Effect of Moxisylyte Hydrochloride (α₁-Blocker) on the Retinal Circulation of Patients with Diabetes mellitus

Abstract

Moxisylyte hydrochloride (α₁-blocker) selectively vasodilates cerebral vessels without reducing blood pressure. We investigated the effect of the drug on retinal circulation in 15 patients (17 eyes) with diabetes mellitus, using the video-densitometric image analysis of fiuorescein angiography. We compared the build-up time (BT), the time constant of washout rate (TC) and the mean circulation time (MCT) before and after oral therapy with moxisylyte. In 16 eyes, BT was shortened significantly and MCT was only slightly shortened 1 h after oral therapy with moxisylyte. After 2 weeks of daily administration, MCT was shortened and TC of the artery was increased significantly in 6 eyes. Since retinal circulation in patients with diabetes mellitus was improved by moxisylyte, the drug may be useful to treat ocular disorders such as diabetic retinopathy.

Do Drug‐likeness Rules Apply to Oral Prodrugs?

“…Prodrugs with route of administration different from oral were discarded for instance: parecoxib [41] which is administrated parenterally, latanoprost [42] for ophthalmologic use acyclovir [43] and tazarotene [44] which are indicated for topical use. The same happened for prodrugs with multiple active metabolites such as delaminid [45] and moxisylyte [46] . Prodrugs still under investigation such as lefradafiban [47] and amelubant [48] or mistaken entries of actual drugs such as netupitant [49] were also disregarded.…”

“…The same happened for prodrugs with multiple active metabolites such as delaminid [45] and moxisylyte. [46] Prodrugs still under investigation such as lefradafiban [47] and amelubant [48] or mistaken entries of actual drugs such as netupitant [49] were also disregarded.…”