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Identification
NameRanolazine
Accession NumberDB00243  (APRD01300)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Ranolazine is an antianginal medication. On January 31, 2006, ranolazine was approved for use in the United States by the FDA for the treatment of chronic angina. [Wikipedia]

Structure
Thumb
SynonymsNot Available
External Identifiers
  • CVT-303
  • RS-43285-003
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ranexatablet, film coated, extended release500 mg/1oralCardinal Health2007-02-12Not applicableUs
Ranexatablet, film coated, extended release500 mg/1oralCarilion Materials Management2006-01-27Not applicableUs
Ranexatablet, film coated, extended release1000 mg/1oralGilead Sciences, Inc.2007-02-12Not applicableUs
Ranexatablet, film coated, extended release500 mg/1oralGilead Sciences, Inc.2006-01-27Not applicableUs
Ranexatablet, film coated, extended release1000 mg/1oralGilead Sciences, Inc.2007-02-12Not applicableUs
Ranexatablet, film coated, extended release500 mg/1oralGilead Sciences, Inc.2006-01-27Not applicableUs
Ranexatablet, film coated, extended release500 mg/1oralCardinal Health2006-01-27Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Ranolazine hydrochloride
95635-56-6
Thumb
  • InChI Key: RJNSNFZXAZXOFX-UHFFFAOYSA-N
  • Monoisotopic Mass: 499.200462037
  • Average Mass: 500.458
DBSALT000388
Categories
UNIIA6IEZ5M406
CAS number95635-55-5
WeightAverage: 427.5365
Monoisotopic: 427.247106559
Chemical FormulaC24H33N3O4
InChI KeyInChIKey=XKLMZUWKNUAPSZ-UHFFFAOYSA-N
InChI
InChI=1S/C24H33N3O4/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3/h4-10,20,28H,11-17H2,1-3H3,(H,25,29)
IUPAC Name
N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide
SMILES
COC1=CC=CC=C1OCC(O)CN1CCN(CC(=O)NC2=C(C)C=CC=C2C)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentAlpha amino acid amides
Alternative Parents
Substituents
  • Alpha-amino acid amide
  • N-arylamide
  • N-piperazineacetamide
  • Methoxybenzene
  • Phenol ether
  • Anisole
  • N-alkylpiperazine
  • Alkyl aryl ether
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Monocyclic benzene moiety
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • Carboxamide group
  • 1,2-aminoalcohol
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of chronic angina. It should be used in combination with amlodipine, beta-blockers or nitrates.
PharmacodynamicsRanolazine 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 actionThe 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 level that ranolazine affects the sodium-dependent calcium channels during myocardial ischemia. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia.
Related Articles
AbsorptionAbsorption 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%.
Volume of distributionNot Available
Protein binding62%
Metabolism

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 eliminationRanolazine is metabolized rapidly and extensively in the liver and intestine; less than 5% is excreted unchanged in urine and feces.
Half life7 hours
ClearanceNot Available
ToxicityIn 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.7425
Blood Brain Barrier-0.5334
Caco-2 permeable-0.5853
P-glycoprotein substrateSubstrate0.8667
P-glycoprotein inhibitor IInhibitor0.7566
P-glycoprotein inhibitor IIInhibitor0.7524
Renal organic cation transporterNon-inhibitor0.7648
CYP450 2C9 substrateNon-substrate0.7965
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7456
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.8287
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8155
Ames testNon AMES toxic0.8529
CarcinogenicityNon-carcinogens0.9128
BiodegradationNot ready biodegradable0.9936
Rat acute toxicity2.3256 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8753
hERG inhibition (predictor II)Inhibitor0.8775
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Gilead sciences inc
Packagers
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseoral1000 mg/1
Tablet, film coated, extended releaseoral500 mg/1
Prices
Unit descriptionCostUnit
Ranexa 1000 mg 12 Hour tablet6.89USD tablet
Ranexa 1000 mg tablet6.63USD tablet
Ranexa 500 mg 12 Hour tablet4.06USD tablet
Ranexa 500 mg tablet4.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6303607 No1999-05-272019-05-27Us
US6369062 No1999-05-272019-05-27Us
US6479496 No1999-05-272019-05-27Us
US6503911 No1999-05-272019-05-27Us
US6525057 No1999-05-272019-05-27Us
US6562826 No1999-05-272019-05-27Us
US6617328 No1999-05-272019-05-27Us
US6620814 No1999-05-272019-05-27Us
US6852724 No1999-05-272019-05-27Us
US6864258 No1999-05-272019-05-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityVery slightly solubleNot Available
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.11 mg/mLALOGPS
logP2.08ALOGPS
logP2.83ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)13.6ChemAxon
pKa (Strongest Basic)7.17ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area74.27 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity123.46 m3·mol-1ChemAxon
Polarizability47.22 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Raghupathi Reddy Anumula, Goverdhan Gilla, Sampath Aalla, Lokeswara Rao Madivada, Prabhaker Macherla, Srinivas Kurella, Kavitha Charagondla, Ramamurthy Kasula, Rajagopala Rao Mandadapu, Krishaniah Charagondla, Malati Vakamulla, Durga Prasad Janaki Bhavanipurapu, “PREPARATION OF RANOLAZINE.” U.S. Patent US20110151258, issued June 23, 2011.

US20110151258
General References
  1. Hale SL, Kloner RA: Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit. J Cardiovasc Pharmacol Ther. 2006 Dec;11(4):249-55. [PubMed:17220471 ]
  2. Fraser H, Belardinelli L, Wang L, Light PE, McVeigh JJ, Clanachan AS: Ranolazine decreases diastolic calcium accumulation caused by ATX-II or ischemia in rat hearts. J Mol Cell Cardiol. 2006 Dec;41(6):1031-8. Epub 2006 Oct 5. [PubMed:17027025 ]
  3. Stone PH, Gratsiansky NA, Blokhin A, Huang IZ, Meng L: Antianginal efficacy of ranolazine when added to treatment with amlodipine: the ERICA (Efficacy of Ranolazine in Chronic Angina) trial. J Am Coll Cardiol. 2006 Aug 1;48(3):566-75. Epub 2006 Jun 15. [PubMed:16875985 ]
  4. Chaitman BR, Pepine CJ, Parker JO, Skopal J, Chumakova G, Kuch J, Wang W, Skettino SL, Wolff AA: Effects of ranolazine with atenolol, amlodipine, or diltiazem on exercise tolerance and angina frequency in patients with severe chronic angina: a randomized controlled trial. JAMA. 2004 Jan 21;291(3):309-16. [PubMed:14734593 ]
  5. Morrow DA, Scirica BM, Karwatowska-Prokopczuk E, Murphy SA, Budaj A, Varshavsky S, Wolff AA, Skene A, McCabe CH, Braunwald E: Effects of ranolazine on recurrent cardiovascular events in patients with non-ST-elevation acute coronary syndromes: the MERLIN-TIMI 36 randomized trial. JAMA. 2007 Apr 25;297(16):1775-83. [PubMed:17456819 ]
External Links
ATC CodesC01EB18
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (203 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Ranolazine can be increased when it is combined with Abiraterone.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Ranolazine.
AliskirenThe serum concentration of Aliskiren can be increased when it is combined with Ranolazine.
AprepitantThe serum concentration of Ranolazine can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Ranolazine.
AtazanavirThe serum concentration of Ranolazine can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Ranolazine.
AzithromycinThe serum concentration of Ranolazine can be increased when it is combined with Azithromycin.
BexaroteneThe serum concentration of Ranolazine can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Ranolazine can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Ranolazine can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Ranolazine.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Ranolazine.
CarbamazepineThe serum concentration of Ranolazine can be decreased when it is combined with Carbamazepine.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Ranolazine.
CarvedilolThe serum concentration of Ranolazine can be increased when it is combined with Carvedilol.
CeritinibThe serum concentration of Ranolazine can be increased when it is combined with Ceritinib.
CetirizineThe serum concentration of Cetirizine can be increased when it is combined with Ranolazine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Ranolazine.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Ranolazine.
CitalopramRanolazine may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Ranolazine can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Ranolazine can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Ranolazine.
ConivaptanThe serum concentration of Ranolazine can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Ranolazine can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Ranolazine can be increased when it is combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Ranolazine.
DabrafenibThe serum concentration of Ranolazine can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Ranolazine can be increased when it is combined with Daclatasvir.
DarunavirThe serum concentration of Ranolazine can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Ranolazine can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Ranolazine.
DeferasiroxThe serum concentration of Ranolazine can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Ranolazine can be increased when it is combined with Delavirdine.
DesloratadineThe serum concentration of Desloratadine can be increased when it is combined with Ranolazine.
DexamethasoneThe serum concentration of Ranolazine can be decreased when it is combined with Dexamethasone.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Ranolazine.
DiltiazemThe serum concentration of Ranolazine can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Ranolazine can be increased when it is combined with Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Ranolazine.
DofetilideRanolazine may increase the QTc-prolonging activities of Dofetilide.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Ranolazine.
DronedaroneThe serum concentration of Ranolazine can be increased when it is combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Ranolazine.
EfavirenzThe serum concentration of Ranolazine can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Ranolazine can be decreased when it is combined with Enzalutamide.
ErythromycinThe serum concentration of Ranolazine can be increased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Ranolazine can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Ranolazine.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Ranolazine.
EtravirineThe serum concentration of Ranolazine can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Ranolazine.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Ranolazine.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Ranolazine.
FluconazoleThe serum concentration of Ranolazine can be increased when it is combined with Fluconazole.
FosamprenavirThe serum concentration of Ranolazine can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Ranolazine can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Ranolazine can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Ranolazine can be increased when it is combined with Fusidic Acid.
GoserelinRanolazine may increase the QTc-prolonging activities of Goserelin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Ranolazine.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Ranolazine.
IbrutinibThe serum concentration of Ranolazine can be increased when it is combined with Ibrutinib.
IdarubicinThe serum concentration of Idarubicin can be increased when it is combined with Ranolazine.
IdelalisibThe serum concentration of Ranolazine can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Ranolazine can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Ranolazine can be increased when it is combined with Indinavir.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Ranolazine.
IsavuconazoniumThe serum concentration of Ranolazine can be increased when it is combined with Isavuconazonium.
ItraconazoleThe metabolism of Ranolazine can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Ranolazine can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Ranolazine.
KetoconazoleThe metabolism of Ranolazine can be decreased when combined with Ketoconazole.
LapatinibThe serum concentration of Ranolazine can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Ranolazine.
LeuprolideRanolazine may increase the QTc-prolonging activities of Leuprolide.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Ranolazine.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Ranolazine.
LoratadineThe serum concentration of Loratadine can be increased when it is combined with Ranolazine.
LovastatinRanolazine may increase the myopathic rhabdomyolysis activities of Lovastatin.
LuliconazoleThe serum concentration of Ranolazine can be increased when it is combined with Luliconazole.
MefloquineThe serum concentration of Ranolazine can be increased when it is combined with Mefloquine.
MetforminThe serum concentration of Metformin can be increased when it is combined with Ranolazine.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Ranolazine.
MifepristoneThe serum concentration of Ranolazine can be increased when it is combined with Mifepristone.
MirabegronThe serum concentration of Ranolazine can be increased when it is combined with Mirabegron.
MitomycinThe serum concentration of Mitomycin can be increased when it is combined with Ranolazine.
MitotaneThe serum concentration of Ranolazine can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Ranolazine can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Ranolazine.
NadololThe serum concentration of Nadolol can be increased when it is combined with Ranolazine.
NafcillinThe serum concentration of Ranolazine can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Ranolazine.
NefazodoneThe serum concentration of Ranolazine can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Ranolazine can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Ranolazine can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Ranolazine can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Ranolazine.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Ranolazine.
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Ranolazine.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Ranolazine.
PalbociclibThe serum concentration of Ranolazine can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Ranolazine.
PhenobarbitalThe serum concentration of Ranolazine can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Ranolazine can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Ranolazine.
PosaconazoleThe metabolism of Ranolazine can be decreased when combined with Posaconazole.
PrimidoneThe serum concentration of Ranolazine can be decreased when it is combined with Primidone.
ProgesteroneThe serum concentration of Ranolazine can be increased when it is combined with Progesterone.
PropranololThe serum concentration of Ranolazine can be increased when it is combined with Propranolol.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Ranolazine.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Ranolazine.
ReserpineThe serum concentration of Ranolazine can be increased when it is combined with Reserpine.
RifabutinThe serum concentration of Ranolazine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Ranolazine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Ranolazine can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Ranolazine.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Ranolazine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Ranolazine.
RitonavirThe serum concentration of Ranolazine can be increased when it is combined with Ritonavir.
RolapitantThe serum concentration of Ranolazine can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Ranolazine can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Ranolazine.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Ranolazine.
SiltuximabThe serum concentration of Ranolazine can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Ranolazine can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Ranolazine.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Ranolazine.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Ranolazine.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Ranolazine.
St. John's WortThe serum concentration of Ranolazine can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Ranolazine can be increased when it is combined with Stiripentol.
SunitinibThe serum concentration of Ranolazine can be increased when it is combined with Sunitinib.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Ranolazine.
TamoxifenThe serum concentration of Ranolazine can be increased when it is combined with Tamoxifen.
TelaprevirThe serum concentration of Ranolazine can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Ranolazine can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Ranolazine.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Ranolazine.
TesmilifeneThe serum concentration of Ranolazine can be decreased when it is combined with Tesmilifene.
TocilizumabThe serum concentration of Ranolazine can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Ranolazine.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Ranolazine.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Ranolazine.
VerapamilThe serum concentration of Ranolazine can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Ranolazine.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Ranolazine.
VoriconazoleThe metabolism of Ranolazine can be decreased when combined with Voriconazole.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function:
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is respon...
Gene Name:
SCN5A
Uniprot ID:
Q14524
Molecular Weight:
226937.475 Da
References
  1. Hale SL, Kloner RA: Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit. J Cardiovasc Pharmacol Ther. 2006 Dec;11(4):249-55. [PubMed:17220471 ]
  2. Rajamani S, Shryock JC, Belardinelli L: Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine. Channels (Austin). 2008 Nov-Dec;2(6):449-60. Epub 2008 Nov 7. [PubMed:19077543 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated sodium channel activity
Specific Function:
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, es...
Gene Name:
SCN9A
Uniprot ID:
Q15858
Molecular Weight:
226370.175 Da
References
  1. Rajamani S, Shryock JC, Belardinelli L: Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine. Channels (Austin). 2008 Nov-Dec;2(6):449-60. Epub 2008 Nov 7. [PubMed:19077543 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
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Drug created on June 13, 2005 07:24 / Updated on June 30, 2016 01:50