Flukonazol of 0,2%

General characteristics. Structure:

Active ingredient: 2 g of a flukonazol.

Excipients: sodium chloride, water for injections.

Medicine with active antifungal action.

Pharmacological properties:

Pharmacodynamics. Flukonazol has the expressed antifungal effect, specifically affects the fungal enzymes dependent on P 450 cytochrome, inhibits synthesis of sterol in cells of mushrooms. It is highly active concerning Candida spp., Microsporum spp., Trichophyton spp., Cryptococcus neoformans, Blastomyces dermatitidis, Coccidioides immitis, Histoplasma capsulatum.

Pharmacokinetics. Flukonazol well gets into all biological liquids, into bodies and body tissues. Concentration of drug in saliva and a phlegm are similar to its levels in plasma. The peak of concentration of a flukonazol in blood serum is reached right after intravenous administration. The elimination half-life of drug makes about 30 hours.

Concentration in plasma is in directly proportional dependence on the entered dose. 90% the level of equilibrium concentration are reached by 4 - 5 day of treatment by drug at introduction of 1 times a day. Linkng with proteins of plasma - 11-12%. At patients with fungal meningitis the maintenance of a flukonazol in cerebrospinal fluid reaches 80% of level it in plasma.

In a corneous layer, epidermis, a derma, stalemate liquid the high concentration exceeding serumal are reached. Flukonazol collects and is long remains in a corneous layer. Flukonazol is brought generally by kidneys; about 80% of the entered dose are removed with urine in not changed look. The clearance of a flukonazol is proportional to clearance of creatinine.

Indications to use:

Flukonazol for infusions apply to treatment of many fungal infections: a cryptococcosis, including cryptococcal meningitis; system candidiasis, including a kandidemiya, the disseminated candidiasis and other forms of invasive candidosis infections (an infection of a peritoneum, an endocardium, eyes, respiratory and uric ways); candidiases of mucous membranes (an oral cavity, a throat, a gullet, noninvasive bronchopulmonary candidiases, a kandiduriya, the atrophic candidiasis of an oral cavity connected with carrying dentures); genital candidiasis: vaginal candidiasis, acute and chronic recurrent, balanitis; skin mycoses, including mycoses of feet, bodies, inguinal area; chromophytosis; onychomycosis; deep local mycoses; prevention of fungal infections at patients with malignant new growths at treatment by cytostatics or performing radiation therapy, or at other states connected with immunity suppression.

Route of administration and doses:

Flukonazol apply intravenously kapelno with a speed no more than 10 ml/min. once a day. At the drive from intravenous administration on reception of tablets and vice versa there is no need to change a daily dose.        

Solution of a flukonazol for infusions is compatible to the following solvents: 20% glucose solution, Ringer's solution, Hartman's solution, solution of chloride potassium in glucose, solution of sodium of bicarbonate of 4,2%, аминофузин, isotonic solution of sodium of chloride.        

At vaginal candidiasis, a candidosis balanitis appoint 100 - 200 mg a day; often after single administration of drug there occurs recovery. At other forms of candidiasis of mucous membranes 50 - 100 mg once a day within 14-30 days are recommended.        

At system candidiasis and cryptococcal infections, including meningitis, in the first day of 400 mg, then 200 - 400 mg once a day depending on weight of an infection; duration of therapy depends on clinical performance; usually the course of treatment at cryptococcal meningitis lasts 6-8 weeks. For prevention of a recurrence of cryptococcal meningitis at patients with AIDS, after end of a full course of primary therapy, drug is appointed to the patient in doses by not less than 200 mg/days during the long period.       

At skin mycoses the recommended dose makes 150-200 mg once a week or    50 mg once a day, therapy duration usually 2-4 weeks. However at mycoses of feet treatment up to 6 weeks can be required. At an onychomycosis the recommended dose makes 150 - 200 mg once a week; treatment should be carried out before full replacement of the affected nail healthy.       

Prevention of fungal infections at patients with malignant new growths - 100 mg every other day, so far the patient is in group of the increased risk, owing to beam or chemotherapy. Patients of advanced age in the absence of renal failures should adhere to the usual mode of a drug dosing.       

At a renal failure the dose of a flukonazol at its single dose does not change. At repeated purpose of drug patients with an impaired renal function should enter at first a shock dose from 50 mg to 400 mg. If the clearance of creatinine (CC) makes more than 50 ml/min., the usual dose of drug (100% of the recommended dose) is applied.         

At KK from 11 to 50 ml/min. the dose equal of 50% recommended is applied. The patient who is regularly on a hemodialysis, one dose of drug is applied after each session of a hemodialysis. To children is more senior than one year at normal function of kidneys флуконазол enter daily 1 times/days at the rate of 1-3 mg/kg/days (at candidiasis of mucous membranes) and 3-12 mg/kg/days (at system candidiases or cryptococcoses) depending on disease severity.   

Children with a renal failure should reduce a daily dose of drug (in the same proportional dependence, as the adult), according to degree of manifestation of a renal failure.       

 At newborns флуконазол it is removed slowly. In the first 2 weeks of life drug is appointed in the same dose (in mg/kg), as to children of more advanced age, but with an interval of 72 hours. To children at the age of 2-4 weeks the same dose is entered with an interval of 48 hours.

Features of use:

At detection of increase in blood of level of liver enzymes it is necessary to define expediency of further use of drug depending on a ratio of the expected medical effect and risk of continuation of treatment. At emergence of skin rash use of drug should be stopped.

Side effects:

Flukonazol, as a rule, is well had. Nausea, diarrhea, an abdominal pain, skin rash, a headache are possible.

Interaction with other medicines:

Anticoagulants: At the patients receiving флуконазол and coumarinic anticoagulants, careful control of a prothrombin time as it can increase is necessary.  

Sulphonylurea drugs: Flukonazol at a concomitant use, can extend an elimination half-life of peroral drugs – sulphonylurea derivatives therefore at their combined use, it is necessary to consider a possibility of development of a hypoglycemia.       

Phenytoinum: Simultaneous use of a flukonazol and Phenytoinum can be followed by increase in concentration of Phenytoinum in clinically significant degree that demands decrease in its dose.

Rifampicin: At a concomitant use of rifampicin and a flukonazol the maximum concentration and an elimination half-life of a flukonazol therefore in need of the combined use, it is necessary to increase a dose of a flukonazol decreases.                                              

Rifabutin: Combined use of a flukonazol and rifabutin is followed by increase in serumal levels of the last, development of a uveitis is possible.                                  

Cyclosporine: At combined use of a flukonazol and cyclosporine it is recommended to control concentration of the last in blood as it can increase. Terfenadin and астемизол: Considering emergence serious, life-threatening, arrhythmias at the patients receiving azolny antifungal means in combination with terfenadiny or with astemizoly joint reception with the specified drugs is contraindicated.           

Tsizaprid: At simultaneous use of a flukonazol and tsizaprid cases of undesirable reactions from heart are described, including paroxysms of ventricular tachycardia. The concomitant use is contraindicated.                                                                                          

Zidovudine: At the combined use increase in concentration of a zidovudine in a blood plasma is possible. The patients receiving such combination should be observed for the purpose of identification of side effects of a zidovudine.

Theophylline: Reception of a flukonazol leads to decrease in average speed of clearance of creatinine from a blood plasma, therefore the risk of development of toxic effect of theophylline and overdose increases. Though no specific manifestations of pharmaceutical incompatibility are described, mixing of solution of a flukonazol with solutions of other drugs before infusion is not recommended.

At use of a flukonazol for the patients who are at the same time receiving other drugs which are metabolized system of P450 cytochrome it is necessary to be careful.

Contraindications:

Hypersensitivity to a flukonazol or relatives on structure to triazolny connections. Children up to 16 years, except for severe or life-threatening forms of infections when the estimated advantage exceeds possible risk for the patient.

Overdose:

At overdose of drug can be rather symptomatic treatment (using auxiliary actions and a gastric lavage if it is necessary). After the 3-hour session of a hemodialysis concentration of a flukonazol in plasma decreases approximately by 50%.

Storage conditions:

List B. In the dry, protected from light place at a temperature from +5 °C to + 25 °C. Drug freezing is not allowed. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 50 ml and 100 ml in polymeric containers.