Biaxin

[clarithromycin]

CONCENTRATION

(after 250 mg q12h)
Tissue Serum
Tissue Type (µg/g) (µg/mL)
Tonsil 1.6 0.8
Lung 8.8 1.7

Clarithromycin extended-release tablets provide extended absorption of clarithromycin from the gastrointestinal tract after oral administration. Relative to an equal total daily dose of immediate-release clarithromycin tablets, clarithromycin extended-release tablets provide lower and later steady-state peak plasma concentrations but equivalent 24-hour AUC’s for both clarithromycin and its microbiologically-active metabolite, 14-OH clarithromycin. While the extent of formation of 14-OH clarithromycin following administration of BIAXIN XL tablets (2 x 500 mg once daily) is not affected by food, administration under fasting conditions is associated with approximately 30% lower clarithromycin AUC relative to administration with food. Therefore, BIAXIN XL tablets should be taken with food.

Text Continues Below

---

In healthy human subjects, steady-state peak plasma clarithromycin concentrations of approximately 2 to 3 µg/mL were achieved about 5 to 8 hours after oral administration of 2 x 500 mg BIAXIN XL tablets once daily; for 14-OH clarithromycin, steady-state peak plasma concentrations of approximately 0.8 µg/mL were attained about 6 to 9 hours after dosing. Steady-state peak plasma clarithromycin concentrations of approximately 1 to 2 µg/mL were achieved about 5 to 6 hours after oral administration of a single 500 mg BIAXIN XL tablet once daily; for 14-OH clarithromycin, steady-state peak plasma concentrations of approximately 0.6 µg/mL were attained about 6 hours after dosing.

When 250 mg doses of clarithromycin as BIAXIN suspension were administered to fasting healthy adult subjects, peak plasma concentrations were attained around 3 hours after dosing. Steady-state peak plasma concentrations were attained in 2 to 3 days and were approximately 2 µg/mL for clarithromycin and 0.7 µg/mL for 14-OH clarithromycin when 250-mg doses of the clarithromycin suspension were administered every 12 hours. Elimination half-life of clarithromycin (3 to 4 hours) and that of 14-OH clarithromycin (5 to 7 hours) were similar to those observed at steady state following administration of equivalent doses of BIAXIN tablets.

Page:  << Prev | 1 | 2 | 3 | 4 | 5 | Next >>