Pharmacokinetics of terbinafine in the nail. 1992

A Y Finlay
Department of Dermatology, University of Wales College of Medicine, Cardiff, UK.

Oral terbinafine is an effective therapy for dermatophyte onychomycosis, presumably because it reaches the infected areas of the nail rapidly and in fungicidal concentrations. For planning optimal clinical dosage regimes, it is necessary to know the rate of terbinafine movement through the nail plate, the concentrations achieved, and the persistence in the nail plate after stopping treatment. In a study of 12 patients receiving terbinafine at 250 mg/day for up to 48 weeks, measurement of terbinafine in distal nail clippings demonstrated that the drug was first detectable 3-18 weeks after starting therapy. A level of 0.25-0.55 ng/mg was quickly achieved and remained stable. Concentrations of terbinafine in distal clippings of unaffected nails were similar to those in affected nails. Although the average nail concentrations are within the fungicidal range for dermatophytes, the anatomy of an infected nail may result in relatively protected areas of infection. This results in the occasional persistence or recurrence of dermatophytic infection observed in some cases. However, the results of this study justify further trials of 'short-term' oral terbinafine therapy for onychomycosis. A current study is addressing the relationship of oral dosage to nail drug concentration and its later persistence in the nail plate.

UI MeSH Term Description Entries
D009262 Nails The thin, horny plates that cover the dorsal surfaces of the distal phalanges of the fingers and toes of primates. Fingernails,Toenails,Fingernail,Nail,Toenail
D009281 Naphthalenes Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
D006118 Griseofulvin An antifungal agent used in the treatment of TINEA infections. Fulvicin-U-F,Grifulvin V,Gris-PEG,Grisactin,Grisefuline,Fulvicin U F,FulvicinUF,Gris PEG,GrisPEG
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077291 Terbinafine A naphthalene derivative that inhibits fungal SQUALENE EPOXIDASE and is used to treat DERMATOMYCOSES of the skin and nails. (E)-N-(6,6-Dimethyl-2-heptenynyl)-N-methyl-1-naphthalenementhamin hydrochloride,DA 5505,Lamisil,SF 86-327,SF-86-327,TDT-067,Terbinafine Hydrochloride,Terbinafine, (Z)-,Terbinafine, (Z)-isomer,SF 86 327,SF 86327,SF86327,TDT 067,TDT067
D000935 Antifungal Agents Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. Anti-Fungal Agents,Antifungal Agent,Fungicides, Therapeutic,Antibiotics, Antifungal,Therapeutic Fungicides,Agent, Antifungal,Anti Fungal Agents,Antifungal Antibiotics
D001393 Azoles Five membered rings containing a NITROGEN atom. Azole
D014009 Onychomycosis A fungal infection of the nail, usually caused by DERMATOPHYTES; YEASTS; or nondermatophyte MOLDS. Nail Fungus,Tinea Unguium,Fungus, Nail,Onychomycoses

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