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Tambocor（醋酸氟卡尼片/注射剂）

2015-12-11 03:57:46 作者：新特药房来源：互联网浏览次数：0 文字大小：【大】【中】【小】

简介： 5月13日，日本卫材制药生产的抗心律失常药Tambocor(氟卡尼，flecainide)在日本获得批准用于儿童心律不齐患者。Tambocor目前用于治疗成人的阵发性房颤、阵发性室上性心动过速和室性心动过速。儿童心律不齐 ...

关键字：醋酸氟卡尼片/注射剂 flecainide 商品名Tambocor 抗心律失常药

5月13日，日本卫材制药生产的抗心律失常药Tambocor(氟卡尼，flecainide)在日本获得批准用于儿童心律不齐患者。Tambocor目前用于治疗成人的阵发性房颤、阵发性室上性心动过速和室性心动过速。
儿童心律不齐通常会引起心悸、眩晕气短和其他症状，严重影响儿童的日常生活，也是导致儿童心源性猝死的主要原因。Tambocor片剂在日本是第一个批准用于治疗儿童心律不齐的药物，将有助于缓解儿童心律不齐治疗药物
治疗类别名称
快速性心律失常的治疗剂
适应症　　
适用于室上性心动过速，房室结或房室折返心动过速，心房颤动，儿童顽固性交界性心动过速及伴有应激综合征者，对其他抗心律失常药无效的病例，氟卡胺常有效．
适用于治疗室性早搏、室性心动过速、房室结内折返性心动过速、预激综合征伴室上性心动过速、未控制的心房颤动伴快速室率。本品具有高效、强效、广谱的特点，其疗效优于奎尼丁、美西律和普罗帕酮。
用法用量　　
口服,成人开始每次100mg,一日2次,其后隔4日每次加50mg,最大量每次200mg;儿童每次50-100mg,一日2次.静脉滴注,成人2mg/kg,15分钟滴完;儿童2mg/kg,10分钟内滴完.
静注：每次1～2mg／kg，缓慢静脉推注，至少在3min以上，需要时，可隔15～20min后再注射0.5mg／kg。儿童每次2mg／kg，于10min内滴完。当本品血浆浓度超过1000μg/ml时，可出现致死性心律失常，应加注意。
由于本品具有独特的电生理效应和血流动力学改变，故与其他心脏活性药物(如抗心律失常药、β受体阻滞药、钙拮抗剂)合用时要特别谨慎。
任何疑问，请遵医嘱！
包装规格[日本药典醋酸氟卡尼片/注射剂]
片剂
50毫克：100片（PTP）
50毫克：500片（PTP/瓶）
100毫克：100片（PTP）
100毫克：500片（PTP）
注射剂
静脉 50毫克（5mL）：10管
生产厂商
卫材有限公司
完整资料附件(注：使用以原处方为准)：
片剂：http://www.info.pmda.go.jp/go/pack/2129009F1020_1_16/
注射：http://www.kegg.jp/medicus-bin/japic_med?japic_code=00055029
細粒10％：http://www.kegg.jp/medicus-bin/japic_med?japic_code=00065517
Therapeutic category name
Tachyarrhythmia therapy agent
Brand Name
Tambocor Tablets 50mg 100mg
composition
This drug is a white plain tablet containing flecainide acetate 50mg in one tablet.
Croscarmellose sodium as an additive, crystalline cellulose, hydrogenated oil, magnesium stearate, it contains a partially gelatinized starch.
Contraindication
Patients with congestive heart failure
[This drug has a negative inotropic effect and may further exacerbate heart failure symptoms. ]
A high degree of atrioventricular block, patients with a high degree of sinoatrial block
[This agent has the effect of inhibiting the atrioventricular conduction, sinoatrial conduction, it may further exacerbate the stimulus conduction. ]
Patients with asymptomatic ventricular premature contraction or non-sustained ventricular tachycardia after myocardial infarction
The results of [clinical trials for sudden death (CAST), there is a report of the death rate increases by the administration of this drug in such patients. See section "Other Notes"]
Women who may possibly be pregnant or pregnant
[See section "pregnant women, maternal, administration to lactating women, etc."]
Patients during administration of ritonavir
[See section of "interaction"]
Patients in the administration of the Mirabegron
[See section of "interaction"]
Patients in the administration of telaprevir
[See section of "interaction"]
Efficacy or effect
Or other anti-arrhythmic drugs can not be used under the following conditions, or in the case of disabledadult
Tachyarrhythmia (paroxysmal atrial fibrillation, flutter, ventricular)
Child
Tachyarrhythmia (paroxysmal atrial fibrillation, flutter, paroxysmal supraventricular, ventricular)
If you want to use this drug in children, etc., that the doctor skilled in arrhythmia treatment of such children be supervised. The atrial flutter and ventricular tachycardia with underlying heart disease, be administered only when the benefit is determined to outweigh the risks.
adult
Tachyarrhythmia (paroxysmal atrial fibrillation, flutter)
Typically, it starts the dosing one day 100mg as flecainide acetate for adults, the effect is increased to 200mg if insufficient, administered orally in divided twice daily. In addition, it wants to lose weight depending on the patient's age and symptoms.
Tachyarrhythmia (ventricular)
Typically, it starts the dosing one day 100mg as flecainide acetate for adults, the effect is increased to 200mg if insufficient, administered orally in divided twice daily. In addition, it will be increased or decreased depending on the patient's age and symptoms.
Child
Tachyarrhythmia (paroxysmal atrial fibrillation, flutter, paroxysmal supraventricular, ventricular)
Typically, infants of more than 6 months, infants and 1 day as flecainide acetate in children 50~100mg / m2 (body surface area), is orally administered divided into two or three times a day. In addition, it will be increased or decreased depending on the patient's age and symptoms. However, the maximum daily dose is I to 200mg / m2.
Typically, a day 50mg / m2 (body surface area) as flecainide acetate for infants less than 6 months, are orally administered in divided two or three times a day. In addition, it will be increased or decreased depending on the patient's age and symptoms. However, the maximum daily dose is I to 200mg/m2.
Careful administration
Patients with underlying heart disease (myocardial infarction, valvular disease, cardiomyopathy, etc.)
[This drug has a negative inotropic effect, which may exacerbate cardiac function. ]
The elderly [see section "administration to the elderly."]
Patients with stimulus conduction disorders (atrioventricular block, sinoatrial block, bundle branch block, etc.)
[This agent has the effect of inhibiting the atrioventricular conduction and sinoatrial conduction, etc., which may further exacerbate the stimulus conduction. ]
Patients with marked sinus bradycardia
[This drug is able to suppress the sinus node function. ]
Patients with a history of congestive heart failure
[This drug has a negative inotropic effect, which may exacerbate cardiac function. ]
Patients with hepatic dysfunction
[This drug because it is metabolized in the liver, such a patient may become overdose. ]
Patients with severe renal dysfunction
[This drug because it is excreted from the kidney, such a patient may become overdose. ]
Patients with serum potassium decreased
[Proarrhythmic effects are likely to occur in these patients, there is a risk of developing a high degree of arrhythmia. ]
Clinically significant adverse reactions
Circulatory organ
Ventricular tachycardia (torsades de pointes, including a) (less than 0.1% to 5%), ventricular fibrillation (less than 0.1%), atrial flutter (less than 0.1% to 5%), advanced atrioventricular block (less than 0.1% to 5%), transient cardiac arrest (less than 0.1%), sinus arrest (or sino-atrial block) (less than 0.1% to 5%), worsening of heart failure (less than 0.1~5%), Adams-Stokes attack (less than 0.1%) that appears is there.
In such a case, that discontinue administration of this drug, to consider the following treatment method (see section "overdose").
Removed from the digestive unabsorbed drug
Dopamine, dobutamine, inotropic agents of isoprenaline such as administration
Auxiliary circulation such as IABP
Pacing or cardioversion
Liver dysfunction, jaundice
AST (GOT), ALT (GPT), since the γ-GTP liver dysfunction with elevated, etc. (frequency unknown) and jaundice (incidence unknown) may occur, carefully observed, if any abnormality is observed such as by discontinuing administration of the drug, to take appropriate action to.
Pharmacology
Effect on experimental arrhythmia
Ventricular arrhythmia that was induced in mice and dogs (chloroform, adrenaline, ouabain, coronary artery ligation) to suppress in oral and intravenous administration. 8) 9) 10)
To suppress atrial arrhythmia was induced than aconitine in intravenous administration in dogs. 8) 11)
Electrophysiological action
In Purkinje fibers and ventricular muscle of the dog, without affecting the resting membrane potential, to reduce the maximum depolarization velocity (Vmax) and action potential amplitude. 12)
Stimulate the Vmax of the guinea pig atrial muscle and ventricular muscle frequency-dependent manner to suppress. 13) 14)
In dogs, and to extend the effective refractory period of ventricular muscle, to shorten the effective refractory period of Purkinje fibers. 12)
Intra-atrial conduction of the dog, His - Purkinje (H-V) to delay the conduction and intraventricular conduction. 15)
Clinical electrophysiological action
If this drug 250mg Note) was orally administered to the arrhythmia patient, sinus cycle, without affecting the sinus node recovery time, it delays the H-V conduction, and prolong the effective refractory period of the ventricular muscle. Also, it is possible to suppress the retrograde accessory pathway, to extend the effective refractory period of the ventriculoatrial conduction system. 16)
Note) 250mg single oral administration is unapproved dose.
The physicochemical knowledge of active ingredient
General name
Flecainide acetate (Flecainide Acetate)
Chemical name
N - [(2RS) -Piperidin-2-ylmethyl] -2, 5-bis (2, 2, 2-trifluoroethoxy) benzamide monoacetate
The molecular formula
C17H20F6N2O3 · C2H4O2
Molecular weight
474.39
Structural formula
Physicochemical properties
Flecainide acetate as a white crystalline powder, there is a slightly peculiar smell or slightly of acetic acid-like smell.
This product is methanol, ethanol (95) or is freely soluble in acetic acid (100), slightly less soluble in water.
Methanol solution (1 → 25) of this product shows no optical rotation.
Melting point
About 150 ℃ (decomposition)
Partition coefficient
0.34 (water-1-octanol system)