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Carvedilol
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Brand Names: Coreg & Coreg CR
Generic Available
Common Dosage Forms:
Tablets: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg.
Capsules (Coreg CR): 10 mg, 10 mg, 20 mg, 40 mg, and 80 mg.
FDA Indications/Dosages:
For the management of essential hypertension when used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics: Start with 6.25 mg given twice a day. After 7-14 days and using standing systolic pressure one hour after dosing as a guide, increase dosage to 12.5 mg twice a day. Further dosage increases to 25 mg twice a day and may be made after another 7-14 days.
For the treatment of mild to moderate heart failure of ischemic or cardiomyopathic origin, in combination with digitalis, diuretics, and an ACE inhibitor, to reduce the progression of disease: Start with 3.125 mg given twice a day for 14 days. Dose may be doubled every 14 days to the highest level tolerated by the patients. The maximum dose is 25 mg twice a day in patients weighing less than 85 kg and 50 mg twice a day in patients weighing more than 85 kg. Take with food to slow the rate of absorption and decrease orthostatic effects.
For the use in patients with left ventricular dysfunction (LVEF of ≤ 40%) following myocardial infarction: Start treatment after the patient is hemodynamically stable and fluid retention has been minimized. Start with 6.25 mg given twice a day. Increase the dose after 3-10 days to 12.5 mg twice a day and again after 3-10 days to the target dose of 25 mg twice daily. A lower starting dose may be used in patients with low blood pressure or heart rate, or mild fluid retention.
Monitor: BP, LFT, BG.
Pharmacology/Pharmacokinetics: Carvedilol is a nonselective beta-adrenergic blocking agent with alpha-1-adrenergic blocking activity. The mechanism of action of carvedilol in the treatment of hypertension may be due to beta-adrenergic blockage resulting in (1) a reduction in cardiac output, (2) a reduction in exercise- and/or isoproterenol-induced tachycardia and (3) reduces reflex orthostatic tachycardia. In congestive heart failure, carvedilol has been shown to reduce systemic blood pressure, pulmonary artery pressure, pulmonary capillary wedge pressure, systemic vascular resistance, and heart rate while increasing stroke volume index. Mean terminal elimination half-life ranges from 7 to 10 hours. 98% is bound to plasma proteins, mainly albumin. Metabolism occurs primarily by aromatic ring oxidation and glucuronidation.
Drug Interactions: Rifampin significantly decreases plasma levels. Cimetidine increases steady-state AUC but not Cmax. Quinidine, fluoxetine, paroxetine, and propafenone may increase plasma levels. Use with reserpine, clonidine, digoxin, or monoamine oxidase inhibitors may produce significant hypotension or bradycardia. Use with diltiazem or verapamil may cause conduction disturbances. May increase digoxin plasma levels. Use with inhibitors of CYP2C9 (amiodarone or fluconazole) may exacerbate bradycardia.
Contraindication/Precautions: Use is contraindicated in patients with NYHA class IV decompensated cardiac failure requiring intravenous inotropic therapy, bronchial asthma or related bronchospastic conditions, second- or third-degree AV block, sick sinus syndrome, cardiogenic shock, or severe bradycardia. Use with caution in patients with hepatic impairment. Discontinue use at the first sign of hepatic dysfunction (e.g., pruritus, dark urine, anorexia, jaundice, right upper quadrant tenderness, or unexplained flu-like symptoms). Use with caution in patients with peripheral vascular disease (can aggravate symptoms), in diabetics (can mask hypoglycemia), and in thyrotoxicosis (can mask hyperthyroidism). Use with caution during anesthesia (due to bradycardia). Pregnancy Category C.
Adverse Effects: Dizziness (32%), diarrhea (12%), bradycardia and hypotension (9%), hyperglycemia (12%), and visual abnormalities (5%) occur in treatment of congestive heart failure. The same effects occur in the treatment of hypertension but at approximately the same rate as seen in placebo.
Patient Consultation:
Store in a cool, dry place away from sunlight and children.
If a dose is missed, take it as soon as possible. If it is closer to the time of your next dose than the dose you missed, skip the missed dose and return to your dosing schedule. Do not double doses.
Take with food to decrease orthostatic hypotension.
Contact a physician if the above side effects are severe or persistent.
Contact lens wearers may experience decreased lacrimation.
Do not discontinue therapy without first consulting physician. Treatment must be tapered over 1 to 2 weeks.
May cause drowsiness. Use caution while operating machinery or when mental alertness is required.
Patients with diabetes need to be aware that this agent can cause masking of hypoglycemic symptoms.
Avoid nonprescription cough, cold, and allergy medications unless otherwise directed.
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Cardiovascular Drugs Market Positive Long-Term Growth Outlook 2018-2026
Some of the common cardiovascular diseases include hypertensive heart disease, rheumatic heart disease, ischemic heart disease, inflammatory heart disease, and cerebrovascular heart disease. Major problems associated with hypertensive heart disease include angina, hypertrophy, and heart failure. These problems are caused due to high blood pressure in the heart’s arteries and muscles, which causes narrowing of arteries and thickening and enlargement of heart.
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The global cardiovascular drug market is primarily driven by increase in prevalence of heart diseases coupled with rising geriatric population and lifestyle related diseases. In order to cater to this increasing population suffering from cardiovascular diseases, drugs for treatment and prevention for these diseases is required. Rising number of diabetic patients is also expected to be another factor for growth of the global cardiovascular drugs market. According American Diabetes Association, in 2015, 30.3 Americans had diabetes, which is 9.4% of the total U.S population.
Manufacturers in the market are focusing on mergers and acquisition and new product launches, which is positively affecting the market growth. However, stringent drug approval process and side effects of some cardiovascular drugs hamper growth of the global cardiovascular drugs market. Moreover, the patent expiry of various blockbuster drugs is also expected to adversely affect revenue growth of the global cardiovascular drugs market.
According to American Heart Association (AHA), in 2013, cardiovascular diseases accounted for over 17.3 million deaths globally, representing 31% of all global deaths. The global number is expected to rise to 23.6 million by 2030. In 2010, the global burden of cardiovascular diseases was US$ 863 billion, and it is expected to rise to US$1044 billion by 2030. Around 2,200 U.S. citizens die due to cardiovascular diseases, everyday, which is one death in every 40 seconds. Moreover, coronary heart disease accounts for (45.1%) of the total cardiovascular disease, followed by stroke (16.5%), high blood pressure (9.1%), heart failure (8.5%), diseases related to arteries (3.2%), and other cardiovascular diseases in the U.S.
Some of the major players operating in the global cardiovascular drugs market are Pfizer Inc., Bayer AG., Novartis AG., Merck and Co. Inc., AstraZeneca Plc, Bristol Myers Squibb Company, Abbott Laboratories, Sun Pharma Industries, Gilead Sciences Inc., Otsuka Holdings Co., Ltd. Takeda Pharmaceutical Company Ltd, Eli Lilly and Company, and Johnson & Johnson.
Increasing R&D activities to launch new products is expected to support in growth of the cardiovascular drugs market
Regional segmentation of the cardiovascular drugs market by Coherent Market Insights comprises of North America, Latin America, Europe, Asia Pacific, Africa, and Middle East. Global cardiovascular drugs market is oligopolistic in nature with few players holding majority of the share. Various strategies are adopted by key market players such as new product launches, and partnerships in order to retain their market position.
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For instance, in December 2017, Medicure Inc. — a Canada-based pharmaceutical company — through its subsidiary Medicure International Inc., acquired exclusive license for 7 years to market and sell cardiovascular drug for the treatment of primary hyperlipidemia or mixed dyslipidemia in the U.S and its territories. In October 2017, the Sun Pharmaceutical Industries’ subsidiary in the U.S received approval from the U.S Food and Drug Administration (FDA) to sell generic version of its Coreg CR. Coreg CR is used to treat various heart conditions including high blood pressure and heart failure. In August 2017, Takeda Pharmaceutical Company Limited and Cardurion Pharmaceuticals entered into partnership to develop next generation products for the treatment of cardiovascular diseases and heart failure.
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Coherent Market Insights is a prominent market research and consulting firm offering action-ready syndicated research reports, custom market analysis, consulting services, and competitive analysis through various recommendations related to emerging market trends, technologies, and potential absolute dollar opportunity.
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