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Amiodarone
drug data and news
Amiodarone 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 | Amiodarone | ||
| Brand Names/Synonyms | Aminodarone; Amiodarona; Amiodarona [Inn-Spanish]; Amiodarone; Amiodarone Base; Amiodarone Hcl; Amiodarone Hydrochloride; Amiodarone [Usan:Ban:Amiodarons; Amiodarone [Usan:Ban:Inn]; Amiodarons; Amiodaronum [Inn-Latin]; Amiodaronumhydrochloride; Amjodaronum; Base; Cordarone; Cordarone I've.; Cordarone Intravenous; L 3428; L-3428; L. 3428; Labaz; Pacerone; Pms-Amiodarone; Uro-Septra | ||
| Indication | For the treatment of life-threatening recurrent ventricular arrhythmias; Recurrent ventricular fibrillation and Recurrent hemodynamically unstable ventricular tachycardia | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Amiodarone is a member of a new class of antiarrhythmic drugs with predominantly Class III (Vaughan Williams' classification) effects. Amiodarone is indicated in the treatment of recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia. After intravenous administration in man, Amiodarone relaxes vascular smooth muscle, reduces peripheral vascular resistance (afterload), and slightly increases cardiac index. | ||
| Mechanism Of Action | The antiarrhythmic effect of Amiodarone may be due to at least two major properties: 1) a prolongation of the myocardial cell-action potential duration and refractory period and 2) noncompetitive a- and b-adrenergic inhibition. | ||
| Amiodarone News (When available) |
Amiodarone and Sotalol helps prevent shocks from implantable ... Feb 26, 2006 Man dies after Vic blunder Mar 1, 2006 Inadvertent toxic drug reaction in the management of atrial ... Feb 28, 2006 Heat can fix heartbeat Mar 2, 2006 Mild Thyroid Abnormalities Absolved of Heart Risks Feb 28, 2006 Tequin Linked to High Risk of Dangerous Glucose Changes Mar 1, 2006 Articles in PubMed by Author: Feb 20, 2006 Circumferential Pulmonary-Vein Ablation for Chronic Atrial ... Mar 1, 2006 Catheter Ablation Restores Rhythm in 74% of A-Fib Patients Mar 2, 2006 Health Tip: Drugs to Avoid While Breast-Feeding Feb 16, 2006 ICD--The beat goes on Feb 15, 2006 Reply to the Editor Feb 17, 2006 Triiodothyronine in neonatal heart surgery: Looking for an answer Feb 14, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... Feb 9, 2006 Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ... 09 Feb 2006 Amiodarone plus beta blocker prevent shocks from implantable ... Jan 11, 2006 Amiodarone Plus Beta-Blocker Prevents ICD Shocks Jan 11, 2006 Medication Plus Beta-blocker Helps Prevent Shocks From Implantable ... Jan 11, 2006 Medication, Beta-Blocker Helps Prevent Implantable Cardioverter ... Jan 10, 2006 Making a Lifesaving Device Less Painful Jan 10, 2006 Medication Helps Prevent Defibrillator Shocks Jan 11, 2006 St. Jude Medical Announces Publication of OPTIC Clinical Study ... Jan 10, 2006 Cordarone Cuts ICD Shocks, but Side Effects May Outweigh Benefit Jan 10, 2006 'Drugs could reduce defibrillator pain' (11.01.06) Jan 11, 2006 FDA Cautions Consumers Against Filling US Prescriptions Abroad Jan 11, 2006 Baby continues to battle near-fatal health problems 4-month-old ... Jan 22, 2006 Head-To-Head Study Shows More Elderly Patients With Community ... Jan 24, 2006 FDA: Drug Name Confusion Makes Imports Dangerous Jan 16, 2006 FDA Warns of Confusion of Over Foreign Prescription Drug Names Jan 13, 2006 FDA Warns Against Buying Medications Abroad Jan 16, 2006 NWA gets extension to file reorganization plan Jan 11, 2006 Lexiva for the treatment of HIV infection in adults in combination ... Jan 19, 2006 FDA warns against buying prescription drugs on the net or overseas Jan 17, 2006 Drug offers new hope for victims of cardiac arrest Nov 30, 2005 Drug shows promise in keeping cardiac arrest patients alive until ... Nov 30, 2005 Merck/Schering-Plough Announces Update for the IMPROVE-IT Trial Nov 15, 2005 New Anti-Arrhythmic Drug in Development for Atrial Fibrillation ... Nov 22, 2005 Overdose did not kill elderly patient Nov 22, 2005 Medication makes sense if symptoms persist Dec 5, 2005 FDA has approved new indication for Avelox: treatment of ... Dec 6, 2005 Irreversible vision loss due to erectile dysfunction drugs Dec 7, 2005 FDA Approves New Indication for Avelox (moxifloxacin HCl) for ... Nov 30, 2005 FDA Approves Avelox for Abdominal Infections Nov 30, 2005 FDA Approves New Indication for AVELOX(R) (moxifloxacin HCl) for ... Nov 30, 2005 FDA Approves Updated Labeling for LEXIVA Nov 18, 2005 Dronedarone also shown to reduce hospitalizations in a post hoc ... Nov 15, 2005 Boehringer Ingelheim Announces 48-Week Results from Aptivus(R) ... Nov 21, 2005 Heart Health: Ask Dr. Zipes Oct 7, 2005 Topics in Thyroid Disease Sep 12, 2005 Bioniche Reports Fiscal Year-End Results and Unveils Plans to ... Sep 28, 2005 Right ventricular outflow tract resection for treatment of ... Oct 4, 2005 Walgreens accused of drug error Sep 22, 2005 Potential Benefits of Amiodarone for Patients Undergoing Open ... Sep 6, 2005 Autoinduction of tumor necrosis factor-a in FRTL-5 rat thyroid ... Aug 10, 2005 Guidelines for the prevention and management of postoperative ... Aug 16, 2005 An Implantable Cardioverter-Defibrillator but Not Amiodarone ... Jul 24, 2005 Perioperative internal thoracic artery steal syndrome after ... Aug 5, 2005 Uncovering the Cause of Heartbeat Disorder Aug 1, 2005 Study Results Presented on Pharmacokinetics of Once-Daily HIV ... Jul 26, 2005 Drug Name Confusion Can Be Deadly, Says FDA Magazine Jul 19, 2005 | ||
| Dosage Forms | TABLET; LIQUID; SOLUTION | ||
| Drug_Category | Vasodilator Agents; Antiarrhythmic Agents; Enzyme Inhibitors; ATC:C01BD01 | ||
| Absorption | Slow and variable; about 20 to 55% of an oral dose is absorbed | ||
| Interactions |
-->Interactions for Amiodarone: Amiodarone is metabolized to desethylamiodarone by the cytochrome P450 (CYP450) enzyme group, specifically cytochromes P450 3A4 (CYP3A4) and CYP2C8. The CYP3A4 isoenzyme is present in both the liver and intestines. Amiodarone is also known to be an inhibitor of CYP3A4. Therefore, amiodarone has the potential for interactions with drugs or substances that may be substrates, inhibitors or inducers of CYP3A4. While only a limited number of in vivo drug-drug interactions with amiodarone have been reported, chiefly with the oral formulation, the potential for other interactions should be anticipated. This is especially important for drugs associated with serious toxicity, such as other antiarrhythmics. If such drugs are needed, their dose should be reassessed and, where appropriate, plasma concentration measured. In view of the long and variable half-life of amiodarone, potential for drug interactions exists not only with concomitant medication but also with drugs administered after discontinuation of amiodarone. Since amiodarone is a substrate for CYP3A4 and CYP2C8, drugs/substances that inhibit these isoenzymes may decrease the metabolism and increase serum concentration of amiodarone. Reported examples include the following: Protease Inhibitors: Protease inhibitors are known to inhibit CYP3A4 to varying degrees. A case report of one patient taking amiodarone 200 mg and indinavir 800 mg three times a day resulted in increases in amiodarone concentrations from 0.9 mg/L to 1.3 mg/L. DEA concentrations were not affected. There was no evidence of toxicity. Monitoring for amiodarone toxicity and serial measurement of amiodarone serum concentration during concomitant protease inhibitor therapy should be considered. Histamine H2 antagonists: Cimetidine inhibits CYP3A4 and can increase serum amiodarone levels. Other substances: Grapefruit juice given to healthy volunteers increased amiodarone AUC by 50% and Cmax by 84%, resulting in increased plasma levels of amiodarone. Grapefruit juice should not be taken during treatment with oral amiodarone. This information should be considered when changing from intravenous amiodarone to oral amiodarone . Amiodarone may suppress certain CYP450 enzymes, including CYP1A2, CYP2C9, CYP2D6, and CYP3A4. This inhibition can result in unexpectedly high plasma levels of other drugs which are metabolized by those CYP450 enzymes. Reported examples of this interaction include the following: Immunosuppressives: Cyclosporine (CYP3A4 substrate) administered in combination with oral amiodarone has been reported to produce persistently elevated plasma concentrations of cyclosporine resulting in elevated creatinine, despite reduction in dose of cyclosporine. HMG-CoA Reductase Inhibitors: Simvastatin (CYP3A4 substrate) in combination with amiodarone has been associated with reports of myopathy/rhabdomyolysis. Cardiovasculars: Cardiac glycosides: In patients receiving digoxin therapy, administration of oral amiodarone regularly results in an increase in serum digoxin concentration that may reach toxic levels with resultant clinical toxicity. Amiodarone taken concomitantly with digoxin increases the serum digoxin concentration by 70% after one day. On administration of oral amiodarone, the need for digitalis therapy should be reviewed and the dose reduced by approximately 50% or discontinued. If digitalis treatment is continued, serum levels should be closely monitored and patients observed for clinical evidence of toxicity. These precautions probably should apply to digitoxin administration as well. Antiarrhythmics: Other antiarrhythmic drugs, such as quinidine, procainamide, disopyramide, and phenytoin, have been used concurrently with amiodarone. There have been case reports of increased steady-state levels of quinidine, procainamide, and phenytoin during concomitant therapy with amiodarone. Phenytoin decreases serum amiodarone levels. Amiodarone taken concomitantly with quinidine increases quinidine serum concentration by 33% after two days. Amiodarone taken concomitantly with procainamide for less than seven days increases plasma concentrations of procainamide and n-acetyl procainamide by 55% and 33%, respectively. Quinidine and procainamide doses should be reduced by one-third when either is administered with amiodarone. Plasma levels of flecainide have been reported to increase in the presence of oral amiodarone; because of this, the dosage of flecainide should be adjusted when these drugs are administered concomitantly. In general, any added antiarrhythmic drug should be initiated at a lower than usual dose with careful monitoring. Combination of amiodarone with other antiarrhythmic therapy should be reserved for patients with life-threatening ventricular arrhythmias who are incompletely responsive to a single agent or incompletely responsive to amiodarone. During transfer to oral amiodarone, the dose levels of previously administered agents should be reduced by 30 to 50% several days after the addition of oral amiodarone. The continued need for the other antiarrhythmic agent should be reviewed after the effects of amiodarone have been established, and discontinuation ordinarily should be attempted. If the treatment is continued, these patients should be particularly carefully monitored for adverse effects, especially conduction disturbances and exacerbation of tachyarrhythmias, as amiodarone is continued. In amiodarone-treated patients who require additional antiarrhythmic therapy, the initial dose of such agents should be approximately half of the usual recommended dose. Antihypertensives: Amiodarone should be used with caution in patients receiving ß-receptor blocking agents (e.g., propranolol, a CYP3A4 inhibitor) or calcium channel antagonists (e.g., verapamil, a CYP3A4 substrate, and diltiazem, a CYP3A4 inhibitor) because of the possible potentiation of bradycardia, sinus arrest, and AV block; if necessary, amiodarone can continue to be used after insertion of a pacemaker in patients with severe bradycardia or sinus arrest. Anticoagulants: Potentiation of warfarin-type (CYP2C9 and CYP3A4 substrate) anticoagulant response is almost always seen in patients receiving amiodarone and can result in serious or fatal bleeding. Since the concomitant administration of warfarin with amiodarone increases the prothrombin time by 100% after 3 to 4 days, the dose of the anticoagulant should be reduced by one-third to one-half, and prothrombin times should be monitored closely. Some drugs/substances are known to accelerate the metabolism of amiodarone by stimulating the synthesis of CYP3A4 (enzyme induction). This may lead to low amiodarone serum levels and potential decrease in efficacy. Reported examples of this interaction include the following: Antibiotics: Other substances, including herbal preparations: Other reported interactions with amiodarone: Sinus bradycardia has been reported with oral amiodarone in combination with lidocaine (CYP3A4 substrate) given for local anesthesia. Seizure, associated with increased lidocaine concentrations, has been reported with concomitant administration of intravenous amiodarone. Dextromethorphan is a substrate for both CYP2D6 and CYP3A4. Amiodarone inhibits CYP2D6. Cholestyramine increases enterohepatic elimination of amiodarone and may reduce its serum levels and t1/2. Disopyramide increases QT prolongation which could cause arrhythmia. Fluoroquinolones, macrolide antibiotics, and azoles are known to cause QTc prolongation. There have been reports of QTc prolongation, with or without TdP, in patients taking amiodarone when fluoroquinolones, macrolide antibiotics, or azoles were administered concomitantly. Hemodynamic and electrophysiologic interactions have also been observed after concomitant administration with propranolol, diltiazem, and verapamil. Volatile Anesthetic Agents:. In addition to the interactions noted above, chronic (> 2 weeks) oral Cordarone administration impairs metabolism of phenytoin, dextromethorphan, and methotrexate. Electrolyte Disturbances Patients with hypokalemia or hypomagnesemia should have the condition corrected whenever possible before being treated with Cordarone I.V., as these disorders can exaggerate the degree of QTc prolongation and increase the potential for TdP. Special attention should be given to electrolyte and acid-base balance in patients experiencing severe or prolonged diarrhea or in patients receiving concomitant diuretics. | ||
| Toxicity | LD50=3 g/kg (oral, rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | (2-butylbenzofuran-3-yl)-[4-(2-diethylaminoethoxy)-3,5-diiodo-phenyl]-methanone | ||
| Chemical Formula | C25H29I2NO3 | ||
| Molecular Weight | 645.312 g/mol | ||
| Smiles String | CCCCC1=C(C2=CC=CC=C2O1)C(=O)C3=CC(=C(C(=C3)I)OCCN(CC)CC)I | ||
| Melting Point | Not Available | ||
| Water Solubility | 50 mg/mL (chloride salt) | ||
| State | Solid | ||
| LogP/Hphobicity | 7.706 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Primarily hepatic via CYP2C8, one active metabolite (desethylamiodarone) | ||
| Half Life | 58 days (range 15-142 days) | ||
| Protein Binding [%] | >96% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Amiodarone.html http://www.rxlist.com/cgi/generic/amiodarone.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00288 | ||
| CAS Registry Number | 1951-25-3 | ||
| KEGG Compound ID | C06823 | ||
| PubChem ID | SID:9041 | ||
| PharmGKB ID | PA448383 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2243836 |
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