JP2731063B2 - Hot flashes due to ovarian loss - Google Patents
Hot flashes due to ovarian lossInfo
- Publication number
- JP2731063B2 JP2731063B2 JP926692A JP926692A JP2731063B2 JP 2731063 B2 JP2731063 B2 JP 2731063B2 JP 926692 A JP926692 A JP 926692A JP 926692 A JP926692 A JP 926692A JP 2731063 B2 JP2731063 B2 JP 2731063B2
- Authority
- JP
- Japan
- Prior art keywords
- hot flashes
- dihydroxyvitamin
- hydroxyvitamin
- ovarian
- active
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】DETAILED DESCRIPTION OF THE INVENTION
【０００１】[0001]
【産業上の利用分野】本発明は、卵巣欠落によるのぼせ
治療剤に関するものである。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a remedy for hot flashes caused by lack of ovaries.
【０００２】[0002]
【従来の技術及び発明が解決しようとする課題】卵巣欠
落によるのぼせは女性ホルモンの低下が発症の原因と考
えられており、卵巣切除、あるいは卵巣機能を低下させ
る治療後に発生することが知られている。2. Description of the Related Art Hot flashes due to ovarian loss are considered to be caused by a decrease in female hormones, and are known to occur after ovariectomy or treatment to reduce ovarian function. I have.
【０００３】症状の程度には個人差があるが、卵巣切除
や卵巣機能を低下させた治療後の女性のほぼ１００％が
罹患すると言われている。[0003] Although the degree of symptoms varies from individual to individual, it is said that almost 100% of women who have undergone ovariectomy or treatment with reduced ovarian function are affected.
【０００４】症状の発生時期は突発的で予想できない。
このため、発症による苦痛は症状の程度以上である。通
常、情動や労作の変化を契機に発症しやすく、神経質な
婦人ほど重症になる傾向があると言われている。[0004] The onset of symptoms is sudden and unpredictable.
Therefore, the pain caused by the onset is more than the degree of symptoms. Usually, it is said that it is easy to develop on changes in emotions and exertion, and nervous women tend to be more severe.
【０００５】また、卵巣欠落によるのぼせは約２年間も
の罹患期間があるため、婦人にとっては計り知れない程
の精神的なストレスになる。特に現代社会では、社会的
なニーズから女性といえども機に応じた判断力、実行力
が男性と同様に要求されるようになっている。このよう
な立場にある婦人にとって、卵巣欠落によるのぼせとい
った肉体的なハンディキャップは可能な限り最小限にと
どめたいところであり、このような社会的ニーズには、
単に医学上の臨床課題を越えた重要性があると言えよ
う。[0005] In addition, hot flashes due to ovarian deficiency have an illness period of about two years, and thus cause incalculable mental stress for women. Especially in modern society, social needs require that women, as well as men, have the ability to make judgments and execute according to their opportunities. For women in such a position, physical handicaps such as hot flashes due to lack of ovaries are to be minimized as much as possible.
It can simply be said that it is more important than medical clinical issues.
【０００６】さて、従来の薬物療法には、女性ホルモン
剤の投与や精神安定剤の投与が挙げられるが、それぞれ
の治療法には下記の問題がある。効果が最も確実とされ
る女性ホルモン剤は子宮体部腺癌の発症リスクを高める
だけでなく、乳癌などホルモン依存性の腫瘍の既往例で
はこの薬剤の使用は禁忌である。また、不整性器出血、
下腹部痛や頭痛といった一般的な副作用もあるため、長
期的な治療には必ずしも適していない。精神安定剤も眠
気などの副作用がある他、必ずしも安定した効果が得ら
れない。以上のことから、経口剤で副作用が少なく、し
かも有効性の高い治療法の開発が望まれている。[0006] Conventional pharmacotherapy includes administration of female hormones and administration of tranquilizers, but each treatment has the following problems. The most reliable female hormones not only increase the risk of developing adenocarcinoma of the uterine corpus, but are contraindicated in patients with a history of hormone-dependent tumors such as breast cancer. Also irregular genital bleeding,
Common side effects, such as lower abdominal pain and headache, are not always suitable for long-term treatment. Mental stabilizers also have side effects such as drowsiness and do not always provide stable effects. In view of the above, there is a demand for the development of a highly effective treatment method that has few side effects with oral preparations.
【０００７】ところで、卵巣欠落によるのぼせが発症し
た婦人には、カルシウム代謝異常、ビタミン代謝異常が
見られる。従って、この症状の発現にはカルシウム代謝
異常ひいてはそれと関連深いビタミンＤの存在が何らか
の影響を有するのではないかと推察される。[0007] Women suffering from hot flashes due to lack of ovaries have abnormal calcium metabolism and vitamin metabolism. Therefore, it is speculated that abnormalities in calcium metabolism and the presence of vitamin D, which is closely related to calcium metabolism, may have some influence on the onset of this symptom.
【０００８】一方、１α―ヒドロキシビタミンＤ、１
α，２４―（Ｒ）―ジヒドロキシビタミンＤ、１α，２
５―ジヒドロキシビタミンＤ等の活性型ビタミンＤ類
は、小腸でのカルシウム吸収促進作用、骨での骨吸収・
骨形成調節作用等を有しており、種々のカルシウム代謝
異常に基づく疾患に対する確立した治療薬である。On the other hand, 1α-hydroxyvitamin D,
α, 24- (R) -Dihydroxyvitamin D, 1α, 2
Activated vitamin D such as 5-dihydroxyvitamin D promotes calcium absorption in the small intestine, bone resorption in bone,
It has a bone formation regulating action and the like, and is an established therapeutic agent for various diseases based on abnormalities in calcium metabolism.
【０００９】[0009]
【課題を解決するための手段】そこで本発明者等は、こ
の活性型ビタミンＤが卵巣欠落によるのぼせにどのよう
な影響を与えるかを鋭意検討した結果、驚くべきこと
に、活性型ビタミンＤは非常に少ない量でしかも副作用
もなく、卵巣欠落によるのぼせを改善する作用があるこ
とを知見し、本発明に到達したものである。即ち、本発
明は活性型ビタミンＤを有効成分とする卵巣欠落による
のぼせ治療剤である。The inventors of the present invention have conducted intensive studies on the effects of this active vitamin D on hot flashes caused by ovarian loss. As a result, surprisingly, the active vitamin D The present inventors have found that the present invention has an effect of improving hot flashes due to ovarian deficiency in a very small amount and without side effects, and has reached the present invention. That is, the present invention is a therapeutic agent for hot flashes due to lack of ovaries containing active vitamin D as an active ingredient.
【００１０】本発明における活性型ビタミンＤとは活性
型ＶＤ2 、活性型ＶＤ3 およびそれらの誘導体を含むも
のであり、その具体例としては、例えば１α―ヒドロキ
シビタミンＤ、１α，２４―（Ｒ）―ジヒドロキシビタ
ミンＤ、１α，２５―ジヒドロキシビタミンＤ、１α，
２４，２５―トリヒドロキシビタミンＤ、２４，２４―
ジフルオロ―１α，２５―ジヒドロキシビタミンＤ、２
６，２６，２６，２７，２７，２７―ヘキサフルオロ―
１α，２５―ジヒドロキシビタミンＤ、２５―ヒドロキ
シビタミンＤ3 ―２６，２３―ラクトン、１α，２５―
ジヒドロキシビタミンＤ3 ―２６，２３―ラクトン等が
挙げられる。なかでも、１α―ヒドロキシビタミン
Ｄ3 、１α，２４―（Ｒ）―ジヒドロキシビタミン
Ｄ3 、１α，２５―ジヒドロキシビタミンＤ3 が好まし
く、特にこれらのなかでも１α―ヒドロキシビタミンＤ
3 が好ましい。The active vitamin D in the present invention includes active VD 2 , active VD 3 and derivatives thereof, and specific examples thereof include, for example, 1α-hydroxyvitamin D, 1α, 24- (R ) -Dihydroxyvitamin D, 1α, 25-dihydroxyvitamin D, 1α,
24,25-trihydroxyvitamin D, 24,24-
Difluoro-1α, 25-dihydroxyvitamin D, 2
6,26,26,27,27,27-hexafluoro-
1α, 25-dihydroxyvitamin D, 25-hydroxyvitamin D 3 -26,23-lactone, 1α, 25-
And dihydroxyvitamin D 3 -26,23-lactone. Among them, 1α-hydroxyvitamin D 3 , 1α, 24- (R) -dihydroxyvitamin D 3 , and 1α, 25-dihydroxyvitamin D 3 are preferred, and 1α-hydroxyvitamin D 3 is particularly preferred.
3 is preferred.
【００１１】これらの有効成分は公知の方法で適当な賦
形剤等を用いて、軟カプセル剤、硬カプセル剤、錠剤、
シロップ剤等の経口剤、注射剤、または外用剤として使
用できる。[0011] These active ingredients can be prepared in a known manner using appropriate excipients and the like to prepare soft capsules, hard capsules, tablets,
It can be used as an oral preparation such as a syrup, an injection, or an external preparation.
【００１２】有効成分の投与量は、通常０．０１〜４．
０μｇ／日／人程度で、好ましくは０．２５〜２．０μ
ｇ／日／人である。このような条件を満足するような製
剤を調整するのが好ましい。The dose of the active ingredient is usually 0.01-4.
0 μg / day / person, preferably 0.25 to 2.0 μm
g / day / person. It is preferable to prepare a preparation that satisfies such conditions.
【００１３】本発明の方法は既存の薬物療法治療剤と併
用することも可能である。[0013] The method of the present invention can be used in combination with an existing drug therapeutic agent.
【００１４】以下実施例を用いて本発明を詳述する。Hereinafter, the present invention will be described in detail with reference to examples.
【００１５】[0015]
【実施例】卵巣欠落によりのぼせの症状が出現した２２
例を対象として、活性型ビタミンＤ3 である１α―ヒド
ロキシビタミンＤ3 を０．５μｇ／日経口投与した。EXAMPLE: Hot flashes appeared due to lack of ovaries22
In the examples, 1α-hydroxyvitamin D 3 , which is active vitamin D 3 , was orally administered at 0.5 μg / day.
【００１６】１ケ月の投与により、２２例中２０例で症
状が消失あるいは軽快し、有効率は９０．９％に達し
た。After one month of administration, the symptoms disappeared or relieved in 20 of 22 cases, and the efficacy rate reached 90.9%.
【００１７】なお、これらの症状において１α―ヒドロ
キシビタミンＤ3 経口投与前後におけるカルシウム代謝
の変化を検討した。In these conditions, changes in calcium metabolism before and after oral administration of 1α-hydroxyvitamin D 3 were examined.
【００１８】血清中のイオン化カルシウム濃度はのぼせ
のないものでは１．２３±０．０５μmol ／ｌ、のぼせ
の高度なもの１．２８μmol ／ｌと、症状が高度になる
に従い上昇する傾向があり、これが本剤の投与により、
１．２６±０．０４μmol ／ｌに低下した。The concentration of ionized calcium in serum is 1.23 ± 0.05 μmol / l for those without hot flashes, and 1.28 μmol / l for those with high hot flashes, and tends to increase as the symptoms become more severe. With the administration of this drug,
It decreased to 1.26 ± 0.04 μmol / l.
【００１９】血清カルシウム濃度も同様に、のぼせのな
いものでは９．５８±０．４６mg／dl、のぼせの高度な
もの９．９８mg／dlと、症状が高度になるに従い上昇す
る傾向があり、これが本剤の投与により、９．８９mg／
dlに低下した。Similarly, the serum calcium concentration is 9.58 ± 0.46 mg / dl for those without hot flashes and 9.98 mg / dl for those with high hot flashes, and tends to increase with increasing symptoms. By administration of this drug, 9.89 mg /
dl dropped.
【００２０】尿中カルシウム排泄量（クレアチニン補
正）ものぼせのないものでは０．２５、のぼせの高度な
もの０．２０と、症状が高度になるに従い下降する傾向
があり、これが本剤の投与により、０．２２±０．１３
と上昇した。Urinary calcium excretion (creatinine correction) 0.25 for those without hot flashes and 0.20 for those with high hot flashes, and tend to decrease as the symptoms become more severe. , 0.22 ± 0.13
And rose.
【００２１】以上より、活性型ビタミンＤ3 である１α
―ヒドロキシビタミンＤ3 の経口投与により、のぼせ症
状発生に関連すると考えられるカルシウム代謝の異常が
正常化され、９０．９％もののぼせ発現例に有効である
ことが明らかになった。As described above, 1α which is an active vitamin D 3
- Oral administration of hydroxyvitamin D 3, the abnormality normalization of possible calcium metabolism and associated symptoms occurred hot flashes, was found to be effective in expressors hot flashes as 90.9%.
【００２２】従って、活性型ビタミンＤは非常に少量で
しかも副作用もなく、卵巣欠落によるのぼせの有力な治
療剤であると言える。Therefore, it can be said that active vitamin D is a very small amount and has no side effects, and is a potent therapeutic agent for hot flashes due to lack of ovaries.
───────────────────────────────────────────────────── フロントページの続き (72)発明者 青木 長寿 東京都千代田区内幸町２丁目１番１号 （飯野ビル） 帝人株式会社内 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Choju Aoki 2-1-1, Uchisaiwaicho, Chiyoda-ku, Tokyo (Iino Building) Teijin Limited
Claims (2)
欠落によるのぼせ治療剤。1. A therapeutic agent for hot flashes caused by ovarian loss, comprising active vitamin D as an active ingredient.
タミンＤ、１α，２４―（Ｒ）―ジヒドロキシビタミン
Ｄ、１α，２５―ジヒドロキシビタミンＤ、１α，２
４，２５―トリヒドロキシビタミンＤ、２４，２４―ジ
フルオロ―１α，２５―ジヒドロキシビタミンＤ、２
６，２６，２６，２７，２７，２７―ヘキサフルオロ―
１α，２５―ジヒドロキシビタミンＤ、２５―ヒドロキ
シビタミンＤ3 ―２６，２３―ラクトン、１α，２５―
ジヒドロキシビタミンＤ3 ―２６，２３―ラクトンから
なる群から選ばれたものである請求項１記載の卵巣欠落
によるのぼせ治療剤。2. The active vitamin D is 1α-hydroxyvitamin D, 1α, 24- (R) -dihydroxyvitamin D, 1α, 25-dihydroxyvitamin D, 1α, 2.
4,25-trihydroxyvitamin D, 24,24-difluoro-1α, 25-dihydroxyvitamin D, 2
6,26,26,27,27,27-hexafluoro-
1α, 25-dihydroxyvitamin D, 25-hydroxyvitamin D 3 -26,23-lactone, 1α, 25-
Dihydroxyvitamin D 3 -26,23- therapeutic hot flashes by the ovaries missing according to claim 1, wherein a member selected from the group consisting of a lactone.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP926692A JP2731063B2 (en) | 1992-01-22 | 1992-01-22 | Hot flashes due to ovarian loss |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP926692A JP2731063B2 (en) | 1992-01-22 | 1992-01-22 | Hot flashes due to ovarian loss |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH05194239A JPH05194239A (en) | 1993-08-03 |
| JP2731063B2 true JP2731063B2 (en) | 1998-03-25 |
Family
ID=11715643
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP926692A Expired - Fee Related JP2731063B2 (en) | 1992-01-22 | 1992-01-22 | Hot flashes due to ovarian loss |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2731063B2 (en) |
-
1992
- 1992-01-22 JP JP926692A patent/JP2731063B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH05194239A (en) | 1993-08-03 |
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