Terbinafine topical

Future Antimycotics for Systemic Treatment. Two new antimycotics for systemic use have now reached the stage of clinical development. The first is a triazole and fluoride analogue of itraconazole. This compound (saperconazole) is extremely active 2i 2cm.%. Jisperpillus spp. and slightly more soluble. Consequentiy, intravenous adruinistration might be possible (34). The second molecule is terbinafine [91161 -71 -6] an aHylamine, C21H25N, that appears to be particularly active against dermatophytes, just like topical naftifine (35). 

Onychomycosis is a chronic infection that rarely remits spontaneously. Adequate treatment is essential to prevent spread to other sites, secondary bacterial infections, cellulitis, or gangrene. Due to the chronic nature and impenetrability of nails, topical agents have low efficacy rates for treating onychomycosis. Oral agents that can penetrate the nail matrix and nail base, such as itraconazole and terbinafine, are more effective than ciclopirox lacquer. Itraconazole and terbinafine demonstrate mycological cure rates of 62%37 and 76%,38 respectively, while ciclopirox has a cure rate of 29% to 36%.39... 

Topical agents with minimal pregnancy risk include bacitracin, benzoyl peroxide, ciclopirox, clindamycin, erythromycin, metronidazole, mupi-rocin, permethrin, and terbinafine. 

The use of topical antifungal agents (imidazole antifungals and terbinafine) is the first-line of treatment in athlete s foot. Patients should be advised to be persistent in treatment and that application of the product should be continued for about 10 days after all traces have disappeared. This will ensure eradication. Patient should be educated on non-pharmacotherapeutic measures and adjunctive therapy that contribute towards the management of the condition. The area should be washed regularly and dried thoroughly as... 

Rub topical terbinafine well into the affected and surrounding areas and do not cover the treated area with an occlusive dressing... 

Topical terbinafine should be used for at least 1 week but no more than 4 weeks... 

Terbinafine and naftifine are allylamines available as topical creams (see Chapter 61). Both are effective for treatment of tinea cruris and tinea corporis. These are prescription drugs in the USA. 

Terbinafine (Lamisil) Tolnaftate (Tinactin) Tretinoin, Topical [Retinoic Acid] (Retin-A, Retin-A Micro Avita,... 

Terbinafine (Lamisil) is an allylamine with activity similar to that of naftifine hydrochloride. It is available as a 1% cream and solution for the topical treatment of dermatophyte infections. 

Management Besides measures as boiling or disinfecting clothes, topical antimycotic therapy is the treatment of choice. Ointments should be applied several centimeters beyond the border of the lesion and treatment should be continued over at least 1 week after clearance of the lesions. However, these recommendations are seldom followed, resulting in chronic or recurrent disease (apart from the problem of resistance). In these cases, and when multilocular lesions or an infection of extensive spread have to be treated, systemic antifun-gals usually for 1-2 weeks are necessary, terbinafine usually giving the best results in dermatophytosis. 

Longstanding remedies such as Compound Benzoic Acid Ointment (Whitfield s ointment) are still acceptable for iruld infections but a topical imidazole (clotrimazole, econazole, miconazole, sulconazole), which is also effective against Candida, is now usually preferred. Tioconazole is effective topically for nail infections. If multiple areas are affected, especially if the scalp or nails are included, and if topical therapy fails, oral itraconazole or terbinafine are used. Griseofulvin has largely been superseded for these indications. 

Terbinafine interferes with ergosterol biosynthesis, and thereby with the formation of the fungal cell membrane. It is absorbed from the gastrointestinal tract and undergoes extensive metabolism in the liver (tj 14 h). Terbinafine is used topically for dermatophyte infections of the skin and orally for infections of hair and nails where the site (e.g. hair), severity or extent of the infection render topical use inappropriate (see p. 315). Treatment (250 mg/d) may need to continue for several weeks. It may cause nausea, diarrhoea, dyspepsia, abdominal pain, headaches and cutaneous reactions. 

Fungal infections superficial dermatophyte or Candida infections purely involving the skin can be treated with a topical imidazole (e.g. clotrimazole, miconazole). Pityriasis versicolor, a yeast infection, primarily involves the trunk m young adults it responds poorly to imidazoles but topical terbinafine or selenium sulphide preparations are effective severe infection may require systemic itraconazole. Invasion of hair or nails by a dermatophyte or a deep mycosis requires systemic therapy terbinafine is the most effective drug. Terbinafine and griseo-fulvin are ineffective against yeasts, for which itraconazole is an alternative. Itraconazole can be used in weekly pulses each month for 3-4 months it is less effective against dermatophytes than terbinafine. 

A 62-year-old diabetic man on stable oral medication with glibenclamide, metformin, Zestoretic (lisino-pril + hydrochlorothiazide), gemfibrozil, and aspirin developed febrile generalized pustular eruptions after 44 days of therapy with oral terbinafine 250 mg/day (50). Withdrawal of terbinafine and symptomatic treatment with hydrotherapy and topical and systemic steroids resulted in complete resolution of fever and pustulosis within 4 days. The erythematous component responded more slowly, and mildly pruritic erythematous plaques persisted for more than 40 days. 

Severe pustular psoriasis provoked de novo by oral terbinafine has been reported in a 65-year-old man 2 weeks after the start of therapy for onychomycosis (52). Treatment of psoriasis was complicated and ultimately required continuous systemic and topical antipsoriatic therapy. 

A 74-year-old woman developed inverse psoriasis after 14 days of therapy with terbinafine 250 mg/day for onychomycosis (53). The lesions resolved almost completely on withdrawal of terbinafine and topical therapy. 

Shear NH, Villars VV, Marsolais C. Terbinafine an oral and topical antifungal agent. Clin Dermatol 1991 9(4) 487-95. 

Alberti I, Kalia YN, Naik A, et al. In vivo assessment of enhancement topical delivery of terbinafine to human stratum corneum. / Control Release 2001 71 319-327. 

Terbinafine (Fig. 10.221), a member of the allyl-amine class of antimycotics, is an inhibitor of the enzyme squalene epoxidase in fungal ergosterol biosynthesis. Terbinafine is orally active, is fungicidal and is effective against a broad range of dermatophytes and yeasts. It can also be used topically as a cream. 

Data is also available suggesting efficacy of topical garlic on fungal infections. For tinea pedis, 1-week topical treatment with ajoene 1% twice daily resulted in mycological cure 60 days later in 100% of patients, compared to 94% for 1% topical terbinafine and 72% for 0.6% topical ajoene (43). Another study showed that 0.6% topical ajoene was as effective as 1% terbinafine cream, both applied twice daily for 1 week, for the treatment of tinea cruris and corposis. After 60 days, effectiveness (clinical plus mycological cure) was 73 vs 71 %,respectively (44). In addition, a0.4% cream was also shown to be effective (45). Although a topical preparation is not available commercially, it could likely be compounded. 

Ledezma E, Lopez JC, Marin P, et al. Ajoene in the topical short-term treatment of tinea cruris and tinea corporis in humans randomized comparative study with terbinafine. Arzneim-Forsch/Drug Res 1999 49 544-547. 

The azoles miconazole (Micatin, others) and econazole (Spectrazole, others) and the allylamines naftifine (Naftin) and terbinafine (Lamisil, others) are effective topical agents for the treatment of localized tinea corporis and uncomplicated tinea pedis. Topical therapy with the azoles is preferred for localized cutaneous candidiasis and tinea versicolor. 

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