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
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.
2000 Feb 15
Vasopressin as an alternative to norepinephrine in the treatment of milrinone-induced hypotension.
2000 Jan
Vascular relaxant effects of toborinone on the isolated canine internal mammary artery.
2001
High calcium and dobutamine positive inotropy in the perfused mouse heart: myofilament calcium responsiveness, energetic economy, and effects of protein kinase C inhibition.
2001
Comparison of dobutamine-based and milrinone-based therapy for advanced decompensated congestive heart failure: Hemodynamic efficacy, clinical outcome, and economic impact.
2001 Dec
Slow induction of milrinone after coronary artery bypass grafting.
2001 Feb
Comparison of systemic vasodilators: effects on flow in internal mammary and radial arteries.
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
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
A randomized multicenter study comparing the efficacy and safety of intravenous milrinone and intravenous nitroglycerin in patients with advanced heart failure.
2001 Jun
Sildenafil (viagra) facilitates weaning of inhaled nitric oxide following placement of a biventricular-assist device.
2001 May
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
Cell-based assay for high-throughput quantitative screening of CFTR chloride transport agonists.
2001 Nov
Effects of milrinone on left ventricular end-systolic pressure-volume relationship of rat hearts in situ.
2001 Sep
Nitric oxide-cGMP pathway facilitates acetylcholine release and bradycardia during vagal nerve stimulation in the guinea-pig in vitro.
2001 Sep 1
Cilostazol (pletal): a dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptake.
2001 Winter
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
The effectiveness and relative effectiveness of intravenous inotropic drugs acting through the adrenergic pathway in patients with heart failure-a meta-regression analysis.
2002 Aug
Phosphodiesterase 3 inhibitors selectively block the spontaneous resumption of meiosis by macaque oocytes in vitro.
2002 Aug
Acute renal failure secondary to milrinone in a patient with cardiac amyloidosis.
2002 Aug
Nitric oxide signalling by selective beta(2)-adrenoceptor stimulation prevents ACh-induced inhibition of beta(2)-stimulated Ca(2+) current in cat atrial myocytes.
2002 Aug 1
[Reversible cardiomyopathy secondary to interferon-alpha in chronic myelogenous leukemia].
2002 Feb
Milrinone increases middle cerebral artery blood flow velocity after cardiopulmonary bypass.
2002 Feb
Effects of milrinone for right ventricular failure after left ventricular assist device implantation.
2002 Jan
Assessing the emetic potential of PDE4 inhibitors in rats.
2002 Jan
Prophylactic intravenous use of milrinone after cardiac operation in pediatrics (PRIMACORP) study. Prophylactic Intravenous Use of Milrinone After Cardiac Operation in Pediatrics.
2002 Jan
The efficacy of preemptive Milrinone or Amrinone therapy in patients undergoing coronary artery bypass grafting.
2002 Jan
Effect of type 3 and type 4 phosphodiesterase inhibitors on the maintenance of bovine oocytes in meiotic arrest.
2002 Jan
Effects of phosphodiesterase III inhibition on length-dependent regulation of myocardial function in coronary surgery patients.
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
Treatment of acute heart failure: out with the old, in with the new.
2002 Mar 27
New mechanism of action for cilostazol: interplay between adenosine and cilostazol in inhibiting platelet activation.
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
Identification of interaction sites of cyclic nucleotide phosphodiesterase type 3A with milrinone and cilostazol using molecular modeling and site-directed mutagenesis.
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