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 N
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)
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

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

References

1. ^ http://www.nejm.org/doi/full/10.1056/NEJM199111213252103

External links

• Mechanism of action

This drug article relating to the cardiovascular system is a stub. You can help Wikipedia by expanding it.v · Categories: Inotropic agents Vasodilators Nitriles Pyridines PDE3 inhibitors 2-Pyridones Cardiovascular system drug stubs Wikimedia Foundation. 2010. Игры ⚽ Нужна курсовая? Rodeo bareback rigging Anneloes Nieuwenhuizen Look at other dictionaries: Milrinone — МИЛРИНОН ( Milrinonе )*. 1,6 Дигидро 2 метил 6 оксо[3,4 бипиридин] 5 карбонитрил. Выпускается в виде лактата. Синоним: Рrimacor . По структуре и действию близок к амринону. Вместо аминогруппы содержит группу СN и имеет дополнительный метильный… …   Словарь медицинских препаратов milrinone — noun An inhibitor of phosphodiesterase III that potentiates the effect of cyclic adenosine monophosphate …   Wiktionary milrinone — A xanthine oxidase inhibitor which increases the force of contraction of the heart; used in congestive heart failure; resembles amrinone; cardiotonic. * * * mil·ri·none mil rə .nōn …   Medical dictionary PDE3 inhibitor — Milrinone, one of the first PDE3 inhibitors used clinically A PDE3 inhibitor is a drug which inhibits the action of the phosphodiesterase enzyme PDE3. They are used for the therapy of acute heart failure and cardiogenic shock. Approved PDE3… …   Wikipedia Amrinone — Systematic (IUPAC) name 5 amino 3,4 bipyridin 6(1H) one Clinical data AHFS/Drugs.com …   Wikipedia Management of heart failure — requires a muitimodal approach. It involves a combination of lifestyle modifications, medications, and possibly the use of devices or surgery. Contents 1 Diet and lifestyle measures 1.1 Fluid restriction 2 Pharmacological management …   Wikipedia Phosphodiesterase inhibitor — A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and… …   Wikipedia Heart failure — Classification and external resources The major signs and symptoms of heart failure. ICD 10 I5 …   Wikipedia Inotrope — An inotrope (pronEng|ˈaɪnətroʊp) is an agent that alters the force or energy of muscular contractions. Negatively inotropic agents weaken the force of muscular contractions. Positively inotropic agents increase the strength of muscular… …   Wikipedia Bipyridine — Bipyridines are a family of chemical compounds with the formula (C5H4N)2, which are formed by the coupling of two pyridine rings. Six isomers of bipyridine exist, but two isomers are prominent: 2,2 bipyridine is a popular ligand in coordination… …   Wikipedia 18+ © Academic, 2000-2024 Contact us: Technical Support, Advertising Dictionaries export, created on PHP, Joomla, Drupal, WordPress, MODx. Mark and share Search through all dictionaries Translate… Search Internet Share the article and excerpts Direct link … Do a right-click on the link above and select “Copy Link”