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:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
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
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	9.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.38 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.80 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 27, 2006	FDA	GILEAD

FDA Adverse Event Reporting System (Female)

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
Pulseless electrical activity	42.96	18.03	20	7571	7501	63473930
Coronary artery disease	41.65	18.03	33	7558	32344	63449087
Cardiac arrest	41.21	18.03	53	7538	92492	63388939
Hyperkalaemia	37.55	18.03	39	7552	54164	63427267
Syncope	35.64	18.03	56	7535	117329	63364102
Sinus bradycardia	35.59	18.03	22	7569	14529	63466902
Catheterisation cardiac	35.14	18.03	15	7576	4588	63476843
Hypotension	34.23	18.03	90	7501	272514	63208917
Serum serotonin increased	32.61	18.03	7	7584	198	63481233
Urinary straining	29.18	18.03	5	7586	40	63481391
Therapeutic response unexpected	28.24	18.03	21	7570	18738	63462693
Product residue present	27.22	18.03	12	7579	3967	63477464
Ventricular tachycardia	27.06	18.03	21	7570	19958	63461473
Pulmonary oedema	25.31	18.03	32	7559	54841	63426590
Hypersensitivity pneumonitis	24.84	18.03	10	7581	2640	63478791
Dyspnoea	24.17	18.03	148	7443	661165	62820266
Myocardial infarction	24.09	18.03	43	7548	99850	63381581
Left ventricular hypertrophy	23.90	18.03	12	7579	5303	63476128
Hypoglycaemia	23.04	18.03	32	7559	60033	63421398
Circumoral swelling	22.82	18.03	4	7587	37	63481394
Death	22.18	18.03	96	7495	374285	63107146
Nodal rhythm	21.39	18.03	8	7583	1735	63479696
Autonomic nervous system imbalance	20.91	18.03	9	7582	2809	63478622
Sinus arrest	20.53	18.03	8	7583	1941	63479490
Myopathy	20.22	18.03	14	7577	11177	63470254
Joint swelling	20.19	18.03	7	7584	327659	63153772
Infusion related reaction	19.56	18.03	3	7588	245518	63235913
Coronary artery bypass	19.01	18.03	8	7583	2361	63479070

FDA Adverse Event Reporting System (Male)

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
Bradycardia	39.74	18.63	74	9773	75344	34871740
Death	36.98	18.63	214	9633	397835	34549249
Electrocardiogram QT prolonged	36.42	18.63	51	9796	40901	34906183
Hypotension	34.18	18.63	138	9709	221511	34725573
Cardiac failure congestive	33.46	18.63	73	9774	83197	34863887
Myocardial infarction	32.57	18.63	91	9756	120994	34826090
Product residue present	27.32	18.63	14	9833	2732	34944352
Heart valve stenosis	27.10	18.63	6	9841	80	34947004
Cardiac failure	26.95	18.63	71	9776	91177	34855907
Ventricular tachycardia	26.50	18.63	35	9812	26544	34920540
Presyncope	25.31	18.63	29	9818	19030	34928054
Tremor	24.12	18.63	64	9783	82523	34864561
Angina unstable	23.15	18.63	22	9825	11631	34935453
Vertigo	22.99	18.63	32	9815	25504	34921580
Asthenia	22.10	18.63	131	9716	245120	34701964
Keratolysis exfoliativa acquired	21.53	18.63	3	9844	0	34947084
Myocardial necrosis	20.67	18.63	6	9841	247	34946837
Aortic bruit	20.67	18.63	6	9841	247	34946837
Respiratory tract haemorrhage	20.39	18.63	9	9838	1261	34945823
Loss of consciousness	20.14	18.63	60	9787	82607	34864477
Myopathy toxic	19.40	18.63	7	9840	579	34946505

FDA Adverse Event Reporting System (Geriatric)

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
Rhabdomyolysis	63.17	16.13	86	14569	103045	79626688
Chromaturia	61.15	16.13	45	14610	25701	79704032
Dyspnoea	60.30	16.13	313	14342	856712	78873021
Death	59.38	16.13	233	14422	566281	79163452
Myocardial infarction	56.10	16.13	112	14543	184017	79545716
Tonic clonic movements	54.03	16.13	19	14636	2245	79727488
Torsade de pointes	50.99	16.13	36	14619	19276	79710457
Gastrointestinal haemorrhage	46.36	16.13	91	14564	147628	79582105
Cardiac arrest	44.61	16.13	98	14557	171998	79557735
Cardiac failure congestive	43.81	16.13	87	14568	142315	79587418
Catheterisation cardiac	42.92	16.13	21	14634	5707	79724026
Sinus bradycardia	40.40	16.13	35	14620	25212	79704521
Angina unstable	39.49	16.13	29	14626	16498	79713235
Ventricular tachycardia	38.67	16.13	43	14612	41892	79687841
Pulseless electrical activity	36.47	16.13	26	14629	14134	79715599
Hypoglycaemia	36.09	16.13	66	14589	101528	79628205
Coronary artery bypass	36.02	16.13	19	14636	6043	79723690
Presyncope	34.30	16.13	40	14615	41014	79688719
Infusion related reaction	31.43	16.13	3	14652	230234	79499499
Asthenia	31.16	16.13	180	14475	511509	79218224
Coronary arterial stent insertion	30.50	16.13	17	14638	6027	79723706
Fall	29.33	16.13	171	14484	487458	79242275
Rheumatoid arthritis	27.71	16.13	3	14652	208467	79521266
Product residue present	26.60	16.13	13	14642	3523	79726210
Drug ineffective	26.36	16.13	106	14549	1080807	78648926
Serum serotonin increased	26.30	16.13	7	14648	323	79729410
Urinary straining	26.12	16.13	5	14650	49	79729684
Intentional overdose	25.93	16.13	59	14596	105901	79623832
Heart valve stenosis	25.31	16.13	6	14649	172	79729561
Pyrexia	24.05	16.13	56	14599	678653	79051080
Hyperkalaemia	24.00	16.13	60	14595	114338	79615395
Rectal haemorrhage	23.91	16.13	47	14608	76253	79653480
Wrong technique in product usage process	23.75	16.13	46	14609	73829	79655904
Acute myocardial infarction	23.59	16.13	47	14608	76989	79652744
Nasopharyngitis	22.90	16.13	9	14646	253872	79475861
Aortic bruit	22.46	16.13	6	14649	281	79729452
Myopathy	22.33	16.13	23	14632	20540	79709193
Labelled drug-drug interaction medication error	21.54	16.13	26	14629	27624	79702109
Cardiac failure	21.53	16.13	70	14585	154772	79574961
Treatment failure	21.32	16.13	3	14652	170483	79559250
Respiratory tract haemorrhage	20.96	16.13	9	14646	1814	79727919
Circumoral swelling	20.82	16.13	4	14651	40	79729693
Bundle branch block left	20.55	16.13	17	14638	11496	79718237
Atrial fibrillation	20.30	16.13	81	14574	197805	79531928
Musculoskeletal stiffness	19.85	16.13	4	14651	175004	79554729
Tremor	19.39	16.13	72	14583	170011	79559722
Myocardial necrosis	19.16	16.13	6	14649	495	79729238
Nodal rhythm	19.12	16.13	10	14645	3125	79726608
Hypotonic urinary bladder	18.64	16.13	4	14651	72	79729661
Melaena	18.46	16.13	37	14618	60853	79668880
Anaemia	18.26	16.13	142	14513	444873	79284860
Loss of consciousness	18.24	16.13	70	14585	167873	79561860
Cardiac pacemaker insertion	18.08	16.13	12	14643	5810	79723923
Therapeutic product effect decreased	18.06	16.13	4	14651	163859	79565874
Dysarthria	18.06	16.13	39	14616	67583	79662150
Myopathy toxic	18.03	16.13	7	14648	1091	79728642
Chest discomfort	17.93	16.13	61	14594	137983	79591750
Keratolysis exfoliativa acquired	17.79	16.13	3	14652	13	79729720
Gravitational oedema	17.65	16.13	8	14647	1831	79727902
Hypersensitivity pneumonitis	17.47	16.13	10	14645	3729	79726004
Ventricular enlargement	16.92	16.13	6	14649	726	79729007
Confusional state	16.85	16.13	108	14547	317889	79411844
Enzyme inhibition	16.57	16.13	3	14652	21	79729712
Vertigo	16.38	16.13	38	14617	69044	79660689
Palatal oedema	16.24	16.13	7	14648	1424	79728309

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C01EB18	CARDIOVASCULAR SYSTEM CARDIAC THERAPY OTHER CARDIAC PREPARATIONS Other cardiac preparations
FDA EPC	N0000175427	Anti-anginal
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D026941	Sodium Channel Blockers
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
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:38633	sodium channel blockers

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

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

🐶 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:

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

External reference:

ID	Source
4025078	VUID
N0000175343	NUI
D05700	KEGG_DRUG
95635-56-6	SECONDARY_CAS_RN
4025078	VANDF
C0073633	UMLSCUI
CHEBI:87681	CHEBI
CHEMBL1404	ChEMBL_ID
CHEMBL1526084	ChEMBL_ID
CHEMBL537649	ChEMBL_ID
D000069458	MESH_DESCRIPTOR_UI
DB00243	DRUGBANK_ID
56959	PUBCHEM_CID
7291	IUPHAR_LIGAND_ID
5946	INN_ID
A6IEZ5M406	UNII
356778	RXNORM
20936	MMSL
309260	MMSL
75657	MMSL
d05719	MMSL
011195	NDDF
420365007	SNOMEDCT_US
420624001	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-774	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	22 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42385-963	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	23 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42385-964	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	23 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42571-324	TABLET, EXTENDED RELEASE	500 mg	ORAL	ANDA	26 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	42571-325	TABLET, EXTENDED RELEASE	1000 mg	ORAL	ANDA	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	45963-418	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-418	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-419	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	45963-419	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
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
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	50228-423	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	50228-424	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	50268-722	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	25 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	50268-723	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	25 sections
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	51407-225	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	51407-225	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	51407-226	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
RANOLAZINE	HUMAN PRESCRIPTION DRUG LABEL	1	51407-226	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
Ranolazine	Human Prescription Drug Label	1	59651-009	TABLET, FILM COATED, EXTENDED RELEASE	500 mg	ORAL	ANDA	27 sections
Ranolazine	Human Prescription Drug Label	1	59651-010	TABLET, FILM COATED, EXTENDED RELEASE	1000 mg	ORAL	ANDA	27 sections
Ranolazine	HUMAN PRESCRIPTION DRUG LABEL	1	60687-549	TABLET, EXTENDED RELEASE	500 mg	ORAL	ANDA	28 sections