2013年4月19日，Alcon宣布美国食品药品管理局(FDA)已批准Simbrinza悬液上市，适用于降低原发性开角型青光眼或高眼压症患者的高眼压。Simbrinza是一种固定剂量复方制剂，包含一种碳酸酐酶抑制剂(布林佐胺1.0%)和一种α2肾上腺素能受体激动剂(酒石酸溴莫尼定0.2%)。用法为患眼每次1滴，每日3次。
FDA批准Simbrinza是基于2项关键3期临床试验的数据。这2项研究共招募了大约1,300例患者，评估了布林佐胺1.0%与溴莫尼定0.2%固定剂量复方制剂每日给药3次的安全性与有效性，并与仅给予其中一种成分进行了比较。这2项研究均达到了其主要终点，证明在3个月内所有时间点的平均眼压方面，Simbrinza相对于单一成分具有统计学优势。在这2项研究中，Simbrinza组患者的3个月时眼压比基线时(22~36 mmHg)下降了5~9 mmHg。
在这2项为期3个月的临床试验中，接受Simbrinza治疗的患者最常报告的不良反应为视力模糊、眼刺激、味觉障碍、口干和眼过敏。Simbrinza组患者有11%停药，主要原因是不能耐受不良反应。Simbrinza的安全性特征与其所含的2种活性成分一致。此外，在接受Simbrinza治疗的患者中未发生明显的心血管或肺部事件。
SIMBRINZA Rx
Generic Name and Formulations:
Brinzolamide 1%, brimonidine tartrate 0.2%; oph susp; contains benzalkonium chloride.
Company:
Alcon Laboratories, Inc.
Indications for SIMBRINZA:
Reduction of elevated intraocular pressure in open-angle glaucoma or ocular hypertension.
Adults and Children's Dose:
<2yrs: contraindicated. ≥2yrs: 1 drop three times daily.
Pharmacological Class:
Carbonic anhydrase inhibitor + alpha-2 agonist.
Contraindications:
Neonates and infants <2yrs.
Warnings/Precautions:
Sulfonamide allergy. Discontinue if serious systemic or hypersensitivity reactions occur. Increased risk of corneal edema in patients with low endothelium cell counts. Severe renal impairment (CrCl <30mL/min): not recommended. Hepatic impairment. Severe cardiovascular disease. Depression. Cerebral or coronary insufficiency. Raynaud’s phenomenon. Orthostatic hypotension. Thromboangitis obliterans. Acute angle-closure glaucoma. Remove soft contact lenses before use; may reinsert 15mins later. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interactions:
Concomitant oral carbonic anhydrase inhibitors: not recommended. Caution with antihypertensives, cardiac glycosides, tricyclic antidepressants, MAOIs. Concomitant high-dose salicylate may produce acid-base and electrolyte alterations. May be potentiated by CNS depressants (eg, alcohol, opiates, barbiturates, sedatives, anesthetics). Separate administration of other oph drugs by ≥5 minutes.
Adverse Reactions:
Blurred vision, eye irritation, dysgeusia, dry mouth, eye allergy.
How Supplied:
Susp—8mL