nimodipine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 1937 | 66085-59-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
| 50 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 14.34 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 11 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 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) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.30 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 28, 1988 | FDA |
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 |
|---|---|---|---|---|---|---|
| Patent ductus arteriosus | 81.51 | 38.01 | 17 | 619 | 3845 | 46681581 |
| Subarachnoid haemorrhage | 49.63 | 38.01 | 14 | 622 | 11139 | 46674287 |
| Cerebral vasoconstriction | 49.23 | 38.01 | 9 | 627 | 1024 | 46684402 |
| Foetal exposure during pregnancy | 46.60 | 38.01 | 17 | 619 | 30730 | 46654696 |
| Premature baby | 42.94 | 38.01 | 14 | 622 | 18098 | 46667328 |
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 |
|---|---|---|---|---|---|---|
| Brain injury | 81.74 | 70.26 | 19 | 504 | 5529 | 29946426 |
| Cerebral ischaemia | 74.46 | 70.26 | 18 | 505 | 6182 | 29945773 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C08CA06 | 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 |
| CHEBI has role | CHEBI:35554 | cardiovascular drugs |
| CHEBI has role | CHEBI:35620 | vasodilator |
| CHEBI has role | CHEBI:35674 | antihypertensive |
| CHEBI has role | CHEBI:38215 | calcium channel blockers |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Subarachnoid intracranial hemorrhage | indication | 21454007 | |
| nerve regeneration after iatrogenic nerve injury | off-label use | 57182000 | |
| Essential tremor | off-label use | 609558009 | DOID:4990 |
| Low blood pressure | contraindication | 45007003 | |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.09 | 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 | BLOCKER | UNKNOWN | CHEMBL | |||||
| Cytochrome P450 2C9 | Enzyme | IC50 | 6 | DRUG MATRIX | |||||
| Cytochrome P450 2C19 | Enzyme | IC50 | 5.40 | DRUG MATRIX | |||||
| Sodium/nucleoside cotransporter 1 | Transporter | Ki | 6.36 | DRUG MATRIX | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | Ki | 5.25 | WOMBAT-PK | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.07 | WOMBAT-PK | |||||
| Cytochrome P450 3A4 | Enzyme | Ki | 6.12 | WOMBAT-PK | |||||
| Mineralocorticoid receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 6.80 | IUPHAR | ||||
| Nuclear receptor subfamily 1 group I member 2 | Nuclear hormone receptor | EC50 | 6.41 | CHEMBL | |||||
| Bile acid receptor | Nuclear hormone receptor | IC50 | 5.05 | CHEMBL | |||||
| Voltage-dependent calcium channel gamma-1 subunit | Ion channel | WOMBAT-PK | |||||||
| Voltage-dependent L-type calcium channel subunit alpha-1F | Ion channel | GATING INHIBITOR | IC50 | 6 | IUPHAR | ||||
| Voltage-dependent L-type calcium channel subunit alpha-1S | Ion channel | GATING INHIBITOR | IC50 | 6 | IUPHAR | ||||
| Cannabinoid receptor 1 | GPCR | Ki | 5.86 | DRUG MATRIX | |||||
| Adenosine receptor A2a | GPCR | Ki | 4.35 | CHEMBL | |||||
| Adenosine receptor A1 | GPCR | Ki | 4.70 | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | GATING INHIBITOR | IC50 | 6.80 | IUPHAR | ||||
| Voltage-dependent L-type calcium channel subunit alpha-1D | Ion channel | GATING INHIBITOR | IC50 | 6.60 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4019390 | VUID |
| N0000147543 | NUI |
| D00438 | KEGG_DRUG |
| 4019390 | VANDF |
| C0028094 | UMLSCUI |
| CHEBI:7575 | CHEBI |
| 6U9 | PDB_CHEM_ID |
| CHEMBL1428 | ChEMBL_ID |
| CHEMBL255033 | ChEMBL_ID |
| D009553 | MESH_DESCRIPTOR_UI |
| DB00393 | DRUGBANK_ID |
| 2523 | IUPHAR_LIGAND_ID |
| 4528 | INN_ID |
| 57WA9QZ5WH | UNII |
| 4497 | PUBCHEM_CID |
| 1423768 | RXNORM |
| 109672 | MMSL |
| 203915 | MMSL |
| 5177 | MMSL |
| d00318 | MMSL |
| 000713 | NDDF |
| 387502003 | SNOMEDCT_US |
| 87285001 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23155-512 | CAPSULE, LIQUID FILLED | 30 mg | ORAL | ANDA | 13 sections |
| Nymalize | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24338-200 | SOLUTION | 60 mg | ORAL | NDA | 25 sections |
| Nymalize | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24338-205 | SOLUTION | 30 mg | ORAL | NDA | 25 sections |
| Nymalize | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24338-230 | SOLUTION | 30 mg | ORAL | NDA | 26 sections |
| Nymalize | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24338-260 | SOLUTION | 60 mg | ORAL | NDA | 26 sections |
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-210 | CAPSULE | 30 mg | ORAL | ANDA | 23 sections |
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63739-797 | CAPSULE, LIQUID FILLED | 30 mg | ORAL | ANDA | 25 sections |
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67877-297 | CAPSULE, LIQUID FILLED | 30 mg | ORAL | ANDA | 26 sections |
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-912 | CAPSULE, LIQUID FILLED | 30 mg | ORAL | ANDA | 26 sections |
| Nimodipine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-209 | CAPSULE, LIQUID FILLED | 30 mg | ORAL | ANDA | 23 sections |