Drug Profile of penicillin

Active ingredient penicillin G potassium

Drug Category (PRESCRIPTION/OTC) prescriptive drug
WHO Essential Drug List

1. PRODUCT DESCRIPTION

Sr. Brand Manufacturer Dosage Strength Price/unit

No Name Form
.
Benza L-A Macter pharma Inj 0.6 MIU 12.75-15
1 1.2MIU 18-22

BENZIABI Zafa pharma Inj 1.2MIU 18-22

2 OTIC
0.6 MIU 12-15

BIOTIC-P English pharma Inj 0.6MIU 12-15

3 1.2MIU 18-22

LA-PEN PDH pharma Inj 0.6 MIU 12-15

4 1.2MIU 18-22

PENIDURE pfizer Inj 0.6 MIU 12-15

5 L-A
1.2MIU 18-22
How to store this drug: - Store in a refrigerator, 2° to 8°C (36° to 46°F). Keep
from freezing.

1. CHEMISTRY OF DRUG

Chemical Class:- N-containing heterocyclic antibiotics

Chemical Nature/Structure: - The basic chemical structure of all penicillin consists of a
beta-lactam ring, a thiazolidine ring, and a side chain (6-aminopenicillanic acid). The
antibacterial activity of the penicillin lies within the beta-lactam ring. Any alteration in
this ring structure forms penicilloic acid and the antibacterial activity of the compound is
lost. The side chain varies with each penicillin compound and generally determines the
spectrum of activity, as well as the pharmacokinetic properties of the compound.
Physical Properties: - Melting point:82-83 °, Boiling point:663.3±55.0 °C(Predicted), Density :
1.2729(rough estimate), refractive index: 1.6930 (estimate), solubility H 2O: 100 mg/mL, form: powder,
pka:2.45±0.50(Predicted), color Crystals, Water Solubility: 2.675g/L (25 ºC)

3. PHARMACOKINETICS
ABSORPTION:- Rapidly absorbed following both intramuscular and subcutaneous injection.
Initial blood levels following parenteral administration are high but transient. Oral absorption in
fasting, healthy humans is only about 15-30% as it is very susceptible to acid-catalyzed
hydrolysis.

i. DISTRIBUTION

Bio- Protein Placental Blood Secreted in Volume of Time

avail- Binding Barrier Brain Distributio for
Milk
ability (%) Barrier n Onset
of
Action
Bind to Crosses poor yes 0.53–0.67 -
serum human blood- L/kg in adults
15-30
proteins placenta. brain with normal
(45-68%), renal function
barrier
 mainly diffusion
albumin.

ii. ELIMINATION
Half Life Site of Active Metabolite Route of Excretion
Metabolism (if Any)
About 16-30% of an n/a
In adults with Penicillin G is
intramuscular dose is
normal renal eliminated by the
metabolized to
function is kidneys. Nonrenal
penicilloic acid, an
reportedly 0.4–0.9 clearance includes
inactive metabolite.
hours hepatic metabolism and,
Small amounts of 6-
to a lesser extent,
aminopenicillanic
biliary excretion.
acid have been
recovered in the
urine of patients on
penicillin G. A small
percentage of the
drug appears to be
hydroxylated into
one or more active
metabolites, which
are also excreted via
urine.

4. CLINICAL PHARMACOLOGY

Pharmacological B lactam
class

Therapeutic Class antibiotic

Inhibits the biosynthesis of cell wall mucopeptide;

Mechanism of bactericidal against sensitive organisms when adequate
action concentrations are reached, and most effective during the
stage of active multiplication; inadequate concentrations
 may produce only bacteriostatic effects.
Spectrum (in case Narrow spectrum
of
antibiotic)
History of previous hypersensitivity to penicillins,
Contraindications cephalosporins.don't inject parentral solution into or near an
artery or nerve
History of patients for any allergy, hay fever, asthma, allergic
rhinitis, in such cases penicillins should be avoided. Penicillin
Precautions
sensitivity test can be done by intra dermal inj of penicillin on
the ventral aspect of forearm of patient, signs of itching
erythema, and wheal formation can be watched for. Adrenaline
and hydrocortisone should be kept ready before administration
of penicillin. For anaphylactic shock
Not assigned.
FDA pregnancy
class

Clinically Monitoring Parameters

Generally, monitoring of patients on penicillin is not required. However, one study
recommended therapeutic drug monitoring during endocarditis treatment caused by
enterococci to determine penicillin exposure and dosing better. This vigilance will
decrease the chance of antibiotic resistance while improving therapeutic impact. With
long-term administration of penicillin, it may be necessary to monitor hematologic,
renal, and hepatic function.

2. DOSAGE SCHEDULE

Sr. Route Recommended Dosage Duration of

No Indication of Child Adult therapy (if
. Administ any)
ration
1 enterococcal IV ≤ 1week and > 2kg 4-6 mui IV 10-14 days
endocarditis 20,000-50,000 u/kg q4h
IV q8h
≤ 1 week and ≤ 2kg:
20,000-50,000 u/kg
IV q12h
> 1 week and ≤ 2kg:
25,000-65,000 u/kg
IV q8h

2 Streptococcal IV > 1 week and > 2kg: 2-3 mui IV 10-14days

meningitis 25,000-65,000 u/kg q4h
IV q6h

3 Streptococcal IV > 1month and < 12 2mui IV q4- 10-14days

infection: years, severe 6h
infection: 40,000-
60,000 u/kg IV q4-6h
> 12 years: usual adult
dose

4 anthrax (setting IV <12 years: 50,000 4 mg IV 10-14days

of bioterrorism) u/kg IV q6h q4h

5 neurosyphilis: IM/IV 100000 to 250000 18-24 10-14 days

units/kg/day in Miu/day in
divided doses every 4- divided
6 hr. doses every
3-4hr
Severe infection up to
400000 unit/kg/day in
divided doses every 4-
6 hr;max24 Miu/day
 3. ADJUSTMENT OF DOSAGE (if required) IN
RENAL/HEPATIC IMPAIRMENT: Most penicillins are
primarily renally eliminated and do not require a dosage adjustment on hepatic
impairment. Because of the nonspecific nature of liver function tests (ALT, AST,
GGT, etc.) and the fact that increases in these markers may not correlate with
intrinsic hepatocellular activity, it is difficult to recommend precise dosage
adjustments for hepatically eliminated drugs. Some penicillins that may warrant a
dosage adjustment in hepatic impairment include nafcillin and mezlocillin. An up
to 50% dose reduction of nafcillin may be appropriate in patients with a
combination of renal and hepatic insufficiency. Mezlocillin’s dose may be reduced
by 50% or the dosing interval doubled in patients with severe hepatic impairment

4. SIDE EFFECTS Benzylpenicillin has low toxicity, except for the nervous system
direct injection into arteries, can cause serious neurotoxic damage, including
hyperreflexia, myoclonic twitches, seizures and coma.

8.ADMINISTRATION GUIDELINES
How to take this drug
Penicillin G administration can be either intravenously or intramuscularly. Penicillin G
benzathine administration ensures a continuous low dose of penicillin G over 2 to 4
weeks.
Can you break or crush tablets
No Counseling
As with any antibiotic, patients must receive counsel to finish the full course of medicine
to prevent bacterial resistance.
INSTRUCTION FOR TOPICAL USE (IF ANY):
N/A
FOR I/V ROUTE

Solvent For Reconstitution Penicillin G potassium is highly water soluble. It may be

dissolved in small amounts of Water for Injection, or Sterile
(for dry powder for injection) Isotonic Sodium Chloride Solution for Parenteral Use

Volume To Be Added/ When the required volume of solvent is greater than the
Concentration capacity of the vial, the penicillin can be dissolved by first
injecting only a portion of the solvent into the vial, then
withdrawing the resultant solution and combining it with
the remainder of the solvent in a larger sterile container.

Temperature And Storage All solutions should be stored in a refrigerator. When

Time After Reconstitution refrigerated, penicillin solutions may be stored for seven
days without significant loss of potency.

Compatible IV fluids THE 20,000,000 UNITS (20 MILLION UNITS) DOSAGE

MAY BE ADMINISTERED BY INTRAVENOUS
INFUSION ONLY.

5. DRUG-DRUG/FOOD/HERB INTERACTIONS

Interacting Severity Mechanism Outcome Management

drug
6. TOXICOLOGY

Toxic Dose Signs & Symptoms of Management/Treatment

Toxicity (including antidote)
Drug Profile of penicillin
Active ingredient penicillin V potassium
Drug Category (PRESCRIPTION/OTC) prescriptive drug
WHO Essential Drug List _

1. PRODUCT DESCRIPTION

Sr. Brand Manufacturer Dosage Strength Price/unit

No Name Form
.
Penvee polyfine syrup 125mg 23-28
1 Pakistan (pvt)
LTD
Penicillin v Lisko Pakistan tablets 250mg 28.75
2 (pvt) LTD
 Penisol vk Lisko Pakistan syrup 125mg/5ml 34-49
3 (pvt) LTD

Penicillin v Hizat syrup 125mg/5ml 21.25-25.00

4 pharmaceutical
industries(pvt)L
td.
Penicillin v Lisko Pakistan tablets 125mg 7.88-9.27
5 (pvt) LTD

How to store this drug:- Store penicillin V tablets at room temperature away from
moisture, heat, and light. Store liquid penicillin V in a refrigerator but do not allow it to
freeze. Throw away any liquid that has not been used within 14 days after it was mixed at
the pharmacy.

1. CHEMISTRY OF DRUG

Chemical Class N-containing heterocyclic antibiotics

Chemical Nature/Structure The basic chemical structure of all penicillins consists of a
beta-lactam ring, a thiazolidine ring, and a side chain (6-aminopenicillanic acid). The
antibacterial activity of the penicillins lies within the beta-lactam ring. Any alteration in
this ring structure forms penicilloic acid and the antibacterial activity of the compound is
lost. The side chain varies with each penicillin compound and generally determines the
spectrum of activity, as well as the pharmacokinetic properties of the compound.

Physical Properties penicillin is white crystalline powder.it is odorless.slightily bitter

taste.ph(0.5% aq solution)5 to 7.4.

3. PHARMACOKINETICS
ABSORPTION penicillin V potassium is absorbed from GI tract in healthy, fasting
adults. Considerable interindividual variation in extent of oral absorption; some patients
may not absorb therapeutic concentrations of oral penicillin. Peak serum concentrations
attained within 30–60 minutes. Food may result in lower and delayed peak serum
concentrations.

i. DISTRIBUTION

Bio- Protein Placental Blood Secreted in Volume of Time

avail- Binding Barrier Brain Distributio for
Milk
ability (%) Barrier n Onset
of
Action
60–73% 75–89%. Crosses poor Distributed Widely 0.5-1
human blood- into human distributed hr.
placenta. brain milk. into body
barrier tissues.
diffusion Highest
concentratio
ns in
kidneys;
ii. ELIMINATION
Half Life Site of Active Metabolite Route of Excretion
Metabolism (if Any)
0.5-0.6 hr. Metabolized in the N/A urine(as unchanged
liver. drug and metabolites)

4. CLINICAL PHARMACOLOGY
Pharmacological Penicillin
class

Therapeutic Class antibiotic

Inhibits the biosynthesis of cell wall mucopeptide;

Mechanism of bactericidal against sensitive organisms when adequate
action concentrations are reached, and most effective during the
stage of active multiplication; inadequate concentrations
may produce only bacteriostatic effects.
Spectrum (in case Broad spectrum
of
antibiotic)
Allergy to penicillins, cephalosporins, or imipenem
Contraindications

History of allergy. Renal impairment. Hypersensitivity to

penicillin,cephalosporin,or other b lactam
Precautions

Use of penicillin products in humans has not shown any

evidence of fetal harm.
FDA pregnancy
class

Clinically Monitoring Parameters

Your doctor may do blood tests to check how well your kidneys are working. If
your kidneys aren’t working well, your doctor may lower your dose of this drug.
 2. DOSAGE SCHEDULE

Sr. Route of Recommended Dosage Duration of

Administration therapy (if
No Indication Child Adult any)
.
1 Streptococcal Oral 125- 125- 10days
infection 250mg 250mg

2 Skin infection Oral 250- 250- -

500mg 500mg
3 fusospirochetos Oral 250- 250- -
is 500mg 500mg
4 Pneumococcal Oral 250- 250- least 2
Infections 500mg 500mg days.

5 Staphylococcal Oral 250- 250- -

Infections 500mg 500mg

6 Rheumatic Oral 125- 125- -

fever 250mg 250mg

3. ADJUSTMENT OF DOSAGE (if required) IN

RENAL/HEPATIC IMPAIRMENT:
Cockcroft-Gault CrCl estimates (using the creatinine clearance calculator) should be used for
drug dosing rather than the automated MDRD eGFR produced by the clinical chemistry
laboratory available on NOTIS.

CrCl (ml/min) Dose

20 – 50 Normal
 10 – 20 Normal
<10 Normal
Refer to renal pharmacist for advice on dosing in haemodialysis and peritoneal dialysis.
Refer to critical care pharmacist for advice on dosing in CVVH

4. SIDE EFFECTS
Upset stomach, nausea, vomiting, diarrhea, and mouth sores may occur. you may
develop a black, "hairy" tongue. serious side effects, including unusual tiredness,
joint/muscle pain, easy bruising/bleeding

8.ADMINISTRATION GUIDELINES
How to take this drug

Do not take this drug with food. Take it on an empty stomach, at least 1 hour before
eating or 2 hours after eating.
Can you break or crush tablets

You can cut or crush the tablet.

Counseling about the drug

Do not share this medication with others. This medication has been prescribed for
your current condition only. Do not use it later for another infection unless your
doctor tells you to. With prolonged treatment, laboratory and/or medical tests (such as
kidney function, complete blood counts) should be performed periodically to monitor
your progress or check for side effects. Consult your doctor for more details.

INSTRUCTION FOR TOPICAL USE (IF ANY):

N/A

FOR I/V ROUTE

Solvent For Reconstitution

(for dry powder for injection)
Volume To Be Added/
Concentration

Temperature And Storage

Time After Reconstitution

Compatible IV fluids

5. DRUG-DRUG/FOOD/HERB INTERACTIONS

Interacting Severity Mechanism Outcome Management

drug
amifampridine N/A Unknown Inc toxicity if Modify
amifampridine therapy/monitor
closely

Ethinylestradi N/A By plasma The therapeutic caution/monitor

ol protein binding efficacy of
competition. Ethinylestradiol
can be decreased
when used in
combination with
Phenoxymethylpen
icillin.
Levonorgestre Antibiotic By altering The therapeutic causion/monitor
l may dec intestinal flora. efficacy of
hormonal Levonorgestrel can
contracepti be decreased when
ve efficacy. used in
combination with
Phenoxymethylpen
icillin.
Choline N/A By plasma Either Inc level of caution/monitor
magnesium protein binding the other
Tri salicylate competition

Dienogest/estr N/A By altering Will dec the level Caution/monitor

adiol valerate intestinal flora or effect of an alternate or
Dienogest/estradiol additional form
valerate of birth control
may be
advisable during
concomitant use
Aspirin N/A By dec renal Either inc level of Minor
clearance the other /significance
unknown

food N/A Take on an Absorption is

empty stomach. increased 1 hour
before or 2 hours
after food

6. TOXICOLOGY

Toxic Dose Signs & Symptoms of Management/Treatment

Toxicity (including antidote)
 Extremely high doses Stomach upset or possibly Seek emergency medical
(5g/kg) diarrhea. attention if you think you have
used too much of this medicine.
Confusion,agitation,hallucination
or seizures