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Carvedilol
drug data and news
Carvedilol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Carvedilol | ||
| Brand Names/Synonyms | CHEMBANK1664; Carvedilol; Carvedilol [Usan:Ban:Inn:Jan]; Carvedilolum [Latin]; Coreg; DQ 2466; HSDB 7044 | ||
| Indication | For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Carvedilol News (When available) |
Mylan Announces Tentative Approval for Carvedilol Tablets Feb 23, 2006 GSK plans to launch cardio drug after July Mar 1, 2006 GSK plans to roll out cardio drug after July Mar 1, 2006 Mylan gets nod for Coreg generic Feb 24, 2006 Restarting hearts of all ages Feb 15, 2006 Wrap up: Sensex adds 61 points Mar 2, 2006 Glaxo pops growth pill Feb 13, 2006 Mylan gets tentative FDA OK for Coreg Feb 23, 2006 probe points to two execs Feb 23, 2006 Myocarditis During Clozapine Treatment Feb 14, 2006 GSK posts 79% growth in Q4 net to Rs 42 cr Feb 14, 2006 2005 - the year of recovery for GSK Feb 9, 2006 Generics Erosion will Result in Slow Growth of Market to Treat ... Feb 1, 2006 2005 - the year of recovery for GSK 09 Feb 2006 Caraco Pharmaceutical Laboratories, Ltd. Announces Tentative FDA ... Jan 31, 2006 Biovail expects rush of late-stage trials in 2006 Jan 12, 2006 Generics Erosion will Result in Slow Growth of Market to Treat ... Feb 1, 2006 Biovail expects flurry of late-stage trials in 2006 Jan 12, 2006 Amiodarone Plus Beta-Blocker Prevents ICD Shocks Jan 11, 2006 Prognosis better for biotechs Jan 14, 2006 Carvedilol, a cardiovascular drug, may improve heart failure and ... Dec 2, 2005 Wyeth’s President, Research & Development, Wyeth Pharmaceuticals ... Dec 9, 2005 Cardiovascular drug may improve heart failure and help prevent ... Nov 16, 2005 Ranbaxy starts Canadian operations Sep 22, 2005 Best Treatments: Managing Heart Failure Sep 24, 2005 Generic giant moves in from India Sep 23, 2005 Ranbaxy Launches in Canada Sep 22, 2005 Strategies to Prevent Type 2 Diabetes Aug 12, 2005 Flamel loses another Micropump contract Sep 6, 2005 Sports Icons Visit Indianapolis to Help Residents Get 'Back in ... Jul 20, 2005 Kopran puts 7 brands on block Jun 27, 2005 Wanbury Ltd (Originally Pearl Organics) Jun 28, 2005 Blood Pressure Control and Prevention of Chronic Kidney Disease Jun 15, 2005 Flamel CEO under fire by rebel shareholders Jun 13, 2005 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Vasodilator Agents; Antihypertensive Agents; Adrenergic Agents; ATC:C07AG02 | ||
| 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 |
-->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. | ||
| Toxicity | Not expected to be toxic following ingestion. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol | ||
| Chemical Formula | C24H26N2O4 | ||
| Molecular Weight | 406.474 g/mol | ||
| Smiles String | COC1=CC=CC=C1OCCNCC(COC2=CC=CC3=C2C4=CC=CC=C4N3)O | ||
| Melting Point | 114-115 °C | ||
| Water Solubility | Practically insoluble in water | ||
| State | Solid | ||
| LogP/Hphobicity | 4.463 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. Demethylation and hydroxylation at the phenol ring produce three active metabolites with b-receptor blocking activity. The 4'-hydroxyphenyl metabolite is approximately 13 times more potent than carvedilol for b-blockade. | ||
| Half Life | 7-10 hours | ||
| Protein Binding [%] | 98% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Carvedilol.html http://www.rxlist.com/cgi/generic3/carvedilol.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00091 | ||
| CAS Registry Number | 72956-09-3 | ||
| KEGG Compound ID | C06875 | ||
| PubChem ID | SID:189887 | ||
| PharmGKB ID | PA448817 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2252317 |
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