Drug intelligence / Profile preview

butorphanol + propofol

Development stage
Phase 4
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous
01

Overview

Butorphanol + propofol is a combination of two pharmaceutical agents used primarily for procedural sedation and anesthesia. Propofol is a rapid-acting sedative-hypnotic agent that acts as a positive allosteric modulator of the GABA-A receptor, enhancing inhibitory neurotransmission in the central nervous system. Butorphanol is a synthetic opioid analgesic with mixed agonist-antagonist activity, primarily acting as an agonist at kappa opioid receptors and partial agonist/antagonist at mu opioid receptors, providing analgesia and sedation with relatively less respiratory depression compared to other opioids. The combination allows for reduced doses of each drug, minimizing adverse effects such as respiratory depression and hemodynamic instability while maintaining effective anesthesia and analgesia. This regimen has been shown to reduce pain on injection from propofol, decrease total anesthetic requirements, improve postoperative recovery profiles, and lower the incidence of certain anesthesia-related adverse events in procedures such as colonoscopy or painless abortion[1][3][4][5].

02

Targets

GABRB2 (GABA-A receptor subunit beta-2)GABRB3 (GABA-A receptor subunit beta-3)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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