Terbinafine


Concise Prescribing Info
Indications/Uses
Dermatophytosis.
Dosage/Direction for Use
Adult : PO 250 mg once daily. Treatment duration: 2-4 wk (tinea cruris), 4 wk (tinea corporis), 2-6 wk (tinea pedis), 6-12 wk (onychomycosis). Topical As 1% cream/gel/spray: Apply once or bid to affected area(s). Treatment duration: 1-2 wk (tinea corporis, tinea cruris), 1 wk (tinea pedis), 2 wk (cutaneous candidiasis and pityriasis).
Dosage Details
Oral
Dermatophytosis
Adult: 250 mg once daily. Treatment duration: 2-4 wk (tinea cruris), 4 wk (tinea corporis), 2-6 wk (tinea pedis), 6-12 wk (onychomycosis).

Topical/Cutaneous
Dermatophytosis
Adult: As 1% cream/gel/spray: Apply once or bid to affected area(s). Treatment duration: 1-2 wk (tinea corporis, tinea cruris), 1 wk (tinea pedis), 2 wk (cutaneous candidiasis and pityriasis).
Renal Impairment
CrCl (mL/min) Dosage
<50 Reduce to 50% of usual dose.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. Chronic or active hepatic disease. Lactation.
Special Precautions
Patient w/ immunosuppression, psoriasis, autoimmune disease (e.g. Lupus erythematosus); presence of lesion (topical). Renal impairment (CrCl <50 mL/min). Pregnancy.
Adverse Reactions
Significant: Depression, taste and smell disturbances, wt loss, anxiety. Rarely, SLE; psoriasis exacerbation; ocular lens and retina changes; blood disorders (e.g. decreased lymphocyte count, neutropenia, agranulocytosis, pancytopenia).
Nervous: Headache.
GI: Dyspepsia, nausea, vomiting, diarrhoea, abdominal distention/pain, toothache, pharyngolaryngeal pain, decreased appetite, feeling of fullness.
Resp: Influenza, nasopharygitis, upper resp tract infections, nasal congestion, rhinorrhea.
Musculoskeletal: Arthralgia, myalgia.
Ophthalmologic: Vision color changes, color confusion, decreased visual acuity.
Dermatologic: Rash, pruritus, urticaria, skin exfoliation.
Others: Fever, application site reactions (e.g. pain/irritation pigmentation disorder, burning sensation).
Potentially Fatal: Hepatic failure. Rarely, serious skin and hypersensitivity reaction (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, exfoliative dermatitis, bullous dermatitis, drug reaction w/ eosinophilia and systemic symptoms [DRESS] syndrome); thrombotic microangiopathy (e.g. thrombocytopenic purpura, haemolytic uraemic syndrome).
Patient Counseling Information
Avoid contact w/ eyes.
MonitoringParameters
Perform LFT before initiation of oral therapy and monitor 4-6 wk thereafter. Monitor CBC for therapy >6 wk.
Overdosage
Symptoms: headache, nausea, upper abdominal pain, and dizziness. Management: Symptomatic and supportive treatment. Administer activated charcoal w/in 1-2 hr after ingestion orally or via nasogastric tube for unconscious patient.
Drug Interactions
Increased serum concentration w/ cimetidine, CYP450 inhibitors (e.g. fluconazole, amiodarone, ketoconazole). Decreased serum concentration w/ rifampicin. May increase plasma concentration of TCA(s), β-blockers, SSRIs, antiarrythmics, MAOI(s) type B. May cause menstrual disturbances (e.g. breakthrough bleeding, irregular cycle) w/ OC. May decrease clearance of despiramine.
Action
Description: Terbinafine is a allylamine derivative that has a wide spectrum of antifungal activity against pathogens of the skin, hair, and nails. It acts by inhibiting squalene epoxidase, the main enzyme responsible for fungal sterol synthesis. Thus, resulting to ergosterol deficiency, leading to membrane disruption and cell death. It is active against dermatophytes, moulds, and certain dimorphic fungi.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Minimal absorption through the skin. Bioavailability: 40%. Time to peak plasma concentration: W/in 2 hr (oral).
Distribution: Distributed into the stratum corneum of the skin, nails, sebum, and hair. Enters breastmilk. Plasma protein binding: >99%.
Metabolism: Rapidly metabolised in the liver by CYP enzymes into inactive metabolites. Undergoes first-pass metabolism.
Excretion: Mainly via urine (80%, as inactive metabolites); faeces (20%). Terminal elimination half-life: 200-400 hr (prolonged use). Plasma elimination half-life: 17-36 hr (oral), 14-35 hr (topical).
Chemical Structure

Chemical Structure Image
Terbinafine

Source: National Center for Biotechnology Information. PubChem Database. Terbinafine, CID=1549008, https://pubchem.ncbi.nlm.nih.gov/compound/Terbinafine (accessed on Jan. 23, 2020)

Storage
Store below 25°C. Protect from light and moisture.
ATC Classification
D01AE15 - terbinafine ; Belongs to the class of other antifungals for topical use.
D01BA02 - terbinafine ; Belongs to the class of antifungals for systemic use.
References
Anon. Terbinafine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/10/2017.

Anon. Terbinafine (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/10/2017.

Buckingham R (ed). Terbinafine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/10/2017.

Douglas Pharmaceuticals Ltd. Terbinafine-DP data sheet 10 December 2012. Medsafe. http://www.medsafe.govt.nz/. Accessed 16/10/2017.

Joint Formulary Committee. Terbinafine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/10/2017.

Lamisil AT Gel (Novartis Consumer Health, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/10/2017.

Lamisil AT Spray (Novartis Consumer Health, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/10/2017.

Lamisil Tablet (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/10/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Terbinafine Hydrochloride (Topical). AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 16/10/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Terbinafine Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 16/10/2017.

Disclaimer: This information is independently developed by MIMS based on Terbinafine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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