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

Dosage adjustment

• 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.

Adverse reactions

CNS: dizziness, headache, vertigo

CV: palpitations

EENT: tinnitus, dry mouth

GI: nausea, vomiting, constipation, abdominal pain

Respiratory: dyspnea

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

Patient monitoring

• Obtain baseline and follow-up ECGs to evaluate drug effects on QT interval.

• Monitor blood pressure regularly in patients with severe renal impairment.

Patient teaching

• 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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


(ra-nole-a-zeen) ,


(trade name)


Therapeutic: antianginals
Pregnancy Category: C


Chronic angina pectoris.


Does not ↓ BP or heart rate; remainder of mechanism is not known.

Therapeutic effects

Decreased frequency of angina.


Absorption: Highly variable.
Distribution: Unknown.
Metabolism and Excretion: Metabolized in the gut (P-glycoprotein) and by the liver (primarily CYP3A and less by CYP2D6); <5% excreted unchanged in urine and feces.
Half-life: 7 hr.

Time/action profile (blood levels)

POunknown2–5 hr12 hr


Contraindicated in: Hypersensitivity;Concurrent use of potent inhibitors of CYP3A;Concurrent use of inducers of CYP3A;Hepatic impairment; Lactation: Lactation.
Use Cautiously in: Renal impairment; Obstetric: Use only when potential benefit outweighs risk to fetus; Pediatric: Safety not established; Geriatric: ↑ risk of adverse reactions in patients >75 yr.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • headache

Ear, Eye, Nose, Throat

  • tinnitus


  • torsades de pointes (life-threatening)
  • palpitations
  • QTc prolongation


  • abdominal pain
  • constipation
  • dry mouth
  • nausea
  • vomiting


Drug-Drug interaction

Ketoconazole, 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).


Oral (Adults) 500 mg twice daily initially, may be ↑ to 1000 mg twice daily.

Availability (generic available)

Extended-release tablet: 500 mg

Nursing implications

Nursing assessment

  • 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 Diagnoses

Ineffective 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.

Patient/Family Teaching

  • 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.

Evaluation/Desired Outcomes

  • Decrease in frequency of angina attacks.
Drug Guide, © 2015 Farlex and Partners
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References in periodicals archive ?
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Food and Drug Administration, Center for Drug Evaluation and Research, Ranexa NDA 21-526 Approval Letter, January 2006, https://www.accessdata.fda.gov/drugsatfda_docs/ label/2006/021526s000lbl.pdf4.
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