Ranolazine

Ranolazine is used as an adjunctive anti-anginal treatment for patient with symptomatic stable angina pectoris who are inadequately controlled or intolerant to first-line anti-anginal tharapies. Ranolazine is a racemic mixture, chemically described as 1-piperazineacetamide, N-(2,6dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-, (±)-. It has an empirical formula of C24H33N3O4. The mechanism of action of ranolazine''s antianginal effects has not been determined. Ranolazine has anti-ischemic and antianginal effects that do not depend upon reductions in heart rate or blood pressure. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). However, the relationship of this inhibition to angina symptoms is uncertain.'

Brands
RAZIN ER RANOLA RANOLA RANZOL
Adult Dose
Dose: 500 to 1000 mg
Single Dose: 750 (750)
Frequency: 12 hourly
Route: oral
Instructions: May be taken with or without food. Dose adjustments may be needed when taken with other drugs.
Neonatal
Paedriatic
Characteristics
It belongs to Anti anginal pharmacological group.The Molecular Weight of Ranolazine is 427.54. Its pKa is 14.25.
Contraindications
Ranolazine is contraindicated in conditions like Hypokalaemia,Ventricular tachycardia,Severe renal impairment,Hypomagnesaemia,Hepatic impairment,Acute myocardial infarction.
Effects
The severe or irreversible adverse effects of Ranolazine, which give rise to further complications include Pulmonary fibrosis, Hematuria, Blurred vision, Tremors, QT prolongation.The signs and symptoms that are produced after the acute overdosage of Ranolazine include Nausea, Vomiting, Confusion, Dizziness, Paresthesia, Syncope.The symptomatic adverse reactions produced by Ranolazine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Vertigo, Headache, Nausea, Vomiting, Tinnitus, Abdominal pain, Dry mouth, Asthenia.
Indications
Ranolazine is primarily indicated in conditions like Angina, Stable angina.
Interactions
Ranolazine is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementDigoxinRanolazine (1000 mg twice daily) causes a 1.5-fold elevation of digoxin plasma concentrations. The dose of digoxin may have to be adjusted.KetoconazoleKetoconazole (200 mg twice daily) increases average steady-state plasma concentrations of ranolazine 3.2-fold [seeDo not use (ranolazine) with strong CYP3A inhibitors, including ketoconazole, itraconazole, clarithromycin, nefazodone, nelfinavir, ritonavir, indinavir, and saquinavir.Metoprolol (Tartrate)Ranolazine 750 mg twice daily increased the plasma concentrations of a single dose of immediate-release metoprolol (100 mg), a CYP2D6 substrate, by 1.8-fold. The exposure to other CYP2D6 substrates, such as tricyclic antidepressants and antipsychotics, may be increased during coadministration with ranolazine, and lower doses of these drugs may be requiredParoxetineCoadministration with ranolazine may increase the plasma concentrations of drugs that are substrates of the CYP450 2D6 isoenzyme. Ranolazine has been shown in vitro to be an inhibitor of CYP450 2D6. However, concomitant use of ranolazine with other drugs that are metabolized by CYP450 2D6 such as tricyclic antidepressants and antipsychotics has not been studied.Caution is advised if ranolazine must be used concurrently with medications that undergo metabolism by CYP450 2D6, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever ranolazine is added to or withdrawn from therapy.RifampicinRifampin (600 mg once daily) decreases the plasma concentration of ranolazine (1000 mg twice daily) by approximately 95% by induction of CYP3A and, probably, P-gp.Avoid co-administration of ranolazinen and CYP3A inducers such as rifampin, rifabutin, rifapentin, phenobarbital, phenytoin and carbamazepine.Verapamil (HCl)Diltiazem (180€“360 mg daily) and verapamil (120 mg three times daily) increase ranolazine steady-state plasma concentrations about 2-foldLimit the dose of ranolazine to 500 mg twice daily in patients on moderate CYP3A inhibitors, including diltiazem, verapamil, aprepitant, erythromycin, fluconazole, and grapefruit juice or grapefruit-containing products.VORICONAZOLEVoriconazole may increase the serum concentration of ranolazine by decreasing its metabolism. Concomitant therapy is contraindicated. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Liver Malfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
tablet Store Between 15°C-30°C.
Warnings
Safety not established in pediatric patients. Ranolazine concentration increases 30% and 60% in in patients with mild and moderate hepatic impairment. Take with caution in patients with renal impairment as its concentration increases upto 50% in patients with varying degree of renal impairment. There are no adequate well-controlled studies in pregnant women. Ranolazine should be used during pregnancy only when the potential benefit to the patient justifies the potential risk to the fetus.
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