TERBINAFINE-VERTEX 250 mg 10 pcs. VERTEX AO tablets

Composition of Terbinafine ointment

The main component is terbinafine hydrochloride. In one tube it is contained in the amount of 1g per 100g of composition. As additional substances, it contains rare cross-linked polyacrylic acid in the amount of 1.5 g, as well as 10 g of propylene glycol, 5 g of petroleum jelly, 0.4 g of sodium hydroxide. A large share of the volume is purified water - here it is 81g.

Terbinafine is available both as an ointment and as a gel or cream. The product for topical use is packaged in aluminum tubes, which are placed in cardboard packages, 1 piece each.

pharmachologic effect

Terbinafine has a pronounced antifungal effect. The ointment is intended for topical use. It is effective in combating dermatophytes, varieties of molds and dimorphic fungi. When applying a small amount of the product, it is possible to achieve a fungicidal effect.

In relation to yeast fungi, Terbinafine can have both fungicidal and fungistatic effects. Its activity is mainly manifested in the treatment of skin lesions by representatives of the genus Candida albicans. The ointment affects biosynthesis processes during the early stage of sterol formation, namely, a deficiency of ergosterol is formed and a simultaneous increase in squalene content. This imbalance of chemical bonds leads to the death of fungal cells. The ointment is safe in relation to the cell membrane of the human body. It does not have any effect on the production of hormones, the functioning of internal organs and the effect of other medications. No more than 5% of the drug is absorbed into the bloodstream if a dense layer is applied. The systemic effect in this case is insignificant.

Modern possibilities of using terbinafine for the treatment of fungal diseases

The incidence rate increases significantly in patients in older age groups, regardless of gender. According to foreign researchers, onychomycosis affects from 2 to 18.5% of the total population of the planet, and in the age group of 70 years and older, 50% of the world’s population is affected by this disease [1,8]. According to various authors, fungal infections of the feet are observed in a third of all European residents [18,20]. As a rule, the development of onychomycosis is preceded by mycosis of the feet - according to our data, only 30% of patients had isolated onychomycosis, in the remaining 70% of patients it was combined with mycosis, which began before the fungal infection of the nails [2]. Thus, treatment of mycosis of the feet is the prevention of the development of onychomycosis. Very often, dermatologists are faced with insufficient awareness of patients - the latter do not know about the presence of a fungal infection, even seeing manifestations on the skin in the form of peeling, intertrigo, hyperkeratosis, and attribute this to physiological characteristics or age-related changes. On the other hand, some patients, seeing changes in the nail plates, regard this as onychomycosis and begin to treat it themselves with all available means. In the presence of mycosis of smooth skin without affecting the nails and involving the hair in the process, a cure can be achieved using only topical antimycotics. One of the most active antimycotics is terbinafine. It belongs to allylamine derivatives. In terms of the breadth of the spectrum of antifungal action, this drug surpasses all other antifungal drugs: polyene antibiotics, azoles (imidazole derivatives - clotrimazole, ketoconazole, etc., as well as first generation triazoles - itraconazole, fluconazole, etc.) and echinocandins. In recent years, many studies have been conducted confirming the high effectiveness and safety of terbinafine (Lamisil) in the treatment of fungal infections. The undoubted advantages of this drug include a large number of its forms for external use - cream, dermgel, spray and film-forming solution for the treatment of types of mycosis. Terbinafine in the form of a cream is ideal for squamous and squamous-hyperkeratotic forms. In the first case, it is enough to apply the cream to the affected area once a day. within 7 days [15]. For the treatment of hyperkeratotic forms of mycosis, use the drug 2 times a day. within 2 weeks. makes it possible to achieve clinical and mycological cure. In a study conducted by Yu.N. Perlamutrov and K.B. Olkhovskaya, it has been shown that complete mycological cure is achieved with the use of terbinafine 1 time per day. within 2 weeks. occurred in 80% of patients, and 2 times a day. – in 93%. At the same time, by the end of the course of treatment, the disappearance of peeling, itching and healing of deep and superficial cracks was observed in patients in both groups, but when using the cream 2 times a day. these symptoms resolved more quickly [4]. For intertriginous and dyshidrotic forms, it is appropriate to prescribe dermgel or spray - they have a pronounced antipruritic and drying effect. It is also convenient to prescribe the spray in the presence of lesions on smooth skin (lichen versicolor, microsporia) in the folds and on the scalp. So, according to A.A. Haldina et al., when applying both spray and dermgel to lesions in large folds, etiological cure was observed in 100% of cases, regardless of the nature of mycosis (Tr. rubrum, Ep. floccosum, C. albicans). When analyzing the dynamics of regression of skin symptoms, it was revealed that when using the spray, the regression of clinical symptoms is somewhat ahead of that when using dermgel, this is especially noticeable with the regression of itching and maceration [7]. There is a high effectiveness of using spray and dermgel for the treatment of patients with pityriasis versicolor. According to L.P. Kotrekhova et al., the effectiveness of dermgel and spray therapy was 94.8 and 93.8%, respectively. At the same time, patients note the ease of use and good organoleptic properties of the drug, such as the absence of greasiness and oily sheen of the skin. The hygroscopic properties of the drug made it possible to apply it to skin folds even in obese patients [3]. A new, and certainly promising form is a film-forming solution, which is applied to the skin of the feet once. N.N. Potekaev et al. treated 20 patients with various forms of mycosis of the feet with Lamisil Uno. Clinical and mycological cure occurred in 80% of patients by the 10th day of observation. The drug was ineffective in the squamous-hyperkeratotic form. For erased, squamous and intertriginous forms, the effectiveness is 100%. I would especially like to note that single use of the drug is very convenient for patients [5]. A randomized, double-blind, placebo-controlled study was conducted on the effectiveness of a single application of a 1% film-forming solution of terbinafine in 324 patients with mycosis of the feet. The result was assessed after 6 weeks. after using the drug. The study found negative culture, microscopy, and mycological cure rates of 91%, 81%, and 78%, respectively, while the placebo response rate was 17% [11]. Another very important point is the possibility of curing mycosis in a short time - with squamous and intertriginous forms of the lesion, the disease is cured in 1 week, while azole drugs must be used for 4 weeks. [17,18]. A longer course of therapy often leads to non-compliance with the treatment regimen; patients stop using the drug after visible improvements and are not treated further, which leads to relapse of the disease. In some cases (with damage to the nail plates, a common skin process, hair involvement), local antifungal therapy is not effective enough, and there is a need to prescribe a systemic drug, the most effective and safe of which is terbinafine [19]. Terbinafine has a fungicidal effect on dermatophytes, molds and some dimorphic fungi; on yeast fungi, depending on their type, it has a fungistatic or fungicidal effect [13,16]. The pronounced antimycotic effect of terbinafine also manifests itself in vivo, which is facilitated by its pharmacokinetics. After oral administration, the maximum concentration of terbinafine in the blood is reached within 2 hours, the drug is almost completely bound to plasma proteins. Due to its lipophilicity, terbinafine quickly diffuses through the dermis and accumulates in the stratum corneum and nail plates, and is also excreted with sebum, resulting in high concentrations of the drug in hair follicles and hair. Stable concentrations of terbinafine in tissues are achieved 10–14 days after the start of oral administration, the half-life of its elimination varies from 24 to 156 days, as a result of which the drug remains in the nail plates for a long time after stopping its use [8,10]. It is known that fungal infections of the scalp can be successfully treated with terbinafine. To confirm this, 3 groups of children aged 2 to 14 years with a confirmed diagnosis of trichophytosis were treated with griseofulvin for a month and terbinafine for 2 weeks. and 1 month It was shown that the effectiveness of therapy was approximately the same and amounted to 100% with griseofulvin, 95% with a 2-week course of terbinafine and 94.1% with a monthly dose [12]. A study was conducted on the effectiveness of oral terbinafine for the treatment of a hyperkeratotic form of mycosis of the feet with a torpid course. The drug at a dose of 125 mg was prescribed daily for 1 month. It was found that the maximum concentration of the drug (247.8 ng) in the stratum corneum of the epidermis was determined by the end of 1 week. treatment, which is 50 times the minimum inhibitory concentration for dermatophytes. After 6 weeks the concentration of the drug decreased to 50.73 ng, and after 8 weeks. terbinafine was no longer detectable in the skin. The effectiveness of therapy was 95% [14]. The low potential for drug interactions with other drugs is also important, because Onychomycosis often affects older people who are forced to take a large number of different medications for other diseases [13]. Thus, based on the analysis of literature data, we can conclude that terbinafine (Lamisil) is a highly effective drug for the treatment of fungal infections, has a large number of different forms, which significantly expand the possibilities of antifungal therapy. Literature 1. Malcolm B. Athlete's foot // Attending physician. 1998. No. 6. 2. Vasenova V.Yu. Immunopathogenesis, morphofunctional characteristics, clinical picture, complex therapy and prevention of onychomycosis: Abstract of thesis. ... doc. honey. Sci. M., 2008. 3. Kotrekhova L.P., Vasilyeva N.V., Raznatovsky K.I., Piotrovskaya I.V. Clinical efficacy and safety of terbinafine (Lamisil spray, Lamisil dermgel) in the treatment of pityriasis versicolor // Clinical dermatology and venereology. 2007. No. 3. P. 35–38. 4. Perlamutrov Yu.N., Olkhovskaya K.B. Optimization of therapy for mycoses of the feet in women using 1% Lamisil cream // Clinical dermatology and venereology. 2006. No. 2. P. 78–80. 5. Potekaev N.N., Serov D.G., Dvoryankova E.V., Zhukovsky R.O. Effective therapy of mycoses of the feet with a single use of a new external form of terbinafine - a film-forming solution of Lamisil Uno // Clinical Dermatology and Venereology. 2008. No. 4. pp. 85–88. 6. Sergeev A.Yu., Ivanov O.L., Sergeev A.Yu. and others. Study of modern epidemiology of onychomycosis // Bulletin of Dermatology and Venereology. 2002. No. 3. P. 31–35. 7. Khaldin A.A., Tsykin A.A., Izyumova I.M. Clinical and etiological effectiveness of 1% Lamisil® spray in the treatment of fungal infections of large skin folds // Russian Journal of Skin and Venereal Diseases. 2007. No. 1. P. 56. 8. Baran R. Onychomycosis: the current approach to diagnosis and therapy. London: Malden MA, 1999. 9. Chen SCA, Sorrell TC New Drugs, Old Drugs. Antifungal agents // Med. J. Austral. 2007. Vol. 187. No. 7. R. 404–409. 10. Cribier BJ, Bakshi R. Terbinafin in the treatment of onychomycosis: a review of its efficacy in high-risk populations and in patients with nondermatophyte infections // BJ Dermatol. 2004. Vol.150. R. 414–420. 11. De Chauvin MF, Viguie-Vallanet C., Kienzler JL, Larnier C. Novel, single-dose, topical treatment of tinea pedis using terbinafine: results of a dose-finding clinical trial. Mycoses. 2008 Jan. Vol. 51(1). R. 1–6. 12. Deng S., Hu H., Abliz P., Wan Z., Wang A., Cheng W., Li R. A random comparative study of terbinafine versus griseofulvin in patients with tinea capitis in Western China. Mycopathologia. 2011 Nov. Vol. 172(5). R. 365–372. 13. Gianni C. Update on antifungal therapy with terbinafine // G Ital Dermatol Venereol. 2010 Jun. Vol. 145(3). R. 415–424. 14. Kikuchi I., Tanuma H., Morimoto K., Kawana S. Usefulness and pharmacokinetic study of oral terbinafine for hyperkeratotic-type tinea pedis // Mycoses. 2008 Nov. Vol. 51(6). R. 523–531. 15. Korting HC, Kiencke P., Nelles S., Rychlik R. Comparable efficacy and safety of various topical formulations of terbinafine in tinea pedis irrespective of the treatment regimen: results of a meta-analysis // Am J Clin Dermatol. 2007. Vol. 8 (6). R. 357–364. 16. Revankar SG, Nailor MD, Sobel JD Use of terbinafine in rare and refractory mycoses // Future Microbiol. 2008 Feb. Vol. 3(1). R. 9–17. 17. Schafer–Korting M., Schoellmann C., Korting HC Fungicidal activity plus reservoir effect allow short treatment courses with terbinafine in tinea pedis // Skin Pharmacol Physiol. 2008. Vol. 21(4). R. 203–210. 18. Schmid–Wendtner MH, Korting H. Topical terbinafine. Reduction of duration of therapy for tinea pedis // Hautarzt. 2008 Dec. Vol. 59 (12). R. 986–991. 19. Singal A., Khanna D. Onychomycosis: Diagnosis and management // Indian J Dermatol Venereol Leprol. 2011 Nov–Dec. Vol. 77(6). R. 659–672. 20. Stock I. Antimycotic therapy of Tinea pedis and other foot mycoses // Med Monatsschr Pharm. 2008 Jul. Vol. 31(7). R. 247–258. Van Duyn Graham L., Elewski BE. Recent updates in oral terbinafine: its use in onychomycosis and tinea capitis in the US // Mycoses. 2011 Nov. Vol. 54 (6). R. 679–685.

Indications for use of Terbinafine

The main indication for prescribing Terbinafine ointment is damage to the skin by a fungal infection. First of all, these are mycoses of the skin of the foot. In addition to fungus on the legs, the remedy treats fungal infections of the groin area, which experts call tinea cruris. In addition, smooth areas of the body infected with fungus can also be treated with ointment.

Diaper rash, in the absence of timely and adequate skin care, can become a breeding ground for the proliferation of pathogenic microorganisms. Fungi of the genus Candida especially love this humid environment. This is a yeast type that quickly spreads in folds, on the crooks of the arms and fingers, as well as on hairy areas of the body (head, armpits, groin). Treatment with Terbinafine ointment makes it possible to get rid of this pathogen.

Signs of lichen versicolor are also a reason to prescribe Terbinafine. Mycosis is a common skin disease that affects not only adults, but also children. The first signs of the spread of a fungal infection are the following markers:

Redness on the skin, usually with clearly defined boundaries of the source of infection. The borders may be uneven and irregular in shape.
The edges of the lesion often have a whitish tint, especially for lesions of fungi of the genus Candida.
The inflamed area is itchy.
The surface of the skin of the affected area peels off.
At the site of inflammation, vesicles with serous contents appear. Violation of the surface of the bubbles leads to the separation of liquid and the formation of crusts.

Fungal infections are transmitted by contact and airborne droplets. In addition, failure to comply with hygiene standards provokes the spread of mycoses. Therefore, when visiting baths, saunas, public showers and other public places with high humidity, it is necessary to avoid contact of bare feet with the floor.

Mycosis can also appear as a result of wearing low-quality shoes made from non-breathable materials. It is also not recommended to wear synthetic socks in closed shoes.

Terbinafine tablets

Registration number: R No. LSR-008787/10

Trade name of the drug: Terbinafine-MFF.

International nonproprietary name: Terbinafine.

Dosage form: Tablets.

Composition per tablet: Active substance:

Terbinafine hydrochloride 281 mg (corresponding to 250 mg terbinafine base).

Excipients (to obtain a tablet weighing 0.390 g):

Colloidal silicon dioxide – 2 mg
Calcium stearate monohydrate (calcium stearate 1-water) – 2 mg
Potato starch - 29 mg
Microcrystalline cellulose (MCC-200) – 47 mg
Lactose monohydrate – 8 mg
Crospovidone (polyplasdone XL-10) – 8 mg
Crospovidone (polyplasdon XL) – 8 mg
Povidone K 90 (plasdon K-90) - 5 mg

Description: Tablets are white or almost white, with a slight specific odor, flat-cylindrical in shape with a chamfer and a score.

Pharmacotherapeutic group: Antifungal agent.

ATX code: D01BA02

Pharmacodynamics: Terbinafine belongs to the group of allylamines and has a wide spectrum of antifungal action. In low concentrations it has a fungicidal effect on dermatophytes Trichophyton spp. (T. rubrum, T. mentagrophytes, Ttonsurans, T. verrucosum, Tviolaceum), Microsporum canis, Epidermophyton floccosum, molds (for example, Scopulariopsis brevicaulis), yeasts, 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 enzyme squalene epoxidase. When administered orally, it is not effective in the treatment of pityriasis versicolor caused by Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Pharmacokinetics: When taken orally, more than 70% is well absorbed; absolute bioavailability due to the “first pass” effect is reduced by 40%. After a single oral dose of 250 mg, the time to reach maximum concentration (TCmax) is about 2 hours; maximum concentration (dmax) - 1 μg/ml. The area under the curve of the infection localization is 2 - 6 weeks; for mycoses of other parts of the body, legs or torso: 2 - 4 weeks; for mycoses caused by fungi of the genus Candida: 2 - 4 weeks; for mycoses of the scalp caused by fungi of the genus Microsporum: more than 4 weeks.

Children: With body weight from 20 to 40 kg: 125 mg 1 time per day. For body weight more than 40 kg: 250 mg once a day. The duration of treatment for mycoses of the scalp is about 4 weeks; for infection with Microsporum canis it can be longer.

Elderly patients are prescribed the drug in the same doses as adults. For patients with hepatic and renal insufficiency, terbinafine is prescribed at a dose of 125 mg once a day.

Side effect:

Dyspeptic disorders (decreased appetite, nausea, diarrhea, feeling of fullness in the stomach, abdominal pain)
Allergic skin reactions (urticaria, rash)
Musculoskeletal reactions (arthralgia, myalgia), aggravation of systemic lupus erythematosus

Disorders of taste, including their loss (recovery occurs within several weeks after cessation of treatment).

Rarely (with a frequency of 0.01 - 0.1%) a hepatotoxic effect is observed (increased activity of “liver” transaminases, liver failure). Malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), psoriasis-like skin rashes, exacerbation of psoriasis, anaphylactoid reactions, agranulocytosis or thrombocytopenia, neutropenia, lymphopenia.

Overdose: Symptoms: Nausea, vomiting, headache, dizziness, pain in the lower abdomen, in the epigastric region, frequent urination.

Treatment: Gastric lavage followed by the use of activated charcoal and/or symptomatic therapy.

Interaction with other drugs: Inhibits the CYP2D6 isoenzyme and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), inhibitors monoamine oxidase B (eg, selegiline) and antipsychotic (eg, chlorpromazine, haloperidol) agents. Drugs that induce cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the metabolism and elimination of terbinafine from the body. Drugs that inhibit cytochrome P450 isoenzymes (for example, cimetidine) can slow down the metabolism and elimination of terbinafine from the body. If these drugs are used concomitantly, a dose adjustment of terbinafine may be required. Menstrual irregularities are possible when taking terbinafine and oral contraceptives simultaneously. Terbinafine reduces the clearance of caffeine by 21% and prolongs its half-life by 31%. Does not affect the clearance of phenazone, digoxin, warfarin. When used together with ethanol or drugs that have hepatoxic effects, there is a risk of developing drug-induced liver damage.

Special instructions: Irregular use of terbinafine or premature cessation of treatment may lead to relapse of the disease. The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails with onychomycosis at the beginning of the course of treatment. If after 2 weeks of treatment of a skin infection there is no improvement in the condition, 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 total damage to most nails, the presence of severe subungual hyperkeratosis, and the ineffectiveness of previous local therapy. When treating onychomycosis, a laboratory-confirmed clinical response is usually observed several months after mycological cure and cessation of treatment, which is due to the rate of regrowth of a healthy nail. Removal of nail plates is not required when treating onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks. In the presence of liver disease, the clearance of terbinafine may be reduced. During treatment, it is necessary to monitor the activity of “liver” transaminases in the blood serum. In rare cases, cholestasis and hepatitis occur after 3 months of treatment. If signs of liver dysfunction occur (weakness, persistent nausea, decreased appetite, excessive abdominal pain, jaundice, dark urine or discolored stools), the drug should be discontinued. Prescribing terbinafine to patients with psoriasis requires caution, because in very rare cases, terbinafine can cause 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 treatment (after 2 weeks) and at the end it is necessary to carry out antifungal treatment of shoes, socks and stockings.

Release form: Tablets 250 mg. 10 or 14 tablets in a blister pack made of polyvinyl chloride film and aluminum foil with thermovarnish. One or two blister packs along with instructions for use are placed in a cardboard pack.

Shelf life: 2 years. Do not use after expiration date.

Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Conditions for dispensing from pharmacies: By prescription.

Instructions

The ointment is used strictly externally. Recommended for use by adults and children over 12 years of age. Before applying the product, it is necessary to remove all contaminants from the surface of the skin and dry it. A small amount of cream is rubbed into the lesion, covering a small area beyond the edges of the inflammation. Repeat the procedure in the morning and evening.

The course of treatment depends on the degree of damage and the type of fungal infection:

smooth skin, including areas on the back, abdomen and lower legs, require 1 week of treatment;
foot fungus goes away within 8-9 days of using Terbinafine ointment;
treatment of candidiasis can last up to 2 weeks;
It also takes 10 to 14 days to get rid of tinea versicolor.

If the use of the ointment does not give the desired effect over time, or during treatment there is a clear progression of the disease, accompanied by growth of the affected area, it is necessary to contact a specialist to prescribe systemic antifungal agents or to change the treatment regimen with local agents.

Terbinafine cream - instructions

Unlike ointment, cream does not penetrate so deeply into the skin. Part of the applied layer is often rubbed off on clothing and surfaces with which the affected area of the body comes into contact. Therefore, the use of cream can be increased up to 3 times a day.

The advantage of the cream is its effectiveness even on moderately wet surfaces, which is especially important for fungal skin infections. If it is not possible to dry the surface due to the constant release of liquid, it is better to buy a cream, since the ointment in this case will be ineffective.

Terbinafine-vertex 250 mg 10 pcs. pills

pharmachologic effect

Terbinafine is an allylamine that has a broad spectrum of activity against fungi that cause diseases of the skin, hair and nails, including dermatophytes.
At low concentrations it has a fungicidal effect on dermatophytes Trychophyton spp. (T. rubrum, T. mentagrophytes, T. verrucosum, T. tonsurans, T. violaceum), Microsporum canis, Epidermophyton floccosum, molds (for example, Aspergillus, Cladosporium, Scopulariopsis brevicaulis), yeasts, mainly Candida albicans. In low concentrations, terbinafine has a fungicidal effect against dermatophytes, molds and some dimorphic fungi. Activity against yeast fungi, depending on their type, can be fungicidal or fungistatic. Terbinafine specifically inhibits the early stage of sterol biosynthesis in the fungal cell. This leads to ergosterol deficiency and intracellular accumulation of squalene, which causes the death of the fungal cell. Terbinafine works 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 affect the metabolism of hormones or other drugs.

When Terbinafine is taken orally, concentrations of the drug are created in the skin, hair and nails, providing a fungicidal effect.

When administered orally, it is not effective in the treatment of pityriasis versicolor caused by Pityrosporum ovale, Pityrosporum orbiculare (Malassezia furfur).

Composition and release form Terbinafine-vertex 250 mg 10 pcs. pills

Tablets - 1 tablet:

Active ingredients: terbinafine (in the form of hydrochloride) - 250 mg;
Excipients: microcrystalline cellulose 0.08 g, hyprolose (hydroxypropylcellulose) 0.025 g, croscarmellose sodium 0.08 g, colloidal silicon dioxide 0.01 g, calcium stearate 0.005 g, lactose monohydrate to obtain a tablet weighing 0.5 g.

Description of the dosage form

Tablets of white or white with a yellowish tint with a chamfer and a score.

Directions for use and doses

For adults:

Inside, after eating. Usual dose: 250 mg 1 time per day.

Children over 3 years old:

For body weight from 20 to 40 kg - 125 mg 1 time per day.

For body weight more than 40 kg - 250 mg 1 time per day.

The duration of the course of treatment and dosage regimen are established individually and depend on the localization of the process and the severity of the disease.

Onychomycosis: duration of therapy is on average 6-12 weeks. If the nails of the fingers and toes are affected (with the exception of the big toe), or if the patient is young, the duration of treatment may be less than 12 weeks. For a big toe infection, a 3-month course of treatment is usually sufficient.

Some patients whose nail growth rate is reduced may require a longer treatment period.

Fungal skin infections: the duration of treatment for interdigital, plantar or “sock” localization of infection is 2-6 weeks; for mycoses of other parts of the body: legs - 2-4 weeks, torso - 2-4 weeks; for mycoses caused by fungi of the genus Candida - 2-4 weeks; for mycoses of the scalp caused by fungi of the genus Microsporum - more than 4 weeks.

The duration of treatment for mycoses of the scalp is about 4 weeks; for infection with Microsporum canis, it may be longer.

Elderly patients are prescribed the drug in the same doses as adults.

For patients with liver or kidney failure - 125 mg 1 time per day.

Pharmacokinetics

After a single oral dose of terbinafine at a dose of 250 mg, its Cmax in plasma is reached after 2 hours and is 0.97 mcg/ml. The half-life of absorption is 0.8 hours, the half-life of distribution is 4.6 hours. Communication with blood plasma proteins - 99%. When taken simultaneously with food, no dose adjustment is required.

Terbinafine quickly penetrates the skin and accumulates in the sebaceous glands. High concentrations are created in the hair follicles and hair; after a few weeks of use it penetrates into the nail plates. Accumulates in the stratum corneum of the skin (the concentration increases 10 times on day 2 after taking 250 mg, 70 times on day 12) and nails (the diffusion rate exceeds the rate of nail growth) in concentrations that provide a fungicidal effect.

Terbinafine is metabolized in the liver to form inactive metabolites. T1/2 is 16-18 hours. T1/2 of the terminal phase is 200-400 hours. It is excreted mainly by the kidneys (70%) in the form of metabolites, as well as through the skin. There is no evidence of drug accumulation in the body. Excreted in breast milk. There have been no changes in steady-state plasma concentrations of terbinafine with age, but patients with impaired renal or hepatic function may have a slower rate of elimination of the drug, resulting in higher blood concentrations of terbinafine.

Indications for use Terbinafine-vertex 250 mg 10 pcs. pills

fungal diseases of the skin and nails (onychomycosis) caused by Trychophyton spp. (T. rubrum, T. mentagrophytes, T.
verrucosum, T. tonsurans, T. violacium), Microsporum spp. (M. canis, M. gypseum) and Epidermophyton floccosum;
mycoses of the scalp (trichophytia, microsporia);
severe, widespread dermatomycosis of smooth skin of the trunk and extremities, requiring systemic treatment;
candidiasis of the skin and mucous membranes.

Contraindications

chronic or active liver disease;
chronic renal failure (creatinine clearance less than 50 ml/min);
children's age (up to 3 years) and with a body weight of up to 20 kg (for this dosage form);
lactation period;
lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
hypersensitivity to terbinafine or other components of the drug.

Caution should be used when:

renal failure (with CC more than 50 ml/min);
alcoholism;
inhibition of bone marrow hematopoiesis;
tumors;
metabolic diseases;
occlusive diseases of the vessels of the extremities;
cutaneous lupus erythematosus or systemic lupus erythematosus.

Application Terbinafine-vertex 250 mg 10 pcs. pills during pregnancy and breastfeeding

Since no studies have been conducted on the safety of Terbinafine in pregnant women, the drug should not be prescribed during pregnancy. Terbinafine is excreted in breast milk, so its use is contraindicated during breastfeeding. Contraindicated in children under 3 years of age and weighing up to 20 kg.

special instructions

Irregular use or early termination of treatment increases the risk of relapse.

The duration of therapy can be influenced by factors such as the presence of concomitant diseases, the condition of the nails with onychomycosis at the beginning of the course of treatment.

If after 2 weeks of treatment of a skin infection there is no improvement in the condition, 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 total damage to most nails, the presence of severe subungual hyperkeratosis, and the ineffectiveness of previous local therapy.

When treating onychomycosis, a laboratory-confirmed clinical response is usually observed several months after mycological cure and cessation of treatment, which is due to the rate of regrowth of a healthy nail.

Removal of nail plates is not required when treating onychomycosis of the hands for 3 weeks and onychomycosis of the feet for 6 weeks.

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

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

Prescribing terbinafine to patients with psoriasis requires caution, because in very rare cases, terbinafine can cause 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 treatment (after 2 weeks) and at the end it is necessary to carry out antifungal treatment of shoes, socks and stockings.

Impact on the ability to drive vehicles and operate machinery

There is no data on the effect of Terbinafine on the ability to drive vehicles and machines.

Overdose

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

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

Side effects Terbinafine-vertex 250 mg 10 pcs. pills

Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less 1/10000, including individual cases.

From the digestive system: very often - a feeling of fullness in the stomach, loss of appetite, dyspepsia, nausea, abdominal pain, diarrhea; rarely - liver dysfunction; very rarely - liver failure, even death.

From the hematopoietic organs: very rarely - neutropenia, agranulocytosis, thrombocytopenia, pancytopenia.

Allergic reactions: very rarely - anaphylactoid reactions (including angioedema).

From the nervous system: often - headache; Uncommon: taste disturbance, including ageusia.

From the skin: very often - skin reactions (including rash, urticaria); very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, psoriasis-like rash, exacerbation of existing psoriasis, alopecia.

From the musculoskeletal system: very often - arthralgia, myalgia.

Other: very rarely - fatigue; cutaneous lupus erythematosus, SLE or their exacerbation.

Drug interactions

Inhibits the CYP2D6 isoenzyme and disrupts the metabolism of drugs such as tricyclic antidepressants and selective serotonin reuptake inhibitors (for example, desipramine, fluvoxamine), beta-blockers (metoprolol, propranolol), antiarrhythmics (flecainide, propafenone), monoamine oxidase B inhibitors (for example, selegiline ) and antipsychotic (eg, chlorpromazine, haloperidol) agents.

Drugs that induce cytochrome P450 isoenzymes (for example, rifampicin) can accelerate the metabolism and elimination of terbinafine from the body. Medicines that are inhibitors of cytochrome P450 isoenzymes (for example, cimetidine) can slow down the metabolism and elimination of terbinafine from the body. If these drugs are used concomitantly, a dose adjustment of terbinafine may be required.

Menstrual irregularities are possible when taking terbinafine and oral contraceptives simultaneously. Terbinafine reduces the clearance of caffeine by 21% and prolongs its half-life by 31%. Does not affect the clearance of phenazone, digoxin, warfarin.

When used together with ethanol or drugs that have hepatotoxic effects, there is a risk of developing drug-induced liver damage.