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The Sound of Evolution
Promethazine
Mechanism of action:
Promethazine is a first-generation antihistamine and a phenothiazine derivative. Promethazine blocks central and peripheral H1 receptors, thereby inhibiting histamine-induced vasodilation and increased capillary permeability. Promethazine can also suppress the chemoreceptor trigger zone (CTZ) in the medulla, reducing vomiting reflexes triggered by various stimuli.
Reference(s):
1. Halpern BN et al. (1948). A new synthetic anti-histamine substance derived from phenothiazine; phenergan, 3,277 R.P. Can Med Assoc J.
2. Nakamura K et al. (1996). CYP2D6 is the principal cytochrome P450 responsible for metabolism of the histamine H1 antagonist promethazine in human liver microsomes. Pharmacogenetics.
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