MACROLIDE
MECHANISM : Macrolide attaches to 50 s ribosome and block the translocation of peptide chain containing T RNA from A site to P site .
One must know about the TRANSLATION process happening in the bacterial cell to understand the above mechanism .
DRUGS :
- Erythromycin
- Roxithromycin
- Clarithromycin
- Azithromycin
- Tacrolimus ( it is an immunosuppresant as well )
- Spiramycin
PHARMACOKINETICS:
- All drugs are taken orally except spiramycin .
- Metabolised in liver
- These drugs are excreted in bile except Clarithromycin in urine.
- Do not cross blood brain barrier
- Crosses placenta
USES:
MACROLIDES ARE BROAD SPECTRUM ANTIBIOTICS.
They are the drug of choices for the following:
- C - Chancroid by Haemophilus ducreyi , Corneybacterium , Campylobacter
- L - Legionella
- A - Atypical pneumonia
- W- Whooping cough by Bordetella pertusis.
Mnemonic to remember the uses is CLAW .
Azithromycin has extended spectrum of uses :
- H.influenza
- Nesseria gonnorrhoea
- Urogenital infection by Chlamydia
Clarithromycin used as prophylaxis and treatment of Mycobacterium avium and H.pylori
Spiramycin is drug of choice for toxoplasmosis in PREGNANCY.
ADVERSE EFFECTS :
- ERYTHROMYCIN causes diarrhoea due to Motilin Stimulation.
- Erythromycin causes ACUTE CHOLESTATIC HEPATITIS
- Erythromycin , Clarithromycin , Roxithromycin causes microsomal enzyme inhibition .
ALL THESE ADVERSE EFFECTS ARE ABSENT IN AZITHROMYCIN .
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