Griseofulvin

Brand Biosynthesis

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Available since: 2019-09-19

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Clinical Pharmacology

Griseofulvin - fungistatic.

Antifungal antibiotic, effective against fungi of the genus Trichophyton, Microsporum, Epidermophyton. It causes a violation of the structure of the mitotic spindle and cell wall synthesis in chitin-containing fungi, inhibits the division of fungal cells in metaphase and protein synthesis due to the disruption of communication with messenger RNA. Accumulates in the cells of the skin, hair, nails. As the infected keratin separates, it is replaced with healthy tissue.

Pharmacokinetics

Absorption is high. WITH_max - 0.5–5 mg / l, T_max after ingestion - 4–5 hours. Communication with plasma proteins - 80%. Selectively accumulates in the stratum corneum and its appendages, as well as in the liver, fatty tissue, skeletal muscle. A small amount is distributed in body fluids and tissues. Penetrates through the placenta. Metabolized in the liver to form inactive metabolites (6-methylgrisofulvin and the glucuronide derivative) .Т_1/2 - 24 hours. Excreted by the kidneys (including 1% - unchanged) and through the intestines (36% - unchanged).

Indications

Mycoses of the skin, hair, nails: trichophytosis, favus, microsporia of the scalp, smooth skin, ring beard and mustache, athlete smooth skin, athlete's foot, inguinal athlete, onychomycosis.

Composition

1 tablet contains:

Active ingredient: griseofulvin 125 mg.

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Dosage and Administration

For oral use during or after meals with vegetable oil. With microsporia, children are prescribed at the rate of 21–22 mg per 1 kg of the patient’s body weight per day, for adults - from 500 to 1000 mg (8 pills per day). The drug is taken daily until the first negative test for mushrooms, then at the same dose every other day for 2 weeks and then 2 times a week for 2 weeks.

With trichophytosis (superficial and infiltrative-suppurative forms) and favus for children - at the rate of 18 mg / kg of body weight in the same way as with microsporia.

With onychomycosis, trichophytia and favus of the scalp, the daily dose for adults weighing up to 50 kg is 625 mg (5 pills). The maximum daily dose is 1 g (8 pills). The daily dose in children and adolescents is 16 mg / kg of body weight.

With onychomycosis, the drug is prescribed daily for the first month, the second month - every other day, then 2 times a week in the same daily dose until the nails regrow are completely. The total duration of treatment is at least 8 months.

Adverse reactions

From the side of the central nervous system: headache, dizziness, disorientation, unusual fatigue or weakness, insomnia, peripheral neuropathy, impaired coordination of movements, limb paresthesia, confusion.

From the digestive tract: nausea, vomiting, diarrhea, gastralgia, candidal stomatitis, hepatitis.

From the side of blood-forming organs: granulocytopenia, agranulocytosis, leukopenia.

Allergic reactions: urticaria, skin rash, pruritus, angioedema, photosensitivity, lupus-like syndrome, erythema multiforme exudative, Lyell's syndrome.

Contraindications

Hypersensitivity, porphyria, systemic lupus erythematosus, lupus erythematosus-like syndrome, systemic blood diseases, leukopenia, acute and subacute liver and kidney diseases with impaired functions, hepatic failure, malignant neoplasms, cerebral circulation disorders, post-stroke condition, uterine bleeding, pregnancy, uterine bleeding, pregnancy. feeding, child age (up to 2 years old - efficacy and safety have not been studied).

Drug interactions

Enhances the action of ethanol. Reduces the activity of estrogen-containing oral contraceptives, anticoagulants of indirect action (due to the induction of microsomal liver enzymes). Barbiturates and primidon reduce antifungal activity.