Clinical Pharmacology Details


RANOLAZINE


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Indications & Dose:

As adjunctive therapy in the treatment of stable angina in patients inadequately controlled or intolerant of firstline antianginal therapies 



Adult: Initially 375 mg twice daily for 2–4 weeks, then increased to 500 mg twice daily, then adjusted according to response to 750 mg twice daily; reduced if not tolerated to 375–500 mg twice daily

Contraindications:

Severe renal impairment

Side Effects:

Cautions:

hypovolaaemia; low systolic blood pressure; acute pulmonary oedema; acute myocardial infarction with acute left ventricular failure and low filling pressures; pregnancy.

Precautions:

Moderate to severe CHF, QT interval prolongation, elderly, body wt <60 kg, mild to moderate hepatic & renal impairment.

Interaction:

DRUGS


CYP2D6 such as antipsychotics, metoprolol, tricyclic antidepressants: Increased plasma levels of these drugs CYP3A inducers, such as carbamazepine, phenobarbital, phenytoin, rifabutin,


rifampin, rifapentin, St. John’s wort:


Decreased blood ranolazine level and decreased effectiveness CYP3A substrates, such as cyclosporine, lovastatin, simvastatin, sirolimus, tacrolimus: Possibly increased blood levels of these drugs CYP3A inhibitors, such as clarithromycin, diltiazem, erythromycin, fluconazole, indinavir, itraconazole, ketoconazole, nefazodone,


nelfinavir, ritonavir, saquinavir, verapamil: Increased blood ranolazine level and increased risk of adverse reactions digoxin: Increased blood digoxin level 

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Asthenia, confusion, dizziness, hallucination, headache, hypoesthesia, paresthesia, syncope,tremor, vertigo
CV: Bradycardia, hypotension, orthostatic hypotension, palpitations, peripheral edema, QTinterval prolongation
EENT: Blurred vision, dry mouth, tinnitus
GI: Abdominal pain, anorexia, constipation, dyspepsia, nausea, vomiting
GU: Elevated blood urea and creatinine levels, hematuria, renal failure
HEME: Eosinophilia, leukopenia, pancytopenia, thrombocytopenia
RESP: Dyspnea, pulmonary fibrosis
SKIN: Diaphoresis, pruritus, rash
Other: Angioedema

Patient And Carer Advice: