Metabolite of amiodarone amiodarone. Medical search. Frequent questions

Pacerone (amiodarone HCl) is an antiarrhythmic drug indicated for treatment of recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia only when these conditions have not responded to documented adequate doses of other available antiarrhythmics or when alternative agents could not be tolerated. (rxlist.com)
Amiodarone is a potent antiarrhythmic drug that is used to treat ventricular and supraventricular tachyarrhythmias. (medscape.com)
Amiodarone is the most effective antiarrhythmic drug for atrial and ventricular arrhythmias and the drug of choice for ventricular arrhythmias in an unstable patient. (journalmc.org)
Amiodarone is a commonly used class III antiarrhythmic drug. (medicaltalk.net)

The cationic amphiphilic drug and its major metabolite desethylamiodarone accumulate in hepatocyte lysosomes and mitochondria and in bile duct epithelium. (toxbank.net)

Mild AIT subsides spontaneously in up to 20% of cases upon discontinuation of amiodarone therapy. (medscape.com)
The patient's absolute neutrophil count recovered 3 days after discontinuation of amiodarone. (journalmc.org)

The effects range from abnormal thyroid function test findings to overt thyroid dysfunction, which may be either amiodarone-induced thyrotoxicosis (AIT) or amiodarone-induced hypothyroidism (AIH). (medscape.com)

Elimination half-life is 6 months and the metabolites are excreted in bile. (radiopaedia.org)
de Bruijn V, Behr C, Sperber S, Walk T, Ternes P, Slopianka M, Haake V, Beekmann K, van Ravenzwaay B (2020): Antibiotic-induced changes in microbiome-related metabolites and bile acids in rat plasma. (basf.com)

For example, the analgesic acetaminophen is converted primarily to non-toxic metabolites, but a small amount is converted to a cytototoxic metabolite. (hanstenandhorn.com)
Use of cytochrome P450 3A4 inducers, 3A4 inhibitors, or 2D6 inhibitors with acetaminophen/caffeine/dihydrocodeine bitartrate requires careful consideration of the effects on the parent drug, codeine, and the active metabolite, morphine. (drugs.com)

The reported prevalence of pulmonary toxicity in patients receiving amiodarone is ~10% (range 2-18%) 8 . (radiopaedia.org)
The FDA was reluctant to officially approve the use of amiodarone, since initial reports had shown increased incidence of serious pulmonary side-effects of the drug. (chemeurope.com)
Some of the well-documented side effects of amiodarone are thyroid gland dysregulation, pulmonary fibrosis, and acute liver failure [ 3 ]. (journalmc.org)

As amiodarone can have serious side effects, it is mainly recommended only for significant ventricular arrhythmias. (wikipedia.org)
Amiodarone may be used in the treatment of ventricular tachycardia in certain instances. (wikipedia.org)
Individuals with hemodynamically unstable ventricular tachycardia should not initially receive amiodarone. (wikipedia.org)
Amiodarone can be used in individuals with hemodynamically stable ventricular tachycardia. (wikipedia.org)
Amiodarone is an antiarrhythmic agent (medication used for irregular heart beat) used for various types of tachyarrhythmias (fast forms of irregular heart beat), both ventricular and supraventricular (atrial) arrhythmias. (chemeurope.com)
Based on Singh's work, the Argentinian physician Dr. Mauricio Rosenbaum began using amiodarone to treat his patients who suffered from supraventricular and ventricular arrhythmias, with impressive results. (chemeurope.com)
The patient initially presented with atrial flutter, which was controlled with beta blockers but was switched to amiodarone after 2 weeks when he developed atrial fibrillation with the rapid ventricular response. (journalmc.org)

Amiodarone can worsen the cardiac arrhythmia brought on by digitalis toxicity. (wikipedia.org)
At oral doses of 400 mg per day or higher, amiodarone can have serious, varied side effects, including toxicity to thyroid, liver, lung, and retinal functions, requiring clinical surveillance and regular laboratory testing. (wikipedia.org)
Amiodarone lung refers to the various manifestations of amiodarone toxicity in the lung including acute lung injury , fibrosis, nodules, hemorrhage and pleural disease. (radiopaedia.org)
Foamy alveolar macrophages and cytoplasmic lamellar bodies containing surfactant-like material are typical of amiodarone exposure and do not necessarily indicate clinically significant toxicity. (radiopaedia.org)
Amiodarone shows typical toxicity associated with redox cycling agents: inhibition of electron transport in oxidative phosphorylation plus inhibition of fatty acid β-oxidation, which causes steatosis. (toxbank.net)
Toxicity of amiodarone and amiodarone analogues on isolated rat liver mitochondria. (toxbank.net)
Hepatocellular Toxicity and Pharmacological Effect of Amiodarone and Amiodarone Derivatives The Journal of Pharmacology and Experimental Therapeutics 2006 Vol. 319, No. 3. (toxbank.net)

Amiodarone hydrochloride is a tri-iodinated antiarrhythmic, comprised of 37% iodine by weight and structurally similar to thyroxine, which is widely distributed in adipose tissue, liver, spleen and lung. (radiopaedia.org)

These intracellular metabolites of adenosine are not vasoactive. (globalrph.com)

Some experts recommend revascularization and β-blockade followed by IV antiarrhythmic drugs, such as procainamide or amiodarone, for patients with recurrent or incessant polymorphic VT due to acute myocardial ischemia. (drugs.com)

XI'AN, China , July 27, 2023 /PRNewswire/ - In three recent articles published in the Journal of Pharmaceutical Analysis (JPA), researchers utilize novel techniques for unraveling the metabolism and hepatotoxicity of amiodarone in 3D HepG2 spheroids, exploring plasma proteomics and its translational applications, and investigating the anti-hepatocellular carcinoma efficacy and mechanisms of ginsenoside Rk3. (pharmaceuticalnewswire.com)

Amiodarone contains approximately 37% iodine by weight. (medscape.com)

Pacerone® (Amiodarone HCl) Tablets are a member of a class of antiarrhythmic drugs with predominantly Class III (Vaughan Williams' classification) effects, available for oral administration in 100 mg and 200 mg strengths of amiodarone hydrochloride. (rxlist.com)
Amiodarone hydrochloride, the active ingredient in Pacerone® Tablets, is a benzofuran derivative: 2-butyl-3-benzofuranyl 4-[2-(diethylamino)-ethoxy]-3,5-diiodophenyl ketone hydrochloride. (rxlist.com)
Amiodarone hydrochloride is a white to cream-colored crystalline powder. (rxlist.com)

I. In type thyrotoxicosis, amiodarone should be respected as much rest as the increased risk o autism higher risk category c for information on abvd may be indicated to support these infants may decrease in androgen hormones, surgery, ocular surface and will not improve outcome if there is chapter. (easternpropane.com)

In the ARCH trial, intravenous amiodarone (2 g administered over 2 d) has been shown to reduce the incidence of atrial fibrillation after open heart surgery when compared to placebo. (wikipedia.org)
citation needed] So-called 'acute onset atrial fibrillation', defined by the North American Society of Pacing and Electrophysiology (NASPE) in 2003, responds well to short duration treatment with amiodarone. (wikipedia.org)
citation needed] The benefit of amiodarone in the treatment of atrial fibrillation in the critical care population has yet to be determined but it may prove to be the agent of choice where the patient is hemodynamically unstable and unsuitable for DC cardioversion. (wikipedia.org)

Behr C, Ramirez-Hincapie S, Cameron HJ, Strauss V, Walk T, Herold M, Beekmann K, Rietjens IMCM, van Ravenzwaay B (2018): Impact of lincosamides antibiotics on the composition of the rat gut microbiota and the metabolite profile of plasma and feces. (basf.com)

Amiodarone was first made in 1961 and came into medical use in 1962 for chest pain believed to be related to the heart. (wikipedia.org)
Amiodarone was initially developed in 1961 at the Labaz company, Belgium, by chemists Tondeur and Binon. (chemeurope.com)

Amiodarone has been used both in the treatment of acute life-threatening arrhythmias as well as the long term suppression of arrhythmias. (wikipedia.org)
Based on papers written by Dr. Rosenbaum developing Singh's theories, physicians in the United States began prescribing amiodarone to their patients with potentially life-threatening arrhythmias in the late 1970s. (chemeurope.com)
[4] [5] By 1980, amiodarone was commonly prescribed throughout Europe for the treatment of arrhythmias, but in the U.S. amiodarone remained unapproved by the Food and Drug Administration , and physicians were forced to directly obtain amiodarone from pharmaceutical companies in Canada and Europe. (chemeurope.com)
In December of 1985, amiodarone was approved by the FDA for the treatment of arrhythmias. (chemeurope.com)
Amiodarone has been widely used for the treatment of various arrhythmias. (journalmc.org)

The initial management of AIT involves deciding whether to discontinue amiodarone therapy. (medscape.com)
More than 35% of patients on long-term amiodarone discontinue the drug due to adverse effects [ 2 ]. (journalmc.org)

Amiodarone causes direct cytotoxic effects, indirect immunological damage and causes phospholipid accumulation. (radiopaedia.org)
Furthermore, amiodarone can induce immunological manifestations such as anti-amiodarone antibodies, lupus-like syndrome, immune-mediated thrombocytopenia, Coombs-positive hemolytic anemia (in canines), and vasculitis [ 12 - 17 ]. (journalmc.org)

Amiodarone has been shown to induce steatosis in both animal models and humans. (toxbank.net)

Men getting testosterone supplementation who also got dutasteride a drug usually used to treat an enlarged prostate gland and which blocks the conversion of testosterone to its potent metabolite DHT did not experience a major difference in changes in certain outcomes such as muscle mass, muscle strength, or sexual function in comparison to men who did not receive dutasteride, states study in the March 7 issue of JAMA . (medindia.net)

Cannabidiol inhibits CYP2C19, increasing levels of the active metabolite of clobazam threefold. (cmaj.ca)
Amiodarone inhibits the mitochondrial b-oxidation of fatty acids and produces microvesicular steatosis of the liver in mice. (toxbank.net)

Amiodarone is available in oral and intravenous formulations. (chemeurope.com)

As a cationic ampiphilic compound, amiodarone causes phospholipidosis, with accumulation of lamellar bodies in lipid-rich organs such as lung and liver. (toxbank.net)

Individuals with baseline depressed lung function should be monitored closely if amiodarone therapy is to be initiated. (wikipedia.org)

Amiodarone accumulation increases tissue attenuation due to the iodine content. (radiopaedia.org)

While amiodarone is not approved for AF by the FDA, it is a commonly prescribed off-label treatment due to the lack of equally effective treatment alternatives. (wikipedia.org)
Low TSH levels and elevated free T4 levels are also commonly seen in the early phases of amiodarone therapy and in patients with severe nonthyroidal illness who have euthyroidism and are treated with amiodarone. (medscape.com)

1 , 2 CYP2C9 inhibitors such as cotrimoxazole, fluoxetine and amiodarone would also be expected to increase THC exposure and psychoactive effects. (cmaj.ca)

Most drugs are metabolized to inactive or less active metabolites by enzymes in the liver and intestine. (hanstenandhorn.com)
The mechanism of action of injectable diazepam have active metabolites time to continue exists. (easternpropane.com)

Amiodarone is an antiarrhythmic medication used to treat and prevent a number of types of cardiac dysrhythmias. (wikipedia.org)
Our Pacerone (Amiodarone HCl) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication. (rxlist.com)

Thyroid abnormalities have been noted in up to 14-18% of patients receiving long-term amiodarone therapy. (medscape.com)
Amiodarone causes abnormal liver function test results in 15-50% of patients. (toxbank.net)

They treated the 3D HepG2 spheroids with AMI at different time points, obtaining 15 AMI metabolites involved in N- desethylation, hydroxylation, deiodination, and desaturation metabolic reactions. (pharmaceuticalnewswire.com)

The antiarrhythmic effect of Amiodarone is due to at least two major properties: a prolongation of the myocardial cell action potential duration and refractory period (potassium channel inhibition) and noncompetitive α- and β-adrenergic inhibition. (toxbank.net)

[3] Today the mechanisms of action of amiodarone and sotalol remain unknown. (chemeurope.com)

Cessation of amiodarone and four to twelve months treatment with corticosteroids can arrest progress and often results in resolution of imaging findings over time 3 . (radiopaedia.org)

[6] This makes amiodarone one of the few drugs approved by the FDA without rigorous randomized clinical trials. (chemeurope.com)
Some drugs are converted to toxic metabolites by drug metabolizing enzymes. (hanstenandhorn.com)

Therefore, the measurement of free T3 levels may be helpful in differentiating conditions, because free T3 levels are increased in hyperthyroidism, while they are decreased in early phases of treatment with amiodarone. (medscape.com)

Despite its proven effectiveness, amiodarone has not been adopted widely, owing to frequent adverse events. (journalmc.org)

While amiodarone has been used in shock-refractory cases, evidence of benefit is poor. (wikipedia.org)

Due to the long half-life of amiodarone, oral loading typically takes days to weeks. (chemeurope.com)

Herein, the second case of severe isolated neutropenia associated with the administration of amiodarone is discussed. (journalmc.org)

Amiodarone has been found to have higher efficacy and lower relapse rates compared to placebo and rate-control medications [ 1 ]. (journalmc.org)
Many medications have been implicated as causal agents of neutropenia, but only one case has been reported describing isolated neutropenia induced by amiodarone [ 18 ]. (journalmc.org)

Amiodarone accumulates in type II pneumocytes 5,7 associated with hyperplasia and septal thickening. (radiopaedia.org)

Amiodarone may increase carvedilol levels resulting in further slowing of the heart rate or cardiac conduction. (nih.gov)
Taking fucus vesiculosus with amiodarone might increase the levels of iodine in the blood. (medlineplus.gov)

Once you know these medicines - which include macrolides and quinine and amiodarone - you can put together that list. (naplexstudyguide.com)

Diseases8

Chemicals and Drugs5

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Antiarrhythmic drug4

Desethylamiodarone1

Discontinuation of amiodarone2

Hypothyroidism1

Bile2

Acetaminophen2

Pulmonary3

Ventricular7

Toxicity7

Thyroxine1

Adenosine1

Procainamide1

Hepatotoxicity1

Iodine by weight1

Hydrochloride3

Thyrotoxicosis1

Atrial fibrillation3

20181

19612

Arrhythmias5

Discontinue2

Immunological2

Induce1

Potent1

Inhibits2

Intravenous1

Lamellar bodies1

Lung1

Accumulation1

Commonly2

Exposure1

Active2

Medication2

Patients2

Deiodination1

Inhibition1

Mechanisms1

Findings1

Drugs2

Treatment1

Widely1

Cases1

Days1

Severe1

Medications2

Type1

Levels2

Include1