Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1994-06-17
1997-01-07
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514178, A61K 3156, A61K 3168
Patent
active
055917321
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT DE 93/00473, filed May 28, 1993.
The invention relates to a medicanent which, apart from its already known action in the metabolism, is able to positively influence the activation state of the central nervous system or physiologically optimize the same and/or is active in the prophylaxis and therapy of osteoporosis.
Apart from other factors, the psychophysiological and psychic capacity of the human being is significantly determined by the state of activation of the central nervous system. This activation can be evaluated by means of the shift of the average alpha-frequency in the electroencephalogram. Each physical or psychic stress to the human being leads to an increase of approximately 4 to 6 Hertz of the frequency as compared with the individual starting value. This increase is linked with an improvement to the psychophysiological capacity. If the stressing is excessive or cannot be adequately controlled, the alpha-frequency decreases after passing through an optimum. As a result the psychophysiological capacity drops and can sink below the starting value prior to the start of stressing.
Research carried out on top sportsmen proved that the increase of the alpha-frequency is triggered by mental concentration connected with completing the task. An appropriate physical activity before controlling the actual stress has the same effect. If the optimum of the activation is exceeded by false preparation, overstressing, fear situations or disturbing external influences, the capacity decreases, errors increase, corrections are associated with more psychic and physical effort. The degree of exhaustion on completing the task is higher.
In middle and old age a cause of the decreasing capacity is an inadequate stress activation of the central nervous system. In phases of longer-term and high psychophysiological stressing and particularly with restricted activation, the setting and maintaining of an optimum activation state of the central nervous system acquires particular significance at this age for maintaining and optimizing capacity.
Through changes in the hormonal balance as from an age of 45 to 50 years there can be a catabolic situation in the calcium metabolism of the bone, which leads to calcium depletion (osteoporosis). A substitution of this function without disturbing the endogenic control system is necessary. For woman in the menopause therapeutical schemes have been tested, but there is no satisfactory solution for men. All the steroid hormones and derivatives tested up to now have revealed clear negative influencing of the endogenic control system.
It has now surprisingly been found that both an optimum activation state of the central nervous system and also (simultaneously or separately therefrom) an activity during prophylaxis and therapy of osteoporosis can be obtained by the application of a medicament having a content of mestanolone and/or Oral-Turinabol.
The medicament can be used as a controlled-release dragee, depot form or buccal tablet, or in the form of a galenic formulation, which permits pernasal application by means of a nasal spray. Preference is given to a content of mestanolone and/or Oral-Turinabol of 5 to 20 mg per ingestion unit.
Mestanolone (STS 646, 17.beta.-hydroxy-17-methyl-5.alpha.androstan-3-one) is a testosterone derivative. As a result of the chemical modification the prevailing androgenic activity of the active ingredient is reduced and the anabolic activity increased. Mestanolone is authorized in Greece under the indication "anabolic/androgen".
It has surprisingly been found that, compared with other anabolically acting steroids (e.g. methandrostenolone), which can be therapeutically used, the anabolic activity of mestanolone is much lower. When administering the same dose (e.g. 10 to 20 mg daily) under mestanolone there is a reduction of the urea concentration in the blood and at 4% it is much lower than with the other steroids (up to 30%).
Research carried out on physically highly stressed test persons revealed that on supplying mestano
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Hacker Rudiger
Mattern Claudia
Cintins Marianne M.
MacMillan Keith
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