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 Y
ATC code	C01CE02
PubChem	CID 4197
DrugBank	APRD00010
ChemSpider	4052 Y
UNII	JU9YAX04C7 Y
KEGG	D00417 Y
ChEBI	CHEBI:50693 Y
ChEMBL	CHEMBL189 Y
Chemical data
Formula	C12H9N3O
Mol. mass	211.219 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16) Y Key:PZRHRDRVRGEVNW-UHFFFAOYSA-N Y
Physical data
Density	1.344 g/cm³
Melt. point	315 °C (599 °F)
Boiling point	449 °C (840 °F)
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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.

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

Synthesis

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

External links

• Mechanism of action