阿替洛尔(氨酰心安)
Atenolol (Tenormine)
【作用与用途】本品为心脏选择性β-受体阻断剂，无膜稳定作用，无内源性拟交感活性。一般用于窦性心动过速及早搏等，也可用于高血压、心绞痛及青光眼。
【用法】成人口服：每天50-100mg，分1-2次服用：用于心绞痛，每次100mg，或每次25-50mg，一天2次，用于高血压，一次50-200mg，一天一次。
以上用药需个体化。青光眼用4%滴眼液点眼。
【副作用】个别患者可出现心动过缓。
【禁忌】严重窦性心动过缓、房室传导阻滞，心力衰竭患者及孕妇禁用。
【药理】药效学
参见盐酸普萘洛尔， 但主要使β1受体的活动处于抑制状态。
药动学
口服吸收约为50％。小剂量可通过血脑屏障。蛋白结合率6－10％。服后2－4小时作用达峰值，作用持续时间较久。半衰期为6-7小时，主要以原形自尿排出。在血液透析时可予以清除。
盐酸普萘洛尔药效学：本品有肾上腺素β受体部位竞争性地抑制儿茶酚胺的作用。通过减弱或防止β受体兴奋而使心脏的收缩力与收缩速度下降,通过传导系统的传导速度减慢,使心脏对运动或应激的反应减弱。因此，用于心绞痛的治疗，减低心肌氧耗，增加运动耐量。由于阻滞心脏起搏点电位的肾上腺素能兴奋故用于治疗心律失常。可能本品通过中枢、肾上腺素能神经元阻滞、抗肾素活性以及心排血量减低等降低血压，适用于治疗高血压。由于本品能拮抗儿茶酚胺效应，也用于治疗嗜铬细胞瘤及甲状腺机能亢进，使β1和β2受体的活动均处于抑制状态。当β受体阻断药与α受体阻断药合用时可拮抗肾上腺素的升高血糖作用。一般认为人类的脂肪分解主要与β1受体激动有关。
【药理作用】
本品为长效、选择性β1肾上腺素受体阻滞药，其心脏选择性作用明显强于美托洛尔，而对血管及支气管平滑肌的β2受体抑制较弱。无内源性拟交感活性，无膜稳定性，也无抑制心肌收缩力的作用。本品可降低高血压患者的血压，减轻由运动所致的血压增高。同时，通过减低心率(8％～34％)和心率、血压乘积(9％～40％)，减少心绞痛发作的严重程度和频率，改善急性心肌梗死患者的耗氧指数。因此早期应用该药可缩小心肌梗死面积和预防再梗死，长期应用可降低心肌梗死或卒中的死亡率。
口服后吸收率达50％～60％，血药达峰时间为2～4h。生物利用度约60％，血浆蛋白结合率约46％，表观分布容积为0.8L／kg。体内分布广泛，极少量进入脑部，能迅速透过胎盘，可积聚于乳汁，但婴儿血药浓度含量甚微。肾功能正常的成年患者消除半减期约5～7h，总清除率约为6L／h(100ml／min)。儿童清除半减期较短(4、5h)。吸收后的药物约46％以原形由尿中排出。肾功能异常者清除率降低，主要与肾小球滤过率有关。
用于治疗心绞痛、心律失常、高血压、甲状腺机能亢进、嗜铬细胞瘤、心肌梗塞，指证同盐酸普萘洛尔。
适用于各种原因所致的中、轻度高血压病，包括老年高血压病和妊娠期高血压。最大降压作用发生在治疗开始2周内。临床适用于缺血性心脏病的治疗，包括不稳定型心绞痛，尤适用于治疗稳定型心绞痛。可降低心绞痛发作频率和严重程度，减少硝酸甘油用量，改善运动耐力和ST段压低，具有明显疗效，对伴或不伴有心肌缺血证据的高血压患者，长期应用本品可降低心肌梗死或卒中的死亡率。而且，对确诊或疑有心肌梗死者，早期应用本品也可降低心血管病的死亡率和非致命性心脏骤停及再梗死的发生率。本品可用于防治室上性心动过速、持续性阵发性反复发作性室上性心动过速及室性心律失常，也可降低冠脉术后室上性心律失常和房颤发生率。对青光眼也有效。
【适应症】
口服成人常用量：开始每日 12.5—25mg，一次服，2周后按需要及耐受量增至 50—100mg。肾功能损害时，肌酐清除率每分钟＜15ml/1.73平方米者，隔天给50mg，每分钟 15—35ml/1.73平方米者，每天最多 50mg。
用于心绞痛，每次 12.5—25mg，一日 2次，可渐增至每日总量 150mg。
用于高血压，每次 25mg，一日 1—2次，可渐增至每日总量 200mg。
【制剂与规格】阿替洛尔片(1)12.5mg(2)25mg
口服: 用于心绞痛,每日1次0.1g,或每次25-50mg,一日2次;用于高血压:每日一次50-200mg;青光眼用4%溶液滴眼.
【用法及用量】口服，一般每次50～100mg，每日1次。用于心绞痛，每次25～100mg，每日1次。视病情而调整给用剂量；用于高血压，每次50～200mg，每日1次。
静脉注射，初始剂量2.5～5mg溶于25％葡萄糖液20mL中稀释，按1mg／min速度静注，如无效，5min后可重复给药，最大给药剂量为10mg。静脉滴注，初始剂量为0.15mg／kg，大于20min滴完，如需要，间隔12h可重复给药1次。青光眼患者用4％溶液滴眼。
对哮喘患者不作为首选治疗。
本品应用过程中，不能突然停药，以免发生停药后综合征。
【剂型与规格】片剂：50mg／片，100mg／片。注射剂：5mg/2ml。
【用法用量】参见盐酸普萘洛尔。
本品与外用李氏药贴、降压申贴、悬压贴等外用中药贴合用可加强降血压效果。与利尿药、钙拮抗药或血管紧张素转换酶抑制药合用，也可增强其降压作用。本品与Ⅰ类抗心律失常药物或维拉帕米合用时必需谨慎，
【给药说明】参见盐酸普萘洛尔。
严重肾功能减退者(肌酐清除率＜ 0.5845ml/秒/1.73平方米)需调整给药剂量。
对儿童、严重心力衰竭者不主张应用。
对进行血透的患者，每次透析后应当日服50mg。
对心脏储备功能不良者使用本品时也必须小心。
显著心动过缓、房室传导阻滞和心源性休克患者禁用。
【不良反应】
①本品的临床效应与血药浓度可不完全平行，剂量调节以临床效应为准；
②肾功能损害时剂量须减少；
③有心力衰竭症状的患者用本品时，应先给洋地黄苷或利尿药，如心力衰竭症状仍存在，应逐渐减量停用；
④本品的停用过程至少 3天，长可达 2周，如有撤药症状，如心绞痛发作，则暂时再给药，待稳定后渐停用；
⑤与饮食共进不影响其生物利用度。
本品应用过程中，不能突然停药，以免发生停药后综合征。
【相互作用】
①心动过缓(＜50次／分钟)、精神抑郁、手足冷、呼吸困难，脚肿较少见；
②罕见的有皮疹、关节痛、胸痛等。
心动过缓,周身性红斑狼疮样反应,多关节病综合症,性功能障碍.大剂量可有心脏停博,可引起死亡.
主要有：
①心动过缓，发生率为0.6％～10％。
②肢端发冷或雷诺现象，2％～35％。
③胃肠道症状，0.5％～30％，表现为恶心、腹泻及胃部不适。
④疲乏或虚弱，1％～51％。
⑤恶梦或睡眠障碍，占6％～26％。
⑥头痛，1％～18％。⑦性功能障碍，1％～14％。通常认为本品发生的副作用较轻，且常见于初期治疗阶段，但一般不影响继续治疗，仅有3％～6％的患者需停止用药。心肌梗死患者静注本品后可出现低血压和心动过缓。

英文药名: Tenormin (Atenolol Tablets)

中文药名: 阿替洛尔片,天诺敏,氨酰心安

生产厂家: AstraZeneca

Generic Name: atenolol (ah TEN oh lol)
Brand Names: Tenormin
What is atenolol?
Atenolol (Tenormin) is in a group of drugs called beta-blockers. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).

Atenolol is used to treat angina (chest pain) and hypertension (high blood pressure). It is also used to treat or prevent heart attack.

Atenolol may also be used for purposes other than those listed in this medication guide.
Important information about atenolol

Do not stop taking atenolol without first talking to your doctor. Stopping suddenly may make your condition worse.

If you need to have any type of surgery, you may need to temporarily stop using atenolol. Be sure the surgeon knows ahead of time that you are using atenolol.

Atenolol can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Avoid drinking alcohol, which could increase drowsiness and dizziness while you are taking atenolol.

Atenolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

If you are being treated for high blood pressure, keep using this medication even if you feel fine. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Store atenolol at room temperature away from moisture and heat.

What should I discuss with my healthcare provider before taking atenolol?
You should not use this medication if you are allergic to atenolol, or if you have certain heart conditions such as slow heartbeats, or heart block.

Before taking atenolol, tell your doctor if you have:asthma, bronchitis, emphysema;aiabetes;low blood pressure;a heart problem such as heart block, sick sinus syndrome, slow heart rate, or congestive heart failure;depression;liver or kidney disease;a thyroidisorder;myastheniagravis;pheochromocytoma; orproblems with circulation (such as Raynaud's syndrome).

If you have any of these conditions, you may need a dose adjustment or special tests to safely take this medication.

FDA pregnancy category D. This medication can cause harm to an unborn baby. Do not use atenolol if you are pregnant. Tell your doctor if you become pregnant during treatment. Use an effective form of birth control while you are using this medication. Atenolol can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take atenolol?
Take atenolol exactly as it was prescribed for you. Do not take the medication in larger amounts or for longer than recommended by your doctor. Follow the directions on your prescription label.

Take this medication with a full glass of water.

Take atenolol at the same time every day.

Do not skip doses or stop taking atenolol without first talking to your doctor. Stopping suddenly may make your condition worse.

To be sure this medication is helping your condition, your blood pressure will need to be checked on a regular basis. Do not miss any visits to your doctor.

If you need to have any type of surgery, tell the surgeon that you are using atenolol. You may need to briefly stop using atenolol before having surgery.

Atenolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

If you are being treated for high blood pressure, keep using atenolol even if you feel fine. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Store atenolol at room temperature away from moisture and heat.

What happens if I miss a dose?
Take the missed dose as soon as you remember. If your next dose is less than 8 hours away, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take 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 uneven heartbeats, shortness of breath, bluish-colored fingernails, dizziness, weakness, fainting, or seizure (convulsions).
What should I avoid while taking atenolol?
Atenolol can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Avoid drinking alcohol, which could increase drowsiness and dizziness while you are taking atenolol.

Atenolol 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. Call your doctor at once if you have any of these serious side effects:Slow or uneven heartbeats;feeling light-headed, fainting;feeling short of breath,even with mild exertion;swelling of your ankles or feet;nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);depression; orcold feeling in your hands and feet.

Less serious atenolol side effects may include:decreased sex drive, impotence, or difficulty having an orgasm;sleep problems (insomnia);tired feeling; oranxiety, nervousness.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

See also: Atenolol side effects in more detail
What other drugs will affect atenolol?
Before taking atenolol, tell your doctor if you are using:allergy treatments (or if you are undergoing allergy skin-testing);amiodarone (Cordarone, Pacerone);clonidine (Catapres);digoxi(digitalis,Lanoxin);disopyramide (Norpace);guanabenz (Wytensin);an MAO inhibitor such as isocarboxazid (Marplan), tranylcypromine (Parnate), phenelzine (Nardil), or selegiline (Eldepryl, Emsam);a diabetes medication such as insulin, glyburide (Diabeta, Micronase, Glynase), glipizide (Glucotrol), chlorpropamide (Diabinese), or metformin (Glucophage);a heart medication such as nifedipine (Procardia, Adalat), reserpine (Serpasil), verapamil (Calan, Verelan, Isoptin), diltiazem (Cartia, Cardizem);medicine for asthma or other breathing disorders, such as albuterol (Ventolin, Proventil), bitolterol (Tornalate), metaproterenol (Alupent), pirbuterol (Maxair), terbutaline (Brethaire, Brethine, Bricanyl), and theophylline (Theo-Dur, Theolair); orcold medicines, stimulant medicines, or diet pills.

If you are using any of these drugs, you may not be able to take atenolol, or you may need dosage adjustments or special tests during treatment.

There may be other drugs not listed that can affect atenolol. 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 atenolol.

What does my medication look like?
Atenolol is available with a prescription under the brand name Tenormin. Other brand or generic forms may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you.
Tenormin 25 mg - round, flat, white, uncoated
Tenormin 50 mg - round, flat, white, uncoated
Tenormin 100 mg - round, flat, white, uncoated

Every effort has been made to ensure that the information provided is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. 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. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects.