Drug intelligence / Profile preview

remifentanil + naloxone

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Intranasal
01

Overview

Remifentanil + naloxone is a combination of two drugs with opposing actions on the opioid system. Remifentanil is a potent, ultra-short-acting synthetic opioid analgesic used primarily as an adjunct to anesthesia for pain management during surgical procedures. It acts as a selective agonist at the mu-opioid receptor, producing rapid-onset and short-duration analgesia, sedation, and respiratory depression[2][6]. Naloxone is an opioid antagonist that rapidly reverses or blocks the effects of opioids by competitively binding to mu-opioid receptors without activating them. It is used in emergency settings to counteract life-threatening central nervous system and respiratory depression caused by opioid overdose[8][10]. The combination of remifentanil with naloxone would theoretically provide potent analgesia (from remifentanil) while allowing for rapid reversal or mitigation of opioid-induced adverse effects (via naloxone). However, there are no known approved pharmaceutical products combining these two agents directly; their interaction is clinically relevant when naloxone is administered to reverse remifentanil’s effects.

02

Targets

MOR (Mu opioid receptor)

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