药品信息:
中文别名： 拉贝洛尔、柳胺苄心安、柳胺羟胺
英文别名： Ibidomide、Presdate、Trandate
生产企业：
药品类别： 作用于植物神经系统药
药理药动
兼有α受体及β受体阻滞作用，其β受体阻滞作用约为普萘洛尔的1/2.5，但无心肌抑制作用，α受体阻滞作用为酚妥拉明的 1/6～1/10。对β受体的作用比α受体强，口服时为3:1，静注时则为 6.9:1。它与单纯β阻滞剂不同，能降低卧位血压和周围血管阻力，一般不降低心排血量或每次心搏量．对卧位病人心率无明显变化，立位或运动时心率则减慢．对高血压的疗效比单纯β阻滞剂为优。口服能迅速吸收，生物利用度约40％，Ｔ1/2为3.5～4.5小时，作用维持 8小时。
[药理作用]本品兼有α及β受体阻滞作用，对α1受体的阻滞作用为酚妥拉明的1/10～1/6，对突触前α2受体无明显作用，对β受体的阻滞作用无选择性，强度为普萘洛尔的1/6～1/4。本身对α与β受体阻滞作用之比在口服时为1∶3，静注时为1∶6.9。本品急性降压作用主要是由于阻断α1受体，长期用药后的降压作用与β受体阻断有密切关系。本品降压时不引起显著反射性心动过速、心收缩力增强或心输出量增加。
药动学
本品口服吸收良好，吸收率达90％以上，但生物利用度仅40％，达峰时间为1～2h，血浆蛋白结合率约为50％，主要分布于肺、肝和肾，表观分布容积3.3～7.9L／kg。本品在肝脏迅速灭活，代谢物60％经肾排泄，其余经胆汁从粪便排出。消除半减期为5.5h，肾功能减退不影响本品清除。
适 应 症
适用于治疗轻度至重度高血压和心绞痛；静注能治疗高血压危象。
适用于：①轻、中度高血压病。②高血压孕妇或先兆子痫。③嗜铬细胞瘤。④急进型高血压和高血压危象。⑤控制全身麻醉时的低血压。由于本品静注给药安全、可靠，故在各种需迅速降压或控制血压时，可作为首选药物。
用法用量
口服,开始每次100mg,日2-3次,如疗效不佳可增至一次200mg,日2-3次.静注一次100-200mg.
[用法及用量]口服，常用量每次100～200mg，每日2～3次，于饭后服用。严重高血压时剂量可增至每次400mg，每日3～4次。每日剂量不超过2400mg。
静注，每次50～100mg，加于25％葡萄糖液20ml内缓慢注射，15min后无效者可重复注射同样剂量1次。本品也可以用1～4mg／min速度静脉滴注。
静注速度不宜过快，静注结束后至少躺卧1h，以防体位性低血压。若发生严重低血压或心动过缓应静注苯肾上腺素或阿托品纠正。
[剂型与规格]片剂：50mg／片，100mg/片，200mg/片。注射剂：25mg/5ml，50mg/5m1。
不良反应
嗜睡,眩晕,乏力,幻觉,头痛,腹或胃部不适,感觉异常,舌根或口周麻,中毒性肝炎,甚至出现死亡.
常见的有头昏及体位性低血压，多发生于服药早期。其他不良反应有乏力、肌痉挛、胃肠道不适、恶心、梦幻、精神抑郁、射精困难、头皮刺痛等。大剂量应用时可见心动过缓或诱发早搏。
禁忌症
儿童,孕妇,哮喘及脑溢血患者忌用静注.
脑溢血、心脏传导阻滞及心动过缓者禁用，哮喘及肝功能减退者慎用。
药物相互作用
西咪替丁为一种强效肝微粒体酶抑制剂，可降低拉贝洛尔在肝内的代谢，延迟这些药物的排泄，导致其血药浓度明显升高。因而，合并用药时需减少药物的剂量以免引起药物不良反应。
相关英文资料
有 效 期 0 年
Chinese alias: labetalol, metoprolol labetalol, Liu amine hydroxylamine
English Synonyms: Ibidomide, Presdate, Trandate
Manufacturer:
Drug Category: acting on the autonomic nervous system drugs
Pharmacology, Pharmacokinetics
Both α and β receptor blockers effect, the β-blocker propranolol effect of approximately 1 / 2.5, but no cardiac inhibition, α receptor blocking effect of phentolamine 1 / 6 to 1/10. Β receptors on stronger than α receptor, when administered orally for three: one, when compared with intravenous 6.9: 1. It is different with the pure β-blockers can reduce supine blood pressure and peripheral vascular resistance, generally do not reduce cardiac output or per stroke volume. Supine patient to no significant changes in heart rate, heart rate while standing position or movement is slowed down. The effect of hypertension than simply β-blockers is superior. Can rapidly absorb oral bioavailability of approximately 40%, T1 / 2 of 3.5 to 4.5 hours, the role for 8 hours.
[Pharmacological action] The product of both α and β receptor blocking action on the α1 receptor blockade as phentolamine 1/10 to 1/6 of the presynaptic α2 receptors had no significant effect β receptor blocking effect of non-selective, strength of propranolol 1/6 to 1/4. Α and β receptor itself blockade ratio is 1:3 when administered orally, intravenously to 1:6.9 when. This product is mainly due to acute hypotensive effect of blocking α1 receptors, long-term antihypertensive effects after treatment with β-blockers are closely related. This product does not cause significant reflex tachycardia when buck, increased cardiac contractility or cardiac output.
Pharmacokinetics
This product is good oral absorption, the absorption rate of more than 90%, but only 40% bioavailability, peak time is 1 ~ 2h, plasma protein binding rate is about 50%, mainly in the lungs, liver and kidneys, the apparent distribution volume of 3.3 ~ 7.9L / kg. This product is rapidly inactivated in the liver, 60% of metabolites excreted by the kidneys, and the remaining bile from the feces. Elimination half-life of 5.5h, renal dysfunction does not affect the product removed.
Indications
For the treatment of mild to severe hypertension and angina; intravenously to treat hypertensive crisis.
Apply to: ① mild to moderate hypertension. ② hypertension or pre-eclampsia in pregnant women. ③ pheochromocytoma. ④ aggressive type of hypertension and hypertensive crisis. ⑤ controlled hypotension during anesthesia. Since the intravenous administration of this product is safe, reliable, so when you need quick buck or a variety of blood pressure control, can be used as the drug of choice.
Dosage
Oral, the beginning of each 100mg, 2-3 times a day, such as poor efficacy may be increased once 200mg, 2-3 times a day. Intravenously once 100-200mg.
[Usage and dosage] oral, the usual dose every 100 ~ 200mg, 2 to 3 times a day, in after meals. Severe hypertension when the dose may be increased each 400mg, 3 to 4 times a day. The daily dose of no more than 2400mg.
Intravenously every 50 ~ 100mg, added to the 25% glucose solution 20ml slow injection, 15min after injection of the same ineffective dose can be repeated one time. This product can also be used 1 ~ 4mg / min infusion rate.
Intravenous speed not too fast, lying down for at least 1h after the intravenous injection to prevent orthostatic hypotension. In case of severe hypotension or bradycardia intravenous phenylephrine or atropine should be corrected.
[Formulations and specifications] tablets: 50mg / tablets, 100mg / tablets, 200mg / tablets. Injection: 25mg / 5ml, 50mg / 5m1.
Adverse reactions
Drowsiness, dizziness, fatigue, hallucinations, headache, abdominal or stomach discomfort, paresthesia, tongue, or perioral numbness, toxic hepatitis, or even death.
Common dizziness and orthostatic hypotension, occurred in the early medication. Other adverse reactions were fatigue, muscle cramps, gastrointestinal discomfort, nausea, fantasy, mental depression, ejaculation difficulties, scalp tingling. Large doses of visible or induced bradycardia premature application.
Contraindications
Children, pregnant women, asthma and stroke patients hanged intravenously.
Stroke, heart block and bradycardia were banned, asthma and liver dysfunction with caution.
Drug Interactions
Cimetidine is a potent inhibitor of hepatic microsomal enzymes, which reduces labetalol metabolism in the liver, delayed excretion of these drugs, resulting in significantly increased plasma concentrations. Thus, when combination therapy reduce the dose of drug required to avoid adverse drug reactions.
Related information in English
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