Milrinone


Milrinone
Milrinone
Systematic (IUPAC) name
2-methyl-6-oxo-1,6-dihydro-3,4'-bipyridine-5-carbonitrile
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a601020
Pregnancy cat. C(US)
Legal status Prescription only
Routes IV only
Pharmacokinetic data
Bioavailability 100% (as IV bolus, infusion)
Protein binding 70 to 80%
Metabolism Hepatic (12%)
Half-life 2.3 hours (mean, in CHF)
Excretion Urine (85% as unchanged drug) within 24 hours
Identifiers
CAS number 78415-72-2 YesY
ATC code C01CE02
PubChem CID 4197
DrugBank APRD00010
ChemSpider 4052 YesY
UNII JU9YAX04C7 YesY
KEGG D00417 YesY
ChEBI CHEBI:50693 N
ChEMBL CHEMBL189 YesY
Chemical data
Formula C12H9N3O 
Mol. mass 211.219 g/mol
SMILES eMolecules & PubChem
Physical data
Density 1.344 g/cm³
Melt. point 315 °C (599 °F)
Boiling point 449 °C (840 °F)
 N(what is this?)  (verify)

Milrinone (Primacor) is a phosphodiesterase 3 inhibitor. It potentiates the effect of cyclic adenosine monophosphate (cAMP).

Milrinone also enhances contraction of the left ventricle by increasing Ca2+-ATPase activity on the cardiac sarcoplasmic reticulum. This increases calcium ion uptake.

It has positive inotropic, vasodilating and minimal chronotropic effects. It is used in the management of heart failure only when conventional treatment with vasodilators and diuretics has proven insufficient. This is due to the potentially fatal adverse effects of milrinone, including ventricular arrhythmias.

Whereas beneficial hemodynamic effects are shown (at least short-term), several studies have shown no or a negative effect on mortality rates of hospitalized patients receiving milrinone.[1]

One negative side to the use of milrinone is the short half-life (1 to 2 hours). This can result in a prolonged weaning and possible adverse outcomes from stopping this medication rapidly.

Synthesis

Milrinone Synthesis.png

Singh, B.; 1983, U.S. Patent 4,413,127.

References

External links