Ralozine SR 500 mg (Tablet (Sustained Release))

Indications

• Treatment of chronic angina
• May be used with beta-blockers, nitrates, calcium channel blockers, anti-platelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers
• Decreases angina episodes in patients with coronary artery disease on maximal doses of amlodipine
• Prolongs the QT interval
• Effect on angina rate or exercise tolerance may differ in women

Pharmacology

• Anti-ischemic and anti-anginal effects
• Does not depend upon reductions in heart rate or blood pressure
• Inhibition of cardiac late sodium current (I_Na)
• Inhibition of I_Kr prolongs the ventricular action potential
• Absorption: C_max - 2-5 hours
• Half-life: 6-22 hours
• Approximately 62% bound to human plasma proteins
• Metabolized mainly by CYP3A and to a lesser extent by CYP2D6
• Metabolized rapidly and extensively in the liver and intestine
• Approximately 75% of the dose excreted in urine and 25% in feces

Dosage & Administration

• Initiate dosing at 500 mg twice daily
• Increase to 1000 mg twice daily if needed
• Swallow tablets whole; do not crush, break or chew
• Maximum recommended daily dose is 1000 mg twice daily
• Pediatric use: Safety and effectiveness not established

Interaction

• Do not use with strong CYP 3A inhibitors
• Limit maximum dose with moderate CYP 3A inhibitors
• Do not use with inducers
• May need to lower the dose with P-gp inhibitors
• May need reduced doses of drugs transported by P-gp or metabolized by CYP2D6 when used together

Contraindications

• With pre-existing QT prolongation
• With hepatic impairment
• Taking QT prolonging drugs
• Taking potent and moderately potent CYP3A inhibitors

Side Effects

• Bradycardia
• Palpitations
• Tinnitus
• Vertigo
• Abdominal pain
• Dry mouth
• Vomiting
• Peripheral edema
• Dyspnea
• Hypotension
• Orthostatic hypotension

Pregnancy & Lactation

• Pregnancy Category C
• No adequate studies on the effect on the developing fetus
• No well-controlled studies in pregnant women
• Use during pregnancy only if potential benefit justifies potential risk to the fetus
• Not known whether excreted in human milk
• Consideration should be made to discontinue nursing or the drug, taking into account the importance of the drug to the mother

Precautions & Warnings

• Blocks QTc and prolongs the QTc interval in a dose-related manner
• Clinical experience did not show increased risk of proarrhythmia or sudden death
• Co-administration with digoxin increases plasma concentrations of digoxin
• Caution should be exercised when co-administering with P-gp inhibitors

Overdose Effects

• Dose-related increases in dizziness, nausea, and vomiting with high oral doses
• Diplopia, paresthesia, confusion, and syncope with high intravenous exposure
• General supportive measures and continuous ECG monitoring may be warranted in overdose
• Unlikely to be effectively cleared by hemodialysis

Therapeutic Class

• Other Anti-anginal & Anti-ischaemic drugs

Storage Conditions

• Keep below 30°C temperature
• Away from light & moisture
• Keep out of the reach of children

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