Ranexa

Ranexa is an antianginal medication. On January 31, 2006, ranolazine was approved for use in the United States by the FDA for the treatment of chronic angina. .
[Wikipedia].

Medicinal name:
  • 12 HR ranolazine 500 MG Extended Release Oral Tablet [Ranexa]
  • 12 HR ranolazine 1000 MG Extended Release Oral Tablet [Ranexa]

Ranexa - Pharmacology:

The mechanism of action of ranolazine is unknown. It does not increase the rate-pressure product, a measure of myocardial work, at maximal exercise. In vitro studies suggest that ranolazine is a P-gp inhibitor. Ranexa is believed to have its effects via altering the trans-cellular late sodium current. It is by altering the intracellular sodium level that ranolazine affects the sodium-dependent calcium channels during myocardial ischemia. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia.

Ranexa mini report

Ranexa NDA
NDA - A product marketed under an approved New Drug Application
Ranexa TABLET, FILM COATED, EXTENDED RELEASE
TABLET, FILM COATED, EXTENDED RELEASE
Ranexa HUMAN PRESCRIPTION DRUG
HUMAN PRESCRIPTION DRUG
Ranexa global name
RANOLAZINE
Ranexa global name
ranolazine
Start - Stop data
START DATA:
2006-Jan-27
Start - Stop data
STOP DATA
not occurred

Ranexa for patients

To ensure safe and effective use of Ranexa, the following information and instructions should be communicated to the patient when appropriate.

Patients should be advised:

  • that Ranexa is only for patients not responding adequately to other antianginal drugs
  • that Ranexa may produce changes in the electrocardiogram (QTc interval prolongation)
  • to inform their physician of any personal or family history of QTc prolongation, congenital long QT syndrome,
  • or proarrhythmic conditions such as hypokalemia
  • that Ranexa should be avoided in patients receiving drugs that prolong the QTc interval such as Class Ia
  • (e.g., quinidine) or Class III (e.g., dofetilide, sotalol) antiarrhythmic agents, erythromycin, and certain
  • antipsychotics (e.g., thioridazine, ziprasidone)
  • that Ranexa should be avoided in patients receiving drugs that are potent or moderately potent inhibitors of
  • CYP3A, including, for example, ketoconazole, HIV protease inhibitors, macrolide antibiotics, diltiazem, and
  • verapamil
  • that grapefruit juice or grapefruit products should be avoided when taking Ranexa
  • that doses of Ranexa higher than 1000 mg twice a day should not be used
  • that Ranexa will not abate an acute angina episode
  • that Ranexa should generally be avoided in patients with mild, moderate or severe liver impairment
  • that Ranexa should generally be avoided in patients with severe renal impairment
  • to inform their physician of any other medications when taken concurrently with Ranexa, including over-the-
  • counter medications
  • to contact their physician if they experience palpitations or fainting spells while taking Ranexa
  • that Ranexa may cause dizziness and lightheadedness; therefore, patients should know how they react to
  • this drug before they operate an automobile, or machinery, or engage in activities requiring mental alertness
  • or coordination
  • that Ranexa may be taken with or without meals
  • that Ranexa tablets should be swallowed whole and not crushed, broken, or chewed

Ranexa Interactions

Pharmacokinetic Interactions:Effects of Other Drugs on Ranexa

Ketoconazole

As a potent inhibitor of CYP3A, ketoconazole (200 mg b.i.d.) increases average steady-state plasma concentrations of ranolazine 3.2-fold.Ranexa should not be used during treatment with ketoconazole.

Diltiazem

As a moderate inhibitor of CYP3A, diltiazem (180 to 360 mg daily) causes dose-dependent mean increases in average ranolazine steady-state concentrations of about 1.8- to 2.3-fold.

Verapamil

Verapamil 120 mg t.i.d. increases ranolazine steady-state plasma concentrations about 2-fold.

Cimetidine

Co-administration of cimetidine does not increase the plasma concentrations of ranolazine.No dose adjustment of Ranexa is required in patients treated with cimetidine.

Digoxin

Co-administration of digoxin does not increase the plasma concentration of ranolazine.No dose adjustment of Ranexa is required in patients treated with digoxin.

Paroxetine

Paroxetine, a potent inhibitor of CYP2D6, increased average steady-state plasma concentrations of ranolazine 1.2-fold.No dose adjustment of Ranexa is required in patients treated with paroxetine or other CYP2D6 inhibitors.

Pharmacokinetic Interactions:Effects of Ranexa on Other Drugs

Digoxin

As a result of an interaction at the P-gp level, co-administration of ranolazine and digoxin results in a 1.5-fold elevation of digoxin plasma concentrations.The dose of digoxin may have to be adjusted when ranolazine is co- administered with digoxin.

Simvastatin

Co-administration of ranolazine and simvastatin results in about a 2-fold increase in plasma concentrations of simvastatin, and its active metabolite.

Warfarin

Ranexa has no significant effect on the pharmacokinetics of (+) R and (-) S warfarin.

Ranexa Contraindications

Ranexa is contraindicated in patients:

  • With pre-existing QT prolongation
  • With hepatic impairment (Child-Pugh Classes A [mild], B [moderate] or C [severe])
  • On QT prolonging drugs
  • On potent and moderately potent CYP3A inhibitors, including diltiazem

Manufacturers name:

  • Cardinal Health
  • Gilead Sciences, Inc
  • Carilion Materials Management

Ranexa tags categories:

Generic name, Overdose, Half Life Ranexa, Food Interactions, Chemical, etc..

Ranexa see also FDA report