Flukonazol таб. 0.15 No. 1,2

General characteristics. Structure:

Acting substance: флуконазол - 50 mg or 150 mg; supportive applications.

Pharmacological properties:

Pharmacodynamics. Antifungal means of a class of triazolny connections. Flukonazol has the expressed antifungal effect, specifically blocks synthesis of fungal stirol. Has specific effect on the fungal enzymes dependent on P450 cytochrome. It is active to various strains of Candida spp. (including visceral candidiasis), Cryptococcus neoformans (including intracranial infections), Microsporum spp. and Trichophytum spp. Flukonazol is active also concerning causative agents of local mycoses: Blastomyces dermatitidis, Coccidioides immitis (including intracranial infections), Hystoplasma capsulatum.

Pharmacokinetics. After intake it is well soaked up in a digestive tract. Meal does not influence absorption of a flukonazol. The maximum concentration in a blood plasma is reached in 0,5 – 1,5 hours after intake. The drug elimination half-life makes the 30th hour of a blood plasma that allows to use drug of 1 times a day when carrying out a course of treatment flukonazoly and provides therapeutic effect at vaginal candidiasis after a single dose of drug. Concentration of active agent in a blood plasma is directly proportional to the accepted dose. 11-12% of a flukonazol contact blood proteins. At a daily single dose of a flukonazol for 4-5 days stable concentration in a blood plasma is reached at 90% of patients. At introduction in the 1st day of treatment shock (double daily) a dose the above-stated effect is reached by 2nd day of treatment.
Flukonazol well gets into all liquids of an organism. In cerebrospinal fluid concentration of a flukonazol reaches 80% of the level of its concentration in a blood plasma.
From an organism флуконазол 80% - in not changed look are removed with urine, and. The clearance of a flukonazol is directly proportional to clearance of creatinine

Indications to use:

The infections caused by kandida, including generalized candidiasis including a kandidemiya, the disseminated candidiasis and other forms of an invasive candidosis infection (internal, an endocardium, eyes, respiratory and uric ways); candidiasis of mucous membranes, including oral cavities and drinks, gullet; noninvasive bronchopulmonary infections, kandiduriya; the skin mucous and chronic atrophic candidiasis of a mucous membrane of an oral cavity (caused by carrying dentures); genital candidiasis - vaginal candidiasis (acute or recurrent), prevention of a recurrence of vaginal candidiasis (with a frequency of emergence of 3 times and more in a year), and also a candidosis balanitis.
Flukonazol apply at cryptococcal infections, dermatomycoses, including mycoses of feet, trunks, inguinal area, herpeses; onychomycosis; deep local mycoses, including a coccidioidomycosis, a paracoccidioidomycosis, a sporotrichosis and histoplasmosis, and also for prevention of fungal infections at patients who receive cytostatic or radiation therapy.

Route of administration and doses:

Inside, by oral administration. Depending on character and course of a fungal infection the daily dose can make from 50 mg to 400 mg. Duration of treatment depends on clinical and mycologic effect. The daily dose for children should not exceed a dose for adults. Flukonazol apply daily 1 time a day.
At a kandidemiya, the disseminated candidiasis and other invasive candidosis infections the dose, as a rule, makes 400 mg for 1 days, and then to 200 mg a day. Depending on clinical effect it is possible to continue therapy and to raise a dose to 400 mg/days. For treatment of generalized candidiasis the dose of a flukonazol for children is more senior than 1 year makes 6-12 mg/kg a day depending on a condition of a disease.
At oropharyngeal candidiasis the adult, as a rule, appoint 50-100 mg of a flukonazol of 1 times a day for 7-14 days. At patients with the expressed immunity oppression treatment is continued if necessary during longer time. At the atrophic candidiasis of a mucous membrane of an oral cavity caused by use of dentures, drug, as a rule, appoint in a dose 50 mg of 1 times a day within 14 days in a complex with local antiseptic agents for processing of a prosthesis. At other candidosis infections of mucous membranes (except for genital candidiasis, for example – izofagit, noninvasive bronchopulmonary infections, a kandiduriya, candidiasis of skin and mucous membranes), the effective daily dose usually makes 50-100 mg lasting treatment of 14-30 days. For prevention of a recurrence of oropharyngeal candidiasis at patients with AIDS after end of a course of primary therapy флуконазол appoint in a dose 150 mg once a week. At candidiasis of mucous membranes the recommended dose of a flukonazol for children is more senior than 1 year of 3 mg/kg a day. In the first day it is possible to appoint a shock dose of 6 mg/kg for bystry achievement of stable equilibrium concentration.
At vaginal candidiasis adults accept флуконазол once 150 mg inside. For decrease in frequency of a recurrence of a disease drug accept in a dose 150 mg once a month. Duration of therapy is determined individually; it varies from 4 to 12 months. In certain cases the frequency of receptions is increased. At the balanitis caused by Candida флуконазол appoint inside once in a dose 150 mg.
For prevention of candidiasis the dose recommended for adults makes 50 - 400 mg of 1 times a day depending on a risk degree of development of a fungal infection. With high risk of a generalized infection, for example, at patients with the estimated expressed or long neutropenia, the recommended dose makes 400 mg of 1 times a day. Flukonazol appoint some days before alleged emergence of a neutropenia; after increase in quantity of neutrocytes more than 1000 in 1 mm3 treatment is continued within 7 days. To children 1 years флуконазол are more senior appoint 3-12 mg/kg a day depending on a condition of the induced neutropenia. At cryptococcal infections in the 1st day usually appoint 400 mg, and then continue treatment in a dose of 200 - 400 mg of 1 times a day. Duration of treatment of cryptococcal infections depends on achievement of clinical and mycologic effect. For treatment of a cryptococcal infection the recommended dose of a flukonazol for children is more senior than 1 year makes 6-12 mg/kg a day depending on a condition of a disease.
At skin infections, including mycoses of feet, smooth skin, inguinal area and candidosis infections the dose recommended for adults makes 150 mg once a week or 50 mg of 1 times a day. Therapy duration usually 2-4 weeks, however at mycosis of legs can be required more long treatment (up to 6 weeks). At herpes the recommended dose makes 300 mg for 2 weeks once a week; some patients have need for reception of thirds of a dose of a flukonazol - 300 mg while sufficient the single dose of 300 — 400 mg of drug in certain cases is. The alternative scheme of treatment is use of drug on 50 mg of 1 times a day within 2-4 weeks. At an onychomycosis (tinea unguium) the dose recommended for adults - 150 mg once a week. Treatment should be continued before full replacement of the affected nail healthy. Repeated growth of nails on fingers of hands and legs requires usually 3-6 and 6-12 months, respectively, however the growth rate of nails can vary in wide borders at different people, and also depending on age. At deep local mycosis use of drug for adults in a dose of 200 - 400 mg/days can be necessary long (up to 2 years). Duration of therapy is determined individually; usually it makes 11 - 24 months at a coccidioidomycosis, 2-17 months at a paracoccidioidomycosis, 1-16 months - at a sporotrichosis and 3-17 months - at histoplasmosis.
For treatment of people of advanced age in the absence of symptoms of a renal failure drug is used in a usual dose. For patients with a renal failure (clearance of creatinine of 11 - 50 ml/min.) an initial shock dose of 50 - 400 mg, the daily dose of a flukonazol for the subsequent introductions is reduced twice. The patient residing on dialysis флуконазол enter after each session of dialysis.

Features of use:

Patients at whom during treatment flukonazoly indicators of function of a liver are broken have to is under observation of the doctor. With the advent of clinical signs of damage of a liver флуконазол it is necessary to cancel.
Patients with AIDS are more inclined to development of heavy skin reactions at use of many drugs. With emergence in the patient receiving treatment concerning a superficial fungal infection, a rash that, perhaps, is caused by use of a flukonazol drug should be cancelled. With the advent of rashes at patients with invasive / system fungal infections it is necessary to watch their state surely, at development of defeats of polymorphic system флуконазол cancel.
Flukonazol define in breast milk in the same concentration, as in blood therefore its use during feeding by breast milk is not recommended.

Side effects:

Nausea, pain in a stomach, diarrhea, a meteorism, an enanthesis, a headache, anaphylactic reactions, hepatotoxic effects are possible.

Interaction with other medicines:

The concomitant use of warfarin and flukonazol leads to increase in a prothrombin time; a flukonazola and пероральньх gipoglikemiziruyushchy drugs of group of derivatives of sulphonylurea (Chlorproramidum, Glibenclamidum, a glipizid and Tolbutamidum) - to increase in the period of their semi-removal (it is necessary to consider a possibility of development of a hypoglycemia); a flukonazol and Phenytoinum - before clinically significant increase in concentration of Phenytoinum (monitoring of concentration and selection of a dose is necessary). Reusable use of a hydrochlorothiazide increases concentration of a flukonazol in a blood plasma, however change of the mode of dosing of a flukonazol, as a rule, is not required.
Flukonazol in a dose of 50 — 200 mg has no significant effect on efficiency of the combined contraceptives for oral administration. Simultaneous use of a flukonazol and rifampicin led to decrease in AUC of a curve (concentration/time) for 25% and duration of an elimination half-life of a flukonazol for 20%. The patients using the given combination of drugs need to consider expediency of increase in a dose of a flukonazol. During use of a flukonazol it is recommended to control concentration of cyclosporine in blood.
Considering developing of the expressed arrhythmia caused by lengthening of an interval of Q-T at patients who received azolny antifungal means in a combination with terfenadiny, a concomitant use of a flukonazol in a dose of 400 mg/days and above with terfenadiny it is contraindicated. Treatment flukonazoly in a dose is lower than 400 mg/days з terfenadiny it is necessary to carry out to combinations under strict observation of the doctor. At simultaneous use of a flukonazol and tsizaprid side reactions from cardiovascular system are possible, including paroxysms of gastric tachycardia.
It is necessary to watch a condition of patients which appoint a combination of a flukonazol and a zidovudine for the purpose of early identification of collateral symptoms of a zidovudine which AUC in this case considerably increases.
Use of a flukonazol by patients who at the same time receive цизаприд астемизол, рифабутин, такролимус or other medicines which are metabolized by system of P450 cytochrome can be followed by increase in concentration of these drugs in blood. The concomitant use of Cimetidinum or antacids has no clinically significant influence on absorption of a flukonazol.

Contraindications:

Hypersensitivity to a flukonazol or azolny connections, close to it on chemical structure; simultaneous use of a terfenadin by patients who receive therapy flukonazoly in a dose of 400 mg/days or bigger; pregnancy, a lactation, age till 1 year.
It is necessary to avoid use of a flukonazol for treatment of pregnant women, except for hard cases and potentially life-threatening fungal infections when the foreseen advantage for the woman exceeds potential risk for a fruit.

Overdose:

It is shown by hallucinations and paranoid behavior. Treatment - symptomatic (including a maintenance therapy and a gastric lavage). Flukonazol is brought generally with urine therefore the artificial diuresis can accelerate drug removal. The session of a hemodialysis 3 hour long reduces the level of a flukonazol in a blood plasma approximately by 50%.

Storage conditions:

To store in the place protected from light at a temperature not over 30 to °s.khranit in the place, unavailable to children!

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets with a dosage of 50 mg or on 2 tablets with a dosage of 150 mg in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.