Ranolazine
Therapeutic Class: Cardiovascular (Other Anti-anginal & Anti-ischaemic drugs)
Indications:
Ranolazine is indicated for the treatment of chronic angina. Ranolazine may be used with beta-blockers, nitrates, calcium channel blockers, anti-platelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers.
Presentation:
Ranolazine 500 SR tablet: Each film-coated sustained release tablet contains Ranolazine INN 500 mg.
Description:
Ranolazine has anti-ischemic and anti-angina effects that do not depend upon reduction in heart rate or blood pressure. It does not affect the rate pressure product, a measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). Thereby it causes a decreased influx of Ca++ through the Na+-Ca++ channel. Thus, it inhibits Ca++ overload and decreases oxygen consumption of the heart.
Dosage & Administration:
Initiate Ranolazine dosing at 500 mg twice daily and increase to 1000 mg twice daily, if needed, based on clinical symptoms. Take Ranolazine with or without meals. Swallow Ranolazine tablets whole; do not crush, break or chew. The maximum recommended daily dose of Ranolazine is 1000 mg twice daily. If a dose of Ranolazine is missed, take the prescribed dose at the next scheduled time; do not double the next dose.
Side Effects:
Cardiac Disorders - bradycardia, palpitations
Ear and Labyrinth Disorders - tinnitus, vertigo
Gastrointestinal Disorders - abdominal pain, dry mouth, vomiting
General Disorders and Administrative Site Adverse Events - peripheral oedema
Respiratory, Thoracic, and Mediastinal Disorders - dyspnea
Vascular Disorders - hypotension, orthostatic hypotension
Precautions:
Heart rhythm problems (e.g., bradycardia, QT prolongation, ventricular tachycardia), liver problems, certain uncorrected mineral imbalances (low potassium/magnesium levels), severe kidney problems.
Use in Pregnancy & Lactation:
Pregnancy Category C
Interaction:
Inhibitors of CYP3A (e.g., ketoconazole, clarithromycin, nelfinavir)
Inducers of CYP3A (e.g., phenobarbital, rifampicin)
P-GP inhibitors (e.g., cyclosporine)
Drug transported by P-GP or metabolized by CYP2D6 (e.g., Digoxin, TCA, etc.)
Ranolazine is indicated for the treatment of chronic angina. Ranolazine may be used with beta-blockers, nitrates, calcium channel blockers, anti-platelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers.
Presentation:
Ranolazine 500 SR tablet: Each film-coated sustained release tablet contains Ranolazine INN 500 mg.
Description:
Ranolazine has anti-ischemic and anti-angina effects that do not depend upon reduction in heart rate or blood pressure. It does not affect the rate pressure product, a measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). Thereby it causes a decreased influx of Ca++ through the Na+-Ca++ channel. Thus, it inhibits Ca++ overload and decreases oxygen consumption of the heart.
Dosage & Administration:
Initiate Ranolazine dosing at 500 mg twice daily and increase to 1000 mg twice daily, if needed, based on clinical symptoms. Take Ranolazine with or without meals. Swallow Ranolazine tablets whole; do not crush, break or chew. The maximum recommended daily dose of Ranolazine is 1000 mg twice daily. If a dose of Ranolazine is missed, take the prescribed dose at the next scheduled time; do not double the next dose.
Side Effects:
Cardiac Disorders - bradycardia, palpitations
Ear and Labyrinth Disorders - tinnitus, vertigo
Gastrointestinal Disorders - abdominal pain, dry mouth, vomiting
General Disorders and Administrative Site Adverse Events - peripheral oedema
Respiratory, Thoracic, and Mediastinal Disorders - dyspnea
Vascular Disorders - hypotension, orthostatic hypotension
Precautions:
Heart rhythm problems (e.g., bradycardia, QT prolongation, ventricular tachycardia), liver problems, certain uncorrected mineral imbalances (low potassium/magnesium levels), severe kidney problems.
Use in Pregnancy & Lactation:
Pregnancy Category C
Interaction:
Inhibitors of CYP3A (e.g., ketoconazole, clarithromycin, nelfinavir)
Inducers of CYP3A (e.g., phenobarbital, rifampicin)
P-GP inhibitors (e.g., cyclosporine)
Drug transported by P-GP or metabolized by CYP2D6 (e.g., Digoxin, TCA, etc.)
Store Ranolazine tablets at 25°C with excursion permitted to 15° to 30°C. Protect from light and moisture.
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