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Affinity of the miotic drug, dapiprazole, at alpha 1-adrenoceptor subtypes A, B and D.

The functional affinities of the alpha 1-adrenoceptor antagonist, dapiprazole, currently being used to reverse diagnostic pupillary dilation, were determined at subtype A in rat vas deferens, at subtype B in guinea-pig spleen and at subtype D in rat aorta and compared with various alpha 1-adrenoceptor subtype-discriminating antagonists. Dapiprazole had relatively high affinity both at rat vas deferens alpha 1A-adrenoceptors (pA2 = 7.93) and at rat aortic alpha 1D-adrenoceptors (pA2 = 8.26), whereas its affinity at guinea-pig splenic alpha 1B-adrenoceptors (pA2 = 7.13) was lower. The reference antagonists, 5-methylurapidil and the 5-methylurapidil/flesinoxan hybrid, B8805-033 ((+/-)- 1,3,5-trimethyl-6[[3[4(2(2,3-dihydro-2-hydroxymethyl)-1,4-benzodioxin -5-yl)-1-piperazinyl]propyl]-amino]2,4(1H,3H)-pyrimidinedione), were 40- and 1500-fold selective for the A subtype, whereas spiperone and BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1- piperazinyl]ethyl]-8-azaspiro[4,5]decane-7,9-dione diHCI) were confirmed as selective for the B and D subtypes of alpha 1-adrenoceptors, respectively. Thus, in functional experiments dapiprazole seems to be moderately selective (approximately 10-fold) for the A and D over the B subtype of alpha 1-adrenoceptors; the possible therapeutic consequence of this is discussed.

Adrenergic alpha-Antagonists↗

Miotics.

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Acetylcholine↗

Miotics in closed-angle glaucoma.

The use of intravenous Diamox with variable doses of Pilocarpine was investigated in the treatment of primary closed-angle glaucoma. It was concluded that one drop of Pilocarpine 3 to 4 hrs after intravenous Diamox is the only parasympathomimetic drug necessary to terminated an acute attack.

Acetazolamide↗

Ultrasonographic study of the effect of different miotics on the eye components.

The effect of topical instillations of carbachol 3%, pilocarpine 2%, aceclidine 2%, aceclidine 2%-adrenaline 1%, and of the Ocusert delivery system was determined and compared in 151 eyes. The depth of the anterior chamber, the thickness and the position of the lens, the length of the vitreous and the refraction were studied. Aceclidine has negligible side effects on the ocular components (maximal change of the anterior chamber 0.20 mm; maximal change of the lens thickness 0.14 mm; maximal myopisation: -1.5 delta. Carbachol has the strongest side effects (maximal change of the anterior chamber 0.80 mm; maximal change of the lens thickness 0.80 mm; maximal myopisation -11.50 delta). Carbachol and pilocarpine may cause an important forward displacement of the lens with the risk of an angle-closure glaucoma in an eye with shallow anterior chamber.

Administration, Topical↗

Simultaneous bilateral "malignant glaucoma" attack in a patient with no antecedent eye surgery or miotics.

Malignant glaucoma is a term commonly used to describe a condition characterized by a sudden increase in intraocular pressure, usually occurring after eye surgery. This report describes a case of malignant glaucoma simultaneously presenting in both eyes, with no antecedent eye disease, medication or surgery. As far as we know this is the first report of spontaneous bilateral glaucoma. Both eyes were operated on according to the technique described by Chandler et al. (1), and the condition was solved. We suggest that, despite its rarity in eyes with no antecedent disease or ocular therapy, a surgeon should be aware of this condition.

Glaucoma↗