ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
Agents Planned for Production
Spray. 1 ml of solution contains terbinafine hydrochloride 10 mg.
Cream. 1 g of cream contains terbinafine hydrochloride 10 mg.
Tablets. Each tablet contains terbinafine hydrochloride 250 mg.
Terbinafine, an allylamine, possesses a wide spectrum of antifungal activity. The mechanism of action lies in a specific inhibition of early stages sterol biosynthesis within fungal cell membranes. This results in ergosterol deficiency and accumulation of high squalene concentrations that finally leads to fungal cell death. Terbinafine acts inhibiting squalene epoxidase enzyme within fungal cell membranes. This enzyme does not belong to cytochrome system P450, therefore Erbinol does not affect the metabolism of hormones or any other drug substances. Terbinafine is effective against the dermatophytes group of fungi, yeast and mould, some species of dimorphic fungi. In low concentrations it also possesses fungicidal activity against dermatophytes (Trychophyton rubrum, Trychophyton mentagrophytes, Trychophyton verrucosum, Trychophyton violaceum, Trychophyton tonsurans, Microsporum canis, Epidermophyton floccosum), mould fungi (including Aspergillus, Cladosporium, Scopulariopsis brevicaulis). Its activity against Candida yeast fungi (mainly Candida albicans) can be both fungicidal and fungistatic depending on the species of fungi. When applied topically, terbinafine possesses activity against Pityrosporum orbiculare (Malassezia furfur) - chromophytosis causative agent.
Applied topically, terbinafine readily and rapidly crosses the dermal skin layer and is accumulated in corneal layer, nails and hair. Its absorption is less than 5%. The drug displays an imperceptible systemic action. When the drug is applied topically, there exists a possibility of its penetration into breast milk. After oral intake absorption is good (>70%); systemic bioavailability is around 50%. Food intake does not affect bioavailability of terbinafine. Terbinafine is transformed in pharmacologically inactive metabolites which undergo mainly urinary excretion.
-mycotic skin infections: foot mycosis, ringworm of the body (tinea corporis), induced by dermathophyts Trichophyton spp., including Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton verrucosum, Trichophyton violaceum, Microsporum canis and Epidermophyton floccosum;
- scaly skin disease (tinea versicolor), induced by Malassezia furfur; -skin candidiasis; - onychomycoses caused by dermathophyts.
DOSAGE AND ADMINISTRATION
Spray and cream for external use only. Before applying the drug, it is important to clean and thoroughly dry the affected skin area(s). The drug is sprayed over the affected and adjacent skin areas in the amount necessary for their sufficient moisturizing, and slightly rubbed in. For adults and children aged 12 years old and older the drug is prescribed 1 or 2 times daily depending on indications. Treatment duration depends on indications and the degree of severity of the disease. In treatment of foot, body, crurae dermathomycosis the duration of therapy is 1 week, once daily. In treatment of scaly skin disease (tinea versicolor) the average duration of therapy is 1 week, two times daily. Generally, an improvement of clinical symptoms is observed in the early period of treatment. In case of irregular therapy or its preterm discontinuation there is a risk of recurrence of the infection. If there is no therapeutic response after one week of treatment, the diagnosis should be revised.
Tablets are administered 250 mg once daily. Duration of therapy in ringworm of the body and skin candidiasis is 2-4 weeks, in onychomycoses caused by dermathophyts 6-12 weeks.
Hypersensitivity to terbinafine or any other excipient of the formulation.
In case of topical application: redness of the skin at the site of application, itch or burning sensation. Rarely: allergic reactions.
In case of oral intake: headache and gastrointestinal symptoms (taste perversion, loss of appetite, flatulence, dyspepsia, abdominal pain, diarrhea, hepatobiliary problems, liver insufficiency), skin reactions (urticaria, rush, Stevens-Johnson syndrome, toxic epidermal necrosis), artralgia, myalgia, anaphylactoid reactions, neutropenia, agranulocytosis, thrompocytopenia.
Preparation is not recommended for children under 12 years. In pregnancy preparation can be used only in case potential benefit exceeds risk for fetus. Breastfeeding should be interrupted during course of therapy.
Concomitant oral intake of Erbinol and hormonal oral contraceptives can cause irregularities of menstrual cycle. Rifampicin and cimetidine could increase elimination of terbinafine.
20 ml of spray for external use in a polyethylene vial with a pulverizer and a cap. One vial with a leaflet in a carton box.
20 g of 1% cream for external use in aluminum tube. One tube with a leaflet in a carton box.
7 tablets in blister. 2 blisters with a leaflet in a carton box.