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Systemic pharmacokinetic interaction: aripiprazole + valproic acid

Molecular classification
Other
01

Overview

The term "Systemic pharmacokinetic interaction: aripiprazole + valproic acid" refers to the clinical drug-drug interaction (DDI) profile between the atypical antipsychotic aripiprazole and the mood stabilizer valproic acid. This entry does not describe a single biological target, such as a receptor or enzyme, but rather the metabolic relationship between two therapeutic agents when co-administered. Aripiprazole is primarily metabolized by the hepatic cytochrome P450 enzymes CYP3A4 and CYP2D6 (FDA, 2021). Clinical studies have shown that valproate co-administration leads to a modest decrease (approximately 25%) in aripiprazole exposure (Cmax and AUC), which is generally not considered clinically significant enough to warrant dose adjustments (Citrome et al., 2005). Conversely, aripiprazole does not appear to significantly alter the steady-state concentrations of valproate. Monitoring this interaction is essential in psychiatric polypharmacy, particularly for patients with bipolar disorder or schizophrenia, to ensure optimal therapeutic outcomes and to monitor for additive side effects like sedation or tremors.

Other names
Aripiprazole-valproate interactionAripiprazole-valproic acid pharmacokinetic interactionPharmacokinetic interaction of aripiprazole and valproate
02

Mechanism of action

Pharmacokinetic interaction involving the modulation of hepatic metabolism via CYP3A4 and CYP2D6 enzymes.

03

Biological functions

Other
04

Disease associations

Bipolar disorderSchizophreniaMania
05

Safety considerations

Additive sedationWeight gainGastrointestinal disturbancesTremor
06

Interacting drugs

Aripiprazole

1 more in the full profile.

07

Biomarkers

Serum aripiprazole concentrationSerum valproic acid concentrationCYP3A4 activityCYP2D6 activity

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