Mechanism:
They bind on 30S ribosome and does the following actions :
- Inhibition of formation of initiation complex
- Inhibition of polysome formation
- Misreading of mRNA
DRUGS:
- Streptomycin
- Gentamicin
- Tobramycin
- Amikacin
- Neomycin
PHARMACOKINETICS:
- They are given parenterally, topically, orally[but not absorbed by GI tract].
- They are not metabolized in body.
- They are excreted unchanged in urine.
- They do not cross blood brain barrier.
USE:
- Active against all GRAM -VE organisms
- Active against GRAM +VE , if used in combination with BETA-LACTAMS or VANCOMYCIN.
- Streptomycin is used as 1st line drug in TB
Drug of choice in tularemia and plague - Amikacin is 2nd line drug in TB.
- Neomycin used orally for gut sterilization.Neomycin used topically for skin infections.
- Spectinomycin used in treating PENICILLINASE-PRODUCING Neisseria gonnorhoea [PPNG].
ADVERSE EFFECTS:
- OTOTOXICITY:
Amikacin, Neomycin causes hearing loss.
Gentamicin , Streptomycin causes vestibular toxicity. Tobramycin causes both. - NEPHROTOXICITY: Neomycin is most Nephrotoxic and not given I.V
Gentamycin is most toxic drug given as I.V Streptomycin is the least toxic. - NEURO-MUSCULAR BLOCKADE:
These drugs decrease the release of Ach as well as decrease the senstivity of post-synaptic membrane.
Hence should not be administered in case of Hypocalcemia, Respiratory depression and Neuromuscular blockers .
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