Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	1909	55985-32-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nicardipine (+/-)-Nicardipine perpidine nicardipine hydrochloride nicardipine HCl	A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. Molecular weight: 479.53 Formula: C26H29N3O6 CLOGP: 5.23 LIPINSKI: 1 HAC: 9 HDO: 1 TPSA: 111.01 ALOGS: -5.29 ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nicardipine
(+/-)-Nicardipine
perpidine
nicardipine hydrochloride
nicardipine HCl

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.

Molecular weight: 479.53
Formula: C26H29N3O6
CLOGP: 5.23
LIPINSKI: 1
HAC: 9
HDO: 1
TPSA: 111.01
ALOGS: -5.29
ROTB: 11

Status: OFP

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

Drug dosage:

Dose	Unit	Route
90	mg	O
90	mg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	7.90 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	4.17 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	30 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	11 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.10 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	4.372		Moderate	0.72
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.574		Moderate	0.72
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	18.621	10^-6 cm/s	Moderate	0.72
dh-clint	Dog hepatocyte intrinsic clearance	168.655	uL/min/10^6 cells	Moderate	0.72
dppb	Dog plasma protein binding (% unbound)	0.480	%	Moderate	0.72
fcs-ppb	Fetal calf serum protein binding (% unbound)	1.280	%	Moderate	0.72
herg	hERG pIC50	5.715	pIC50	Moderate	0.72
hh-clint	Human hepatocyte intrinsic clearance	180.717	uL/min/10^6 cells	Moderate	0.72
hlm-clint	Human liver microsomal intrinsic clearance	295.801	uL/min/mg protein	Moderate	0.72
hppb	Human plasma protein binding (% unbound)	0.510	%	Moderate	0.72
kinase-safety-class	ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ZAP70	42
kinase-selectivity-class	AXL,BRAF,CDK9,GRK2,MAPK7,STK33,TEK	7
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	2.612		Moderate	0.72
mh-clint	Mouse hepatocyte intrinsic clearance	216.770		Moderate	0.72
mppb	Mouse plasma protein binding (% unbound)	0.470		Moderate	0.72
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	9.247		Moderate	0.72
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		High	1
pppb	Pig plasma protein binding (% unbound)	0.950	%	Moderate	0.72
rh-clint	Rat hepatocyte intrinsic clearance	276.694	uL/min/10^6 cells	Moderate	0.72
rh-fuinc	Rat hepatocyte fraction unbound in incubation	5.470	%	Moderate	0.72
rppb	Rat plasma protein binding (% unbound)	0.430	%	Moderate	0.72
solubility-dd	Solubility at pH 7.4 in DMSO	3.083	uM	Moderate	0.72

Approvals:

Date	Agency	Company	Orphan
Dec. 21, 1988	FDA	CHIESI USA INC

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
Premature delivery	245.04	24.82	102	8166	38660	90581519
Acute kidney injury	188.94	24.82	186	8082	320201	90299978
Hyponatraemia	155.99	24.82	115	8153	133423	90486756
Cerebral vasoconstriction	154.64	24.82	33	8235	1201	90618978
Premature baby	125.54	24.82	56	8212	25021	90595158
Eosinophilia	121.71	24.82	57	8211	28476	90591703
Acute generalised exanthematous pustulosis	121.22	24.82	46	8222	13657	90606522
Posterior reversible encephalopathy syndrome	118.63	24.82	52	8216	22287	90597892
Maternal exposure during pregnancy	114.58	24.82	152	8116	359911	90260268
Exposure during pregnancy	105.57	24.82	119	8149	238291	90381888
Hyperkalaemia	104.08	24.82	68	8200	64896	90555283
Hypotension	101.37	24.82	136	8132	325261	90294918
Hepatic cytolysis	96.71	24.82	50	8218	30866	90589313
Low birth weight baby	91.81	24.82	34	8234	9433	90610746
Cerebral haemorrhage	88.76	24.82	49	8219	34473	90585706
Acute pulmonary oedema	87.77	24.82	33	8235	9547	90610632
Acute motor-sensory axonal neuropathy	82.41	24.82	16	8252	359	90619820
Rash maculo-papular	81.00	24.82	49	8219	40884	90579295
Hepatocellular injury	79.70	24.82	43	8225	28915	90591264
Foetal exposure during pregnancy	76.28	24.82	48	8220	42927	90577252
Bradycardia	73.47	24.82	61	8207	83786	90536393
Cholestasis	73.23	24.82	44	8224	36255	90583924
Drug interaction	70.37	24.82	105	8163	276348	90343831
Ischaemic stroke	69.75	24.82	36	8232	22130	90598049
Foetal growth restriction	67.09	24.82	27	8241	9353	90610826
Drug reaction with eosinophilia and systemic symptoms	61.80	24.82	42	8226	42716	90577463
Lactic acidosis	60.02	24.82	44	8224	50419	90569760
Hyperlactacidaemia	59.81	24.82	20	8248	4116	90616063
Pre-eclampsia	59.55	24.82	26	8242	11022	90609157
Haemorrhagic transformation stroke	57.74	24.82	15	8253	1284	90618895
Fall	56.47	24.82	131	8137	481679	90138500
Rash pustular	53.56	24.82	22	8246	8027	90612152
Orthostatic hypotension	53.23	24.82	38	8230	41789	90578390
Renal failure	52.17	24.82	62	8206	130945	90489234
Premature labour	51.75	24.82	25	8243	13351	90606828
Fatigue	50.86	24.82	21	8247	1154002	89466177
Hemivertebra	50.77	24.82	9	8259	120	90620059
Hypokalaemia	50.49	24.82	61	8207	131055	90489124
Subarachnoid haemorrhage	50.41	24.82	27	8241	17877	90602302
Rhabdomyolysis	48.47	24.82	39	8229	51217	90568962
Thrombocytopenia	48.43	24.82	76	8192	208649	90411530
Haemangioma congenital	48.23	24.82	11	8257	545	90619634
Pain	47.44	24.82	16	8252	996325	89623854
Respiratory distress	44.15	24.82	33	8235	38913	90581266
Haematoma	44.08	24.82	33	8235	39015	90581164
Arthralgia	43.67	24.82	9	8259	778513	89841666
Purpura	43.62	24.82	23	8245	14755	90605424
Congenital choroid plexus cyst	42.10	24.82	9	8259	330	90619849
Myocardial calcification	39.23	24.82	8	8260	232	90619947
Cardiac arrest	39.05	24.82	48	8220	104887	90515292
Caesarean section	38.71	24.82	23	8245	18554	90601625
Toxic skin eruption	36.75	24.82	21	8247	15753	90604426
Haemodynamic instability	36.73	24.82	19	8249	11720	90608459
Altered state of consciousness	36.37	24.82	27	8241	31505	90588674
Paradoxical drug reaction	35.80	24.82	15	8253	5751	90614428
Anaphylactic shock	34.09	24.82	26	8242	31591	90588588
Metabolic encephalopathy	33.52	24.82	15	8253	6737	90613442
Delayed ischaemic neurological deficit	33.21	24.82	4	8264	0	90620179
Diabetic ketosis	32.47	24.82	8	8260	553	90619626
Patent ductus arteriosus	32.15	24.82	13	8255	4556	90615623
Wrong patient received product	31.92	24.82	12	8256	3465	90616714
Alopecia	31.57	24.82	4	8264	495067	90125112
Diabetic metabolic decompensation	30.44	24.82	10	8258	1947	90618232
Cutaneous lupus erythematosus	29.50	24.82	11	8257	3107	90617072
Drug hypersensitivity	28.95	24.82	4	8264	463605	90156574
Mixed liver injury	28.74	24.82	14	8254	7609	90612570
Coma	28.27	24.82	34	8234	72598	90547581
Foetal distress syndrome	27.68	24.82	9	8259	1696	90618483
Shock	27.42	24.82	22	8246	28756	90591423
Anuria	27.41	24.82	17	8251	14801	90605378
Tumour rupture	27.34	24.82	6	8262	249	90619930
Peripheral swelling	27.17	24.82	3	8265	413103	90207076
Hypoventilation	27.04	24.82	12	8256	5284	90614895
HELLP syndrome	26.33	24.82	8	8260	1209	90618970
Gestational hypertension	26.06	24.82	10	8258	3052	90617127
Hypersensitivity	25.98	24.82	5	8263	454672	90165507
Pulmonary oedema	25.71	24.82	30	8238	62050	90558129
Intra-abdominal haematoma	25.66	24.82	9	8259	2135	90618044
Agranulocytosis	25.63	24.82	23	8245	34979	90585200
Hypertrophic cardiomyopathy	25.32	24.82	9	8259	2219	90617960
Sinus bradycardia	25.31	24.82	17	8251	16935	90603244

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
Premature baby	135.32	20.59	67	6303	23086	42591879
Low birth weight baby	106.65	20.59	44	6326	9911	42605054
Foetal disorder	106.37	20.59	26	6344	1053	42613912
Cerebral vasoconstriction	105.33	20.59	20	6350	235	42614730
Acute kidney injury	97.23	20.59	186	6184	367151	42247814
Neutropenia neonatal	94.93	20.59	23	6347	897	42614068
Blood lactic acid	87.42	20.59	18	6352	328	42614637
Foetal exposure during pregnancy	71.33	20.59	58	6312	47253	42567712
Eosinophilia	68.73	20.59	49	6321	32850	42582115
Rash maculo-papular	62.99	20.59	49	6321	37454	42577511
Cerebral haemorrhage	61.34	20.59	49	6321	38917	42576048
Ureteric compression	60.30	20.59	13	6357	298	42614667
Cholestasis	46.79	20.59	39	6331	32840	42582125
Hypertensive crisis	46.49	20.59	25	6345	10181	42604784
Anaphylactoid reaction	41.75	20.59	16	6354	2967	42611998
Antiphospholipid antibodies positive	41.17	20.59	10	6360	394	42614571
Pyelocaliectasis	40.82	20.59	13	6357	1396	42613569
Haematoma muscle	39.18	20.59	14	6356	2136	42612829
Haemorrhagic transformation stroke	37.76	20.59	13	6357	1778	42613187
Maternal exposure during pregnancy	37.21	20.59	19	6351	6959	42608006
Cerebral infarction	36.33	20.59	33	6337	31136	42583829
Thalamus haemorrhage	35.23	20.59	11	6359	1108	42613857
Drug reaction with eosinophilia and systemic symptoms	33.17	20.59	36	6334	42039	42572926
Pneumonia aspiration	32.94	20.59	39	6331	50039	42564926
Phlebitis deep	32.12	20.59	5	6365	15	42614950
Foetal growth restriction	29.97	20.59	15	6355	5268	42609697
Fatigue	29.80	20.59	14	6356	435627	42179338
Hyperkalaemia	29.19	20.59	47	6323	80411	42534554
Hepatocellular injury	27.45	20.59	25	6345	23653	42591312
Bradycardia	27.09	20.59	47	6323	85437	42529528
Extravasation	27.07	20.59	11	6359	2379	42612586
Focal segmental glomerulosclerosis	26.39	20.59	11	6359	2537	42612428
Kidney small	26.39	20.59	5	6365	58	42614907
Anaemia neonatal	26.20	20.59	7	6363	405	42614560
Bronchopulmonary dysplasia	26.19	20.59	8	6362	749	42614216
Brain herniation	25.33	20.59	13	6357	4810	42610155
Haemolytic anaemia	25.16	20.59	18	6352	12109	42602856
Anuria	23.65	20.59	17	6353	11515	42603450
Poisoning deliberate	23.25	20.59	16	6354	10118	42604847
Paradoxical drug reaction	22.68	20.59	12	6358	4726	42610239
Dizziness	22.29	20.59	5	6365	249249	42365716
Death	21.86	20.59	23	6347	471162	42143803
Aortic dissection	21.28	20.59	10	6360	3062	42611903
Hepatic cytolysis	21.20	20.59	23	6347	26821	42588144
Haemorrhagic cerebral infarction	20.87	20.59	7	6363	884	42614081
Cerebral haematoma	20.78	20.59	12	6358	5598	42609367

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
Acute kidney injury	278.40	20.34	367	13398	635063	109940471
Cerebral vasoconstriction	246.63	20.34	53	13712	1448	110574086
Eosinophilia	186.47	20.34	106	13659	57830	110517704
Cerebral haemorrhage	137.62	20.34	91	13674	64877	110510657
Rash maculo-papular	135.91	20.34	95	13670	74127	110501407
Premature delivery	134.78	20.34	69	13696	30563	110544971
Hyperkalaemia	117.03	20.34	112	13653	135684	110439850
Posterior reversible encephalopathy syndrome	114.45	20.34	64	13701	33797	110541737
Cholestasis	112.12	20.34	80	13685	64438	110511096
Hepatic cytolysis	106.72	20.34	73	13692	54980	110520554
Hyponatraemia	104.53	20.34	132	13633	217521	110358013
Acute generalised exanthematous pustulosis	95.87	20.34	49	13716	21615	110553919
Hepatocellular injury	95.44	20.34	66	13699	50576	110524958
Hypotension	88.90	20.34	199	13566	523650	110051884
Haemorrhagic transformation stroke	88.66	20.34	27	13738	3010	110572524
Drug reaction with eosinophilia and systemic symptoms	86.87	20.34	76	13689	82019	110493515
Blood lactic acid	84.89	20.34	18	13747	460	110575074
Bradycardia	80.53	20.34	98	13667	155419	110420115
Drug interaction	71.74	20.34	178	13587	500005	110075529
Acute motor-sensory axonal neuropathy	71.70	20.34	16	13749	522	110575012
Ischaemic stroke	71.29	20.34	51	13714	41212	110534322
Acute pulmonary oedema	71.04	20.34	37	13728	16959	110558575
Fatigue	68.60	20.34	33	13732	1215925	109359609
Cerebral infarction	67.26	20.34	54	13711	51784	110523750
Exposure during pregnancy	67.14	20.34	93	13672	167331	110408203
Lactic acidosis	65.99	20.34	69	13696	92742	110482792
Ureteric compression	62.54	20.34	13	13752	301	110575233
Haematoma	59.58	20.34	53	13712	58423	110517111
Renal failure	58.83	20.34	103	13662	226471	110349063
Hypokalaemia	58.20	20.34	91	13674	182357	110393177
Paradoxical drug reaction	57.82	20.34	27	13738	9790	110565744
Pain	56.79	20.34	24	13741	954931	109620603
Pre-eclampsia	54.72	20.34	25	13740	8625	110566909
Respiratory distress	52.20	20.34	53	13712	68821	110506713
Maternal exposure during pregnancy	51.39	20.34	104	13661	254779	110320755
Hypertensive crisis	51.23	20.34	34	13731	24338	110551196
Rash pustular	50.97	20.34	27	13738	12802	110562732
Subarachnoid haemorrhage	47.41	20.34	35	13730	29667	110545867
Cardiac arrest	46.65	20.34	86	13679	196667	110378867
Pneumonia aspiration	46.65	20.34	54	13711	81179	110494355
Anuria	46.49	20.34	32	13733	24309	110551225
Hyperlactacidaemia	46.37	20.34	22	13743	8264	110567270
Pyelocaliectasis	46.12	20.34	13	13752	1106	110574428
Altered state of consciousness	44.86	20.34	45	13720	57581	110517953
Purpura	41.79	20.34	30	13735	24358	110551176
Premature labour	41.31	20.34	21	13744	9151	110566383
Mixed liver injury	41.26	20.34	23	13742	12056	110563478
Fall	40.25	20.34	165	13600	603317	109972217
Orthostatic hypotension	39.66	20.34	45	13720	66204	110509330
Thrombocytopenia	38.67	20.34	113	13652	348772	110226762
Abdominal discomfort	37.72	20.34	3	13762	393855	110181679
Delayed ischaemic neurological deficit	37.61	20.34	5	13760	3	110575531
Peripheral swelling	36.24	20.34	4	13761	404030	110171504
Brain herniation	36.19	20.34	19	13746	8844	110566690
Myocardial calcification	35.94	20.34	8	13757	258	110575276
Thalamus haemorrhage	34.97	20.34	12	13753	1952	110573582
Drug intolerance	34.10	20.34	5	13760	406507	110169027
Drug hypersensitivity	32.97	20.34	8	13757	454082	110121452
Haematoma muscle	32.92	20.34	14	13751	4076	110571458
Rhabdomyolysis	32.87	20.34	56	13709	120345	110455189
Phlebitis deep	32.12	20.34	5	13760	19	110575515
Arthralgia	31.99	20.34	30	13735	779602	109795932
Haemolytic anaemia	31.93	20.34	24	13741	20896	110554638
Anaphylactoid reaction	31.83	20.34	16	13749	6810	110568724
Alopecia	31.75	20.34	4	13761	364749	110210785
Poisoning deliberate	31.14	20.34	26	13739	26305	110549229
Anaphylactic shock	30.83	20.34	35	13730	51511	110524023
Caesarean section	30.80	20.34	20	13745	13797	110561737
Nasopharyngitis	30.54	20.34	6	13759	394355	110181179
Antiphospholipid antibodies positive	30.27	20.34	9	13756	924	110574610
Swelling	30.19	20.34	4	13761	351037	110224497
Haemorrhagic cerebral infarction	30.03	20.34	10	13755	1485	110574049
Foetal growth restriction	29.83	20.34	12	13753	3038	110572496
Angioedema	29.82	20.34	48	13717	98452	110477082
Coma	29.80	20.34	53	13712	117816	110457718
Weight decreased	29.00	20.34	11	13754	468046	110107488
Dizziness	28.47	20.34	27	13738	698166	109877368
Atrioventricular block complete	28.36	20.34	22	13743	20060	110555474
Toxic skin eruption	28.14	20.34	25	13740	27490	110548044
Shock	28.07	20.34	34	13731	53554	110521980
Pulmonary hypoplasia	27.71	20.34	5	13760	53	110575481
Aortic dissection	27.31	20.34	13	13752	4920	110570614
Agranulocytosis	27.30	20.34	36	13729	61724	110513810
Septic shock	26.77	20.34	60	13705	157468	110418066
HELLP syndrome	26.48	20.34	8	13757	868	110574666
Sinusitis	26.44	20.34	3	13762	296685	110278849
Gestational hypertension	26.11	20.34	10	13755	2224	110573310
Diabetic ketosis	25.95	20.34	8	13757	928	110574606
Confusional state	25.76	20.34	121	13644	468559	110106975
Metabolic acidosis	25.40	20.34	45	13720	99699	110475835
Respiratory failure	25.04	20.34	71	13694	215261	110360273
Cutaneous lupus erythematosus	24.99	20.34	11	13754	3477	110572057
Thrombotic microangiopathy	24.99	20.34	24	13741	29125	110546409
Headache	24.83	20.34	45	13720	882332	109693202
Dyspnoea	24.14	20.34	65	13700	1106807	109468727
Cerebral haematoma	24.11	20.34	15	13750	9617	110565917
Hypoventilation	23.88	20.34	14	13751	8067	110567467
Hypoaesthesia	23.87	20.34	5	13760	314218	110261316
Haemodynamic instability	23.81	20.34	21	13744	22867	110552667
Circulatory collapse	23.71	20.34	28	13737	42965	110532569
Alexithymia	23.30	20.34	4	13761	31	110575503
Haemorrhage intracranial	23.24	20.34	23	13742	28946	110546588
Vasoplegia syndrome	23.18	20.34	12	13753	5427	110570107
Macroglossia	22.46	20.34	8	13757	1453	110574081
Metabolic encephalopathy	22.21	20.34	15	13750	11045	110564489
Muscle spasms	22.02	20.34	4	13761	278153	110297381
Acute respiratory distress syndrome	21.97	20.34	30	13735	53168	110522366
Nausea	21.71	20.34	80	13685	1235610	109339924
Systemic lupus erythematosus	21.62	20.34	3	13762	254335	110321199
Brain contusion	21.61	20.34	8	13757	1620	110573914
Hepatic function abnormal	21.10	20.34	39	13726	89256	110486278
Diabetic metabolic decompensation	20.77	20.34	10	13755	3879	110571655
Porphyria	20.55	20.34	5	13760	239	110575295
Pancytopenia	20.48	20.34	65	13700	209548	110365986
Ventricular tachycardia	20.35	20.34	28	13737	49981	110525553

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C08CA04	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
FDA CS	M0006414	Dihydropyridines
FDA MoA	N0000000069	Calcium Channel Antagonists
FDA EPC	N0000175421	Dihydropyridine Calcium Channel Blocker
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002121	Calcium Channel Blockers
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D014665	Vasodilator Agents
MeSH PA	D049990	Membrane Transport Modulators
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000182140	Cytochrome P450 2C19 Inhibitors
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
CHEBI has role	CHEBI:35554	cardiovascular drug
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:35620	vasodilator agent
CHEBI has role	CHEBI:35674	antihypertensive agent
CHEBI has role	CHEBI:38215	calcium channel blocker
CHEBI has role	CHEBI:88230	autophagy inhibitor
CHEBI has role	CHEBI:53784	antispasmodic drug
CHEBI has role	CHEBI:176497	geroprotector

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs

amlodipine barnidipine benidipine celecoxib cilnidipine clevidipine felodipine isradipine lacidipine lercanidipine levamlodipine manidipine show all 17 →

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Angina pectoris	indication	194828000
Prinzmetal angina	off-label use	87343002
Raynaud's phenomenon	off-label use	266261006
Portal hypertension	contraindication	34742003	DOID:10762
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003
Chronic idiopathic constipation	contraindication	82934008
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Cerebral hemorrhage	contraindication	274100004
Cerebral infarction	contraindication	432504007	DOID:3526
Severe Aortic Valve Stenosis	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.02	Basic
pKa2	2.37	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 0.86% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
20MG/200ML (0.1MG/ML)	CARDENE IN 4.8% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	July 31, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	11547758	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	DISCN	INJECTABLE	INTRAVENOUS	7659291	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 0.83% SODIUM CHLORIDE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	RX	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF
40MG/200ML (0.2MG/ML)	CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER	CHIESI	N019734	Nov. 7, 2008	DISCN	INJECTABLE	INTRAVENOUS	8455524	April 18, 2027	METHOD FOR TREATING ACUTE ELEVATIONS OF BLOOD PRESSURE IN HUMAN SUBJECT IN NEED THEREOF

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Voltage-gated L-type calcium channel	Ion channel	Q01668 Q13936	CAC1D_HUMAN CAC1C_HUMAN	BLOCKER			CHEMBL	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.32	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.49	CHEMBL
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN				WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.78	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	6.55	WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN		Ki	5.55	WOMBAT-PK
Malate dehydrogenase cytoplasmic	Enzyme	P40925	MDHC_HUMAN		IC50	4.30	CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.38	WOMBAT-PK
Beta-lactamase	Enzyme		AMPC_ECOLI		IC50	4.70	CHEMBL
Adenosine receptor A1	GPCR		AA1R_RAT		Ki	4.71	CHEMBL
Adenosine receptor A2a	GPCR		AA2AR_RAT		Ki	4.20	CHEMBL
Adenosine receptor A3	GPCR		AA3R_RAT		Ki	4.96	CHEMBL
Equilibrative nucleoside transporter 1	Transporter		S29A1_RAT		Ki	5.27	CHEMBL
Quinolone resistance protein NorA	Transporter		NORA_STAAU		IC50	4.64	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		IC50	5.85	CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		IC50	5.44	CHEMBL
Voltage-gated L-type calcium channel	Ion channel		CAC1C_RAT CAC1D_RAT CAC1S_RAT		Ki	9.08	CHEMBL
Potassium voltage-gated channel subfamily A member 4	Ion channel		KCNA4_RAT	BLOCKER	IC50	6.10	IUPHAR

External reference:

ID	Source
4019858	VUID
N0000147944	NUI
D00617	KEGG_DRUG
54527-84-3	SECONDARY_CAS_RN
4019350	VANDF
4019858	VANDF
C0028005	UMLSCUI
CHEBI:7550	CHEBI
CHEMBL1484	ChEMBL_ID
CHEMBL1200326	ChEMBL_ID
D009529	MESH_DESCRIPTOR_UI
DB00622	DRUGBANK_ID
2559	IUPHAR_LIGAND_ID
4745	INN_ID
CZ5312222S	UNII
4474	PUBCHEM_CID
235230	RXNORM
2278	MMSL
5171	MMSL
d00315	MMSL
000712	NDDF
004518	NDDF
108526002	SNOMEDCT_US
108527006	SNOMEDCT_US
372502001	SNOMEDCT_US
CZ5312222S	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9542	INJECTION	2.50 mg	INTRAVENOUS	NDA	25 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9593	INJECTION	2.50 mg	INTRAVENOUS	NDA	26 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9633	INJECTION	0.20 mg	INTRAVENOUS	NDA	27 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9634	INJECTION	0.10 mg	INTRAVENOUS	NDA	27 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9689	INJECTION	25 mg	INTRAVENOUS	NDA	27 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0517-0735	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	ANDA	26 sections
Nicardipine Hydrochloride	Human Prescription Drug Label	1	0781-3204	INJECTION	2.50 mg	INTRAVENOUS	ANDA	12 sections
Nicardipine Hydrochloride	Human Prescription Drug Label	1	0781-9324	INJECTION	2.50 mg	INTRAVENOUS	ANDA	12 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	24658-750	CAPSULE	20 mg	ORAL	ANDA	19 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	24658-751	CAPSULE	30 mg	ORAL	ANDA	19 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	25021-333	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	ANDA	27 sections
NICARDIPINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	35573-457	CAPSULE	20 mg	ORAL	ANDA	13 sections
NICARDIPINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	35573-458	CAPSULE	30 mg	ORAL	ANDA	13 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	40042-047	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	ANDA	20 sections
NICARDIPINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	42571-394	INJECTION	2.50 mg	INTRAVENOUS	ANDA	25 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42806-501	CAPSULE	20 mg	ORAL	ANDA	19 sections
Nicardipine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42806-502	CAPSULE	30 mg	ORAL	ANDA	19 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-009	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	23 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-016	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	NDA	23 sections
Cardene IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-021	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	23 sections
Cardene IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-024	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	NDA	23 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-026	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	23 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-028	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	NDA	23 sections
CARDENE IV	HUMAN PRESCRIPTION DRUG LABEL	1	43066-029	INJECTION, SOLUTION	2.50 mg	INTRAVENOUS	NDA	24 sections
Nicardipine Hydrochloride in Sodium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	44567-850	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	ANDA	23 sections
Nicardipine Hydrochloride in Sodium Chloride	HUMAN PRESCRIPTION DRUG LABEL	1	44567-851	INJECTION, SOLUTION	0.20 mg	INTRAVENOUS	ANDA	23 sections
NICARDIPINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1428	INJECTION, SOLUTION	0.10 mg	INTRAVENOUS	NDA	17 sections
NICARDIPINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1482	INJECTION	25 mg	INTRAVENOUS	NDA	17 sections
NICARDIPINE HYDROCHLORIDE	Human Prescription Drug Label	1	55150-183	INJECTION, SOLUTION	25 mg	INTRAVENOUS	ANDA	24 sections
NICARDIPINE HYDROCHLORIDE	Human Prescription Drug Label	1	55150-183	INJECTION, SOLUTION	25 mg	INTRAVENOUS	ANDA	24 sections

Ask DrugCentral

Try a sample question

nicardipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: