Stewart W C
Storm Eye Institute, Medical University of South Carolina, Charleston 29425-2236, USA.
Klin Monbl Augenheilkd. 1996 Jul;209(1):A7-13.
Apraclonidine is a alpha 2 adrenergic agonic which is a para-amino derivative of clonidine. This molecular alteration helps prevent apraclonidine from crossing the blood-brain barrier so it minimally influences the heart rate and blood pressure. Apraclonidine reduces the intraocular pressure primarily by an aqueous suppressant mechanism. Its ocular hypotensive efficacy as monotherapy is similar to timolol maleate 0.5% up to eight hours post dosing, but is less than timolol maleate by 12 hours following instillation. As an adjunctive agent apraclonidine decreases the intraocular pressure approximately 16% over that of timolol maleate done. These clinical effects are stable out of three months after the initiation of therapy. Apraclonidine is also additive to maximally tolerated medical therapy. As many as 60% of these patients do not require additional therapy after adding apraclonidine for as long as five months. Apraclonidine also is useful to prevent transiently increased intraocular pressure following anterior segment laser procedures and intraocular surgery. Apraclonidine is well tolerated systemically with no serious adverse event attributed previously to this medicine. The most common ocular side effect is anterior segment intolerance in between 8-36% of patients. Symptoms of itching, as well as burning, and signs of conjunctival inflammation may appear. The intolerance quickly resolves upon discontinuation of the medicine. In summary, apraclonidine is useful in chronic therapy for chronic open-angle glaucoma and helping to prevent acute increased intraocular pressure following anterior segment laser procedures.
阿可乐定是一种α2肾上腺素能激动剂,是可乐定的对氨基衍生物。这种分子结构的改变有助于防止阿可乐定穿过血脑屏障,因此它对心率和血压的影响极小。阿可乐定主要通过抑制房水生成机制来降低眼压。单次给药后长达8小时,其作为单一疗法的降眼压效果与0.5%的马来酸噻吗洛尔相似,但滴眼后12小时的效果则不如马来酸噻吗洛尔。作为辅助药物,阿可乐定比马来酸噻吗洛尔降低眼压的幅度约高16%。这些临床效果在治疗开始后的三个月内保持稳定。阿可乐定与最大耐受量的药物治疗联合使用时也具有相加作用。多达60%的患者在加用阿可乐定长达五个月后不再需要额外治疗。阿可乐定还有助于预防眼前节激光手术和眼内手术后眼压的短暂升高。阿可乐定的全身耐受性良好,此前未发现与此药物相关的严重不良事件。最常见的眼部副作用是8%至36%的患者出现眼前节不耐受。可能会出现瘙痒、烧灼感等症状以及结膜炎症的体征。停药后这种不耐受情况会迅速缓解。总之,阿可乐定可用于慢性开角型青光眼的长期治疗,并有助于预防眼前节激光手术后眼压的急性升高。