Drug intelligence / Profile preview

methadone + fentanyl

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral, Intravenous, Transdermal, Intranasal, Inhalation, Sublingual, Intramuscular
01

Overview

A combination of two potent synthetic opioids. Methadone is a long-acting synthetic opioid analgesic that works as a full μ-opioid receptor agonist and NMDA receptor antagonist. It's used for severe pain management and as a maintenance treatment for opioid use disorder. Methadone has a long duration of action compared to other opioids, making it effective for preventing withdrawal symptoms in people dependent on opioids. Fentanyl is a powerful synthetic opioid that is similar to morphine but 50 to 100 times more potent. It's prescribed for severe pain management but is also manufactured and used illegally. Fentanyl has become a major contributor to overdose deaths in the United States. When combined, they represent a potentially dangerous drug combination due to their additive central nervous system depressant and respiratory depressant effects. This combination can significantly increase the potential for fatal overdoses.

02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)NET (Norepinephrine Transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)MOR (Mu opioid receptor)SERT (Sodium-dependent serotonin transporter)σR (Sigma receptors)

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