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Review Article

Soft Anticholinergics

[ Vol. 3 , Issue. 1 ]

Author(s):

Gondi N. Kumar and Nicholas Bodor   Pages 23 - 36 ( 14 )

Abstract:


The soft drug (pharmacologically active compounds which undergo predictable, preferably one-step, deactivation to a nontoxic moiety, after achieving the desired pharmacological effect) approach was applied to design and evaluate soft anticholinergics based on several known anticholinergics (propantheline, atropine and scopolamine. These compounds are intended for selective local action with decreased potential for systemic side effects. The new compounds synthesized were found to be potent anticholinergics both in vitro and in vivo. A propantheline soft analog was equipotent with propantheline in inhibiting indomethacin-induced gastric ulceration in rats and exhibited a shorter duration of systemic anticholinergic action in rabbits than propantheline. The methatropine and methscopolamine soft analogs were potent anticholinergics with very short duration of mydriatic action in rabbits compared to their hard analogs. In contrast to their hard analogs, they exhibited no systemic anticholinergic activity on topical administration into the rabbit eye. The potent anticholinergic activity combined with increased metabolic lability of the compounds described in this article fulfill the design requirements of ideal soft drugs.

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