User:Mr. Ibrahem/Valproate
Clinical data | |
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Trade names | Depakote, Epilim, Convulex, others |
Other names | Valproic acid; Sodium valproate (sodium); Valproate semisodium (semisodium); 2-Propylvaleric acid |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682412 |
License data |
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Pregnancy category |
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Routes of administration | By mouth, intravenous |
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Pharmacokinetic data | |
Bioavailability | Rapid absorption |
Protein binding | 80–90%[1] |
Metabolism | Liver—glucuronide conjugation 30–50%, mitochondrial β-oxidation over 40% |
Elimination half-life | 9–16 hours[1] |
Excretion | Urine (30–50%)[1] |
Identifiers | |
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Chemical and physical data | |
Formula | C8H16O2 |
Molar mass | 144.211 g·mol−1 |
3D model (JSmol) | |
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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]
- ^ 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.
- ^ 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.
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 22 September 2020.
- ^ "Valproate banned without the pregnancy prevention programme". GOV.UK. Retrieved 26 April 2018.
- ^ Owens MJ, Nemeroff CB (2003). "Pharmacology of valproate". Psychopharmacol Bull. 37 Suppl 2: 17–24. PMID 14624230.
- ^ 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.
- ^ "Valproic acid". DrugBank. University of Alberta. 29 July 2017. Archived from the original on 31 July 2017. Retrieved 30 July 2017.
- ^ 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.
- ^ 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.
- ^ International Medical Products Price Guide (PDF) (2015 ed.). Management Sciences for Health. 2016. p. A-140. Retrieved 23 February 2020.
- ^ "NADAC as of 2019-11-27 | Data.Medicaid.gov". Centers for Medicare and Medicaid Services. Retrieved 25 November 2019.
- ^ "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
- ^ "Divalproex Sodium - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.