Pronunciation:

(TER bin a feen)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Oral: Onychomycosis of the toenail or fingernail due to susceptible dermatophytes

Topical: Antifungal for the treatment of tinea pedis (athlete's foot), tinea cruris (jock itch), and tinea corporis (ringworm) [OTC/prescription formulations]; tinea versicolor [prescription formulations]

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

Oral:

1% to 10%:

Central nervous system: Headache, dizziness, vertigo

Dermatologic: Rash, pruritus, urticaria

Gastrointestinal: Diarrhea, dyspepsia, abdominal pain, appetite decrease, taste disturbance

Hematologic: Lymphocytopenia

Hepatic: Liver enzymes increased

Ocular: Visual disturbance

<1%, postmarketing and/or case reports: Angioedema, agranulocytosis, allergic reactions, alopecia, anaphylaxis, arthralgia, changes in ocular lens and retina, fatigue, hepatic failure, malaise, myalgia, neutropenia, precipitation/exacerbation of cutaneous and systemic lupus erythematosus, Stevens-Johnson syndrome, thrombocytopenia, toxic epidermal necrolysis, vomiting

Topical: 1% to 10%:

Dermatologic: Pruritus, contact dermatitis, irritation, burning, dryness

Local: Irritation, stinging

Drug Interactions:

Effects of drugs metabolized by CYP2D6 (including beta-blockers, SSRIs, MAO inhibitors, tricyclic antidepressants) may be increased; warfarin effects may be increased

CYP2D6 substrates: Terbinafine may increase the levels/effects of CYP2D6 substrates. Example substrates include amphetamines, selected beta-blockers, dextromethorphan, fluoxetine, lidocaine, mirtazapine, nefazodone, paroxetine, risperidone, ritonavir, thioridazine, tricyclic antidepressants, and venlafaxine.

CYP2D6 prodrug substrates: Terbinafine may decrease the levels/effects of CYP2D6 prodrug substrates. Example prodrug substrates include codeine, hydrocodone, oxycodone, and tramadol.

Rifampin: Rifampin increases terbinafine clearance (100%).

Stability:

Cream: Store at 5°C to 30°C (41°F to 86°F).

Solution: Store at 5°C to 25°C (41°F to 77°F); do not refrigerate

Tablet: Store below 25°C (77°F); protect from light

Mechanism of Action:

Pharmacodynamics/Kinetics:

Absorption: Topical: Limited (<5%); Oral: >70%

Distribution: Vd: 2000 L; distributed to sebum and skin predominantly

Protein binding, plasma: >99%

Metabolism: Hepatic; no active metabolites; first-pass effect; little effect on CYP

Bioavailability: Oral: 40%

Half-life elimination:

Topical: 22-26 hours

Oral: Terminal half-life: 200-400 hours; very slow release of drug from skin and adipose tissues occurs; effective half-life: ~36 hours

Time to peak, plasma: 1-2 hours

Excretion: Urine (70% to 75%)

Dosage:

Children 12 years and Adults:

Topical cream, solution:

Athlete's foot (tinea pedis): Apply to affected area twice daily for at least 1 week, not to exceed 4 weeks [OTC/prescription formulations]

Ringworm (tinea corporis) and jock itch (tinea cruris): Apply cream to affected area once or twice daily for at least 1 week, not to exceed 4 weeks; apply solution once daily for 7 days [OTC formulations]

Adults:

Oral:

Superficial mycoses: Fingernail: 250 mg/day for up to 6 weeks; toenail: 250 mg/day for 12 weeks; doses may be given in two divided doses

Systemic mycosis: 250-500 mg/day for up to 16 months

Topical solution: Tinea versicolor: Apply to affected area twice daily for 1 week [prescription formulation]

Dosing adjustment in renal impairment: GFR <50 mL/minute: Oral administration is not recommended.

Dosing adjustment in hepatic impairment: Clearance is decreased by ~50% with hepatic cirrhosis; use is not recommended.

Monitoring Parameters:

Patient Education:

Additional Information:

A meta-analysis of efficacy studies for toenail infections revealed that weighted average mycological cure rates for continuous therapy were 36.7% (griseofulvin), 54.7% (itraconazole), and 77% (terbinafine). Cure rate for 4-month pulse therapy for itraconazole and terbinafine were 73.3% and 80%. Additionally, the final outcome measure of final costs per cured infections for continuous therapy was significantly lower for terbinafine.

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Cream, as hydrochloride (Lamisil® AT™): 1% (15 g, 30 g)

Solution, as hydrochloride [topical spray] (Lamisil®, Lamisil® AT™): 1% (30 mL)

Tablet (Lamisil®): 250 mg

International Brand Names: