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QuickView for Ranolazine (compound)

Name: ranolazine
PubChem Compound ID: 56959
Molecular formula: C24H33N3O4
Molecular weight: 427.537 g/mol
RS-43285; RAN D; KEG-1295; 142387-99-3; 1-Piperazineacetamide, N-(2,6-dimethylphenyl)-4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)-; Ranolazine; ( -)-Ranolazine; Ran4; RS-43285-003; Ranexa.
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Name: ranolazine
Name (isomeric): DB00243
Drug Type: small molecule
Ranolazine 2HCl; Ranolazine Dihydrochloride; (-)-Ranolazine
Brand: Ranexa
Category: Enzyme Inhibitors
CAS number: 142387-99-3
Indication: For the treatment of chronic angina. It should be used in combination with amlodipine, beta-blockers or nitrates.
Pharmacology: Ranolazine has antianginal and anti-ischemic effects that do not depend upon reductions in heart rate or blood pressure. It is the first new anti-anginal developed in over 20 years.
Mechanism of Action:
The mechanism of action of ranolazine is unknown. It does not increase the rate-pressure product, a measure of myocardial work, at maximal exercise. In vitro studies suggest that ranolazine is a P-gp inhibitor. Ranolazine is believed to have its effects via altering the trans-cellular late sodium current. It is by altering the intracellular sodium ...
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Absorption: Absorption is highly variable. After oral administration of ranolazine as a solution, 73% of the dose is systemically available as ranolazine or metabolites. The bioavailability of oral ranolazine relative to that from a solution is 76%.
Protein binding: 62%
Biotransformation: Hepatic, metabolized mainly by CYP3A and to a lesser extent by CYP2D6. The pharmacologic activity of the metabolites has not been well characterized.
Route of elimination: Ranolazine is metabolized rapidly and extensively in the liver and intestine; less than 5% is excreted unchanged in urine and feces.
Half Life: 7 hours
Toxicity: In the event of overdose, the expected symptoms would be dizziness, nausea/vomiting, diplopia, paresthesia, and confusion. Syncope with prolonged loss of consciousness may develop.
Affected organisms: Humans and other mammals
Food interaction:
Grapefruit and grapefruit juice should be avoided throughout treatment.
Take without regard to meals.
Drug interaction:
TramadolRanolazine may decrease the effect of Tramadol by decreasing active metabolite production.
NelfinavirIncreased levels of ranolazine - risk of toxicity
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ranolazine by decreasing its metabolism. Additive QTc prolongation may also occur. Concomitant therapy is contraindicated.
AmiodaronePossible additive effect on QT prolongation
AmprenavirAmprenavir, a strong CYP3A4 inhibitor, may increase the serum concentratin of ranolazine by inhibiting its metabolism. Concomitant therapy is contraindicated.
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