Griseofulvin

When ATH:
D01BA01

Characteristic.

Antifungal. Antibiotic, produced by fungi Penicillium nigricans (griseofulvin). White or white with a yellowish tinge naimelchayshy crystalline powder with low specific (mushroom) odor. Practically insoluble in water and petroleum ether, slightly soluble in ethanol, methanol, acetone, benzene, ethyl acetate, acetic acid. Solubility in dimethylformamide at 25 °C: 12-14 G / 100 mL. Stable at high temperature, incl. autoclaving. Molecular weight 352,77.

Pharmacological action.
Antifungal, fungistatic.

Application.

Mycosis of the skin, scalp and nails: crusted ringworm, ringworm, microsporia scalp, microsporia smooth skin, tinea beard and mustache, athlete smooth skin, jock itch, onychomycosis.

Contraindications.

Hypersensitivity, porphyria, systemic lupus erythematosus, lupus-like syndrome, systemic blood diseases, leukopenia, organic diseases of liver and kidneys, hepatocellular insufficiency, malignant neoplasms.

Restrictions apply.

Children up to age 2 years (efficacy and safety have not been determined).

Pregnancy and breast-feeding.

There is evidence of teratogenic and embryotoxic effects of griseofulvin in animals (oral application in pregnant rats reported the presence in litter Young multiple disorders). Displaying, griseofulvin that suppresses spermatogenesis in rats, although studies in humans is not established. Experiments on dogs have shown, that griseofulvin may cause adverse effects in the offspring.

Contraindicated in pregnancy (griseofulvin crosses the placenta, adequate and well-controlled studies in pregnant women has not been). FROM 1977 it was reported two cases of conjoined twins birth patients, taking griseofulvin in the I trimester of pregnancy. If the pregnancy is the period of treatment with griseofulvin, you must inform the patient of the potential risk to the fetus.

Use in breast-feeding is not recommended (unknown, whether griseofulvin penetrates into breast milk). Adequate data are not available.

Side effects.

From the digestive tract: nausea, vomiting, dry mouth, diarrhea, abdominal pain, thrush, increase in liver transaminases, jaundice, hepatitis.

From the nervous system and sensory organs: headache, dizziness, excessive fatigue or weakness, insomnia, peripheral neuropathy, limb paresthesia, dystaxia, lethargy, disorientation, confusion, depression, violation of taste sensitivity.

Cardio-vascular system and blood (hematopoiesis, hemostasis): granulocytopenia, agranulocytosis, leukopenia.

Allergic reactions: rash, itch, hives, angioedema, photosensitivity, lupus-like syndrome, erythema multiforme exudative, topical epidermal necrolysis (Lyell's syndrome).

Cooperation.

Griseofulvin induces liver microsomal enzymes and thereby may enhance metabolism in the liver and, Consequently, weaken the activity of anticoagulants (requires monitoring of PV, may require dose adjustment of anticoagulant), oral hypoglycemic agents (control of blood glucose levels, a correction dose of antidiabetic agent), oral contraceptives estrogensoderjath, teofillina (monitor its concentration in blood with possible dose adjustments). Inductors microsomal enzymes (incl. barbiturates, rifampicin) may increase the metabolism of griseofulvin and reduce its fungistatic activity. It enhances the effect of ethanol.

Dosing and Administration.

Inside (during or immediately after a meal), in one or more steps. The daily dose for adults - 500 mg (in severe mycosis dose increase), for children - 10 mg / kg. The highest daily dose - 1 g. The duration of treatment depends on the thickness of the infection and keratin and the site of infection is: with the defeat of the scalp - 4-6 weeks, fixtures - 2-4 Sun, stop - 4-8 Sun, fingers - at least 4 Months, toes - at least 6 Months.

Precautions.

Before initiation of therapy with griseofulvin is necessary to identify the type of fungus, caused by an infection. Griseofulvin is not suitable for prophylactic use, it is not used for the treatment of mild infections, for which purpose only enough antifungals for topical use. Griseofulvin is not effective for treating bacterial infections, candidiasis, gistoplazmoza, aktinomikoza, sporotrichosis, xromomikoza, kokcidioidoza, North American blastomycosis, kryptokokkoza, tinea versicolor and nocardiosis.

If used with a diet low in fat, griseofulvin must be taken with 1 tablespoon of vegetable oil. During treatment, you can not drink alcoholic beverages.

With the development of granulocytopenia griseofulvin treatment should be discontinued. Because therapy is prolonged, A periodic monitoring of liver function, kidney, gemopoéza.

In elderly patients with age-related changes in hepatic function may increase the risk of hepatotoxicity (requires strict clinical and laboratory monitoring).

During therapy with griseofulvin, patients should avoid direct sunlight and UV radiation.

During the treatment and for 6 Months after the men and women of childbearing age should use effective contraceptive measures (negative influence on the reproductive function in both men, and women).

Do not appoint outpatient drivers transport, as well as people, professional activities which require quick reaction and attention.

Cooperation