OVERVIEW

PRODUCT INFORMATION

CHEMICAL FORMULA AND STRUCTURE

View in own window

DRUG	CAS REGISTRY NUMBER	MOLECULAR FORMULA	STRUCTURE
Tiagabine	115103-54-3	C20-H25-N-O2-S2

ANNOTATED BIBLIOGRAPHY

References updated: 19 February 2018

• Zimmerman HJ. Anticonvulsants. In, Zimmerman, HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott, 1999: pp. 498-516.

  (Expert review of anticonvulsants and liver injury published in 1999; tiagabine is not discussed).
• Pirmohamed M, Leeder SJ. Anticonvulsant agents. In, Kaplowitz N, DeLeve LD, eds. Drug-induced liver disease. 3rd ed. Amsterdam: Elsevier, 2013: pp 423-42.

  (Review of anticonvulsant induced liver injury; tiagabine is not discussed).
• McNamara JO. Pharmacology of the epilepsies. In, Brunton LL, Chabner BA, Knollman BC, eds. Goodman & Gilman’s the pharmacological basis of therapeutics. 12th ed. New York: McGraw-Hill, 2011, pp. 583-607.

  (Textbook of pharmacology and therapeutics).
• Wallace SJ. A comparative review of the adverse effects of anticonvulsants in children with epilepsy. Drug Saf 1996; 15: 378-93. [PubMed: 8968693]

  (Systematic review; ALT elevations occur in 4% of children on phenytoin, 6% on valproate, 1% on carbamazepine but none reported in children on tiagabine or gabapentin).
• Wilby J, Kainth A, Hawkins N, et al. Clinical effectiveness, tolerability and cost-effectiveness of newer drugs for epilepsy in adults: a systematic review and economic evaluation. Health Technol Assess 2005; 9: 1-157, iii-iv. [PubMed: 15842952]

  (Extensive systematic review of anticonvulsant medications including assessment of serious, rare and long-term adverse events; tiagabine adverse events were limited to neurological effects; no mention of hepatotoxicity).
• Pollack MH, Tiller J, Xie F, Trivedi MH. Tiagabine in adult patients with generalized anxiety disorder: results from 3 randomized, double-blind, placebo-controlled, parallel-group studies. J Clin Psychopharmacol 2008; 28: 308-16. [PubMed: 18480688]

  (Summary of 3 randomized controlled trials of tiagabine vs placebo for 10 weeks; little or no evidence of efficacy for generalized anxiety disorder found; side effects included headache, dizziness, nausea, fatigue and somnolence but no mention of liver toxicity or ALT elevations).
• Forbes RA, Kalra H, Hackett LP, Daly FF. Deliberate self-poisoning with tiagabine: an unusual toxidrome. Emerg Med Australas 2007; 19: 556-8. [PubMed: 18021110]

  (Overdose of tiagabine associated with vomiting, coma, myoclonus, hypertension and pilerection, but no mention of liver injury or jaundice).
• Winhusen T, Somoza E, Ciraulo DA, et al. A double-blind, placebo-controlled trial of tiagabine for the treatment of cocaine dependence. Drug Alcohol Depend 2007; 91: 141-8. [PubMed: 17629631]

  (Randomized controlled trial [n=141] of tiagabine vs placebo for cocaine dependence found no evidence of efficacy, but also “no pattern of physical or laboratory abnormality” attributable to tiagabine).
• LaRoche SM. A new look at the second-generation antiepileptic drugs: a decade of experience. Neurologist 2007; 13: 133-9. [PubMed: 17495757]

  (Review of second generation anticonvulsants approved since 1994 including felbamate, gabapentin, lamotrigine, topiramate, tiagabine, levetiracetam, oxcarbazepine, zonisamide and pregabalin: no mention of liver toxicity from tiagabine).
• Bauer J, Cooper-Mahkorn D. Tiagabine: efficacy and safety in partial seizures—current status. Neuropsychiatr Dis Treat 2008; 4: 731-6. [PMC free article: PMC2536540] [PubMed: 19043517]

  (Review of pharmacology, clinical efficacy and side effects of tiagabine; no mention of liver toxicity or ALT elevations).
• Chalasani N, Fontana RJ, Bonkovsky HL, Watkins PB, Davern T, Serrano J, Yang H, Rochon J; Drug Induced Liver Injury Network (DILIN). Causes, clinical features, and outcomes from a prospective study of drug-induced liver injury in the United States. Gastroenterology 2008; 135: 1924-34. [PMC free article: PMC3654244] [PubMed: 18955056]

  (Among 300 cases of drug induced liver disease in the US collected between 2004 and 2008, valproate accounted for 6 cases, lamotrigine 5, phenytoin 5, gabapentin and topiramate 1 each; none were due to tiagabine).
• Knowles SR, Dewhurst N, Shear NH. Anticonvulsant hypersensitivity syndrome: an update. Expert Opin Drug Saf 2012; 11: 767-78. [PubMed: 22794330]

  (Updated review of anticonvulsant hypersensitivity syndrome; associated with phenytoin, phenobarbital, lamotrigine and carbamazepine and rarely with zonisamide, valproate and oxcarbazepine; tiagabine is not mentioned).
• Drugs for epilepsy. Treat Guidel Med Lett 2013; 11: 9-18. [PubMed: 23348233]

  (Concise review of indications and side effects of anticonvulsants; tiagabine is approved only for treatment of partial seizures and has prominent gastrointestinal and CNS side effects; no mention of hepatotoxicity).
• Chalasani N, Bonkovsky HL, Fontana R, Lee W, Stolz A, Talwalkar J, Reddy KR, et al.; United States Drug Induced Liver Injury Network. Features and outcomes of 899 patients with drug-induced liver injury: The DILIN Prospective Study. Gastroenterology 2015; 148: 1340-52.e7. [PMC free article: PMC4446235] [PubMed: 25754159]

  (Among 899 cases of drug induced liver injury enrolled in a US prospective study between 2004 and 2013, 40 [4.5%] were attributed to anticonvulsants, but none specifically to tiagabine).
• Zaccara G, Giovannelli F, Giorgi FS, Franco V, Gasparini S, Benedetto U. Tolerability of new antiepileptic drugs: a network meta-analysis. Eur J Clin Pharmacol 2017; 73: 811-7. [PubMed: 28378057]

  (Metaanalysis of the comparative tolerability of 18 new anticonvulsant agents, found best tolerability [lowest rates of withdrawal for adverse events] with levetiracetam, brivaracetam and gabapentin and lowest scores for tolerability from eslicarbazepine, oxcarbazepine, lacosamide and topiramate; tiagabine had an intermediate level of tolerability).
• Drugs for epilepsy. Med Lett Drugs Ther 2017; 59 (1526): 121-30. [PubMed: 28746301]

  (Concise review of the drugs available for therapy of epilepsy does not list tiagabine as either a first or second line drug for epilepsy and mentions that it is approved for adjunctive treatment of partial seizures, but has gastrointestinal and neurologic side effects and is associated with de novo seizures in patients treated off label for bipolar illness or neuropathic pain).