FLUCONAZOLE tablet

Χώρα: Ηνωμένες Πολιτείες

Γλώσσα: Αγγλικά

Πηγή: NLM (National Library of Medicine)

Δραστική ουσία:

FLUCONAZOLE (UNII: 8VZV102JFY) (FLUCONAZOLE - UNII:8VZV102JFY)

Διαθέσιμο από:

Direct Rx

INN (Διεθνής Όνομα):

FLUCONAZOLE

Σύνθεση:

FLUCONAZOLE 200 mg

Οδός χορήγησης:

ORAL

Τρόπος διάθεσης:

PRESCRIPTION DRUG

Θεραπευτικές ενδείξεις:

Fluconazole, the first of a new subclass of synthetic triazole antifungal agents, is available as tablets for oral administration. Fluconazole is designated chemically as 2,4-difluoro-α,α1-bis(1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol with a molecular formula of C13H12F2N6O and molecular weight 306.3. The structural formula is: Fluconazole USP is a white crystalline solid which is slightly soluble in water and saline. Fluconazole tablets USP contain 50, 100, 150, or 200 mg of fluconazole USP and the following inactive ingredients: dibasic calcium phosphate anhydrous, ferric oxide (iron oxide, red), magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate, and starch. Fluconazole tablets meets USP Dissolution Test 2. Close

Καθεστώς αδειοδότησης:

Abbreviated New Drug Application

Αρχείο Π.Χ.Π.

FLUCONAZOLE- FLUCONAZOLE TABLET
DIRECT RX
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FLUCONAZOLE
Pharmacokinetics and Metabolism
The pharmacokinetic properties of fluconazole are similar following
administration by the
intravenous or oral routes. In normal volunteers, the bioavailability
of orally administered
fluconazole is over 90% compared with intravenous administration.
Peak plasma concentrations (Cmax) in fasted normal volunteers occur
between 1 and 2
hours with a terminal plasma elimination half-life of approximately 30
hours (range: 20 to
50 hours) after oral administration.
In fasted normal volunteers, administration of a single oral 400 mg
dose of fluconazole
leads to a mean Cmax of 6.72 mcg/mL (range: 4.12 to 8.08 mcg/mL) and
after single
oral doses of 50 to 400 mg, fluconazole plasma concentrations and AUC
(area under
the plasma concentration-time curve) are dose proportional.
The Cmax and AUC data from a food-effect study involving
administration of fluconazole
tablets to healthy volunteers under fasting conditions and with a
high-fat meal indicated
that exposure to the drug is not affected by food. Therefore,
fluconazole may be taken
without regard to meals. (See DOSAGE AND ADMINISTRATION.)
Administration of a single oral 150 mg tablet of fluconazole to ten
lactating women
resulted in a mean Cmax of 2.61 mcg/mL (range: 1.57 to 3.65 mcg/mL).
Steady-state concentrations are reached within 5 to 10 days following
oral doses of 50
to 400 mg given once daily. Administration of a loading dose (on day
1) of twice the
usual daily dose results in plasma concentrations close to
steady-state by the second
day. The apparent volume of distribution of fluconazole approximates
that of total body
water. Plasma protein binding is low (11 to 12%). Following either
single- or multiple-oral
doses for up to 14 days, fluconazole penetrates into all body fluids
studied (see table
below). In normal volunteers, saliva concentrations of fluconazole
were equal to or
slightly greater than plasma concentrations regardless of dose, route,
or duration of
dosing.