PHARMACOLOGY negative cocci, non- β-

lactamase-producing anaerobes.
PENICILLIN - Little activity against gram-
negative rods.
 Share features of chemistry,
- Susceptible to hydrolysis by β-
mechanism of action,
lactamases.
pharmacology, immunologic
characteristics with cephalosporins,  Extended-spectrum penicillins
- Ex. Ampicillin and the
monobactams, carbapenems, β-
antipseudomonal penicillins
lactamase inhibitors.
- Have improved activity against
 Basic structure:
gram-negative organisms.
- Thiazolidine ring
- Relatively susceptible to
- β-lactam ring
hydrolysis by β-lactamases.
- These 2 rings forms 6-
aminopenicillanic acid nucleus Mechanism of Action
which is essential for the
biologic activity of the  Inhibits bacterial growth by
compounds. interfering with the transpeptidation
 Hydrolysis of the β-lactam ring by reaction of the bacterial cell wall
bacterial β-lactamase produces synthesis.
penicilloic acid which lacks  Covalently binds to the active site
antibacterial activity. of penicillin-binding proteins (PBP,
an enzyme) involved in the process
Classification of forming a cross-link between
peptides = stops peptidoglycan
 Antistaphylococcal penicillins
sysnthesis = cell dies
- Ex. Nafcillin
- Resistant to staphylococcal β- Resistance
lactamases.
- Active against staphylococci  4 General Mechanisms:
and streptococci but not against  Inactivation of antibiotic by β-
- Enterococci, anaerobic bacteria lactamase
and gram-negative cocci and - Most common mechanism of
rods. resistance.
 Penicillin - Produced by S. aureus, H.
- Ex. Penicillin G influenza, E. coli (prefers
- Greatest activity against gram- penicillins to cephalosporins)
positive organisms, gram-

MPrejoles 
- AmpC β-lactamase (produced periplasm back across the outer
by P. aeruginosa and membrane.
enterobacter sp) and extended-
spectrum β-lactamases
Pharmacokinetics
hydrolyzes both cephalosporins
and penicillins.  Nafcillin
- Carbapenems = highly resistant - Not suitable for oral
to hydrolysis by penicillinases administration since
and cephalosporinases; gastrointestinal absorption is
hydrolyzed by metallo-β erratic.
lactamase and carbapenemases.  Dicloxacillin, ampicillin and
amoxicillin
 Modification of target PBPs - Acid-stable
- Basis of methicillin resistance in - Relatively well absorbed
staphylococci and of penicillin  Absorption of most oral penicillins
resistance in pneumococci and (amoxicillin being an exception) is
enterococci. impaired by food.
- Administered at least 1-2 hours
 Impaired penetration of drug before or after a meal.
to target PBPs  IV administration of penicillin G is
- Occurs only in gram-negative
preferred to the IM route
species because of their
- Irritation and local pain from IM
impermeable outer cell wall injection of large doses.
membrane (absent in gram-
 Widely distributed in body fluids
negative bacteria)
and tissues with a few exceptions.
- Absence of the proper channel
 Benzathine and procaine penicillins
(porins) or downregulation of its
- Formulated to delay absorption
production.
= prolonged blood and tissue
concentrations.
 Antibiotic efflux
 Penicillin concentrations in most
- Gram-negative bacteria
tissues are equal to those in serum.
produces efflux pump
 Also excreted into sputum and milk
- Consists of cytoplasmic and
to levels 3-15% of those in serum.
periplasmic protein components
that efficiently transport come  Poor penetration into the eye, the
β-lactam antibiotics from the prostate, and the central nervous
system

MPrejoles 
 - In active inflammation of the - High-dose penicillin G can also
meninges (meningitis) = be given as a continuous
concentrations of 1-5 mcg/mL intravenous infusion.
can be achieved with a daily
parenteral dose of 18-24 million  Penicillin V
units which can kill susceptible - Oral form of penicillin.
strains pneumococci and - Only for minor infections
meningococci. because3 of its relatively poor
 Rapidly excreted by the kidneys bioavailability, dosing four
- 10% by glomerular filtration; times a day, and its narrow
90% by tubular secretion. antibacterial spectrum.
 Nafcillin = cleared by biliary
excretion  Benzathine penicillin and
 Oxacillin, dicloxacillin, and procaine penicillin G
cloxacillin = eliminated by both - For intramuscular injection;
kidney and biliary excretion. yield low but prolonged drug
levels.
Clinical Uses - Single injection of benzathine
penicillin (1.2 million units) =
 Penicillin
effective for β-hemolytic
streptococcal pharyngitis;
 Penicillin G
prevents reinfection if given IM
- Drug of choice for caused by
streptococci, meningococci, once every 3-4 weeks
- Benzathine penicillin G, 2.4
some enterococci, penicillin-
million units IM once a week
susceptible pneumococci, non-
for 1-3 weeks = effective
β-lactamase-producing
treatment of syphilis.
staphylococci, Treponema
pallidum and certain other
spirochetes, Clostridium  Penicillins Resistant to
species, Actinomyces and Staphylococcal Beta Lactamase
certain other gram-positive rods, (Methicillin, Nafcillin and
and non- β-lactamase-producing Isoxazolyl Penicillins)
gram-negative anaerobic - Listeria monocytogenes,
organisms. enterococci, and methicillin-
- Effective dose range = 4 and 24 resistant strains of staphylococci
million units per day IV in four are resistant.
to six divided doses.

MPrejoles 
 - Isoxazolyl penicillin (oxacillin, lactam antibiotics against
cloxacillin or dicloxacillin) pneumococci.
o 0.25-0.5 g orally every 4-
6 hours (15-25 mg/kg/d  Amoxicillin
for children) = treatment - Better absorbed orally
of mild to moderate - 250-500 mg three times daily.
localized staphylococcal - Given orally to treat urinary
infections. tract infections, sinusitis, otitis,
o Relatively acid-stable and lower respiratory tract
and have reasonable infections.
bioavailability.
o Food interferes with  Ampicillin
absorption; administered - Effective for shigellosis (not
1 hour before or after amoxicillin).
meals. - Dosages of 4-12 g/d
o Serious systemic intravenously, is useful for
staphylococcal infections treating serious infections
= oxacillin or nafcillin, 8- caused by susceptible
12 g/d, is given by organisms, including anaerobes,
intermittent intravenous enterococci, L. monocytogenes
infusion of 1-2 g every 4- and β-lactamase negative strains
6 hours (50-100 mg/kg/d of gram-negative cocci and
for children) bacilli such As E.coli and
Salmonella sp.
 Extended-Spectrum Penicillins - Not active against Klebsiella sp,
(Aminopenicillins, Enterobacter sp, P aeruginosa,
Carboxypenicillins, and Citrobacter sp, Serratia
Ureidopenicillins) marcescens, indole-positive
- Have greater activity than proteus species and other gram-
penicillin against gram-negative negative aerobes.
bacteria because of their
enhanced ability to penetrate the  Carbenicillin
gram-negative outer membrane. - First antipseudomonal
- Inactivated by many β- carboxypenicillin
lactamases. - No longer used in the USA
- Ampicillin and amoxicillin are
the most active of the oral β  Ticarcillin

MPrejoles 
 - Activity similar to that of alkaline hydrolysis bound to
carbenicillin host protein.
- Less active than ampicillin - Anaphylactic shock (very rare –
against enterococci. 0.05% of recipients); serum
sickness-type reactions (now
 Ureidopenicillins, piperacillin, rare--urticaria, fever, joint
mezlocillin and azlocillin swelling, angioneurotic edema,
- Also active against selected intense pruritus, and respiratory
gram-negative bacilli such as compromise occurring 7-12
Klebsiella pneumonia. days after exposure); and a
- Antipseudomonal penicillin is variety of skin rashes.
frequently used in combination - Oral lesions, fever, interstitial
with an aminoglycoside or nephritis (an autoimmune
fluoroquinolone for reaction to a penicillin-protein
pseudomonal infections outside complex), eosinophilia,
the urinary tract. hemolytic anemia and other
hematologic disturbances and
 Beta Lactamase Inhibitors vasculitis.
 Clavulanic acid, sulbactam, or - Seizures – high dose penicillin
tazobactam in patients with renal failure.
- used in combination with - Neutropenia – associated with
ampicillin, amoxicillin, nafcillin
ticarcillin, and piperacillin - Hepatitis – caused by oxacillin
- extends the activity of these - Interstitial nephritis – caused by
penicillins to include β- methicillin
lactamase-producing strains of - Gastrointestinal upset,
S. aureus as well as some β- particularly nausea, vomiting
lactamase-producing gram- and diarrhea (Large doses of
negative bacteria. oral penicillin)
- Pseudomembranous colitis –
Adverse Reactions associated with ampicillin
 Hypersensitivity Reactions - Vaginal candidiasis
- Antigenic determinants: - Skin rashes not allergic in nature
degradation products of -Ampicillin and
penicillins, particularly amoxicillin
penicilloic acid and products of -Usually when use in viral
infections

MPrejoles 
 - Similar to penicillin  Cephalexin and cephradine
- More stable to many bacterial β- -0.25-0.5 g four times daily (15-
lactamases 30 mg/kg/d)
- Broader spectrum of activity  Cefadroxil
- Strains of E. coli and Klebsiella -0.5-1 g twice daily
sp expressing extended-  Excretion: glomerular filtration
spectrum βlactamases can and tubular secretion.
hydrolyze most cephalosporin.  Parenteral
- Not active against enterococci,  Cefazolin
L. monocytogenes. - only 1st generation parenteral
cephalosporin still in general
use.
FIRST-GENERATION
- Intravenous infusion of 1 g
CEPHALOSPORINS
- Usual intravenous dosage of
 Cefazolin, cefadroxil, cephalexin, cefazolin for adults is 0.5-2 g
cephalothin, cephapirin and intravenously every 8 hours
cephradine. - Can also be administered
 Very active against gram-positive intramuscularly
cocci, such as pneumococci, - Excretion: kidney
streptococci, and staphylococci
Clinical Uses
 Sensitive to E. coli, K.
pneumoniae, and Proteus  Oral drugs
mirabilis - Urinary tract infections and
 Poor activity to P. aeruginosa, staphylococcal or streptococcal
indole-positive proteus species, infections, including cellulitis or
Enterobacter sp, S. marcescens, soft tissue abscess.
Citrobacter sp, and Acinetobacter  Cefazolin
sp. - Drug of choice for surgical
 Anaerobic cocci (eg. Peptococci, prophylaxis
peptostreptococci) are usually - Does not penetrate the central
sensitive nervous system and cannot be
 Bacteriodes fragilis is not used to treat meningitis.
sensitive. - Alternative to an
antistaphylococcal penicillin for
Pharmacokinetics & Dosage patients who are allergic to
penicillin.
 Oral

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SECOND-GENERATION - Children: 20-40 mg/kg/d up to a
CEPHALOSPORINS maximum of 1 g/d
- Cefaclor is more susceptible to
 Cefaclor, cefamandole, cefonicid, β-lactamase hydrolysis
cefuroxime, cefprozil, loracarbef, compared with the other agents
and ceforanide; and the - Not predictably active against
structurally related cephamycins penicillin-non-susceptible
cefoxitin, cefmetazole, and pneumococci except for
cefotetan (have activity against cefuroxime axetil
anaerobes).
 Parental
 Active against organisms - intramuscular administration is
inhibited by first-generation painful and should be avoided
drugs, but in addition they have - All are renally cleared and
extended gram-negative coverage. require dosage adjustment in
 Klebsiella sp (including those renal failure.
resistant to cephalothin) are
usually sensitive. Clinical Uses
 Active against H influenzae but
 Active against β-lactamase-
not against serratia or B. fragilis
producing H influenza or
- Cefamandole, cefuroxime,
Moraxella catarrhalis
cefonicid, ceforanide and
 Used to treat sinusitis, otitis, and
cefaclor
lower respiratory tract infections
 Active against B. fragilis and
 Cefoxitin, cefotetan or
some serratia strains but are less
cefmetazole
active against H. influenza.
- mixed anaerobic infections such
- Cefoxitin, cefmetazole, and
as peritonitis, diverticulitis, and
cefotetan
pelvic inflammatory disease
 None is active against enterococci
 Cefuroxime
or P. aeruginosa
- community-acquired pneumonia
Pharmacokinetics & Dosage = active against β-lactamase-
producing H influenzae or K
 Oral pneumoniae and some
- cefaclor, cefuroxime axetil, penicillin-non-susceptible
cefprozil, and loracarbef pneumococci.
- Adult dose: 10-15 mg/kg/d in - Crosses the blood-brain barrier
two to four divided doses - Less effective in treatment of
meningitis than ceftriaxone or

MPrejoles 
 cefotaxime and should not be  Serratia, Providencia, and
used. Citrobacter also produce a
chromosomally encoded
cephalosporinase that, when
THIRD-GENERATION
constitutively expressed cen
CEPHALOSPORINS
confer resistance to third
 Cefoperazone generation cephalosporins.
 Cefotaxime  Ceftizoxime and moxalactam
 Ceftazidime - Active against B. fragilis
 Ceftizoxime  Cefixime, Cefdinir, Ceftibuten
 Ceftriaxone and Cefpodoxime
 Cefixime - Oral agents possessing similar
activity
 Cefpodoxime proxetil
- Cefixime and ceftibuten are
 Cefdinir
much less active against
 Cefditoren pivoxil
pneumococci and have poor
 Ceftibuten
activity against S. aureus
 Moxalactam
Pharmacokinetics & Dosage
Antimicrobial Activity
 Penetrate body fluids and tissues
 Have expanded gram-negative
well
coverage
 Achieve levels in the
 Some are able to cross the blood-
cerebrospinal fluid sufficient to
brain barrier
inhibit most susceptible pathogens
 Are active against Citrobacter, S. except cefoperazone and all oral
marcescens, and Providencia preparations.
 Also effective against β-  Ceftriaxone
lactamase-producing strains of - (half-life 7-8 hours) can be
haemophilus and Neisseria injected once every 24 hours at
 Ceftazidime and cefoperazone a dosage of 15-50 mg/kg/d
- The only two drugs with useful - Single daily 1-g dose is
activity against P. aeruginosa sufficient for most serious
 Are hydrolyzed by constitutively infections.
produced AmpC β lactamase, and - 2 g every 12 hours
they are not reliably active against recommended for treatment of
Enterobacter species. meningitis.

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  Cefoperazone  Should be avoided in treatment of
- (half-life 2 hours) can be infused enterobacter infections due to
every 8-12 hours in a dosage of emerging resistance.
25-100 mg/kg/d  Ceftriaxone and Cefotaxime
 Remaining drugs in the group - Treatment of meningitis,
(half-life 1-1.7 hours) can be including meningitis caused by
infused every 6-8 hours in pneumococci, meningococci, H
dosages between 2 and 12 g/d, influenzae, and susceptible
depending on the severity of enteric gram negative rods, but
infection. not by L. monocytogenes.
 Cefixime - Most active cephalosporins
- Oral dose 200 mg twice daily or against penicillin-non-
400 mg once daily for urinary susceptible strains of
tract infections. pneumococci and are
- Single 400 mg dose for recommended for empirical
uncomplicated gonococcal therapy of serious infections
urethritis and cervicitis. caused by these strains.
 Cefpodoxime proxetil or  Meningitis caused by strains of
cefditoren pivoxil pneumococci with penicillin
- Adult dose: 200-400 mg twice MICs > 1 mcg/mLmay not
daily. respond even to these agents, and
 Ceftibuten addition of vancomycin is
- 400 mg once daily. recommended.
 Cefdinir  Empirical therapy of sepsis of
- 300 mg/12 hours unknown cause in both the
 Cefoperazone and ceftriaxone immunocompetent and the
- Excretion is mainly through the immunocompromised patient.
biliary tract.  Treatment of infections for which
 Others are excreted by the kidney. a cephalosporin is the least toxic
drug available.
Clinical Use  Ceftazidime + other antibiotics
 Used to treat a wide variety of - Used in neutropenic, febrile
serious infections caused by immunocompromised patients.
organisms that are resistant to
most other drugs.
FOURTH-GENERATION
CEPHALOSPORINS

MPrejoles 
 Cefepime - Not active against extended-
- More resistant to hydrolysis by spectrum β-lactamase-producing
chromosomal β lactamases. strains.
- Hydrolyzed by - Clinical experience with this
extendedspectrum β lactamases. drug and similar investigational
- Good activity against P drugs is limited; their role is not
aeruginosa, Enterobacteriaceae, yet defined.
S aureus, and S pneumoniae
- Highly active against
Haemophilus and Neisseria sp.
- Penetrates well into
cerebrospinal fluid.
- Cleared by the kidneys and has Adverse Effects of Cephalosporins
half-life of 2 hours.
- Good activity against most  Allergy
penicillin-non-susceptible - Anaphylaxis, fever, skin rashes,
strains of streptococci. nephritis, granulocytopenia, and
- Useful on treatment of hemolytic anemia.
enterobacter infections. - Frequency of cross-allergenicity
 Cephalosporins active against between penicillin and
methicillin-resistant cephalosporins is uncertain but
staphylococci is probably around 5-10%.
- Currently under development. - Cross-allergenicity more
 Ceftaroline fosamil common with penicillin and
- Prodrug of the active metabolite early generation of
ceftaroline. cephalosporins.
- First such drug to be approved  Toxicity
for clinical use in the USA. - Oral irritation can produce pain
- Has increased binding to after intramuscular injection and
penicillin-binding protein 2a, thrombophlebitis after
which mediates methicillin intravenous injection.
resistance in staphylococci – - Renal toxicity
BACTERICIDAL - Interstitial nephritis and
- Has some activity against tubular necrosis.
enterococci and a broad gram- - cause the withdrawal of
negative spectrum. cephaloridine from clinical use.

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 - Cefamandole, cefmetazole, - Penicillin-allergic patients
cefotetan and cefoperazone tolerate aztreonam without
- Contains methylthiotetrazole reaction.
group. - Adverse reactions: skin rashes
- hypoprothrombinemia and and elevations of serum
bleeding disorders. aminotransferases.
- severe disulfiramlike
BETA-LACTAMSE INHIBITORS
reactions.
(CLAVULANIC ACID,
SULBACTAM, & TAZOBACTAM)

 Potent inhibitors of many but not

all bacterial β lactamases and can
protect hydrolysable penicillins
from inactivation by these
MONOBACTAMS
enzymes.
 Drugs with a monocyclic β-lactam  Most active against Ambler class
ring. A β lactamases produced by
 Spectrum of activity is limited to staphylococci, H influenzae, N
aerobic gram-negative rods gonorrheae, salmonella, shigella,
(including P. aeruginosa) E. coli, and K pneumoniae.
 No activity against gram-positive  Not good inhibitors of class C β
bacteria or anaerobes. lactamases produced by
 Aztreonam Enterobacter sp, Citrobacter sp, S
- Only monobactam available in marcescens, and P. aeruginosa.
the USA.  Do inhibit chromosomal β
- Gram-negative spectrum is lactamases of B. fragilis and M.
similar to that of the third- catarrhalis.
generation cephalosporins.  Available only in fixed
- Stable to many β-lactamases combinations with specific
except AmpC β lactamases and penicillins.
extended-spectrum β  Ampicillin-sulbactam is active
lactamases. against β-lactamase-producing S.
- Penetrates well into the aureus and H. influenzae but not
cerebrospinal fluid. against serratia, which produces a
- IV dose: every 8 hours in a dose β lactamase that is not inhibited
of 1-2 g. by sulbactam.

MPrejoles 
  Piperacillin-tazobactam does not - Not significantly degraded by
inhibit P. aeruginosa renal dehydropeptidase and do
not require an inhibitor.
CARBAPENEMS  Ertapenem
 Doripenem, ertapenem, imipenem - less active than the other
and meropenem. carbapenems against P.
 Imipenem aeruginsa and Acinetobacter
- First drug of this class. species.
- Has a wide spectrum with good - Not degraded by renal
activity against many gram- dehydropeptidase.
negative rods, including P.  Penetrate body tissues and fluids
aeruginosa, gram-positive well, including the cerebrospinal
organisms, and anaerobes. fluid.
- Resistant to most β lactamases  All are cleared reanally.
but not carbapenemases or  Imipenem dose: 0.25-0.5 g given
metallo- β lactamases. intravenously every 6-8 hours.
- Enterococcus faecium,  Meropenem adult dose: 0.5-1 g
methicillin-resistant strains of intravenously every 8 hours.
staphylococci, Clostridium  Doripenem adult dose: 0.5 g
difficile, Burkholderia cepacia, administered as a 1- or 4-hour
and Stenotrophomonas infusion every 8 hours.
maltophilia are resistant.  Ertapenem dose: longest half-
- Inactivated by life; administered as a once-daily
dehydropeptidases in renal dose of 1 g intravenously or
tubules. intramuscularly; IM is irritating,
- administered together with an formulated with 1% lidocaine.
inhibitor of renal  Indicated for infections caused by
dehydropeptidase, cilastatin for susceptible organisms that are
clinical use. resistant to other available drugs,
 Doripenem and meropenem eg, P. aeruginosa.
- Similar to imipenem but have  For treatment of mixed aerobic
slightly greater activity against and anaerobic infections.
gram-negative aerobes and  Active against many penicillin-
slightly less activity against non-susceptible strains of
gram-positives. pneumococci.

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  Highly active in the treatmet of  Active only against gram-
enterobacter infections because positive bacteria except
they are resistant to destruction by Flavobacterium.
the β lactamase produced by these
Mechanism of Action
organisms.
 Also the treatment of choice for  Inhibits cell wall synthesis
infections caused by extended-  Inhibits the transglycosylate,
spectrum β-lactamase-producing preventing further elongation of
gram-negative bacteria. peptidoglycan and cross-linking.
 Ertapenem is insufficiently active
against P. aeruginosa Antibacterial Activity
 Imipenem, meropenem or  Bactericidal for gram-positive
doripenem, with or without an bacteria.
aminoglycoside, may be effective
 Susceptible to most pathogenic
treatment for febrile neutropenic
staphylococci, including those
patients.
producing β lactamase and those
Adverse Reaction resistant to nafcillin and
methicillin.
 More common with imipenem  Kills staphylococci relatively
 Nausea, vomiting, diarrhea, skin slowly and only if cell are actively
rashes and reactions at the dividing.
infusion sites.  Synergistic in vitro with
 Siezures = excessive levels of gentamicin and streptomycin
imipenem in patients with renal against Enterococcus faecium and
insufficiently. Enterococcus faecalis strains.
 Patients allergic to penicillins may
be allergic to carbapenems as Pharmacokinetics
well.  Poorly absorbed from the
intestinal tract.
 Administered orally only for the
VANCOMYCIN treatment of antibiotic-associated
colitis caused by C. difficile.
 Produced by Streptococcus
orientalis and Amycolatopsis  Parenteral dose is IV.
orientalis.  Widely distributed in the body.
 Cerebrospinal fluid levels 7-30%
of simultaneous serum

MPrejoles 
 concentrations are achieved if  Oral vancomycin for antibiotic-
there is meningeal inflammation. associated colitis caused by C.
 Ninety percent of the drug is difficile
excreted by glomerular filtration. - 0.125-0.25 g every 6 hours

Clinical Use Adverse Reactions

 Parenteral vancomycin  Encountered in about10% of

- Bloodstream infections and cases.
endocarditis caused by  Irritating to tissue, resulting in
methicillin-resistant phlebitis at the site of injection.
staphylococci.  Chills and fever
 Vancomycin + gentamicin  Ototoxicity is rare
- Alternative regimen for  Common reaction
treatment of enterococcal - “red man” or “red neck”
endocarditis in a patient with syndrome
serious penicillin allergy. - Caused by release of histamine.
 Vancomycin + Cefotaxime,
Ceftriaxone, or Rifampin
- Recommended for treatment of
meningitis suspected or known
to be caused by a penicillin TEICOPLANIN
resistant strain of
 Similar to vancomycin in
pneumococcus.
mechanism of action and
 Recommended dose for patients
antibacterial spectrum.
with normal renal function
 Can be given intramuscularly as
- 30-60 mg/kg/d in two or three
well as intravenously
divided doses.
 Long half-life (45-70 hours) =
 Dose for serious infections
once-daily dosing
- Starting dose of 45-60 mg/kg/d
 Available in Europe; not approved
should be given with titration of
for use in the United States.
the dose to achieve through
levels of 15-20 mcg/mL. TELAVANCIN
 Dosage in children
- 40 mg/kg/d in three or four  Active versus gram-positive
divided doses. bacteria, including strains with
reduced susceptibility to
vancomycin.

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  2 mechanisms of action  Novel cyclic lipopeptide
- Inhibits cell wall synthesis fermentation product of
- Disrupts the bacterial cell Streptomyces roseosporus.
membrane potential and  Activity is similar to that of
increases membrane vancomycin except that it is more
permeability. rapidly bactericidal in vitro and
 Approved for treatment of may be active against
complicated skin and soft tissue vancomycin-resistant strains of
infections at a dose of 10 mg/kg enterococci and S. aureus
IV daily.  Known to bind to the cell
 Potentially teratogenic, so membrane via calcium-dependent
administration to pregnant woman insertion of its lipid tail =
must be avoided. depolarization of the cell
membrane with potassium efflux
DALBAVANCIN
and rapid cell death.
 Semisynthetic lipoglycopeptide  Cleared renally
derived from teicoplanin.  Approved doses are 4 mg/kg/
 Shares the same mechanism of dose for treatment of skin and soft
action as vancomycin and tissue infections.
teicoplanin.  6 mg/kg/ dose for treatment of
 Has improved activity against bacteremia and endocarditis once
many gram-positive bacteria daily in patients with normal renal
including methicillin-resistant and function and every other day in
vancomycin-intermediate S. patients with creatinine clearance
aureus. of less than 30 mL/min.
 Not active against most strains of  Can cause myopathy = monitor
vancomycin-resistant enterococci. creatine phosphokinase levels
 Extremely long half-life of 6-11 weekly.
days, which allows for once  Not to be usede to treat
weekly intravenous pneumonia since pulmonary
administration. surfactant antagonizes it.
 Development of dalbavancin has  Can also cause al allergic
been put on hold pending pneumonitis in patients receiving
additional clinical trials. prolonged therapy (> 2 weeks)
 Effective alternative to
DAPTOMYCIN vancomycin.

MPrejoles 
FOSFOMYCIN  Solutions of bacitracin containing
100-200 units/mL in saline
 Stable salt = fosfomycin
- For irrigation of joints, wounds,
trometamol
or the pleural cavity.
 Inhibits a very early stage of
bacterial cell wall synthesis. CYCLOSERINE
 Active against both gram-positive
 Produced by Streptomyces
and gram-negative organisms.
orchidaceous
 Available in both oral and
 Inhibits many gram-positive and
parenteral formulations.
gram-negative organisms, but it is
- Only the oral preparations
used almost exclusively to treat
approved for use in the USA.
tuberculosis caused by strains of
 Active drug is excreted by the
Mycobacterium tuberculosis
kidney.
resistant to first-line agents.
 Approved for use as a single 3-g
 Most of the drug is excreted in
dose for treatment of
active form into the urine.
uncomplicated lower urinary tract
 Dosage for treating tuberculosis is
infections in woman.
0.5 to 1 g/d in two or three
 Appears to be safe for use in
divided doses.
pregnancy.
 Causes serious dose-related
central nervous system toxicity
BACITRACIN with headaches, acute psychosis,
and convulsions.
 Cyclic peptide mixture first
obtained from the Tracy strain of
Bacillus subtilis in 1943.
 Active against gram-positive
 Inhibits cell wall formation
 Highly nephrotoxic when
administered systematically and is
only used topically.
 500 units/g in an ointment base
- Suppression of mixed bacterial
flora in surface lesions of the
skin, in wounds, or on mucous
membranes

MPrejoles 