部份中文布林唑胺/噻吗洛尔处方资料（仅供参考）
英文名：Brinzolamide/Timolol
商品名：Azarga eye drops suspension
中文名：布林唑胺/噻吗洛尔
生产商：爱尔康
药品简介
组 成：
BRINZOLAMIDE………………10MG/ML
TIMOLOL MALEATE…………5MG/ML
药理特性：
Brinzolamide是碳酸酐酶II的抑制剂，在眼睛中它是主要的异构酶，碳酸酐脢抑制 剂是藉由减少眼内液体的分泌来降低眼内压。
Timolol：是乙型-1 和乙型-2(非选择性的)的肾上腺素接受体阻断剂，Timolol藉由减少纤毛上皮细胞形成房水的作用来降低眼内压。
适应症：
用于治疗曾使用单方治疗效果不佳的隅角开放性青光眼或高眼压成人患者，以降低其眼内压。
剂量及使用方法：
一般的剂量为每一眼一滴，一天使用一到两次。
警语︰
和许多局部眼用的药物一样，本药会被全身性地吸收。全身投予乙型肾上腺素阻断剂所见到的相同副作用可能发生于局部眼用。例如：全身或眼部投予Timolol Maleate后，曾发生严重的呼吸反应及心脏反应，包括气喘患者由于支气管痉孪而死亡，以及少数与心脏衰竭有关之死亡案例。
禁忌：下列患者禁用本品：
(1) 支气管气喘
(2) 有支气管气喘病史
(3) 严重慢性阻塞性肺部疾病
(4) 窦性心跳徐缓
(5) 二级或三级房室阻塞
(6) 明显心脏衰竭
(7) 心脏性的休克
(8) 对本品任一成分
AZARGA 10MG/ML+5MG/ML EYE DROPS, SUSPENSION
Active Ingredient/Synonyms
Brinzolamide|Brinzolamide
Description
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Indication
For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Mechanism of Action
Brinzolamide is a highly specific inhibitor of CA-II, which is the main CA isoenzyme involved in the secretion of aqueous humor. Inhibition of CA in the ciliary process of the eye slows the formation of bicarbonate, and reduces sodium and fluid transport. This results in a reduction in the rate of aqueous humor secretion and the intraocular pressure. Brinzolamide is absorbed systemically following topical ocular administration. Since it has a high affinity for CA-II, brinzolamide binds extensively to red blood cells, where CA-II is primarily found. As sufficient CA-II activity remains, adverse effects resulting from the systemic inhibition of CA by brinzolamide are not observed. The metabolite N-desethyl brinzolamide is also formed. This metabolite binds to CA and accumulates in red blood cells as well. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I (CA-I).
Pharmacodynamics
Used in the treatment of glaucoma, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide can decrease intraocular pressure by approximately 16-19% in patients with elevated intraocular pressure.
Pharmacokinetics
Absorption:
Absorbed into systemic circulation following topical ocular application
Distribution:
Not Available
Metabolism:
Ophthalmic
Elimination:
Not Available