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Tiagabine: profile and news
Anticonvulsant Treatment for Psychiatric and Seizure Indications ... May 4, 2006 Cephalon's Fentanyl Effervescent Buccal Tablet Reduces Intensity ... May 5, 2006 Cephalon Reports First-Quarter Financial Results May 2, 2006 Cephalon Receives Approvable Letter for NUVIGIL(TM) (armodafinil) May 1, 2006 Neuropathic Pain: An Update on Effective Management Strategies May 5, 2006 Cephalon Receives Approvable Letter for NUVIGIL (armodafinil) May 1, 2006 Cephalon Reports First-Quarter Financial Results May 2, 2006 Cephalon, Inc. Provides Update on Regulatory Status of SPARLON(TM) Apr 24, 2006 Cephalon, Inc. Provides Update on Regulatory Status of SPARLON(TM) Apr 24, 2006 Other information Indication For the treatment of partial seizures Pharmacology Tiagabine is used primarily as an anticonvulsant for the adjunctive treatment of epilepsy. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Mechanism Of Action Though the exact mechanism by which Tiagabine exerts its effect on the human body is unknown, it does appear to operate as a selective GABA reuptake inhibitor. Drug Category Neuroprotective Agents; Anticonvulsants; ATC:N03AG06 Brand Names/Synonyms Gabitril; Tiagabina [Inn-Spanish]; Tiagabine; Tiagabine [Inn]; Tiagabinum [Inn-Latin] Dosage Forms Not Available Absorption Tiagabine is nearly completely absorbed (>95%). Interactions -->Interactions for Tiagabine: In evaluating the potential for interactions among co-administered antiepilepsy drugs (AEDs), whether or not an AED induces or does not induce metabolic enzymes is an important consideration. Phenytoin, phenobarbital and carbamazepine are ge nerally classified as enzyme inducers; valproate and gabapentin are not. GABITRIL is considered to be a non-enzyme inducing AED. The drug interaction data described in this section were obtained from studies involving either healthy subjects or patients with epilepsy. Effects of GABITRIL on other Antiepilepsy Drugs (AEDs) : Carbamazepine: Tiagabine had no effect on the steady-state plasma concentrations of carbamazepine or its epoxide metabolite in patients with epilepsy. Valproate: Tiagabine causes a slight decrease (about 10%) in steady-state valproate concentrations. Phenobarbital or Primidone : No formal pharmacokinetic studies have been performed examining the addition of tiagabine to regimens containing phenobarbital or primidone. The addition of tiagabine in a limited number of patients in three well-controlled studies caused no systematic changes in phenobarbital or primidone concentrations when compared to placebo. Effects of other Antiepilepsy Drugs (AEDs) on GABITRIL : Phenytoin: Population pharmacokinetic analyses indicate that tiagabine clearance is 60% greater in patients taking phenytoin with or without other enzyme- inducing AEDs. Phenobarbital (Primidone): Population pharmacokinetic analyses indicate that tiagabine clearance is 60% greater in patients taking phenobarbital (primidone) with or without other enzyme-inducing AEDs. Valproate: The addition of tiagabine to patients taking valproate chronically had no effect on tiagabine pharmacokinetics, but valproate significantly decreased tiagabine binding in vitro from 96.3 to 94.8%, which resulted in an increase of approximately 40% in the free tiagabine concentration. The clinical relevance of this in vitro finding is unknown. Interaction of GABITRIL with Other Drugs : Theophylline: A single 10 mg dose of tiagabine did not affect the pharmacokinetics of theophylline at steady state. Warfarin: No significant differences were observed in the steady-state pharmacokinetics of R-warfarin or S-warfarin with the addition of tiagabine given as a single dose. Prothrombin times were not affected by tiagabine. Digoxin: Concomitant administration of tiagabine did not affect the steady-state pharmacokinetics of digoxin or the mean daily trough serum level of digoxin. Ethanol or Triazolam: No significant differences were observed in the pharmacokinetics of triazolam (0.125 mg) and tiagabine (10 mg) when given together as a single dose. The pharmacokinetics of ethanol were not affected by multiple-dose administration of tiagabine. Tiagabine has shown no clinically important potentiation of the pharmacodynamic effects of triazo lam or alcohol. Because of the possible additive effects of drugs that may depress the nervous system, ethanol or triazolam should be used cautiously in combination with tiagabine. Oral Contraceptives: Multiple dose administration of tiagabine (8 mg/day monotherapy) did not alter the pharmacokinetics of oral contraceptives in healthy women of childbearing age. Antipyrine : Antipyrine pharmacokinetics were not significantly different before and after tiagabine multiple-dose regimens. This indicates that tiagabine does not cause induction or inhibition of the hepatic microsomal enzyme systems responsible for the metabolism of antipyrine. Interaction of GABITRIL with Highly Protein Bound Drugs: Chemical IUPAC Name 1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylicacid Chemical Formula C20H25NO2S2 Half Life 7-9 hours Drug Type Approved Drug # Accession No APRD00344 CAS Registry Number 115103-54-3 |
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