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promethazine
- Development stage
- Approved
- Lead developer
- Sanofi
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular, Intravenous, Rectal, Topical
01
Overview
Promethazine is a first-generation antihistamine and phenothiazine derivative used primarily to treat allergy symptoms, prevent motion sickness, manage nausea and vomiting, provide sedation before or after surgery, and as an adjunct for pain relief. It acts mainly as a strong antagonist of the histamine H1 receptor (antihistaminic effect), but also exhibits anticholinergic (muscarinic acetylcholine receptor antagonist), antiemetic, sedative-hypnotic, antivertigo, and local anesthetic properties. Promethazine also has moderate affinity for serotonin 5-HT2A/2C receptors, dopamine D2 receptors, alpha-1 adrenergic receptors (all as antagonists), and is a non-competitive NMDA receptor antagonist. Its sedative effects are thought to result from central antagonism at histamine H1 receptors with additional contributions from other neurotransmitter systems[1][3][4][5][6].
- Brand names
- PhenerganPrometheganPhenadoz
- Other names
- promethazine
02
Targets
HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)HTR3A (5-hydroxytryptamine receptor 3A)mAChR (Muscarinic acetylcholine receptors)NMDAR (Glutamate receptor ionotropic, NMDA)DRD2 (Dopamine D2 Receptor)HRH1 (Histamine H1 Receptor)KCNH2 (Voltage-gated potassium channel subfamily H member 2)
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