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Amiodarone

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Company Name: Henan DaKen Chemical CO.,LTD.
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Products Intro: Product Name:Amiodarone
CAS:1951-25-3
Purity:99% Package:100g,500g,1KG,10KG,100KG
Company Name: Henan Tianfu Chemical Co.,Ltd.
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Products Intro: CAS:1951-25-3
Purity:99% Package:500G;1KG;5KG;25KG
Company Name: Mainchem Co., Ltd.
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Products Intro: Product Name:Amiodarone
CAS:1951-25-3
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Products Intro: CAS:1951-25-3
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Company Name: Hubei Jusheng Technology Co.,Ltd.
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Products Intro: Product Name:amiodarone
CAS:1951-25-3
Purity:99% Package:5KG;1KG Remarks:C25H29I2NO3
Amiodarone Basic information
Product Name:Amiodarone
Synonyms:(2-butyl-3-benzofuranyl)(4-(2-(diethylamino)ethoxy)-3,5-diidophenyl)methanone;2-butyl-3-(3,5-diiodo-4-(2-diethylaminoethoxy)benzoyl)benzofuran;2-butyl-3-(3,5-diiodo-4-(beta-diethylaminoethoxy)benzoyl)benzofuran;2-butyl-3-(3,5-diiodo-4-(beta-diethylaminoethoxy)-benzoyl)benzofuran;2-butyl-3-(4’-beta-n-diethylaminoethoxy-3’,5’-diiodobenzoyl)benzofuran;2-butyl-3-benzofuranylp-((2-diethylamino)ethoxy)-m,m-diiodophenylketone;2-n-butyl-3’,5’-diiodo-4’-n-diethylaminoethoxy-3-benzoylbenzofuran;Amiodarone Base
CAS:1951-25-3
MF:C25H29I2NO3
MW:645.31
EINECS:217-772-1
Product Categories:CEFOMONIL
Mol File:1951-25-3.mol
Amiodarone Structure
Amiodarone Chemical Properties
density 1.5730 (estimate)
storage temp. 2-8°C
pka6.56(at 25℃)
Stability:Stable. Incompatible with strong oxidizing agents.
CAS DataBase Reference1951-25-3(CAS DataBase Reference)
Safety Information
Hazard Codes Xn
Risk Statements 20/21/22
Safety Statements 36
WGK Germany 3
RTECS OB1361000
MSDS Information
ProviderLanguage
Amiodarone English
Amiodarone Usage And Synthesis
Usesantibacterial
DefinitionChEBI: A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.
Brand nameCordarone (Wyeth-Ayerst).
Biological FunctionsAmiodarone (Cordarone) is an iodine-containing benzofuran derivative identified as a class III agent because it predominantly prolongs action potentials. Amiodarone also blocks sodium and calcium channels and is a noncompetitive β-receptor blocker.Amiodarone is effective for the treatment of most arrhythmias. Toxicity associated with amiodarone has led the U. S. Food and Drug Administration (FDA) to recommend that it be reserved for use in patients with life-threatening arrhythmias.
General DescriptionAmiodarone, 2-butyl-3-benzofuranyl-4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl ketone (Cordarone),was introduced as an antianginal agent. It has very pronouncedclass III action and is especially effective in maintainingsinus rhythm in patients who have been treated bydirect current shock for atrial fibrillation. Like class IIIantiarrhythmic drugs, amiodarone lengthens the effective refractoryperiod by prolonging the action potential duration inall myocardial tissues. Amiodarone is eliminated very slowlyfrom the body, with a half-life of about 25 to 30 days after oraldoses. Although the drug has a broad spectrum of antiarrhythmicactivity, its main limitation is a slow onset of action.Drug action may not be initiated for several days, and thepeak effect may not be obtained for several weeks.
Clinical UseAmiodarone has adverse effects involving many differentorgan systems. It also inhibits metabolism of drugscleared by oxidative microsomal enzymes. It contains iodinein its molecular structure and, as a result, has an effecton thyroid hormones. Hypothyroidism occurs in up to 11%of patients receiving amiodarone. The principal effect isthe inhibition of peripheral conversion of T4 to T3. Serumreverse T3 (rT3) is increased as a function of the dose as wellas the length of amiodarone therapy. As a result, rT3 levelshave been used as a guide for judging adequacy of amiodaronetherapy and predicting toxicity.
Side effectsAmiodarone’s most significant adverse effects include hepatitis, exacerbation of arrhythmias, worsening of congestive heart failure, thyroid dysfunction, and pulmonary fibrosis. Pulmonary fibrosis is frequently fatal and may not be reversed with discontinuation of the drug. Interestingly, despite significant prolongation of the QT interval, the risk of torsades de pointes is relatively low. Patients with underlying sinus node dysfunction tend to have significant worsening of nodal function, frequently requiring pacemaker implantation. Corneal microdeposits develop in most adults receiving amiodarone. As many as 10% of patients complain of halos or blurred vision. The corneal microdeposits are reversible with stoppage of the drug.
Photosensitization occurs in 10% of patients. With continued treatment, the skin assumes a blue-gray coloration. The risk is increased in patients of fair complexion. The discoloration of the skin regresses slowly, if at all, after discontinuation of amiodarone.
Amiodarone inhibits the peripheral and possibly intrapituitary conversion of thyroxine (T4) to triiodothyronine (T3) by inhibiting 5 -deiodination. The serum concentration of T4 is increased by a decrease in its clearance, and thyroid synthesis is increased by a reduced suppression of the pituitary thyrotropin T3. The concentration of T3 in the serum decreases, and reverse T3 appears in increased amounts.Despite these changes, most patients appear to be maintained in an euthyroid state. Manifestations of both hypothyroidism and hyperthyroidism have been reported.
Tremors of the hands and sleep disturbances in the form of vivid dreams, nightmares, and insomnia have been reported in association with the use of amiodarone. Ataxia, staggering, and impaired walking have been noted. Peripheral sensory and motor neuropathy or severe proximal muscle weakness develops infrequently. Both neuropathic and myopathic changes are observed on biopsy. Neurological symptoms resolve or improve within several weeks of dosage reduction.
Safety ProfilePoison by intravenous and intraperitoneal routes. Human systemic effects by ingestion: photosensitivity of the skin. A flammable liquid. When heated to decomposition it emits very toxic fumes of Iand NO,. A coronary vasoddator
Enzyme inhibitorThis photosensitive benzofuran (FWfree-base = 645.32 g/mol; CAS 19774-82- 4 (HCl) ), also known as Nexterone and systematically as (2-{4-[ (2-butyl-1- benzofuran-3-yl) carbonyl]-2,6-diiodophenoxy}ethyl) diethylamine, is a non-selective ion channel blocker and an a- and b-adrenergic receptor agonist and antiarrhythmic agent used for various types of cardiac dysrhythmias, both ventricular and atrial. Key Pharmacokinetic Parameters: See Appendix II in Goodman & Gilman’s THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, 12th Edition (Brunton, Chabner & Knollmann, eds.) McGraw-Hill Medical, New York. Target (s) : Na+ channels; phosphol2+ipase A1; calmodulin-dependent action ; protein kinase C ; Ca channels (6,1+0,1+6); carnitine palmitoyltransferase (I7); K+ channels; Na/K-exchanging ATPase; lysosomal phospholipases; phospholipase A2; phospholipase C; cholestenol D-isomerase, or sterol D7,8-isomerase; phosphatidylglycerol-selective phospholipase A2; retinyl ester hydrolase.
Drug interactionsAmiodarone increases the hypoprothrombinemic response to warfarin (an oral anticoagulant) by reducing its metabolism. Patients receiving digoxin may undergo an increase in serum digoxin concentrations when amiodarone is added to the treatment regimen. Amiodarone interferes with hepatic and renal elimination of flecainide, phenytoin, and quinidine.
PrecautionsAmiodarone is contraindicated in patients with sick sinus syndrome and may cause severe bradycardia and secondand third-degree atrioventricular block. Amiodarone crosses the placenta and will affect the fetus, as evidenced by bradycardia and thyroid abnormalities. The drug is secreted in breast milk.
Amiodarone Preparation Products And Raw materials
Raw materialsDiethyl carbonate-->Salicylaldehyde-->4-Methoxybenzoyl chloride-->Amiodarone hydrochloride
Tag:Amiodarone(1951-25-3) Related Product Information
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