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QuickView for Vigabatrin (compound)


PubChem
Name: Vigabatrin
PubChem Compound ID: 10219440
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)
Molecular formula: C6H11NO2
Molecular weight: 129.157 g/mol
DrugBank
Identification
Name: Vigabatrin
Name (isomeric): DB01080
Drug Type: small molecule
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)
Brand: 4-Amino-5-hexenoic acid, GVG, gamma-Vinyl GABA, Vigabatrine, Vigabatrine [French], Vigabatrinum [Latin], Vigabatrin [USAN:BAN:INN], Sabril (TN), 4-Aminohexenoic acid, Vigabatrina [Spanish]
Category: GABA Agents, Enzyme Inhibitors, Anticonvulsants
CAS number: 60643-86-9
Pharmacology
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.
Mechanism of Action:
It is believed that vigabatrin increases brain concentrations of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the CNS, by irreversibly inhibiting enzymes that catabolize GABA (gamma-aminobutyric acid transaminase GABA-T) or block the reuptake of GABA into glia and nerve endings. Vigabatrin may also work by suppressing repetitiv...
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Absorption: Rapidly absorbed following oral administration. Food may slightly decrease the rate, but not the extent, of absorption.
Protein binding: Little to none
Biotransformation: Almost no metabolic transformation. Does not induce the hepatic cytochrome P450 system.
Route of elimination: Vigabatrin is not significantly metabolized; it is eliminated primarily through renal excretion.
Half Life: 5-8 hours in young adults, 12-13 hours in elderly.
Clearance: 2.4 +/- 0.8 L/h [Infant] 5.7 +/- 2.5 L/h [Children]
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TriprolidineThe CNS depressants, Triprolidine and Vigabatrin, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
MefloquineMefloquine may decrease the serum concentration of Vigabatrin. This may increase the risk of seizure in patients receiving Vigabatrin to prevent seizures. Consider alternate therapy or monitor for changes in Vigabatrin serum concentration, therapeutic or adverse effects if Mefloquin is initiated, discontinued or dose changed.
FosphenytoinVigabatrin decreases the effect of hydantoin
PhenytoinVigabatrin decreases the effect of hydantoin
MethotrimeprazineAdditive CNS depression may occur. Dose adjustments may be required if one agent is added to existing therapy with the other agent. Monitor for increased CNS depression during concomitant therapy.

Targets