Griseofulvin

Instruction manual

For medical use of the drug

Structure:

Active ingredient: griseofulvin;

1 tablet contains griseofulvin 125 mg;

excipients: lactose monohydrate, corn starch, polyethylene glycol, povidone, magnesium stearate.

Dosage form.

Tablets.

Basic physico-chemical properties: tablets of white or white with a yellowish tint color, round in shape with a biconvex surface. On the surface of the tablets marbling is allowed.

Pharmacotherapeutic group.

Antifungal drugs for systemic use. Code ATX D01B A01.

Pharmacological properties.

Pharmacodynamics

griseofulvin is an antibiotic produced by Penicillinum nigricans mold, a fungistatic agent active against various dermatomycetes (trichophytons, microsporums, epidermophytons). The drug inhibits the division of fungal cells in metaphase, disrupting the structure of the mitotic spindle. griseofulvin to various degrees accumulates in the cells of the skin, hair, nails, providing resistance to fungal infection. With the death of affected keratin, its replacement with a healthy one.

Pharmacokinetics

it is metabolized in the liver with the formation of the main metabolites: 6-methylgryofeofulvin and glucuronide derivative. The half-life is 24 hours. It is excreted by the kidneys. Less than 1% is excreted in urine unchanged, with 36% in feces.

Clinical characteristics.

Indications.

Mycoses of the skin, hair and nails caused by fungi of the genus trichophyton, microsporum, epydermophyton: trichophytosis, favus, microsporia of the scalp and smooth skin, epidermophytosis of the skin (including inguinal epidermophytosis), dermatomycosis of the feet and hands, onychomycosis.

Contraindications

• Hypersensitivity to griseofulvin and to other components of the drug; severe leukopenia and systemic blood diseases; severe liver and kidney disease; porphyria; systemic lupus erythematosus; malignant neoplasms; lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome (the drug contains lactose).

Interaction with other drugs and other types of interactions.

The interaction of griseofulvin with other drugs

Griseofulvin induces cytochrome P450, therefore, it can enhance the metabolism in the liver and, therefore, weaken the effect of a number of drugs.

Cyclosporine: a decrease in the concentration of cyclosporine in blood plasma; it should monitor its level in blood plasma during treatment with griseofulvin and, if necessary, adjust the dose of cyclosporine.

Methadone: a decrease in plasma methadone levels with a risk of withdrawal. The frequency of methadone intake should be increased to 2-3 times a day.

Oral anticoagulants: decrease in their effect; more frequent monitoring of prothrombin time, international normalized ratio (INR) and dose adjustment of oral anticoagulants during treatment with griseofulvin and within 8 days after its withdrawal are necessary.

Hormonal contraceptives: decreased contraceptive effectiveness, menstrual irregularities are possible. For more details, see the “Application Features” section.

Estrogens and progestins (non-contraceptive): a decrease in their effectiveness due to an increase in metabolism in the liver. Clinical monitoring of the patient is necessary, dose adjustment of estrogen or progestin is possible during treatment with griseofulvin and after its withdrawal.

It is also possible to reduce the effectiveness of oral antidiabetic drugs (control of blood glucose with a possible dose adjustment of these drugs), theophylline (monitoring its concentration in the blood with a possible dose adjustment).

The interaction of other drugs with griseofulvin

Inductors of microsomal enzymes (includingbarbiturates, rifampicin, doxercalciferol, phenylbutazone, primidone, other sedative and hypnotic drugs that induce microsomal enzymes) can increase the metabolism of griseofulvin and reduce its fungistatic activity.

Alcohol: disulfiram-like reactions are possible, manifested by fever, sensation of hot flashes, nausea, vomiting, diarrhea, paresthesia of the limbs. Enhances the effect of ethanol.

Concomitant use of nicotinamide (vitamin B₃), alpha-tocopherol (vitamin E) with griseofulvin increases the concentration of griseofulvin in blood serum and skin.

Effect on laboratory results

A false-positive result is possible in the determination of vanillyl mandelic acid in urine.

Features of the application.

Griseofulvin should not be prescribed for prophylactic use, it should not be used to treat mild mycosis, in which it is sufficient to prescribe local antifungal agents.

Before starting treatment, it is necessary to identify the type of fungus that caused the disease.

With candidiasis, bacterial infections, histoplasmosis, actinomycosis, sporotrichosis, chromoblastomycosis, coccidioidomycosis, North American blastomycosis, cryptococcosis (torulose), pityriasis versicolor, nocardiosis, the drug is not effective!

Patients should be carefully examined before starting long-term treatment. With caution, prescribe the drug with hypersensitivity to penicillins, with hypocoagulation conditions, with mild and moderate impaired liver function (with severe impaired liver function, the drug is contraindicated).

In elderly patients, due to age-related changes in liver function, the risk of manifestations of hepatotoxicity of the drug increases (anorexia, nausea, vomiting, fatigue, jaundice, abdominal pain, dark urine, increased activity of hepatic transaminases). Therefore, periodic careful clinical and laboratory monitoring of liver function is necessary.

For better absorption of griseofulvin and to minimize digestive disorders, it is advisable to include foods with a high fat content (for example, milk, ice cream) in the diet. When using the drug, it is recommended to take vitamin preparations: ascorbic acid and B vitamins.

With the development of granulocytopenia, Griseofulvin treatment should be discontinued.

Griseofulvin can increase the sensitivity of the skin to sunlight, so during treatment, direct sunlight and artificial ultraviolet radiation should be avoided.

Griseofulvin can cause serious birth defects in a child when used by women during pregnancy, as well as induce chromosomal aberrations in spermatocytes. Since griseofulvin reduces the effectiveness of hormonal contraceptives (oral, parenteral), it is necessary to use additional preservatives (for example, condoms) during treatment. It is advisable for women to plan a pregnancy no earlier than 1 month after the end of the course of treatment; men should not plan future paternity during treatment and for 6 months after stopping the drug.

Isolated lethal cases have been reported that have been associated with griseofulvin and are associated with cardiac arrest, Spina bifida, multiple birth defects, adrenal cortex insufficiency, primary biliary cirrhosis, systemic lupus erythematosus, and peripheral neuropathy.

During prolonged treatment with the drug and / or the use of high doses, it is recommended to regularly monitor the hematopoiesis system, liver and kidney functional status indicators.

As with other antibiotics, prolonged treatment with Griseofulvin can lead to increased growth of resistant microflora, in particular fungi, and the development of superinfection, which requires appropriate measures.

To prevent re-infection, it is necessary to disinfect clothes, bedding, underwear, shoes.

During treatment with griseofulvin, you must refrain from drinking alcohol!

The drug should not be used in patients with carbohydrate tolerance disorders such as lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome (the drug contains lactose). If you are intolerant of certain sugars, consult your doctor before taking this medication.

Use during pregnancy or lactation.

Griseofulvin crosses the placenta. adequate studies on the safety of its use during pregnancy have not been conducted. limited data show that griseofulvin led to serious birth defects when taken by women during pregnancy. use of the drug during pregnancy is contraindicated. women of reproductive age should use effective contraceptive methods during treatment and within 1 month after its discontinuation, and men - within 6 months after discontinuation of the drug (see the section "features of use").

It is not known whether griseofulvin passes into breast milk, so if it is necessary to take the drug, breast-feeding for the period of treatment should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

The drug can adversely affect the reaction rate when driving vehicles or other mechanisms.

Dosage and administration.

Take the tablets during or after a meal (with 1 teaspoon of vegetable oil).

With microsporia, adults should prescribe 1 g of griseofulvin per day. The daily dose is preferably divided into 2 doses.

Take the drug daily until the first negative result of mycological examination, then - in the same dose for 2 weeks every other day and 4 times - over the next 2 weeks.

For onychomycosis, trichophytosis, favus of the scalp, the daily dose of griseofulvin for adults weighing up to 50 kg is 625 mg (5 tablets), with a larger weight, an additional 125 mg for every 10 kg is prescribed.

The treatment period for severe mycoses can last up to 12 months. The course of treatment for lesions of the skin of the body - 2-4 weeks, scalp - 4-6 weeks, skin of the feet - 4-8 weeks, fingernails - at least 4 months, toenails - at least 6 months.

Take the drug until complete clinical and laboratory recovery.

Children.

The drug is prescribed for children with body weight from 25 kg at a dose of 10 mg / kg per day, divided into 2 doses.

Overdose.

No cases of overdose of griseofulvin have been reported.

Nausea, vomiting, headache, paresthesia, confusion, vertigo, urticaria, porphyria are possible.

Adverse Reactions

Digestive system: dyspepsia, nausea, vomiting, diarrhea, discomfort / pain in the epigastrium, anorexia, changes in taste perception, glossitis.

Immune system: hypersensitivity reactions, incl. anaphylactic reactions, allergic reactions.

Skin and subcutaneous tissue: urticaria, skin rashes, including erythematous rashes, photosensitivity reactions; angioedema, erythema nodosum, erythema multiforme, eczema, toxic epidermal necrolysis, Stevens-Johnson syndrome. Alopecia, purpura, acne are possible.

Nervous system and mental disorders: headache, which usually goes away with continued treatment, feeling tired, weakness, dizziness, confusion, sleep disturbances (includingdrowsiness), irritability, anxiety, agitation, nightmares, depression; peripheral neuropathy (including limb paresthesia), migraine, impaired coordination.

Hemopoietic system: granulocytopenia, leukopenia, neutropenia, thrombocytopenia, anemia, exacerbation of porphyria and systemic lupus erythematosus.

Urinary system: dysuria, proteinuria, interstitial nephritis, acute renal failure.

Reproductive system and mammary glands: irregular menstruation, metroragia, erectile dysfunction, miscarriage, unplanned pregnancy.

Hepatobiliary system: possible manifestations of hepatotoxicity, including increased activity of hepatic transaminases, hepatitis, intrahepatic cholestasis.

Cardiovascular system: palpitation, tachycardia, arrhythmia, extrasystole, syncope, cardiomyopathy, hot flashes, vasculitis.

Sensory organs: tinnitus, vertigo, conjunctival hemorrhage, conjunctivitis, eye pain.

Respiratory system: dyspnea, bronchospasm / exacerbation of bronchial asthma, pneumofibrosis.

Others: alcohol intolerance, candidal stomatitis, hyperthermia, chest pain, swelling of the face; reported cases of arthropathy, griseofulvin-induced myositis, gout, flu-like syndrome, which manifested itself as headache, arthralgia, myalgia, sore throat.

Serious adverse reactions with griseofulvin are rare, usually associated with high doses of the drug and / or a long course of treatment.

Shelf life.

4 years.

Storage conditions.

In the original packaging at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Packaging.

20 tablets in a blister, 2 blisters in a pack.

Vacation category.

On prescription.

Manufacturer.

Public Joint Stock Company “Scientific and Production Center“ Borshchag Chemical and Pharmaceutical Plant ”.

The location of the manufacturer and the address of the place of business.

Ukraine, 03134, Kiev, st. peace, 17.