Drug intelligence / Profile preview

valproic acid + ertapenem

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral (valproic Acid), Intravenous (ertapenem)
01

Overview

This is a combination of two drugs, valproic acid and ertapenem. Valproic acid is an antiepileptic drug primarily used to treat epilepsy and bipolar disorder by increasing gamma-aminobutyric acid (GABA) levels in the brain, thereby stabilizing neuronal activity. Ertapenem is a carbapenem-class broad-spectrum beta-lactam antibiotic used to treat various serious bacterial infections. When administered together, this combination results in a clinically significant drug-drug interaction where ertapenem markedly reduces plasma concentrations of valproic acid, likely by inhibiting the enzyme acylpeptide hydrolase responsible for converting valproic acid-glucuronide back to active valproic acid. This leads to subtherapeutic levels of valproic acid and increases the risk of breakthrough seizures or loss of seizure control. The interaction is considered highly clinically significant; co-administration should generally be avoided unless no alternatives exist[1][2][3][4][5].

02

Targets

ABAT (4-aminobutyrate aminotransferase)PBP (Penicillin-binding protein family)NaV (Voltage-gated sodium channels)

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