About: Vigabatrin     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • An analogue of gamma-aminobutyric acid, vigabatrin 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). Off-label uses include treatment of cocaine dependence. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # 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":http://www.ncbi.nlm.nih.gov/pubmed/2757904 # Browne TR: Pharmacokinetics of antiepileptic drugs. Neurology. 1998 Nov;51(5 Suppl 4):S2-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9818917 # 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":http://www.ncbi.nlm.nih.gov/pubmed/12883229 # 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":http://www.ncbi.nlm.nih.gov/pubmed/11682253 # Tulloch JK, Carr RR, Ensom MH: A systematic review of the pharmacokinetics of antiepileptic drugs in neonates with refractory seizures. J Pediatr Pharmacol Ther. 2012 Jan;17(1):31-44. doi: 10.5863/1551-6776-17.1.31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23118657 # Clayton LM, Stern WM, Newman WD, Sander JW, Acheson J, Sisodiya SM: Evolution of visual field loss over ten years in individuals taking vigabatrin. Epilepsy Res. 2013 Mar 28. pii: S0920-1211(13)00074-0. doi: 10.1016/j.eplepsyres.2013.02.014. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23541931 # Hawker DD, Silverman RB: Synthesis and evaluation of novel heteroaromatic substrates of GABA aminotransferase. Bioorg Med Chem. 2012 Oct 1;20(19):5763-73. doi: 10.1016/j.bmc.2012.08.009. Epub 2012 Aug 16. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22944334 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Neonates, 50 mg/kg = 7.5 ± 2.1 hours (due to reduced renal function); Infants = 5.7 hours; Adults = 7.5 hours; Elderly = 12 - 13 hours (en)
http://linked.open...ugbank/indication
  • For use as an adjunct in treatment resistant epilepsy, refractory complex partial seizures, and secondary generalized seizures. It is also used as monotherapy in infantile spasms in West syndrome. (en)
sameAs
Title
  • Vigabatrin (en)
adms:identifier
http://linked.open...mechanismOfAction
  • 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). Duration of action is determined by rate of GABA-T re-synthesis. Vigabatrin may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels. Although administered as a racemic mixture, only the S(+) enantiomer is pharmacologically active. (en)
http://linked.open...drugbank/packager
http://linked.open...outeOfElimination
  • Eliminated primarily through renal excretion as unchanged drugs (80%). (en)
http://linked.open.../drugbank/synonym
  • Vigabatrin (en)
  • 4-Amino-5-hexenoic acid (en)
  • GVG (en)
  • Vigabatrine (en)
  • gamma-Vinyl GABA (en)
  • Vigabatrina (en)
  • Vigabatrinum (en)
  • gamma-Vinyl-gamma-aminobutyric acid (en)
http://linked.open...drugbank/toxicity
  • LD50, oral, rat: 3000 mg/kg; Visual field defects may occur following cumulative doses in excess of 2 kg. (en)
http://linked.open...umeOfDistribution
  • 1.1 L/kg (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • Not protein bound (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
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http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Rapidly absorbed following oral administration, absorption is comparable between neonates, infants, and children. Cmax, 50 mg/kg dose, neonates= 14 mg/L; Tmax, 50 mg/kg dose, neonates = 2.1 hours; However, extent of absorption is higher and elimination half life is longer in neonates compared to children and infants. This is because neonates have reduced renal function compared to the aforementioned population groups. AUC, 50 mg/kg dose, neonates = 142.6 ± 44.0 mg/L/hr; Food may slightly decrease the rate (Cmax decreased by 33%, Tmax increased to 2 hours), but not the extent of absorption. Furthermore, vigabatrin does not cross the blood-brain-barrier well, thus high doses are needed. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 60643-86-9 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • Infants = 2.4 ± 0.8 L/h; Children = 5.7 ± 2.5 L/h (en)
http://linked.open...gbank/containedIn
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http://linked.open...bank/Ghose-Filter
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http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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