Stem definition | Drug id | CAS RN |
---|---|---|
calcium channel blockers, nifedipine derivatives | 1909 | 55985-32-5 |
Dose | Unit | Route |
---|---|---|
90 | mg | O |
90 | mg | P |
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) | 23 % | 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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 21, 1988 | FDA | CHIESI USA INC |
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 |
---|---|---|---|---|---|---|
Cerebral vasoconstriction | 132.80 | 20.56 | 31 | 7128 | 1002 | 46677901 |
Acute pulmonary oedema | 130.03 | 20.56 | 48 | 7111 | 7843 | 46671060 |
Hyponatraemia | 104.10 | 20.56 | 101 | 7058 | 101231 | 46577672 |
Premature delivery | 96.37 | 20.56 | 53 | 7106 | 22016 | 46656887 |
Exposure during pregnancy | 93.10 | 20.56 | 98 | 7061 | 108114 | 46570789 |
Posterior reversible encephalopathy syndrome | 84.95 | 20.56 | 43 | 7116 | 15098 | 46663805 |
Acute kidney injury | 83.70 | 20.56 | 138 | 7021 | 235717 | 46443186 |
Hepatocellular injury | 79.63 | 20.56 | 52 | 7107 | 29470 | 46649433 |
Acute motor-sensory axonal neuropathy | 74.17 | 20.56 | 16 | 7143 | 358 | 46678545 |
Maternal exposure during pregnancy | 64.53 | 20.56 | 79 | 7080 | 102470 | 46576433 |
Cerebral haemorrhage | 62.27 | 20.56 | 44 | 7115 | 28327 | 46650576 |
Low birth weight baby | 60.91 | 20.56 | 25 | 7134 | 5409 | 46673494 |
Hyperkalaemia | 60.53 | 20.56 | 55 | 7104 | 50654 | 46628249 |
Premature labour | 54.50 | 20.56 | 29 | 7130 | 11270 | 46667633 |
Bradycardia | 53.33 | 20.56 | 58 | 7101 | 66240 | 46612663 |
Haemorrhagic transformation stroke | 51.59 | 20.56 | 15 | 7144 | 1155 | 46677748 |
Orthostatic hypotension | 51.25 | 20.56 | 37 | 7122 | 24621 | 46654282 |
Cholestasis | 50.59 | 20.56 | 38 | 7121 | 26855 | 46652048 |
Eosinophilia | 47.33 | 20.56 | 32 | 7127 | 19185 | 46659718 |
Lactic acidosis | 46.90 | 20.56 | 40 | 7119 | 33869 | 46645034 |
Fall | 45.86 | 20.56 | 132 | 7027 | 328965 | 46349938 |
Haemangioma congenital | 43.93 | 20.56 | 11 | 7148 | 479 | 46678424 |
Purpura | 43.68 | 20.56 | 24 | 7135 | 9934 | 46668969 |
Acute generalised exanthematous pustulosis | 42.17 | 20.56 | 23 | 7136 | 9382 | 46669521 |
Paradoxical drug reaction | 41.15 | 20.56 | 15 | 7144 | 2361 | 46676542 |
Hemivertebra | 40.30 | 20.56 | 8 | 7151 | 117 | 46678786 |
Thrombocytopenia | 39.38 | 20.56 | 70 | 7089 | 126511 | 46552392 |
Caesarean section | 39.34 | 20.56 | 27 | 7132 | 16576 | 46662327 |
Drug interaction | 39.06 | 20.56 | 92 | 7067 | 203002 | 46475901 |
Fatigue | 38.47 | 20.56 | 23 | 7136 | 608674 | 46070229 |
Toxic skin eruption | 36.29 | 20.56 | 23 | 7136 | 12364 | 46666539 |
Hypotension | 35.98 | 20.56 | 97 | 7062 | 232492 | 46446411 |
Premature baby | 34.97 | 20.56 | 26 | 7133 | 18086 | 46660817 |
Hypertension | 34.59 | 20.56 | 86 | 7073 | 196270 | 46482633 |
Ischaemic stroke | 34.53 | 20.56 | 25 | 7134 | 16697 | 46662206 |
Patent ductus arteriosus | 34.09 | 20.56 | 15 | 7144 | 3847 | 46675056 |
Congenital choroid plexus cyst | 33.37 | 20.56 | 8 | 7151 | 290 | 46678613 |
Hypokalaemia | 33.10 | 20.56 | 53 | 7106 | 87971 | 46590932 |
Haematoma | 33.07 | 20.56 | 32 | 7127 | 31840 | 46647063 |
Agranulocytosis | 32.37 | 20.56 | 27 | 7132 | 22158 | 46656745 |
Renal failure | 31.75 | 20.56 | 60 | 7099 | 113534 | 46565369 |
Pain | 31.55 | 20.56 | 17 | 7142 | 476931 | 46201972 |
Gestational hypertension | 31.45 | 20.56 | 12 | 7147 | 2143 | 46676760 |
Subarachnoid haemorrhage | 30.92 | 20.56 | 20 | 7139 | 11133 | 46667770 |
Arthralgia | 30.63 | 20.56 | 9 | 7150 | 364594 | 46314309 |
Foetal growth restriction | 29.27 | 20.56 | 16 | 7143 | 6551 | 46672352 |
Tumour rupture | 29.05 | 20.56 | 6 | 7153 | 108 | 46678795 |
Anaphylactic shock | 28.19 | 20.56 | 24 | 7135 | 20250 | 46658653 |
Foetal arrhythmia | 26.80 | 20.56 | 6 | 7153 | 160 | 46678743 |
Metabolic encephalopathy | 26.42 | 20.56 | 14 | 7145 | 5389 | 46673514 |
Pre-eclampsia | 26.35 | 20.56 | 16 | 7143 | 7978 | 46670925 |
Cutaneous lupus erythematosus | 26.19 | 20.56 | 11 | 7148 | 2518 | 46676385 |
Rhabdomyolysis | 25.84 | 20.56 | 32 | 7127 | 41877 | 46637026 |
Drug reaction with eosinophilia and systemic symptoms | 25.76 | 20.56 | 27 | 7132 | 29521 | 46649382 |
Rash maculo-papular | 25.25 | 20.56 | 26 | 7133 | 27848 | 46651055 |
Drug hypersensitivity | 24.53 | 20.56 | 4 | 7155 | 243821 | 46435082 |
Acquired haemophilia | 24.36 | 20.56 | 8 | 7151 | 923 | 46677980 |
Haemodynamic instability | 24.28 | 20.56 | 15 | 7144 | 7710 | 46671193 |
Nausea | 24.13 | 20.56 | 43 | 7116 | 687411 | 45991492 |
Cardiogenic shock | 24.02 | 20.56 | 20 | 7139 | 16364 | 46662539 |
Mixed liver injury | 23.90 | 20.56 | 11 | 7148 | 3132 | 46675771 |
Blood pressure decreased | 23.68 | 20.56 | 36 | 7123 | 57123 | 46621780 |
Intra-abdominal haematoma | 23.50 | 20.56 | 9 | 7150 | 1622 | 46677281 |
Foetal exposure during pregnancy | 23.14 | 20.56 | 26 | 7133 | 30721 | 46648182 |
Wrong patient received product | 22.95 | 20.56 | 9 | 7150 | 1728 | 46677175 |
Metabolic acidosis | 22.93 | 20.56 | 29 | 7130 | 38751 | 46640152 |
Respiratory distress | 22.35 | 20.56 | 26 | 7133 | 31890 | 46647013 |
Rheumatoid arthritis | 21.92 | 20.56 | 5 | 7154 | 240210 | 46438693 |
Porphyria acute | 21.84 | 20.56 | 6 | 7153 | 376 | 46678527 |
Altered state of consciousness | 21.55 | 20.56 | 22 | 7137 | 23326 | 46655577 |
Walking disability | 21.29 | 20.56 | 8 | 7151 | 1370 | 46677533 |
Sinus bradycardia | 20.57 | 20.56 | 17 | 7142 | 13765 | 46665138 |
Bronchiolitis | 20.57 | 20.56 | 9 | 7150 | 2276 | 46676627 |
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 |
---|---|---|---|---|---|---|
Cerebral vasoconstriction | 113.31 | 19.13 | 21 | 4950 | 191 | 29947316 |
Blood lactic acid | 78.24 | 19.13 | 17 | 4954 | 363 | 29947144 |
Acute kidney injury | 69.69 | 19.13 | 145 | 4826 | 273697 | 29673810 |
Premature baby | 64.41 | 19.13 | 38 | 4933 | 16653 | 29930854 |
Foetal disorder | 63.93 | 19.13 | 16 | 4955 | 642 | 29946865 |
Cerebral haemorrhage | 62.00 | 19.13 | 48 | 4923 | 32839 | 29914668 |
Neutropenia neonatal | 56.80 | 19.13 | 14 | 4957 | 527 | 29946980 |
Low birth weight baby | 49.98 | 19.13 | 23 | 4948 | 6053 | 29941454 |
Foetal exposure during pregnancy | 45.15 | 19.13 | 42 | 4929 | 36829 | 29910678 |
Antiphospholipid antibodies positive | 43.25 | 19.13 | 10 | 4961 | 285 | 29947222 |
Cholestasis | 33.62 | 19.13 | 30 | 4941 | 24920 | 29922587 |
Haemorrhagic cerebral infarction | 33.53 | 19.13 | 10 | 4961 | 776 | 29946731 |
Eosinophilia | 32.58 | 19.13 | 28 | 4943 | 22132 | 29925375 |
Phlebitis deep | 31.59 | 19.13 | 5 | 4966 | 15 | 29947492 |
Rash maculo-papular | 31.19 | 19.13 | 29 | 4942 | 25389 | 29922118 |
Bradycardia | 29.90 | 19.13 | 45 | 4926 | 65481 | 29882026 |
Paradoxical drug reaction | 28.08 | 19.13 | 12 | 4959 | 2650 | 29944857 |
Brain herniation | 27.18 | 19.13 | 13 | 4958 | 3727 | 29943780 |
Extravasation | 25.27 | 19.13 | 10 | 4961 | 1818 | 29945689 |
Kidney small | 25.20 | 19.13 | 5 | 4966 | 67 | 29947440 |
Cerebral haematoma | 24.86 | 19.13 | 13 | 4958 | 4501 | 29943006 |
Hypertension | 23.63 | 19.13 | 58 | 4913 | 121296 | 29826211 |
Drug reaction with eosinophilia and systemic symptoms | 23.09 | 19.13 | 26 | 4945 | 28462 | 29919045 |
Hyperkalaemia | 22.84 | 19.13 | 40 | 4931 | 65970 | 29881537 |
Injection site oedema | 22.65 | 19.13 | 5 | 4966 | 115 | 29947392 |
Aortic dissection | 22.47 | 19.13 | 10 | 4961 | 2432 | 29945075 |
Renal failure | 22.37 | 19.13 | 59 | 4912 | 128907 | 29818600 |
Hypertensive crisis | 22.12 | 19.13 | 15 | 4956 | 8342 | 29939165 |
Fatigue | 22.06 | 19.13 | 13 | 4958 | 320660 | 29626847 |
Death | 21.24 | 19.13 | 17 | 4954 | 357266 | 29590241 |
Phlebitis | 21.16 | 19.13 | 11 | 4960 | 3764 | 29943743 |
Respiratory gas exchange disorder | 20.78 | 19.13 | 6 | 4965 | 416 | 29947091 |
Cerebral infarction | 19.57 | 19.13 | 23 | 4948 | 26350 | 29921157 |
Blood fibrinogen decreased | 19.44 | 19.13 | 7 | 4964 | 982 | 29946525 |
Macroglossia | 19.44 | 19.13 | 5 | 4966 | 224 | 29947283 |
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 | 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 |
MeSH PA | D014665 | Vasodilator Agents |
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 |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 7.02 | Basic |
pKa2 | 2.37 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Voltage-gated L-type calcium channel | Ion channel | BLOCKER | CHEMBL | CHEMBL | |||||
Nuclear receptor subfamily 1 group I member 2 | Nuclear hormone receptor | WOMBAT-PK | |||||||
Cytochrome P450 2C9 | Enzyme | IC50 | 6.55 | WOMBAT-PK | |||||
Cytochrome P450 3A4 | Enzyme | IC50 | 6.38 | WOMBAT-PK | |||||
Multidrug resistance protein 1 | Transporter | IC50 | 5.32 | CHEMBL | |||||
Malate dehydrogenase cytoplasmic | Enzyme | IC50 | 4.30 | CHEMBL | |||||
Adenosine receptor A3 | GPCR | Ki | 5.49 | CHEMBL | |||||
ATP-binding cassette sub-family G member 2 | Transporter | IC50 | 4.78 | CHEMBL | |||||
Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | Ki | 5.55 | WOMBAT-PK | |||||
Adrenergic receptor alpha-2 | GPCR | IC50 | 5.85 | CHEMBL | |||||
Equilibrative nucleoside transporter 1 | Transporter | Ki | 5.27 | CHEMBL | |||||
Beta-lactamase | Enzyme | IC50 | 4.70 | CHEMBL | |||||
Adenosine receptor A3 | GPCR | Ki | 4.96 | CHEMBL | |||||
Adrenergic receptor alpha-1 | GPCR | IC50 | 5.44 | CHEMBL | |||||
Adenosine receptor A2a | GPCR | Ki | 4.20 | CHEMBL | |||||
Voltage-gated L-type calcium channel | Ion channel | Ki | 9.08 | CHEMBL | |||||
Adenosine receptor A1 | GPCR | Ki | 4.71 | CHEMBL | |||||
Potassium voltage-gated channel subfamily A member 4 | Unclassified | BLOCKER | IC50 | 6.10 | IUPHAR |
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Nicardipine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9542 | INJECTION | 2.50 mg | INTRAVENOUS | NDA | 26 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 | 0378-1020 | CAPSULE | 20 mg | ORAL | ANDA | 22 sections |
Nicardipine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-1430 | CAPSULE | 30 mg | ORAL | ANDA | 22 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 |
Cardene IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10122-313 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | NDA | 23 sections |
Cardene IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10122-314 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | NDA | 23 sections |
Cardene IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10122-325 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | NDA | 23 sections |
Nicardipine Hydrochloride | Human Prescription Drug Label | 1 | 14593-124 | 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 | 40042-047 | INJECTION, SOLUTION | 2.50 mg | INTRAVENOUS | ANDA | 20 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 | 24 sections |
CARDENE IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-016 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | NDA | 24 sections |
Cardene IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-021 | INJECTION, SOLUTION | 0.10 mg | INTRAVENOUS | NDA | 24 sections |
Cardene IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-024 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | NDA | 24 sections |
CARDENE IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-026 | INJECTION, SOLUTION | 0.10 mg | INTRAVENTRICULAR | NDA | 24 sections |
CARDENE IV | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43066-028 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | NDA | 24 sections |
nicardipine hydrochloride | Human Prescription Drug Label | 1 | 47335-882 | INJECTION | 2.50 mg | INTRAVENOUS | NDA | 24 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 | 55648-631 | INJECTION | 2.50 mg | INTRAVENOUS | ANDA | 16 sections |