Pharmacology Ahmad Iqbal Butt Roll # 60

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Pharmacology Ahmad Iqbal Butt Roll # 60

CEPHALOSPORINS
Cephalosporin discovery credit to Brotzu in 1945. First introduced into clinical use in 1964(cephalothin) A class of beta lactam antibiotics

Dr.T.V.Rao MD

Introduction to Cephalosporins..
They were first isolated from the cultures of cephalosprium acremonium They are structurally and pharmaclological related to penicillins Derived from 7aminocephalosporanic Acid

Dr.T.V.Rao MD

Mechanism of action
It binds to Penicillins binding protiens and inhibition of formation of cell wall These are bactericidal Agents Resistance Poor penetration of bacteria by the drug Lack of penicillin binding protein for a specific drug Degradation of drug by beta lactamases Failure of activation of autolytic enzyme in cell wall

Dr.T.V.Rao MD

Classifications of Cephalosporins
4-Generations Based upon: The spectrum of anti microbial activity These Generations increased Gram negative and decreased Gram positive Activity

Dr.T.V.Rao MD

First Generation
Cephalexin , po Cephazolin Cephalothin Cephradine , po Active against G + cocci (except enterococci) s.pneumoniae, s.pyogenes Use 1 Urinary tract infection 2 prophylaxis of surgical wound infecion 3 Cellucitis Modest activity against Gbactria
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Second Generation
Cefoxitin Cefuroxine Cefaclor Cefprozil Mainly effective against G-Bacteria Modest activity against G+Bacteria Use primary upper and lower respiratory tract infection

Dr.T.V.Rao MD

Third Generation
Ceftriaxone Cefotaxine Enhanced G-activity Use Meningitis Gonorrhea (neisseria Gonorrhea)

Dr.T.V.Rao MD

Fourth Generation
Cefepime
Active against strep, staphylo, Aerobic Gm-

Use
Infection caused by s.pneumonia

Dr.T.V.Rao MD

Uses
Pharyngitis Tonsilitis Otitis Pneumonia UTI Skin infection Bone infection Surgical prophylaxis

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Adverse Effect
Hypersensitivity Reaction most common, Anaphylaxis, Bronchospasm, urticaria Nephrotoxicity Thrombophelebitis Super Infection Diarrhea Bleeding disorder, flushing, vomiting with alcohol intake
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Pharmacokintics
Cephalosporin are given Orally and Parent rally Extent of binding to plasma protein vary from one to another Mostly excreted unchanged by kidney Half life 30-90 min
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Contraindications
Hypersensitivity to cephalosporins or penicillins combination with aminoglycosides and loop diuretics b/c of their peritonial causing nephrotoxicity

Dr.T.V.Rao MD

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