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
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.
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.