benidipine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 3880 | 105979-17-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1.90 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.23 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1991 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Hepatic function abnormal | 93.43 | 25.99 | 43 | 2530 | 34378 | 46649111 |
| Cerebral infarction | 62.76 | 25.99 | 29 | 2544 | 23337 | 46660152 |
| Inappropriate antidiuretic hormone secretion | 62.67 | 25.99 | 25 | 2548 | 14077 | 46669412 |
| Renal impairment | 46.52 | 25.99 | 36 | 2537 | 74336 | 46609153 |
| Blood urea increased | 42.91 | 25.99 | 23 | 2550 | 25329 | 46658160 |
| Altered state of consciousness | 41.83 | 25.99 | 22 | 2551 | 23326 | 46660163 |
| Blood creatinine increased | 37.26 | 25.99 | 32 | 2541 | 76371 | 46607118 |
| Cardiac failure | 34.03 | 25.99 | 31 | 2542 | 79917 | 46603572 |
| Platelet count decreased | 33.53 | 25.99 | 34 | 2539 | 99990 | 46583499 |
| Decreased appetite | 32.09 | 25.99 | 46 | 2527 | 193790 | 46489699 |
| Interstitial lung disease | 29.18 | 25.99 | 24 | 2549 | 53925 | 46629564 |
| Hyperuricaemia | 26.78 | 25.99 | 10 | 2563 | 4707 | 46678782 |
| Disseminated intravascular coagulation | 26.01 | 25.99 | 15 | 2558 | 18990 | 46664499 |
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 |
|---|---|---|---|---|---|---|
| Interstitial lung disease | 71.39 | 23.42 | 54 | 2910 | 60143 | 29889371 |
| Hepatic function abnormal | 43.93 | 23.42 | 35 | 2929 | 41910 | 29907604 |
| Cerebral infarction | 43.56 | 23.42 | 29 | 2935 | 26344 | 29923170 |
| Renal impairment | 42.91 | 23.42 | 47 | 2917 | 84137 | 29865377 |
| Platelet count decreased | 38.79 | 23.42 | 50 | 2914 | 106079 | 29843435 |
| Blood urea increased | 32.44 | 23.42 | 26 | 2938 | 31355 | 29918159 |
| Liver disorder | 31.53 | 23.42 | 25 | 2939 | 29697 | 29919817 |
| Cardiac failure | 28.42 | 23.42 | 38 | 2926 | 83380 | 29866134 |
| Dyslalia | 27.61 | 23.42 | 7 | 2957 | 501 | 29949013 |
| Drug eruption | 23.58 | 23.42 | 17 | 2947 | 17509 | 29932005 |
| Blood pressure decreased | 23.44 | 23.42 | 26 | 2938 | 47049 | 29902465 |
| Prinzmetal angina | 23.43 | 23.42 | 7 | 2957 | 922 | 29948592 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C08CA15 | CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives |
| 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 |
Drug Use (View source of the data)
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.05 | Basic |
| pKa2 | 2.23 | 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]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-gated L-type calcium channel | Ion channel | BLOCKER | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | BLOCKER | IC50 | 6.84 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 4G9T91JS7E | UNII |
| D02045 | KEGG_DRUG |
| 91599-74-5 | SECONDARY_CAS_RN |
| C0053108 | UMLSCUI |
| CHEBI:135806 | CHEBI |
| CHEMBL2074972 | ChEMBL_ID |
| CHEMBL2105555 | ChEMBL_ID |
| CHEMBL2218858 | ChEMBL_ID |
| DB09231 | DRUGBANK_ID |
| 6137 | INN_ID |
| C061004 | MESH_SUPPLEMENTAL_RECORD_UI |
| C050883 | MESH_SUPPLEMENTAL_RECORD_UI |
| 656668 | PUBCHEM_CID |
| 10159 | IUPHAR_LIGAND_ID |
| 008170 | NDDF |
| 008171 | NDDF |
Pharmaceutical products:
None