Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-11-21
1998-09-22
MacMillan, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514823, 514816, A61K 31485
Patent
active
058114513
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to the combined use of opiate antagonists and of calcium salts for the preparation of medicaments for the treatment of endorphin-related pathologies.
The invention also relates to pharmaceutical compositions for human and veterinary use containing as active principle opiate antagonists in combination with calcium salts and optionally with proteases, prostaglandins and Vitamin C and K. The compositions of the invention may optionally be in form of kit-of-parts, consisting of separate dosage forms for the contemporaneous or sequential administration of the above mentioned active principles.
BACKGROUND OF THE PRIOR ART
The neurons of the nigro-striatal system, together with many other nervous structures, synthesize low nuclear weight compounds, endorphins, having actions practically identical with that of phenantrene alkaloids of morphine. These endogenous opioids (endorphins) play an essential biological role in the Central Nervous System of every animal, man included.
The endogenous opiate peptides, enkephalins and endorphins, consisting of aminoacid (from 5 to 31) sequences, are present at the hypothalamic, cerebral and spinal level as well as in the endocrine glands (adrenal glands, hypophysis, ovaries, testis), and gastrointestinal system, muscle-skeletal system and immunitary system. The functions of the up-to-new known endorphins are multiple; the most known are: morphine-like analgesic properties, behavioural effects, neuromodulator functions.
These peptides, play also a remarkable role in functions such as memory, response to stress, pain transmission, regulation of appetite, temperature, respiratory frequency, libido, immunity etc.
The endorphins, ubiquitary present in mammals, inside and outside the central nervous system, derive from at least three different precursors: pre-pro-opiomelanocortine (POMC), pre-pro-enkephaline A and pre-pro-enkephaline B, yielding three classes of peptides related thereto, having well defined biological activity.
In particular, pre-pro-opiomelanocortine produces, as a result of lytic processes, differentiated in the various tissues, alpha-, beta- and gamma-endorphins; pre-pro-enkephalin A yields met-enkephalin and leu-enkephalin whereas pre-pro-enkephalin B is the precursor of alpha-neo-endorphin, beta-neo-endorphin and dinorphine. The role and distribution of these peptides in the various tissues have been widely studied, with particular reference to their ability of interacting with the opiate receptors.
The endorphins have been in fact recognized as defense agents able to induce analysis and sedation in organisms subjected to stress of different kind and aetiology.
For instance, an increased production of endorphins was noticed after traumatic injuries, nervous, endocrine, metabolic or infectious diseases, physical fatigue, delivery, insomnia, surgical operations, alimentary or pharmacological intoxication, etc.
The endorphins are found in the organisms both in a form bound to the receptors present in the various tissues and organs and in free form, in the plasma and in the liquor. The ratio between free and bound endorphins may be increased in relation to the increased production, the reduced catabolism or the competitive removal from the receptors of the bound endorphins, for instance by the opiate antagonists such as naloxone, naltrexone and derivatives and analogs.
The free endorphins, if not rapidly removed by catabolic mechanisms, bind again to the respective receptors, inducing a series of biochemical effects impairing the cellular metabolism, interfere with the nervous function and induce a pathogenetic action of the affected organs.
SUMMARY OF THE INVENTION
It has now been surprisingly found that the administration of opiate antagonists in combination with calcium ions is able to effectively antagonize said pathogenetic actions, resulting to be useful, both in human and in veterinary clinical practice, in pathologies characterized by high free and bound endorphin levels, hereinafter defined endorp
REFERENCES:
patent: 4241066 (1980-12-01), Kobylecki et al.
J. of Biological Chemistry, vol. 264, No. 5, 1989, pp. 347-353, Attali et al.
Peptides, vol. 13, 1992, pp. 947-951, Wang et al.
Minoia Paolo
Sciorsci Raffaele Luigi
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