User:Mr. Ibrahem/Valproate

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Mr. Ibrahem/Valproate
INN: valproic acid
Clinical data
Trade namesDepakote, Epilim, Convulex, others
Other namesValproic acid; Sodium valproate (sodium); Valproate semisodium (semisodium); 2-Propylvaleric acid
AHFS/Drugs.comMonograph
MedlinePlusa682412
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth, intravenous
Legal status
Legal status
Pharmacokinetic data
BioavailabilityRapid absorption
Protein binding80–90%[1]
MetabolismLiver—glucuronide conjugation 30–50%, mitochondrial β-oxidation over 40%
Elimination half-life9–16 hours[1]
ExcretionUrine (30–50%)[1]
Identifiers
  • 2-propylpentanoic acid
Chemical and physical data
FormulaC8H16O2
Molar mass144.211 g·mol−1
3D model (JSmol)
  • O=C(O)C(CCC)CCC
  • InChI=1S/C8H16O2/c1-3-5-7(6-4-2)8(9)10/h7H,3-6H2,1-2H3,(H,9,10) checkY
  • Key:NIJJYAXOARWZEE-UHFFFAOYSA-N checkY
  (verify)

Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches.[2] They are useful for the prevention of seizures in those with absence seizures, partial seizures, and generalized seizures.[2] They can be given intravenously or by mouth, and the tablet forms exist in both long- and short-acting formulations.[2]

Common side effects of valproate include nausea, vomiting, sleepiness, and dry mouth.[2] Serious side effects can include liver failure, and regular monitoring of liver function tests is therefore recommended.[2] Other serious risks include pancreatitis and an increased suicide risk.[2] Valproate is known to cause serious abnormalities in babies if taken during pregnancy,[2][4] and as such it is not typically recommended for women of childbearing age who have migraines.[2]

Valproate's precise mechanism of action is unclear.[2][5] Proposed mechanisms include affecting GABA levels, blocking voltage-gated sodium channels, and inhibiting histone deacetylases.[6][7] Valproic acid is a branched short-chain fatty acid (SCFA) made from valeric acid.[6]

Valproate was first made in 1881 and came into medical use in 1962.[8] It is on the World Health Organization's List of Essential Medicines.[9] It is available as a generic medication.[2] The wholesale cost in the developing world is about US$0.40 per day as of 2015.[10] In the United States, the wholesale cost is roughly US$1.30 per day as of 2019.[11] It is marketed under the brand names Depakote, among others.[2] In 2017, it was the 126th most commonly prescribed medication in the United States, with more than five million prescriptions.[12][13]

References[edit]

  1. ^ a b c "Depakene, Stavzor (valproic acid) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 21 February 2014. Retrieved 13 February 2014.
  2. ^ a b c d e f g h i j k l "Valproic Acid". The American Society of Health-System Pharmacists. Archived from the original on 2017-07-31. Retrieved Oct 23, 2015.
  3. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 22 September 2020.
  4. ^ "Valproate banned without the pregnancy prevention programme". GOV.UK. Retrieved 26 April 2018.
  5. ^ Owens MJ, Nemeroff CB (2003). "Pharmacology of valproate". Psychopharmacol Bull. 37 Suppl 2: 17–24. PMID 14624230.
  6. ^ a b Ghodke-Puranik Y, Thorn CF, Lamba JK, Leeder JS, Song W, Birnbaum AK, Altman RB, Klein TE (April 2013). "Valproic acid pathway: pharmacokinetics and pharmacodynamics". Pharmacogenet. Genomics. 23 (4): 236–241. doi:10.1097/FPC.0b013e32835ea0b2. PMC 3696515. PMID 23407051.
  7. ^ "Valproic acid". DrugBank. University of Alberta. 29 July 2017. Archived from the original on 31 July 2017. Retrieved 30 July 2017.
  8. ^ Scott, D.F. (1993). The history of epileptic therapy : an account of how medication was developed (1. publ. ed.). Carnforth u.a.: Parthenon Publ. Group. p. 131. ISBN 9781850703914.
  9. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  10. ^ International Medical Products Price Guide (PDF) (2015 ed.). Management Sciences for Health. 2016. p. A-140. Retrieved 23 February 2020.
  11. ^ "NADAC as of 2019-11-27 | Data.Medicaid.gov". Centers for Medicare and Medicaid Services. Retrieved 25 November 2019.
  12. ^ "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
  13. ^ "Divalproex Sodium - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
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