Mycomax capsules 150mg, 3pcs

Composition

1 capsule contains:

Active ingredient:

fluconazole 150 mg;

Auxiliary substances:

lactose monohydrate;

pregelatinated starch;

colloidal silicon dioxide;

magnesium stearate;

sodium lauryl sulfate.

Pharmacological action

of MYCOMAX – antifungal.

Pharmacodynamics

Fluconazole, a member of the class of triazole antifungal agents, is a powerful selective inhibitor of sterol synthesis in fungal cells.

The drug is effective in opportunistic mycoses, including those caused by Candida spp., Cryptococcus neoformans, Microsporum spp., Trichophyton spp. The activity of fluconazole is also shown in models of endemic mycoses, including infections caused by Blastomyces dermatitidis, Coccidiodes immitis and Histoplasma capsulatum.

Pharmacokinetics

After oral use, fluconazole is well absorbed, its bioavailability is 90%. Cmax after oral use on an empty stomach at a dose of 150 mg is 90% of the plasma content when administered intravenously at a dose of 2.5–3.5 mg/l. Simultaneous food intake does not affect the absorption of the drug taken orally. Cmax in plasma is reached in 0.5-1.5 hours after use.

T1 / 2 of fluconazole is about 30 h. Plasma concentrations are directly proportional to the dose. 90% of the equilibrium concentration is reached by 4-5 days of treatment with the drug (when taken 1 time/day).

The introduction of a shock dose (on the first day),2 times higher than the usual daily dose, allows you to reach a level corresponding to 90% of the equilibrium concentration by the second day. The apparent volume of distribution approaches the total water content of the body. Binding to plasma proteins is 11-12%.

Fluconazole penetrates well into all body fluids. Concentrations of the drug in saliva and sputum are similar to its plasma levels. In patients with fungal meningitis, the content of fluconazole in the cerebrospinal fluid reaches 80% of its plasma level.

In the stratum corneum, epidermis, dermis and sweat fluid, high concentrations are achieved that exceed serum levels.

Fluconazole is mainly excreted by the kidneys; approximately 80% of the administered dose is excreted unchanged in the urine. The clearance of fluconazole is proportional to creatinine clearance. No metabolites of fluconazole were detected in the peripheral blood.

Indications

• cryptococcosis, including cryptococcal meningitis and other localization of the infection (including the lungs, skin), as in patients with normal immune response, and various forms of immunosuppressive therapy (including patients with AIDS, organ transplant); the drug can be used for the prevention of cryptococcal infections in AIDS patients;
• generalized candidiasis, including candidemia, disseminated candidiasis and other forms of invasive Candida infections (infection of the peritoneum, endocardium, eyes, respiratory and urinary tract); candiduria,. The treatment may be performed in patients with malignant tumors, patients in intensive care, patients undergoing cytotoxic or immunosuppressive therapy, and the presence of other predisposing factors to the development of Candida;
• candidiasis of the mucous membranes, including the oral cavity and pharynx (including atrophic oral candidiasis associated with wearing dentures), esophagus, non-invasive bronchopulmonary candidiasis; prevention of relapse of oropharyngeal candidiasis in patients with AIDS,
• genital candidiasis: vaginal candidiasis (acute and chronic recurrent), prophylactic use to reduce the frequency of recurrences of vaginal candidiasis (3 or more episodes per year); candidal balanitis;
• prevention of fungal infections in patients with malignancies who are predisposed to such infections as a result of chemotherapy with cytostatics or radiation therapy;
• fungal skin infections, including athlete’s foot, body, groin, pityriasis versicolor, onychomycosis; candidiasis of the skin;
• deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, sporotrichosis and histoplasmosis in patients with normal immune systems.

Contraindications

• hypersensitivity to the drug or similar azole compounds;
• concomitant use of terfenadine or astemizole and other drugs that extend the QT interval;
• children (up to 3 years).

With caution:  hepatic and / or renal failure, concomitant use of potentially hepatotoxic drugs, alcoholism.

Side effects

From the digestive system:  changes in taste, vomiting, nausea, diarrhea, flatulence, abdominal pain, rarely-impaired liver function (jaundice, hepatitis, hepatonecrosis, hyperbilirubinemia, increased ALT, AST, ALP activity).

Nervous system disorders: headache, dizziness, rarely convulsions.

From the side of hematopoietic organs:  rarely-leukopenia, thrombocytopenia, neutropenia, agranulocytosis.

Allergic reactions:  skin rash, rarely-malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), anaphylactoid reactions.

Other services:  rarely-impaired renal function, alopecia, hypercholesterolemia, hypertriglyceridemia, hypokalemia.

Interaction

When using fluconazole with warfarin, the PV increases (on average by 12%). In this regard, it is recommended to carefully monitor the indicators PV in patients receiving the drug in combination with coumarin anticoagulants.

Fluconazole increases the plasma half-life of oral hypoglycemic agents-sulfonylurea derivatives (chlorpropamide, glibenclamide, glipizide, tolbutamide) in healthy people. The combined use of fluconazole and oral hypoglycemic agents in diabetic patients is allowed, but the doctor should keep in mind the possibility of hypoglycemia.

Concomitant use of fluconazole and phenytoin may lead to an increase in the concentration of phenytoin in plasma to a clinically significant degree. Therefore, if the combined use of these drugs is necessary, it is necessary to monitor the concentration of phenytoin with dose adjustment in order to maintain the level of the drug within the therapeutic interval.

Combination with rifampicin resulted in a 25% decrease in AUC and a 20% reduction in plasma T1/2 of fluconazole. Therefore, it is advisable to increase the dose of fluconazole in patients receiving rifampicin at the same time.

It is recommended to monitor the concentration of cyclosporine in the blood of patients receiving fluconazole, because the use of fluconazole and cyclosporine in patients with a transplanted kidney (when taking fluconazole at a dose of 200 mg/day) leads to a slow increase in the concentration of cyclosporine in plasma.

Patients who are receiving high doses of theophylline or who are likely to develop theophylline intoxication should be monitored for early detection of symptoms of overdose of theophylline, since taking fluconazole leads to a decrease in the average rate of clearance of theophylline from plasma.

Concomitant use of fluconazole and terfenadine, cisapride has been associated with cases of adverse cardiac reactions, including paroxysms of ventricular tachycardia(torsades de pointes).

Concomitant use of fluconazole and hydrochlorothiazide may increase the plasma concentration of fluconazole by 40%.

There are reports of interaction between fluconazole and rifabutin, accompanied by an increase in serum levels of the latter. Cases of uveitis have been reported with concomitant use of fluconazole and rifabutin. Patients receiving rifabutin and fluconazole concomitantly should be carefully monitored.

In patients receiving a combination of fluconazole and zidovudine, an increase in the concentration of zidovudine is observed, which is caused by a decrease in the conversion of the latter to its main metabolite, so an increase in the side effects of zidovudine should be expected.

How to take, course of use and dosage

Inside.

Adults with cryptococcal meningitis and cryptococcal infections of other localizations are usually prescribed 400 mg on the first day, and then continue treatment at a dose of 200-400 mg once a day. The duration of treatment for cryptococcal infections depends on the clinical efficacy confirmed by mycological examination; for cryptococcal meningitis, it is usually continued for at least 6-8 weeks.

To prevent recurrence of cryptococcal meningitis in AIDS patients, after completing a full course of primary treatment, fluconazole is prescribed at a dose of 200 mg / day for a long period of time.

For candidaemia, disseminated candidiasis and other invasive candida infections, the dose is usually 400 mg on the first day, and then 200 mg each. In case of insufficient clinical efficacy, the dose of the drug can be increased to 400 mg / day. The duration of therapy depends on the clinical efficacy.

For oropharyngeal candidiasis, the drug is usually prescribed 50-100 mg once a day; the duration of treatment is 7-14 days. If necessary, in patients with a pronounced decrease in immunity, treatment can be longer.

When atrophic candidiasis of the oral cavity associated with wearing dentures, fluconazole is usually prescribed 50 mg 1 time a day for 14 days in combination with local antiseptics to treat the prosthesis.

In other localizations of candidiasis (with the exception of genital candidiasis), for example, esophagitis, non-invasive bronchopulmonary lesions, candiduria, candidiasis of the skin and mucous membranes, etc.the effective dose is usually 50-100 mg / day with a treatment duration of 14-30 days. To prevent relapses of oropharyngeal candidiasis in patients with AIDS after completing a full course of primary therapy, the drug can be prescribed 150 mg once a week.

With vaginal candidiasis, fluconazole is taken once orally at a dose of 150 mg. To reduce the frequency of relapses of vaginal candidiasis, the drug can be used at a dose of 150 mg once a month. The duration of therapy is determined individually; it varies from 4 to 12 months. Some patients may require more frequent use.

When balanitis caused by Candida, fluconazole is prescribed once in a dose of 150 mg orally.

For the prevention of candidiasis, the recommended dose of fluconazole is 50-400 mg once a day, depending on the degree of risk of fungal infection. If there is a high risk of generalized infection, for example, in patients with expected severe or long-term persistent neutropenia, the recommended dose is 400 mg once a day. Fluconazole is prescribed a few days before the expected occurrence of neutropenia; after an increase in the number of neutrophils more than 1000/mm3, treatment is continued for another 7 days.

For mycoses of the skin, including mycoses of the feet, skin of the groin area, and candidiasis of the skin, the recommended dose is 150 mg once a week or 50 mg once a day. The duration of therapy in normal cases is 2-4 weeks, but with mycoses of the feet, longer therapy may be required (up to 6 weeks).

With pityriasis versicolor — 300 mg once a week for 2 weeks, some patients require a third dose of 300 mg per week, while in some cases a single dose of 300-400 mg is sufficient; an alternative treatment regimen is the use of 50 mg once a day for 2-4 weeks.

For onychomycosis, the recommended dose is 150 mg once a week. Treatment should be continued until the infected nail is replaced (uninfected nail regrowth). It normally takes 3-6 and 6-12 months, respectively, for the nails to regrow on the fingers and feet.

Deep endemic mycoses may require the use of the drug at a dose of 200-400 mg / day for a period of up to 2 years. The duration of therapy is determined individually; it can be 11-24 months – with coccidioidomycosis; 2-17 months – with paracoccidioidomycosis; 1-16 months – with sporotrichosis and 3-17 months – with histoplasmosis.

In children, as with similar infections in adults, the duration of treatment depends on the clinical and mycological effect. In children, the drug should not be used in a daily dose that would exceed that of adults. The drug is used daily 1 time a day.

For mucosal candidiasis, the recommended dose of fluconazole is 3 mg / kg / day. On the first day, a shock dose of 6 mg/kg may be prescribed in order to achieve constant equilibrium concentrations more quickly.

For the treatment of generalized candidiasis or cryptococcal infection, the recommended dose is 6-12 mg / kg / day, depending on the severity of the disease.

For the prevention of fungal infections in children with reduced immunity, in whom the risk of infection is associated with neutropenia, which develops as a result of cytotoxic chemotherapy or radiation therapy, the drug is prescribed at 3-12 mg / kg / day, depending on the severity and duration of preservation of induced neutropenia.

In children with impaired renal function, the daily dose of the drug should be reduced (in the same proportion as in adults) in accordance with the severity of renal failure.

In elderly patients with no impaired renal function, the usual dosage regimen should be followed. Patients with renal insufficiency (creatinine clearance —

Use of the drug in patients with impaired renal function

, Fluconazole is mainly excreted unchanged in the urine. With a single dose, no dose change is required. When re-prescribing the drug to patients with impaired renal function, a shock dose of 50 to 400 mg should first be administered. If the creatinine clearance is >50 ml / min, the usual dose of the drug is used (100% of the recommended dose). When Creatinine clearance is from 11 to 50 ml / min, a dose equal to 50% of the recommended dose is used. Patients who are regularly on dialysis, one dose of the drug is used after each hemodialysis session.

Overdose

Symptoms: hallucinations, paranoid behavior.

Treatment: symptomatic, gastric lavage, forced diuresis. Hemodialysis for 3 hours reduces the plasma concentration by approximately 50%.

Special instructions

In rare cases, the use of Mycomax was accompanied by a toxic effect on the liver, including with a fatal outcome, mainly in patients with serious concomitant diseases.

Liver function should be monitored during treatment.

If there are signs of liver damage that may be associated with taking fluconazole, the drug should be discontinued.

Form of production

Capsules

Storage conditions

Keep out of reach of children, dry, protected from light, at a temperature of 10 to 25°C.

Shelf

life is 3 years.

Active ingredient

Fluconazole

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For children as prescribed by a doctor, For adults

Indications

Thrush, Nail Fungus, Skin Fungus Fungus and