Flexyx

Flexyx drugs: Flecaine

Flecaine - General Information:

A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial arrhythmias and tachycardias. Paradoxically, however, in myocardial infarct patients with either symptomatic or asymptomatic arrhythmia, flecainide exacerbates the arrhythmia and is not recommended for use in these patients. [PubChem]

Pharmacology:

Flecaine has local anesthetic activity and belongs to the membrane stabilizing (Class 1) group of antiarrhythmic agents; it has electrophysiologic effects characteristic of the IC class of antiarrhythmics.

Flecaine for patients

Flecaine Interactions

Drug Interactions.   TAMBOCOR has been administered to patients receiving digitalis preparations or beta-adrenergic blocking agents without adverse effects. During administration of multiple oral doses of TAMBOCOR to healthy subjects stabilized on a maintenance dose of digoxin, a 13%-19% increase in plasma digoxin levels occurred at six hours postdose.

In a study involving healthy subjects receiving TAMBOCOR and propranolol concurrently, plasma flecainide levels were increased about 20% and propranolol levels were increased about 30% compared to control values. In this formal interaction study, TAMBOCOR and propranolol were each found to have negative inotropic effects; when the drugs were administered together, the effects were additive. The effects of concomitant administration of TAMBOCOR and propranolol on the PR interval were less than additive. In TAMBOCOR clinical trials, patients who were receiving beta blockers concurrently did not experience an increased incidence of side effects. Nevertheless, the possibility of additive negative inotropic effects of beta blockers and flecainide should be recognized.

Flecainide is not extensively bound to plasma proteins. In vitro studies with several drugs which may be administered concomitantly showed that the extent of flecainide binding to human plasma proteins is either unchanged or only slightly less. Consequently, interactions with other drugs which are highly protein bound (e.g., anticoagulants ) would not be expected. TAMBOCOR has been used in a large number of patients receiving diuretics without apparent interaction. Limited data in patients receiving known enzyme inducers ( phenytoin, phenobarbital, carbamazepine ) indicate only a 30% increase in the rate of flecainide elimination. In healthy subjects receiving cimetidine (1 gm daily) for one week, plasma flecainide levels increased by about 30% and half-life increased by about 10%.

When amiodarone is added to flecainide therapy, plasma flecainide levels may increase two-fold or more in some patients, if flecainide dosage is not reduced.

Drugs that inhibit cytochrome P450IID6, such as quinidine , might increase the plasma concentrations of flecainide in patients that are on chronic flecainide therapy; especially if these patients are extensive metabolizers.

There has been little experience with the coadministration of TAMBOCOR and either disopyramide or verapamil. Because both of these drugs have negative inotropic properties and the effects of coadministration with TAMBOCOR are unknown, neither disopyramide nor verapamil should be administered concurrently with TAMBOCOR unless, in the judgment of the physician, the benefits of this combination outweigh the risks. There has been too little experience with the coadministration of TAMBOCOR with nifedipine or diltiazem to recommend concomitant use.

Flecaine Contraindications

TAMBOCOR is contraindicated in patients with pre-existing second- or third-degree AV block, or with right bundle branch block when associated with a left hemiblock (bifascicular block), unless a pacemaker is present to sustain the cardiac rhythm should complete heart block occur. TAMBOCOR is also contraindicated in the presence of cardiogenic shock or known hypersensitivity to the drug.

Additional information about Flecaine

Flecaine Indication: For the prevention of paroxysmal supraventricular tachycardias (PSVT), including atrioventricular nodal reentrant tachycardia, atrioventricular reentrant tachycardia and other supraventricular tachycardias of unspecified mechanism associated with disablin.
Mechanism Of Action: Flecaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
Drug Interactions: Amiodarone Amiodarone increases the effect and toxicity of flecainide
Cimetidine Cimetidine increases serum levels of flecainide
Cisapride Increased risk of cardiotoxicity and arrhythmias
Mesoridazine Increased risk of cardiotoxicity and arrhythmias
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Thioridazine Increased risk of cardiotoxicity and arrhythmias
Duloxetine Possible increase in the levels of this agent when used with duloxetine
Quinupristin This combination presents an increased risk of toxicity
Ritonavir Ritonavir increases the toxicity of the anti-arrhythmic
Food Interactions: Take without regard to meals.
Generic Name: Flecainide
Synonyms: Flecainida [Inn-Spanish]; Flecainide acetate; Flecainidum [Inn-Latin]
Where to order Flecainide (and Flecaine analogs) online:
Drug Category: Antiarrhythmic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Flecainide: Flecaine; Tambocor;
Absorption: Nearly complete following oral administration.
Toxicity (Overdose): Oral LD50 is 50-498 mg/kg in rat. Symptoms of overdose include nausea and vomiting, convulsions, hypotension, bradycardia, syncope, extreme widening of the QRS complex, widening of the QT interval, widening of the PR interval, ventricular tachycardia, AV nodal block, asystole, bundle branch block, cardiac failure, and cardiac arrest.
Protein Binding: 40%
Biotransformation: Hepatic. Flecainide does not undergo any consequential presystemic biotransformation. The two major urinary metabolites are meta-O-dealkylated flecainide (active, but about one-fifth as potent) and the meta-O-dealkylated lactam of flecainide (non-active metabolite).
Half Life: 20 hours (range 12-27 hours)
Dosage Forms of Flecaine: Tablet Oral
Chemical IUPAC Name: N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
Chemical Formula: C17H20F6N2O3
Flecainide on Wikipedia: http://en.wikipedia.org/wiki/Flecainide
Organisms Affected: Humans and other mammals