Trade Names:Lamisil- Tablets 250 mg- Granules, oral 125 mg/packet- Granules, oral 187.5 mg/packet
Trade Names:Lamisil AT- Cream 1%Apo-Terbinafine (Canada)CO Terbinafine (Canada)Gen-Terbinafine (Canada)PMS-Terbinafine (Canada)Sandoz Terbinafine (Canada)
Inhibits squalene epoxidase, resulting in ergosterol deficiency and a corresponding accumulation of squalene within the fungal cell leading to fungal cell death.
Absorption from oral terbinafine is greater than 70%; bioavailability is about 40%. Terbinafine C max is 1 mcg/mL, T max occurs 2 h after a 250 mg dose. AUC is 4.56 mcg•h/mL and is increased less than 20% with food. At steady state in comparison to single dose, C max is 25% higher and AUC is increased 2.5 times.
Terbinafine is more than 99% protein bound and there are no specific binding sites. It is distributed to the sebum and skin.
Prior to excretion, terbinafine is extensively metabolized by at least 7 CYP isoenzymes. There are no major metabolites that have antifungal activity similar to terbinafine.
Terbinafine half-life is 200 to 400 h, and the drug is about 70% eliminated in the urine.
In renal function impairment (CrCl approximately 50 mL/min), terbinafine Cl is decreased 50%.Hepatic Function Impairment
In hepatic cirrhosis, terbinafine Cl is decreased 50%.
Treatment of onychomycosis of the toenail or fingernail caused by dermatophytes.Topical
Interdigital tinea pedis, tinea cruris, or tinea corporis caused by Epidermophyton floccosum , Trichophyton mentagrophytes , or Trichophyton rubrum .Oral granules
Treatment of tinea capitis in patients 4 yr of age and older.
Patients weighing less than 25 kg, administer 125 mg once daily for 6 wk. Patients weighing 25 to 35 kg, administer 187.5 mg once daily for 6 wk. Patients weighing more than 35 kg, administer 250 mg once daily for 6 wk.Onychomycosis of Toenail and FingernailAdults
250 mg once daily for 6 wk.Toenail onychomycosis
250 mg once daily for 12 wk.Tinea Corpis, Tinea Cruris, Tinea PedisAdults and Children 12 yr of age and older
TopicalTinea corpis, tinea cruris
Apply to affected areas and surrounding skin once daily for 1 wk.Tinea pedis
Apply twice daily for 1 to 2 wk.
Store oral granules at 59° to 86°F. Store tablets below 77°F. Protect from light. Store topical cream at 68° to 77°F.
Terbinafine decreases the Cl of IV caffeine 19%.Cimetidine
Terbinafine Cl is decreased 33% by cimetidine.Cyclosporine
Terbinafine increases the Cl of cyclosporine 15%.CYP2C9 and CYP3A4 inhibitors (eg, amiodarone, ketoconazole)
Terbinafine plasma concentrations may be elevated, increasing the risk of adverse reactions.Dextromethorphan
Plasma dextromethorphan concentrations may be elevated, increasing the pharmacologic effects and adverse reactions. Terbinafine inhibits dextromethorphan metabolism via the CYP2D6 enzyme.Paroxetine, tricyclic antidepressants (eg, amitriptyline, desipramine, imipramine), venlafaxine
Plasma concentrations of these agents may be elevated, increasing the pharmacologic effects and risk of adverse reactions.Rifampin
Terbinafine Cl is increased 100% by rifampin.Warfarin
Spontaneous reports of increases and decreases in PT time have been reported.
None well documented.
Headache (7%); fatigue, malaise (postmarketing).
Rash (6%); pruritus (3%); urticaria (1%); acute generalized exanthematous pustulosis and precipitation and exacerbation of cutaneous systemic lupus erythematosus; hair loss; psoriasiform eruptions and exacerbation of psoriasis; serious skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (postmarketing).
Nasopharyngitis (10%); yellow-blue color vision confusion (5%); taste disturbance (3%); nasal congestion, pharyngolaryngeal pain, rhinorrhea (2%); toothache (1%); reduced visual acuity, taste loss, visual field defects (postmarketing).
Diarrhea (6%); vomiting (5%); dyspepsia, upper abdominal pain (4%); nausea (3%); abdominal pain (2%); acute pancreatitis (postmarketing).
Liver abnormalities (3%); hepatic injury, liver failure (postmarketing).
Agranulocytosis, anemia, pancytopenia, severe neutropenia, thrombocytopenia (postmarketing).
Allergic reactions including anaphylaxis, angioedema (postmarketing).
Weight loss (postmarketing).
Arthralgia, myalgia, rhabdomyolysis (postmarketing).
Cough (6%); upper respiratory tract infection (5%).
Pyrexia (7%); influenza (2%).
Pretreatment serum transaminases (ALT and AST) are advised for all patients.
Category B .
Excreted in breast milk.
Safety and efficacy not established (tablets).Oral granules
Safety and efficacy not established in children younger than 4 yr of age.Topical cream
Safety and efficacy not established in children younger than 12 yr of age.
Use of oral granules have not been studied in elderly patients.
Use in patients with CrCl less than 50 mL/min has not been studied. Do not use in patients with renal function impairment (CrCl up to 50 mL/min).
Not recommended in patients with active or chronic liver disease.
Transient increases in absolute lymphocyte counts have been observed. Severe neutropenia has also been reported.
Liver failure, some fatal or leading to liver transplantation, have occurred during postmarketing experience.
Precipitation and exacerbation of cutaneous and systemic lupus erythematosus have been reported during postmarketing experience.
Serious skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, have occurred during postmarketing experience.
Changes in the ocular lens and retina have been reported.
Abdominal pain, dizziness, frequent urination, headache, nausea, rash, vomiting.
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