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Aminoglycosides

They include streptomycin, gentamicin, tobramycin,


amikacin, nitelmicin, neomycin, kanamycin, Paromomycin,
Viomycin. They are water soluble and are more active in alkaline
medium.

Mechanism:

Bactericidal by irreversible inhibition of protein synthesis.


They are bound to receptors on 30S subunits of bacterial
ribosomes
Resistance may be due to
1. Decreased Uptake
2. Altered Receptor
3. Or Produce Enzymes Which Inactivate The Drug.

Pharmacokinetics: They are not or poorly absorbed from gut, so


given by injection and used orally for local effect in gut. 10% is bound
to proteins. They are highly polar, don't enter C.N.S or eye (so in
meningitis they are given Intrathecal). High level in renal cortex and
inner ear. Excreted by glomeruli, so dose is adjusted in renal
impairment. They pass through placenta.

Adverse effects:

1. Ototoxicity &Nephrotoxicity.
2. Neuromuscular blocking effect after intrapleural or
intraperitoneal application due to decreased Ach release or
decreased sensitivity of post-synaptic sites.
3. Contact dermatitis may follow topical neomycin application.

Streptomycin is bactericidal on gram ve cocci but bacteriostatic in


T.B.

Used in T.B., plague, brucellosis, tularemia, endocarditis (with


penicillin), given I.M 1g/day.

Orally for intestinal infection.


Gentamicin: Bactericidal on many gram ve bacteria and some gram
+ve It is given I.M or I.V 3-5mg/kg/day in divided doses. It may be
combined with Carbenicillin or ticarcillin.

Used in UT infections, severe infections (sepsis, pneumonia) caused


by gram ve organisms, meningitis (given Intrathecal), endocarditis
(combined with penicillin G). Topically for infected burns, wounds, skin
lesion and prevention of catheter infection.

Toxicity: nephrotoxicity and ototoxicity.

Amikacin: as gentamicin, but has broad activity as it is resistant to


aminoglycoside inactivating enzymes, dose 15 mg/kg/day divided.

Neomycin: Is extremely toxic for systemic use so used topically for


skin infection by staphylococci and many gram ve bacilli and orally
for local action on gut.

Used in acute intestinal infections, to sterilize bowel before surgery, in


treatment of hyperlipidemia.

Side effects: Malabsorption syndrome, superinfection and contact


dermatitis.