Ranolazine
Cardiac Therapy · Anti-anginal
Indications
Adjunctive therapy in the treatment of stable angina in patients inadequately controlled on 1st line antianginal therapy.
Dosage
Adults: Initially 375 mg twice daily, increasing after 2-4 wk to 500 mg twice daily. Max, 750 mg twice daily according to response. Children: Not recommended.
Adverse Effects
Dizziness, headache, GI upset, asthaenia.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Severe renal impairment ( CrCl <30mL/min), moderate or severe hepatic impairment. Precautions: Moderate to severe CHF, CYP2D6 poor metabolisers, QT interval prolongation, elderly, body wt < 60 kg, mild to moderate hepatic & renal impairment.
Interactions
CYP3A4 inhibitors & inducers, CYP2D6 inhibitors (e.g., paroxetine) or substrates (e.g., TCADs, antipsychotics), calcium channel blockers, anti-arrhythmics, anticonvulsants, macrolides, digoxin, drugs that prolong QT intervals. P-gp inhibitors (e.g., verapamil, cyclosporin) or substrates, CYP2B6 substrates (bupropion, efavirenz, cyclophosphamide), digoxin.
Advice to Patient
Take with or without meals. Swallow tablets whole, do not chew, crush or break them. Reduce intake of grapefruit and grapefruit juice during treatment.
Pharmacokinetics
Absorption: Highly variable. Metabolism: Extensive, hepatic, intestines. Bioavailability: Tab: 76% (compared to solution). Half-life elimination: Ranolazine: Terminal: 7 hrs. Metabolites: 6-22 hrs. Time to peak, plasma: 2-5 hrs. Excretion: Primarily urine, faeces.
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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