Alpha-adrenergic blockade: a possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo.

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Zupko I, Janossy K, Maul K, Marki A, Falkay G

Alpha-adrenergic blockade: a possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo.

Life Sci. 2003 Jan 24;72(10):1093-102.

PubMed ID

12505540 [ View in PubMed

]

Abstract

Benzodiazepines are frequently used for the treatment of maternal psychiatric disorders during pregnancy. Besides their anxiolytic effect, they are reported to exert a direct relaxing action on several smooth muscle preparations, including the uterus. In the present study, the possibility of the involvement of alpha(1)-adrenergic receptors in this peripheral effect is investigated. The tocolytic potencies of diazepam, midazolam and nitrazepam are assessed in vivo in a postpartum rat model, together with other drugs known to bind to alpha-adrenoceptors (e.g. alpha(1)-antagonists, tricyclic compounds and droperidol). The interactions of some benzodiazepines and norepinephrine were also examined in an isolated in vitro system. The affinities of these agents for the receptor in question were additionally tested by radioligand displacement assay. A correlation was found between the tocolytic potencies and inhibition constants of the tested drugs, suggesting that the smooth muscle-relaxing effect of these benzodiazepines is mediated through modulation of the alpha(1)-adrenergic receptors.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Droperidol	Alpha-1A adrenergic receptor	Protein	Humans	Yes	Antagonist	Details