Griseofulvin

General characteristics. Structure:

International and chemical names: Griseofulvin, (1'S,6'R)-7-hlor-2,4,6-trimetoksi-6-metilCpiro [coumarone-2 (3H'), 1 '-[2] tetrahydrobenzene]-3,4 '-dion;
main physical and chemical properties: tablets of color, white or white with a yellowish shade, a round form, with a biconvex surface. On a surface of tablets the mramornost is allowed; structure: 1 tablet contains griseofulvin 0,125 g; excipients: lactoses monohydrate, calcium stearate, potato starch.

Pharmacological properties:

Pharmacodynamics. Griseofulvin is the antibiotic produced by a mold fungus of Penicillinum nigricans, fungistatic means active in relation to various dermatomitseta (trikhofitona, Microsporums, epidermofitona). Drug inhibits division of fungal cells in metaphase, breaking structure of a mitotic spindle. Griseofulvin in different degree collects in cells of skin, a hair, nails, providing resistance to a fungal infection. In process of dying off of the struck keratin there is a replacement with its healthy.

Pharmacokinetics. It is metabolized in a liver with formation of the main metabolites: 6 methylgriseofulvins and glyukuronidny derivative. The elimination half-life makes 24 h. It is removed by kidneys. With urine in not changed look less than 1%, with a stake – 36% are removed.

Indications to use:

Trichophytosis, favus and microsporia of a pilar part of the head and smooth skin, the epidermophitia of integuments caused trikhofitony and also the damages of nails (onychomycoses) caused by a pathogenic fungi (trikhofitony, a red epidermofiton).

Route of administration and doses:

Pill is taken during food in three steps together with 1 teaspoon of vegetable oil. At a microsporia the adult appoint 1 g of Griseofulvin a day, to children (from 3 years) – at the rate of 21-22 mg/kg a day. Drug is accepted daily to the first negative take of a mycologic research, then in the same dose within 2 weeks every other day also by 4 times for 2 weeks.
At an onychomycosis, a trichophytosis, a favus of a pilar part of the head the daily dose of Griseofulvin for adults at body weight to 50 kg makes 625 mg (5 tablets), with a bigger weight appoint in addition 125 mg to each 10 kg. To children and teenagers appoint 16 mg/kg a day. At mycoses which will difficult respond to treatment the course of therapy can proceed up to 12 months.

Features of use:

With care appoint drug at hypersensitivity to penicillin, at hypocoagulative states. To patients whose professional activity requires speed of response and special attention drug is not appointed. At use of drug reception of vitamin drugs is recommended: ascorbic acid and vitamin drugs of group B. At candidiasis drug is inefficient. During treatment by Griseofulvin it is necessary to abstain from alcohol intake.

Side effects:

From the alimentary system: hepatitis, nausea, vomiting, diarrhea, pains in epigastriums.
Allergic reactions: urticaria, skin rashes, multiformny erythema, toxic epidermal necrosis.
From TsNS and peripheral nervous system: peripheral neuropathy, dizziness, confusion of consciousness.
From system of a hemopoiesis: granulocytopenia, leukopenia.
Others: candidosis stomatitis, a photosensitization, sometimes – a lupus.

Interaction with other medicines:

Due to stimulation of microsomal enzymes of a liver Griseofulvin decrease in efficiency of indirect coagulants and oral contraceptives is possible. The concomitant use with barbiturates leads to easing of antifungal properties of Griseofulvin.

Contraindications:

Hypersensitivity to drug components, the expressed leukopenia and general diseases of blood, organic lesions of a liver and kidneys, a porphyria, malignant new growths, pregnancy, a lactation, children's age up to 3 years.

Overdose:

Clinical manifestations of overdose of Griseofulvin are not known.

Storage conditions:

To store in the dry place at a temperature from 15 °C to 25 °C.

Period of validity - 3 years 6 months.

Issue conditions:

According to the recipe

Packaging:

On 20 tablets in a blister strip packaging. On the 2nd packaging in a pack.