Bicrolid Mechanism of Action

Pharmacology: BICROLID contains Clarithromycin a semi-synthetic macrolide antibiotic. It exerts its anti-bacterial action by binding to the 50S ribosomal subunit of susceptible organism and inhibiting protein synthesis.
BICROLID is rapidly absorbed from the gastro-intestinal tract after oral administration.
Food does not affect the extent of bioavailability, therefore BICROLID may be given concomitantly with meals.
In fasting healthy human subjects, peak serum concentrations were attained within 2 hours after oral dosing.
Peak serum concentrations were approximately 1 mcg/ml with a 250 mg dose administered every 12 hours and 2-3 mcg/ml with a 500 mg dose administered every 12 hours.
The elimination half-life was about 3 to 4 hours with 250 mg administered every 12 hours but increased to 5 to 7 hours with 500 mg administered every 12 hours.
After a 250 mg dose every 12 hours, approximately 20% of the dose is excreted in the urine as the unchanged parent drug. After a 500 mg dose every 12 hours, the urinary excretion of Clarithromycin is somewhat greater, approximately 30%.
The major metabolite found in urine is 14-OH Clarithromycin which also has clinically significant anti-microbial activity.
Clarithromycin and the 14-OH Clarithromycin metabolite is distributed readily into body tissues and fluids. No data is available on CSF (Cerebro Spinal Fluid) penetration.
BICROLID is active in vitro against a variety of aerobic and anaerobic Gram-positive and Gram-negative organisms.
Against Haemophilus influenzae, 14-OH Clarithromycin is twice as active as the parent compound.
Beta-lactamase production should have no effect on Clarithromycin activity.