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isradipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 1511 | 75695-93-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
| 5 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.01 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) | 0.77 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 19.50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 26 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.04 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.30 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.021 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.406 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 51.168 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 98.175 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.360 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.400 | % | High | 1 |
| herg | hERG pIC50 | 4.930 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 71.945 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 266.686 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.350 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK4,PDPK1,PIK3CB,PIK3CG,PRKDC,STK33,TEK | 25 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,PDK4,PIK3CD | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.663 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 103.039 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.900 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.875 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.590 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 229.087 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 14.180 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.360 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 24.322 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 20, 1990 | FDA | SMITHKLINE BEECHAM |
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 |
|---|---|---|---|---|---|---|
| Drug interaction | 47.44 | 37.77 | 25 | 466 | 276428 | 90351528 |
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 |
|---|---|---|---|---|---|---|
| Retinal disorder | 53.32 | 40.04 | 9 | 317 | 1166 | 42619843 |
| Diverticulitis intestinal perforated | 49.33 | 40.04 | 7 | 319 | 289 | 42620720 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Diverticulitis intestinal perforated | 45.19 | 35.09 | 7 | 800 | 550 | 110587942 |
| Tubulointerstitial nephritis | 36.42 | 35.09 | 14 | 793 | 54270 | 110534222 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C08CA03 | 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 |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
| 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 |
Related Drugs by ATC class:
C08CA Dihydropyridine derivatives 17 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Angina pectoris | off-label use | 194828000 | |
| Raynaud's phenomenon | off-label use | 266261006 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Low blood pressure | contraindication | 45007003 | |
| Chronic heart failure | contraindication | 48447003 | |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Peripheral edema | contraindication | 271809000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 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-dependent L-type calcium channel subunit alpha-1D | Ion channel | GATING INHIBITOR | IC50 | 9.30 | IUPHAR | CHEMBL | |||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | GATING INHIBITOR | IC50 | 8.80 | IUPHAR | CHEMBL | |||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | Ki | 5.51 | WOMBAT-PK | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.30 | CHEMBL | |||||
| Nuclear receptor subfamily 1 group I member 2 | Nuclear hormone receptor | WOMBAT-PK | |||||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | IC50 | 6.97 | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1D | Ion channel | IC50 | 6.66 | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1F | Ion channel | GATING INHIBITOR | IC50 | 6.70 | IUPHAR | ||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | GATING INHIBITOR | IC50 | 7.50 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4019560 | VUID |
| N0000147660 | NUI |
| D00349 | KEGG_DRUG |
| 4019560 | VANDF |
| C0071304 | UMLSCUI |
| CHEBI:6073 | CHEBI |
| CHEMBL399539 | ChEMBL_ID |
| CHEMBL1648 | ChEMBL_ID |
| CHEMBL400875 | ChEMBL_ID |
| DB00270 | DRUGBANK_ID |
| D017275 | MESH_DESCRIPTOR_UI |
| 3784 | PUBCHEM_CID |
| 4488 | IUPHAR_LIGAND_ID |
| 5724 | INN_ID |
| YO1UK1S598 | UNII |
| 33910 | RXNORM |
| 4939 | MMSL |
| 73302 | MMSL |
| d00270 | MMSL |
| 003570 | NDDF |
| 108533002 | SNOMEDCT_US |
| 386862002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16252-539 | CAPSULE | 2.50 mg | ORAL | ANDA | 20 sections |
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16252-540 | CAPSULE | 5 mg | ORAL | ANDA | 20 sections |
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-062 | CAPSULE | 2.50 mg | ORAL | ANDA | 20 sections |
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64850-910 | CAPSULE | 2.50 mg | ORAL | ANDA | 17 sections |
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64850-911 | CAPSULE | 5 mg | ORAL | ANDA | 17 sections |
| Isradipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-1333 | CAPSULE | 5 mg | ORAL | ANDA | 20 sections |