Terbinafin cream 1%, 30g

Composition

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of 1 g of cream contains:  

Active ingredients:  

terbinafine hydrochloride 10 mg;

Auxiliary substances:

benzyl alcohol,

polysorbate 60 (tween 60),

sorbitan monostearate,

cetyl alcohol,

isopropyl myristate,

cetyl palmitate,

sodium hydroxide,

purified water.

Pharmacological action

Terbinafine belongs to the group of allylamines, has a wide spectrum of antifungal action. In low concentrations, it has a fungicidal effect on Trychophyton dermatophytes (T. rubrum, T. mentagrophytes, T. tonsurans, T. verrucosum, T. violaceum), Microsporum canis, Epidermophyton floccosum, mold fungi (for example. Scopulariopsis brevicaulis), yeast fungi, mainly Candida albicans.

For fungi Candida spp. and their mycelial forms have a fungicidal or fungistatic effect, depending on the type of fungus. Terbinafine disrupts the early stage of biosynthesis of the main component of the fungal cell membrane, ergosterol, by inhibiting the squalene oxidase enzyme.

When administered orally, it is not effective in the treatment of multicolored lichen caused by Pityrosporum ovale, Pityrosporum orbiculare, Malassezia furfur.

Pharmacokinetics

When taken orally, it is well absorbed, after 0.8 hours, half of the dose taken is absorbed; after 4.6 hours, half of the dose taken is distributed in the body. 1-2 hours after ingestion of a single dose of 250 mg, the maximum concentration of the drug in blood plasma reaches 0.97 mcg / ml. Bioavailability is 80%. Food intake does not affect the bioavailability of terbinafine.

Terbinafine binds intensively to plasma proteins (99%), is rapidly distributed in tissues, and penetrates the dermal layer of the skin and nail plates. Penetrates the secret of the sebaceous glands and accumulates in high concentrations in the hair follicles, hair, skin and subcutaneous tissue.

The half-life is 16-18 hours, the terminal phase half — life is 200-400 hours.

Biotransformed in the liver to inactive metabolites. 80% of the dose is excreted by the kidneys in the form of metabolites, the rest (20%) is excreted through the intestine.

It does not accumulate in the body. The age of patients does not affect the pharmacokinetics of terbinafine, but elimination may decrease with kidney or liver damage, leading to high concentrations of terbinafine in the blood. It is excreted in breast milk.

Indications

• Prevention and treatment of fungal skin infections, including athlete’s foot (“fungus” of the foot), Jock itch (tinea cruris), fungal infections smooth skin of the body (tinea corporis), caused by dermatophytes such as Trichophyton (including T. rubrum, T. mentagrophytes, T. verruco-sum, T. violaceum), Microsporum canis and Epidermophyton floccosum.
• Yeast infections of the skin, mainly those caused by the Candida genus (for example, Candida albicans), in particular diaper rash.
• Multi-colored lichen (Pityriasis versicolor), caused by Pityrosporum orbiculare (also known as Malassezia furfur).

Use during pregnancy and lactation

No teratogenic properties of terbinafine were found in experimental studies.

The use of the drug during pregnancy is possible in cases where the intended benefit to the mother exceeds the possible risk to the fetus. Terbinafine is excreted in breast milk.

If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided.

Contraindications

• Chronic or active liver disease;
• chronic renal failure (CC less than 50 ml/min);
• children’s age (up to 12 years) and weighing up to 20 kg (for this dosage form);
• lactation;
• lactase deficiency, lactose intolerance, malabsorption glucosegalactose;
• hypersensitivity to terbinafine or any other components of the drug.

Care should be taken when:

• renal failure (with creatinine clearance greater than 50 ml/min);
• alcoholism;
• suppression of bone marrow hematopoiesis;
• tumors;
• metabolic diseases;
• occlusive diseases of the vessels of the extremities;
• cutaneous lupus erythematosus or systemic lupus erythematosus.

Side effects

For external use: itching and burning of the skin, hyperemia at the application site, possible allergic reactions.

Interaction

No drug interactions are known for terbinafine ointment/cream.

How to take, course of use and dosage

Adults and children over 12 years of age: apply to the affected skin and adjacent areas in a thin layer, lightly rubbing,1 or 2 times a day.

The duration of treatment depends on the indication and severity of the disease.

The course of treatment is 2-4 weeks on average.

Duration and frequency of application: dermatomycosis of the trunk, legs, feet-1 time a day for 1 week; candidiasis of the skin-1-2 times a day for 1-2 weeks; multi-colored lichen-1-2 times a day for 2 weeks.

Overdose

Symptoms:  headache, dizziness, nausea, vomiting, epigastric pain, frequent urination, rash.

Treatment:  measures to remove the drug (gastric lavage, taking activated charcoal); if necessary, symptomatic maintenance therapy.

Special instructions

Irregular use of terbinafine or premature discontinuation of treatment may lead to relapse of the disease. If there is no improvement in the condition after 2 weeks of treatment for a skin infection, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.

Systemic use in onychomycosis is justified only in the case of damage to most nails, the presence of pronounced subungual hyperkeratosis, and the ineffectiveness of previous local therapy. In the treatment of onychomycosis, a laboratory-confirmed clinical response is usually observed several months after mycological treatment and discontinuation of treatment, due to the rate of regrowth of a healthy nail. Removal of nail plates in the treatment of onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks is not required.

In the presence of liver disease, the clearance of terbinafine may be reduced. During treatment, it is necessary to monitor the activity of “hepatic” transaminases in the blood serum.

In rare cases, cholestasis and hepatitis occur after 3 months of treatment. If signs of impaired liver function appear (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, dark urine or discolored feces), the drug should be discontinued.

Prescribing terbinafine to patients with psoriasis requires caution, because in very rare cases, terbinafine can provoke an exacerbation of psoriasis. When treating with terbinafine, general hygiene rules should be observed to prevent the possibility of re-infection through underwear and shoes. During the course of treatment (after 2 weeks) and at the end of it, it is necessary to perform antifungal treatment of shoes, socks and stockings.

Form of production

Cream for external use

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Terbinafine

Dosage form

cream

Description

For adults, Pregnant women as prescribed by a doctor, Children over 12 years of age

Indications

Mushroom