nisoldipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 1942 | 63675-72-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.25 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 5 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 5.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 15 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 2, 1995 | FDA | SHIONOGI INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C08CA07 | 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:35554 | cardiovascular agent |
| CHEBI has role | CHEBI:35620 | vasodilator agents |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| CHEBI has role | CHEBI:38215 | calcium channel blockers |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitors |
| FDA PE | N0000178477 | Decreased Blood Pressure |
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Low blood pressure | contraindication | 45007003 | |
| Chronic heart failure | contraindication | 48447003 | |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Hepatic failure | contraindication | 59927004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.37 | 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 | BLOCKER | UNKNOWN | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | GATING INHIBITOR | IC50 | 7.10 | IUPHAR | CHEMBL | |||
| Voltage-dependent P/Q-type calcium channel subunit alpha-1A | Ion channel | WOMBAT-PK | |||||||
| Adenosine receptor A3 | GPCR | Ki | 5.40 | DRUG MATRIX | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | Ki | 5.34 | WOMBAT-PK | |||||
| Cytochrome P450 1A2 | Enzyme | IC50 | 6 | DRUG MATRIX | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.59 | CHEMBL | |||||
| Adenosine receptor A2a | GPCR | Ki | 5.64 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.64 | WOMBAT-PK | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | GATING INHIBITOR | IC50 | 8 | IUPHAR | ||||
| Voltage-dependent L-type calcium channel subunit alpha-1D | Ion channel | GATING INHIBITOR | IC50 | 7 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4020942 | VUID |
| N0000148422 | NUI |
| D00618 | KEGG_DRUG |
| 4020942 | VANDF |
| C0028116 | UMLSCUI |
| CHEBI:7577 | CHEBI |
| CHEMBL1726 | ChEMBL_ID |
| DB00401 | DRUGBANK_ID |
| D015737 | MESH_DESCRIPTOR_UI |
| 4499 | PUBCHEM_CID |
| 2524 | IUPHAR_LIGAND_ID |
| 4753 | INN_ID |
| 4I8HAB65SZ | UNII |
| 7435 | RXNORM |
| 147682 | MMSL |
| 5178 | MMSL |
| d03825 | MMSL |
| 004175 | NDDF |
| 108524004 | SNOMEDCT_US |
| 386861009 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2096 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2096 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2097 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2097 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2098 | TABLET, FILM COATED, EXTENDED RELEASE | 25.50 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2098 | TABLET, FILM COATED, EXTENDED RELEASE | 25.50 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2099 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2099 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | ANDA | 16 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2222 | TABLET, FILM COATED, EXTENDED RELEASE | 20 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2222 | TABLET, FILM COATED, EXTENDED RELEASE | 20 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2223 | TABLET, FILM COATED, EXTENDED RELEASE | 30 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2223 | TABLET, FILM COATED, EXTENDED RELEASE | 30 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2224 | TABLET, FILM COATED, EXTENDED RELEASE | 40 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-2224 | TABLET, FILM COATED, EXTENDED RELEASE | 40 mg | ORAL | ANDA | 25 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0677-1978 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | NDA authorized generic | 27 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0677-1979 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | NDA authorized generic | 27 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0677-1980 | TABLET, FILM COATED, EXTENDED RELEASE | 25.50 mg | ORAL | NDA authorized generic | 27 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0677-1981 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | NDA authorized generic | 27 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5931 | TABLET, FILM COATED, EXTENDED RELEASE | 40 mg | ORAL | ANDA | 26 sections |
| SULAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5993 | TABLET, FILM COATED, EXTENDED RELEASE | 25.50 mg | ORAL | NDA | 26 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66993-472 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | NDA AUTHORIZED GENERIC | 26 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66993-473 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | NDA AUTHORIZED GENERIC | 26 sections |
| Nisoldipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66993-475 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | NDA AUTHORIZED GENERIC | 26 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-500 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | NDA | 25 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-500 | TABLET, FILM COATED, EXTENDED RELEASE | 8.50 mg | ORAL | NDA | 25 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-501 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | NDA | 25 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-501 | TABLET, FILM COATED, EXTENDED RELEASE | 17 mg | ORAL | NDA | 25 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-503 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | NDA | 25 sections |
| Sular | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70515-503 | TABLET, FILM COATED, EXTENDED RELEASE | 34 mg | ORAL | NDA | 25 sections |