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QuickView for Valproic acid (compound)


PubChem
Name: Valproic Acid
PubChem Compound ID: 10154225
Description: A fatty acid with anticonvulsant properties used in the treatment of epilepsy. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of voltage dependent sodium channels.
Molecular formula: C8H16NaO2
Molecular weight: 167.201 g/mol
DrugBank
Identification
Name: Valproic Acid
Name (isomeric): DB00313
Drug Type: small molecule
Description: A fatty acid with anticonvulsant properties used in the treatment of epilepsy. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of voltage dependent sodium channels.
Synonyms:
Valproato semisodico [Spanish]; n-Dipropylacetic acid; Propylvaleric acid; Myproic Acid; Valproate semisodique [French]; Valproate semisodium; Kyselina 2-propylvalerova; Di-n-propylacetic acid; DPA; Sodium hydrogen divalproate.
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Brand: Convulex, Penta-Valproic, Mylproin, Epilim, Epival, Depakene, Valproic acid USP, Sprinkle, Nu-Valproic, Valcote, Alti-Valproic, Deproic, Baceca, Valparin, Delepsine, Dom-Valproic, Novo-Valproic, PMS-Valproic Acid, Ergenyl, Valproic acid USP24, Epilex, Avugane, Med Valproic, Depakine
Category: GABA Agents, Enzyme Inhibitors, Antimanic Agents, Anticonvulsants
CAS number: 99-66-1
Pharmacology
Indication: For use as sole and adjunctive therapy in the treatment of simple and complex absence seizures, and adjunctively in patients with multiple seizure types which include absence seizures.
Pharmacology:
Valproic Acid is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder. It is also used to treat migraine headaches and schizophrenia. In epileptics, valproic acid is used to control absence seizures, tonic-clonic seizures (grand mal), complex partial seizures, and the seizures associated with ...
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Mechanism of Action:
Valproic Acid binds to and inhibits GABA transaminase. The drug's anticonvulsant activity may be related to increased brain concentrations of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the CNS, by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. Valproic Acid may also work by ...
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Absorption: Rapid absorption from gastrointestinal tract.
Protein binding: The plasma protein binding of valproate is concentration dependent and the free fraction increases from approximately 10% at 40 µg/mL to 18.5% at 130 µg/mL.
Biotransformation: Valproic Acid is metabolized almost entirely by the liver. In adult patients on monotherapy, 30-50% of an administered dose appears in urine as a glucuronide conjugate. Mitochondrial ß-oxidation is the other major metabolic pathway, typically accounting for over 40% of the dose. Usually, less than 15-20% of the dose is eliminated by other oxidative mechanisms. Less than 3% of an administered dose is excreted unchanged in urine.
Route of elimination: Valproate is metabolized almost entirely by the liver. Less than 3% of an administered dose is excreted unchanged in urine.
Half Life: 9-16 hours
Clearance: total valproate cl=0.56 L/hr/1.73 m2 free valproate cl=4.6 L/hr/1.73 m2 4.8 +/- 0.17 L/hr/1.73 m2 [males, unbound clearance] 4.7+/- 0.07 L/hr/1.73 m2 [females, unbound clearance]
Toxicity: Oral, mouse: LD50 = 1098 mg/kg; Oral, rat: LD50 = 670 mg/kg. Symptoms of overdose may include coma, extreme drowsiness, and heart problems.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Do not take with milk.
Take with food.
Drug interaction:
CarbamazepineDecreases the effect of valproic acid
LamotrigineValproic acid may increase the adverse effects of Lamotrigine by increasing Lamotrigine serum concentration. The Lamotrigine dose should be reduced by 50% during concomitant therapy. Monitor for changes in Lamotrigine therapeutic and adverse effects if Valproic acid is initiated, discontinued or dose changed.
TipranavirTipranavir decreases the concentration of Valproic acid. Monitor Valproid acid efficacy.
RifampinRifampin may reduce the serum concentration of Valproic acid by increasing Valproic acid metabolism. Valproic acid dose adjustments may be required during concomitant therapy. Monitor Valproic acid serum concentrations, efficacy and toxicity if Rifampin is initiated, discontinued or dose changed.
FelbamateFelbamate, a CYP2C19 inhibitor, may decrease the metabolism of Valproic acid, a CYP2C19 substrate. Consider alternate therapy or monitor for changes in Valproic acid therapeutic and adverse effects if Felbamate is initiated, discontinued or dose changed.
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