Fluconazole

Chemical name

альфа-(2,4-Дифторфенил)- альфа-(1Н-1,2,4-триазол-1-��лметил)-1H-1,2,4-триазол-1 -этанол

Gross

C13-H12-F2-N6-O

Characteristics

Crystalline powder white, or nearly white, odourless, with a characteristic taste, it is difficult soluble in water and alcohol izopropilovom, sparingly soluble in ethanol and chloroform, soluble in acetone and easily soluble in methanol (injection isoosmotichen).

Of drugs

The drugs-antimycotic. Does a zitohrom P450-zawisimah enzymes and vsokoseleguo ingibiruet sterolov synthesis in cellular membranes mushrooms. Effective in infections caused by fungi of Candida spp. , Cryptococcus neoformans, Microsporum spp. , Trichophyton spp. , As well as infections caused by the disease Blastomyces dermatitidis, Coccidioides immitis and Histoplasma Capsulatum.horosho drawn from the blood. Bioavailability of 90%, eating does not affect the removals. Linking plasma protein-11-12%. C_max achieved through 0.5-1.5 h after administration. Equilibrium concentration to 4-5 day treatment (to 1 per day). It penetrates into all body fluids organism. Write mainly kidneys, 80% in an unmodified form. Ground proportional klirensu creatinine. T_1/2 about 30 hours When in / with the introduction of a similar pharmacokinetic characteristics.

Indications

Kriptokokkoz : chriptokokkovi meningitis, infections of the skin and light; Prevention of the recurrence of cryptococcosis in AIDS patients; Generalizovanny candidiasis : candidemia, disseminated candidiasis and other forms of invasive infections kandidozhnykh (defeated edge, endocarda, eyes, respiratory and urinary tract); Candidiasis mucous membranes of the oral cavity and pharynx, oesophagus, bronholegocny candidiasis, candiduria, kandidozy skin and mucous membranes, atroficski candidiasis of the oral cavity (associated with carrying dentures), the prevention of relapse orofaringealnogo candidiasis in patients with AIDS; genital candidiasis : vaginal (acute or recurrent), including relapse prevention, kandidozny balanit; prevention of fungal infections in malignant tumors; mikozy skin (feet, body shapes field), otrubevidnyi zoster, onihomikoz, skin candidiasis; deep endemic mikozy (koktsidiomikoz, parakoktsidiomikoz, sporotrihoz, gistoplazmoz) in patients with nenarushennym immunity.

Pregnancy and lactation

When pregnancy is possible only when life-threatening severe infections, if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breast-feeding (flukonazola concentration in breast milk with plasma).

Contraindications

Гиперчувствительност ь (incl. other derivative azola), simultaneous terfenadina or astemizola, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : headache, Sudorogi.so the circulatory system and blood (blood, gemostaz) : lakopenia, anaemia, a change in the blood (in patients with weakened immune). For part of the intestine : nausea, pain in the abdomen, diarrhoea, flatulence, the liver, Gepatotoksicnosti.so the urogenital system : violation of the Pocek.so skin : rashes, fatigue Stevens-Johnson, toxic It'sa Nekroliz.prochie : alopecia, anaphylacticskie reaction.

Patient interaction

Increases T_1/2 of plasma gipoglikemicakih oral drugs (derivatives sulfonylureas), the concentration fenitoina, rifabutin, alone in the blood. When coupled with the admission varfarinom increased protrombinovoe time (12%), with rifampitsinom reduces AUC (25%) and T_1/2 of plasma (20%), with cizapridom-increased risk of cardiovascular violations, including Evolution paroxizmalna ventricular tachycardia.

Overdosing

Symptoms : nausea, vomiting, diarrhoea, Sudorogi.lechenie : washing stomach, big diurez, Hepatology, symptomatic therapy.

Precautions

Be wary appoint patients with impaired kidney (with Cl creatinine less than 50 ml / min dose should be adjusted), in places with immunosuppressed (after birth, AIDS, etc.). There is a need to closely monitor the blood and the liver. When signs of hepatotoxicity, rashes, bulleznah changes mnogoformna eritema therapy should be abolished.

Dosing and Administration

Inside, in / 386/1989 Adults with kriptokokkovh infections, 200-400 mg / day; Generalizovannom to 4-8-400 mg, followed by 200 mg per day; Orofaringealnom at 4-8, 50 mg / day for 7-14 days; Waginalnom at 4-8, one 150 mg; Mikozah in on the 150 mg once a week. Children 4-8 in the mucous membranes, 3-6 mg / kg / day, with generalizovannom 4-8, 6-12 mg / kg / day, for the prevention of fungal infections, 3-12 mg / kg / sut.

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