QuickView for Divalproex sodium (compound)

Summary
General Info

DrugBank

Identification

Name:	Divalproex Sodium
Name (isomeric):	DB00510
Drug Type:	small molecule
Synonyms:	Valproate semisodium
Brand:	Depakote CP, Depakote, Epival, Depakote Sprinkle, Depakote ER
Category:	GABA Agents, Antimanic Agents, Anticonvulsants
CAS number:	76584-70-8

Pharmacology

Indication:	For treatment and management of seizure disorders, mania, and prophylactic treatment of migraine headache.
Pharmacology:	Divalproex is a stable co-ordination compound comprised of sodium valproate and valproic acid in a 1:1 molar relationship and formed during the partial neutralization of valproic acid with 0.5 equivalent of sodium hydroxide. Divalproex is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder. I... show more » Divalproex is a stable co-ordination compound comprised of sodium valproate and valproic acid in a 1:1 molar relationship and formed during the partial neutralization of valproic acid with 0.5 equivalent of sodium hydroxide. Divalproex 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, divalproex is used to control absence seizures, tonic-clonic seizures (grand mal), complex partial seizures, and the seizures associated with Lennox-Gastaut syndrome. Divalproex is believed to affect the function of the neurotransmitter GABA (as a GABA transaminase inhibitor) in the human brain. Divalproex dissociates to the valproate ion in the gastrointestinal tract. show less «
Mechanism of Action:	Divalproex 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. Divalproex may also work by suppre... show more » Divalproex 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. Divalproex may also work by suppressing repetitive neuronal firing through inhibition of voltage-sensitive sodium channels. show less «
Absorption:	Rapid absorption from gastrointestinal tract.
Protein binding:	80-90%
Biotransformation:	Divalproex is metabolized almost entirely by the liver. Mitochondrial ß-oxidation is the other major metabolic pathway, typically accounting for over 40% of the dose.
Route of elimination:	Valproate is metabolized almost entirely by the liver.
Half Life:	9-16 hours
Toxicity:	Overdosage with divalproex may result in somnolence,heart block,and deep coma. Fatalities have been reported; however patients have recovered from divalproex levels as high as 2120 µg/mL.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take with food to reduce irritation.

Food slows the rate of absorption but the extent of absorption is not affected.

Drug interaction:

Acetylsalicylic acid	Acetylsalicylic acid increases the effect of divalproex sodium.
Talbutal	Divalproex sodium increases the effect of the barbiturate, talbutal.
Primidone	Divalproex sodium increases the effect of the barbiturate, primidone.
Mephenytoin	Valproate increases the effect of hydantoin
Magnesium salicylate	The salicylate, magnesium salicylate, increases the effect of divalproex sodium.

Acetylsalicylic acid	Acetylsalicylic acid increases the effect of divalproex sodium.
Talbutal	Divalproex sodium increases the effect of the barbiturate, talbutal.
Primidone	Divalproex sodium increases the effect of the barbiturate, primidone.
Mephenytoin	Valproate increases the effect of hydantoin
Magnesium salicylate	The salicylate, magnesium salicylate, increases the effect of divalproex sodium.
Cholestyramine	Cholestyramine decreases the levels of valproate
Felbamate	Felbamate increases the effect of valproate
Trisalicylate-choline	The salicylate, trisalicylate-choline, increases the effect of divalproex sodium.
Pentobarbital	Divalproex sodium increases the effect of the barbiturate, pentobarbital.
Methylphenobarbital	Divalproex sodium increases the effect of the barbiturate, methylphenobarbital.
Dihydroquinidine barbiturate	Divalproex sodium increases the effect of the barbiturate, dihydroquinidine barbiturate.
Nimodipine	Valproic acid increases the effect of nimodipine
Phenobarbital	Divalproex sodium may increase the effect of the barbiturate, phenobarbital.
Fosphenytoin	Valproate increases the effect of hydantoin
Hexobarbital	Divalproex sodium increases the effect of the barbiturate, hexobarbital.
Bismuth Subsalicylate	The salicylate, bismuth subsalicylate, increases the effect of divalproex sodium.
Risperidone	Risperidone increases the effect and toxicity of valproic acid
Butalbital	Divalproex sodium increases the effect of the barbiturate, butalbital.
Amobarbital	Divalproex sodium increases the effect of the barbiturate, amobarbital.
Erythromycin	Erythromycin increases the effect of valproic acid
Butethal	Divalproex sodium increases the effect of the barbiturate, butethal.
Secobarbital	Divalproex sodium increases the effect of the barbiturate, secobarbital.
Salicylate-sodium	The salicylate, salicylate-sodium, increases the effect of divalproex sodium.
Aprobarbital	Divalproex sodium increases the effect of the barbiturate, aprobarbital.
Methohexital	Divalproex sodium increases the effect of the barbiturate, methohexital.
Ritonavir	Possible decrease of valproate levels
Quinidine barbiturate	Divalproex sodium increases the effect of the barbiturate, quinidine barbiturate.
Butabarbital	Divalproex sodium increases the effect of the barbiturate, butabarbital.
Salsalate	The salicylate, salsalate, increases the effect of divalproex sodium.
Ethotoin	Valproate increases the effect of hydantoin
Carbamazepine	Carbamazepine may decrease the effect of divalproex by increasing it metabolism. Divalproex may decrease the serum concentration of carbamazepine. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or altered (i.e. dosages adjusted).
Heptabarbital	Divalproex sodium increases the effect of the barbiturate, heptabarbital.
Lamotrigine	Valproic acid increases the effect of lamotrigine
Meropenem	Decreased plasma antiepileptic levels
Josamycin	Erythromycin increases the effect of valproic acid
Phenytoin	Valproate increases the effect of hydantoin

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Targets

4-aminobutyrate aminotransferase, mitochondrial