Drug intelligence / Profile preview

alprazolam + gabapentin + dexmedetomidine

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

A combination of three central nervous system active medications. **Alprazolam** is a benzodiazepine that binds to GABA type-A receptors to enhance their inhibitory effect on neurotransmission. It has anxiolytic properties. **Gabapentin** has anxiolytic and antinociceptive properties. It is used for treatment of postherpetic neuralgia, adjunctive treatment of partial-onset seizures, and various types of peripheral neuropathic pain. **Dexmedetomidine** is a highly selective α2 agonist used as a sedative in various clinical settings. It provides sedation with minimal respiratory depression. When combined, these medications can have additive central nervous system (CNS) depressant effects, including sedation and respiratory depression. Drug interactions between the components are noted as moderate (dexmedetomidine and gabapentin; alprazolam and gabapentin) or increasing the risk/severity of CNS depression (dexmedetomidine and alprazolam). This combination requires careful monitoring for excessive sedation, respiratory depression, and hemodynamic changes.

02

Targets

GABRR (GABA-A receptor subunit rho)ADRA2A (α2A)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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