Chemical Property of Vigabatrin
Chemical Property:
- Melting Point:209°
- Boiling Point:73?°C749?mm Hg(lit.)
- Flash Point:9℃
- PSA：63.32000
- Density:1.108?g/mL?at 25?°C(lit.)
- LogP:1.06480
- Storage Temp.:Desiccate at +4°C
- Solubility.:Freely soluble in water, slightly soluble in methanol, practically insoluble in methylene chloride.
- Purity/Quality:
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99%, *data from raw suppliers
Vigabatrin *data from reagent suppliers
Safty Information:
- Pictogram(s):
R36/37/38:;
- Hazard Codes:Xi,T,F
- Statements:
36/37/38-39/23/24/25-23/24/25-11
- Safety Statements:
26-36-45-36/37-16-7
- MSDS Files:
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SDS file from LookChem
Total 1 MSDS from other Authors
Useful:
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Description
Vigabatrin is a second- generation anti- epileptic drug (AED), known under the proprietary brand name of Sabril? (Sanofi, Paris) in the UK and USA. Vigabatrin, the gamma-vinyl derivative of GABA, is a new anticonvulsant reportedly
effective in the treatment of intractable seizures unresponsive to currently available
therapy. Mechanistically vigabatrin is a potent irreversible GABA aminotransferase
inhibitor which modifies the enzyme's active-site by Michael addition. Other potential
indications have been suggested for vigabatrin, including depression and schizophrenia.
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Indications
Epilepsy: adjunctive therapy of focal seizures with or without secondary generalization not satisfactorily controlled with other AEDs.
Recommendations summarized from NICE (2012)
Seizure types: on referral to tertiary care (focal seizures), contraindicated (generalized tonic- clonic seizures, tonic/ atonic seizures, absence seizures, myoclonic seizures).
Epilepsy types: on referral to tertiary care (benign epilepsy with centrotemporal spikes, panayiotopoulos syndrome, late- onset childhood occipital epilepsy), contraindicated (absence syndromes, idiopathic generalized epilepsy, juvenile myoclonic epilepsy, Dravet syndrome, Lennox– Gastaut syndrome).
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Uses
antineoplastic antibiotic Vigabatrin is a selective GABA transaminase inhibitor.
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Biological Functions
Vigabatrin (Sabril) is a relatively specific irreversible inhibitor
of GABA-transaminase (GABA-T), the major
enzyme responsible for the metabolism of GABA in the
mammalian CNS. As a result of inhibition of GABA-T,
there is an increase in the concentration of GABA in the
brain and consequently an increase in inhibitory neurotransmission.
Vigabatrin is well absorbed orally and is
distributed to all body systems.The major route of elimination
for vigabatrin is renal excretion of the parent compound;
no metabolites have been identified in humans.
At present, the primary indication for vigabatrin is
in the treatment of patients with partial seizures, but it
appears to be an effective and generally well tolerated
antiepileptic medication for other seizure types as well.
It should not be used in patients with absence epilepsy
or with myoclonic seizures. Vigabatrin is not approved
as an AED in the United States, although it is approved
in many other countries.
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Drug interactions
Potentially hazardous interactions with other drugs
Antidepressants: anticonvulsant effect antagonised,
convulsive threshold lowered; avoid with St John’s
wort.
Antiepileptics: concentration of phenytoin reduced.
Antimalarials: mefloquine antagonises
anticonvulsant effect.
Antipsychotics: anticonvulsant effect antagonised.
Orlistat: increased risk of convulsions.
