Safety of oral terbinafine: results of a postmarketing surveillance study in 25,884 patients

Hall, Michael

doi:10.1001/archderm.133.10.1213

Cited by 70 publications

(74 citation statements)

References 11 publications

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“…187 Serious adverse drug reactions, most commonly involving the liver and the hematologic system, are only rarely reported with terbinafi ne use (0.04%). 188 Hepatotoxicity ranging from mild transaminitis to fulminant liver failure has been reported as a consequence of oral terbinafi ne use. It is estimated that 2.2% of patients treated with terbinafi ne will experience changes in their liver function tests.…”

Section: Adverse Effectsmentioning

confidence: 99%

Update on terbinafine with a focus on dermatophytoses

Newland¹,

Abdel‐Rahman

2009

CCID

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Since terbinafi ne was introduced on the world market 17 years ago, it has become the leading antifungal for the treatment of superfi cial fungal infections, aided by unique pharmacologic and microbiologic profi les. This article reviews mode of action, antimycotic spectrum and disposition profi le of terbinafi ne. It examines the data, accumulated over 15 years, on the comparative effi cacy of terbinafi ne (vs griseofulvin, itraconazole, fl uconazole) in the management of the infections for which it is primarily indicated (eg, dermatophytoses) and provides a brief discussion on its use for the treatment of non-dermatophyte infections. Finally, the available data on the newest topical and systemic formulations are introduced.

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Section: Adverse Effectsmentioning

confidence: 99%

Update on terbinafine with a focus on dermatophytoses

Newland¹,

Abdel‐Rahman

2009

CCID

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“…At regular doses (Յ250 mg daily), terbinafine is generally well tolerated, although cases of hepatotoxicity have been reported (34). At higher doses, similar rates of adverse events have been reported in 401 patients receiving terbinafine at 500 mg daily and in patients receiving 250 mg daily (5); more recently, a trial in 63 patients of terbinafine at 250 mg q12h versus 500 mg q12h in the treatment of sporotrichosis reported a slightly higher rate of adverse events in patients in the 500 mg q12h arm (2).…”

Section: Discussionmentioning

confidence: 99%

Terbinafine in Combination with Other Antifungal Agents for Treatment of Resistant or Refractory Mycoses: Investigating Optimal Dosing Regimens Using a Physiologically Based Pharmacokinetic Model

Dolton

Perera

Pont

et al. 2014

Antimicrob Agents Chemother

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dTerbinafine is increasingly used in combination with other antifungal agents to treat resistant or refractory mycoses due to synergistic in vitro antifungal activity; high doses are commonly used, but limited data are available on systemic exposure, and no assessment of pharmacodynamic target attainment has been made. Using a physiologically based pharmacokinetic (PBPK) model for terbinafine, this study aimed to predict total and unbound terbinafine concentrations in plasma with a range of highdose regimens and also calculate predicted pharmacodynamic parameters for terbinafine. Predicted terbinafine concentrations accumulated significantly during the first 28 days of treatment; the area under the concentration-time curve (AUC)/MIC ratios and AUC for the free, unbound fraction (fAUC)/MIC ratios increased by 54 to 62% on day 7 of treatment and by 80 to 92% on day 28 compared to day 1, depending on the dose regimen. Of the high-dose regimens investigated, 500 mg of terbinafine taken every 12 h provided the highest systemic exposure; on day 7 of treatment, the predicted AUC, maximum concentration (C max ), and minimum concentration (C min ) were approximately 4-fold, 1.9-fold, and 4.4-fold higher than with a standard-dose regimen of 250 mg once daily. Close agreement was seen between the concentrations predicted by the PBPK model and the observed concentrations, indicating good predictive performance. This study provides the first report of predicted terbinafine exposure in plasma with a range of high-dose regimens.T he allylamine antifungal terbinafine is a well-established agent in the treatment of onychomycosis (1). Due to its broad antifungal spectrum, interest in terbinafine has expanded to include its use in a range of cutaneous and subcutaneous mycoses, such as sporotrichosis, eumycetoma, and chromoblastomycosis (2-4), as well as in combination with other antifungal agents to treat resistant or refractory invasive fungal infections (IFIs), as described in numerous case reports (1, 5). In support of the latter indication, synergistic in vitro antifungal activity has been demonstrated with terbinafine in combination with azole antifungals for many important fungal pathogens, including Aspergillus spp., zygomycetes, Fusarium spp., Paecilomyces spp., Candida albicans, dematiaceous molds, and the highly resistant Scedosporium prolificans (6-11).High dose is a consistent feature of terbinafine use in these indications, with daily doses of up to 1,000 mg daily (1) used to boost the plasma concentrations of terbinafine, which are known to be low following standard dosing, such as the standard dosing regimen of 250 mg daily in onychomycosis, due to extensive accumulation in skin and adipose tissue (12). However, no studies have assessed the systemic exposure of higher-dose terbinafine treatment (Ͼ250 mg daily) or divided daily doses (every 12 h [q12h] or q8h), factors that are likely to be crucial to the utility of terbinafine in effectively treating systemic mycoses in combination with other antifungals. This pauci...

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“…Terbinafine is a large-spectrum antifungal allylamine, usually prescribed for nail and cutaneous dermatophytosis [18]. Benign side effects are observed in about 10% of patients, usually affecting the digestive tract and the skin (ageusia, nausea, diarrhea, erythema, pruritus, urticaria), occurring in 4.9 and 2.3% of patients, respectively [19, 20]. In rare cases, there have been reports of hepatitis, severe hematological abnormalities, and serious cutaneous side effects have been reported, such as bullous pemphigoid [21], acute generalized exanthematous pustulosis [22,23,24], toxic epidermal necrolysis [25, 26], hypersensitivity reaction (‘DRESS syndrome’) [27], erythema multiforme [26, 28], pustular psoriasis [29] or SCLE [11,12,13,14,15,16,17].…”

Section: Discussionmentioning

confidence: 99%

Terbinafine-Induced Subacute Cutaneous Lupus Erythematosus

Farhi¹,

Viguier²,

Cosnes

et al. 2006

Dermatology

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Background: Nearly 10% of lupus erythematosus (LE) are drug induced. More than 60 different drugs are involved in iatrogenic LE. We report herein 3 cases of terbinafine-induced LE. Observations: Three patients receiving terbinafine for a suspected dermatophytic infection developed a subacute cutaneous LE, within 7 weeks following terbinafine introduction. The patients’ medical history included sicca syndrome, lung carcinoma and Kikuchi disease, respectively. Clinical remission occurred within 15 weeks following terbinafine withdrawal. Discussion: Sixteen cases of terbinafine-induced LE have been previously reported, including 13 women. The median age was 54 years. Prior autoimmunity was reported in 10 cases, including 5 pre-existing LE. The median delay between terbinafine introduction and LE onset was 5 weeks. The median time until clinical recovery following terbinafine withdrawal was 8 weeks. Conclusion: Terbinafine should be prescribed only in patients with proven dermatophytosis. We recommend cautious monitoring in patients with pre-existing autoimmunity. The diagnosis of terbinafine-induced LE should lead to the immediate and definitive withdrawal of the drug.

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Safety of oral terbinafine: results of a postmarketing surveillance study in 25,884 patients

Cited by 70 publications

References 11 publications

Update on terbinafine with a focus on dermatophytoses

Update on terbinafine with a focus on dermatophytoses

Terbinafine in Combination with Other Antifungal Agents for Treatment of Resistant or Refractory Mycoses: Investigating Optimal Dosing Regimens Using a Physiologically Based Pharmacokinetic Model

Terbinafine-Induced Subacute Cutaneous Lupus Erythematosus

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