AMINOGLYCOSIDES

Streptomycin* Tobramycin* Kanamycin

* most commonly used

Gentamicin* Amikacin Neomycin(topical)

Antibacterial Spectrum
Bactericidal ( exclusive for aerobic G- bacteria ) M. Tuberculosis ( streptomycin & amikacin ) Not effective against G+ & anaerobes

AMINOGLYCOSIDES ( Cont. )
Pharmacokinetics Polycations ( highly charged )
Poorly absorbed from GIT ( parenteral or topical ) No distribution to most cells , including CNS Only 10 % bind of the drug bind to plasma protein No significant metabolic breakdown Excreted unchanged in urine ( glomerular filtration) Half- life 2-3 hrs

AMINOGLYCOSIDES ( Cont. )
Mechanism of action
Inhibit protein synthesis ( 30 s subunit ) Bactericidal Inhibition of cell wall synthesis increases their entrance into cells ( synergism ) eg.: Piperacillin or ceftazidime + gent. or tobra. Against P.aeruginosae

Clinical Use
T.B ( streptomycin, i.m ) P. Aeruginosa infections ( other than UTIs ) an aminoglycoside+ piperacillin or an aminoglycoside+ ceftazidime (p.aeruginosa UTIs, ciprofloxacin preferred) Brucellosis in combination with a tetracycline( severe cases) Topical Creams, ointments or solution for infected burns, wounds or skin lesions . Ear & eye drops and ointments

Adverse Effects
Ototoxicity & nephrotoxicity ( directly related to serum conc. ) Neuromuscular blockade ( very high dose )

Special problems with AGS use:

Narrow toxic- therapeutic ratio Monitoring of serum levels