates protein 1. Peptide.
synthesis and overall growth
Anterior of most cells and tissues.
pituitary 2. Thyroid stimulating 2. Stimulates synthesis and 2. Peptide.
hormone (TSH). secretion of thyroid
hormones (thyroxine and
triiodothyronine).

4
 3. Adrenocorticotropic 3. Stimulates synthesis and 3. Peptide.
hormone (ACTH). secretion of adrenal cortical
hormones (cortisol,
androgens and aldosterone).
4. Prolactin. 4. Promotes development of 4. Peptide.
the female breasts and
secretion of milk.
5. Follicle stimulating 5. Causes growth of follicles 5. Peptide.
hormone (FSH). in the ovaries and sperm
maturation in Sertoli cells of
testes.
6. Luteinizing hormone 6. Stimulates testosterone 6. Peptide.
(LH). synthesis in Leydig cells of
testes; stimulates ovulation,
formation of corpus luteum
and estrogen and
progesterone synthesis in the
ovaries.
1. Antidiuretic hormone 1. Increases water 1. Peptide.
(ADH) (also called reabsorption by the kidneys
Posterior vasopressin). and causes vasoconstriction
pituitary and increased blood pressure.
2. Oxytocin. 2. Stimulates milk ejection 2. Peptide.
from breasts and uterine
contractions.
1. Thyroxine (T4) and 1. Increases the rates of 1. Amine.
triiodothyronine (T3). chemical reactions in most
cells, thus increasing body
metabolic rate.
Thyroid 2. Calcitonin. 2. Promotes deposition of 2. Peptide.
calcium in the bones and
decreases extra cellular fluid
calcium ion concentration.
1. Cortisol. 1. Has multiple metabolic 1. Steroid.
functions for controlling
metabolism of proteins,
carbohydrates and fats; also
Adrenal has anti- inflammatory
cortex effects.
2. Aldosterone. 2. Increases renal sodium 2. Steroid.
reabsorption, potassium
secretion and hydrogen ion
secretion.
Adrenal 1. Epinephrine and nor 1. Same effects as 1. Amine.
medulla epinephrine. sympathetic stimulation.

5
Pancreas 1. Insulin ( cells). 1. Promotes glucose entry in 1. Peptide.
many cells and in this way
controls carbohydrate
metabolism.

2. Glucagon ( cells). 2. Increases synthesis and 2. Peptide.

release of glucose from the
liver into the body fluids.
Parathyroid Parathyroid hormone 1. Controls serum calcium 1. Peptide.
(PTH). ion concentration by
increasing calcium
absorption by the gut and
kidneys and releasing
calcium from bones.
Testes 1. Testosterone 1. Promotes development of 1. Steroid.
male reproductive system
and male secondary sexual
characteristics.
1. Estrogens. 1. Promote growth and 1. Steroid.
development of female
reproductive system, female
breasts, and female
secondary sexual
characteristics.
Ovary 2. Progesterone. 2. Stimulates secretion of 2. Steroid.
‘uterine milk’ by the uterine
endometrial glands and
promotes development of
secretory apparatus of
breasts.
1. Human chorionic 1. Promotes growth of corpus 1. Peptide.
gonadotropin (HCG). luteum and secretion of
estrogens and progesterone
by corpus luteum.
2. Human 2. Promotes development of 2. Peptide.
somatomammotropin. some fetal tissues as well as
Placenta mother breasts.
3. Estrogens. 3. Secretion of estrogen from 3. Steroid.
ovaries.
4. Progesterone. 4. Secretion of progesterone 4. Steroid.
from ovaries.
1. Progesterone. 1. It maintains the pregnancy. 1. Steroid.
2. Relaxin. 2. It causes the relaxation of 2. Steroid.
Corpus cervix, birth canal, ligament
luteum of symphysis, pubis during
parturition.

6
 3. Inhibin. 3. It causes the inhibition of 3. Steroid.
the secretion of FSH and LH.
Uterus 1. Prostaglandin F2 1. It causes the lyses of 1. Steroid.
corpus luteum.
Kidney 1. Renin 1. Catalyzes conversion of 1. Peptide.
angiotensin to angiotensin 1
(acts as an enzyme).
2.1,25.Dihydroxycholec 2. Increases intestinal 2. Steroid.
alciferol. absorption of calcium and
bone mineralization.
3. Erythropoietin. 3. Increases erythrocyte 3. Peptide.
production.
Heart 1. Atrial natriuretic 1. Increases sodium excretion 1. Peptide.
peptide (ANP). by kidneys, reduce blood
pressure.
Stomach 1. Gastrin 1. Stimulates HCL secretion 1. Peptide.
by parietal cells.
1. Secretin. 1. Stimulates pancreatic 1. Peptide.
acinar cells to release
Small bicarbonate and water.
intestine 2. Cholecystokinin. 2. Stimulates gall bladder 2. Peptide.
contraction and release of
pancreatic enzymes.

Hormones of adrenal cortex

There are two main groups of hormones of adrenal cortex as follows:-

1. Mineral corticoids: - related to mineral or electrolyte metabolism.
2. Glucocorticoids: - related to glucose metabolism.

Synthetic mineral corticoids are not practically used but synthetic glucocorticoids
are available and are practically used.

Glucocorticoids

The first glucocorticoids of clinical interest were cortisone, hydrocortisone, prednisone

and prednisolone. The activity of these compounds is similar in quality, the only
difference being in degree of effect. In general, prednisone and prednisolone are from
three to five times more effective than cortisone or hydrocortisone but this refers only to
the glucocorticoid, anti- inflammatory, eosinophil and lymphocyte suppressive actions.
The later glucocorticoid, e.g. triamcinolone, fluocinolone, flumethasone, betamethasone
and dexamethasone are considerably more potent than prednisolone as glucogenic and
anti- inflammatory agents.

7
Indications:-

1. A major use for the glucocorticoids in dairy practice is in the treatment of bovine
ketosis.

2. Glucocorticoids are used in the treatment of pregnancy toxemia in sheep.

3. Glucocorticoids are used to increase the ability of the body to resist the stresses of
trauma, environmental emotions, fatigue etc.

4. Glucocorticoids are used to dampen the inflammatory response in case of skin

disease, eye conditions and arthritis.

5. Glucocorticoids are used to initiate parturition. Administration of a single

injection of dexamethasone (10-30mg), betamethasone (20-30mg), or
flumethasone (5-10mg) to a cow in late pregnancy is followed by parturition
within 72 hours. Unfortunately, these induced parturitions are accompanied by a
very high incidence of retained placenta and there is an increase in calf mortality
to about 15%. For this reasons, the technique remains more of an oddity than a
commercially viable practice.

Contraindications:-

1. Late pregnancy.
2. Major surgery – Causing delayed wound healing.
3. Deep corneal ulceration – progress to penetration.
4. Diabetes mellitus.
5. Cardiac insufficiency.
6.
Dosage:-

Prednisolone and product with similar activity:-

Large animal: - 100-200 mg i /m daily.
Small animals: - 2-20 mg i /m.

Initially followed by oral therapy:-

Dogs: - 0.5-1 mg /kg body weight daily by mouth.
Cats: - 1 mg /kg body weight daily by mouth.

Dexamethasone and products with similar activity:-

Large animal (Cattle, horse):- 10-30 mg i /m daily.
Small animal (Calf, sheep, goat, pig and foal):- 2-5 mg i /m daily.
Dog: - 0.5-2 mg i /m daily.
Cat: - 0.25-0.5 mg i /m daily.

8
Intra articular:-
Large animal: - 2-10 mg.
Peri articular:-
Small animals: - 0.25-5 mg.
Oral:-
Small animals: - 0.25-2 mg.

The hormones controlling reproductive function

Those drugs whose primary action is to modify some feature of the reproductive process
fall into the following groups:-

1. Those which influence gonadal function. e.g. Gonadotrophins, Gonadotrophin

releasing hormones etc.

2. Those which mimic gonadal function. e.g. Sex steroids, androgens, anti-
androgens, estrogens, anti- estrogens, progestogens etc.

3. Drugs which influence uterine function.

e.g. Ecbolics- Ergometrine, methyl ergometrine and oxytocin etc.
Uterine spasmolytics – Perphenazine, heroin, clenbuterol etc.
Cervical dilators – Proquamezine, fenpiprane, fenpipramide and prostaglandins
etc.

Gonadotrophins

Gonadotrophins are the group of drugs which is responsible for the development of the
gonads. These are FSH, LH or ICSH, HCG and PMSG.

Indications of gonadotrophins in horse:-

1. Achieving ovulation in female and cryptorchidism in male and deficiencies in

sperm production and sex drive in the stallion.
Dose: - 1500-5000 i.u i /m twice weekly.
2. In anoestrus.
Dose: - 1500-3000 i.u i /v, i /m, or s /c. Repeated if necessary after 2-3 days.
3. In prolonged estrus.
4. Nymphomania in mares.
Dose: - 1500-5000 i.u i /v. Repeated one month later.
5. Where lactation has failed after parturition.
Dose: - 1500-3000 i.u. s /c, i /m. Repeated 24 hours later.
6. Impaired spermatogenesis.
Dose: - 3000 i.u. i /m twice weekly over a period of 3-6 hours.

9
Indications in cattle:-

Similar to horse. In cattle PMSG and HCG is usually used.

Androgens

Androstenidione and dehydroepiandrosterone of adrenal cortex. Biologically active form

of testosterone is 5  dihydrotestosterone.

Androgens are of importance for their anabolic growth promoting actions and for the
maintenance of libido, spermatogenesis and seminal fluid production.

Uses of androgens:-
1. Deficient sex drive in bull.
2. In the female mammary tumors can be controlled by reducing size.
3. Pseudo pregnancy (Pseudocyesis) in bitch.
4. Estrus suppression in bitch and queen cat.
5. Ageing and debility.
6. Alopecia of hormonal origin.
7. Cryptorchidism in case of failure to respond with gonadotrophins.
8. Banalities in castrated lambs.
9. Feminization in pubertal dogs.
10. Urethral calculi in castrated male cat.

Dosage:-

Bitch / dog:-
Methyl testosterone: - 5-30 mg daily in divided doses i /m.
Testosterone propionate: - 205-5 mg every 2-3 days.
Testosterone phenyl propionate: - 5-10 mg every 7-14 days.

Queen cat / cat:-

Methyl testosterone:-5-10 mg daily or on alternate days.
Testosterone propionate: - 5 mg every 2-3 days.
Testosterone phenyl propionate: - 10 mg every 10-14 days.

Stallion and bull:-

Testosterone propionate: - 25-50 mg twice weekly.
Testosterone phenyl propionate: - 20-50 mg every 7-10 days.

Ram, buck and boar:-

Testosterone propionate:-10-20 mg twice weekly.
Testosterone phenyl propionate: - 10-20 mg every 10-14 days.

10
Side effects:-

Androgens have sodium retaining activity causing cardiac insufficiency. It causes

prostatic hypertrophy.

Anti androgens
Delmadinone acetate.

Dose: - The dose is 1-2 mg / kg by i /m or s /c injection. Effect occurs in about four

days and persists for 3-4 weeks at which time treatment may be repeated.

Estrogens

Estradiol monobenzoate, stilboestrol, stilboestrol dipropionate and dienestrol.

Uses of estrogens:-

1. Anestrous and sub estrus.

2. Removing the retained placenta and for mummified fetus.
3. Used for fattening the animals as growth promotion.
4. Induction of early estrus.
5. Excessive libido in dogs.
6. Lactation can be diminished by oral doses.
7. Used for caponize the cockrels by implementation of 15 mg stilbestrol at the
neck just below the head s /c.

Dosage:-

Cattle and horse:-

Estradiol and stilbestrol injection: - 5-15 mg once.
Dienestrol: - 5 mg once.

Sheep and goat:-

Estradiol and stilbestrol injection: - 0.25 mg.

Sow:-
Estradiol and stilbestrol injection: - 5-10 mg.

Bitch:-
Estradiol and stilbestrol injection: - 0.5-15 mg.

Dog:-
Estradiol and stilbestrol injection: - 0.5-10 mg.

11
Poultry:-
Stilbestrol implants: 15 mg s /c.
Stilbestrol hexoestrol implants: - 7.5-15 mg.

Progesterone

Progesterone suppresses the release of FSH by pituitary gland.

Uses:-
1. Habitual and threatened abortion.
2. The control of estrus.
3. Estrus suppression.
4. Synchronization of estrus.
5. Induction of estrus with ovulation in ewe.

Dosage:-
Mare / cow: - 100 mg i / m or s /c.
Sheep / goat: - 10-50 mg i /m or s /c.
Bitch / cat: - 10-25 mg i /m or s /c.

Side effects:-

Excess causes fatness in bitches when used to prevent estrus.

Drugs which influence uterine contractility

The Ecbolics: - An ecbolic is an agent which stimulates contraction in the uterus at

term. Certain drugs have the ability to induce parturition before full term and are known
as abortifacients.Ecbolics are used at term usually when parturition has commenced.

e.g. Ergot alkaloids such as ergometrine, methyl ergometrine and oxytocin etc.

Indications:-

1. To favour parturition where position and presentation are normal and cervix
dilated.
2. Properly and rapid involution of uterus.
3. Post parturient hemorrhage.
4. Retention of placenta.
Dosage:-
Ergometrine maleate as tablets or by injection.
Horse / cow: - 10-20 mg.
Sheep and pig: - 0.5-1 mg.
Dog and cat: - 0.1-1 mg.

12
 Oxytocin

This injection is derived from an extract of the posterior lobe of the pituitary glands.
Synthetic oxytocin may also be used in the official injection.

Uses:-

1. Expulsion of fetus in uterine inertia.

2. Expulsion of fetal debris and uterine involution.
3. Functional agalactia.
4. In case of mastitis to rapid removal of infected milk.

Dosage:-

Horse and cow: - 10-40 i.u. i /m.

2.5-10 i.u. i /m or i /v.
Sheep, goat and pig: - 2.5-10 i.u. i /m.
0.5-2.5 i.u. i /m or i /v.
Dog and cat: - 0.5-5 i.u. i /m.
Up to 0.5 i.u. i /m or i /v.

Uterine spasmolytics:-

These are the drugs which suppress the uterine contractions. e.g.
perphenazine, heroin and clenbuterol etc.

Cervical dilators:-

proquamezine, fenpiprane and fenpipramide etc.

13
 Drugs affecting uterus and gonads

Prostaglandins

Cloprostenol, fluprostenol and prostalene are the synthetic preparation.

Uses:-

1. Induction of early parturition.

2. Induce abortion.
3. Expulsion of mummified fetus.
4. Resolution of pyometra.
5. Persistent corpus luteum.

Dosages:-

Horse and cattle:-

Prostalene: - 2 mg s /c.
Cloprostenol: - 500 g i /m.
Fluprostenol: - 250 g i /m.

Side effects:-
Sweating, diarrhoea, mild and transient scouring, vascular, gastrointestinal or
respiratory tract disorders.

Contraindications:-
1. Pregnancy.
2. Asthmatic patient.

14
 Antifungal drugs

These drugs are also called antimycotic drugs.

These are of two types:-
1. Fungicidal – Which kills the fungus.
2. Fungistatic - Which inhibits the growth and multiplication of fungus. Most
of the drugs are fungistatic.
The commonly used antimycotic drugs are as follows:-
A. Organic acids with their salts

1. Benzoic acid: - It has bacteriostatic and fungistatic properties; hence it is

used as a preservative of food stuffs. In fungal infection of animal benzoic
acid (6%) is combined with salicylic acid (3%) to make Whitfield’s
ointment (also known as compound ointment of Benzoic acid). This is
effective against Trichophyton infection in cattle and in man.(Ring worm
infection)

2. Salicylic acid: - It has antipyretic, keratolytic and some fungistatic action.

It is suitable for topical ring worm treatment. It softens the crust and then
acts on the organisms. It is applied as Whitfield’s ointment.

3. Undecylenic acid: - This is an effective topical fungistatic agent specially

Microsporum species. At higher concentrations, the acid tends to be
irritant, so the zinc or copper salts are often used in combination, both to
minimize this effect and to use the antifungal action of copper salts.

B. Antifungal antibiotics:-
1. Amphotericin B: - It is derived from Streptomyces venezuelae and is
effective against coccidiomycosis, histoplasmosis, candidiasis and
blastomycosis. These systemic mycoses are difficult to treat and
amphotericin B is the suitable drug to use.

Mode of action: - The mode of action of polyenes antibiotic or Amphotericin

B is the inhibition of the synthesis of ergosterol in the fungal cell wall.

Toxicity: - Toxicity mainly involves the kidneys. In man, the signs include
fever, headache, anorexia etc. Amphotericin B is not effective against the
dermatophytes or dermatophytosis (ring worm).

2. Natamycin: - This is derived from Streptomyces natiliensis. It is effective

against the dermatophytes or ring worm in animals. It is applied as a
suspension containing 0.1 mg/ml of Natamysin.

1
 3. Nystatin: - It is used to treat candidiasis. Administration is topical. It is not
effective against the dermatophytes.
4. Griseofulvin: - It is derived from Penicillium griseofulvium. Both
Trichophyton and Microsporum species are affected but the drug has no
antibacterial activity. Highly effective against the dermatophytes.

Mode of action: - The mode of action of griseofulvin on the dermatophyte is

due to interference with the polymerization of the micro tubular protein into
microtubules. It has fungistatic effect. It is interacts with microtubules and
interferes with mitosis.

Side effects: - Side effects in man are depression of the leukocyte count, with
headache, malaise and rashes. Allergic reaction also occur.

Dose: - Small animal’s → 15-20 mg /kg body weight for 3-4 weeks.
Large animal’s → 10 mg /kg body weight for 3-4 weeks.

C. Imidazole derivatives:-
1. Miconazole, econazole and cotrimazole – are in human use not in animals.
2. Fluconazole
3. Ketoconazole – It may be teratogenic effect.
Dose: - 1-2% as cream or lotion.

D. Miscellaneous antifungals:-
1. Dichlorophen: -This compound is an effective taenicide which affect
cestodes. It is also bactericidal (for Staphylococcus aureus). This
compound is non irritant and in many cases even relieves irritation within
in a few hours of first application. Toxicity is very low and the compound
is effective against both Trichophyton and Microsporum species. At a
concentration of 2% it is used in ointment form and in alcoholic solutions.

2. Monosulfiram: - It has fungicidal and miticidal (insecticide) activities are

both useful. e.g. ear preparations.

3. Copper sulphate: - For ring worm treatment. It is applied daily as an up to

5% ointment or paste, or 1-2% in aqueous solutions. Copper undecylenate
is particularly effective.

4. Crystal violet: - It is an effective Microsporum and Trichophyton species.

It is well known as dark greenish-purple metallic-looking coarse crystals
which are soluble (1:200) in water, fully soluble in alcohol and chloroform
but not soluble in ether.
.

2
 Antiviral antibiotics
Rifampicin: - Rifampicin has both antibacterial and antiviral activity.

Mode of action: - The mode of action of rifampicin due to interference with the assembly
of viral particles (inhibition of RNA polymerase), resulting in abnormal viruses which (at
least in vitro) have reduced survival.

Rifamycin: - Rifamycin has antiviral activity.

Streptovaricins: - Streptovaricins obtained from a strain of Streptomyces spectabilis and

have antiviral activity.

Mode of action: - It inhibits the replication in vitro of the orthopox viruses and certain
RNA tumor viruses. The mode of action is to inhibit RNA polymerase, but in this the
streptovaricins less efficient than the rifamycins.

Bleomycins: - Bleomycins are used in the treatment of cancer but it inhibit vaccinia virus
in vivo and in vitro.

Antiviral agents

Methisasone: - It has been used in the prevention and treatment of small pox in man.
There is less curative than prophylactic activity.

Side effects: - Side effects in man include anorexia, nausea and vomiting.

Amantadine: - It is effective against a number of DNA and RNA viruses in vitro.

Amantadine is indicated in man for the treatment of influenza A viruses.
It has been used experimentally in influenza infections in Turkeys and horses and has
been shown to be effective.

Mode of action: - The mode of action of amantadine is to inhibit the penetration of virus
into the cell or to inhibit the uncoating of the virus particle.

Idoxuridine: - Its mode of action involves inhibition of enzymes involved in DNA

synthesis in infected cells.

Vidarbine: - The mode of action of this compound is to inhibit an enzyme on the

pathway to DNA synthesis. It is used against herpes infections of the eye, skin and brain.

Interferon: - Interferon is thus an important part of the body defense mechanisms.

Interferon appears to prevent the early multiplication of the virus particles.

3
Oseltamivir and Zanamivir: - They are neuraminidase inhibitor. In influenza virus, the
action of neuraminidase is involved in the budding of new virus from infected cells. They
are potent inhibitor of influenza A & B viral neuraminidase, thus inhibit release of virion
arrest further spread of infection. So they clinical use in Bird Flu/ Avian influenza.

The stages of viral replication of a host cell:-

Attachment to host cell

↓
Penetration and uncoating
↓
Transcription
↓
Binding of viral messenger RNA to host ribosomes
↓
Synthesis of viral induced enzymes
↓
Synthesis of viral RNA or DNA
↓
Synthesis of viral structural proteins
↓
Release of mature virus particles.

Figure: The stages of viral infection of a host cell.

4
 PHT-302

Anti-coccidial Drugs

General Mode of action of Anti-coccidial drug:

All the drugs affect the parasites membrane permeability which causes influx of positively
charge ions (cat ions), as a result osmotic environment of the cells are charged and the cells are
ruptured.

Example:
1) Clazuril and diclazuril:
It is used mainly for the treatment of pigeon coccidiosis. It has coccidiocidal effect on Schizont
and gametocytes to coccidia. E.g. - Eimeria labbeana, Eimeria columbianum

Dose:
In poultry 2.5mg/ Bird/ Month

Contraindication:
It must not be administered with drugs that may cause vomiting.

2) Monensin sodium:
Monensin is a metabolic product of Streptomyces cinnamonensis. It is highly effective against all
species of coccidia produces disease in animal & bird. It has additional growth promotional
properties.

Mode of action:
Its action is primarily coccidial & it is believed to act by interfering with intracellular ion
transport.
It forms complexes with the Na & K ion in the developing parasite
Dosage :
Animal Dose
Broiler and layer 100-120 PPM with feed continuously.
Turkeys 100 PPM continuously up to 16 weeks of age.
Cattle 13-33 PPM in feed.
Sheep 33 PPM in feed.

Contraindication:
Monensin must not be given to chickens laying eggs for human consumption.

3) Narasin
The organism Streptomyces aureofaciens naturally produces Narasin.
This is currently used only for the treatment of Eimeria spp of broiler chicks.
It is effective against all intestinal and caecal coccidia if administered continuously in diet.

Dose: 70 PPM in feed continuously.

Contraindication:
Narasin should not be given to egg laying chickens and other birds.
1
Muhibur Rahman, DVM-16th Batch, SAU
 PHT-302

4) Maduramicin
It is a product of Actinomyces jumaensis. It has 12-24 fold greater potency than other anti-
coccidial drug.

Dose:
Broilers: 5 PPM continuously in feed
Contraindication:
Maduramicin should only be used in broiler chickens which must not be slaughtered for human
consumption until 5 days after the last treatment.

5) Amprolium hydrochloride
Amprolium is very active as a preventive agent against all Eimeria spp in broilers

Mode of action: its action cheaply upon the 1st generation Schizont so important for early stage
of infection
Dose: 0.0125% in feed continuously

2
Muhibur Rahman, DVM-16th Batch, SAU
 PHT-3O2

Anti-protozoan drugs
Mention the name of two drugs use for the treatment of each disease
Trypanosomiasis Quinapyramine 4mg/kg bwt as 10-30% solution s/c
compound
8-12mg/kg bwt as 10% solution i/v
Suramin (Antrypol)
Theileriosis Oxytetracycline 5-10mg/kg bwt i/v or i/m for 5days

Halofuginone 1-2 mg/kg bwt orally

Piroplasmosis Imidocarb 2-4 mg/kg bwt s/c

Dimenazine 3.5 mg/kg bwt i/m single dose if needed

repeated after 24 hrs
Anaplasmosis Imidocarb 2-5 mg/kg bwt s/c

Tetracycline 500 mg/kg bwt/day continued for 60 days

hydrochloride
Black head Nitrothiazole 12-24 mg/bird with feed
disease Dimetridazole 0.0125% in feed
Tetracycline 10-20 mg/kg bwt in feed
Ring worm Natamycin 0.1mg/kg bwt of suspension

Griseofulvin Small animal:15-20 mg/kg bwt for 3-4 wks

Large animal: 10 mg/kg bwt for 3-4 wks

Muhibur Rahman, DVM-16th Batch, SAU

 ),'

.I

Herbal medicine (or 'herbal!~.r.n') is the study and use. of med·i~i1~.l~properties of plants.
. ' ;

Plants have the ability to synthesize a wide variety of chemical cbmpounds th~t are used to perform
important biological functions and to defend attack from predai..ors such as insects, fungi and
'
herbivorous mammals. Many of these phytochemlca ls have beneficial effects on long-term health when
consumed by humans, and can be used to effectively treat human diseases.
25% of drugs pre.scribed worldwide come from plant

According t o WHO, 80% pop-alation depends on plant for their primary health care.

Traditional Chinese medicine (TCM)

Ayurvedic medicine

Unani medicine

Modern medicine

Herbs are any plant with leaves, seeds, or flowers used for flavoring, food, medicine, or perfume.

Areas of potential interests in veterinary herbal

Growth promoter
Antistress and adaptogen (Herbs like Ashwagandha , Tulsi, Amla, Ginger enhance non-specific resistance
of the body) · ·

lmmunomodulator

Prevention and control of n).etabolic

,
di~order

Maintenance of reproductive health

How herbal drug·s can administer?

They can be fed fresh, dried, made into powders, made into tir:ictures, given as tablets, made into teas,
made into creams and ointments or used in .any other physical form that seems appropriate to
circumstance and to the particular herb. Dried herbs and tinctures can be kept for a year, at least.

Are herbal medicines safe?

In general, herbal medicines are very safe if used properly and responsibly. How.ever, there are some
cautionary notes.
some herbs are only safe bel~w certain doses. If too much is given, toxicity may develop.
Be certain to identi_fy plants correctly - mistakes can be fatal!
Se extremely careful when using herbs alongside conventional medicines. It is likely that herbs can
dangerously su.mmate with drugs being used for the same purpose effect or counteract drugs.
 Use of some common herb:al drugs in human and veterinary medicine
,,... /
Scientific name /parts used) Common name [;Pharmacological '1Xes I
" action
,

/
\I t/1. llium sativu,;n (Bulb) Garlic Antibacterial, Prevent heart
antiviral and diseases
antifungal (In vitro) (atherosclerosis, high
cholesterol and high
Antioxidant
blood pressure) and

Anti-inflammatory cancer, regulate

blood sue;ar
Immune-stimulant
I
/

Anticancer agent

,.,.zingiber officinaf! (Root/

rhizome)
Ginger
-
Carminative

sialics
-
Appetizer, dyspesia,
gastroparesis, colic,
cohstipation

Centella asiatica (leaves and Thankuni Mild adaptogen, mild Anxiety, reduce
root) antibacterial, hypertension, aid in
antiviral. anti- ,wound healing,
inflammatorx:, revitalize the brain
antioxidant, and nervous system,
increase attention
anti-ulcerogenic,
span and
anxiolytic, cerebral
concentration and
tonic, a circulatory
combat ae;ine;
stimulant, and a
diuretic

Neem Anthelmentics, , Skin diseases,

Azadirachta indica (Bark, /

leaves, flowers and seeds) antiseQtic, diuretic, inflammations and

contracegtive, fevers, and more

febrifuge, recently rheumatic

oarasiticide and disorders, insect
insecticide . repellent and
insecticide effects,
treatment of~,
leprosy, malaria,
ophthalmia,
· , tuberculosis

Adaptogen, Parasitic diseases of

Ocimum tenuiflorum (Leaves Tulsi
antistre ss, skin especially_ring
and seed)
wor.rr.'~ p-arasiticide
 f; . :1
, 1,. \

expector ant and antiseptic

't'
Withania somnife ra "(Berries, Ashwaga ndha Locally applied to
leaves and roots)
\
tumors, tubercul ar
glands, carbuncles,
and ulcers
,,.
·- .•

Oil contained in bulb Locally in insect

VA/luim cepa (Bulb and seeds) Piyaz/ Onion
V
is stimulan t, diuretic bites, scorpion bites
and,expec;;torant and highly infected
\I~ . ' J\I'•
'fi'}:·' and inflamma tory
,;,·It'"'':'-:'i' I
!

swellings {mixed with

'
•
mustard oil), external

'i' 1] .\ .
and internal
dem-ulcent if use

roasted

Kh'oyer Astringent Persistent diarrhoea

Acacia catechu (Woods/ .,
and dysenter y

.~ nus commun is (Seed) Veranda Purgative and constipa tion,

e)(ternal protectiv e indigestion and
impactio n
•
./

.. l yrminal ia arjuna (Bark) Arjun Analgesic and anti- Arthritis

,,
/ inflamma tory
Backache

~ se of herbal drugs In modern medicine

to cancer
Researchers, now a day, examine herbs to find new drugs to treat diseases ranging from cold
~nd AIDS,

Most Important herbal drugs which are in curr~nt u~a in modern medicine:
Atropine: Atropa be/Jadona

Ephedrine: Ephedra sinica ./ ·

Pilocarpine: Pilocarpus jabordani

Morphine: Opium plants

Cardiac digitalis: Digitalis purpurea

/
Arecholine; Arecha catachye

Reserpine: Rowalpia surpentina