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Suprax

Clinical Pharmacology
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CLINICAL PHARMACOLOGY

Suprax, given orally, is about 40%-50% absorbed whether administered with or without food; however, time to maximal absorption is increased approximately 0.8 hours when administered with food. The oral suspension produces average peak concentrations approximately 25%-50% higher than the tablets, when tested in normal adult volunteers. Two hundred and 400 mg doses of oral suspension produce average peak concentrations of 3 mcg/mL (range 1 to 4.5 mcg/mL) and 4.6 mcg/mL (range 1.9 to 7.7 mcg/mL), respectively, when tested in normal adult volunteers. The area under the time versus concentration curve is greater by approximately 10%-25% with the oral suspension than with the tablet after doses of 100 to 400 mg, when tested in normal adult volunteers. This increased absorption should be taken into consideration if the oral suspension is to be substituted for the tablet. Because of the lack of bioequivalence, tablets should not be substituted for oral suspension in the treatment of otitis media. (See DOSAGE AND ADMINISTRATION). Cross-over studies of tablet versus suspension have not been performed in children.

Peak serum concentrations occur between 2 and 6 hours following oral administration of 400 mg of Cefixime suspension. Peak serum concentrations occur between 2 and 5 hours following a single administration of 200 mg of suspension.

TABLE


Serum Levels of Cefixime after Administration of Tablets (mcg/mL)
DOSE 2h 4h 6h 8h 12h 24h
100 mg 0.3 0.8 1 0.7 0.4 0.2 0.02
200 mg 0.7 1.4 2 1.5 1 0.4 0.03
400 mg 1.2 2.5 3.5 2.7 1.7 0.6 0.04
Serum Levels of Cefixime after Administration of Oral Suspension (mcg/mL)
DOSE 1h 2h 4h 6h 8h 12h 24h
100 mg 0.7 1.1 1.3 0.9 0.6 0.2 0.02
200 mg 1.2 2.1 2.8 2 1.3 0.5 0.07
400 mg 1.8 3.3 4.4 3.3 2.2 0.8 0.07

Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours. In animal studies, it was noted that cefixime is also excreted in the bile in excess of 10% of the administered dose. Serum protein binding is concentration independent with a bound fraction of approximately 65%. In a multiple dose study conducted with a research formulation which is less bioavailable than the tablet or suspension, there was little accumulation of drug in serum or urine after dosing for 14 days. The serum half-life of cefixime in healthy subjects is independent of dosage form and averages 3-4 hours but may range up to 9 hours in some normal volunteers. Average AUCs at steady state in elderly patients are approximately 40% higher than average AUCs in other healthy adults.

Brand Name: Suprax
Generic Name: Cefixime
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