Ranolazine

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Ranolazine API

 

Haorui supplies high quality Ranolazine API produced by our GMP facility that has been successfully inspected by the FDA. We offer competitive prices and support our products with reliable technical and regulatory services.  Ranolazine API is available from R&D to commercial quantities. Please contact us for more details.

The following information is provided for general information purposes ONLY.

Ranolazine Description

Ranolazine is available as a film-coated, non-scored, extended-release tablet for oral administration.

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, a molecular weight of 427.54 g/mole, and the following structural formula:

Ranexa
  (ranolazine) Structural Formula Illustration

Ranolazine is a white to off-white solid. Ranolazine is soluble in dichloromethane and methanol; sparingly soluble in tetrahydrofuran, ethanol, acetonitrile, and acetone; slightly soluble in ethyl acetate, isopropanol, toluene, and ethyl ether; and very slightly soluble in water.

Ranolazine tablets contain 500 mg or 1000 mg of ranolazine and the following inactive ingredients: carnauba wax, hypromellose, magnesium stearate, methacrylic acid copolymer (Type C), microcrystalline cellulose, polyethylene glycol, sodium hydroxide, and titanium dioxide. Additional inactive ingredients for the 500 mg tablet include polysorbate 80 and FD&C Yellow No. 6 Lake; additional inactive ingredients for the 1000 mg tablet include lactose monohydrate, triacetin, and Iron Oxide Yellow.

Ranolazine 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.

Ranolazine Dosage and Administration

                                         Dosing Information

Initiate Ranolazine dosing at 500 mg twice daily and increase to 1000 mg twice daily, as 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.

                                          Dose Modification

Dose adjustments may be needed when Ranolazine is taken in combination with certain other drugs. Limit the maximum dose of Ranolazine to 500 mg twice daily in patients on diltiazem, verapamil, and other moderate CYP3A inhibitors. Down-titrate Ranolazine based on clinical response in patients concomitantly treated with P-gp inhibitors, such as cyclosporine.

Ranolazine Side Effects

                                         Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

A total of 2,018 patients with chronic angina were treated with ranolazine in controlled clinical trials. Of the patients treated with Ranolazine, 1,026 were enrolled in three double-blind, placebo-controlled, randomized studies (CARISA, ERICA, MARISA) of up to 12 weeks duration. In addition, upon study completion, 1,251 patients received treatment with Ranolazine in open-label, long-term studies; 1,227 patients were exposed to Ranolazine for more than 1 year, 613 patients for more than 2 years, 531 patients for more than 3 years, and 326 patients for more than 4 years.

At recommended doses, about 6% of patients discontinued treatment with Ranolazine because of an adverse event in controlled studies in angina patients compared to about 3% on placebo. The most common adverse events that led to discontinuation more frequently on Ranolazine than placebo were dizziness (1.3% versus 0.1%), nausea (1% versus 0%), asthenia, constipation, and headache (each about 0.5% versus 0%). Doses above 1000 mg twice daily are poorly tolerated.

In controlled clinical trials of angina patients, the most frequently reported treatment-emergent adverse reactions ( > 4% and more common on Ranolazine than on placebo) were dizziness (6.2%), headache (5.5%), constipation (4.5%), and nausea (4.4%). Dizziness may be dose-related. In open-label, long-term treatment studies, a similar adverse reaction profile was observed.

Ranolazine Clinical Trials 1

Ranolazine Patents 1

Ranolazine Patents 2

Ranolazine Patents 1

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