Use of prostacyclin derivatives to prevent or to treat disorders

Details Use of prostacyclin derivatives to prevent or to treat disorders Use of prostacyclin derivatives to prevent or to treat disorders

1995-06-23

1998-09-29

Gerstl, Robert

Drug, bio-affecting and body treating compositions

In vivo diagnosis or in vivo testing

Magnetic imaging agent

424 943, 424 95, 514530, 514169, A61K 31557

Patent

active

058143017

DESCRIPTION:

BRIEF SUMMARY
Contrast media are essential auxiliary agents in medical diagnosis. They make possible increasingly greater contrast in the pictures obtained as well as better detection of the various tissues and organs. Among other things, they are used in x-ray, ultrasonic and magnetic resonance processes. There are a multitude of undesirable side effects with respect to this very useful application, such as, for example, changes of endothelial cells, damage of the erythrocytes, influencing of the blood clotting system, disorder of the microcirculatory system up to complete hemostasis, increase of the already existing disorder of the microcirculatory system in the pathogenic tissue, changes of the blood-brain barrier or negative influencing of the blood pressure. The disorder of the microcirculatory system is especially important. The microcirculatory system is functionally the most important part of the circulatory system. The metabolism takes place in the area of the microcirculatory system. In the case of a disorder of the microcirculatory system, among others, reduction of the blood cell-perfused branch points, increase of adhesions of the blood cells on the inner wall of the venules and erythrocyte aggregation can be observed. The arteriolar vasomotion is also impaired. A number of diseases, not only of the cardiovascular system, are attributable to disorders of the microcirculatory system. Therefore, it is absolutely desirable to avoid or to treat immediately a disorder of the microcirculatory system as a consequence of administering a contrast medium.
A multitude of pharmacological effects are already known from chemically stable prostacyclin derivatives.
It has now been found, surprisingly, that the prostacyclin derivatives of this invention maintain or restore the microcirculatory system to a significant extent when administered shortly before or after administering x-ray, ultrasonic or NMR contrast media or when jointly administered with said contrast media.
The invention relates to the use of a prostacyclin derivative or of the corresponding .beta.-cyclodextrin clathrate or of the form encapsulated with liposomes for the production of a pharmaceutical agent to prevent or to treat disorders of the microcirculatory system when x-ray, NMR or ultrasonic contrast media are administered.
This invention preferably relates to the use of one or more prostacyclin derivatives of general formula I ##STR2## in which R.sup.1 means hydrogen or a C.sub.1 -C.sub.4 alkyl radical, atom, the hydroxy group, in which the hydroxy group can be in .alpha.- or .beta.-position, group, means hydrogen, its salts with physiologically compatible bases, as well as its .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates as well as its form encapsulated with liposomes or ataprost, beraprost, BW-15AU, ciprostene, CS 570, FCE 22509, naxaprostene, RS-93427, SC 39902 or taprostene for the production of a pharmaceutical agent to prevent or to treat disorders of the microcirculatory system when x-ray, ultrasonic or NMR contrast media are administered.
This invention especially preferably relates to the use of the prostacyclin derivatives iloprost, iloprost-clathrate, cicaprost, cicaprost-clathrate, eptaloprost or eptaloprost-clathrate.
As alkyl groups in R.sup.1, straight- or branched-chain alkyl groups with 1-4 C atoms are to be considered, such as, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl. Alkyl groups R.sup.1 can optionally be substituted by halogen atoms, methoxy, ethoxy, phenyl or (C.sub.1 -C.sub.2)-dialkylamines.
As substituents, there can be mentioned, for example, fluorine, chlorine or bromine atoms, phenyl, dimethylamine, diethylamine, methoxy or ethoxy. Preferred alkyl groups R.sup.1 are methyl, ethyl, dimethylaminopropyl.
As alkyl group R.sup.2, methyl and ethyl can be mentioned.
The hydroxy groups in R.sup.3 and W can be present as free hydroxy groups, in which the hydroxy group in W is preferably in .alpha.-position or can be functionally modified, for example, by etherification or esterification. Fre

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