Drug-Excipient Compatibility

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Cefixime, sold under the brand name 

Suprax among others, is an antibiotic medication


used to treat a number of bacterial infections.[4] These infections include otitis media, strep
throat, pneumonia, urinary tract infections, gonorrhea, and Lyme disease.[4] For gonorrhea
typically only one dose is required.[6] In the United States it is a second-line treatment
to ceftriaxone for gonorrhea.[4] It is taken by mouth.[4]
Cefixime

Clinical data

Trade names Suprax, others[1]

AHFS/Drugs.com Monograph

MedlinePlus a690007

License data  US DailyMed: Cefixime

Routes of By mouth (capsule, suspension,


administration or tablet)[2]

ATC code  J01DD08 (WHO)

Legal status

Legal status  UK: POM (Prescription


only) [3]
 US: ℞-only
 In general: ℞ (Prescription
only)

Pharmacokinetic data

Bioavailability 30 to 50%[4]

Protein binding Approximately 60%

Elimination half- Variable
life Average 3 to 4 hours

Excretion Kidney and biliary

Chemical and physical data

Formula C16H15N5O7S2

Molar mass 453.44 g·mol−1


Human Pharmacokinetics:

Absorption:

SUPRAX (cefixime), given orally, is about 40% to 50% absorbed.

In adults a single 200 mg tablet of SUPRAX produces an average peak serum concentration of

approximately 2 µg/mL (range 1 to 4 µg/mL); a single 400 mg tablet produces an average

concentration of approximately 3.5 µg/mL (range 1.3 to 7.7 µg/mL). The oral suspension, in

adults, following 200 mg and 400 mg doses produces average concentrations of 2.8 µg/mL

(range 1 to 4.5 µg/mL) and 4.4 µg/mL (range 1.9 to 7.7 µg/mL), respectively. The area under the

time versus concentration curve is greater by approximately 26.4% with the oral suspension than

with the tablet after doses of 400 mg. This increased absorption should be taken into

consideration if the oral suspension is to be substituted for the tablet.

Peak serum concentrations occur between 2 and 6 hours following oral administration of a single

200 mg tablet, a single 400 mg tablet or 400 mg suspension of SUPRAX. Peak serum

concentrations occur between 2 and 5 hours following a single administration of 200 mg

suspension. See Tables 7 and 8.

Table 7 - Serum Levels of Cefixime in Adults after Administration of Tablets (µg/mL)

tablets

Table 8 - Serum Levels of Cefixime in Adults after Administration of Oral Suspension

The serum half-life of cefixime in healthy subjects is independent of dosage form and averaged

3 to 4 hours but may range up to 9 hours in some normal volunteers.


Metabolism:

There is no evidence of metabolism of cefixime in vivo.

Excretion:

Cefixime is excreted by renal and biliary mechanisms.

The urinary recoveries of orally administered 200 mg and 400 mg doses of cefixime in

12 healthy men are presented in Table 9. Over a 24 hour period, approximately 20% and 16% of

a 200 mg and 400 mg dose of cefixime, respectively was excreted in the urine. An additional

10% or more was recovered from bile.

Table 9 - Mean urinary excretion of cefixime after 200 and 400 mg dose in 12 healthy men

Distribution and Accumulation:

Cefixime appears to be widely distributed, however, adequate tissue concentration data relating

to tablet and suspension are not available.

Serum protein binding is concentration independent with a bound fraction of approximately

65%. Multiple dose studies conducted with 200 mg or 400 mg tablets in normal volunteers

showed there was little or no accumulation of drug in serum or urine after dosing for 14 days.

Adequate data on cerebrospinal fluid (CSF) levels of cefixime are not available.

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