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Carvedilol
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DRUG INFO
Carvedilol
Drug Name:
Carvedilol
Indication: For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin.
Pharmacology: Carvedilol is a nonselective beta-adrenergic blocking agent with alpha1-blocking activity and is indicated for the treatment of hypertension and mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Carvedilol is a racemic mixture in which nonselective b-adrenoreceptor blocking activity is present in the S(-) enantiomer and a-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol has no intrinsic sympathomimetic activity. The effect of Carvedilol's b-adrenoreceptor blocking activity has been demonstrated in animal and human studies showing that Carvedilol (1) reduces cardiac output in normal subjects; (2) reduces exercise-and/or isoproterenol-induced tachycardia and (3) reduces reflex orthostatic tachycardia.
Mechanism Of Action: Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilols beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca2+ in OH- free radical-treated myocardium. Carvedilol and its metabolites also prevent OH- radical-induced decrease in sarcoplasmic reticulum Ca2+-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage.
Drug Category: Vasodilator Agents; Antihypertensive Agents; Adrenergic Agents; ATC:C07AG02
Brand Names/Synonyms: CHEMBANK1664; Carvedilol; Carvedilol [Usan:Ban:Inn:Jan]; Carvedilolum [Latin]; Coreg; DQ 2466; HSDB 7044
Dosage Forms: TABLET
Absorption: Carvedilol 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.
Interactions:
DrugBank: Interactions for Carvedilol
Interactions for Carvedilol:
(Also see CLINICAL PHARMACOLOGY, Pharmacokinetic Drug-Drug
Interactions.)
Inhibitors of CYP2D6; poor metabolizers of debrisoquin: Interactions of carvedilol with strong
inhibitors of CYP2D6 (such as quinidine, fluoxetine, paroxetine, and propafenone) have not been studied, but these
drugs would be expected to increase blood levels of the R(+) enantiomer of carvedilol . Retrospective analysis of
side effects in clinical trials showed that poor 2D6 metabolizers had a higher rate of dizziness during up-titration,
presumably resulting from vasodilating effects of the higher concentrations of the a-blocking R(+) enantiomer.
Catecholamine-depleting Agents: Patients taking both agents with b-blocking
properties and a drug that can deplete catecholamines (e.g., reserpine and monoamine oxidase inhibitors) should be
observed closely for signs of hypotension and/or severe bradycardia.
Clonidine: Concomitant administration of clonidine with agents with b-blocking properties may potentiate blood-pressure- and heart-rate-lowering effects. When concomitant
treatment with agents with b-blocking properties and clonidine is to be terminated, the
b-blocking agent should be discontinued first. Clonidine therapy can then be discontinued
several days later by gradually decreasing the dosage.
Cyclosporine: Modest increases in mean trough cyclosporine concentrations were observed following
initiation of carvedilol treatment in 21 renal transplant patients suffering from chronic vascular rejection. In
about 30% of patients, the dose of cyclosporine had to be reduced in order to maintain cyclosporine concentrations
within the therapeutic range, while in the remainder no adjustment was needed. On the average for the group, the dose
of cyclosporine was reduced about 20% in these patients. Due to wide interindividual variability in the dose
adjustment required, it is recommended that cyclosporine concentrations be monitored closely after initiation of
carvedilol therapy and that the dose of cyclosporine be adjusted as appropriate.
Digoxin: Digoxin concentrations are increased by about 15% when digoxin and carvedilol are
administered concomitantly. Both digoxin and COREG slow AV conduction. Therefore, increased monitoring of digoxin is
recommended when initiating, adjusting, or discontinuing COREG.
Inducers and Inhibitors of Hepatic Metabolism: Rifampin reduced plasma concentrations of carvedilol
by about 70%. Cimetidine increased AUC by about 30% but caused no change in Cmax.
Calcium Channel Blockers: Isolated cases of conduction disturbance (rarely with hemodynamic
compromise) have been observed when COREG is co-administered with diltiazem. As with other agents with b-blocking properties, if COREG is to be administered orally with calcium channel blockers of the
verapamil or diltiazem type, it is recommended that ECG and blood pressure be monitored.
Insulin or Oral Hypoglycemics: Agents with b-blocking properties may
enhance the blood-sugar-reducing effect of insulin and oral hypoglycemics. Therefore, in patients taking insulin or
oral hypoglycemics, regular monitoring of blood glucose is recommended.
Chemical IUPAC Name: 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Chemical Formula: C24H26N2O4
Half Life: 7-10 hours
Drug Type: Approved Drug
# Accession No: APRD00091
CAS Registry Number: 72956-09-3
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Carvedilol News
(When available)
2005 - the year of recovery for GSK 09 Feb 2006
...for epilepsy/bipolar disorder, climbed 24% to £849 million; Valtrex (valaciclovir), for herpes, was up 21% to £695 million; and Coreg (carvedilol) for heart ... - Pharma Times (subscription),
Caraco Pharmaceutical Laboratories, Ltd. Announces Tentative FDA ... Jan 31, 2006
...today that the US Food and Drug Administration (FDA) have granted tentative approval for the Company's ANDA for the remaining strengths of Carvedilol tablets. ... - PharmaLive.com (press release),
Biovail expects rush of late-stage trials in 2006 Jan 12, 2006
...late-stage trials are its once-daily treatment for chronic pain, Tramadol/NSAID QD combination, targeted for late 2006, and its Carvedilol QD hypertension ... - Reuters Canada,
Generics Erosion will Result in Slow Growth of Market to Treat ... Feb 1, 2006
...finds that recent guidelines recommending more widespread use of beta blockers should spur near- term increased sales of carvedilol, GlaxoSmithKline's Coreg ... - PR Newswire (press release),
Biovail expects flurry of late-stage trials in 2006 Jan 12, 2006
Among the products expected to enter the late-stage trial phase are its Tramadol/NSAID QD combination targeted for late 2006 and its Carvedilol QD targeted for ... - Metro Toronto,
Amiodarone Plus Beta-Blocker Prevents ICD Shocks Jan 11, 2006
...the occurrence of ICD shocks in 412 patients who were randomized to receive amiodarone plus a beta-blocker (either metoprolol, carvedilol, or bisoprolol ... - Medscape (subscription)
Prognosis better for biotechs Jan 14, 2006
That includes its once-daily treatment for chronic pain, Tramadol/NSAID QD combination, targeted for late 2006, and its Carvedilol QD hypertension treatment ... - Metro Toronto,
New Shortage of Diabetes Drug Avandamet And Coreg Jan 12, 2006
DiabeticNews.com, GlaxoSmithKline Plc on Wednesday said it is experiencing a new shortage of its Coreg heart drug and diabetes drug Avandamet in the United States, due to ...
Glaxo Faces Imposed Slowdown In Puerto Rico Jan 13, 2006
New Ratings 0757 GMT [Dow Jones] GlaxoSmithKline (GSK) in focus on talk that supply of heart drug Coreg from a plant in Puerto Rico is being hampered by new procedures ...
UPDATE 1-Glaxo has new shortage of heart, diabetes drugs Jan 11, 2006
Reuters CHICAGO, Jan 11 (Reuters) - GlaxoSmithKline Plc (GSK.L: Quote, Profile, Research) on Wednesday said it is experiencing a new shortage of its Coreg heart drug ...
Glaxo has new shortage of diabetes and heart drugs Jan 11, 2006
Scotsman, CHICAGO (Reuters) - GlaxoSmithKline on Wednesday said it is experiencing a new shortage of its Coreg heart drug and diabetes drug Advandamet in the United ...
Glaxo has new shortage of diabetes and heart drugs Jan 11, 2006
Reuters.uk, CHICAGO (Reuters) - GlaxoSmithKline (GSK.L: Quote, Profile, Research) on Wednesday said it is experiencing a new shortage of its Coreg heart drug and diabetes ...
European Stocks May Decline; BASF and Bayer Might Fall on Oil Jan 12, 2006
Bloomberg The supply of heart drug Coreg from a plant in Puerto Rico is being hampered by new procedures required by the US Food and Drug Administration, which found ...
FTSE heads higher, countering fall in telecoms Jan 12, 2006
Reuters.uk, But rival GlaxoSmithKline (GSK.L: Quote, Profile, Research) dipped 0.4 percent after it said it was experiencing a new shortage of its Coreg heart drug and ...
Bellway, GCap, Virgin, SkyePharma: UK, Irish Equity Preview Jan 12, 2006
Bloomberg GlaxoSmithKline Plc (GSK LN): Europe's biggest drugmaker said the supply of heart drug Coreg from a plant in Puerto Rico is being hampered by new procedures ...
Weak telecoms and drugs hold FTSE near breakeven Jan 12, 2006
Reuters.uk, ...weighted drug firm GlaxoSmithKline (GSK.L: Quote, Profile, Research) dragged on the market as investors fretted over new shortages of its Coreg heart drug and ...
FTSE counters fall in telecoms Jan 12, 2006
Scotsman, But rival GlaxoSmithKline dipped 0.4 percent after it said it was experiencing a new shortage of its Coreg heart drug and diabetes drug Avandamet in the United ...
Drug Supply Shortages Hit GlaxoSmithKline Jan 11, 2006
Forbes Shortages for several drugs such as Coreg, for high blood pressure, Avandamet, for diabetes, and Paxil CR, for depression, were reported this afternoon by ...
Synova Healthcare, Inc. Announces Chief Scientific Officer Jan 4, 2006
PR Newswire (press release), Product Development for SmithKline Beecham Pharmaceuticals (now GlaxoSmithKline), where he worked on several key brands including Tagamet(R), Coreg(R) and ...
Synova Healthcare, Inc. Announces Chief Scientific Officer Jan 4, 2006
Yahoo! News (press release) Development for SmithKline Beecham Pharmaceuticals (now GlaxoSmithKline), where he worked on several key brands including Tagamet®, Coreg® and Hycamtin®. ...
A Quick Guide for using www.medicare.gov Dec 27, 2005
Paynesville Press, ...ill") has heart failure, atrial fibrilation, diabetes, high blood pressure, high cholesterol, glaucoma, and asthma and takes a host of medications: coreg (25 mg ...
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