Drug intelligence / Profile preview

desomorphine

Development stage
Unknown
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous
01

Overview

Desomorphine is a semi-synthetic opioid analgesic first synthesized in the United States in 1932 and briefly marketed by Hoffman-LaRoche under the brand name Permonid for post-operative pain. It is a morphinane alkaloid and a derivative of morphine with modifications that make it more lipophilic and about 8–10 times more potent than morphine. Desomorphine acts primarily as a mu-opioid receptor agonist with less activity at kappa- and delta-opioid receptors. It has a faster onset of action and shorter duration compared to morphine but carries an increased risk of dependence, respiratory depression, hypotension, urinary retention, and other side effects. Medical use was discontinued due to its high addictive potential and severe adverse effects. In recent years, illicitly produced desomorphine—commonly known as "krokodil"—has been used recreationally as a cheap heroin substitute; this form is often contaminated with toxic byproducts leading to severe tissue damage at injection sites[1][3][4][7][8].

Brand names
Permonid
Other names
krokodilcrocodildesomorfina
02

Targets

KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)

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