ranolazine

ranolazine,

an antianginal.

indications This drug is used in combination with other antianginals (such as amlodipine, beta-blockers, or nitrates) to treat chronic stable angina pectoris in those who have not responded to other treatment options.

contraindications Preexisting Q-T prolongation, hepatic disease (Child-Pugh class A, B, or C), hypokalemia, renal failure, torsades de pointes, ventricular arrhythmia, ventricular tachycardia, and known hypersensitivity to this drug prohibit its use.

adverse effects Adverse effects of this drug include headache, dizziness, palpitations, nausea, vomiting, constipation, dry mouth, peripheral edema, and dyspnea. A life-threatening side effect of this drug is Q-T prolongation.

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ranolazine

Ranexa

Pharmacologic class: Piperazine derivative

Therapeutic class: Antianginal

Pregnancy risk category C

Action

Unclear. Appears to modulate myocardial metabolism by partially inhibiting fatty acid oxidation, thereby increasing glucose oxidation and generating more adenosine triphosphate.

Availability

Tablets (extended-release): 500 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

Contraindications

• Hypersensitivity to drug or its components
• Hepatic impairment
• Preexisting QT interval prolongation
• Concurrent use of drugs that cause QT interval prolongation or inhibit CYP3A (including diltiazem)

Precautions

Use cautiously in:
• patients receiving concurrent digoxin therapy
• patients age 75 and older
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Administer without regard to meals.
• Don't give with grapefruit juice.

Route	Onset	Peak	Duration
P.O.	Unknown	2-5 hr	Unknown

Adverse reactions

CNS: dizziness, headache, vertigo

CV: palpitations

EENT: tinnitus, dry mouth

GI: nausea, vomiting, constipation, abdominal pain

Respiratory: dyspnea

Other: peripheral edema

Interactions

Drug-drug. CYP3A inhibitors such as diltiazem, ketoconazole, macrolide antibiotics, paroxetine, protease inhibitors, verapamil: increased ranolazine blood level

Digoxin, simvastatin: increased blood levels of these drugs

Drug-food. Grapefruit juice: 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.
• Advise patient not to chew or crush tablets.
• Instruct patient to consult prescriber before taking other prescription or over-the-counter drugs.
• 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.

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ranolazine

Cardiology An anti-anginal metabolic modulator, which inhibits partial fatty acid oxidation, maintaining glucose oxidation without lactic acid buildup. See CARISA.