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terbinafine hydrochloride tablet
----------Terbinex (terbinafine Hydrochloride tablets equivalent to 250mg base)
Terbinex™ Terbinafine Hydrochloride Tablets contain the synthetic allylamine antifungal compound terbinafine hydrochloride. Chemically, terbinafine
Terbinafine hydrochloride is a white to off-white fine crystalline powder. It is freely soluble in methanol and methylene chloride, soluble in ethanol, and
Following oral administration, terbinafine is well absorbed (>70%) and the bioavailability of Terbinafine Hydrochloride Tablets as a result of first-pass
Terbinafine hydrochloride is a synthetic allylamine derivative. Terbinafine hydrochloride is hypothesized to act by inhibiting squalene epoxidase, thus
The following in vitro data are available, but their clinical significance is unknown. In vitro, terbinafine exhibits satisfactory MIC’s against most strains of
The efficacy of Terbinafine Hydrochloride Tablets in the treatment of onychomycosis is illustrated by the response of patients with toenail and/or
Results of the first toenail study, as assessed at week 48 (12 weeks of treatment with 36 weeks follow-up after completion of therapy), demonstrated
In a second toenail study of dermatophytic onychomycosis, in which nondermatophytes were also cultured, similar efficacy against the dermatophytes
Results of the fingernail study, as assessed at week 24 (6 weeks of treatment with 18 weeks follow-up after completion of therapy), demonstrated
The mean time to overall success was approximately 10 months for the first toenail study and 4 months for the fingernail study. In the first toenail study, for
Terbinafine Hydrochloride Tablets are indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea
Prior to initiating treatment, appropriate nail specimens for laboratory testing (KOH preparation, fungal culture, or nail biopsy) should be obtained to confirm
Terbinafine Hydrochloride Tablets are contraindicated in individuals with hypersensitivity to terbinafine or to any other ingredients of the formulation.
Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of Terbinafine Hydrochloride Tablets for the treatment of
onychomycosis in individuals with and without pre-existing liver disease.
In the majority of liver cases reported in association with terbinafine hydrochloride use, the patients had serious underlying systemic conditions and
an uncertain causal association with terbinafine hydrochloride. The severity of hepatic events and/or their outcome may be worse in patients with active or
chronic liver disease (see PRECAUTIONS). Treatment with Terbinafine Hydrochloride Tablets should be discontinued if biochemical or clinical evidence
of liver injury develops (see PRECAUTIONS below).
There have been isolated reports of serious skin reactions (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash
occurs, treatment with terbinafine hydrochloride should be discontinued.
General: Terbinafine Hydrochloride Tablets are not recommended for patients with chronic or active liver disease.
In patients with renal impairment (creatinine clearance ≤50 mL/ min), the use of terbinafine hydrochloride has not been adequately studied, and therefore, is not
During postmarketing experience, precipitation and exacerbation of cutaneous and systemic lupus erythematosus have been reported infrequently in patients
Changes in the ocular lens and retina have been reported following the use of Terbinafine Hydrochloride Tablets in controlled trials. The clinical significance of
hydrochloride treated patients (1.7%) and 3/137 placebo-treated patients (2.2%) had decreases in ALC to below 1000/mm3 on two or more occasions.
The clinical significance of this observation is unknown. However, in patients with known or suspected immunodeficiency, physicians should consider
monitoring complete blood counts in individuals using Terbinafine Hydrochloride therapy for greater than six weeks.
Isolated cases of severe neutropenia have been reported. These were reversible upon discontinuation of terbinafine hydrochloride with or without supportive
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include
the following drug classes; tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g. flecainide and
propafenone) and monoamine oxidase inhibitors Type B. Coadministration of Terbinafine Hydrochloride Tablets should be done with careful monitoring and
may require a reduction in dose of the 2D6-metabolized drug. In a study to assess the effects of terbinafine on desipramine in healthy volunteers
characterized as normal metabolizers, the administration of terbinafine resulted in a 2-fold increase in Cmax and a 5-fold increase in AUC. In this study, these
effects were shown to persist at the last observation at 4 weeks after discontinuation of terbinafine hydrochloride.
In vitro studies with human liver microsomes showed that terbinafine does not inhibit the metabolism of tolbutamide, ethinylestradiol, ethoxycoumarin, and
In vivo drug-drug interaction studies conducted in healthy volunteer subjects showed that terbinafine does not affect the clearance of antipyrine or digoxin.
Terbinafine decreases the clearance of caffeine by 19%. Terbinafine increases the clearance of cyclosporine by 15%.
There have been spontaneous reports of increase or decrease in prothrombin times in patients concomitantly taking oral terbinafine and warfarin, however, a
causal relationship between Terbinafine Hydrochloride Tablets and these changes has not been established.
Terbinafine clearance is increased 100% by rifampin, a CYP450 enzyme inducer, and decreased 33% by cimetidine, a CYP450 enzyme inhibitor. Terbinafine
clearance is unaffected by cyclosporine.
There is no information available from adequate drug-drug interaction studies with the following classes of drugs: oral contraceptives, hormone replacement
therapies, hypoglycemics, theophyllines, phenytoins, thiazide diuretics, and calcium channel blockers.
In a 28-month oral carcinogenicity study in rats, an increase in the incidence of liver tumors was observed in males at the highest dose tested, 69 mg/kg/day [2x
the Maximum Recommended Human Dose (MRHD) based on AUC comparisons of the parent terbinafine]; however, even though dose limiting toxicity was not
achieved at the highest tested dose, higher doses were not tested.
The results of a variety of in vitro (mutations in E. coli and S. typhimurium, DNA repair in rat hepatocytes, mutagenicity in Chinese hamster fibroblasts,
chromosome aberration and sister chromatid exchanges in Chinese hamster lung cells), and in vivo (chromosome aberration in Chinese hamsters,
micronucleus test in mice) genotoxicity tests gave no evidence of a mutagenic or clastogenic potential. Oral reproduction studies in rats at doses up to
300 mg/kg/day (approximately 12x the MRHD based on body surface area comparisons, BSA) did not reveal any specific effects on fertility or other
reproductive parameters. Intravaginal application of terbinafine hydrochloride at 150 mg/day in pregnant rabbits did not increase the incidence of abortions or
premature deliveries nor affect fetal parameters.
Pregnancy Category B: Oral reproduction studies have been performed in rabbits and rats at doses
up to 300 mg/kg/day (12x to 23x the MRHD, in rabbits and rats, respectively, based on BSA) and have revealed no evidence of impaired
fertility or harm to the fetus due to terbinafine. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction
studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is
recommended that terbinafine hydrochloride not be initiated during pregnancy.
After oral administration, terbinafine is present in breast milk of nursing mothers. The ratio of terbinafine in milk to plasma is 7:1. Treatment with
terbinafine hydrochloride is not recommended in nursing mothers.
The safety and efficacy of Terbinafine Hydrochloride Tablets have not been established in pediatric patients.
The most frequently reported adverse events observed in the three US/Canadian placebo-controlled trials are listed in the table below. The adverse events
Adverse events, based on worldwide experience with Terbinafine Hydrochloride Tablets use, include: idiosyncratic and symptomatic hepatic injury and more
rarely, cases of liver failure, some leading to death or liver transplant, (see WARNINGS and PRECAUTIONS), serious skin reactions (see WARNINGS),
severe neutropenia (see PRECAUTIONS), thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Psoriasiform eruptions or
exacerbation of psoriasis, acute generalized exanthematous pustulosis and precipitation and exacerbation of cutaneous and systemic lupus erythematosus
have been reported in patients taking Terbinafine Hydrochloride Tablets. Terbinafine Hydrochloride Tablets may cause taste disturbance (including taste
loss) which usually recovers within several weeks after discontinuation of the drug. There have been isolated reports of prolonged (greater than one year)
taste disturbance. Taste disturbances associated with oral terbinafine have been reported to be severe enough to result in decreased food intake leading to
significant and unwanted weight loss.
Other adverse reactions which have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
Clinical adverse effects reported spontaneously since the drug was marketed include altered prothrombin time (prolongation and reduction) in patients
concomitantly treated with warfarin and Terbinafine Hydrochloride Tablets and agranulocytosis (rare).
Clinical experience regarding overdose with Terbinafine Hydrochloride Tablets is limited. Doses up to 5 grams (20 times the therapeutic daily dose) have
Terbinafine Hydrochloride Tablets, one 250 mg tablet, should be taken once daily for 6 weeks by patients with fingernail onychomycosis.
Terbinex™ Terbinafine Hydrochloride Tablets
Supplied as white, round, flat faced beveled edge tablets debossed with IG on one side and 209 on the other.
Bottle of 42 tablets packaged with 12 mL bottle of Eco Formula NDC 68712-037-01
Store tablets at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]; in a tight container.
Protect from light.
INVAGEN Pharmaceuticals, Inc.
A wide range of in vivo studies in mice, rats, dogs, and monkeys, and in vitro studies using rat, monkey, and human
hepatocytes suggest that peroxisome proliferation in the liver is a rat-specific finding. However, other effects, including
increased liver weights and APTT, occurred in dogs and monkeys at doses giving Css trough levels of the parent terbinafine 2-3x those seen in humans at
the MRHD. Higher doses were not tested.
Revised: 08/2009 JSJ Pharmaceuticals
Reproduced with permission of U.S. National Library of Medicine
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