ranolazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	2359	95635-55-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ranolazine hydrochloride ranolazine ranexa renexa ranolazine HCl	An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS. Molecular weight: 427.55 Formula: C24H33N3O4 CLOGP: 1.01 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 74.27 ALOGS: -3.59 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ranolazine hydrochloride
ranolazine
ranexa
renexa
ranolazine HCl

An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.

Molecular weight: 427.55
Formula: C24H33N3O4
CLOGP: 1.01
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 74.27
ALOGS: -3.59
ROTB: 9

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1.50	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	42.50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.80 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.38 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Jan. 27, 2006	FDA	GILEAD

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Electrocardiogram QT prolonged	125.91	18.03	82	7509	59448	63421983
Bradycardia	110.55	18.03	82	7509	73145	63408286
Chest pain	89.22	18.03	119	7472	215840	63265591
Tonic clonic movements	65.95	18.03	18	7573	1417	63480014
Torsade de pointes	65.60	18.03	32	7559	13319	63468112
Dizziness	62.69	18.03	150	7441	429775	63051656
Angina pectoris	62.47	18.03	41	7550	30037	63451394
Drug interaction	55.92	18.03	99	7492	229032	63252399
Chromaturia	45.33	18.03	27	7564	16690	63464741
Stent placement	45.25	18.03	17	7574	3738	63477693

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Chest pain	154.52	18.63	184	9663	126578	34820506
Dizziness	149.76	18.63	240	9607	218281	34728803
Syncope	86.24	18.63	117	9730	91334	34855750
Angina pectoris	79.79	18.63	68	9779	31295	34915789
Drug interaction	78.97	18.63	187	9660	225759	34721325
Stent placement	59.74	18.63	29	9818	5049	34942035
Coronary artery disease	55.16	18.63	68	9779	48237	34898847
Dyspnoea	54.02	18.63	229	9618	376553	34570531
Rhabdomyolysis	45.19	18.63	74	9773	68089	34878995
Chromaturia	42.14	18.63	34	9813	14486	34932598

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Chest pain	196.36	16.13	250	14405	282054	79447679
Dizziness	157.64	16.13	317	14338	526124	79203609
Electrocardiogram QT prolonged	134.27	16.13	120	14535	90266	79639467
Drug interaction	131.30	16.13	256	14399	414927	79314806
Bradycardia	123.59	16.13	138	14517	135419	79594314
Angina pectoris	119.78	16.13	89	14566	51643	79678090
Syncope	109.15	16.13	149	14506	179300	79550433
Stent placement	101.57	16.13	40	14615	6480	79723253
Coronary artery disease	91.44	16.13	84	14571	65390	79664343
Hypotension	65.14	16.13	203	14452	440114	79289619

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C01EB18	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Other cardiac preparations
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:38633	sodium channel blockers
FDA EPC	N0000175427	Anti-anginal
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Angina pectoris	indication	194828000
Cirrhosis of liver	contraindication	19943007	DOID:5082
Torsades de pointes	contraindication	31722008
Kidney disease	contraindication	90708001	DOID:557
Prolonged QT interval	contraindication	111975006
Congenital long QT syndrome	contraindication	442917000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.4	acidic
pKa2	6.91	Basic
pKa3	2.91	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	IC50	5.17	CHEMBL	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.92	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Voltage-gated sodium channel Nav1.5 cardiac isoform	Unclassified		Q5YLN7_CANLF		IC50	5.16	CHEMBL

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External reference:

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ID	Source
011195	NDDF
20936	MMSL
309260	MMSL
356778	RXNORM
4025078	VUID
4025078	VANDF
420365007	SNOMEDCT_US
420624001	SNOMEDCT_US
56959	PUBCHEM_CID
5946	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ASPRUZYO SPRINKLE	HUMAN PRESCRIPTION DRUG LABEL	1	47335-624	GRANULE	500 mg	ORAL	NDA	26 sections
ASPRUZYO SPRINKLE	HUMAN PRESCRIPTION DRUG LABEL	1	47335-625	GRANULE	1000 mg	ORAL	NDA	26 sections
Ranexa	HUMAN PRESCRIPTION DRUG LABEL	1	43353-880	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	NDA	28 sections
Ranolazine	Human Prescription Drug Label	1	27241-125	TABLET, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
Ranolazine	Human Prescription Drug Label	1	27241-126	TABLET, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	29300-296	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	25 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	29300-297	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	25 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	31722-668	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	29 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	31722-669	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	29 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-773	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	22 sections

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