Sebozol, 2% ointment 15 g

Antifungal agent. It has fungicidal and fungistatic action. The mechanism of action is inhibition of ergosterol synthesis and changes in lipid composition of the membrane. It is active against the causative agent of variegated lichen Malassezia furfur, causative agents of some dermatomycoses (Trichophyton, Epidermophyton floccosum, Microsporum), causative agents of candidiasis (Candida) as well as causative agents of systemic mycoses (Cryptococcus).

It is also active against Gram-positive cocci: Staphylococcus spp., Streptococcus spp.

Pharmacokinetics

Ketoconazole is a weak double-base compound that dissolves and is absorbed in an acidic environment. Cmax of ketoconazole in plasma is about 3.5 mcg/ml and is reached 1-2 hours after a single oral dose of 200 mg with meal. Bioavailability of ketoconazole is maximal when taken with food. Absorption of ketoconazole is decreased in patients with low acidity of gastric juice, for example, such as those who take antacids, such as aluminum hydroxide, and antisecretory drugs such as histamine H2-receptor blockers and proton pump inhibitors, as well as in patients with achlorhydria caused by a particular disease.

The binding to plasma proteins, mainly to the albumin fraction, is 99%. Ketoconazole is widely distributed in the tissues, but only a small part of the drug penetrates into the cerebrospinal fluid.

After absorption from the gastrointestinal tract, ketoconazole is metabolized in the liver to form a large number of inactive metabolites.

In vitro studies have shown that the CYP3A4 isoenzyme is involved in the metabolism of ketoconazole. The main pathways of metabolism are oxidation and cleavage of the imidazole and piperazine rings, oxidative O-dealkylation and aromatic hydroxylation. Ketoconazole is not an inducer of its own metabolism. Excretion from plasma is biphasic: during the first 10 h T1/2 is 2 h, subsequently – 8 h.

About 13% is excreted in the urine, of which 2-4% is unchanged. It is excreted mainly with bile in the gastrointestinal tract and about 57% is excreted with feces.

Indications

For external use: treatment and prevention of fungal skin lesions of the scalp; smooth skin dermatomycosis; inguinal epidermophytosis; epidermophytosis of the hands and feet, skin candidiasis.

For topical use: treatment of acute and chronic recurrent vaginal candidiasis; prevention of vaginal fungal infections when the resistance of the body is low and during treatment with antibacterial agents and other drugs that disrupt the normal vaginal microflora.

For oral administration (when other therapies are unavailable and intolerant): blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis.

Active ingredient

Composition

In 1 g of the ointment ketoconazole 20 mg.

How to take, the dosage

For topical and external use, the dosing regimen depends on the indication and the dosage form used.

Side effects

Nervous system and sensory organs: headache, dizziness, somnolence, paresthesias.

Gastrointestinal system disorders: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, increased liver transaminases in the blood, jaundice, hepatitis (high mortality, the risk increases with use over 14 days).

Urogenital system disorders: gynecomastia, decreased libido, impotence, oligospermia, menstrual disorders.

Allergic reactions: urticaria, skin itching.

Other: photophobia, alopecia, arthralgia, fever, thrombocytopenia; local reactions – hyperemia and irritation of the vaginal mucosa, vaginal itching (suppositories); local skin irritation, burning, rash, contact dermatitis (cream, ointment); skin irritation, itching and burning, increased greasiness or dry hair (shampoo).

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