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Amiodarone

MCE China：Amiodarone

Brand：MedChemExpress (MCE)

Cat. No.HY-14187

CAS：1951-25-3

Purity：98.32%

Storage：-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

In Vivo：Amiodarone can be used in animal modeling to create pulmonary toxicity and liver injury models. After a single oral dose of Amiodarone in rats, the pharmacokinetic characteristics detectable include an absorption half-life of approximately 1.83 hours and a clearance half-life ranging from 15 hours (at a 100 mg/kg dose) to 105 hours (at a 200 mg/kg dose), with an average oral bioavailability of 39%. Amiodarone is primarily distributed in the lungs, liver, thyroid, and adipose tissue, with drug concentrations in the lungs and adipose tissue being significantly higher than in other tissues. Following long-term oral administration, the accumulation of Amiodarone in adipose tissue is notably increased[3][4][5]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of pulmonary toxicity[4] Background Amiodarone promotes the release of cytokines such as TNF, TGF-β, IL-4, and IL-8 by activating NF-κB, while also enhancing the involvement of natural killer cells in immune regulation. This leads to the release of reactive oxygen species, leukocyte aggregation, and intracellular lipid accumulation, thereby inducing pulmonary damage [4]. Specific Mmodeling Methods Rat: Fischer • male • 9 to 10 weeks oldAdministration: 175 mg/kg • po • once daily, 5 days a week for 12 weeks Note (1) Amiodarone is suspended in a 0.5% methylcellulose solution (HY-125861). (2) The rats are weighed weekly and the drug dose is adjusted if necessary, higher doses of amiodarone could be fatal. Modeling Indicators Histological Changes: The number of macrophages, neutrophils, and lymphocytes in the bronchi and alveoli of rats is significantly increased.Phenotypic Observations: Lung sections of rats show interstitial thickening with accumulation of mononuclear cells, alveoli filled with numerous foamy macrophages, and mild fibrosis. Correlated Product(s): Methyl cellulose (HY-125861) Opposite Product(s): / .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of liver injury[5] Background Amiodarone is metabolized in the liver by the cytochrome P450 3A4 enzyme to produce metabolites such as desethylamiodarone (DEA), leading to mitochondrial dysfunction, increased intracellular oxidative stress, and lipid metabolism disorders, which in turn activate macrophages (Kupffer cells) in the liver, thereby inducing liver injury in mice[5]. Specific Mmodeling Methods Mice: Balb/cCrSlc • male • 8-week-oldAdministration: 1000 mg/kg • po • single dose Note 1. Amiodarone is dissolved in corn oil.2. Prior to oral administration of Amiodarone, pre-treatment with Dexamethasone (HY-14648) was conducted to induce cytochrome P450 3A4 enzyme expression. Dexamethasone was dissolved in corn oil and administered at a dose of 60 mg/kg via intraperitoneal injection once daily for 3 days. Amiodarone was administered orally 24 hours after the final dose of Dexamethasone. Modeling Indicators Molecular Changes: The levels of alanine aminotransferase (ALT) and triglycerides in the plasma of mice are significantly elevated. The release of cytochrome c into the cytosol of liver cells is increased. The ratio of reduced glutathione to oxidized glutathione disulfide in the liver is significantly decreased, indicating increased oxidative stress and reduced cellular antioxidant capacity in the liver. Correlated Product(s): Dexamethasone (HY-14648) Opposite Product(s): /

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References：

[1]. Singh, B.N. and E.M. Vaughan Williams, The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br J Pharmacol, 1970. 39(4): p. 657-67.  [Content Brief]

[2]. Rosenbaum, M.B., et al., Clinical efficacy of amiodarone as an antiarrhythmic agent. Am J Cardiol, 1976. 38(7): p. 934-44.  [Content Brief]

[3]. Plomp TA, et al. Pharmacokinetics and body distribution of amiodarone and desethylamiodarone in rats after oral administration. In Vivo. 1987 Sep-Oct;1(5):265-79.  [Content Brief]

[4]. Wilson BD, et al. Amiodarone-induced pulmonary toxicity in the rat. Lung. 1989;167(5):301-11.  [Content Brief]

[5]. Takai S, et al. Establishment of a mouse model for amiodarone-induced liver injury and analyses of its hepatotoxic mechanism. J Appl Toxicol. 2016 Jan;36(1):35-47.  [Content Brief]