PHARMACOLOGY

Pharmacotherapeutic Group:Antifungal Agent

Pharmacodynamic Properties:Fluconazole interacts with an enzyme 14 α demethylase necessary to convert lanosterol to ergosterol. Ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular components and thus leading to cell death.

Pharmacokinetic Properties:

Absorption: Well absorbed after oral administration, Peak plasma concentrations after 1-2 hr(oral), may be increased  with multiple dosing

Distribution: Widely distributed. Protein binding: 12%

Excretion: Via urine (80% as unchanged , 11% as metabolites), Elimination half life: 30 hr, increased in renal impairment.

 INDICATIONS

Superficial mucosal candidiasis, Vaginal Candidiasis, Oropharyngeal and Esophageal Candidiasis, Pityriasis Versicolor, Cutaneous candidiasis, Systemic Candidiasis, Cryptococcal infections, prophylaxis of fungal infections in immunocompromised patients

 DOSAGE & ADMINISTRATION

Superficial mucosal candidiasis: 50-100mg daily for 7-14 days; Vaginal candidiasis: 150mg single dose; Cutaneous candidiasis: 50mg daily for up to 6 weeks

 ADVERSE DRUG REACTIONS

Nausea, abdominal pain, vomiting, diarrhoea, flatulence, elevated liver function values, headache, rashes, exfoliative dermatitis.

 PRECAUTIONS

Pregnancy, lactation, renal or hepatic impairment, may prolong QT interval

 DRUG INTERACTIONS

Decreased absorption with concurrent sucralfate, magnesium-aluminum antacids, calcium, iron, zinc and multivitamins. Increased methotrexate and caffeine levels when taken concurrently with ciprofloxacin.  Concurrent use with corticosteroids may increase tendon rupture.

 CONTRAINDICATIONS

Hypersensitivity, co administration of other drugs known to prolong the QT interval and which are metabolized by enzyme CYP3A4 such as cisapride, astemizole, erythromycin, pimozide and quinidine.

 PRESENTATION

FAZOLE: Each box contains 20 Blister of 1 Capsule per strips