Fungavis - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate 70 mg, corn starch 17 mg, povidone low molecular weight 16 mg, magnesium stearate 3 mg, crospovidone 3 mg, silicon dioxide colloid 1 mg.

Description:

Tablets of white or almost white color, flatornwith chamfer and risk.

Pharmacotherapeutic group:antifungal agent

ATX: & nbsp

J.02.A.B.02 Ketoconazole

D.01.A.C.08 Ketoconazole

Pharmacodynamics:

Ketoconazole is a synthetic imidazoledioxole derivative with fungicidal or fungistatic action against dermatophytes, yeast-like (Candida, Pityrosporum, Torulopsis, Cryptococcus), dimorphic fungi and higher fungi (eumycetes). Less sensitive to the action of ketoconazole Aspergillus spp., Sporothrix schenckii, others Dermatiacceae, Mucor spp. and other fikomitsety, except for Entomophthorales.

Ketoconazole inhibits the synthesis of ergosterol in fungi, which leads to a change in the composition of lipid components in membranes.

When taking a daily therapeutic dose of 200 mg (in 1 dose), a transient decrease in the leveltestosterone in the blood plasma; normalization of testosterone levels occurs within 24 hours after administration of ketoconazole. During prolonged therapy with this dosage, testosterone concentration usually differs slightly from control.

Pharmacokinetics:

The average maximum concentration of ketoconazole in plasma is 3.5 mg / ml achieved 1-2 hours after a single oral intake of 200 mg of the drug during meals.

The connection with plasma proteins is 99%. A small part of the drug penetrates into the cerebrospinal fluid.

The metabolites formed are not active. The main ways of metabolism are oxidation and cleavage of imidazole and piperazine rings, oxidative O-dealkylation and aromatic hydroxylation.

Excretion from the plasma is biphasic: during the first 10 hours, the elimination half-life is 2 hours, and in the subsequent - 8 hours. About 13% of the dose is excreted in the urine, of which 2 to 4% is unchanged drug substance. The drug is excreted, mainly with bile.

Indications:

Infections of smooth skin, scalp, nails caused by dermatophytes and / or yeast-like fungi (dermatophytosis caused by fungi of the genus Candida, colorful lichen, dandruff, folliculitis caused by fungi of the genus Pityrosporum, chronic candidiasis of the skin and mucous membranes) in those cases when local treatment of large areas of affected areas, significant depth of skin lesions, and also without the effect of previous local treatment can not be used.

Infections of the gastrointestinal tract caused by yeast-like fungi.

Chronic recurrent vaginal candidiasis in the absence of the effect of local therapy.

Systemic fungal infections, for example, paracoccidiomycosis, histoplasmosis, coccidiomycosis, blastomytoLake.

Prophylactic use in patients with reduced protective forces of the body (congenital or caused by the disease, or the effects of drugs).

Contraindications:

Acute and chronic diseases of the liver, kidneys; hypersensitivity to the components of the drug; lactation period; children's age up to 3 years.

Contraindicated simultaneous administration of ketoconazole with substrates CYP3A4: terfenadine, astemizole, cisapride, triazolam and oral forms of midazolam, quinidine, pimozide; inhibitors of HMG-CoA reductase, such as simvastatin and lovastatin.

Pregnancy and lactation:

Studies on the use of ketoconazole in pregnant women are not available, so it is not recommended to use it during pregnancy, except when the potential benefits of treatment can justify the possible risk to the fetus.

Ketoconazole penetrates into breast milk, breast-feeding while taking the drug is contraindicated.

Dosing and Administration:

Ketoconazole should be taken by mouth in 1 dose during meals.

PAdults and children weighing more than 30 kg

Fungal lesions of the skin, gastrointestinal tract and systemic mikoz: It is recommended to take 1 tablet (200 mg) of ketoconazole daily during meals. In case there is no adequate response to this dose, you can increase the dose to 2 tablets (400 mg) once a day.

Vaginal candidiasis: 2 tablets (400 mg) once a day with meals for 5 days.

The use of children older than 3 years with a body weight of 15 to 30 kg

1/2 tablets (100 mg) per day. Treatment according to the above scheme should be carried out at least a week after all symptoms disappear, until negative results of microbiological studies are obtained.

Preventative use in patients with immunodeficiency

Adults - 2 tablets (400 mg) per day; children - 4-8 mg / kg body weight per day, but not more than 400 mg.

The average duration of treatment is:

- with vaginal candidiasis - 7 days;

- with cutaneous mycoses caused by dermatophytes - about 4 weeks;

- with colored lichen-10 days;

- at a candidiasis of a skin and an oral cavity - 2-3 weeks;

- with fungal lesions of the scalp - 1-2 months;

- with paracoccidiomycosis, histoplasmosis, coccidiomycosis, the optimal duration of treatment is 3-6 months.

Side effects:Classification of the incidence of adverse events (WHO): very often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1000, <1/100); rarely (≥ 1/10 000, <1/1000); very rarely (<1/10 000), including individual messages.

The most common side effects are disorders of the gastrointestinal tract: Often - vomiting; often - decreased appetite, indigestion, nausea, abdominal pain, diarrhea.

Rarely headache, insomnia, arthralgia, fever, reversible increase in the activity of hepatic enzymes, hepatotoxicity, menstrual disorders, dizziness, photophobia, paresthesia, hypercreatininaemia, allergic reactions (urticaria, skin rash, fever), arthralgia, exanthema.

Rarely - thrombocytopenia, alopecia, impotence and reversible increase in intracranial pressure (e.g., papilledema, swelling fontanel in children), a temporary decrease in testosterone levels in the blood plasma, reversible gynecomastia and oligospermia, decrease of libido, allergic reactions including anaphylactic shock, anaphylactic and anaphylactoid reactions, angioedema.

Overdose:

Cases of overdose and clinical symptoms are not described, however, when taken in large doses, an increase in side effects is possible.

Support measures are recommended. During the first hour after ingestion, vomiting may be caused, gastric lavage performed and Activated carbon. Careful monitoring of the patient's condition and symptomatic treatment are necessary. There is no specific antidote.

Interaction:

Drugs that affect the metabolism of ketoconazole:

- rifampicin, rifabutin, carbamazepine, isoniazid and phenytoin significantly reduce the bioavailability of ketoconazole;

- while taking drugs that reduce the acidity of the gastric juice, the absorption of ketoconazole worsens.Patients with achlorhydria or patients taking medications that suppress the secretion of hydrochloric acid in the stomach (eg, H2-histamine receptors or inhibitors of the "proton pump") it is desirable to take ketoconazole with sour drinks. Taking antacid preparations, for example, aluminum hydroxide, should be performed no earlier than 2 hours after taking ketoconazole;

- ritonavir increases the bioavailability of ketoconazole, and as a result of this, it is necessary to reduce the dose of ketoconazole when combined.

Ketoconazole may enhance or prolong the effect of the following drugs drugs (metabolized with the participation of cytochrome P 450, especially from the group CYP3A):

- oral anticoagulants;

- HIV protease inhibitors, such as indinavir, saquinavir;

- antineoplastic agents such as alkaloids Barvinka pink, docetaxel;

- enzyme-cleavable CYP3A4 calcium channel blockers (incl. verapamil);

- cyclosporine;

- digoxin, carbamazepine, buspirone, sildenafil, alprazolam, midazolam, rifabutin, methylprednisolone;

- drugs, in the appointment of which you want to monitor their levels in the plasma, the effect and side effects,should be used in a smaller dose;

Ketoconazole when taken together:

- weaken the effect of amphotericin B;

- reduces the stimulating effect of corticotropin on the adrenal glands;

- in patients receiving oral contraceptives with a low content of hormones increases the risk of bleeding "breakthrough";

- increases the toxicity of phenytoin.

Is known to occur disulfirampodobnoy reaction to alcohol, characterized by redness, rash, peripheral edema, nausea and headache. All symptoms disappear completely within a few hours.

Special instructions:

Use with caution in hepatic failure, while receiving potentially hepatotoxic drugs, alcoholism, achlorhydria, hypochlorhydria, pregnancy, children's age (up to 3 years) (safety and efficacy have not been established), over the age of 50 years, with adrenal insufficiency and pituitary gland.

In some cases, when taking the drug, there is an insignificant, transient asymptomatic increase in the activity of "bakedчнtransaminase or alkaline phosphatase.This reaction is not dangerous and does not require mandatory cessation of treatment, however, such patients should be under special supervision.

If the duration of treatment with ketoconazole exceeds 2 weeks, it is necessary to monitor liver function: before treatment, two weeks and then monthly. In case of detection of violations of the liver, treatment should be discontinued.

It is necessary to familiarize patients who are prescribed long-term treatment with ketoconazole, with symptoms of liver disease (fatigue, general weakness, elevatedande body temperature, darkening of urine, decolorization of feces, jaundice).

In patients with adrenal insufficiency or borderline conditions, as well as in patients undergoing significant stress (surgical intervention), when taking the drug at a dose of 400 mg or more, adrenal function should be monitored.

Effect on the ability to drive transp. cf. and fur:

When treating the drug may be dizzy, it is recommended to refrain from engaging in potentially hazardous activities.

Form release / dosage:

Tablets of 200 mg.

Packaging:

For 1, 2 or 3 contour mesh packages together with instructions for use in a pack of cardboard.

Packing for hospitals: 100, 200, 300, 400 or 500 contour mesh packages together with instructions for use in corrugated cardboard boxes.

For 500, 1000 or 2000 tablets in cans of polymer with lids.

By 1, 2, 3, 4, 5, 6 cans along with instructions for use in boxes made of corrugated cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001734

Date of registration:29.11.2011

The owner of the registration certificate:ZIO-HEALTH, JSC ZIO-HEALTH, JSC Russia

Manufacturer: & nbsp

ZIO-HEALTH, JSC Russia

Information update date: & nbsp24.02.2012

Illustrated instructions

Instructions

Fungavis (Fungavis)