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
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)
DescriptionSources: http://www.drugbank.ca/drugs/DB00235Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/cdi/milrinone.html
Sources: http://www.drugbank.ca/drugs/DB00235
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL241 Sources: http://www.drugbank.ca/drugs/DB00235 |
0.45 µM [IC50] | ||
Target ID: CHEMBL290 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10644042 |
1.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Milrinone Lactate Approved UseMilrinone lactate injection is indicated for the short-term intravenous treatment of patients with acute decompensated heart failure. Launch Date2002 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
162 μg/L EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3053125 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3053125 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.749 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7728786 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7728786 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.92 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7728786 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/7728786 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3053125 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3053125 |
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 |
PubMed
Title | Date | PubMed |
---|---|---|
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 |
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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
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/milrinone.html
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24622828
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.
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C744
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m7548
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155120
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Milrinone lactate
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ACTIVE MOIETY
SUBSTANCE RECORD