Bis(trimethaphan)-nitroprusside salts and use thereof for blood

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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548107, A61K 3138, C07D49516

Patent

active

047405066

ABSTRACT:
There are described the novel compound bis-(trimethaphan)-nitroprusside of formula ##STR1## and solvates, especially hydrates or alcoholates thereof, as well as a process for the manufacture thereof from an alkali nitroprusside and a soluble trimethaphan salt, especially sodium nitroprusside and trimethaphan camsylate, in solution, especially in water.
Furthermore, there are described pharmaceutical compositions which contain the novel active substance (I) in solid form, in form of concentrated solutions or in form of diluted solutions suitable for infusion purposes.
In particular there are described compositions which contain (I) in concentrated solution in at least 40% ethanol or in solid form as well as compositions which contain, in addition to (I), a soluble, physiologically acceptable thiosulphate, in particular sodium thiosulphate.
The preparation of infusion solutions from the concentrated solutions or mixtures, the preparation of an especially well soluble micronized mixture of (I) and thiosulphate and the use of the concentrate for the preparation of infusion solutions are also described.
The compound (I) and its solvates and the pharmaceutical compositions containing (I) are suitable for therapeutic use, particularly in the lowering of blood pressure, in the achievement of peripheral vasodilation, in the elimination of arterial spasms and/or in the reduction of myocardial oxygen consumption and of the work load of the heart after heart attack.

REFERENCES:
MacRae et al., "Anaestheria", 36, pp. 312-315, (1981).

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