The effect of a single oral dose of pergolide on intraocular pressure and pupil diameter.

Abstract

1. The ocular hypotensive effect of a single oral dose of 25 micrograms pergolide, a dopamine 2‐receptor agonist, was studied in 12 normal human volunteers, using a non‐invasive method. 2. An oral dose of timolol 20 mg was used as a positive control. 3. The effects of both drugs on pupil diameter were also studied, using a photographic method. 4. Considering the first 6 h post‐dosing measurements, using multiple linear regression analysis comparing drug with placebo and including the baseline values as continuous independent variables, both pergolide and timolol had a significant ocular hypotensive effect in both eyes (P less than 0.0001) with no significant effects on pupil diameter. 5. Further topical application studies in normal and glaucomatous eyes are needed to evaluate the usefulness of pergolide in the treatment of glaucoma.

Natural Ergot Alkaloids in Ocular Pharmacotherapy: Known Molecules for Novel Nanoparticle-Based Delivery Systems

“…This is a sympatholytic drug composed of a combination of equal parts of three dehydrogenated derivatives of ergot alkaloids: dihydroergocristine, dihydroergocornine, and dihydroergocryptine methane sulfonates. Moreover, ergoline derivatives with a predominant dopaminergic activity, such as bromocriptine, lergolide, pergolide, cianergolide, and lisuride, were shown to decrease IOP in rabbits, monkeys, and humans [ 31 , 32 , 33 , 34 ]. A United States (US) patent also reported the production of a formulation comprising bromocriptine as the active ingredient, suitable for ocular instillation and used as an anti-glaucomic agent [ 35 ].…”

A comparative study of topical natural ergot alkaloids on the intraocular pressure and aqueous humor dynamics in oclular normotensive and α-chymotrypsin-induced ocular hypertensive rabbits

“…More recently, ergoline derivatives with a predominant dopaminergic activity, such as bromocriptina, lergotrile, pergolide, cianergolide and lisuride, have been shown to lower intraocular pressure in a dose-related fashion in rabbits, monkeys and men [1,13,[29][30][31]42].…”

Lisuride Acts at Multiple Sites to Induce Ocular Hypotension and Mydriasis

“…Moreover, bromocriptine and pergolide lowered IOP in normal [6][7][8][9] and glaucomatous humans [10,11], and the hypotensive effect of pergolide was antagonized by domperidone, a peripherally acting DA 2 -receptor antagonist [12]. Lisuride, a semisynthetic ergot alkaloid stereochemically related to isolysergic acid with a substituted amino group in position 8S, is purported to stimulate dopamine receptors.…”