Phenoxybenzamine is a /¡-chloroamine that is structurally related to alkylating agents used in chemotherapy. The mechanism of its long-lasting blockage of a-adrenoreceptors can evidently be explained by its irreversible alkylation. The irreversible blockage most likely occurs after briefly affecting a1- and a^adrenoreceptors. It is possible that the ¡-chlorethylamine region in tissue of the organism forms a highly reactive ethylenimo-nium intermediate, which then alkylates the receptor. Such blockages are irreversible and are called nonequilibrium receptor blockers.
Phenoxybenzamine is used in treating pheochromocytoma, swelling of the medullary layer of the adrenal glands, during which a large quantity of epinephrine is produced, which leads to a significant elevation of blood pressure. A synonym of this drug is diben-zyline.
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