milrinone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cardiac stimulants, amrinone derivatives 1809 78415-72-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • primacor
  • milrinone
  • corotrop
  • corotrope
  • milrinone lactate
A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.
  • Molecular weight: 211.22
  • Formula: C12H9N3O
  • CLOGP: -0.03
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 65.78
  • ALOGS: -3
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Bocci G, Oprea TI, Benet LZ
S (Water solubility) 0.21 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 85 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.35 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 86 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.25 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 6.20 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) 0.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1987 FDA SANOFI AVENTIS US

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
Drug ineffective for unapproved indication 72.07 44.98 29 1695 34034 63453264
Cardiac arrest 70.84 44.98 39 1685 92506 63394792
Pulmonary hypertension 66.30 44.98 28 1696 37095 63450203
Respiratory failure 64.70 44.98 38 1686 101820 63385478
Drug ineffective 63.90 44.98 106 1618 1044659 62442639
Hypotension 59.34 44.98 53 1671 272551 63214747
Cardiogenic shock 58.66 44.98 21 1703 17911 63469387
Ventricular tachycardia 56.44 44.98 21 1703 19958 63467340
Right ventricular dysfunction 54.01 44.98 12 1712 1807 63485491
Multiple organ dysfunction syndrome 46.36 44.98 25 1699 56727 63430571

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
Drug ineffective 141.88 38.45 134 1441 456617 34498739
Off label use 38.74 38.45 68 1507 419456 34535900

FDA Adverse Event Reporting System (Geriatric)

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
Drug ineffective 165.61 36.77 199 2736 1080714 78660739
Cardiac arrest 86.30 36.77 62 2873 172034 79569419
Cardiogenic shock 82.32 36.77 37 2898 41877 79699576
Pulmonary hypertension 77.47 36.77 37 2898 48043 79693410
Drug ineffective for unapproved indication 72.26 36.77 36 2899 51202 79690251
Ventricular tachycardia 69.78 36.77 33 2902 41902 79699551
Hypotension 61.43 36.77 78 2857 440239 79301214
Right ventricular failure 60.07 36.77 25 2910 23472 79717981
Off label use 58.01 36.77 112 2823 907103 78834350
Respiratory failure 53.77 36.77 48 2887 180863 79560590
Multiple organ dysfunction syndrome 44.06 36.77 36 2899 120210 79621243
Heparin-induced thrombocytopenia 41.49 36.77 15 2920 9667 79731786
Cardiac failure chronic 39.45 36.77 15 2920 11120 79730333
Cardiac failure 38.08 36.77 37 2898 154805 79586648
Cardiomyopathy 36.97 36.77 19 2916 28755 79712698

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CE02 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Phosphodiesterase inhibitors
FDA MoA N0000175086 Phosphodiesterase 3 Inhibitors
FDA EPC N0000175598 Phosphodiesterase 3 Inhibitor
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:38147 cardiotonic drugs
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:50568 3,5-cyclic nucleoside monophosphate phosphodiesterase inhibitors
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Decompensated cardiac failure indication 195111005
Myocardial infarction contraindication 22298006 DOID:5844
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Pulmonic valve stenosis contraindication 56786000 DOID:6420
Kidney disease contraindication 90708001 DOID:557
Idiopathic hypertrophic subaortic stenosis contraindication 360465008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.97 acidic
pKa2 6.24 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
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme INHIBITOR IC50 6.36 CHEMBL CHEMBL
cGMP-specific 3',5'-cyclic phosphodiesterase Enzyme IC50 6.13 CHEMBL
cGMP-inhibited 3',5'-cyclic phosphodiesterase B Enzyme IC50 6.55 CHEMBL
Phosphodiesterase 3 Enzyme Ki 6.82 CHEMBL
Phosphodiesterase 4 Enzyme IC50 5.22 CHEMBL
Cyclic nucleotide phosphodiesterase PDE3A Enzyme IC50 6.07 CHEMBL
Cyclic AMP-specific phosphodiesterase SSPDE4A1A Enzyme IC50 4.89 CHEMBL
Uncharacterized protein Enzyme IC50 6 CHEMBL
cGMP-specific 3',5'-cyclic phosphodiesterase Enzyme IC50 5.30 CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4A Enzyme Ki 5.33 CHEMBL

External reference:

IDSource
4023601 VUID
N0000021606 NUI
D00417 KEGG_DRUG
100286-97-3 SECONDARY_CAS_RN
4020722 VANDF
4023601 VANDF
C0128513 UMLSCUI
CHEBI:50693 CHEBI
MIL PDB_CHEM_ID
CHEMBL189 ChEMBL_ID
DB00235 DRUGBANK_ID
CHEMBL1200977 ChEMBL_ID
D020105 MESH_DESCRIPTOR_UI
4197 PUBCHEM_CID
5225 IUPHAR_LIGAND_ID
5383 INN_ID
JU9YAX04C7 UNII
155120 RXNORM
43671 MMSL
5116 MMSL
6676 MMSL
d00302 MMSL
004083 NDDF
004084 NDDF
108480007 SNOMEDCT_US
108481006 SNOMEDCT_US
373441005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9326 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9326 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9373 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9373 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9374 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9374 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9708 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9708 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9709 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9709 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9710 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0143-9710 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0143-9718 INJECTION, SOLUTION 200 ug INTRAVENOUS ANDA 21 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0143-9718 INJECTION, SOLUTION 200 ug INTRAVENOUS ANDA 21 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0143-9719 INJECTION, SOLUTION 200 ug INTRAVENOUS ANDA 21 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0143-9719 INJECTION, SOLUTION 200 ug INTRAVENOUS ANDA 21 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-6010 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-6010 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-6011 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 0338-6011 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 23 sections
MILRINONE LACTATE HUMAN PRESCRIPTION DRUG LABEL 1 0409-0212 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 11 sections
Milrinone Lactate in Dextrose Human Prescription Drug Label 1 0409-1983 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate in Dextrose Human Prescription Drug Label 1 0409-1983 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate in Dextrose Human Prescription Drug Label 1 0409-2045 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate in Dextrose Human Prescription Drug Label 1 0409-2045 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 19 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0409-2776 INJECTION, SOLUTION 200 ug INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6065 INJECTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6067 INJECTION 1 mg INTRAVENOUS ANDA 25 sections
Milrinone Lactate in Dextrose HUMAN PRESCRIPTION DRUG LABEL 1 25021-313 INJECTION, SOLUTION 0.20 mg INTRAVENOUS ANDA 23 sections
Milrinone Lactate HUMAN PRESCRIPTION DRUG LABEL 1 42677-313 INJECTION, SOLUTION 1 mg INTRAVENOUS ANDA 12 sections