Hugues F C, Le Jeunne C, Munera Y, Dufier J L
Laboratoire de Thérapeutique appliquée, Hôpital Laennec, Paris.
J Fr Ophtalmol. 1987;10(8-9):485-90.
Systemic effects of two topical B adrenergic blocking agents, carteolol and metipranolol, recently introduced in the treatment of open angle chronic glaucoma, were investigated in two groups of 10 asthmatic patients, according to a controlled trial device. Saline eye drops as placebo, then, 30 mn later beta blocker eye-drops, were instillated at usual dose. Heart rate, systolic and diastolic blood pressure, vital capacity (VC) and expiratory outflow (FEV1), were checked every 15 mn during 90 mn. They did not vary under placebo. After carteolol and metipranolol, heart rate decreased more than 10% in 7 out of 10 patients in each group (extreme individual changes: -16.7 and -25.0%). Bradycardia was always sino atrial. FEV1 was lowered in 3 patients with carteolol and in 6 with metipranolol (extreme individual values: -32.3 and -31.8%). If time is not taken in consideration, the lowest values were -8.6 +/-4.6% with carteolol and -17.9 +/- 3.3% with metipranolol. CV was reduced only in 1 patient under carteolol and 2 patients under metipranolol. Systemic blood pressure remained unchanged. 7 patients complained of ocular pain when metipranolol was instillated. Comparison of both ocular topics shows that metipranolol lowers heart rate and FEV1 more than carteolol, which has a sympathomimetic intrinsic activity. These two drugs have the same clinical efficiency. Our results point out the risks outcoming from their systemic diffusion, and the absolute necessity to comply with the general rules of good use of beta blockers, even with eye drops, mainly the contra-indications and the strict adjustment of individual doses.
根据对照试验方法，在两组各10名哮喘患者中研究了最近用于治疗开角型慢性青光眼的两种局部用β肾上腺素能阻滞剂（卡替洛尔和美替洛尔）的全身效应。先滴入生理盐水眼药水作为安慰剂，30分钟后再按常规剂量滴入β受体阻滞剂眼药水。在90分钟内每隔15分钟检查心率、收缩压和舒张压、肺活量（VC）和呼气流量（FEV1）。在使用安慰剂期间这些指标没有变化。使用卡替洛尔和美替洛尔后，每组10名患者中有7名心率下降超过10%（个体最大变化分别为-16.7%和-25.0%）。心动过缓均为窦性。使用卡替洛尔时有3名患者FEV1降低，使用美替洛尔时有6名患者FEV1降低（个体最大降低值分别为-32.3%和-31.8%）。若不考虑时间因素，卡替洛尔的最低降低值为-8.6±4.6%，美替洛尔为-17.9±3.3%。使用卡替洛尔时只有1名患者肺活量降低，使用美替洛尔时有2名患者肺活量降低。全身血压保持不变。滴入美替洛尔时7名患者主诉眼痛。两种眼科用药的比较显示，美替洛尔比具有拟交感神经内在活性的卡替洛尔更能降低心率和FEV1。这两种药物具有相同的临床疗效。我们的结果指出了它们全身扩散带来的风险，以及即使使用眼药水也绝对必须遵守β受体阻滞剂合理使用的一般规则，主要是禁忌证和严格调整个体剂量。
