ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
Antiinfectives for Systemic Use
Capsules. Capsule contains fluconazole 50 mg/100 mg/150 mg/200 mg.
PHARMACODYNAMICS. Fluconazole is triazole-derivative antifungal agent.
Fluconazole exerts its antifungal activity by altering cellular membranes
resulting in increased membrane permeability, leakage of essential elements
(e.g. amino acids, potassium), and impaired uptake of precursor molecules (e.g.
purine and pyrimidine precursors to DNA). The drugs inhibit cytochrome P-450
14-a-desmethylase in susceptible fungi, which leads to accumulation of C-14
methylated sterols (e.g. lanosterol) and decreased concentrations of ergosterol.
Fluconazole usually is fungistatic in action. Fluconazole is active against some
strains of Candida, including some strains of C. albicans, C. dubliniensis, C.
guilliermondii, C. kefyr, C. glabrata, C. parapsilosis, C. lusitaniae, and C.
tropicalis. Fluconazole has in vitro activity against some strains of
Cryptococcus neoformans. Fluconazole is active in vitro against some strains of
Blastomyces dermatitidis, Histoplasma capsulatum (including in immunosupressed
persons). PHARMACOKINETICS. The drug is rapidly and almost completely absorbed
from the Gl tract. Oral bioavailability of fluconazole exceeds 90%. Fluconazole
is only 11 -12% bound to plasma proteins. Concentrations attained in saliva,
sputum, nails, blister fluid, blister skin, and vaginal tissue are approximately
equal to plasma concentrations. CSF concentrations may be 50-94% of plasma
concentrations. The plasma elimination half-life of fluconazole is approximately
30 hours. Fluconazole is eliminated principally by renal excretion.
candidosis of mucosa membrane of mouth, faring, esophagus; non-invasive
candidosis of respiratory tract, candiduria; generalized candidosis, including
candidemia, disseminated candidiosis; uncomplicated and complicated vulvovaginal
candidiasis; criptococcosis, including meningitis caused byC. neoformans;
prophylaxis of fungal infections in cancer patients; dermatomycoses,
onichomycoses, invasive endemic mycoses.
Fluconazole is contraindicated in patients with known hypersensitivity to the
drug. Concomitant intake of drugs prolonging QT-interval (e.g. terphenadine,
From GIT: mild to moderate nausea, vomiting, abdominal pain, diarrhea, elevation
of hepatic enzymes. From CNS: headache, dizziness, fatigue, seizures. From blood
system: leucopenia, thrombocytopenia, neutropenia, agranulocytosis. Allergy:
skin rash, multiform ecssudative dermatitis, epidermal necrosis, anaphylactic
reactions. Other: renal damage, alopecia, dislipidemia, hypokaliemia.
Capsules should be taken as a whole, regardless of food Intake. 0000000000000
Vaginal candidosis: 150 mg single dose. For prophylaxis It can be administered
150 mg once a month. Oropharlngeal and esophageal candidosis: 200 mg at first
day and 100 mg in following days. Duration of course of therapy is 7-14 days.
Candidemia, dissiminated candidosis and other invasive variants of candidosis:
400 mg in first day and 200 mg during following days. Duration of course of
therapy depends on clinical situation. Prophylaxis of candidosis: dose range
50-400 mg per day depending on degree of risk. Cryptococcal meningitis and
cryptococcal infections of other localization: 400 mg in first day and 200 mg
during following days. Duration of therapy should be 10-12 weeks after
confirmation of sterility of CSF. Mycoses of skin: 150 mg in a week or 50 mg
daily. Course of therapy 2-4 weeks. Onichomycoses: 150 mg in a week. Duration of
cours of therapy up to the complete replacement of infected nail. Dosing in
children. Oropharingeal and esophageal candidosis: 6 mg/kg of body weight at
first day and 3 mg/kg of body weight in following days. Duration of course of
therapy is 7-14 days. Generalized candidosis and cryptococcosis: 12 mg/kg of
body weight at first day and 6 mg/kg of body weight in following days.
Prophylaxis of candidosis: dose range 3-12 mg/kg of body weight depending on
degree of risk. In patients with compromised renal function dose should be
corrected according to the instruction.
4 or 7 capsules with 50 mg of fluconazole in blister. One blister with leaflet
in carton box. 7 capsules with 100 mg of fluconazole in blister. One blister
with leaflet in carton box. 1 capsule with 150 mg of fluconazole in blister. One
blister with leaflet in carton box. 7 capsules with 200 mg of fluconazole in
blister. One blister with leaflet in carton box.