felodipine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1142 72509-76-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • felodipine
  • (RS)-Felodipine
  • (+/-)-Felodipine
  • flodil
  • dl-Felodipine
A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.
  • Molecular weight: 384.25
  • Formula: C18H19Cl2NO4
  • CLOGP: 5.30
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 1
  • TPSA: 64.63
  • ALOGS: -4.73
  • ROTB: 6

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
5 mg O

ADMET properties:

PropertyValueReference
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) 0.25 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.87 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 15 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 4.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11 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) 10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 25, 1991 FDA ASTRAZENECA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bradycardia 78.92 43.60 21 301 9960 2347803
Vomiting 78.81 43.60 34 288 71568 2286195
Acute kidney injury 72.85 43.60 25 297 28097 2329666
Orthostatic hypotension 64.12 43.60 14 308 2865 2354898
Hyponatraemia 64.03 43.60 19 303 13306 2344457
Intentional overdose 58.10 43.60 17 305 11304 2346459
Polyuria 57.45 43.60 11 311 1171 2356592
Dizziness 51.83 43.60 24 298 58641 2299122
Hypokalaemia 50.26 43.60 15 307 10639 2347124
Hypotension 47.46 43.60 19 303 32417 2325346
Toxicity to various agents 47.28 43.60 19 303 32735 2325028
Oedema peripheral 45.72 43.60 17 305 23746 2334017

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypotension 61.61 44.74 25 269 29629 1716858
Bradycardia 60.76 44.74 19 275 10515 1735972
Syncope 55.23 44.74 19 275 14150 1732337
Orthostatic hypotension 46.09 44.74 12 282 3419 1743068

Pharmacologic Action:

SourceCodeDescription
ATC C07FB02 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
ATC C08CA02 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
ATC C09BB05 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175421 Dihydropyridine Calcium Channel Blocker
FDA CS M0006414 Dihydropyridines
MeSH PA D000889 Anti-Arrhythmia Agents
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
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:38070 anti-arrhythmia drug
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Prinzmetal angina off-label use 87343002
Angina pectoris off-label use 194828000
Raynaud's phenomenon off-label use 266261006
Hyperkalemia contraindication 14140009
Myocardial infarction contraindication 22298006 DOID:5844
Acute cerebrovascular insufficiency contraindication 29322000
Immunosuppression contraindication 38013005
Angioedema contraindication 41291007 DOID:1558
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Aortic valve stenosis contraindication 60573004 DOID:1712
Transplantation contraindication 77465005
Chronic idiopathic constipation contraindication 82934008
Hereditary angioneurotic edema contraindication 82966003 DOID:14735
Hyponatremia contraindication 89627008
Kidney disease contraindication 90708001 DOID:557
Disorder of connective tissue contraindication 105969002 DOID:65
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Disease of liver contraindication 235856003 DOID:409
Peripheral edema contraindication 271809000
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Hemodialysis with High-Flux Membrane contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.68 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel BLOCKER WOMBAT-PK CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER WOMBAT-PK CHEMBL
Adenosine receptor A3 GPCR Ki 6.22 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 5.34 DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 5.17 WOMBAT-PK
Aldehyde oxidase Enzyme IC50 6.52 WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.43 CHEMBL
Bile acid receptor Nuclear hormone receptor IC50 5.30 CHEMBL
Cystic fibrosis transmembrane conductance regulator Ion channel ACTIVATOR Ki 8.40 IUPHAR

External reference:

IDSource
4020159 VUID
N0000148116 NUI
C0015772 UMLSCUI
D00319 KEGG_DRUG
108535009 SNOMEDCT_US
4316 RXNORM
386863007 SNOMEDCT_US
4716 MMSL
d00231 MMSL
4020159 VANDF
62563 MMSL
003602 NDDF
CHEMBL1480 ChEMBL_ID
CHEMBL428768 ChEMBL_ID
DB01023 DRUGBANK_ID
OL961R6O2C UNII
4877 INN_ID
225 PDB_CHEM_ID
CHEBI:585948 CHEBI
D015736 MESH_DESCRIPTOR_UI
3333 PUBCHEM_CID
4190 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 0603-3581 TABLET, EXTENDED RELEASE 2.50 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 0603-3582 TABLET, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 0603-3583 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 0615-6572 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 0615-6573 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 13668-132 TABLET, EXTENDED RELEASE 2.50 mg ORAL ANDA 17 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 13668-133 TABLET, EXTENDED RELEASE 5 mg ORAL ANDA 17 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 13668-134 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 17 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 23155-048 TABLET, EXTENDED RELEASE 2.50 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 23155-049 TABLET, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 23155-050 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 50090-4808 TABLET, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 53489-368 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL ANDA 11 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 53489-369 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 11 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 53489-370 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 11 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 54868-0823 TABLET, FILM COATED 2.50 mg ORAL ANDA 12 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 54868-0826 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 12 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 54868-5197 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 12 sections
FELODIPINE HUMAN PRESCRIPTION DRUG LABEL 1 55648-411 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL ANDA 10 sections
FELODIPINE HUMAN PRESCRIPTION DRUG LABEL 1 55648-412 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
FELODIPINE HUMAN PRESCRIPTION DRUG LABEL 1 55648-414 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 57237-108 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 57237-109 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 57237-110 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 59746-369 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 59746-370 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL ANDA 10 sections
Felodipine HUMAN PRESCRIPTION DRUG LABEL 1 59746-371 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL ANDA 10 sections
FELODIPINEEXTENDED-RELEASE TABLETS HUMAN PRESCRIPTION DRUG LABEL 1 63304-435 TABLET, EXTENDED RELEASE 2.50 mg ORAL NDA 11 sections
FELODIPINEEXTENDED-RELEASE TABLETS HUMAN PRESCRIPTION DRUG LABEL 1 63304-436 TABLET, EXTENDED RELEASE 5 mg ORAL NDA 11 sections
FELODIPINEEXTENDED-RELEASE TABLETS HUMAN PRESCRIPTION DRUG LABEL 1 63304-437 TABLET, EXTENDED RELEASE 10 mg ORAL NDA 11 sections