Ranolazine
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Contents |
Indications
- adjuvant therapy of chronic angina pectoris
Contraindications
- pre-existing QT prolongation
- hepatic insufficiency ( Child-Pugh classes A,B,C)
- coadministration of drugs that prolong QT interval
- no benefit for acute onset coronary artery disease
Dosage
- Tabs: 500 ( orange)
Pharmacokinetics
- metabolized by cyt P450 3A4 & to a lesser extent cyt P450 2D6
Monitor
- ECG, baseline and follow-up
Adverse-effects
- increased QT interval
- dizziness (6%), headache (6%), constipation (4%), nausea (4%)
- others < 2%
- palpitations, tinitus, vertigo, abdominal pain, xerostomia, vomiting, peripheral edema, dyspnea
Drug-interactions
- drugs that inhibit cyt P450 3A4 increase ranolazine levels ( diltiazem, verapamil, HIV protease inhibitors, macrolides)
- drugs that inhibit cyt P450 2D6 do not increase ranolazine levels significantly
- ranolazine inhibits cyt P450 3A4 & cyt P450 2D6, thus may increase levels of drugs metabolized by these enzymes ( simvastatin levels doubled)
- ranolazine inhibits P-glycoprotein and may increase levels of drugs eliminated in part by P-glycoprotein ( digoxin levels increased 1.5 fold)
- avoid other drugs that prolong QT interval ( amiodarone, erythromycin, quinidine, sotalol, etc)
Mechanism-of-action
- inhibits late Na+ current
- no significant effect on heart rate or blood pressure
- facilitates myocardium functioning during ischemia
- reduces intracellular Na+ & Ca+2 during myocardial ischemia
- partially inhibits fatty acid oxidation, thus increases glucose oxidation
- may decrease myocardial oxygen demand
- inhibits P-glycoprotein
More General Terms
References
- Prescriber's Letter 13(3): 2006 New Drug: Ranexa (ranolazine) Detail-Document#: [1] (subscription needed) [2]
- Morrow DA et al, Effects of ranolazine on recurrent cardiovascular events in patients with non ST_segment elevation acute coronary syndromes: The MERLIN-TIMI 36 randomized trial, JAMA 2007, 297:1775 PMID: &dopt=Abstract
