Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Ibopamine is an original dopamine analogue. The drug, instilled in the conjunctival sac, induces mydriasis and is well-tolerated. In the present study, we have investigated the pharmacokinetic and pharmacodynamic characteristics of ibopamine after ocular application. Ibopamine produces a dose-dependent mydriasis endowed with very interesting characteristics: rapid onset, marked pupil dilation and rapid return to normal pupillary diameter. Ibopamine is well absorbed through the cornea, it is rapidly hydrolysed by esterases to epinine and the mydriatic effect is correlated with the concentration of epinine in the aqueous humor. The results of the experiments with the alpha 1-antagonists bunazosin and thymoxamine, and with reserpine, suggest that the mydriatic effect of ibopamine is obtained by direct stimulation of the alpha 1-adrenergic receptors; pretreatment with bunazosin almost completely inhibits the mydriatic activity of ibopamine; the mydriasis is also antagonized by thymoxamine. Pretreatment with reserpine has no effect on the extent of the mydriasis induced by ibopamine.
Soldati
L
L
Inpharzam Ricerche S.A., Zambon Group, Taverne, Switzerland.
Gianesello
V
V
Galbiati
I
I
Gazzaniga
A
A
Virno
M
M
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology; D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D003846:Deoxyepinephrine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D005260:Female; D008297:Male; D013948:Moxisylyte / Q000494:pharmacology; D009184:Mydriatics / Q000493:pharmacokinetics*; D011680:Pupil / Q000187:drug effects; D011799:Quinazolines / Q000494:pharmacology; D011817:Rabbits; D012110:Reserpine / Q000494:pharmacology; D013552:Swine; D013997:Time Factors
D000316:Adrenergic alpha-Agonists; D009184:Mydriatics; D011799:Quinazolines; D012110:Reserpine; C023487:ibopamine; C018176:bunazosin; D013948:Moxisylyte; D003846:Deoxyepinephrine