Drug intelligence / Profile preview

diazepam + gabapentin

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Rectal
01

Overview

Diazepam + gabapentin is a combination of two pharmaceutical drugs, each with distinct mechanisms of action. Diazepam is a long-acting benzodiazepine that acts as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor, enhancing the inhibitory effects of GABA in the central nervous system. It is primarily used for anxiety disorders, muscle spasms, alcohol withdrawal symptoms, and as an adjunct in certain seizure disorders[6][8]. Gabapentin is an anticonvulsant and structural analogue of GABA but does not bind directly to GABA receptors; instead, it binds to the alpha-2-delta subunit of voltage-gated calcium channels in the CNS, reducing excitatory neurotransmitter release. Gabapentin is mainly indicated for partial seizures and neuropathic pain[4][10]. The combination may be used off-label under special circumstances where both indications overlap (such as complex seizure management or severe neuropathic pain with comorbid anxiety), but co-administration increases risks such as CNS depression (drowsiness, dizziness, confusion) and should be closely monitored[1][3][9].

02

Targets

CACNA2D2 (α2δ-2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)GABRR (GABA-A receptor subunit rho)

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