TIMOLOL MALEATE（马来酸噻吗洛尔）
本品主要成分及其化学名称为：主要成分是马来酸噻吗洛尔，其化学名为：（一）-1-（叔丁氨基）-3-［（4-吗啉基-1，2，5-噻二唑-3-基）氧］-2-丙醇顺丁稀二酸盐。
C13H24N4O3S·C4H4O4，
分子量：432.49
性状：本品为无色的澄明液体。
适应症：对原发性开角型青光眼具有良好的降低眼内压疗效。对于某些继发性青光眼，高眼压症，部分原发性闭角型青光眼以及其他药物及手术无效的青光眼，加用本品滴眼可进一—步增强降眼压效果。
用法用量：滴眼，一次1滴，一日1—2次，如眼压已控制，可改为一日1次。如原用其他药物，住改用本品治疗时．原药物不宜突然停用，应自滴用本品的第二天起逐渐停用
禁忌：
1．支气管哮喘者或有支气管哮喘史者，严重慢性阻塞性肺部疾病。
2．窦性心动过缓，II或III度房室传导阻滞，明显心衰，心源性休克。
3．对本品过敏者。
注意事项：
1．当出现呼吸急促、脉搏明显减慢、过敏等症状时，请立即停止使用本品。
2．使用中若出现脑供血不足症状时应立即停药，
3．心功能损害者，使用本品时应避免服用钙离子拮抗剂．
4．对无心衰史的患者，如出现心衰症状应立即停药。
5.正在服用儿茶酚胺耗竭药(如利血平)者，使用本品时应严密观察。
6．冠状动脉疾患、糖尿病、甲状腺功能亢进和重症肌无力患者，用本品滴眼时需遵医嘱。
7．本品慎用于自发性低血糖患者及接受胰岛素或口服降糖药治疗的患者，因p受体阻滞剂可掩盖低血糖症状。
8．本品不宜单独用于治疗闭角型青光眼。
9．与其他滴眼液联合使用时，请间隔lO分钟以上。
10．定期复查眼压，根据眼压变化调整用药方案
11．用前应摇匀，避免容器尖端接触眼睛，防止滴眼液污染。
[孕妇及哺乳期妇女用药]
本品对于孕妇的安全性尚未确定。滴眼后可在哺乳期妇女乳汁中测到本品，因对授乳婴儿具有多种潜在不良反应．需根据滴用本品对母亲的重要性决定终止哺乳或终止用药，[儿童用药]本品对于儿童的安全性和疗效尚未确定。
药物相互作用：
1．与肾上腺素合用可引起瞳孔扩大。
2．不主张两种局部p受体阻断剂同时应用。
3．本品与钙通道拮抗剂合用应慎重，囚可引起房室传导阻滞，左心室衰竭及低血压。肘心功能受损的患者，应避免两种药合并使用
4．正在服用儿茶酚胺耗竭药(如利血平)者，使用本品时应严密观察，因可引起低血压和明显的心动过缓。
5．本品与洋地黄类和钙通道拮抗剂合用可进一步延长房室传导时间。 6，本品与奎宁丁合用能引起心率减慢等全身p受休阻断的副作用。可能的原因是奎宁丁可抑制P450酶和CYPZD6对噻吗洛尔的代谢作用。
药理作用：
药理作用：马来酸噻吗洛尔是一种非选择性p—肾上腺能受体阻滞剂，没有明显的内源性拟交感活性和局麻作用，对心肌无直接抑制作用。本品为马来酸噻吗洛尔滴眼液．对高眼压患者和正常人均有降低眼内压作用、其降低眼内压的确切机理尚不清楚，眼压描记和房水荧光光度研究提示本品的降眼压作用与减少房水生成有关非临床毒理研究：致癌性：动物实验显示长期大量口服马来酸噻吗洛尔可使雄性大鼠肾卜腺嗜铬细胞瘤，雌性小鼠良性及恶性肺部肿瘤，良性子宫息肉及乳腺痛的发生率明显增高。生殖毒性：动物实验显示大剂量门服马来酸噻吗洛尔，对雄、雌性小鼠的生殖功能均无影响。
孕妇及哺乳期妇女用药：本品对于孕妇的安全性尚未确定。滴眼后可在哺乳期妇女乳汁中测到本品，因对授乳婴儿具有多种潜在不良反应，需根据滴用本品对母亲的重要性决定终止哺乳或终止用药。
儿童用药：本品对于儿童的安全性和疗效尚未确定。
药物相互作用：
1.与肾上腺素合用可引起瞳孔扩大。
2.不主张两种局部β受体阻断剂同时应用。
3.本品与钙通道拮抗剂合用应慎重，因可引起房室传导阻滞，左心室衰竭及低血压。对心功能受损的患者，应避免两种药合并使用。
4.正在服用儿茶酚胺耗竭药（如利血平）者，使用本品时应严密观察，因可引起低血压和明显的心动过缓。
5.本品与洋地黄类和钙通道拮抗剂合用可进一步延长房室传导时间。6.本品与奎宁丁合用能引起心率减慢等全身β受体阻断的副作用。可能的原因是奎宁丁可抑制P450酶和CYPZD6对噻吗洛尔的代谢作用。
药物过量：过量应用本品可引起类似全身应用β受体阻断剂的副作用，如头晕，头痛，气短，心动过缓，支气管痉挛及心搏停止。
包装：聚乙烯塑料眼药瓶。
贮藏：遮光，密闭保存。
药物毒理：药理作用： 马来酸噻吗洛尔是一种非选择性β-肾上腺能受体阻滞剂，没有明显的内源性拟交感活性和局麻作用。对心肌无直接抑制作用。本品为马来酸噻码洛尔滴眼液，对高眼压患者和正常人均有降低眼内压作用。其降低眼内压的确切机理尚不清楚，眼压描记和房水荧光光度研 究提示本品的降眼压作用与减少房水生成有关。 非临床毒理研究： 致癌性：动物实验显示长期大量口服马来酸噻吗洛尔可使雄性大鼠肾上腺嗜铬细胞瘤，雌牲小鼠良性及恶性肺部肿瘤，良性子宫息肉及乳腺癌的发生率明显增高。 生殖毒性：动物实验显示大剂量口服马来酸噻吗洛尔，对雄、雌性小鼠的生殖功能均无影响。 
药代动力学：动物实验显示，用0．5本品对家兔单剂量滴眼，房水和血中的药物峰浓度出现在用药后30分钟，半衰期为1．5小时。全身吸收的马来酸噻吗洛尔在肝内代谢，70％的药物原型随尿排出。对6个接受治疗者的血浆药物浓度测定显示，每日用0．5％本品滴眼2次，早晨滴药后的平均血浆峰浓度为0．46ng／ml，下午滴眼后约为0．35ng/ml.

What is Istalol?

Istalol ophthalmic (for the eyes) is a beta-blocker that also reduces pressure inside the eye.
Istalol is used to treat open-angle glaucoma and other causes of high pressure inside the eye.
Istalol may also be used for other purposes not listed in this medication guide.

Important information about Istalol
Do not allow the dropper to touch any surface, including the eyes or hands. If the dropper becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.

Do not use any other eye medication unless your doctor has prescribed it for you. If you use another eye medication, use it at least 10 minutes before or after using Istalol. Do not use the medications at the same time.

Istalol can cause blurred vision. Be careful if you drive or do anything that requires you to be able to see clearly.

Before using Istalol
Do not use Istalol if you are allergic to timolol, or if you have:
asthma or severe chronic obstructive pulmonary disease (COPD);
certain serious heart conditions, especially "AV block"; or
severe or uncontrolled congestive heart failure.

If you have any of these other conditions, you may need a dose adjustment or special tests to safely use Istalol:
breathing problems such as bronchitis or emphysema;
a history of heart disease or congestive heart failure;
diabetes;
history of stroke, blood clot, or circulation problems;
a thyroid disorder;
a muscle disorder such as myasthenia gravis;
kidney disease; or
liver disease.

FDA pregnancy category C. Istalol may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Istalol passes into breast milk and could cause harm to a nursing baby. Do not use Istalol without telling your doctor if you are breast-feeding a baby. Do not use this medicine for a child younger than 2 years old.

How should I use Istalol?
Use Istalol exactly as it was prescribed for you. Do not use the medication in larger amounts, or use it for longer than recommended by your doctor. Follow the instructions on your prescription label.

Wash your hands before using Istalol eye drops. Do not use Istalol while you are wearing contact lenses. Istalol may contain a preservative that can be absorbed by soft contact lenses. Wait at least 15 minutes after using Istalol before putting your contact lenses in.

To apply the eye drops:
Tilt your head back slightly and pull down your lower eyelid. Hold the dropper above the eye with the dropper tip down. Look up and away from the dropper as you squeeze out a drop, then close your eye.
Gently press your finger to the inside corner of the eye (near your nose) for about 1 minute to keep the liquid from draining into your tear duct. If you use more than one drop in the same eye, wait about 5 minutes before putting in the next drop.
Do not allow the dropper tip to touch any surface, including the eyes or hands. If the dropper becomes contaminated it could cause an infection in your eye, which can lead to vision loss or serious damage to the eye.

Do not use Istalol eye drops if the liquid has changed colors or has particles in it. Call your doctor for a new prescription.

If you need to have any type of surgery, especially eye surgery, tell the surgeon ahead of time that you are using Istalol. You may need to stop using the medicine for a short time.

Store Istalol at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.

What happens if I miss a dose?
Use the medication as soon as you remember. If it is almost time for the next dose, skip the missed dose and use the medicine at the next regularly scheduled time. Do not use extra medicine to make up the missed dose.

What happens if I overdose?
Seek emergency medical attention if you think you have used too much of this medicine.
Overdose symptoms may include feeling dizzy or short of breath, headache, slow heart beat, chest pain, or fainting.

What should I avoid while using Istalol?
Istalol can cause blurred vision. Be careful if you drive or do anything that requires you to be able to see clearly.

Do not use any other eye medication unless your doctor has prescribed it for you. If you use another eye medication, use it at least 10 minutes before or after using Istalol. Do not use the medications at the same time.

Istalol side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using Istalol and call your doctor at once if you have any of these serious side effects:
swelling or redness of your eyelids;
eye redness, discomfort, or sensitivity to light;
drainage, crusting, or oozing of your eyes or eyelids;
depressed mood, confusion, hallucinations, unusual thoughts or behavior;
wheezing, gasping, or other breathing problems;
swelling, rapid weight gain;
chest pain, slow or uneven heart rate; or
feeling short of breath, even with mild exertion.

Less serious side effects may include:
blurred vision, double vision, drooping eyelid;
burning or stinging in your eye;
headache, weakness, drowsiness;
numbness, tingling, or cold feeling in your hands or feet;
ringing in your ears;
dry mouth;
nausea, diarrhea, loss of appetite, upset stomach;
skin rash or worsening psoriasis;
sleep problems (insomnia); or
cough, stuffy nose.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

See also: Istalol side effects in more detail

What other drugs will affect Istalol?
Before using Istalol, tell your doctor if you are using any of the following drugs:
clonidine (Catapres);
quinidine (Cardioquin, Quinadex, Quinaglute);
reserpine;
digitalis (digoxin, Lanoxin, Lanoxicaps);
acetazolamide (Diamox), dichlorphenamide (Daranide), or methazolamide (Neptazane);
oral timolol (Blocadren);
any other beta-blocker such as atenolol (Tenormin), bisoprolol (Zebeta), labetalol (Normodyne, Trandate), metoprolol (Lopressor, Toprol), nadolol (Corgard), penbutolol (Levatol), pindolol (Visken), propranolol (Inderal, InnoPran), sotalol (Betapace), and others;
a calcium channel blocker such as diltiazem (Tiazac, Cartia, Cardizem), felodipine (Plendil), nifedipine (Procardia, Adalat), verapamil (Calan, Covera, Isoptin, Verelan), and others; orantidepressants such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), or sertraline (Zoloft).

This list is not complete and there may be other drugs that can interact with Istalol. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.
Where can I get more information?
Your pharmacist can provide more information about Istalol.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Istalol only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.