Drug intelligence / Profile preview

dextromoramide

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous, Rectal
01

Overview

Dextromoramide is a potent synthetic opioid analgesic structurally related to methadone and classified as a diphenylmethane derivative. It is approximately three times more potent than morphine but has a shorter duration of action. Dextromoramide acts primarily as an agonist at the mu-opioid receptor (MOR) in the central nervous system, inhibiting neurotransmitter release and providing rapid and effective pain relief within 15–30 minutes of administration. Its high oral bioavailability allows for effective oral dosing with minimal difference from parenteral administration. The drug is mainly used for the management of severe pain conditions such as post-operative pain, cancer-related pain, and certain chronic pain syndromes[1][2][6][7]. Tolerance develops relatively slowly compared to other short-acting opioids, and it tends to cause less constipation than many other opioids[1]. Dextromoramide was originally developed by Paul Janssen.

Brand names
PalfiumPalphiumJetriumDimorlin
Other names
dextromoramide tartrate
02

Targets

MOR (Mu opioid receptor)

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