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

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1909 55985-32-5

Description:

MoleculeDescription

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:

DoseUnitRoute
90 mg O
90 mg P

ADMET properties:

PropertyValueReference
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):

PropertyDescriptionValueUnitConfidenceSimilarity
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:

DateAgencyCompanyOrphan
Dec. 21, 1988 FDA CHIESI USA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 7.02 Basic
pKa2 2.37 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Voltage-gated L-type calcium channel Ion channel BLOCKER CHEMBL CHEMBL
Multidrug resistance protein 1 Transporter IC50 5.32 CHEMBL
Adenosine receptor A3 GPCR Ki 5.49 CHEMBL
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor WOMBAT-PK
ATP-binding cassette sub-family G member 2 Transporter IC50 4.78 CHEMBL
Cytochrome P450 2C9 Enzyme IC50 6.55 WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 5.55 WOMBAT-PK
Malate dehydrogenase cytoplasmic Enzyme IC50 4.30 CHEMBL
Cytochrome P450 3A4 Enzyme IC50 6.38 WOMBAT-PK
Beta-lactamase Enzyme IC50 4.70 CHEMBL
Adenosine receptor A1 GPCR Ki 4.71 CHEMBL
Adenosine receptor A2a GPCR Ki 4.20 CHEMBL
Adenosine receptor A3 GPCR Ki 4.96 CHEMBL
Equilibrative nucleoside transporter 1 Transporter Ki 5.27 CHEMBL
Quinolone resistance protein NorA Transporter IC50 4.64 CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 5.85 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 5.44 CHEMBL
Voltage-gated L-type calcium channel Ion channel Ki 9.08 CHEMBL
Potassium voltage-gated channel subfamily A member 4 Ion channel BLOCKER IC50 6.10 IUPHAR

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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