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 |
|
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 |
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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
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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Milrinone lactate
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ACTIVE MOIETY
SUBSTANCE RECORD