Aminoglycosdes Flashcards
Source
Natural and synthetic
Chemistry
Polar (highly ionized and poorly lipid soluble)
Absorption
poorly absorbed orally
They may be also given topically as skin ointments,
systemic infections
They must be given IM or IV
treatment of GIT infections and bowel sterilization.
Oral
treatment of respiratory tract infections,
inhalation
treatment of meningitis
intra-thecally
Streptomycin given
Intra-pleural
→ Intra-peritoneum
Distribution
1.Cannot pass BBB even in meningitis
2.Pass placental barrier and may induce fetal deafness.
3 .Minimal plasma protein binding except streptomycin.
4. Concentrated in renal cortex
5. CN8 → deafness “Imbalance (vertigo)
Execrations
excreted unchanged in unine
Action on bacteria:
Bactericidal (but bacteriostatic on T.B. bacilli)
Mechanism of Action
1.Aminoglycosides diffuse into bacterial cell by an active oxygen-dependent
transport (They are inactive against anaerobes)
2. They bind to 30 S ribosomal subunit leading to inhibition of the codon- anticodon
recognition
Adverse effects
- Ototoxicity: given frequently for long periods and with other ototoxic drugs as aspirin
- Nephrotoxicity
- Skeletal muscle weakness due to inhibition of acetylcholine release from
presynaptic area and decreased sensitivity of Nm-receptors in NMJ (curare-like action).
Dosage readjustment
Normal dose / serum creatinine
Interval readjusment
Creatinine serum x 8