Terbisil, cream 1% 15 g

Pharmacodynamics

Antifungal drug.

Terbinafine is an allylamine derivative. It has a wide spectrum of antifungal action. In therapeutic concentrations terbinafine has fungicidal action against dermatophytes, yeast-like fungi and some dimorphic fungi. Activity against yeast fungi, depending on their species, may be fungicidal or fungistatic.

Terbinafine specifically inhibits the early stage of sterol biosynthesis in the fungal cell by inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus. This leads to ergosterol deficiency and intracellular accumulation of squalene, which causes cell death of the fungus. Squalene epoxidase is not part of the cytochrome P 450 system, so terbinafine has no effect on the metabolism of hormones or other drugs.

When applied externally, terbinafine is active against: dermatophytes – Trichophyton. Microsporum. Epidermophyton; yeast-like fungi of the genus Candida, such as: Candida albicans.

When applied externally, terbinafine is also active against: Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics

Absorption

Less than 5% of the dose is absorbed when the cream is applied topically.

Distribution

The binding to plasma proteins is 99%. When applied externally, it quickly penetrates through the dermal layer of the skin and accumulates in the lipophilic stratum corneum. Terbinafine also penetrates into the secretion of sebaceous glands, which leads to high concentrations in hair follicles and nails.

Terbinafine is excreted with breast milk.

Metabolism and excretion

Terbinafine is metabolized in the liver to form inactive metabolites. Most of the inactive metabolites (71%) are excreted in the urine, a smaller portion (22%) in the feces.

The T 1/2 is 11 to 17 h. There is no evidence of cumulation of the drug in the body.

Pharmacokinetics in special clinical cases

In patients with impaired hepatic or renal function the elimination rate of terbinafine from the body may be reduced.

Indications

Active ingredient

Composition

1 g of cream for external use contains:

The active ingredient:

terbinafine 10 mg.

Auxiliary substances:

sodium hydroxide,

benzyl alcohol,

sorbitan monostearate,

cetyl palmitate,

cetyl alcohol,

cetostearyl alcohol (cetyl alcohol 60%, stearyl alcohol 40%),

p> polysorbate 60,

isopropyl myristate,

purified water.

How to take, the dosage

The duration of therapy is determined by the nature and severity of the disease. Irregular use or premature termination of treatment leads to relapse of the disease.

Terbizil in the form of cream is used 1-2 times a day; with candidiasis of the skin and variegated shingles – up to 2 times a day. Before applying the cream the affected areas should be cleaned and dried. The cream is applied in a thin layer to the affected skin and adjacent areas and lightly rubbing. For infections accompanied by diaper rash (under the breasts, between the fingers, between the buttocks, in the groin area), the cream can be applied under a bandage.

The average duration of application of the cream:

Use in elderly patients

The same dosages of Terbisil are prescribed for elderly patients as for adults.

Patients with significant hepatic or renal impairment (creatinine clearance less than 50 ml/min or serum creatinine concentration greater than 300 µmol/L) the drug dose should be reduced by half.

Interaction

Drug interactions of Terbisil in cream form have not been described.

Special Instructions

It should be taken into account that if during treatment with Terbizil the patient has liver dysfunction (weakness, nausea of unclear etiology, lack of appetite, jaundice, darkened urine or pale stools) the drug should be stopped.

Hepatic transaminases should be monitored during treatment.

Terbisil in cream form is intended for external use only. Avoid contact of the cream with the mucous membrane of the eyes. If the cream comes into contact with the eyes, flush them with copious amounts of water and consult a physician if necessary.

When treating with Terbisil, general rules of hygiene should be followed to prevent the possibility of reinfection (through clothing or shoes).

Please note that irregular use or premature withdrawal of the drug leads to a recurrence of the disease.

If there is no improvement after 2 weeks of use of the drug in cream form, the diagnosis and sensitivity of the causative agent to terbinafine should be clarified.

The use in children

The use of the cream in children is only possible after careful assessment of the benefit-risk ratio.

Hypatic disorders

Patients with significant hepatic impairment should have the dose reduced by half.

Patients with significant renal impairment (creatinine clearance less than 50 ml/min or serum creatinine concentration greater than 300 µmol/L) the dose should be reduced by half.

Contraindications

High sensitivity to the components of the drug. Pregnancy and lactation (breast-feeding).

Side effects

Topical reactions: when using the cream rarely – itching, burning or hyperemia at the application site (requiring discontinuation of therapy).

Overdose

There are no data on overdose of terbinafine when used topically.

Pregnancy use

Due to the lack of data on the safety of the use of terbinafine in pregnant women, Terbizil in this category of patients is used only in cases where the expected positive effect exceeds the potential risk.

Terbinafine is excreted with breast milk, so the use of the drug during lactation is contraindicated.

Similarities