Drug intelligence / Profile preview

dezocine

Development stage
Phase 4
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Dezocine is an atypical opioid analgesic primarily used for the treatment of moderate to severe pain. It acts as a partial agonist at the μ-opioid receptor and as an antagonist at the κ-opioid receptor, with additional activity as a serotonin–norepinephrine reuptake inhibitor. Dezocine provides potent analgesia comparable to or greater than morphine and is often administered intravenously or intramuscularly, especially in postoperative settings. Unlike other opioids acting on the κ-opioid receptor, it does not cause dysphoria or hallucinations at therapeutic doses. Dezocine was first synthesized in 1970 and introduced for medical use in 1986; while discontinued in the United States since 2011, it remains widely used in China[1][2][5]. Its side effect profile includes dizziness and mild gastrointestinal discomfort; respiratory depression has a ceiling effect at higher doses[1]. The drug is metabolized hepatically via glucuronidation[2].

Brand names
Dalgan
Other names
地佐辛
02

Targets

KOR (Kappa opioid receptor)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)MOR (Mu opioid receptor)

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