U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry UNKNOWN
Molecular Formula C12H9N3O.C3H6O3
Molecular Weight 301.2973
Optical Activity UNSPECIFIED
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MILRINONE LACTATE

SMILES

CC(O)C(O)=O.CC1=C(C=C(C#N)C(=O)N1)C2=CC=NC=C2

InChI

InChIKey=VWUPWEAFIOQCGF-UHFFFAOYSA-N
InChI=1S/C12H9N3O.C3H6O3/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8;1-2(4)3(5)6/h2-6H,1H3,(H,15,16);2,4H,1H3,(H,5,6)

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/cdi/milrinone.html

Milrinone, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Milrinone inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, Milrinone also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. Milrinone is indicated for the treatment of congestive heart failure. Milrinone was marketed under the brand name Primacor.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.45 µM [IC50]
1.0 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Milrinone Lactate

Approved Use

Milrinone lactate injection is indicated for the short-term intravenous treatment of patients with acute decompensated heart failure.

Launch Date

2002
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
162 μg/L
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
454 μg/L
75 μg/kg bw single, intravenous
dose: 75 μg/kg bw
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1.749 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
439 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.92 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
0.758 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
0.94 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: HEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
1.7 h
75 μg/kg bw single, intravenous
dose: 75 μg/kg bw
route of administration: Intravenous
experiment type: SINGLE
co-administered:
MILRINONE plasma
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
The use of milrinone in pre-transplant assessment of patients with congestive heart failure and pulmonary hypertension.
1999 Apr
[The effects of intravenous milrinone for the patient undergoing CABG].
2000 Feb
Vasopressin in the treatment of milrinone-induced hypotension in severe heart failure.
2000 Feb 15
Vasopressin as an alternative to norepinephrine in the treatment of milrinone-induced hypotension.
2000 Jan
[The effects of milrinone on hemodynamics in patients undergoing cardiac surgery].
2001 Apr
Milrinone for the treatment of cerebral vasospasm after subarachnoid hemorrhage: report of seven cases.
2001 Apr
Comparison of milrinone versus nitroglycerin, alone and in combination, on grafted internal mammary artery flow after cardiopulmonary bypass: effects of alpha-adrenergic stimulation.
2001 Dec
Milrinone versus dobutamine in heart failure subjects treated chronically with carvedilol.
2001 Dec
Inhibition of cyclic-3',5'-nucleotide phosphodiesterase abrogates the synergism of hypoxia with lipopolysaccharide in the induction of macrophage TNF-alpha production.
2001 Dec
The additive pulmonary vasodilatory effects of inhaled prostacyclin and inhaled milrinone in postcardiac surgical patients with pulmonary hypertension.
2001 Dec
Comparison of dobutamine-based and milrinone-based therapy for advanced decompensated congestive heart failure: Hemodynamic efficacy, clinical outcome, and economic impact.
2001 Dec
Natriuretic peptides like NO facilitate cardiac vagal neurotransmission and bradycardia via a cGMP pathway.
2001 Dec
Mouse oocyte mitogenic activity is developmentally coordinated throughout folliculogenesis and meiotic maturation.
2001 Dec 1
Slow induction of milrinone after coronary artery bypass grafting.
2001 Feb
Pharmacodynamic effects of milrinone with and without a bolus loading infusion.
2001 Feb
[Effect of colforsin daropate hydrochloride after cardiopulmonary bypass].
2001 Jan
Milrinone echocardiographic viability test: a pilot study.
2001 Jul
The effects of alpha-human atrial natriuretic peptide and milrinone on pial vessels during blood-brain barrier disruption in rabbits.
2001 Jul
Surgical issues in heart failure: what's new?
2001 Jun
Dose response to nitric oxide in adult cardiac surgery patients.
2001 Jun
Comparison of the hemodynamic effects of milrinone with dobutamine in patients after cardiac surgery.
2001 Jun
Inhibition of phosphodiesterase type III before aortic cross-clamping preserves intramyocardial cyclic adenosine monophosphate during cardiopulmonary bypass.
2001 Jun
Diazepam and rolipram differentially inhibit cyclic AMP-specific phosphodiesterases PDE4A1 and PDE4B3 in the mouse.
2001 Mar 19
Improved survival with simendan after experimental myocardial infarction in rats.
2001 May 11
The role of cGMP hydrolysing phosphodiesterases 1 and 5 in cerebral artery dilatation.
2001 May 18
Synergistic interaction of diazepam with 3',5'-cyclic adenosine monophosphate-elevating agents on rat aortic rings.
2001 Oct 5
Modulation of TNF and GM-CSF release from dispersed human nasal polyp cells and human whole blood by inhibitors of different PDE isoenzymes and glucocorticoids.
2002
[Reversible cardiomyopathy secondary to interferon-alpha in chronic myelogenous leukemia].
2002 Feb
Effect of type 3 and type 4 phosphodiesterase inhibitors on the maintenance of bovine oocytes in meiotic arrest.
2002 Jan
Mechanisms of leptin secretion from white adipocytes.
2002 Jul
Effects of milrinone on hemodynamics and regional blood flow in the hypoxic dog.
2002 Jun
Cardiac performance during vasopressin infusion in postcardiotomy shock.
2002 Jun
Physical compatibility of milrinone lactate injection with intravenous drugs commonly used in the pediatric intensive care unit.
2002 Mar 1
Novel use of a short-acting intravenous beta blocker in combination with inotropic therapy as a bridge to chronic oral beta blockade in patients with advanced heart failure.
2002 May
A potential role for AMP-activated protein kinase in meiotic induction in mouse oocytes.
2002 May 1
New mechanism of action for cilostazol: interplay between adenosine and cilostazol in inhibiting platelet activation.
2002 Oct
Lipopolysaccharide-induced acute renal failure in conscious rats: effects of specific phosphodiesterase type 3 and 4 inhibition.
2002 Oct
Potentiation of slow component of delayed rectifier K(+) current by cGMP via two distinct mechanisms: inhibition of phosphodiesterase 3 and activation of protein kinase G.
2002 Sep
Exhaled nitric oxide: a marker of pulmonary hemodynamics in heart failure.
2002 Sep 18
Subtype-specific roles of cAMP phosphodiesterases in regulation of atrial natriuretic peptide release.
2002 Sep 20
Patents

Patents

Sample Use Guides

Usual Adult Dose for Congestive Heart Failure Loading dose: 50 mcg/kg IV over 10 minutes. Maintenance infusion: 0.375 to 0.75 mcg/kg/min.
Route of Administration: Intravenous
Milrinone caused the human thoracic artery samples to relax at 10⁻⁴ M concentrations by 44%, when the external Ca²⁺ corresponded to the physiological standard.
Name Type Language
MILRINONE LACTATE
MART.   MI   ORANGE BOOK   VANDF   WHO-DD  
Common Name English
MILRINONE LACTATE [VANDF]
Common Name English
MILRINONE LACTATE [ORANGE BOOK]
Common Name English
MILRINONE LACTATE [MART.]
Common Name English
MILRINONE LACTATE [MI]
Common Name English
PRIMACOR
Brand Name English
Milrinone lactate [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C744
Created by admin on Fri Dec 15 16:24:31 GMT 2023 , Edited by admin on Fri Dec 15 16:24:31 GMT 2023
Code System Code Type Description
MERCK INDEX
m7548
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PRIMARY Merck Index
RXCUI
155120
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PRIMARY RxNorm
EVMPD
SUB14579MIG
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PRIMARY
ChEMBL
CHEMBL189
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PRIMARY
EPA CompTox
DTXSID40881375
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PRIMARY
NCI_THESAURUS
C29263
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PRIMARY
FDA UNII
9K8XR81MO8
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PRIMARY
DRUG BANK
DBSALT000891
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PRIMARY
WIKIPEDIA
Milrinone lactate
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PRIMARY
DAILYMED
9K8XR81MO8
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PRIMARY
CAS
100286-97-3
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PRIMARY
PUBCHEM
172293
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PRIMARY
SMS_ID
100000076228
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PRIMARY
CHEBI
34850
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PRIMARY