Coreg is a product of GlaxoSmithKline. 

Coreg received U.S. Food and Drug Administration (FDA) approval in 1995. 

Note: World-drugs.net sells generic version of Coreg

GlaxoSmithKline (GSK) is a premier research-based pharmaceutical company with a powerful combination of skills and resources that provides a platform for delivering strong growth in today's rapidly changing healthcare environment.

GSK's aim is to improve the quality of human life by enabling people to do more, feel better and live longer.

GlaxoSmithKline is centered in the UK and has operations based in the US ; the new company is one of the industry leaders, with an estimated seven per cent of the world's pharmaceutical market.

GSK also has leadership in four major therapeutic areas - anti-infectives, central nervous system (CNS), respiratory and gastro-intestinal/metabolic. In addition, it is a leader in the important area of vaccines and has a growing portfolio of oncology products.

GSK also has a Consumer Healthcare portfolio comprising over-the-counter (OTC) medicines; oral care products and nutritional healthcare drinks, all of which are among the market leaders. 

3. ABOUT COREG MEDICATION

What is High Blood Pressure (Hypertension)?

High blood pressure, also known as hypertension, is a serious illness affecting your heart and blood vessels. It occurs when the blood exerts too much pressure against the walls of the blood vessels. In fact, that is what the term hypertension means: "too much" (hyper) "pressure" (tension). It affects upwards of 58 million people nationwide.

High blood pressure is risky because it places you at risk for certain life threatening and disabling conditions. If left untreated, high blood pressure could lead to heart attack, kidney disease, and/or stroke.

This happens because as your blood continuously exerts too much pressure against the walls of the blood vessels, it places extra stress on the heart and blood vessels.

Blood pressure is measured in two numbers, systolic (top or higher number) and diastolic (lower number). The higher number is the maximum pressure, which occurs when the heart beats (systole), and the lower number is the lowest pressure measured when the heart relaxes between beats (diastole), just before the next contraction. A systolic reading of 140 or greater and a diastolic reading of 90 or greater is considered high.

The normal blood pressure is less than 120/80. In fact, for every 20/10 increase in blood pressure, your risk of cardiovascular events, such as heart attack or stroke, is DOUBLED.

High blood pressure is also called the "silent killer" because the symptoms are rarely seen or felt. So, even though it might be upsetting to be told that you have high blood pressure, it's good that your doctor has discovered it. Treatment can help avoid the serious, long-term effects of high blood pressure.

What are antihypertensives?

Antihypertensives are medicines used to treat hypertension or high blood pressure. Although some patients do not need to take medication to control their high blood pressure, anyone who is prescribed medication needs to take it exactly as prescribed to avoid the serious medical problems associated with the condition. People taking Antihypertensives are also encouraged to make healthy lifestyle changes, such as quitting smoking, losing weight and getting regular exercise. Furthermore, they are encouraged to speak with their physician before taking any prescription medications, such as narcotics, or over-the-counter medications, such as diet pills.

Finally, people with high blood pressure are urged to be patient as the type and level of their medication are adjusted for optimal results. This is especially important because the vast majority of patients have no symptoms, making hypertension the silent killer.

There are a wide variety of Antihypertensives and combinations of different medications that are available, and it may take some time before the ideal treatment has been found and finely tuned to the patients needs.

Antihypertensives include:

Diuretics ("water pills")
Diuretics are sometimes called "water pills" because they work in the kidney and flush excess water and sodium from the body.

Beta Blockers
Beta-blockers reduce nerve impulses to the heart and blood vessels. This makes the heart beat slower and with less force. Blood pressure drops and the heart works less hard.

Some common beta-blockers include:

• Acebutolol
• Atenolol
• Betaxolol
• Bisoprolol
• Carvedilol
• Metoprolol
• Nadolol
• Penbutolol
• Pindolol
• Propranolol
• Timolol

Coreg blocks beta-receptors in the heart, which causes the heart to beat more slowly and with less force. This means that the heart uses less effort and so requires less oxygen from the blood. The pain of angina is caused by not enough oxygen reaching the heart when it's workload is increased, eg during exercise. Coreg prevents this pain by decreasing the oxygen demand of the heart, so that it always has a sufficient supply.

Due to the heart beating more slowly and with less force, the pressure at which blood is pumped out of the heart to the rest of the body is reduced. This is one way in which Coreg reduces blood pressure.

Coreg also blocks receptors called alpha-receptors that are present on the walls of blood vessels. Blocking these receptors causes the blood vessels to widen, which means that there is more space and less resistance in the blood vessels. This is another mechanism by which the pressure in the blood vessels is lowered.

The widened blood vessels also allow more blood to reach the heart, which is another way in which Coreg prevents the pain of angina.

Alpha Blockers
Alpha-blockers reduce nerve impulses to blood vessels, which allows blood to pass more easily, causing the blood pressure to go down.

Alpha-Beta Blockers
Alpha-beta-blockers work the same way as alpha-blockers but also slow the heartbeat, as beta-blockers do. As a result, less blood is pumped through the vessels and the blood pressure goes down.

Nervous System Inhibitors
Nervous system inhibitors relax blood vessels by controlling nerve impulses. This causes the blood vessels to become wider and the blood pressure to go down.

Angiotensin Converting Enzyme (ACE) Inhibitors
Angiotensin converting enzyme (ACE) inhibitors prevent the formation of a hormone called angiotensin II, which normally causes blood vessels to narrow. The ACE inhibitors cause the vessels to relax and blood pressure goes down.

Calcium Channel Blockers
CCBs keep calcium from entering the muscle cells of the heart and blood vessels. This causes the blood vessels to relax and pressure goes down.

Angiotensin Receptor Blockers (formal medical name angiotensin-2-receptor antagonists, known as "sartans" for short). These agents are sometimes prescribed together, for instance an ACE inhibitor along with a calcium channel blocker.

Angiotensin antagonists shield blood vessels from angiotensin II. As a result, the vessels become wider and blood pressure goes down. 

4.COREG EFFECTIVENESS
(When is Coreg best taken?)

Coreg is rapidly and extensively absorbed following oral administration, with absolute bioavailability of approximately 25% to 35% due to a significant degree of first-pass metabolism. Following oral administration of Coreg dose, the apparent mean terminal elimination half-life of Coreg generally ranges from 7 to 10 hours. Plasma concentrations achieved are proportional to the oral Coreg dose administered. When administered with food, the rate of absorption is slowed, as evidenced by a delay in the time to reach peak plasma levels, with no significant difference in extent of bioavailability. Taking Coreg with food should minimize the risk of orthostatic hypotension.

Coreg is extensively metabolized. Following oral administration of radiolabelled Coreg to healthy volunteers, Coreg accounted for only about 7% of the total radioactivity in plasma as measured by area under the curve (AUC). Less than 2% of the dose was excreted unchanged in the urine. Coreg is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. The metabolites of Coreg are excreted primarily via the bile into the feces. Demethylation and hydroxylation at the phenol ring produce 3 active metabolites with b-receptor blocking activity. Based on preclinical studies, the 4'-hydroxyphenyl metabolite is approximately 13 times more potent than carvedilol for b-blockade. 

5.COREG EFFECTS ON SPECIAL POPULATION
(How do different people react to Coreg?)

Pregnancy
Coreg belongs to pregnancy Category C. Studies performed in pregnant rats and rabbits given carvedilol revealed increased post-implantation loss in rats at doses of 300 mg/kg/day (50 times the MRHD as mg/m2) and in rabbits at doses of 75 mg/kg/day (25 times the MRHD as mg/m2). In the rats, there was also a decrease in fetal body weight at the maternally toxic dose of 300 mg/kg/day (50 times the MRHD as mg/m2), which was accompanied by an elevation in the frequency of fetuses with delayed skeletal development (missing or stunted 13th rib). In rats the no-observed-effect level for developmental toxicity was 60 mg/kg/day (10 times the MRHD as mg/m2); in rabbits it was 15 mg/kg/day (5 times the MRHD as mg/m2). There are no adequate and well-controlled studies in pregnant women. Coreg should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers
It is not known whether Coreg is excreted in human milk. Studies in rats have shown that Coreg and/or its metabolites cross the placental barrier and are excreted in breast milk.

Pediatric Use
Safety and efficacy of Coreg in patients younger than 18 years have not been established.

Geriatric Use
Of the 765 patients with congestive heart failure randomized to Coreg in US clinical trials, 31% (235) were 65 years or older, and 7.3% (56) were 75 years or older. Of the 1,156 patients randomized to Coreg in a long-term, placebo-controlled trial in severe heart failure, 47% (547) were 65 years or older, and 15% (174) were 75 years or older. Of 3,025 patients receiving Coreg in congestive heart failure trials worldwide, 42% were 65 years or older.

Of the 2,065 hypertensive patients in US clinical trials of efficacy or safety who were treated with Coreg, 21% (436) were 65 years or older. Of 3,722 patients receiving Coreg in hypertension clinical trials conducted worldwide, 24% were 65 years or older. With the exception of dizziness in hypertensive patients (incidence 8.8% in the elderly vs. 6% in younger patients), no overall differences in the safety or effectiveness were observed between the older subjects and younger subjects in each of these populations. Similarly, other reported clinical experience has not identified differences in responses between the elderly and younger subjects, but greater sensitivity of some older individuals cannot be ruled out.

Elderly: Plasma levels of Coreg average about 50% higher in the elderly compared to young subjects. 

6.COREG EFFECTS ON MEDICAL CONDITIONS
(How does Coreg affect your existing condition/ailment?)

Hepatic Impairment: Compared to healthy subjects, patients with cirrhotic liver disease exhibit significantly higher concentrations of Coreg (approximately 4- to 7-fold) following single-dose therapy.

Renal Insufficiency: Although Coreg is metabolized primarily by the liver, plasma concentrations of Coreg have been reported to be increased in patients with renal impairment. Based on mean AUC data, approximately 40% to 50% higher plasma concentrations of Coregwere observed in hypertensive patients with moderate to severe renal impairment compared to a control group of hypertensive patients with normal renal function. However, the ranges of AUC values were similar for both groups. Changes in mean peak plasma levels were less pronounced, approximately 12% to 26% higher in patients with impaired renal function.

Consistent with its high degree of plasma protein binding, Coreg does not appear to be cleared significantly by hemodialysis. 

7.OTHER/ALTERNATE USES OF COREG
What else does Coreg treat?

Coreg also reduces the force of heart muscle contraction and lowers blood pressure. By reducing the heart rate and the force of muscle contraction, Coreg reduces heart muscle oxygen demand. Since angina occurs when oxygen demand of the heart exceeds supply,

Coreg is helpful in treating angina

8.ADVERSE/SIDE EFFECTS of COREG
What are the side effects of Coreg?

Coreg has been evaluated for safety in patients with congestive heart failure (mild, moderate, and severe heart failure), in patients with left ventricular dysfunction following myocardial infarction and in hypertensive patients. The observed adverse event profile was consistent with the pharmacology of the drug and the health status of the patients in the clinical trials. Adverse events reported for each of these patient populations are provided below. Excluded are adverse events considered too general to be informative, and those not reasonably associated with the use of the drug because they were associated with the condition being treated or are very common in the treated population. Rates of adverse events were generally similar across demographic subsets (men and women, elderly and non-elderly, blacks and non-blacks).

Congestive Heart Failure

Coreg has been evaluated for safety in congestive heart failure in more than 4,500 patients worldwide of which more than 2,100 participated in placebo-controlled clinical trials. Approximately 60% of the total treated population in placebo-controlled clinical trials received Coreg for at least 6 months and 30% received Coreg for at least 12 months.

Table below shows adverse events reported in patients with mild-to-moderate heart failure enrolled in US placebo-controlled clinical trials.

Cardiac failure and dyspnea were also reported in these studies, but the rates were equal or greater in patients who received placebo.

The following adverse events were reported with a frequency of >1%

Body as a Whole : Allergy, malaise, hypovolemia, fever, leg edema.

Cardiovascular : Fluid overload, postural hypotension, aggravated angina pectoris, AV block, palpitation, hypertension.

Central and Peripheral Nervous System : Hypesthesia, vertigo, paresthesia.

Gastrointestinal : Melena, periodontitis. 

Liver and biliary System: SGPT increased, SGOT increased

Metabolic and Nutritional: Hyperuricemia, hypoglycemia, hyponatremia, increased alkaline phosphatase, glycosuria, hypervolemia, diabetes mellitus, GGT increased, weight loss, hyperkalemia, creatinine increased.

Musculoskeletal : Muscle cramps.

Platelet, Bleeding and Clotting : Prothrombin decreased, purpura, thrombocytopenia.

Psychiatric : Somnolence.

Reproductive, male: Impotence.

Special Senses: Blurred vision.

Urinary System : Renal insufficiency, albuminuria, hematuria.