part I

ANTIMICROBIAL AGENTS
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ANTIBIOTICS

AMINOGLYCOSIDES


MOA: irreversibly bind with 30S ribosome,inhibit protein synthesis. Broad spectrum:active against
both G-ve & G+ve. Active only against aerobes becoz Anaerobes lacks Oxygen-Drug transport
system.


INTERACTIONS:- ototoxic effects of the aminoglycosides, including Streptomycin, are
potentiated by the co-administration of ethacrynic acid, furosemide, mannitol and possibly
other diuretics.
Contra-indicated in pregnant ladies,cause fetal deafness.
a. Ototoxicity
Cochlear damage
Vestibular damage
b. Nephrotoxicity
Neuromuscular blockade


Amikacin (Amikin) indi cat ed in t he short-term treat ment of serious i nfecti ons due to
suscepti ble strains of Gram-negative bact eri a, including Pseudomonas
speci es, Escherichia coli , species of iProt eus, Provi denci a
speci es,Klebsiel la-Enterobact er-Serrat ia speci es and Aci netobacter
(Mima-Herell ea) species

Gentamicin(Garamycin
, G-Mycitin)
used for skin infections like Impetigo,Folliculitis,
Neomycinsulfate
(Neofradin, generic)
dermatosis, impetigo, wounds, burns, ulcers, conjunctivitis, blepharitis and sty
Streptomycin
Used in TB,PLAGUE,TULAREMIA(sub acute bacterial Endocarditis)
Tobramycin(nebcin)

Skin, bone, and ski n struct ure inf ections caused by P. aeruginosa, Proteus spp, E.
coli , Kl ebsiell a spp, Ent erobacter spp, and S. aureus. Sept icemi a in the pedi atri c
pati ent and adult caused by P. aeruginosa, E. coli, and Klebsi ell a .






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CARBAPENEMS

Synthetic Beta-Lactamantibiotics,active against Beta-Lactamase producing G+ve &
G-ve,,Anaerobes, P.Aeruginosa
MOA:-
Exerts its bactericidal activity by inhibiting bacterial cell wall biosynthesis. They
inactivate PBP by binding to it thereby inhibitng the cell wall synthesis.


Doripenem (Doribax) Imipenem-Cilastatin(Primaxin)
Ertapenem (Invanz) Meropenem (Merrem)




CEPHALOSPORINS
Note:- Bicyclic ring structure
beta-lactam ring (in common with penicillins)
Mechanism of action: binds to penicillin binding proteins and inhibition of formation of cell wall
.
9. Classification, and Trade Names


Route of Trade Names
Administration
First Generation

Cefazolin IM, IV Ancef (Glaxo), Kefzol (Lilly)

Cephalothin IM, IV Keflin (Lilly)
Cephapirin IM, IV Cefadyl (Apothecon)
Cefadroxil IV, PO Duricef (Bristol-Myers Squibb)
Cephalexin PO Keflex & Keflet (Lilly)
Cefanex (Apothecon)
Cephradine PO Velosef (Apothecon)
Second Generation

Cefuroxime IM, IV Zinacef (Glaxo-SK), Kefurox (Lilly)
Cefamandole IM, IV Mandol (Lilly)
Cefoxitin IM, IV Mefoxin (Merck)
Cefonicid IM, IV Monocid (Glaxo-SK)
Cefotetan IM, IV Cefotan (Stuart)
Cefmetazole IV Zefazone (Pharmacia/Pfizer)
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Cefuroxime axetil PO Ceftin (Glaxo-SK)
Cefaclor PO Ceclor (Lilly)
Cefdinir PO Omnicef (Pfizer)
Cefprozil PO Cefzil (Bristol-Myers Squibb)
Loracarbef PO Lorabid (Lilly)
Third Generation

Cefotaxime IM, IV Claforan (Hoechst-Roussel)
Ceftizoxime IM, IV Cefizox (Fujisawa)
Ceftriaxone IM, IV Rocephin (Roche)
Ceftazidime IM, IV Fortaz & Ceptaz (Glaxo SK),
Tazidime (Lilly), Tazicef (Glaxo SK)
Cefoperazone IM, IV Cefobid (Roerig)
Cefixime PO Suprax (Lederle)
Ceftibuten PO Cedax (Schering Plough)
Cefpodoxime axetil PO Vantin (Pharmacia/Pfizer)
Cefepime IM, IV Maxipime (Bristol-Myers Squibb)

INTERACTIONS.
Interactions:
.Cause/worsen diarrhea with diphenoxylate-atropine (LOMOTIL)
.Birth control pills not advised with cephlsprns.
.Increase risk of excess bleeding wih
*.Anticoagulants(Warfarin),
*.Blood viscosity reducing agents like Pentoxxiphylline(Trental)
*.Anti-Seizure medicines like Divalproex(DEPAKOTE), & Valproic acid(DEPAKENE).


Effect Description
Cephalosporins with Ethanol

Alcoholic beverages taken with or up to 72
Methylthioltetrazol

h after cefametazole, cefoperazone cefazolin,
Group

or cefotetan may produce a disulfiram-like
rxn. Flushing, sweating, tachycardia
Cephalosporins Aminoglycosides Nephrotoxicity of AGs may be potentiated
with some cephs., especially cephalothin
Cephalosporins with Anticoagulants Hypoprothrombinemic effects of
Methylthioltetrazol

anticoagulants are increased. Bleeding
Group

complications may occur. An additional

problem is depletion of the gut flora

resulting in decreased Vitamin K synthesis
(problem with 2nd & 3rd gen. cephs)
Cephalosporins Urine glucose testing May lead to false positives in diabetics
taking cephalosporins
Probenicid Cephalosporins Probenicid inhibits renal tubular secretion

of cephalosporins that are primarily renally
excreted.
Antacids Cephalosporins Reduced absorption of ceclor CD, cefdivir,
and cefpodoxime
H
2
antagonists Cefpodoxine, Reduced absorption of cefpodoxime and

Cefuroxine

Celuoxime
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FIRST GENERATION
NOTE:- Good activity against wide spectrum of gram +ve,including Pencillinase producing
Staphylococci,some E.Coli,Proteus mirabilis.
Inactive against:
*.MRSA(Methicillin Resistant Staphy.Aureus.
*.Entorococci.

Cefadroxil (Duricef, Ultracef)
Cefazolin (Ancef, Kefzol)
Cephalexin (Keflex, Panixine DisperDose) (third-line alternative for the treatment of urinary tract
infection in pregnant women (after nitrofurantoin and trimethoprim)
Cephradine (Velosef)
SECOND GENERATION
NOTE:-more stable to hydrolysis by Beta-lactamase produced by G-ve,so enhanced activity against E.Coli
& Salmonella.
Cefaclor (Ceclor, Raniclor)( 1
st
line treatment for Otitis Media,Sinusitis, cellulitis, diabetic foot infection and
mastitis)
Cefotetan (Cefotan)
Cefoxitin (Mefoxin)(have anaerobic activity)
Cefprozil (Cefzil)
Cefuroxime (Ceftin [oral], Zinacef [parenteral])

THIRD GENERATION
*.The third-generation cephalosporins except for cefoperazone penetrate cerebrospinal fluid and
are indicated for the treatment of bacterial meningitis.
*. Cefotaxime and ceftizoxime have the best gram-positive coverage of the third-generation
agents. Ceftazidime and cefoperazone are the only third-generation drugs that provide
antipseudomonal coverage.
*.Ceftriaxone's long half-life allows for once-daily dosing, making ceftriaxone an excellent drug
for outpatient antibiotic therapy of community-acquired infections
Cefdinir (Omnicef)
Cefditoren (Spectracef)
Cefixime (Suprax)
Cefoperazone (Cefobid)
Cefotaxime (Claforan)
Cefpodoxime (Vantin)
Ceftazidime (Fortaz, Ceptaz, Tazidime, Tazicef)
Ceftibuten (Cedax)
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Ceftizoxime (Cefizox)
Ceftriaxone (Rocephin) (appropriate 1
st
line treatment for Gonnorrhoea,Pelvic InflammatoryDisease
(PID,,Surgical prophylaxis,,used in Lyme Disease.)).
FOURTH GENERATION
Cefepime (Maxipime) (pneumonia,Intra abdominal infections,UTI)

FLUOROQUINOLONES

MOA: Synthetic agents that inhibit DNA Gyrase(Topoisomerse II & IV), during bacterial growth &
reproduction.BroadSpectrum active against both G-ve & G+ve.

FIRST GENERATION
Nalidixic acid(Neggram)

SECOND GENERATION

Ciprofloxacin (Cipro,CiproXR,ProquinXR)(Infectiousdiarrhea,Typhoid fever, Acute sinusitis,UTI)
Ofloxacin (Floxin)(Gonococcal infections,Prostatis,LRTI)
Norfloxacin (Noroxin, Chibroxin ophthalmic)

THIRD GENERATION
Levofloxacin (Levaquin)

FOURTH GENERATION
Moxifloxacin (Avelox)
Gemifloxacin (Factive)
Gatifloxacin(Zymar)

















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First-line indications Second-line indications
Sexuall y transmitted infections
Gonorrhoea ceftriaxone in
combination with azithromycin
Pelvic inflammatory disease
ceftriaxone in combination with
doxycycline and metronidazole
Epididymo-orchitis ceftriaxone in
combination with doxycycline
Respiratory tract infections
Otitis media first-line amoxicillin,
second-line erythromycin,
co-trimoxazole or cefaclor
Sinusitis first-line amoxicillin,
second-line doxycycline,
co-trimoxazole or cefaclor
Serious infections
Meningitis ceftriaxone is an
alternative to benzylpenicillin
Skin infections
Cellulitis first-line flucloxacillin,
second-line erythromycin,
roxithromycin, co-trimoxazole or
cefaclor
Diabetic foot infections first-line
amoxicillin clavulanate, second-line
co-trimoxazole or cefaclor in
combination with metronidazole
Mastitis first-line flucloxacillin,
second-line erythromycin or cefaclor
Urinary tract infections in pregnancy
First-line nitrofurantoin, second-line
trimethoprim, third-line cephalexin

Continued

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