Noack E
Klin Monbl Augenheilkd. 1986 Jul;189(1):1-3. doi: 10.1055/s-2008-1050735.
Long-term treatment of glaucoma and ocular hypertension is being carried out increasingly by topical application of beta-adrenergic drugs. They bind to the beta 2-subtypes of beta-receptors in the unpigmented epithelia of the ciliary processes with high affinity. Aqueous humor production is thus inhibited. On the other hand the velocity of penetration through the cornea and the drug accumulation at this location increase with rising lipophilicity of the beta-blocker used. In this respect timolol and metipranolol, which was recently introduced on the Austrian market, possess favorable pharmacokinetic characteristics due to their intermediate lipophilicity. A calculation shows that one drop of 0.1% metipranolol solution produces supramaximal concentrations for several hours at the place of pharmacodynamic action. This is confirmed by the clinical efficacy, at the same time reducing the risk of local and systemic side effects.
青光眼和高眼压症的长期治疗越来越多地通过局部应用β-肾上腺素能药物来进行。它们以高亲和力与睫状突无色素上皮中的β受体的β2亚型结合。从而抑制房水生成。另一方面,随着所用β受体阻滞剂亲脂性的增加,其透过角膜的速度以及在该部位的药物蓄积也会增加。在这方面,噻吗洛尔和最近在奥地利市场推出的美替洛尔由于具有中等亲脂性而具有良好的药代动力学特性。计算表明,一滴0.1%的美替洛尔溶液在药效作用部位可产生数小时的超最大浓度。这已得到临床疗效的证实,同时降低了局部和全身副作用的风险。