N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzamidmonoacetat

Bezeichnung:N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzamidmonoacetat

CAS-Nr54143-56-5

Englisch Name:FLECAINIDE ACETATE

CBNumberCB9295801

SummenformelC19H24F6N2O5

Molgewicht474.39

MOL-Datei54143-56-5.mol

Synonyma

N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzamidmonoacetat

N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzamidmonoacetat physikalisch-chemischer Eigenschaften

Schmelzpunkt	145-147℃
storage temp.	2-8°C
Löslichkeit	Soluble in water and in anhydrous ethanol. It is freely soluble in dilute acetic acid and practically insoluble in dilute hydrochloric acid.
Aggregatzustand	Solid
Farbe	White
Wasserlöslichkeit	Soluble in dilute acetic acid, dimethyl sulfoxide, ethanol, methanol and water.
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 1 month.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36/37/38-63
S-Sätze:	22-26-36/37/39-45-46
RIDADR	3249
WGK Germany	-
RTECS-Nr.	CV5792550
HazardClass	6.1(b)
PackingGroup	III
HS Code	2933399090

Gefahreninformationscode (GHS)

FLECAINIDE ACETATE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R63:Kann das Kind im Mutterleib möglicherweise schädigen.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
Flecainide acetate (54143-56-5) is an open Na+?channel blocker that inhibits fast Na+?current in cardiac muscle in a use- and concentration-dependent manner.1?Orally-active class Ic antiarrhythmic agent2,3. Inhibits hERG potassium channels at clinically relevant concentrations.4
Chemische Eigenschaften
White or almost white, very hygroscopic, crystalline powder.
Verwenden
Flecainide acetate is used as a sodium channel blocker and as an anti-arrhythmic. In general, it is used to regulate heartbeats of the upper heart and lower heart chambers. It can also be used to slow down an overactive heart. It is also useful in the treatment of ventricular tachycardias and ventricular arrhythmias.
Verwenden
Class I antiarrhythmic.
Definition
ChEBI: An acetate salt obtained by combining flecainide with one molar equivalent of acetic acid. An antiarrhythmic agent used to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).
Trademarks
Tambocor (3M Pharmaceuticals).
Allgemeine Beschreibung
Flecainide acetate, N-(2-piperidinylmethyl)-2,5-bis (2,2,2-trifluoroethoxy)benzamide monoacetate(Tambocor), is a class IC antiarrhythmic drug withlocal anesthetic activity; it is a chemical derivative of benzamide.The drug undergoes biotransformation, forming ameta-O-dealkylated compound, whose antiarrhythmic propertiesare half as potent as those of the parent drug, and ameta-O-dealkylated lactam of flecainide with little pharmacologicalactivity. Flecainide acetate is given orally to suppresschronic ventricular ectopy and ventricular tachycardia.It has some limitations because of CNS side effects.
Biologische Aktivität
Open Na + channel blocker that inhibits fast Na + current in cardiac muscle in a use- and concentration-dependent manner. Orally-active class Ic antiarrhythmic agent.
Biochem/physiol Actions
Class IC antiarrhythmic agent; sodium channel blocker
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Anti-arrhythmics: concentration increased by amiodarone - halve dose of flecainide; increased myocardial depression with other anti-arrhythmics.
Antidepressants: concentration increased by fluoxetine; increased risk of ventricular arrhythmias with tricyclics.
Antihistamines: increased risk of ventricular arrhythmias with mizolastine - avoid.
Antihypertensives: increased myocardial depression and bradycardia with beta-blockers; increased myocardial depression and asystole with verapamil.
Antimalarials: concentration increased by quinine; avoid with artemether/lumefantrine.
Antimuscarinics: increased risk of ventricular arrhythmias with tolterodine.
Antipsychotics: increased risk of ventricular arrhythmias with antipsychotics that prolong the QT interval and phenothiazines; increased risk of arrhythmias with clozapine.
Antivirals: concentration possibly increased by fosamprenavir, indinavir, lopinavir, ritonavir and saquinavir, increased risk of ventricular arrhythmias - avoid; use telaprevir with caution.
Diuretics: increased cardiac toxicity if hypokalaemia occurs.
Stoffwechsel
Flecainide is extensively metabolised (subject to genetic polymorphism), the 2 major metabolites being m-Odealkylated flecainide and m-O-dealkylated lactam of flecainide, both of which may have some activity. Its metabolism appears to involve the cytochrome P450 isoenzyme CYP2D6, which shows genetic polymorphism.
Flecainide is excreted mainly in the urine, approximately 30% as unchanged drug and the remainder as metabolites. About 5% is excreted in the faeces. Haemodialysis removes only about 1% of unchanged flecainide.
Lager
Desiccate at +4°C
Einzelnachweise
1) Rouet and Ducouret (1994), Use- and concentration-dependent effects of flecainide in guinea pig right ventricular muscle; J. Cardiovasc. Pharmacol.,?24?177 2) Singh?et al. (1984),?The electrophysiology and pharmacology of verapamil, flecainide, and amiodarone: correlations with clinical effects and antiarrhythmic actions; Ann. N.Y. Acad. Sci.,?432?210 3) Banitt?et al.?(1977),?Anti-arrhythmics. 2. Synthesis and antiarrhythmic activity of N-(piperidylalkyl)trifluoroethoxybenzamides; J. Med. Chem.,?20?821 4) Melgari?et al.?(2015),?Molecular basis of hERG potassium channel blockade by the class Ic antiarrhythmic flecainide; J. Mol. Cell. Cardiol.,?86?42

N-(Piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluorethoxy)benzamidmonoacetat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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