Melena J, Santafé J, Segarra J
Departamento de Farmacología, Facultad de Farmacia, Universidad del País Vasco, Vitoria, Spain.
J Pharmacol Exp Ther. 1998 Jan;284(1):278-82.
The effect of calcium channel blockers (CCBs) on intraocular pressure (IOP) remains still controversial, although some preliminary reports suggest that these drugs may be effective in the management of ocular hypertension and low-tension glaucoma. The aim of the present work was to assess the effect of topical diltiazem on IOP in an animal model for glaucoma, the betamethasone-induced ocular hypertension in rabbits. IOP was measured with a manometrically calibrated applanation pneumatonograph. Ocular hypertension was produced in 120 rabbits by weekly subconjunctival injection of a betamethasone suspension into the left eye. The experiments examining the ocular actions of diltiazem were carried out in two stages. In the first one, the ability of topical diltiazem to prevent the rise in IOP induced by betamethasone was studied. In a second phase, the effect of topical diltiazem on IOP in betamethasone-induced ocular hypertensive rabbits was assessed. Diltiazem was topically applied once daily for 5 days a week into the left eye. The effect of five different concentrations of diltiazem was evaluated to obtain dose-response curves. Topical diltiazem was found to prevent in a dose-related fashion the betamethasone-induced IOP rise as well as to reduce IOP in rabbits made ocular hypertensive by weekly subconjunctival injection of betamethasone. Unilateral topical administration did not produce a clear effect on IOP in the untreated eye. This is the first report describing the ocular hypotensive action CCBs in animal model for glaucoma. These findings are in agreement with preliminary evidence suggesting that CCBs may have a beneficial effect in human ocular hypertension.
钙通道阻滞剂(CCB)对眼压(IOP)的影响仍存在争议,尽管一些初步报告表明这些药物可能对治疗高眼压症和低眼压性青光眼有效。本研究的目的是评估局部应用地尔硫䓬对青光眼动物模型(即倍他米松诱导的兔眼高眼压)眼压的影响。眼压通过压力校准的压平式眼压计测量。通过每周向左眼结膜下注射倍他米松混悬液,在120只兔中诱导高眼压。研究地尔硫䓬眼部作用的实验分两个阶段进行。第一阶段,研究局部应用地尔硫䓬预防倍他米松诱导的眼压升高的能力。第二阶段,评估局部应用地尔硫䓬对倍他米松诱导的高眼压兔眼压的影响。地尔硫䓬每周5天每天一次局部应用于左眼。评估了五种不同浓度地尔硫䓬的效果以获得剂量反应曲线。发现局部应用地尔硫䓬能以剂量相关的方式预防倍他米松诱导的眼压升高,并降低通过每周结膜下注射倍他米松导致高眼压的兔的眼压。单侧局部给药对未治疗眼的眼压未产生明显影响。这是第一份描述CCB在青光眼动物模型中降眼压作用的报告。这些发现与初步证据一致,表明CCB可能对人类高眼压症有有益作用。