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GSK公司与Flamel Technologies公司近日联合宣布，美国FDA已批准了一天一次的磷酸卡维地洛缓释片商品名为Coreg CR，用于治疗高血压、中到重度心衰、心脏病发生后心脏泵血能力较弱。
卡维地洛是一种新的第三代β-受体阻滞剂，是一种新型有多种药理活性的药物，具有β和α1，受体阻滞作用，无内源性拟交感活性，高浓度时有钙拮抗作用，且具有明显的抗自由基、抗氧化作用，有调节代谢紊乱、阻止平滑肌细胞增值及抑制心肌细胞凋亡的作用。因此，卡维地洛不仅有较好的降压作用，还能够逆转心血管重构，有利于心力衰竭、心肌梗死、动脉粥样硬化、血管再狭窄等疾病的治疗。
普通片剂每天需服用两次，该药采用Flamel公司的专有技术保证药物有效成分的释放能持续24小时，每天只服用一次能增加患者的依从性，该药将在2007年第一季度正式投放市场。Coreg CR的规格有10 mg、20 mg、40 mg、80 mg。
Generic Name for COREG CR
Carvedilol (as phosphate) 10mg, 20mg, 40mg, 80mg; ext-rel caps.
Legal Classification:
Rx
Pharmacological Class for COREG CR
Noncardioselective β-blocker/α1-blocker.
Manufacturer of COREG CR
GlaxoSmithKline Pharmaceuticals
Indications for COREG CR
Hypertension.
Adult dose for COREG CR
Take with food in the AM. Swallow whole or may open capsules and sprinkle beads on a spoonful of applesauce and take immediately. ≥18yrs: initially 20mg once daily, may double dose every 1–2 weeks if tolerated and needed. Max daily dose of 80mg. Switching from immediate-release carvedilol: see literature. ≥65yrs: switching from highest dose of immediate-release carvedilol (25mg twice daily) to Coreg CR: initially Coreg CR 40mg; if tolerated for ≥2weeks, may increase to 80mg.
Children's dosing for COREG CR
<18 years: not recommended.
Also:
COREG
Contraindications for COREG CR
Cardiogenic shock or decompensated HF requiring intravenous inotropic therapy. Asthma, related bronchospastic conditions. 2nd or 3rd-degree AV block, sick sinus syndrome, or severe bradycardia, unless paced. Severe hepatic impairment.
Warnings/Precautions for COREG CR
Peripheral vascular disease. Nonallergic bronchospasm. Diabetes (monitor blood glucose). Hyperthyroidism. Monitor renal function in ischemic heart disease, diffuse vascular disease, underlying renal insufficiency, and/or if systolic BP <100mmHg. Avoid abrupt cessation. Prinzmetal's angina. Pheochromocytoma. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.
Interactions for COREG CR
May be potentiated by CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone), alcohol (separate by 2 hours). Bradycardia, hypotension with catecholamine depletors (eg, reserpine, MAOIs). Carvedilol levels reduced by rifampin. Increased absorption with cimetidine. Caution with drugs that affect cardiac conduction (esp. diltiazem, verapamil). May potentiate antidiabetic agents. Monitor digoxin, cyclosporine when changing carvedilol dose. Anesthesia.
Adverse Reactions for COREG CR
Bradycardia, orthostatic hypotension, dizziness, nasopharyngitis, GI upset, edema.
How is COREG CR supplied
CR caps—30, 90
Tabs—100
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