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 | 94.47 | 27.15 | 43 | 2630 | 36856 | 53309537 |
| Cerebral infarction | 67.33 | 27.15 | 30 | 2643 | 24414 | 53321979 |
| Inappropriate antidiuretic hormone secretion | 63.55 | 27.15 | 25 | 2648 | 14926 | 53331467 |
| Renal impairment | 48.11 | 27.15 | 37 | 2636 | 83281 | 53263112 |
| Blood urea increased | 44.23 | 27.15 | 23 | 2650 | 26208 | 53320185 |
| Blood creatinine increased | 44.02 | 27.15 | 35 | 2638 | 82627 | 53263766 |
| Altered state of consciousness | 42.52 | 27.15 | 22 | 2651 | 24814 | 53321579 |
| Cardiac failure | 36.67 | 27.15 | 32 | 2641 | 85812 | 53260581 |
| Platelet count decreased | 35.89 | 27.15 | 35 | 2638 | 108064 | 53238329 |
| Decreased appetite | 31.79 | 27.15 | 46 | 2627 | 214928 | 53131465 |
| Interstitial lung disease | 29.44 | 27.15 | 24 | 2649 | 58598 | 53287795 |
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 | 76.66 | 24.08 | 57 | 3009 | 64944 | 32445516 |
| Cerebral infarction | 46.05 | 24.08 | 30 | 3036 | 27584 | 32482876 |
| Renal impairment | 44.79 | 24.08 | 49 | 3017 | 91923 | 32418537 |
| Hepatic function abnormal | 43.36 | 24.08 | 35 | 3031 | 44805 | 32465655 |
| Platelet count decreased | 37.66 | 24.08 | 50 | 3016 | 114541 | 32395919 |
| Blood urea increased | 32.90 | 24.08 | 26 | 3040 | 32247 | 32478213 |
| Liver disorder | 31.20 | 24.08 | 25 | 3041 | 31629 | 32478831 |
| Cardiac failure | 30.08 | 24.08 | 40 | 3026 | 91633 | 32418827 |
| Dyslalia | 26.94 | 24.08 | 7 | 3059 | 580 | 32509880 |
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 | IC50 | 5.31 | IUPHAR | SCIENTIFIC LITERATURE | |||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | BLOCKER | IC50 | 6.84 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 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 |
| C061004 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10159 | IUPHAR_LIGAND_ID |
| C050883 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6137 | INN_ID |
| 4G9T91JS7E | UNII |
| 656668 | PUBCHEM_CID |
| 008170 | NDDF |
| 008171 | NDDF |
Pharmaceutical products:
None