物质信息
ID:955
名称和标识
商标名
Vigabatrin [USAN:BAN:INN]Vigabatrina [Spanish]Vigabatrine [French]4-Aminohexenoic acidSabril (TN)GVGVigabatrineVigabatrinum [Latin]gamma-Vinyl GABA4-Amino-5-hexenoic acid
IUPAC标准名
4-aminohex-5-enoic acid
IUPAC传统名
vigabatrin
别名
Vigabatrin
化合物性质
理化性质
溶解度
55.1 mg/mL
疏水性(logP)
0.1
描述信息
Drug Groups
approved
Description
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
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]
* 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]
•
Browne TR: Pharmacokinetics of antiepileptic drugs. Neurology. 1998 Nov;51(5 Suppl 4):S2-7.
[Pubmed]
•
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]
•
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]
External Links
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参考文献
• Browne TR: Pharmacokinetics of antiepileptic drugs. Neurology. 1998 Nov;51(5 Suppl 4):S2-7. Pubmed
• 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
• 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
• 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