LUMIGAN（比马前列素眼用溶液0.01％）

部份中文卢美根处方资料（仅供参考）
通用名：贝美前列素滴眼液
商品名：卢美根
英文名：Bimatoprost Ophthalmic Solution
中文拼音：Beimeiqianliesu Diyany
本品主要成份为贝美前列素。
性状
本品为无色澄明液体。
用法用量
推荐剂量为每日一次，每晚滴一滴于患眼。每日使用本品次数不得超过一次，因为有资料表明频繁使用本品可导致其眼压效果减弱。
首次滴用本品约4小时后眼压开始降低，约于8－12小时之内作用达到最大。
本品可以与其它滴眼剂同时使用以降低眼压。如果同时使用多种治疗药物，则每两种药物的使用应当至少间隔五分钟。
禁忌
本品禁用于对贝美前列素或本品中其它任何成份过敏者。
警告
有报道本品会引起色素组织的变化。包括色素增加，睫毛增生和虹膜及眶周围组织（眼睑）的色素增加。这些变化可能是永久性的。卢美根可逐渐改变眼睛的颜色，通过增加黑色素细胞中的黑素体（色素颗粒）数目使虹膜中的褐色素增加。本品对色素细胞的长期影响以及对黑色素细胞的潜在损伤和/或色素颗粒在眼睛其他部位的沉积情况目前还不清楚。
注意事项
一般情况：有报道患者因使用多剂量包装的滴眼液而致细菌性角膜炎。大多数情况下，包装容器是由于患者同时患有角膜疾病或眼睛上皮表面破裂而被污染的（参加患者须知）。
患者虹膜褐色素沉着的变化是逐渐发生的，可能在数年内也不会有明显变化。通常，褐色素沉着以瞳孔为中心向周边进行扩散，但是整个虹膜或部分的褐色素也会更深。也该经常检查患者眼睛的颜色变化，以便提供更多有关色素沉着的资讯，并且依据临床情况，如果色素沉着继续则应停止用药。停止用药后虹膜的褐色素不会再增加，但已改变的颜色可能是永久性的。虹膜上的痣和斑点不受治疗的影响。患有活动性内眼炎症（如葡萄膜炎）的患者须谨慎用本品。
曾有报道，有患者使用本品后出现了黄斑水肿包括囊样黄斑水肿。无晶体患者、晶状体后囊撕裂的假性无晶体患者或已知有黄斑水肿危险的患者应谨慎用本品。
本品治疗闭角型、炎性及出血性青光眼尚无评价。
配戴有隐形眼镜时不应使用本品。
患者须知：患者应被告知，部分患者使用此药会出现睫毛变长、颜色变深、眼部皮肤颜色加深的现象，此现象可能是永久性的。
只需要治疗单侧眼睛的患者应该被告知出现两眼间睫毛长度，颜色或粗细不同和两眼的眼睑皮肤及虹膜颜色不同的可能。
患者应该被告知勿将药瓶的瓶口直接接触眼睛、眼周组织、手指以及其它物体的表面、以免药液被可致眼睛感染的细菌污染。使用被污染的药液会严重损伤眼睛进而使视力下降。
患者应该被告知在使用过程中，若眼部出现任何状况（如外伤或感染）或进行眼科手术，应立即资讯医生是否可以继续使用此多剂量包装的滴眼液。
患者应该告知在在使用过程中，若眼部出现反应，特别是结膜炎和眼睑反应时应及时咨询医生。
使用本品前应当摘下隐形眼镜，并在滴药15分钟后再配戴。应告诉患者本品中含有苯扎氯铵会被软性隐形眼镜吸收。
如果同时还使用其它药物，每两种药物的使用至少间隔5分钟。
孕妇及哺乳期妇女用药
孕妇：对妊娠期的妇女使用本品还缺少足够有良好对照的研究。因为动物的生殖试验还不能直接遇见人类反应，仅仅当作使用本品的益处远远大于其带给胎儿的危险性时，方可给孕妇使用。
哺乳期妇女：虽然动物试验表明动物的乳汁中分泌有贝美前列腺素，但本品是否会从人类乳汁中分泌还不清楚。由于许多药物都会分泌乳汁中，因此给哺乳期妇女使用本品应当谨慎。
儿童用药
儿童患者使用本品的安全性和有效性尚未确立。
老年患者用药
使用本品的安全性和有效性在老年人和成年人之间没有明显的临床差异。
药物相互作用
本品可以与其它滴眼剂同时使用以降低眼内压。如果同时使用多种治疗药物，则每两种药物的使用应当至少间隔五分钟。
药物过量
没有关于人体使用本品过量的的资料报导。如果过量使用本品，应该根据出现的症状进行相应处理。
贮藏
保持包装完整，储存于2－25C
包装
塑料滴瓶装无菌眼药水，1支/盒
http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=A5E67C75-DB88-4372-BB07-C8DD15C97631
LUMIGAN®
(bimatoprost ophthalmic solution) 0.03%
DESCRIPTION
LUMIGAN® (bimatoprost ophthalmic solution) 0.03% is a synthetic prostamide analog with ocular hypotensive activity. Its chemical name is (Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[1E,3S)-3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl]-5-N-ethylheptenamide, and its molecular weight is 415.58. Its molecular formula is C25H37NO4. Its chemical structure is:
Bimatoprost is a powder, which is very soluble in ethyl alcohol and methyl alcohol and slightly soluble in water. LUMIGAN® is a clear, isotonic, colorless, sterile ophthalmic solution with an osmolality of approximately 290 mOsmol/kg.
Contains: Active: bimatoprost 0.3 mg/mL; Preservative: Benzalkonium chloride 0.05 mg/mL; Inactives: Sodium chloride; sodium phosphate, dibasic; citric acid; and purified water. Sodium hydroxide and/or hydrochloric acid may be added to adjust pH. The pH during its shelf life ranges from 6.8-7.8.
CLINICAL PHARMACOLOGY
Mechanism of Action:
Bimatoprost is a prostamide, a synthetic structural analog of prostaglandin with ocular hypotensive activity. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Elevated IOP presents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Pharmacokinetics:
Clinical Studies:
In clinical studies of patients with open angle glaucoma or ocular hypertension with a mean baseline IOP of 26 mmHg, the IOP-lowering effect of LUMIGAN® (bimatoprost ophthalmic solution) 0.03% once daily (in the evening) was 7-8 mmHg.
Results of dosing for up to five years with products in this drug class showed that the onset of noticeable increased iris pigmentation occurred within the first year of treatment for the majority of the patients who developed noticeable increased iris pigmentation. Patients continued to show signs of increasing iris pigmentation throughout the five years of the study. Observation of increased iris pigmentation did not affect the incidence, nature or severity of adverse events (other than increased iris pigmentation) recorded in the study. IOP reduction was similar regardless of the development of increased iris pigmentation during the study.
In patients with a history of liver disease or abnormal ALT, AST and/or bilirubin at baseline, LUMIGAN® had no adverse effect on liver function over 48 months.
INDICATIONS AND USAGE
LUMIGAN® (bimatoprost ophthalmic solution) 0.03% is indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension.
CONTRAINDICATIONS
LUMIGAN® (bimatoprost ophthalmic solution) 0.03% is contraindicated in patients with hypersensitivity to bimatoprost or any other ingredient in this product.
WARNINGS
LUMIGAN® (bimatoprost ophthalmic solution) 0.03% has been reported to cause changes to pigmented tissues. The most frequently reported changes have been increased pigmentation of the iris, periorbital tissue (eyelid) and eyelashes, and growth of eyelashes. Pigmentation is expected to increase as long as LUMIGAN® is administered. After discontinuation of LUMIGAN® pigmentation of the iris is likely to be permanent while pigmentation of the periorbital tissue and eyelash changes have been reported to be reversible in some patients. Patients who receive treatment should be informed of the possibility of increased pigmentation. The effects of increased pigmentation beyond 5 years are not known.
PRECAUTIONS
ADVERSE REACTIONS
In clinical trials, the most frequent events associated with the use of LUMIGAN® (bimatoprost ophthalmic solution) 0.03% occurring in approximately 15% to 45% of patients, in descending order of incidence, included conjunctival hyperemia, growth of eyelashes, and ocular pruritus. Approximately 3% of patients discontinued therapy due to conjunctival hyperemia.
Ocular adverse events occurring in approximately 3 to 10% of patients, in descending order of incidence, included ocular dryness, visual disturbance, ocular burning, foreign body sensation, eye pain, pigmentation of the periocular skin, blepharitis, cataract, superficial punctate keratitis, eyelid erythema, ocular irritation, and eyelash darkening. The following ocular adverse events reported in approximately 1 to 3% of patients, in descending order of incidence, included: eye discharge, tearing, photophobia, allergic conjunctivitis, asthenopia, increases in iris pigmentation, and conjunctival edema. In less than 1% of patients, intraocular inflammation was reported as iritis.
Systemic adverse events reported in approximately 10% of patients were infections (primarily colds and upper respiratory tract infections). The following systemic adverse events reported in approximately 1 to 5% of patients, in descending order of incidence, included headaches, abnormal liver function tests, asthenia and hirsutism.
OVERDOSAGE
No information is available on overdosage in humans. If overdose with LUMIGAN® (bimatoprost ophthalmic solution) 0.03% occurs, treatment should be symptomatic.
In oral (by gavage) mouse and rat studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m2 is at least 70 times higher than the accidental dose of one bottle of LUMIGAN® for a 10 kg child.
DOSAGE AND ADMINISTRATION
The recommended dosage is one drop in the affected eye(s) once daily in the evening. The dosage of LUMIGAN® (bimatoprost ophthalmic solution) 0.03% should not exceed once daily since it has been shown that more frequent administration may decrease the intraocular pressure lowering effect.
Reduction of the intraocular pressure starts approximately 4 hours after the first administration with maximum effect reached within approximately 8 to 12 hours.
LUMIGAN® may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart.
Storage: LUMIGAN® should be stored in the original container at 2°to 25°C (36° to 77°F).