| Item |
Information |
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Drug Groups
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approved |
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Description
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An analogue of gamma-aminobutyric acid. It is an irreversible inhibitor of 4-aminobutyrate transaminase, the enzyme responsible for the catabolism of gamma-aminobutyric acid. (From Martindale The Extra Pharmacopoeia, 31st ed) |
| Indication |
For use as an adjunctive treatment (with other drugs) in treatment resistant epilepsy, complex partial seizures, secondary generalized seizures, and for monotherapy use in infantile spasms in West syndrome. |
| Pharmacology |
Vigabatrin, is an anticonvulsant chemically unrelated to other anticonvulsants. Vigabatrin inhibits the catabolism of GABA. It is an analog of GABA, but it is not a receptor agonist. Vigabatrin irreversibly inhibits the enzyme GABA transaminase. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Almost no metabolic transformation. Does not induce the hepatic cytochrome P450 system. |
| Absorption |
Rapidly absorbed following oral administration. Food may slightly decrease the rate, but not the extent, of absorption. |
| Half Life |
5-8 hours in young adults, 12-13 hours in elderly. |
| Protein Binding |
Little to none |
| Elimination |
Vigabatrin is not significantly metabolized; it is eliminated primarily through renal excretion. |
| Distribution |
* 1.1 L/kg |
| Clearance |
* 2.4 +/- 0.8 L/h [Infant]
* 5.7 +/- 2.5 L/h [Children] |
| References |
| • |
Gram L, Larsson OM, Johnsen A, Schousboe A: Experimental studies of the influence of vigabatrin on the GABA system. Br J Clin Pharmacol. 1989;27 Suppl 1:13S-17S.
[Pubmed]
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| • |
Browne TR: Pharmacokinetics of antiepileptic drugs. Neurology. 1998 Nov;51(5 Suppl 4):S2-7.
[Pubmed]
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| • |
Lindberger M, Luhr O, Johannessen SI, Larsson S, Tomson T: Serum concentrations and effects of gabapentin and vigabatrin: observations from a dose titration study. Ther Drug Monit. 2003 Aug;25(4):457-62.
[Pubmed]
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| • |
Zwanzger P, Baghai TC, Schuele C, Strohle A, Padberg F, Kathmann N, Schwarz M, Moller HJ, Rupprecht R: Vigabatrin decreases cholecystokinin-tetrapeptide (CCK-4) induced panic in healthy volunteers. Neuropsychopharmacology. 2001 Nov;25(5):699-703.
[Pubmed]
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