Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1997-04-15
1998-11-10
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514178, 514179, A61K 3156
Patent
active
058344519
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/01561 filed Aug. 7, 1995.
TECHNICAL FIELD
The present invention relates to a remedy efficacious for symptomatic improvement in myotonic dystrophy and various other diseases manifesting myotonia.
BACKGROUND ART
Myotonic dystrophy (hereinafter referred to sometimes as MyD) is an autosomal-dominant hereditary disease caused by abnormalities of the long arm of chromosome 19 and its morbidity is said to be 4 to 5 in 100,000. MyD is a degenerative disease, the cardinal symptoms of which are muscular atrophy and decreased muscle strength dominantly found in muscles of the face and neck and in distal muscles of the limbs, and appearance of repetitive muscle cell membrane action potentials in skeletal muscles on contraction and consequent delays in relaxation (myotonia), and which is complicated by multiple organ disorders.
There is no causal therapy available for MyD and in clinical practice today symptomatic therapies are being attempted for said myotonia and complicating organ disorders.
Thus, medicines such as procainamide, diphenylhydantoin, taurine are administered for the treatment of myotonia.
However, the above-mentioned medicines have the drawback that their administration results in adverse reactions such as induction and aggravation of the conduction disorders of the heart as complications of MyD, gastrointestinal disorders, central nervous system symptoms, etc. and that the therapeutic results are not necessarily reproducible.
In MyD, not only the above-mentioned myotonia but also decreased muscle strength and muscular atrophy, which can be the most serious detracting factor in the patient's activity of daily living, are encountered but no established therapy for such disorders is available as of the present time.
SUMMARY OF THE INVENTION
In view of the above state of the art, the present invention has for its object to provide a remedy which is very efficacious for said myotonia, decreased muscle strength, and muscular atrophy and highly safe to use.
The present invention resides essentially in utilizing dehydroepiandrosterone sulfate or a pharmacologically acceptable salt thereof in the treatment of myotonic dystrophy and myotonia.
DETAILED DISCLOSURE OF THE INVENTION
The present invention is now described in detail.
Dehydroepiandrosterone sulfate (hereinafter referred to briefly as DHEA-S) and dehydroepiandrosterone (briefly, DHEA) are adrenocortical androgens produced and released from the human adrenal cortex. They are C.sub.19 steroid hormones which are intrinsic to Primates. DHEA-S is readily converted to DHEA in vivo. In view of its metabolic pathways, it can be theoretically further transformed into testosterone and estrogen but the actual conversion rates are extremely low. The physiological activities of DHEA-S and DHEA have been little elucidated and although it has been found that DHEA has androgen-like activity, its activity as a male hormone is weak.
Research by the inventors of the present invention revealed that blood DHEA and DHEA-S levels are significantly lower in MyD patients than in healthy individuals in the same decade of life and that, therefore, DHEA and DHEA-S could be used as remedies for MyD.
DHEA-S in accordance with the present invention, has the structure (1) shown below, as is disclosed in Japanese Kokoku Publication Sho-55-27884. ##STR1##
In Japan, dehydroepiandrosterone sulfate sodium salt (hereinafter briefly referred to as DHEA-S.Na) according to the present invention, has been on the market since 1984 as a remedy for insufficient maturity of the cervical canal in the third pregnancy trimester, which is to be used as the main ingredient in the trademark Mylis Injection.
Therefore, the above-mentioned DHEA-S or a pharmacologically acceptable salt thereof is a per se known substance. However, the use thereof as a remedy for MyD has never been suggested.
DHEA-S is generally used in the form of sodium salt. It can also be used for parenteral administration in the form of solutions of other water-soluble salts, such as th
REFERENCES:
patent: 4005200 (1977-01-01), Utsumi et al.
Carter, J.N. and K.S. Steinbeck, "Reduced Adrenal Androgens in Patients with Myotonic Dystrophy", Journal of Clinical Endocrinology and Metabolism, vol. 60 No. 3, Mar. 1985, pp. 611-614.
Endo Tomio
Ohsawa Nakaaki
Sugino Masakazu
Goldberg Jerome D.
Kanebo Ltd.
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