Factors determining the potency of mydriatic drugs in man.
1 The mydriasis resulting from topical application of five atropine-like drugs was measured photographically in man. Drug potency was obtained from log dose-response curves. 2 The in vitro potency of eight cholinoceptor blocking drugs, including those studied in man, was obtained by measuring their affinity constants for binding to the receptors of an isolated preparation of the rabbit sphincter pupillae. Values agreed closely with those obtained for the muscarinic receptors of guinea-pig ileum. 3 In vitro and in vivo potency was compared to obtain a quantitative measure of the relative ease with which drugs gain access to the receptors after topical application. 4 The large differences that occur in the intensity and duration of the mydriatic response to atropine-like drugs is primarily the result of differences in their ability to blcok the receptors. Only with tropicamide does its relatively high accessibility affect its potency in man.
D000287:Administration, Topical; D000328:Adult; D000577:Amides / Q000494:pharmacology; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D002217:Carbachol / Q000037:antagonists & inhibitors; D002794:Choline / Q000031:analogs & derivatives / Q000494:pharmacology; D003519:Cyclopentolate / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006801:Humans; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009184:Mydriatics / Q000008:administration & dosage / Q000494:pharmacology*; D011680:Pupil / Q000187:drug effects; D011725:Pyridines / Q000494:pharmacology; D011817:Rabbits; D011950:Receptors, Cholinergic / Q000187:drug effects; D011976:Receptors, Muscarinic / Q000187:drug effects; D014326:Tropanes / Q000494:pharmacology
D000577:Amides; D009184:Mydriatics; D011725:Pyridines; D011950:Receptors, Cholinergic; D011976:Receptors, Muscarinic; D014326:Tropanes; D001285:Atropine; D002217:Carbachol; D003519:Cyclopentolate; D002794:Choline