Pharmacologic class: Piperazine derivative
Therapeutic class: Antianginal
Pregnancy risk category C
Unclear. Appears to modulate myocardial metabolism by partially inhibiting fatty acid oxidation, thereby increasing glucose oxidation and generating more adenosine triphosphate.
Tablets (extended-release): 500 mg, 1,000 mg
Indications and dosages
➣ Chronic angina
Adults: Initially, 500 mg P.O. twice daily, increased to maximum recommended dosage of 1,000 mg P.O. twice daily if needed
• Concurrent use of moderate CYP3A inhibitors, such as diltiazem, verapamil, and erythromycin
• Concurrent use of P-gp inhibitors such as cyclosporine
• Liver cirrhosis
• Concurrent use of strong CYP3A inhibitors (such as ketoconazole, clarithromycin, nelfinavir)
• Concurrent use of CYP3A inducers (such as rifampin, phenobarbital, St. John's wort)
Use cautiously in:
• concurrent digoxin therapy, QT-interval prolongation, drugs that prolong QT interval, moderate CYP3A inhibitors (including diltiazem, verapamil, aprepitant, erythromycin, fluconazole, grapefruit juice, or grapefruit-containing products)
• patients age 75 and older
• pregnant or breastfeeding patients
• children (safety and efficacy not established).
• Administer without regard to meals.
• Don't give with grapefruit juice.
CNS: dizziness, headache, vertigo
EENT: tinnitus, dry mouth
GI: nausea, vomiting, constipation, abdominal pain
Other: peripheral edema
Drug-drug. CYP3A inducers such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentin: decreased ranolazine plasma concentration
CYP3A inhibitors such as diltiazem, ketoconazole, macrolide antibiotics, paroxetine, protease inhibitors, verapamil: increased ranolazine blood level
Digoxin, simvastatin: increased blood levels of these drugs
P-gp inhibitors (such as cyclosporine): increased ranolazine exposure
Drug-food. Grapefruit juice and grapefruit-containing products: increased ranolazine blood level
• Obtain baseline and follow-up ECGs to evaluate drug effects on QT interval.
• Monitor blood pressure regularly in patients with severe renal impairment.
• Inform patient that drug can be taken with or without food, but not with grapefruit juice or grapefruit-containing products.
• Advise patient not to chew or crush tablets.
• Instruct patient to consult prescriber before taking other prescription or over-the-counter drugs or herbal products.
• Inform patient that drug isn't intended for acute angina episodes.
• Caution patient to avoiding driving and other hazardous activities until drug effects are known.
• Advise female with childbearing potential to tell prescriber if she is pregnant or plans to become pregnant.
• Advise female not to breastfeed during therapy.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and foods mentioned above.
Time/action profile (blood levels)
|PO||unknown||2–5 hr||12 hr|
Adverse Reactions/Side Effects
Central nervous system
Ear, Eye, Nose, Throat
- torsades de pointes (life-threatening)
- QTc prolongation
- abdominal pain
- dry mouth
Drug-Drug interactionKetoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir significantly ↑ levels; concurrent use contraindicated.Rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, and carbamazepine significantly ↓ levels; concurrent use contraindicated.Verapamil, diltiazem, aprepitant, erythromycin, and fluconazole ↑ levels (do not exceed ranolazine dose of 500 mg twice daily).Cyclosporine may ↑ levels.Paroxetine may ↑ levels.May ↑ levels of simvastatin.May ↓ metabolism and ↑ effects of metoprolol, tricyclic antidepressants, and antipsychotics ; dosage adjustments may be necessary.May ↑ digoxin levels; dose adjustment may be required.St. John's wort significantly ↓ levels (contraindicated).Grapefruit juice↑ levels (do not exceed ranolazine dose of 500 mg twice daily).
Availability (generic available)
- Assess location, duration, intensity, and precipitating factors of anginal pain.
- Monitor ECG at baseline and periodically during therapy to evaluate effects on QT interval.
- Lab Test Considerations: Monitor renal function after starting and periodically during therapy in patients with moderate to severe renal impairment (CCr < 60 mL/min) for ↑ serum creatinine accompanied by ↑ BUN. Usually has a rapid onset, but does not progress during therapy and is reversible with discontinuation of ranolazine.
- May cause transient eosinophilia.
- May cause small mean ↓ in hematocrit.
Potential Nursing DiagnosesIneffective tissue perfusion (Indications)
Activity intolerance (Indications)
- Ranolazine should be used in combination with amlodipine, beta blockers, or nitrates.
- Do not administer with grapefruit juice or grapefruit products.
- Oral: May be administered without regard to food. Tablets should be swallowed whole; do not break, crush, or chew.
- Instruct patient to take ranolazine as directed. If a dose is missed, take the usual dose at the next scheduled time; do not double doses. Explain to patient that ranolazine is used for chronic therapy and will not help an acute angina episode.
- Advise patient to avoid grapefruit juice and grapefruit products when taking ranolazine.
- May cause dizziness and light-headedness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
- Advise patient to notify health care professional if fainting occurs.
- Inform patient that ranolazine may cause changes in the ECG. Patient should inform health care professional if they have a personal or family history of QTc prolongation, congenital long QT syndrome, or proarrhythmic conditions such as hypokalemia.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Decrease in frequency of angina attacks.