药品信息:
通用名称：普萘洛尔
英文名称：Propranolol
中文别名：恩得来、恩特来、心得安、萘心安、萘氧丙醇胺
英文别名：Inderal、Propranololum
规格
盐酸普萘洛尔片10mg, 20mg, 40mg, 80mg, 120mg。
心得安长效胶囊 40mg, 60mg, 80mg, 120mg, 160mg。
药理作用
药效学
普萘洛尔能竞争性的阻断β受体，大剂量尚有膜稳定作用，抑制Na离子内流，从而产生抗心律失常作用。
1、降低自律性。抑制窦房结、心房、浦肯野纤维自律性，此作用在运动及情绪激动时尤为明显，也能降低儿茶酚胺所致的迟后去极而防止触发活动。
2、减慢传导。在其阻断β受体的浓度时，并不影响传导速度，但当血药浓度超过100ng/ml时，由于膜稳定性作用，可降低0相上升速率，明显减慢房室结及浦肯野纤维的传导。
3、对动作电位时程和有效不应期的影响。治疗量缩短动作电位时程和有效不应期，高浓度时则使之延长，对房室结的有效不应期有明显的延长作用。
药动学
口服后胃肠道吸收较完全(90％), 1～1.5小时血药浓度达峰值,但进入全身循环前即有大量被肝代谢而失活,生物利用度为30％。与血浆蛋白的结合率很高, 为93%, 半衰期为2～3小时,经肾脏排泄,主要为代谢产物,小部分(＜1％)为原形物。 不能经透析排出。
适应症
用于治疗：
①心律失常，纠正室上性快速心律失常、室性心律失常、泮地黄类及儿茶酚胺引起的快速心律失常；
②心绞痛（典型心绞痛，即劳力型心绞痛）；
③高血压，作为第一线用药，单独或与其他药物合并应用；
④肥厚性心肌病，用于减低流出道压差，减轻心绞痛、心悸与昏厥等症状；
⑤嗜铬细胞瘤，用于控制心动过速；
⑥甲状腺机能亢进症用于控制心率过快，也用于治疗甲状腺危象或危象先兆；甲状腺次全切除术的术前准备；对病情较重的甲亢患者在抗甲状腺药物或放射性碘治疗尚未奏效前用以控制症状。
⑦心肌梗塞；作为次级预防；
⑧二尖瓣脱垂综合征。
用法用量
1．抗心律失常口服，一次 10—30mg，一日 3—4次，应根据需要及耐受程度调整用量。严重心律失常应急时可静脉注射 1—3mg，以每分钟不超过 1mg的速度静注，必要时 2分钟后可重复一次，以后隔 4小时一次。小儿用量尚未确定，一般口服按体重每日 0.5—1.0mg/kg，分次服；静脉注射按体重 0.01—0.1mg/kg，缓慢注入，一次量不宜超过 1mg。
2．心绞痛口服，开始 5—10mg，每日 3—4次，每 3日可增加 10—20mg，可渐增至每日200mg，分次服。
3．高血压口服，一次 5—10mg，每日 3—4次，按需要及耐受程度逐渐调整，至症状被控制。
4．肥厚性心肌病口服，一次 10—20mg，每日 2—4次，按需要及耐受程度逐渐调整。
5．嗜铬细胞瘤口服，一次 10—50mg，一日 3—4次，术前用 3天，常与 α受体阻滞药同用，一般应先用 α受体阻滞药，待药效出现并稳定后再加用本品。
任何疑问，请遵医嘱！
禁用/慎用
(1)本品可通过胎盘进入胎儿体内，有报道妊娠高血压者用后可致宫内胎儿发育迟缓，分娩时无力造成难产，新生儿可产生低血压、低血糖、呼吸抑制及心率减慢，尽管也有报告对母亲及胎儿均无影响，但必须权衡利弊，不宜作为孕妇第一线治疗药物。
(2)可从乳汁分泌小量，故哺乳期妇女应用必须权衡利弊。
(3)老年人对本品代谢与排泄能力低，应适当调节剂量。
(4)下列情况应禁用：
①支气管哮喘；
②心源性休克；
③心传导阻滞(Ⅱ至Ⅲ度房室传导阻滞)；
④重度心力衰竭；
⑤窦性心动过缓。
(5)下列情况应慎用：
①过敏史；
②充血性心力衰竭；
③糖尿病；
④肺气肿或非过敏性支气管炎；
⑤肝功能不全；
⑥甲状腺功能低下；
⑦雷诺综合征或其他周围血管疾病；
⑧肾功能减退。
给药说明
①用量必须强调个体化，不同个体、不同疾病用量不尽相同，肝、肾功能不全者用小量；
②糖尿病患者虽可引起血糖过低，但在非糖尿病人中则无降血糖作用；
③注意血药浓度不能完全预示药理效应，故还应根据心率及血压等临床征象指导临床用药；
④口服可以在空腹时，也可与食物共进，后者可使本品在肝内代谢减慢，生物利用度增值；
⑤冠心病患者使用本品不宜骤停，否则可出现心绞痛、心肌梗塞或室性心动过速；
⑥甲亢病人用本品也不可骤停，否则使甲亢症状加重；
⑦长期用本品者撤药须逐渐递减剂量，至少经过 3天，一般为 2周；
⑧长期应用可在少数病人出现心力衰竭，倘若出现，可用洋地黄苷类和(或)利尿药纠正，并渐递减达停用。
应用本品过程中应定期检查血常规、血压、心功能、肝功能、肾功能，糠尿病病人应定期查血糖。
(1)甲亢合并心功能不全者慎用，因本品可使心脏收缩功能减弱，必须采用时，应合用强心药。
(2)作为手术前准备，其优点为奏效快，疗程短，往往数天至一周左右即可控制症状，使心率降至正常范围。由于本品作用往往短暂，故必须一直用药到手术日晨，在手术中必要时需静脉注射，手术后也需继续应用，一直到血 T4、T3降至正常。单用本品作手术前准备不如抗甲状腺药物加碘剂可靠，故主要用于不能耐受抗甲状腺药物者及急需紧急手术者。
不良反应
由于本品能透入神经系统，故可出现中枢神经系统不良反应。
①较常见的有眩晕或头昏(低血压所致)、心率过慢(＜50次／分钟)；
②较少见的有支气管痉挛及呼吸困难、充血性心力衰竭、神志模糊(尤见于老年人)、精神抑郁，反应迟钝；
③更少见的有发热和咽痛(粒细胞缺乏)、皮疹(过敏反应)、出血倾向(血小板减小)；
④不良反应持续存在时，须格外警惕的有四肢冰冷、腹泻、倦怠、眼口或皮肤干燥、恶心、指趾麻木、异常疲乏等。
应严密观察血压及心律变化,如心律变慢,立即停药.乏力,嗜睡,头晕,失眠,恶心,皮疹. 个别病例有周身性红斑狼疮样反应,多关节病综合症,幻视,性功能障碍(或性欲下降).剂量过大时引起低血压(血压下降),心动过缓,惊厥,呕吐. 可诱发缺血性脑梗塞,可有心源性休克,甚至死亡。
它可引起哮喘；可发生Ⅰ型过敏反应及Ⅳ型迟发过敏反应颇似Lyell综合征；可出现荨麻疹、牛皮癣样皮疹。有报告可发生过敏性肺炎；脱发；及致有硬化性腹膜炎。
此药的停药反应并不限于心血管，也常见有头痛、震颤及焦虑，有时也可出现精神异常。
药物相互作用
(1)与可乐定同用而须停药时，须先停用本品，数天后再逐步减停可乐定，以免血压波动。
(2)与洋地黄苷类同用，可发生房室传导阻滞而致心率过慢，故须严密观察。
(3)与肾上腺素、苯福林或拟交感胺类同用，可引起显著高血压、心率过慢，也可能出现房室传导阻滞，故须严密观察。
(4)可使非去极化肌松药如氯化筒箭毒碱、加拉碘铵等增效，时效也延长。
(5)可影响血糖水平，故与降糖药同用时，须调整后者的剂量。
(6)与异丙肾上腺素或黄嘌呤同用，可使后两者疗效减弱。
(7)与单胺氧化酶抑制剂同用，可致极度低血压，禁用。
(8)与吩噻嗪类同用，可使两者的血药浓度均升高。
(9)与利血平同用，两者作用相加，β受体阻滞作用增强，有可能出现心动过缓及低血压。
苯巴比妥及异烟肼使普萘洛尔的清除增多并减低它们在周身的利用率。
西咪替丁为一种强效肝微粒体酶抑制剂，可降低普萘洛尔、拉贝洛尔、美托洛尔等药物在肝内的代谢，延迟这些药物的排泄，导致其血药浓度明显升高。因而，合并用药时需减少上述药物的剂量以免引起药物不良反应。
注意事项
（1）除对心脏的β受体（β1受体）有阻断作用外，对支气管及血管平滑肌的β受体（β2受体）亦有阻断作用，可引起支气管痉挛及鼻粘膜微细血管收缩，故忌用于哮喘及过敏性鼻炎病人。
（2）忌用于窦性心动过缓、重度房室传导阻滞、心源性休克、低血压症病人。充血性心力衰竭病人（继发于心动过速者除外），须等心衰得到控制后始可用本品。不宜与抑制心脏的麻醉药（如乙醚）合用。
（3）有增加洋地黄毒性的作用，对已洋地黄化而心脏高度扩大、心率又较不平稳的病人忌用。
（4）不宜与单胺氧化酶抑制剂（如帕吉林）合用。
（5）本品剂量的个体差异较大，宜从小到大试用，以选择适宜的剂量。长期用药时不可突然停药。
（6）副作用可见乏力、嗜睡、头晕、失眠、恶心、腹胀、皮疹、晕厥、低血压、心动过缓等，须注意。
Inderal - Used for: Treating high blood pressure or atrial fibrillation. It is used in patients with angina to decrease angina frequency and increase exercise tolerance. It is used to decrease the risk of heart death in certain patients who have survived a heart attack. It is used to manage certain types of tremors, a heart condition called hypertrophic subaortic stenosis, or certain symptoms of pheochromocytoma (an adrenal tumor). It is used to prevent migraine headaches. It may also be used for other conditions as determined by your doctor.
Inderal is a beta-blocker. It works by slowing down the heart and decreasing the amount of blood it pumps out. This helps to decrease blood pressure, helps the heart pump more efficiently, and reduces the workload on the heart. Exactly how Inderal works to treat migraines or tremors is not known.
Inderal is a non-selective beta-blocker. This medication has antihypertensive, antianginal and antiarrhythmic action.
The hypotensive effect is associated with a decrease in minute volume of blood, sympathetic stimulation of peripheral vascular disease, decreased activity of the renin-angiotensin system (has a value in patients with initial hypersecretion of renin), sensitivity of baroreceptors of the aortic arch (not going to enhance their activity in response to decreased blood pressure) and the effect on the CNS. The hypotensive effect is stabilized by the end of the second week of the prescription course.
The antianginal effect of Inderal is due to reduced myocardial oxygen demand (due to the negative chronotropic and inotropic effect). The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of AV-holding.
The ability of this drug to prevent the development of headache of vascular origin is due to a decrease in expression of the expansion of cerebral arteries due to beta-adrenoblockade vascular receptors, inhibition induced by catecholamines platelet aggregation and lipolysis, reduction of platelet adhesiveness, prevention of activation of coagulation factors during the release of adrenaline, the stimulation of oxygen supply to tissues and decreased secretion of renin.
Reduction of tremor during treatment with Inderal caused mainly by the blockade of peripheral beta2-adrenergic receptors.
This medicine increases the atherogenic properties of blood; strengthens uterine contractions (spontaneous or induced by means of stimulating the myometrium); increases the tone of the bronchi; in high doses cause sedation.
Inderal, the prototype of the beta-adrenergic receptor antagonists, is a competitive, nonselective beta-blocker similar to nadolol without intrinsic sympathomimetic activity. Propanolol is a racemic compound; the l-isomer is responsible for adrenergic blocking activity. Indication: For the prophylaxis of migraine. Inderal is in a group of drugs called beta-blockers. Beta-blockers affect the heart and circulation (blood flow through arteries and veins). Inderal is used to treat tremors, angina (chest pain), hypertension (high blood pressure), heart rhythm disorders, and other heart or circulatory conditions. It is also used to treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches. Inderal may also be used for other purposes not listed in this medication guide. Inderal is a non-selective beta blocker mainly used in the treatment of hypertension. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis of migraines in children. Inderal is available in generic form as Inderal hydrochloride, as well as an AstraZeneca and Wyeth product under the trade names Inderal, Inderal LA, Avlocardyl (also available in prolonged absorption form named "Avlocardyl Retard"), Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum (depending on marketplace and release rate)
Control of hypertension ; management of angina pectoris ; long-term prophylaxis after recovery from acute myocardial infarction; control of cardiac arrhythmias ; prophylaxis of migraine ; management of essential tremor ; control of anxiety and anxiety tachycardia ; adjunctive management of thyrotoxicosis and thyrotoxic crisis ; management of hypertrophic obstructive cardiomyopathy ; and management of pheochromocytoma (Inderal should only be started in the presence of effective α-blockade).
Inderal helps to keep your blood pressure under control. It may also be used to treat certain heart diseases such as angina pectoris (chest pain) and arrhythmia (irregular heart beats). Inderal may also be used to relieve palpitations (fast and irregular heartbeats) commonly experienced by people with an overactive thyroid gland. Inderal is also used together with other medicines to prevent migraine or in the treatment of specific complications caused by liver disease.
Control of hypertension. Management of angina pectoris. Long-term prophylaxis after recovery from acute myocardial infarction. Control of cardiac arrhythmias. Prophylaxis of migraine. Management of essential tremor. Control of anxiety and anxiety tachycardia. Adjunctive management of thyrotoxicosis and thyrotoxic crisis. Management of hypertrophic obstructive cardiomyopathy. Management of phaeochromocytoma (Inderal should only be started in the presence of effective α-blockade).
Indications: hypertension, arrhythmias, angina pectoris, myocardial infarction, migraine
Indications: hypertension, angina pectoris, hypertrophic obstructive cardiomyopathy, arrhythmias, hyperthyroidism Indications: angina pectoris, hypertension, arrhythmias, myocardial infarction, hypertrophic subaortic stenosis
Indications: arrhythmias, hypertrophic obstructive cardiomyopathy, phaeochromocytoma, hyperthyroidism, angina pectoris
Indications: hypertension, angina pectoris, myocardial infarction, arrhythmias, migraine
OralAngina pectoris caused by coronary atherosclerosis (excluding InnoPran XL ); cardiac arrhythmias (excluding ER); essential tremor (excluding ER); hypertension; hypertrophic subaortic stenosis (excluding InnoPran XL ); migraine prophylaxis (excluding InnoPran XL ); MI (excluding ER); pheochromocytoma (excluding ER).IVCardiac arrhythmias.
Indications: Hypertension.
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