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Functional differences between free alternators and non-alternators successfully treated for strabismic amblyopia.

Visual acuity was examined in patients successfully treated for strabismic amblyopia, and with equal refractive error in the two eyes (no more of 4 diopters of hyperopia). Patients able to freely alternate fixation showed equal visual acuity in the two eyes without optical correction. An optical correction in front of the ex-amblyopic eye was needed, in order to achieve equal visual acuity in patients unable to freely alternate fixation. No correction was necessary for the sound eye. This difference is attributed to a residual anomaly of accomodation of the ex-amblyopic eye. It is concluded that the concept of cure of strabismic amblyopia based on the attainment of equal visual acuity needs re-evaluation.

Accommodation, Ocular↗

Cholinomimetic activities of minaprine.

The cholinomimetic activities of the antidepressant drug minaprine have been investigated, in vitro and in vivo, in rodents. Minaprine, and its metabolite SR 95070B [3-(2-morpholinoethylamino)-4-methyl-6-(2-hydroxyphenyl) pyridazine hydrochloride] selectively displaced [3H]-pirenzepine from its cortical and hippocampal binding sites, and only weakly inhibited the binding of [3H]-N-methylscopolamine in either the rat cerebellum, heart and salivary glands, or the guinea-pig ileum. In mice, none of these drugs induced the typical cholinergic side-effects up to lethal doses. Minaprine and SR 95070B antagonized rotations induced by an intrastriatal injection of pirenzepine in mice, after intraperitoneal and/or oral administration. Minaprine also antagonized atropine-induced mydriasis in mice. Both minaprine and SR 95070B potentiated the tremorigenic effect of oxotremorine without inducing tremor when injected alone. Finally, minaprine and SR 95070B, after parenteral and/or oral injection, antagonized the scopolamine-induced deficit in passive avoidance learning, and enhanced short-term retention in the social memory test, in rats. The muscarinic agonists arecoline, oxotremorine and RS 86 [2-ethyl-8-methyl-2,8 diazaspiro-4,5 decan-1,3 dion hydrobromide], as well as the acetylcholine esterase inhibitors physostigmine and tacrine were active in most of these models. These results indicate that minaprine, and its metabolite SR 95070B, have cholinomimetic activities which could be, at least in part, mediated by their selective affinity for M1 muscarinic receptors. Thus minaprine could represent a potential useful drug for the treatment of senile dementias and cognitive impairments occurring in elderly people.

Animals↗

The effect of nasolacrimal occlusion on drug-induced mydriasis.

BACKGROUND: Nasolacrimal occlusion has been shown to improve the efficacy of some topically applied ocular drugs. The aim of this study was to investigate the effect of nasolacrimal occlusion on tropicamide-induced mydriasis. METHODS: We compared pupillary dilatation by 0.125% tropicamide with and without nasolacrimal occlusion in 40 healthy volunteers. RESULTS: Analysis of variance with repeated measures failed to show any advantage due to nasolacrimal occlusion in drug-induced mydriasis. CONCLUSION: Nasolacrimal occlusion did not increase the mydriasis obtained with 0.125% tropicamide.

Adult↗

The influence of topically applied bethanidine on intraocular pressure and pupil in the rabbit.

Bethanidine sulphate was administered topically to the eyes of conscious rabbits using a 0.5%, 1%, 2% and 5% solution of the drug. The intraocular pressures and pupil sizes were measured in the right treated and left control eyes at 0,1,2,3, 6 and 24 hrs. With all concentrations a pressure decrease with a maximum between 3 and 6 hrs after topical treatment occured. The 5% solution of bethanidine sulphate showed a delayed effect which was submaximal when compared to the 2% bethanidine solution. Using the 1% and 2% solution a ppressure decrease probably due to systemic action of the drug happened in the untreated control eyes. In all experiments the pressure responses had disappeared after 24 hrs in the treated and untreated eyes respectively. By means of the experimental conditions in this study no significant pupillary reactions were found after bethanidine application. The tension effect of 0.5% adrenaline borate remained essentially unchanged when repeated with additional 1% topical bethanidine. Some aspects of sympatholytic drug action on the intraocular pressure in the rabbit are discussed.

Animals↗

[Behavior of fluorescein dye in the vascularized cornea of the animal eye after local application of certain drugs (author's transl)].

In pigmented rabbits we investigated the much-used drugs pilocarpine, atropine, and tropicamide (Mydriaticum, Roche) with regard to their possible influence on the permeability of newly formed corneal vessels. Sodium fluorescein was chosen as test substance. Corneal vessels were produced by introcorneal injection of 0.1 N NaOH. Their development required 2--3 weeks and their growth about 4--6 weeks. A 2-week period of stability followed and was used for the local application of the above drugs. An evident influence on the diffusion of fluorescein could not be ascertained. Tropicamide induced a narrowing of the dye column in the corneal vessels. This phenomenon may be due to a narrowing of supplying vessels. In all cases, dye diffusion took place especially at the peripheral loops of the corneal vessels.

Animals↗

[Retinoscopy under cycloplegic and non-cycloplegic conditions in children comparison of measurements of three examiners (author's transl)].

The refractive status of 100 eyes were measured by three ophthalmologists utilizing retinoscopy under non-cycloplegic and cycloplegic conditions. The statistical analysis of the results was done by multiple regression. The retinoscopic measurements of sphere and cylinder of the three examiners show smaller differences under cycloplegic than under non-cycloplegic conditions. The largest differences in the measurements of axis were found in cases of small cylinder power. Especially in children and in patients with strabismus, the authors feel that measurements of the refractive state have to be carried out under cycloplegia.

Accommodation, Ocular↗

L-654,284 a new potent and selective alpha 2-adrenoceptor antagonist.

L-654,284 [(2R, 12bS)-N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]-furo[2,3-a] quinolizine-2-yl)-N-methyl-2-hydroxyethanesulfonamide) was tested in several in vitro and in vivo models for alpha 2-adrenoceptor antagonist activity and compared to several reference agents. In vitro L-654,284 completed for the binding of 3H-clonidine or 3H-rauwolscine (Ki's 0.8 nM, 1.1 nM) and blocked the presynaptic effects of clonidine in the rat isolated vas deferens (pA2, 9.1). L-654,284 exhibited marked alpha 2-vs. alpha 1-adrenoceptor selectivity in vitro, inhibiting 3H-prazosin binding with a Ki of 110 nM and blocking the effects of methoxamine on the vas deferens with a pA2 of 7.5. In vivo L-654,284 at 22 nmoles/kg i.v. doubled the ED50 of clonidine to produce mydriasis in rats. Given orally, the potency of L-654,284 in this test was reduced by a factor of 5.5. L-654,284 also potently increased cerebrocortical NE turnover in the rat, another in vivo index of alpha 2-adrenoceptor blockade in the central nervous system. In the periphery, L-654,284 demonstrated alpha 2-adrenoceptor selectivity by preferentially blocking the pressor effects of UK 14304 versus those of methoxamine in the pithed rat. Overall, L-654,284 was generally a more potent alpha 2-adrenoceptor antagonist than RX 781094 with comparable alpha 2/alpha 1 selectivity and was several times more potent and alpha 2-selective than WY 26703 or yohimbine. In addition, L-654,284 had better (5-6 times) oral bioavailability than RX 781094 or WY 26703.

Adrenergic alpha-Antagonists↗