Ranolazine

Drug Overview

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drug details
nameRanolazine
classificationAntianginal, Anti-ischemic agent
pharmacokinetics
absorptionRanolazine is absorbed from the gastrointestinal tract with variable absorption, with peak plasma concentrations occurring 2 to 6 hours after oral administration.
distributionRanolazine is highly protein bound, primarily to albumin.
metabolismRanolazine is extensively metabolized in the liver by CYP3A4, and to a lesser extent by CYP2D6 and CYP1A2.
excretionRanolazine and its metabolites are primarily excreted in the urine. The elimination half-life is prolonged in patients with hepatic impairment.
dosage
initial dosageGenerally started at 500 mg twice daily, titrated up to a maximum of 1000 mg twice daily, aiming for a target steady-state trough concentration of 100-200 ng/mL.
adult dosageDosage must be individualized based on response and adverse effects. Consult a healthcare professional for appropriate dosage.
important noteDosage adjustments may be necessary in patients with hepatic or renal impairment.
indicationsRanolazine is used for the treatment of chronic angina, particularly when other treatments (beta-blockers, calcium channel blockers, nitrates) are ineffective or not tolerated.
safety in pregnancyPregnancy Category C. Limited data exist. Potential risks and benefits must be carefully considered by the prescribing physician. Use should be avoided unless clearly necessary.
safety in breastfeedingIt is unknown if ranolazine is excreted in breast milk. Use is not recommended due to potential risks to the infant.
side effects
1Headache
2Dizziness
3Constipation
4Nausea
5Vomiting
6Diarrhea
7Abdominal pain
8Vertigo
9Edema
10Lightheadedness
11Sleep disturbances
12Increased heart rate
13Heart palpitations
14Increased blood pressure
15Hypotension
16Arrhythmias
17Serious cardiac events
18Elevated liver enzymes
alternatives
1Nitrates
2Beta-blockers
3Calcium channel blockers
4Ivabradine
contraindications
1Severe hepatic impairment
2Severe renal impairment (creatinine clearance <30 mL/min)
3Hypersensitivity to ranolazine
4Concomitant use with strong CYP3A4 inhibitors
5Severe hypotension
6Recent stroke or transient ischemic attack
7Known drug-induced long QT syndrome
drug interactionsRanolazine interacts with many medications, particularly those metabolized by CYP3A4. Careful monitoring and dosage adjustments may be necessary. A thorough medication reconciliation is crucial.
warnings and precautions
1Monitor ECG for QTc interval prolongation, especially during initial treatment or dose changes.
2Regular liver function tests are recommended during treatment.
3Patients with pre-existing cardiac conditions may require careful monitoring and dose adjustments.
4Caution is advised in patients with renal impairment or a history of QT prolongation.
5Avoid alcohol consumption while taking this medication.
additional informations
age considerationsDosage and monitoring should be carefully evaluated by a healthcare professional, considering the patient's age and overall health.
weight considerationsWeight is not a primary factor in adjusting the dosage, but overall health, including organ function, will be considered.
special instructionsDo not discontinue use without consulting your healthcare provider.
important disclaimerThis information is for educational purposes only and should not be substituted for professional medical advice. Always consult a healthcare provider before starting or changing any medication.

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