Amrinone

Structural formula
General
Non-proprietary name	Amrinone
other names	3-Amino-5- (4-pyridinyl) -2 (1 H ) -pyridinone Inamrinone (USAN)
Molecular formula	C 10 H 9 N 3 O
External identifiers / databases
CAS number 60719-84-8 EC number 262-390-0 ECHA InfoCard 100,056,700 PubChem 3698 DrugBank DB01427 Wikidata Q422724
Drug information
ATC code	C01 CE01
Drug class	PDE inhibitors
properties
Molar mass	187.2 g · mol -1
Physical state	firmly
Melting point	294-297 ° C
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances danger H and P phrases H: 301 P: 301 + 310
Toxicological data	102 mg kg −1 ( LD 50 ,  rat ,  oral )
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Amrinone is in the German language no longer available drug , which - as enoximon and milrinone - the phosphodiesterase - inhibitors (PDE) from Bipyridintyp belongs. It causes blood pressure to drop and increases the force of the heart to contract .

Mechanism of action

Amrinone inhibits the isoenzyme III of phosphodiesterase, which catalyzes the breakdown of cAMP . It does not work on membrane receptors .

At the heart of the accumulation of cAMP causes the activation of protein kinase A . This phosphorylates the calcium channels and opens them, so that more calcium ions (Ca ²⁺ ) flow into the heart muscle cells . This increases the contraction force of the heart muscle cells (positive inotropy ).

In the smooth muscle cells of the peripheral blood vessels, however, the Ca ²⁺ concentration decreases and the vessel wall slackens, so that the blood pressure decreases.

Amrinone thus belongs to the group of inodilators .

application

Studies hardly report long-term benefits, but they do report frequent side effects . Amrinone has only been used for the short-term treatment of heart failure ( NYHA IV ) patients who have not responded to digitalis , diuretics, or ACE inhibitors . Because it lowers pulmonary arterial blood pressure, it has also been used in primary or secondary pulmonary hypertension and after heart-lung transplants .

Unwanted side effects are:

• ventricular arrhythmias ,
• supra- and ventricular tachycardias up to ventricular fibrillation ,
• Drop in blood pressure,
• Nausea , vomiting , abdominal pain , fever , myalgias , taste disturbances, spleen swelling .

Contraindications are:

• Lack of volume ,
• Cardiac arrhythmias ,
• Renal failure ,
• Pregnancy and breastfeeding,
• Heart failure ,
• Severe obstructive aortic or pulmonary valve disease.

Dobutamine increases the effect of PDE inhibitors additively.

Commercial preparations

Amrinon, which was introduced in 1981, is no longer available as a commercial product in Germany, Austria, Belgium, Luxembourg and Switzerland. Until 2005 it was sold under the trademark Wincoram ^® . In the USA, Amrinone is sold under the trademark Inocor ^® .

literature

• Reinhard Larsen: Anesthesia and intensive medicine in cardiac, thoracic and vascular surgery. (1st edition 1986) 5th edition. Springer, Berlin / Heidelberg / New York et al. 1999, ISBN 3-540-65024-5 , pp. 50-52.

Individual evidence

1. ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, p. 95, ISBN 978-0-911910-00-1 .
2. ↑ ^{a b c} Amrinon data sheet from Sigma-Aldrich , accessed on March 9, 2011 ( PDF ).

Web links

• Amrinon at unizh.ch

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !