Drug intelligence / Profile preview

levacetylmethadol

Development stage
Phase 4
Lead developer
Hikma Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Levacetylmethadol is a synthetic opioid analgesic primarily used for the management of opioid dependence, especially in patients who do not respond adequately to other treatments such as methadone. It acts as an agonist at the mu-opioid receptor, producing effects similar to morphine but with a longer onset and duration of action. Levacetylmethadol is structurally related to methadone and shares many pharmacological properties, including its use in maintenance therapy for narcotic addiction. The drug was approved by the FDA in 1993 but has since been withdrawn from most markets due to safety concerns, particularly life-threatening ventricular arrhythmias (QT interval prolongation). Its principal therapeutic actions are analgesia and sedation, with a slower onset and more prolonged withdrawal syndrome compared to morphine[1][2][3][4].

Brand names
Orlaam
Other names
levomethadyl acetatelevo-alpha-acetylmethadollevacetylmethadol hydrochloride
02

Targets

MOR (Mu opioid receptor)CHRNA3 (nAChR α3 subunit)CHRNB4 (nAChR β4 subunit)

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