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ANTIBIOTICSSUBMITTED TO:

Mr. NASEEM ABBAS SB

SUBMITTED BY:

Mr. NOMAN HAFEEZ KHOSA

SUBJECT:

Mchanism of Antimicrobial Drugs

DISCIPLINE:

BS-MICROBIOLOGY

DATED: (March11, 2015.)

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SHORT HISTORY OF ANTIBIOTICS AND OF DEVELOPING RESISTANCES.A.Waksman introduced the term „antibiotic“in 1942. In forties to sixties, the term “antibiotic” was clearly differed from the term “chemotherapeutic drug”: Antibiotics were natural drugs produced by several fungi or bacteria. Chemotherapeutic drugs were man-made substances. Nevertheless the differences were abolished after chemical synthesis of some antibiotics has been realized and new drugs have been developed from the natural products with binding various side chains to the basic structure.From this point of view, the history of antibiotics begun in 1932 when the first sulfonamide was prepared. The boom of sulfonamides appeared thereafter with about 5.000 substances developed during years 1932-1945. Sulfonamides were effective in urinary tract infections, shigellosis, pneumococcal pneumonia and even in purulent meningitis. But the effect of sulfonamides was totally exceeded with penicillin and streptomycin. It was a happy chance that these two antibiotics covered the whole spectrum of bacteria. Penicillin was very effective against the most danger microbes of that time – pneumococci and streptococci – and also against other important pathogens like staphylococci, meningococci, gonococci, Corynebacterium diphteriae, or Treponema pallidum. Streptomycin killed the gram-negative aerobic bacteria and Mycobacterium tuberculosis.

β-Lactam antibioticsBenzylpenicillins Penicillin G(benzylpenicillin sodium, procaine benzylpenicillin, benzathine penicillin)

Phenoxy-penicillins(oral penicillins)Penicillin VPropicillin

Penicillinaseresistantpenicillins(anti-staphylococcalpenicillins)OxacillinDicloxacillinFlucloxacillin

AminobenzylpenicillinsAmpicillinAmoxicillin

Ureidopenicillins(broad-spectrumpenicillins)MezlocillinPiperacillin

β -Lactam/

β -lactamase InhibitorsAmpicillin/sulbactamAmoxicillin/clavulanatePiperacillin/tazobactamSulbactam in freeCombinations

Cephalosporins(first generation)CefazolinCefalexin (oral)Cefadroxil (oral)

Cephalosporins(secondgeneration)CefuroximeCefotiam

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Cefuroxime axetilCefaclor (oral)Loracarbef

Cephalosporins(third and fourthgeneration)CefotaximeCeftriaxone

CeftazidimeCefepimeCefixime (oral)Cefpodoximeproxetil (oral)Ceftibuten (oral)MonobactamsAztreonamCarbapenemsImipenem

MeropenemErtapenemDoripenemb -Lactamase inhibitorsClavulanic acidSulbactamTazobactam

Other substancesAminoglycosidesStreptomycinGentamicinTobramycinNetilmicinAmikacinTetracyclinesTetracyclineDoxycyclineMinocyclineQuinolonesGroup I:NorfloxacinGroup II:EnoxacinOfloxacinCiprofloxacinGroup III:LevofloxacinGroup IV:MoxifloxacinI: Indications essentially limited to UTIII: Widely indicated

III: Improved activity against Gram-positive and atypicalpathogensIV: Further enhanced activity against Gram-positive andatypical pathogens, also against anaerobic bacteriaLincosamidesClindamycinAzol derivativesMiconazoleKetoconazoleFluconazoleItraconazoleVoriconazolePosaconazoleNitroimidazolesMetronidazoleGlycopeptideAntibioticsVancomycinTeicoplaninTelavancin

PolyenesAmphotericin BNystatinMacrolidesErythromycinSpiramycinRoxithromycinClarithromycinAzithromycinGlycylcyclinesTigecyclineEchinocandinsCaspofunginAnidulafunginMicafunginStreptograminesQuinupristin/DalfopristinKetolidesTelithromycinOxazolidinonesLinezolidLipopeptidesDaptomycinEpoxidesFosfomycinPolymyxinsColistin(polymyxin E)

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Polymyxin B Ansamycins Rifampicin

http://www.lf3.cuni.cz/studium/materialy/infekce/en_atb.pdf http://www.springer.com/978-3-642-18401-7

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