lercanidipine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 4157 100427-26-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lercanidipine hydrochloride
  • lercanidipine
  • masnidipine
  • zanidip
  • lercanidipine HCl
  • Molecular weight: 611.74
  • Formula: C36H41N3O6
  • CLOGP: 8
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 1
  • TPSA: 111.01
  • ALOGS: -6.59
  • ROTB: 14

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 10 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

None

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
Hyponatraemia 354.81 16.26 297 17130 101035 46567600
Acute kidney injury 330.64 16.26 422 17005 235433 46433202
General physical health deterioration 161.26 16.26 207 17220 115562 46553073
Lactic acidosis 138.61 16.26 109 17318 33800 46634835
Hyperkalaemia 137.85 16.26 129 17298 50580 46618055
Hypotension 120.71 16.26 267 17160 232322 46436313
Fall 118.19 16.26 328 17099 328769 46339866
Confusional state 112 16.26 208 17219 159684 46508951
Hypokalaemia 111.02 16.26 150 17277 87874 46580761
Drug interaction 90.80 16.26 220 17207 202874 46465761
Cholestasis 88.01 16.26 76 17351 26817 46641818
Anaemia 78.23 16.26 241 17186 255538 46413097
Hepatocellular injury 76.16 16.26 73 17354 29449 46639186
Pemphigoid 73.76 16.26 38 17389 5653 46662982
Pallor 72.84 16.26 64 17363 23102 46645533
Rheumatoid arthritis 70.44 16.26 5 17422 240210 46428425
Pain 67.61 16.26 48 17379 476900 46191735
Labile hypertension 64.15 16.26 18 17409 490 46668145
Drug ineffective 59.94 16.26 101 17326 677737 45990898
Bradycardia 59.03 16.26 96 17331 66202 46602433
Cell death 56.93 16.26 24 17403 2264 46666371
Hypertension 56.25 16.26 181 17246 196175 46472460
Atrial fibrillation 53.62 16.26 119 17308 103471 46565164
Drug hypersensitivity 52.89 16.26 13 17414 243812 46424823
Orthostatic hypotension 52.59 16.26 55 17372 24603 46644032
Death 51.22 16.26 31 17396 335517 46333118
Hypertensive crisis 49.72 16.26 41 17386 13574 46655061
Vasoplegia syndrome 46.84 16.26 17 17410 1075 46667560
Eosinophilia 43.02 16.26 44 17383 19173 46649462
Sopor 41.87 16.26 44 17383 19784 46648851
Myopathy 41.64 16.26 31 17396 8850 46659785
Toxic skin eruption 40.50 16.26 35 17392 12352 46656283
Poisoning deliberate 40.17 16.26 29 17398 7897 46660738
Anuria 38.80 16.26 33 17394 11398 46657237
Epileptic encephalopathy 36.57 16.26 10 17417 247 46668388
Product dose omission issue 36.49 16.26 9 17418 168511 46500124
Medication error 36.38 16.26 51 17376 30860 46637775
Renin increased 35.92 16.26 9 17418 156 46668479
Electrocardiogram QT prolonged 34.86 16.26 66 17361 51259 46617376
Sinusitis 34.52 16.26 4 17423 129764 46538871
Immune-mediated pancreatitis 33.35 16.26 7 17420 52 46668583
Rhabdomyolysis 32.39 16.26 57 17370 41852 46626783
Cardiac failure 31.82 16.26 83 17344 79865 46588770
Product prescribing error 31.26 16.26 38 17389 20009 46648626
Inappropriate antidiuretic hormone secretion 31.04 16.26 32 17395 14070 46654565
Helplessness 28.68 16.26 8 17419 213 46668422
Labelled drug-drug interaction medication error 28.40 16.26 25 17402 9036 46659599
Ischaemic stroke 28.21 16.26 33 17394 16689 46651946
Nasopharyngitis 26.75 16.26 12 17415 153986 46514649
Spontaneous haematoma 26.41 16.26 10 17417 712 46667923
Walking disability 26.32 16.26 12 17415 1366 46667269
Renal artery stenosis 26.27 16.26 13 17414 1775 46666860
Cerebral haematoma 26.09 16.26 16 17411 3323 46665312
Hallucination, gustatory 25.92 16.26 6 17421 73 46668562
Traumatic haematoma 25.81 16.26 12 17415 1428 46667207
Hyperglycaemic hyperosmolar nonketotic syndrome 25.54 16.26 9 17418 522 46668113
Necrotising myositis 25.37 16.26 8 17419 328 46668307
Acute pulmonary oedema 25.19 16.26 22 17405 7869 46660766
Exposure during pregnancy 24.98 16.26 5 17422 108207 46560428
Wrong product administered 24.94 16.26 19 17408 5611 46663024
Treatment failure 24.43 16.26 3 17424 93084 46575551
Mental status changes postoperative 24.36 16.26 7 17420 208 46668427
Gamma-glutamyltransferase increased 24.31 16.26 43 17384 31697 46636938
Tachycardia 24.20 16.26 87 17340 99535 46569100
Arrhythmia 23.89 16.26 45 17382 34796 46633839
Confusion postoperative 23.86 16.26 7 17420 224 46668411
Altered state of consciousness 23.80 16.26 36 17391 23312 46645323
Prothrombin time shortened 23.53 16.26 12 17415 1747 46666888
Radiation fibrosis 23.50 16.26 5 17422 40 46668595
Tongue oedema 23.43 16.26 16 17411 3990 46664645
Sprue-like enteropathy 23.20 16.26 8 17419 435 46668200
Abdominal discomfort 22.96 16.26 14 17413 151151 46517484
Arthralgia 22.48 16.26 66 17361 364537 46304098
White blood cell count decreased 22.40 16.26 7 17420 112224 46556411
Postural tremor 22.18 16.26 6 17421 142 46668493
Renal failure 21.74 16.26 92 17335 113502 46555133
Haematochezia 21.58 16.26 45 17382 37448 46631187
Retroperitoneal fibrosis 21.14 16.26 7 17420 336 46668299
Adenocarcinoma metastatic 21.02 16.26 5 17422 69 46668566
Ultrasound liver abnormal 20.95 16.26 4 17423 17 46668618
Rhonchi 20.93 16.26 12 17415 2203 46666432
Arterial spasm 20.89 16.26 5 17422 71 46668564
Disorientation 20.89 16.26 44 17383 36874 46631761
Infusion related reaction 20.77 16.26 6 17421 101202 46567433
Pseudophaeochromocytoma 20.51 16.26 5 17422 77 46668558
Degenerative mitral valve disease 20.25 16.26 4 17423 21 46668614
Degenerative aortic valve disease 20.10 16.26 4 17423 22 46668613
Shock haemorrhagic 19.76 16.26 20 17407 8604 46660031
Coma 19.65 16.26 57 17370 58292 46610343
Joint swelling 19.42 16.26 20 17407 166053 46502582
Hallucination, olfactory 19.42 16.26 6 17421 230 46668405
Haematoma 19.22 16.26 39 17388 31833 46636802
Injection site pain 19.15 16.26 8 17419 107144 46561491
Cerebral salt-wasting syndrome 19.15 16.26 4 17423 29 46668606
Oedema peripheral 18.96 16.26 113 17314 159593 46509042
Hypocalcaemia 18.87 16.26 35 17392 26750 46641885
Hallucination, visual 18.85 16.26 28 17399 17845 46650790
Frontotemporal dementia 18.82 16.26 6 17421 255 46668380
Blood creatinine increased 18.79 16.26 67 17360 76336 46592299
Swelling 18.26 16.26 12 17415 124499 46544136
Miosis 18.18 16.26 17 17410 6640 46661995
Polyneuropathy 18.03 16.26 22 17405 11622 46657013
Status epilepticus 17.85 16.26 24 17403 13955 46654680
Asthma 17.76 16.26 6 17421 91536 46577099
Purpura 17.38 16.26 20 17407 9938 46658697
Depression 17.19 16.26 23 17404 170081 46498554
Haematemesis 17.08 16.26 35 17392 28771 46639864
Polyuria 17.06 16.26 17 17410 7178 46661457
Arthritis 16.97 16.26 4 17423 77312 46591323
Tinnitus 16.85 16.26 34 17393 27639 46640996
Somnolence 16.85 16.26 108 17319 156413 46512222
Intestinal villi atrophy 16.84 16.26 5 17422 167 46668468
Convulsive threshold lowered 16.74 16.26 6 17421 366 46668269
Pulmonary haematoma 16.57 16.26 4 17423 59 46668576

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
Acute kidney injury 228.25 14.29 449 14351 273393 29664285
Lactic acidosis 102.60 14.29 100 14700 31113 29906565
Hyperkalaemia 75.84 14.29 125 14675 65885 29871793
General physical health deterioration 64.16 14.29 148 14652 99796 29837882
Death 61.51 14.29 52 14748 357231 29580447
Metabolic acidosis 57.21 14.29 81 14719 37380 29900298
Hyponatraemia 44.71 14.29 101 14699 67101 29870577
Drug ineffective 39.87 14.29 67 14733 340320 29597358
Hypertensive crisis 37.68 14.29 32 14768 8325 29929353
Cerebral haematoma 37.67 14.29 25 14775 4489 29933189
Pemphigoid 36.37 14.29 30 14770 7498 29930180
Vascular purpura 35.99 14.29 17 14783 1580 29936098
Nephroangiosclerosis 35.98 14.29 10 14790 196 29937482
Hypoglycaemia 35.44 14.29 78 14722 50903 29886775
Syncope 35.28 14.29 107 14693 84796 29852882
Drug interaction 34.84 14.29 192 14608 199376 29738302
Supine hypertension 33.79 14.29 10 14790 247 29937431
Hemiplegia 33.13 14.29 27 14773 6634 29931044
Completed suicide 32.80 14.29 5 14795 99487 29838191
Ischaemic stroke 32.25 14.29 40 14760 16235 29921443
Retinal artery occlusion 32.14 14.29 16 14784 1668 29936010
Haematoma 29.69 14.29 47 14753 23906 29913772
Bradycardia 29.51 14.29 85 14715 65441 29872237
Hypokalaemia 28.55 14.29 71 14729 50121 29887557
Orthostatic hypotension 28.28 14.29 46 14754 23933 29913745
Pain 27.36 14.29 27 14773 172614 29765064
Drug abuse 27.33 14.29 4 14796 82068 29855610
Coma 27.11 14.29 61 14739 40388 29897290
Cholestasis 26.94 14.29 46 14754 24904 29912774
Sprue-like enteropathy 26.82 14.29 9 14791 338 29937340
Inappropriate antidiuretic hormone secretion 25.78 14.29 30 14770 11392 29926286
Abdominal compartment syndrome 24.96 14.29 11 14789 870 29936808
Hepatocellular injury 24.96 14.29 45 14755 25426 29912252
Wrong drug 24.72 14.29 6 14794 67 29937611
Angioedema 24.33 14.29 53 14747 34331 29903347
Platelet count decreased 24.32 14.29 11 14789 106118 29831560
Vasoplegia syndrome 24.03 14.29 12 14788 1259 29936419
Electrocardiogram QT prolonged 23.96 14.29 54 14746 35781 29901897
Renal artery arteriosclerosis 23.80 14.29 5 14795 27 29937651
Mesenteric vein thrombosis 23.16 14.29 9 14791 517 29937161
Hyperlactacidaemia 23.12 14.29 15 14785 2591 29935087
Hypomagnesaemia 22.57 14.29 34 14766 16564 29921114
Narrow anterior chamber angle 22.06 14.29 4 14796 8 29937670
Bundle branch block right 22.06 14.29 22 14778 7020 29930658
Torsade de pointes 21.68 14.29 22 14778 7168 29930510
Renal artery restenosis 20.91 14.29 4 14796 12 29937666
Mesenteric artery thrombosis 20.80 14.29 8 14792 447 29937231
Laryngeal leukoplakia 20.67 14.29 5 14795 55 29937623
Hypertension 20.61 14.29 116 14684 121238 29816440
Presyncope 20.58 14.29 32 14768 16024 29921654
White blood cell count decreased 20.35 14.29 8 14792 83939 29853739
Respiratory alkalosis 20.17 14.29 11 14789 1383 29936295
Pancreatitis acute 19.79 14.29 41 14759 25654 29912024
Interstitial lung disease 19.71 14.29 70 14730 60127 29877551
Lens dislocation 19.64 14.29 4 14796 18 29937660
Bundle branch block left 19.61 14.29 18 14782 5186 29932492
Acute pulmonary oedema 19.11 14.29 21 14779 7494 29930184
Crystal urine 18.94 14.29 5 14795 80 29937598
Confusional state 18.53 14.29 122 14678 134712 29802966
Autoimmune enteropathy 18.41 14.29 4 14796 26 29937652
Anti factor VIII antibody positive 18.09 14.29 5 14795 96 29937582
Urethral cancer 17.91 14.29 4 14796 30 29937648
Traumatic haemothorax 17.86 14.29 6 14794 226 29937452
Cholangiocarcinoma 17.80 14.29 9 14791 970 29936708
Pneumocystis jirovecii infection 17.78 14.29 10 14790 1335 29936343
Rash maculo-papular 17.77 14.29 39 14761 25379 29912299
Intermittent claudication 17.74 14.29 12 14788 2222 29935456
Melaena 17.51 14.29 45 14755 32392 29905286
Cardiac failure congestive 17.46 14.29 10 14790 84397 29853281
Cell death 17.37 14.29 12 14788 2299 29935379
Cutaneous vasculitis 16.75 14.29 13 14787 2978 29934700
Renal failure 16.71 14.29 115 14685 128851 29808827
Pneumonia 16.71 14.29 97 14703 334209 29603469
Post thrombotic syndrome 16.20 14.29 5 14795 143 29937535
Shock haemorrhagic 16.04 14.29 22 14778 9843 29927835
Disease progression 15.77 14.29 10 14790 79864 29857814
Duodenal ulcer perforation 15.66 14.29 10 14790 1682 29935996
Livedo reticularis 15.53 14.29 11 14789 2193 29935485
Basal ganglia haematoma 15.52 14.29 4 14796 58 29937620
Cerebral haemorrhage 15.12 14.29 43 14757 32844 29904834
Oedema peripheral 14.68 14.29 96 14704 105736 29831942
Acute coronary syndrome 14.61 14.29 25 14775 13548 29924130
Vitamin B12 decreased 14.46 14.29 8 14792 1034 29936644
Eosinophilia 14.37 14.29 33 14767 22127 29915551

Pharmacologic Action:

SourceCodeDescription
ATC C08CA13 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
ATC C09BB02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
ATC C09DB08 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS
Angiotensin II receptor blockers (ARBs) and calcium channel blockers
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.96 Basic
pKa2 2.09 Basic

Orange Book patent data (new drug applications)

None

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 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
D01849 KEGG_DRUG
132866-11-6 SECONDARY_CAS_RN
C0526399 UMLSCUI
CHEBI:135930 CHEBI
CHEMBL250270 ChEMBL_ID
CHEMBL2106419 ChEMBL_ID
DB00528 DRUGBANK_ID
C060343 MESH_SUPPLEMENTAL_RECORD_UI
6971 INN_ID
V7XTJ4R0BH UNII
65866 PUBCHEM_CID
135056 RXNORM
007361 NDDF
007362 NDDF
356862006 SNOMEDCT_US
395768003 SNOMEDCT_US
395986007 SNOMEDCT_US

Pharmaceutical products:

None