英文药名: Rythmol(propafenone tablets)

中文参考药名: 普罗帕酮片

生产厂家: Abbott

药品名称

普罗帕酮 Propafenone
中文别名：普罗帕酮、丙胺苯丙酮、丙苯酮、丙酚酮、利他脉、利它脉、普鲁帕酮、替罗帕酮、心律平、盐酸普罗帕酮、羟丙苯丙酮
英文别名：Baxarytmon、Berarytmon、Bexarytmon、Fenopraine、Rythmol、Rytmonorma
药品类别：抗心律失常药
规格

盐酸普罗帕酮片150mg , 225mg, 300mg
药理药动

药效学
本品属Ic类抗心律失常药。其电生理效应是抑制快钠离子内流，减慢收缩除极速度，使传导速度减低，轻度延长动作电位间期及有效不应期，主要作用在心房及心肌传导纤维，故对房性心律失常可能有效。对房室旁路的前向及逆向传导速度也有延长作用。可提高心肌细胞阈电位。故本品具有减低传导速度，延长有效不应期及降低兴奋性消除折返性心律失常的作用。此外本品也有轻度β受体阻滞作用及慢钙离子通道阻滞作用，轻至中度抑制心肌收缩力，后者的程度与剂量有关。
药动学
口服吸收良好，首次关卡效应明显。生物利用度因剂量及剂型而异，约4.8～23.5％。剂量增加2倍, 血药浓度可增加5 倍, 呈饱和动力学特点。吸收后主要分布肺组织，其浓度比心肌及肝脏组织内浓度高10倍，比骨骼肌及肾脏高20倍。 稳态表观分布容积为1.9～3.0L/kg。蛋白结合率约为97％。单次服药半衰期约3～4小时，多次服药约6～7小时, 口服后0.5～1小时作用开始, 2～3小时达最大作用, 作用可持续6～8小时(4～22小时)。口服2～3小时血药浓度达峰值, 有效血药浓度个体差异大, 平均约588～800ng/ml(64～3271ng/ml), 且血药浓度与剂量不成比例增加, 故用药需个体化。 中毒血药浓度约1000ng/ml。主要经肝脏代谢，其代谢产物5-羟基-丙胺基苯丙酮具有药理活性。约1％以原药经肾排出, 90%以氧化代谢物经肠道及肾脏清除。
适 应 症

口服适用于室性早搏及阵发性室性心动过速。其次为室上性心律失常，包括房性早搏、阵发性室上性心动过速及预激综合征伴室上性心动过速、心房扑动或心房颤动,但纠正心房颤动或心房扑动效果差。
静注适用于阵发性室性心动过速及室上性心动过速( 包括伴预激综合征者)。
用法用量

1．口服成人常用量：一次100—200mg，6～8小时一次。
成人处方极量：一日900mg，分次服。
小儿常用量：一次按体重5—7mg／kg，一日 3次，起效后用量减半，维持疗效。
2．静脉注射
成人常用量：一次按体重 1～1.5mg／kg，静注5分钟，必要时20分钟后可重复一次。以后可以每分钟0.5—1mg速度滴入维持。
小儿常用量：一次按体重1mg／kg，静注5分钟，必要时20分钟后可重复一次。
任何疑问，请遵医嘱！
不良反应

不良反应与剂量相关。
(1)心血管：可产生心动过缓心脏停搏及传导阻滞，尤其原有窦房结或房室结功能障碍者，应停药并静脉用阿托品或异丙肾上腺素。必要时起搏治疗。有促心律失常作用。4.4％产生低血压，尤其在原有心功能不全者，可用升压药、异丙肾上腺素等，也可加重或诱发心力衰竭，故对原有心力衰竭者应合用强心及利尿药。
(2)胃肠：食欲减退、恶心、呕吐及便秘，也可产生口干及舌唇麻木。减药或停药可消失。
(3)神经：头晕、目眩。减药或停药可消失。
(4)其他：肝脏转氨酶升高，停药后 2—4周恢复正常。
禁忌症

(1)老年人用药后可能引起血压下降，应注意观察。
(2)以下情况应禁用：
①窦房结功能障碍；
②Ⅱ或Ⅲ度房室传导阻滞，双束支传导阻滞(除非已有起博器)；
③心源性休克。
(3)以下情况应慎用：
①严重窦性心动过缓；
②Ⅰ度房室传导阻滞；
③低血压；
④肝或肾功能障碍。
药物相互作用

(1)其他抗心律失常药，包括维拉帕米、普萘洛尔、胺碘酮及奎尼丁等，可能增加本品不良反应。
(2)降压药可使本品的降压作用增强。

Rythmol and Rythmol SR can both be generically prescribed as propafenone and is commonly used in the treatment of irregular heart rates. Rythmol steadies the heart’s rhythm in order to establish strong and steady beats. While rare, there have been instances of a worsening and permanent irregular heart beat as a result of taking Rythmol. Patients and physicians need to assess this risk together.

Not all patients will benefit from Rythmol. A thorough medical examination along with a history assessment is necessary to determine what is best for the patient. Patients with a medical history which includes asthma, COPD, or any respiratory disorder, liver disease, myasthenia gravis, kidney disease, or any type of heart disease or pacemaker may not be able to handle Rythmol without special monitoring. Some patients will not be able to tolerate it at all.

The American Food and Drug Administration rated Rythmol as a pregnancy risk assessment category C. This means that it has yet to be determined whether or not a developing fetus would suffer ill effects from this medication. Rythmol does pass through the mother’s breast milk and may affect a nursing infant. Women who are pregnant or nursing should find alternative medicines if at all possible.

It is important to the patient’s health that doses are not skipped, as this can cause irregular heart rates within hours. However, in the event of an accidentally skipped dose, the patient should take the dose as soon as possible. If it is almost time for the next dose of Rythmol, the patient should skip the missed dose and resume dosing at the next regular dose. The patient should never take an additional dose to make up for missed medication.

If an overdose is suspected, the patient will need immediate health care. Tiredness, fatigue, dizziness, fainting, slow heart rate, seizures, confusion, and worsening irregular heart rate are tell tale symptoms of an overdose.

Patients may experience some side effects, especially when taking their first few doses of Rythmol. Mild side effects generally are not cause for alarm but should be reported to the prescribing physician. Mild side effects include tiredness, dizziness, headaches, blurry vision, changes in the ability to taste, stomach discomfort, constipation, vomiting, and decreased appetite.

Some patients may experience much more severe side effects when starting Rythmol. Serious side effects and allergic reactions require swift action by an emergency room physician. Serious side effects may include symptoms such as new irregular heart rate, worsening irregular heart rate, swelling of the ankles and legs, unusual bruising or bleeding, shortness of breath, chest pain, chest discomfort, infection, fever, sore throat or mouth, and mouth ulcers.

Patients often need to be educated about the likelihood of medicines interacting. Some medicines mixed with Rythmol can make the patient extremely ill. Medicines such as blood thinners, barbiturates, beta blockers, tricyclic antidepressants, local anesthetic, HIV protease inhibitor, digoxin, tolterodine, theophylline, quinidine, cyclosporine, digoxin, quinidine, sparfloxacin, and cimetidine. Patients should be urged to inquire with the prescribing physician before taking any new medicines including over the counter medicines, prescription medicines, herbal supplements, and vitamins. Interactions can be fatal.

Patients taking Rythmol should never alter their own dose, miss doses, or change their dosing regimen. The results could be dangerous to their condition.Patients should use caution when operating a vehicle or machinery while they adjust to the medicine.