Drug intelligence / Profile preview

gabapentin + buprenorphine

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Sublingual, Transdermal, Buccal, Intravenous, Intramuscular, Subcutaneous
01

Overview

Gabapentin + buprenorphine is a combination of two pharmaceutical drugs, each with distinct mechanisms of action. Gabapentin is an anticonvulsant and neuropathic pain agent that modulates the activity of voltage-gated calcium channels in the central nervous system, thereby reducing neuronal excitability and neurotransmitter release. It is primarily used for epilepsy, neuropathic pain, and restless leg syndrome[6][10]. Buprenorphine is a partial agonist at the mu-opioid receptor and antagonist at the kappa-opioid receptor; it acts as an opioid analgesic and is widely used in opioid use disorder (OUD) treatment to reduce withdrawal symptoms and cravings[8]. When combined, these drugs can potentiate each other's central nervous system depressant effects, increasing risks such as sedation, respiratory depression, impaired cognition, coma or death. This combination should only be used under close medical supervision due to significant interaction risks[1][4][5].

02

Targets

KOR (Kappa opioid receptor)MOR (Mu opioid receptor)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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