Latin name
Terbinafine
Release form
cream
Pharmacological action
Terbinafine is an antifungal agent. It has a wide spectrum of action against fungi that cause diseases of the skin, hair and nails, including:
dermatophytes, such as Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum (e.g. M. canis), Epidermophyton floccosum
yeast of the genus Candida (e.g. C. albicans) and Pityrosporum.
In low concentrations, terbinafine has a fungicidal effect on dermatophytes, molds and some dimorphic fungi. Activity against yeast fungi, depending on their type, can be fungicidal or fungistatic.
The mechanism of action is associated with a specific suppression of the early stage of sterol biosynthesis in the fungal cell. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes the death of the fungal cell. The action of terbinafine is carried out by inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. Terbinafine does not significantly affect the metabolism of hormones or other drugs.
Pharmacokinetics
When prescribing terbinafine orally in the skin, hair and nails, drug concentrations are created that provide a fungicidal effect.
After a single oral administration of terbinafine in a dose of 250 mg, its maximum plasma concentration is reached after 2 hours and is 0.97 mcg / ml. The half-absorption period is 0.8 hours, and the half-life is 4.6 hours. Although the bioavailability of terbinafine varies moderately under the influence of food, but not to the extent that dose adjustment is required.
Terbinafine binds significantly to plasma proteins (99%). It quickly penetrates the dermal layer of the skin and concentrates in the lipophilic stratum corneum. Terbinafine also penetrates the secretion of the sebaceous glands, which leads to the creation of high concentrations in the hair follicles, hair and in the skin, rich in sebaceous glands. Terbinafine has also been shown to penetrate the nail plates in the first few weeks after starting therapy.
Terbinafine is metabolized rapidly and substantially with the participation of at least seven isoenzymes of cytochrome P450, with the major role played by the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of the biotransformation of terbinafine, metabolites are formed that do not have antifungal activity and are excreted mainly in the urine. The final half-life is 17 hours. There is no evidence of cumulation of the drug in the body. No changes in the equilibrium concentration of terbinafine in plasma depending on age, but in patients with impaired renal or hepatic function, the rate of excretion of the drug may be slowed, which leads to higher concentrations of terbinafine in the blood.
With topical application of a spray or cream, less than 5% of the dose is absorbed, thus, the systemic effect of the drug is minimal.
Contraindications
Hypersensitivity, severe hepatocellular and renal failure, blood diseases, tumors, metabolic diseases, vascular pathology of the extremities, pregnancy, breast-feeding, children (up to 12 years).
Special instructions
Irregular use of terbinafine or premature discontinuation of treatment can lead to a relapse of the disease. If after 2 weeks of treatment for a skin infection, there is no improvement, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.
Systemic use for onychomycosis is justified only in the case of damage to most nails, the presence of severe subungual hyperkeratosis, and the ineffectiveness of previous local therapy. In the treatment of onychomycosis, a clinical laboratory-confirmed response is usually observed a few months after mycological cure and cessation of treatment, due to the rate of growth 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, terbinafine clearance may be reduced. During treatment, it is necessary to monitor the activity indicators of “liver” transaminases in the blood serum.
In rare cases, after 3 months of treatment, cholestasis and hepatitis occur. If there are signs of impaired liver function (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, dark urine, or discolored feces), the drug should be discontinued.
Prescribing terbinafine to psoriasis patients requires caution, as in very rare cases, terbinafine can trigger an exacerbation of psoriasis. In the treatment with terbinafine, general hygiene rules should be followed to prevent the possibility of reinfection through underwear and shoes. In the treatment process (after 2 weeks) and at the end it is necessary to produce antifungal treatment of shoes, socks and stockings.
Composition of
1 g of cream contains:
Active ingredient:
terbinafine hydrochloride 10 mg
Excipients:
benzyl alcohol,
polysorbate 60 (tween 60),
sorbitan monoste alcohol
isopropyl myristate,
cetyl palmitate,
sodium hydroxide,
purified water.
Dosage and Administration
Terbinafine can be applied to the skin 1 or 2 times a day. Before applying, it is necessary to clean and dry the affected areas. A thin layer is applied to the affected skin and adjacent areas and rubbed lightly. For infections accompanied by diaper rash (under the mammary glands, in the interdigital spaces, between the buttocks, in the inguinal region), the place of application of the cream can be covered with gauze, especially at night.
Average duration of treatment:
dermatomycosis of the trunk, limbs, legs: 1-2 weeks
dermatomycosis of the feet: 2-4 weeks
candidiasis of the skin: 1-2 weeks
versicolor versicolor: 2 weeks
mycosis of the nail plate: 3-6 months.
A decrease in the severity of clinical manifestations is usually observed in the early days of treatment. In the case of irregular treatment or premature termination of it, there is a risk of a renewed infection. If after two weeks of treatment there are no signs of improvement, the diagnosis should be verified.
Use of the drug in the elderly: There is no reason to assume that for the elderly it is necessary to change the dosage of the drug or that they have side effects that differ from those in younger patients.
Kids: Experience with children is limited.
Side effects
Sensation of heaviness and pain in the epigastric region, taste disturbance, loss of appetite, nausea, diarrhea, cholestasis, neutropenia, thrombocytopenia, skin allergic reactions, burning sensation, skin redness and itching in the area of application of the cream.
Storage conditions
Store at a temperature not exceeding 25 РC.
Term hodnosty
3 years
Deystvuyuschee substances
Terbinafine
Terms of the pharmacy
Over-the-counter
Form of Treatment
cream
Vertex, Russia
Terbinafine
Release form
cream
Pharmacological action
Terbinafine is an antifungal agent. It has a wide spectrum of action against fungi that cause diseases of the skin, hair and nails, including:
dermatophytes, such as Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum (e.g. M. canis), Epidermophyton floccosum
yeast of the genus Candida (e.g. C. albicans) and Pityrosporum.
In low concentrations, terbinafine has a fungicidal effect on dermatophytes, molds and some dimorphic fungi. Activity against yeast fungi, depending on their type, can be fungicidal or fungistatic.
The mechanism of action is associated with a specific suppression of the early stage of sterol biosynthesis in the fungal cell. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes the death of the fungal cell. The action of terbinafine is carried out by inhibiting the enzyme squalene epoxidase in the cell membrane of the fungus. This enzyme does not belong to the cytochrome P450 system. Terbinafine does not significantly affect the metabolism of hormones or other drugs.
Pharmacokinetics
When prescribing terbinafine orally in the skin, hair and nails, drug concentrations are created that provide a fungicidal effect.
After a single oral administration of terbinafine in a dose of 250 mg, its maximum plasma concentration is reached after 2 hours and is 0.97 mcg / ml. The half-absorption period is 0.8 hours, and the half-life is 4.6 hours. Although the bioavailability of terbinafine varies moderately under the influence of food, but not to the extent that dose adjustment is required.
Terbinafine binds significantly to plasma proteins (99%). It quickly penetrates the dermal layer of the skin and concentrates in the lipophilic stratum corneum. Terbinafine also penetrates the secretion of the sebaceous glands, which leads to the creation of high concentrations in the hair follicles, hair and in the skin, rich in sebaceous glands. Terbinafine has also been shown to penetrate the nail plates in the first few weeks after starting therapy.
Terbinafine is metabolized rapidly and substantially with the participation of at least seven isoenzymes of cytochrome P450, with the major role played by the isoenzymes CYP2C9, CYP1A2, CYP3A4, CYP2C8 and CYP2C19. As a result of the biotransformation of terbinafine, metabolites are formed that do not have antifungal activity and are excreted mainly in the urine. The final half-life is 17 hours. There is no evidence of cumulation of the drug in the body. No changes in the equilibrium concentration of terbinafine in plasma depending on age, but in patients with impaired renal or hepatic function, the rate of excretion of the drug may be slowed, which leads to higher concentrations of terbinafine in the blood.
With topical application of a spray or cream, less than 5% of the dose is absorbed, thus, the systemic effect of the drug is minimal.
Contraindications
Hypersensitivity, severe hepatocellular and renal failure, blood diseases, tumors, metabolic diseases, vascular pathology of the extremities, pregnancy, breast-feeding, children (up to 12 years).
Special instructions
Irregular use of terbinafine or premature discontinuation of treatment can lead to a relapse of the disease. If after 2 weeks of treatment for a skin infection, there is no improvement, it is necessary to re-determine the causative agent of the disease and its sensitivity to the drug.
Systemic use for onychomycosis is justified only in the case of damage to most nails, the presence of severe subungual hyperkeratosis, and the ineffectiveness of previous local therapy. In the treatment of onychomycosis, a clinical laboratory-confirmed response is usually observed a few months after mycological cure and cessation of treatment, due to the rate of growth 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, terbinafine clearance may be reduced. During treatment, it is necessary to monitor the activity indicators of “liver” transaminases in the blood serum.
In rare cases, after 3 months of treatment, cholestasis and hepatitis occur. If there are signs of impaired liver function (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, dark urine, or discolored feces), the drug should be discontinued.
Prescribing terbinafine to psoriasis patients requires caution, as in very rare cases, terbinafine can trigger an exacerbation of psoriasis. In the treatment with terbinafine, general hygiene rules should be followed to prevent the possibility of reinfection through underwear and shoes. In the treatment process (after 2 weeks) and at the end it is necessary to produce antifungal treatment of shoes, socks and stockings.
Composition of
1 g of cream contains:
Active ingredient:
terbinafine hydrochloride 10 mg
Excipients:
benzyl alcohol,
polysorbate 60 (tween 60),
sorbitan monoste alcohol
isopropyl myristate,
cetyl palmitate,
sodium hydroxide,
purified water.
Dosage and Administration
Terbinafine can be applied to the skin 1 or 2 times a day. Before applying, it is necessary to clean and dry the affected areas. A thin layer is applied to the affected skin and adjacent areas and rubbed lightly. For infections accompanied by diaper rash (under the mammary glands, in the interdigital spaces, between the buttocks, in the inguinal region), the place of application of the cream can be covered with gauze, especially at night.
Average duration of treatment:
dermatomycosis of the trunk, limbs, legs: 1-2 weeks
dermatomycosis of the feet: 2-4 weeks
candidiasis of the skin: 1-2 weeks
versicolor versicolor: 2 weeks
mycosis of the nail plate: 3-6 months.
A decrease in the severity of clinical manifestations is usually observed in the early days of treatment. In the case of irregular treatment or premature termination of it, there is a risk of a renewed infection. If after two weeks of treatment there are no signs of improvement, the diagnosis should be verified.
Use of the drug in the elderly: There is no reason to assume that for the elderly it is necessary to change the dosage of the drug or that they have side effects that differ from those in younger patients.
Kids: Experience with children is limited.
Side effects
Sensation of heaviness and pain in the epigastric region, taste disturbance, loss of appetite, nausea, diarrhea, cholestasis, neutropenia, thrombocytopenia, skin allergic reactions, burning sensation, skin redness and itching in the area of application of the cream.
Storage conditions
Store at a temperature not exceeding 25 РC.
Term hodnosty
3 years
Deystvuyuschee substances
Terbinafine
Terms of the pharmacy
Over-the-counter
Form of Treatment
cream
Vertex, Russia