Pharmacology and clinical experience with tiagabine.
Tiagabine (TGB), a recently approved anti-epileptic drug (AED), has a specific and unique mechanism of action involving the inhibition of gamma-aminobutyric acid (GABA) re-uptake into neurones and glia. TGB is potent and has linear and predictable pharmacokinetics. It does not induce or inhibit hepatic metabolism and has no clinically significant effects on the serum concentrations of other AEDs or commonly used non-AEDs. Double-blind, placebo-controlled studies in primarily hepatic enzyme-induced patients showed that TGB 30 - 56 mg/day is an effective add-on treatment for all subtypes of partial seizures. The most common adverse effects in the trials were dizziness, asthenia (weakness), somnolence, accidental injury, infection, headache, nausea and nervousness. These side effects were usually mild to moderate in severity and generally did not require medical intervention. Long-term safety studies show continued efficacy of TGB over time and no evidence of tolerance for efficacy. Open studies confirm that patients with medically refractory partial epilepsy can be successfully converted to TGB monotherapy and that TGB may be effective for other seizure types, such as infantile spasms.
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Office of Clinical Trials and Research, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, MA 02215, USA. sschacht@caregroup.harvard.edu
D001682:Biological Availability; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004827:Epilepsy / Q000188:drug therapy*; D018755:GABA Agonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D015337:Multicenter Studies as Topic; D009557:Nipecotic Acids / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016032:Randomized Controlled Trials as Topic; D000078308:Tiagabine
D018755:GABA Agonists; D009557:Nipecotic Acids; D000078308:Tiagabine