近日，美国FDA批准GSK公司开发的β阻滞剂Coreg CR（carvedilol phosphate，磷酸卡维地洛）缓释胶囊/缓释片已获美国批准，用于三种心血管疾病的治疗：高血压、心肌梗死、左心室功能不全及轻至中度心力衰竭。
批准日期：公司：葛兰素
COREG CR(卡维地洛磷酸[Carvedilol Phosphate])缓释胶囊 供口服使用
美国初步批准: 1995
作用机制
卡维地洛是一种消旋混合物, 其中非选择性β‑adrenoreceptor 阻塞活动存在于S(-) 映体, α1‑adrenergic阻挡活动存在于R(+)和S (-) 对映体在同等效力。卡维地洛没有内在的 sympathomimetic 活动。
适应症和用法
COREG CR是一种用于治疗的阿尔法/β肾上腺素阻断剂:
•mild严重慢性心力衰竭。
临床稳定患者心肌梗死后
•left心室功能不全。
高血压.
剂量和管理
带上食物。不要压碎或咀嚼胶囊。在上滴定过程中个性化的剂量和监测。
•Heart 失败: 每天10毫克开始, 并增加到20, 40, 然后80毫克一次每日超过间隔至少2周。如果不耐受更高剂量, 则保持较低剂量。
心肌梗死后
•Left心室功能不全: 每天20毫克开始, 每天增加40毫克80毫克, 间隔3到10天。可以使用较低的起始剂量或较慢的滴定。
•Hypertension: 开始在20毫克一次每日并且增加, 如果需要为血压控制到40毫克然后80毫克一次每日间隔1到2星期。
•Elderly患者(65岁): 当从更高剂量的卡维地洛直接释放到 COREG CR时, 应考虑较低的起始剂量, 以降低低血压和晕厥的风险。
剂型和强度
胶囊: 10mg, 20mg, 40mg, 80mg
禁忌
•Bronchial哮喘或相关bronchospastic条件。
•Second或三级AV块。
•Sick窦综合征。
•Severe心动过缓 (除非有永久性起搏器到位)。
•Patients在心源性休克或失代偿心力衰竭需要使用IV强心剂治疗。
•Severe肝损伤。
•History严重过敏反应 (如史蒂文斯-约翰逊综合征, 过敏性反应, 水肿) 对卡维地洛或 COREG 的任何组成部分。
警告和预防措施
•Acute在停止治疗后加重冠状动脉疾病: 不要突然停止。
•Bradycardia, 低血压, 加重心力衰竭/液体滞留可能发生。根据需要减少剂量。
•Non过敏性痉挛 (如慢性支气管炎和肺气肿): 避免β‑blockers。但是, 如认为有必要, 应谨慎使用, 最低有效剂量。
•Diabetes: 监测葡萄糖为β‑blockers 可能掩盖低血糖症状或加重高血糖。
不良反应
COREG CR 的安全状况与即刻释放卡维地洛相似。最常见的不良事件立即释放卡维地洛:
心肌梗死后•Heart 衰竭和左心室功能障碍 (≥10%): 头晕、疲劳、低血压、腹泻、高血糖、乏力、心动过缓、体重增加。
•Hypertension (≥5%): 头晕。
药物相互作用
•CYP P450 2D6 酶抑制剂可能增加, 利福平可能降低卡维地洛水平。
•Hypotensive 剂 (如利血平, 毛抑制剂, 可乐定) 可能增加低血压和/或严重心动过缓的风险。
•Cyclosporine 或地高辛水平可能增加。
•Both 洋地黄苷和β阻滞剂减缓房室传导, 降低心率。伴随使用可以增加心动过缓的风险。
•Amiodarone 可能增加卡维地洛水平, 从而进一步减慢心率或心脏传导。
•Verapamil 或地尔硫类钙通道阻滞剂可能影响心电图和/或血压。
•Insulin 和口服 hypoglycemics 的作用可能会增强。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=06400a4c-42b4-440a-92b4-1f47f98ac7ba
This information is not meant to provide medical advice. Your doctor should always be your main source of information about your condition and how to manage it.
Hypertension: COREG CR is approved to treat patients with high blood pressure, which is also known as hypertension.
Left Ventricular Dysfunction Following Myocardial Infarction: COREG CR is approved to treat patients who had a heart attack that worsened how well the heart pumps.
Heart Failure: COREG CR is approved to treat patients with certain types of heart failure.
Important Safety Information for Coreg CR® (carvedilol phosphate) Extended-release Capsules, 10, 20, 40 and 80 mg capsules
It is important for patients to take their medicine every day as directed by their doctor or health care provider. If patients stop taking COREG CR suddenly, they could have chest pain and/or a heart attack. If the doctor decides that a patient should stop taking COREG CR, the doctor may slowly lower the dose over a period of time before stopping it completely.
Some people should not take COREG CR, including patients with the following conditions: severe heart failure requiring intravenous medications to help support circulation; asthma or other breathing problems; a slow heartbeat or certain conditions that can cause the heart to skip a beat (irregular heartbeat); liver problems; or allergy to COREG CR or any of its ingredients.
Possible serious side effects of COREG CR include slow heart beat, low blood pressure (which may cause dizziness or fainting when standing up), worsening heart failure (which may include signs and symptoms such as weight gain or increased shortness of breath), changes in blood sugar, and peripheral vascular disease symptoms (such as leg pain when walking that goes away at rest, numbness or no feeling in legs or feet while resting, and cold legs or feet).
COREG CR is a beta-blocker. Beta-blockers may mask the symptoms of an overactive thyroid or low blood sugar (especially a fast heartbeat), or may alter blood sugar levels. People with diabetes should report any changes in blood sugar levels to their doctor.
Rare but serious allergic reactions (including hives or swelling of the face, lips, tongue, and/or throat that may cause difficulty in breathing or swallowing) may happen with COREG CR and can be life-threatening. Medicines to treat a severe allergic reaction may not work as well while taking COREG CR.
Common side effects of COREG CR include shortness of breath, weight gain, diarrhea, and tiredness. If you wear contact lenses, you may have fewer tears or dry eyes that can become bothersome.
If you experience dizziness or fainting when you stand up, you should sit or lie down. Do not drive a car, use machinery, or do anything that needs you to be alert if you have these symptoms. Call your doctor right away if you have any side effects that bother you or don't go away.
Tell your doctor what other medications you are taking. Take COREG CR exactly as your doctor has prescribed with food only one time each day. Capsules should not be chewed or crushed.