GRISEOFULVIN (Griseofulvinum; synonym: grizovin, fultsin, Sporostatin etc.; joint venture. B) — the antifungal antibiotic formed at biosynthesis of Penicillium griseofulvum and other species of mushrooms (on the boat. class.). Total formula C 17 H 17 O 6 Cl, pier. weight 352,77. It is active concerning all types of trikhofiton, many types of mikrosporon, achorions, and also epidermofiton. Yeast-like fungi of a sort Candida, actinomycetes, and also the majority of the pathogenic fungi causing generalized deep mycoses are steady against G. Works only fungistaticly. Cross resistance of activators to G. and other antibiotics is not revealed. Increase of stability in the course of G.'s treatment is not observed. G.'s activity decreases in the presence of blood serum (binding by 80%). The mechanism of antifungal action of G. is probably connected with disturbance of synthesis of a cell wall of dermatophytes, formation of complexes with soluble RNA and suppression of proteinaceous synthesis.
At intake of G. it is well soaked up, reaching the maximum concentration in 4 — 5 hours after introduction. Increase in an optimum daily dose of G. does not give increase in its level in blood. High-disperse powder G. with a particle size no more than 4 microns is soaked up approximately twice best of all, than usual fine-crystalline. Selectively collects in a corneous layer of epidermis, a matrix of nails, a radical zone of hair, protecting again formed keratin from defeat by fungi. In bottoms of a corneous layer of G. it is found out in 3 days of treatment, in averages — in 10 — 15 days, in upper — only to 30 — to the 50th day that speaks about need of long therapy. It is removed with a stake and urine (apprx. 1% in biologically active form and to 75% — in the form of inactive metabolites).
Indication to G.'s use the following diseases are: a favus of a pilar part of the head and smooth skin, a trichophytosis of a pilar part of the head and smooth skin (including chronic), a microsporia of a pilar part of the head and smooth skin, the epidermophitia of smooth skin caused by a red epidermofiton (trikhofitony), the onychomycoses caused by achorion, trikhofitona and a red epidermofiton, a trichophytosis and a favus limf, nodes and bones.
It is not effective at an actinomycosis, zymonematoses, candidiases, chromozymonematoses, koktsidiomikoza, histoplasmosis and other generalized mycoses, and also at a pitiriazisa and an erythrasma. Appoint only at typical a wedge, the picture of mycoses confirmed with repeated laboratory researches.
Apply only inside preferential in a high-disperse form — to adults and children 15 years usually in a single dose of 125 mg (1 tablet) 4 times a day are more senior; to children up to 3 years — on 0,5 tablets 2 — 3 times a day; from 3 to 7 years on 1 tablet 2 times a day; from 7 to 15 years on 1 tablet 3 times a day. Duration of therapy is defined by the term of complete regeneration of an affected area: for mycoses of a pilar part of the head — 1 — 3 month, onychomycoses — 3 — 8 months. During the first 3 weeks of G. accept daily, then in 1 or 2 days. At G.'s treatment mycoses of a pilar part of the head are not required to a X-ray epilation, at onychomycoses it is reasonable to remove nail plates with a surgical method or keratolytic means. Treatment is continued before obtaining quadruple negative results of the microscopic examination made at an interval of 2 — 5 days.
Suspension G. is intended to hl. obr. for treatment of children. It contains in 1 ml 15 mg of an antibiotic. Appoint before food to children up to 3 years on 1 teaspoon 2 — 3 times a day, from 3 to 7 years — on a dessertspoon 2 times a day, from 7 to 15 years in the same dose 3 times a day.
In therapeutic doses of G. it is transferred well. However at certain patients the headache, dizziness are observed. At increase in doses sleeplessness, disturbance of orientation can join. Often side effect is shown in a loss of appetite, weight in a stomach, nausea, diarrhea. Allergic reactions (makulopapulezny or urtikarny rash, a photosensitization) can be connected with a sensitization to G. or to an infestant. As a rule, side reactions proceed easily and demand not the termination of treatment, and only dose declines of drug. At G.'s treatment it is recommended to appoint ascorbic to - that, thiamin, Riboflavinum, nicotinic to - that.
it is contraindicated at general diseases of blood, damage of kidneys and liver, malignant new growths, pregnancy. The drivers of transport, pilots, persons occupied at high-rise works should not appoint drug on an outpatient basis. It is not necessary to appoint suspension G. at diabetes.
release in tablets on 0,125 g and suspension in bottles on 100 and 200 ml. It is stored in the dry place at the room temperature.
See also Antifungal antibiotics .
Bibliography: Navashin G. M and Fomina I. P. Reference book on antibiotics, page 269, M., 1974.
S. M. Navashin.