Milrinone

Milrinone

File:Milrinone.svg
Systematic (IUPAC) name
2-methyl-6-oxo-1,6-dihydro-3,4'-bipyridine-5-carbonitrile
Clinical data
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	IV only
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	100% (as IV bolus, infusion)
Protein binding	70 to 80%
Metabolism	Hepatic (12%)
Biological half-life	2.3 hours (mean, in CHF)
Excretion	Urine (85% as unchanged drug) within 24 hours
Identifiers
CAS Number	78415-72-2
ATC code	C01CE02 (WHO)
PubChem	CID 4197
DrugBank	APRD00010
Chemical data
Formula	C12H9N3O
Molar mass	211.219 g/mol[[]]
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Milrinone (Primacor) is a phosphodiesterase 3 inhibitor. It potentiates the effect of cyclic adenosine monophosphate (cAMP).

Milrinone also enhances relaxation 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 short half-life (1 to 2 hours). This can result in a prolonged weaning and possible adverse outcomes from stopping this medication rapidly.

Synthesis

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

External links

• Mechanism of action

es:Milrinona