Propafenone
(Synonyms: SA-79) 目录号 : GC25786Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
Cas No.:54063-53-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
Application of 10 µM propafenone decreases the Kv currents by 51%, as measured at +60 mV.[2]
[1] H M Bryson, et al. Drugs. 1993 Jan;45(1):85-130. [2] An JR, et al. Korean J Physiol Pharmacol. 2018 Sep;22(5):597-605.
| Cas No. | 54063-53-5 | SDF | Download SDF |
| 别名 | SA-79 | ||
| 分子式 | C21H27NO3 | 分子量 | 341.44 |
| 溶解度 | DMSO: 68 mg/mL (199.16 mM);Water: Insoluble;Ethanol: 41 mg/mL (120.08 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9288 mL | 14.6439 mL | 29.2877 mL |
| 5 mM | 0.5858 mL | 2.9288 mL | 5.8575 mL |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9288 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias
Drugs 1993 Jan;45(1):85-130.PMID:7680987DOI:10.2165/00003495-199345010-00008.
Propafenone is an orally active sodium channel blocking agent with beta-adrenoceptor antagonist and weak calcium antagonist activity. The pharmacokinetic profile of Propafenone is complex, characterised as typically nonlinear, saturable, stereoselective and dependent on both dose and debrisoquin metaboliser phenotype; individualised dosage titration is required. Both placebo- and drug-controlled studies have confirmed the efficacy of Propafenone in the treatment of premature ventricular complexes, ventricular couplets and nonsustained ventricular tachycardia; in a large meta-analysis, Propafenone together with amiodarone, flecainide and encainide were significantly more effective in the control of ventricular ectopy than other antiarrhythmic agents. However, the use of Propafenone in these indications, like that of other antiarrhythmic agents, is likely to be limited to patients with a favourable risk-to-benefit ratio. Propafenone has also demonstrated efficacy in the treatment of malignant ventricular arrhythmias (ventricular fibrillation and sustained ventricular tachycardia); preliminary mortality data obtained with Propafenone have been encouraging in this patient group. In addition, Propafenone has a favourable noncardiac tolerability profile and beta-adrenoceptor antagonist activity, which may offer advantages in some specific patient groups. The area of research concerning Propafenone which has shown the greatest expansion over the past 5 years is in the treatment of supraventricular arrhythmias. Propafenone has marked efficacy in patients with Wolff-Parkinson-White syndrome and has been recommended as a first-line prophylactic agent in those with rapid anterograde conduction. Propafenone is also effective in the conversion of atrial fibrillation to sinus rhythm, although comparative studies are required to determine advantages over more established agents. Propafenone use has been successfully extended to children with limited data demonstrating consistent efficacy in the control of junctional ectopic tachycardia. As with all antiarrhythmic agents, Propafenone has the potential to induce arrhythmias. Comparative studies are required to assess in more detail the cardiac tolerability profile of Propafenone against other class Ic agents. In conclusion, Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias, although its use in patients with potentially malignant arrhythmias will remain limited for the present. Due to its unique pharmacodynamic profile, Propafenone deserves consideration as an individual agent.
Propafenone: a new antiarrhythmic agent
Clin Pharm 1988 Dec;7(12):869-77.PMID:3061720doi
The chemical and pharmacologic properties, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, and dosage of Propafenone are reviewed. Propafenone is a class IC antiarrhythmic agent that is structurally similar to the beta blockers but that has only weak beta-blocking and calcium-channel-blocking activity. It is well absorbed after oral administration, but systemic bioavailability is only 12% after a 300-mg dose. Among extensive metabolizers (greater than 90% of the United States population), bioavailability seems to vary nonlinearly with dose and increases substantially with food; these effects are not seen in poor metabolizers. Elimination is primarily hepatic, with a mean elimination half-life after oral administration of 5.5 hours in extensive metabolizers and 17.2 hours in poor metabolizers. The relationship between plasma Propafenone concentration and clinical response varies considerably among individual patients; therefore, plasma concentrations have limited usefulness in predicting efficacy or electrophysiologic effects. Propafenone is effective in treating ventricular tachycardia and in suppressing premature ventricular complexes (PVCs). It is less effective in the treatment of refractory ventricular tachycardia. Concurrent administration of digoxin, warfarin, or metoprolol with Propafenone has been shown to increase the serum concentrations of those three drugs, while cimetidine slightly increases the Propafenone concentrations. Additive pharmacologic effect can occur when lidocaine, procainamide, and quinidine are combined with Propafenone. Overall, 21% to 32% of patients experience adverse effects, with 3% to 7% of these serious enough to warrant discontinuing therapy. The most common adverse effects are dizziness or lightheadedness, metallic taste, and nausea and vomiting; the most serious adverse effects are proarrhythmic events.(ABSTRACT TRUNCATED AT 250 WORDS)
Propafenone: a novel type Ic antiarrhythmic agent
DICP 1989 Mar;23(3):196-202.PMID:2655298DOI:10.1177/106002808902300301.
Propafenone is an investigational type Ic anti-arrhythmic agent that markedly slows conduction velocity in all cardiac tissues. Propafenone also possesses weak beta- and calcium-channel blocking properties. The bioavailability of Propafenone is dose-dependent. Hepatic metabolism of this agent is polymorphic and appears to correlate with the ability of the liver to oxidize debrisoquin sulfate. Propafenone is effective in suppressing spontaneous ventricular ectopy; however, the drug may be less effective in patients with sustained ventricular tachycardia or ventricular fibrillation when evaluated using programmed stimulation. Propafenone is also useful in the treatment of supraventricular tachycardias including atrioventricular (AV) nodal reentrant tachycardia, AV reentrant tachycardia associated with the Wolff-Parkinson-White syndrome, and atrial fibrillation. Adverse reactions seen with Propafenone affect the gastrointestinal, central nervous, and cardiovascular systems. Comparative studies with currently available type Ic agents are needed to better define Propafenone's place in therapy.
Propafenone in the treatment of cardiac arrhythmias. A risk-benefit appraisal
Drug Saf 1995 Jan;12(1):55-72.PMID:7741984DOI:10.2165/00002018-199512010-00005.
Propafenone is a potent antiarrhythmic agent effective in either supraventricular or ventricular tachyarrhythmias. For proper utilisation, some important pharmacological aspects must be considered, such as nonlinear pharmacokinetics, inability in some patients (poor debrisoquine metabolisers) to oxidise the drug in the liver, existence of at least one active metabolite (5-hydroxy-propafenone) and ability to exert a slight beta-blocking activity. Like all the other antiarrhythmic drugs, Propafenone may be associated with adverse effects and may exert proarrhythmic effects. For this reason, its usage must be based on a careful analysis of the risk-benefit ratio, by considering the patient's profile as well as the characteristics of the arrhythmia and its prognostic significance. Propafenone appears to be very effective, and has a favourable risk-benefit profile in the treatment of all supra-ventricular arrhythmias. Particularly, it is effective in converting atrial fibrillation to sinus rhythm and in preventing atrial fibrillation recurrences, and is very effective in the pharmacological control of the arrhythmias of the Wolff-Parkinson-White syndrome. Propafenone is also effective in suppressing ventricular premature complexes and nonsustained ventricular tachycardias. However, because of potential proarrhythmic effects, its use in these arrhythmias must be considered after a careful analysis of the risk-benefit profile, which could be favourable in some patients, but less favourable in others (e.g. patients with coronary artery disease and ventricular dysfunction). In malignant ventricular arrhythmias, further studies are needed to define the limitations of antiarrhythmic drugs in comparison with non-pharmacological treatments, mainly cardioverter/defibrillators. At present, like the other class I antiarrhythmic agents, Propafenone does not seem to be a first choice prophylactic agent for malignant ventricular arrhythmias, although more data from controlled studies are needed.
Propafenone-theophylline interaction
Pharmacotherapy 1993 Jan-Feb;13(1):68-71.PMID:8437970doi
A 63-year-old man with ventricular tachycardia (VT) refractory to drug therapy was admitted for surgical ablation of the VT with coronary artery bypass graft surgery. He developed increased theophylline concentrations with decreased calculated theophylline clearance after Propafenone therapy for recurrent VT was initiated. Within 1 day after the addition of Propafenone 150 mg every 8 hours to a drug regimen that included theophylline sustained-release tablets 300 mg every 12 hours, the patient demonstrated increased theophylline serum concentrations and decreased calculated theophylline clearance. Despite a decrease in theophylline dosage, theophylline concentrations continued to rise as the dosage of Propafenone was increased to 300 mg every 8 hours. Theophylline was discontinued due to a rising theophylline level, improved oxygenation, and absence of wheezing. Both Propafenone and theophylline are hepatically metabolized by the cytochrome P-450 enzyme system. The decrease in theophylline clearance of 25% to 69% in this patient may be due to competitive metabolism resulting in enzyme inhibition and increased theophylline concentrations. Since Propafenone and 5-OH-propafenone levels were not measured, it is unknown whether Propafenone clearance was affected as well. Health care practitioners should be aware of this possible drug interaction and monitor theophylline concentrations and the electrocardiogram closely if the agents are coadministered.