WordNet
- of or related to the synthetic phase of metabolism
- characterized by or promoting constructive metabolism; "some athletes take anabolic steroids to increase muscle size temporarily"
- any of several fat-soluble organic compounds having as a basis 17 carbon atoms in four rings; many have important physiological effects
PrepTutorEJDIC
- ステロイド(脂肪溶解性の有機化合物の総称)
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/08/28 13:53:53」(JST)
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この項目では、筋肉増強剤としてのステロイドについて説明しています。
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アナボリック・ステロイド(anabolic steroid)は、生体の化学反応によって外界より摂取した物質から蛋白質を作り出す作用―すなわち蛋白同化作用を有するステロイドホルモンの総称。多くは男性ホルモン作用も持っている。
『アナボリック』の語源は『構築する』を意味するギリシャ語の『anabolein』で、一般的には単に『ステロイド』と呼ばれるが[1]、糖質コルチコイド成分の『ステロイド』（副腎皮質ホルモンなど）とは異なる。
アナボリックステロイドは筋肉増強剤として使用されることが主で、ドーピング薬物として知られる[2]。短期間での劇的な筋肉増強を実現するとともに、常態で得ることのできる水準を遥かに超えた筋肉成長を促す作用[3]から、運動選手らの間で長年にわたり使用されてきた[4]。
瓶詰めにされた多種の注射用アナボリックステロイド
目次
- 1 歴史
- 2 効果と適応
- 2.1 副作用
- 3 社会への蔓延
- 3.1 米国
- 3.2 日本
- 3.3 欧州
- 4 種類
- 5 出典
- 5.1 文献
- 6 関連項目
歴史
1935年に発見された物質テストステロンは、経口摂取されず、注射により体内に投与しても速やかに肝臓で代謝によって活性を失ってしまう―すなわち作用時間が短いという性質を有していた。そこで、この物質の代替物としての、多種の調整を加えたテストステロンアナログの開発が望まれた。[4]
やがて東西冷戦の激化に伴いオリンピックがイデオロギーの戦場と化してゆくという流れのなかで、数多の東欧の東側諸国が、自国の運動選手らに対するドーピングを組織的に行い始める。するとそれに対抗する形で、多くの国々がテストステロンの代替物としての合成薬の研究に着手。そして1955年―米国の重量挙げ選手団の専属医によって、ついに望まれていた形の『筋肉増強剤』が開発されるに至った。[5] それはテストステロンの類似物質、あるいは体内に取り込まれたのちにテストステロンに変換されるという物質であり、これがすなわちアナボリックステロイドであった。[4]
かくして誕生するに至ったアナボリックステロイドは、耐久性の運動競技や有酸素運動における能力の向上をもたらすものとして、1960年代の初め頃から重量挙げの選手やボディビルダーらの間で注目を集め始めた。[4]
1975年になると、国際オリンピック委員会によって、オリンピックにおける使用禁止物質の一覧に新たにアナボリックステロイドが加えられた。[4] そしてその翌1976年に開催されたモントリオールオリンピックにおいて、ようやく確立されるに至った検出技術を用いたうえで、オリンピック史上初となるアナボリックステロイドの使用検査が行われることとなった。[6]
やがて1980年代も後半に差し掛かると、1988年に開催されたソウルオリンピックにおいて、100メートル競走優勝者のベン・ジョンソンによるスタノゾロール[7]の使用が発覚したことで、アナボリックステロイドはスポーツ界を超えた一般社会からのドーピング一般に対する関心を惹起することとなった。[6]
効果と適応
男性ホルモン作用（アンドロゲン作用）については「男性ホルモン」を参照
そもそも生体から分泌される男性ホルモンの代表であるテストステロンの効力を改善するために合成されたことから[8]、そのテストステロンに類似した物質であり[3]、『蛋白同化ステロイド』[3]や『蛋白質同化性ステロイド』[4]あるいは『蛋白同化剤』[9]や『タンパク質同化ホルモン』[10]との訳語に明らかであるように、蛋白同化作用を強める働きを持つ。蛋白同化とはすなわち、摂取したタンパクを細胞内組織に変える働き（主に筋肉において）のことである。
その化学構造、17β-hydroxy-4-androsten-3-one.
アナボリックステロイドには『アナボリック・アンドロジェニックステロイド』(anabolic-androgenic steroid - AAS)―『男性ホルモン作用蛋白同化ステロイド』という異称がある。[11] 。
米国スポーツ医学会は、数名の個体において、アナボリックステロイドが適切な食事摂取の下で脂肪を付けること無く体重を増加させることに寄与し、また、強度の運動と適切な食事の下で達せられる筋力増加がその使用によってより促進されることを認めている。[12]
アナボリックステロイドは医療用に処方されることがある。その蛋白同化作用を用いて、骨粗鬆症や慢性の腎疾患の治療、あるいは怪我や火傷による体力の消耗状態の改善などを目的に用いられている。[文献1 1] こうして医療用に処方されるアナボリックステロイドには、メスタノロン製剤とメテノロン製剤という2種類のそれがある。[文献1 2] 前者は骨粗鬆症、下垂体性小人症、慢性腎疾患、悪性腫瘍、外傷/熱傷による著しい消耗状態などの治療に用いられ[文献1 1]、ヘモグロビン量や赤血球数の増加などの造血作用をも示す後者は、これらに加えて再生不良性貧血による骨髄の消耗状態の治療に用いられている。[文献1 3] 再生不良性貧血は骨髄中の造血幹細胞が何らかの原因で傷害されて生じる貧血である。一般に再生不良性貧血の治療は免疫抑制療法・骨髄移植・蛋白同化ステロイド療法などがある。そのうち蛋白同化ステロイドは軽傷例に使用する。蛋白同化ステロイドの疾患への効果のメカニズムとして、腎臓に作用してエリスロポエチン(赤血球産生を刺激するホルモン)を出させる働きと、造血幹細胞に直接作用して増殖を促す働きが考えられている。
HIVによる消耗状態に対する投与の治験も行われている。[1]
副作用
アナボリックステロイドには多くの副作用がある。その副作用は用量依存性で、最も一般的な副作用は血圧上昇とコレステロール値上昇である。空腹時血糖値や耐糖能検査の変化も見られている。テストステロンなどのアナボリックステロイドは、循環器疾患や冠動脈疾患のリスクを増大させる。にきびはアナボリックステロイド使用者によく見られ、多くの場合はテストステロン濃度増加に伴い皮脂腺が刺激されて起きる。
高用量のアナボリックステロイドを経口使用すると、アナボリックステロイドが消化管で代謝（C-17α位のアルキル化）され、その生物学的利用率および安定性が増すため、肝障害を起こすことがある。
高血圧、血中LDLコレステロールの増加、血中HDLコレステロールの低下により、心血管系の病気を誘発する原因ともなる。特に「心臓の運動」となる有酸素運動と組み合わせると、顕著な心肥大を起こさせるので絶対に組み合わせてはいけない。有名ランナーや自転車競技の選手が数多く心疾患で死亡している。
国際がん研究機関の査定に基づけば、アナボリックステロイドは、ヒトに対する発癌性(Group2A)をおそらく有している。[13]
起こり得るその副作用群をまとめれば次のようになる。[9][3]
-
- 肝障害、悪性肝臓腫瘍（肝臓癌）、前立腺癌、高コレステロール血症、高血圧症、心筋梗塞、糖尿病、睡眠時無呼吸症候群、性腺刺激ホルモン分泌低下性性機能低下症、体液性免疫異常、ニキビ、筋断裂、毛髪の消失、しゃがれ声化あるいは金切り声化など。
-
- 多毛症：顔、乳首の間、背中、肩、大腿の裏、臍下、殿部などといった、体毛が少ない部分への異常な出現。
- 精神的症状：鬱病的症状、妄想、気分変動の激化、パラノイア、苛立ち。
-
- 行動変化：攻撃性や突発的な暴力衝動の発現。
- 使用者が男性の場合：『女性化』 ― 乳房の女性化、すなわち男性の乳房発育。声の高音化、睾丸の萎縮、無精子症（すなわち精液中の精子の減少）、前立腺の肥大、可逆性の生殖不能症。テストステロンなどの男性ホルモンの体内における自然分泌量が低下するために起こる[8]。
- 使用者が女性の場合：『男性化』 ― 不可逆的な男性化あるいは男性化徴候、胎盤の男性化、声の深化、胸部の矮小化、無月経。
- 使用者の年齢によっては：思春期前期における早期骨端閉鎖。
筋肉増強剤としてステロイドを使用することは大変危険な行為であり、また筋肉増強剤に「正しい使い方」というものは存在しない。ステロイドをきちんと理解して使えば危険はないという情報は何ら科学的根拠が示されていない。使用することで健康に深刻なダメージを受けるリスクがあるから一般にドーピングとして禁止されているのであり、「こう使えば安全」「この薬なら危険が少ない」という情報で、使用する事は危険である。法に触れないということと、健康上問題がないということは必ずしも一致しない。
社会への蔓延
スポーツ選手が自分達の競技パフォーマンス向上のため、特に筋力を向上させることを目的にステロイドを使用する事は古くから行われていた。競技の公平性や選手の健康のために、様々な検査方法でドーピングの蔓延を防ごうと努力され、オリンピックをはじめとする大会では各種の厳重な検査を実施している。しかし、規制対象外の薬品を新たな増強剤として採用したり、増強剤の使用痕跡が出ないような薬品が開発されたりと、あの手この手で検査をすり抜ける試みが後を絶たない。中には国家が中心になってドーピングを行っている場合もあり、近年では検査をごまかす能力に長けた大国のドーピング違反者が減り、逆にドーピング歴の浅い小国が検査に引っかかる機会が多いという現象も起きている。法で規制されている国々には、しばしば使用者への販売を目的とする密輸品や偽造品の闇市場がある。[要出典]
米国
アメリカ合衆国においては、著名なメジャーリーガーらにステロイド使用の疑惑が持たれたり、「見栄えを良くしたい」といった理由でステロイドを使う青少年が出現して社会問題となった。一般層における使用の理由は、運動能力の向上ではなく、『肉体的魅力』の向上であることが主であるという[11]。自身が常用者であることを明かしたアメリカ人はおおよそ110万人に上っているとの2004年度の研究がある[14]。
カリフォルニア州などの一部の州は未成年による購買を法で規制しているが、インターネットを介して簡単に購入することが可能という状況にある。セントラル・ミシガン大学のトレイシー・オルリッチ博士の調査によると、米国における10代のステロイド使用者の数は2003年に30万人に達したという。[15] 米国国立薬物乱用研究所の2004年度の研究は、正確な統計の作成は困難であるものの、中学2年生と高校2年生だけで50万人が使用しているとの見積もりを示している。[14]
その常用者の一人としての著名なプロレスラー ―ハルク・ホーガン
町山智浩によれば、『ステロイドが生まれてからというもの、（米国の）スポーツ選手の身体は急激に変化していった』という。いわゆるアメコミのヒーローらは全てが『筋肉隆々』であり、星条旗の前で逞しい胸を張るスーパーマンが『アメリカ人男性』の理想として子供らに刷り込まれた。そしてそのような男性はフィクションの世界にしか存在し得ないものであったが、『ステロイドがそのありえない身体を現実にしてしまった』のだという。[要出典]
近年、ステロイド使用が明らかになったスポーツ選手には陸上のティム・モンゴメリ、ラショーン・メリット、マリオン・ジョーンズらがいる。
エンターテインメントの世界にも深く浸透している。1980年代より米国の『筋肉スター』の象徴としてその座を二分してきた映画俳優のアーノルド・シュワルツェネッガーとシルベスター・スタローンは両者ともステロイド使用者であり、同時期の米国のプロレスにおける『筋肉スター』の象徴であった『ミスター・アメリカ』ことハルク・ホーガンもステロイドの常用者であった。[16]
街の犯罪者らの間でも身体強化のために日常的に使用されており、更にはそれらと仕事で対することになる警察官らの間でも多く使用されているという。専門家の報告によれば、犯罪多発都市の警察官のうちの実に4人に1人がステロイドの使用者であり、その使用率の増加を示す事例も数多に上っている。[17] 闘犬用の犬に摂取させるブリーダーがいるという話もある。[18]
少女らによる使用の増加が社会問題になってもいる。その用途はすなわちモデルのような細い身体を手に入れるためのダイエットを目的としたものであり、ある2005年の報告によると、女子高校生のおおよそ5%、女子中学生のおおよそ7%が、少なくとも一度はステロイドを使用した経験を持っている。[19]
バリー・ボンズやホセ・カンセコ、マーク・マグワイアなどといった記録的な野球選手らのステロイド常用の発覚、そしてステロイドが原因と見られる著名なプロレスラーらの夭折が相次いで発生した2000年代にあっては、社会―特にスポーツ界におけるステロイドの蔓延という問題を議会が大きく取り上げるに至り、時のブッシュ政権は、ステロイドの危険性を啓発するための学校教育プログラムに巨費を投じた。[16]
CNNは、ステロイドを常習したプロレスラーのダイナマイト・キッドに対する独占取材を行い、身体がボロボロになり困窮と車椅子生活を送るその姿を紹介した。[20]
日本
日本においては個人での所有・使用に関しては合法とされているが、オリンピック種目を中心としたほとんどのスポーツではルールで使用を禁じている。オリンピックで日本人選手の禁止薬物使用が発覚した例は存在せず、このことからも、日本におけるステロイド使用者の率は国外に比して低いものと考えられる[21]。
法的に所有が禁止されていないため、インターネット販売を通じて入手し使用している者が一部に存在し、また具体的な薬のプロフィールやステロイドサイクルを掲載した情報もネットを中心に出回っているが、その内容の正確性は当然のことながら何の保証もされていない。
欧州
1970年代から1980年代に掛けてのオリンピックを席巻したドイツ民主共和国（東ドイツ）では、その選手団へのステロイドの投与を国家が主体となって組織的に行っていた。[22] 東ドイツの男子代表選手による使用の記録としては、初期のもので1963年のそれが残されている。女子選手らによるステロイドの使用は、1968年のメキシコオリンピックを控えた時期から本格的に始まった。更に男性ホルモンなどの使用が加わった1970年代にあっては、オリンピックのほぼあらゆる競技でこうしたドーピングが行われた結果、東ドイツの選手らによる金メダルの獲得数が突出するようになり、やがて東ドイツは米国やソビエト連邦に並ぶ『スポーツ大国』と呼ばれるようになるに至った。[23]
イギリスにあっては、異性の気を惹きたいという理由で10代前半の少年らまでもがステロイドを乱用している―2000年代の後半におけるそのような話題がきっかけとなり、政府機関の専門家らが、ボディビルダーや特に10代の少年らの間でのステロイドの急激な蔓延現象についての警告を発するに至っている。2007年度に明かされた統計によれば、ステロイドを使用した経験を持つ英国民は20万人に達しており、そのおおよそ5分の1にあたる4万人ほどはその前年にも使用、更にはそのうちの2万人ほどは、その統計が取られた月の直前月にも使用していたという。[24]
種類
| この節は検証可能な参考文献や出典が全く示されていないか、不十分です。出典を追加して記事の信頼性向上にご協力ください。（2009年11月） |
注射用の『シピオン酸テストステロン』(Depo-Testosterone)
- ステロイドアナボリックホルモン
- テストステロンプロドラッグ
- テストステロンシピオナート-Testola･Testo（経口）、Depo-Testosterone（注射） CAS:58-20-8
- テストステロンエナント酸エステル-Delatestryl（注射） CAS:315-37-7
- テストステロンエステル-混合物-Sustanon 250（注射）
- テストステロンニコチン酸-Bolfortan（注射）
- メチルテストステロン（methyltestosterone）-Android（経口） CAS:58-18-4
- デヒドロクロルメチルテストステロン（dehydrochlormethyl-testosterone）-Turnibol（経口）
- エチルエストレノール（ethlestrenol）-Maxibolin（経口） CAS:965-90-2
- オキシメステロン（oxymetholone）-Anadrol（経口） CAS:145-12-0
- ステンボロン-Anatrofin（注射） CAS:5197-58-0
- トレンボロン（trenbolone acetate、19-nortestosterone）-Finajet（経口）（注射） CAS:10161-33-8
- メステロロン（mesterolone）-Proviron（経口） CAS:1424-00-6
- メタンドロステノロン（methandrostenolone）-Dianabol（経口） CAS:72-63-9
- ヘキソキシメストローラム-Enoltestovis（注射）
- メテノロン-プリモボラン（経口） CAS:153-00-4
- メテノロンエナント酸塩-プリモボランデポー（注射） CAS:303-42-4
- ナンドロロン（経口）
- ナンドロロンデカン酸エステル-Deca-Durabolin（注射） CAS:360-70-3
- ナンドロロンフェンプロピオン酸エステル-Durabolin（注射） CAS:62-90-8
- ボルデノン（boldenone undecylonate）-Boldenon QV 200（経口）、Equipoise（注射） CAS:13103-34-9
- 非ステロイドアナボリックホルモン
- オキサンドロロン（oxandrolone）-Oxandrin･Anavar（経口） CAS:53-39-4
- スタノゾロール（stanozolol）-Winstrol・Cetabon（経口）、Winstrol-V（注射） CAS:10418-03-8
出典
- ^ 『ステロイド』って何？---医療関係者とスポーツ関係者の違い--- 日本薬剤師会
- ^ Hartgens and Kuipers (2004), p. 515 （英語）
Kicman AT, Gower DB (July 2003) "Anabolic steroids in sport: biochemical, clinical and analytical perspectives.". Annals of clinical biochemistry 40 (Pt 4): 321–56. doi:10.1258/000456303766476977. PMID 12880534. （英語） - ^ a b c d 筋肉増強剤（蛋白同化ステロイド）の危険性 - All About
- ^ a b c d e f 蛋白質同化性ステロイド（筋肉増強剤）（Anabolic Steroids）
- ^ より高く、より速く、より強く - 栄光へのドーピング X51.ORGによる訳
- ^ a b 知ってほしいドーピングの知識
- ^ ドーピングの歴史 日本オリンピック委員会
- ^ a b ドーピングに関する諸問題
- ^ a b 蛋白同化剤・ステロイド剤とその副作用 日本自転車競技連盟
- ^ アナボリックステロイドの意味 国語辞典 goo辞書
- ^ a b 一般層に広がる「ドーピング」：高学歴の若いホワイトカラーが中心 WIRED.jp 2007年10月30日
- ^ Michael Powers, "Performance-Enhancing Drugs" in Joel Houglum, in Gary L. Harrelson, Deidre Leaver-Dunn, "Principles of Pharmacology for Athletic Trainers", SLACK Incorporated, 2005, ISBN 1556425945, p. 330 （英語）
- ^ IARC Monographs- Classifications - Group2a 2008年3月20日更新版 （英語） 国際がん研究機関
- ^ a b Steroid Abuse in Today's Society - A Guide for Understanding Steroids and Related Substances （英語） 米国麻薬取締局 2004年3月
- ^ 『USAスポーツ狂騒曲 アメリカは今日もステロイドを打つ』 P.16 町山智浩 ISBN 9784087805161
- ^ a b 『USAスポーツ狂騒曲 アメリカは今日もステロイドを打つ』 序章 町山智浩 ISBN 9784087805161
- ^ 「ドーピング警察官」が増加 WIRED.jp 2007年10月25日
- ^ アメリカの闘犬という残忍な文化
- ^ 米国少女たちの危険なダイエット＝ステロイド使用が社会問題に livedoor (AP通信)
- ^ 『デス・グリップ・インサイド・プロ・レスリング』(Death Grip Inside Pro Wrestling) （英語） 2007年11月10日 CNN
- ^ 【FIGHTS SPIRAL】の概念（禁止薬物編）
- ^ 第六部 ドーピング〈３〉 毎日注射、果ては死…旧東独選手衝撃告白 読売新聞
- ^ 第六部 ドーピング〈２〉 旧東独薬まみれの「金」 読売新聞
- ^ Boys of 12 using anabolic steroids to 'get girls' （英語） 2007年11月30日 ガーディアン
文献
- 『薬と病気の本』 橋本信也 2006年8月10日 第7版 ISBN 4832703188
- ^ a b 頁．806：『たんぱく同化ステロイド剤』
- ^ 頁．805：『男性ホルモン薬』
- ^ 頁．807：『メテノロン（プリモボラン）』
関連項目
- メジャー・リーグ薬物使用疑惑
- ミッチェル報告書に記述された選手一覧
- ドーピング
- バルコ・スキャンダル
- Juiced〜禁断の肉体改造〜
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wiki en
Chemical structure of the natural anabolic hormone testosterone, 17β-hydroxy-4-androsten-3-one
Chemical structure of the synthetic steroid methandrostenolone (Dianabol). 17α-Methylation (upper-right corner) enhances oral bioavailability.
Anabolic steroids, technically known as anabolic-androgenic steroids (AAS), are drugs that are structurally related to the cyclic steroid ring system and have similar effects to testosterone in the body. They increase protein within cells, especially in skeletal muscles. Anabolic steroids also have androgenic and virilizing properties, including the development and maintenance of masculine characteristics such as the growth of the vocal cords, testicles (primary sexual characteristics) and body hair (secondary sexual characteristics). The word anabolic comes from the Greek ἀναβολή anabole, "that which is thrown up, mound", and the word androgenic from the Greek ἀνδρός andros, "of a man" + -γενής -genes, "born".
Anabolic steroids were first made in the 1930s, and are now used therapeutically in medicine to stimulate muscle growth and appetite, induce male puberty and treat chronic wasting conditions, such as cancer and AIDS. The American College of Sports Medicine acknowledges that AAS, in the presence of adequate diet, can contribute to increases in body weight, often as lean mass increases and that the gains in muscular strength achieved through high-intensity exercise and proper diet can be additionally increased by the use of AAS in some individuals.[1]
Health risks can be produced by long-term use or excessive doses of anabolic steroids.[2][3] These effects include harmful changes in cholesterol levels (increased low-density lipoprotein and decreased high-density lipoprotein), acne, high blood pressure, liver damage (mainly with oral steroids), and dangerous changes in the structure of the left ventricle of the heart.[4] Conditions pertaining to hormonal imbalances such as gynecomastia and testicular atrophy may also be caused by anabolic steroids.
Ergogenic uses for anabolic steroids in sports, racing, and bodybuilding as performance-enhancing drugs are controversial because of their adverse effects and the potential to gain unfair advantage is considered cheating. Their use is referred to as doping and banned by all major sporting bodies. For many years, AAS have been by far the most detected doping substances in IOC-accredited laboratories.[5][6] In countries where AAS are controlled substances, there is often a black market in which smuggled, clandestinely manufactured or even counterfeit drugs are sold to users.
Contents
- 1 List of anabolic steroids
- 1.1 Exogenous anabolic androgenic steroids
- 1.2 Endogenous anabolic androgenic steroids
- 1.2.1 Metabolites and isomers
- 2 Pharmacology
- 2.1 Routes of administrations
- 2.2 Mechanism of action
- 2.3 Anabolic and androgenic effects
- 2.3.1 Body composition and strength improvements
- 3 Medical and ergogenic uses
- 3.1 Medical uses
- 3.2 Ergogenic use and abuse
- 4 Adverse effects
- 4.1 Neuropsychiatric
- 4.1.1 DSM assertion
- 4.1.2 Personality profiles
- 4.1.3 Mood and anxiety
- 4.1.3.1 Aggression and hypomania
- 4.1.3.2 Depression and suicide
- 4.2 Physiological
- 4.2.1 Cancer
- 4.2.2 Cardiovascular
- 4.2.3 Growth defects
- 4.2.4 Feminization
- 4.2.5 Masculinization
- 4.2.6 Kidney problems
- 4.2.7 Liver problems
- 4.1 Neuropsychiatric
- 5 AAS abuse
- 5.1 Abuse potential
- 5.1.1 DSM
- 5.1.2 ICD
- 5.1.3 National Institute on Drug Abuse
- 5.2 Causes and treatment
- 5.2.1 Childhood trauma
- 5.3 Illicit use by groups
- 5.3.1 Criminals
- 5.3.2 Governments
- 5.3.2.1 Law enforcement
- 5.3.3 Sports
- 5.3.3.1 Professional wrestling
- 5.4 Tragedies involving AAS abuse
- 5.4.1 Chris Benoit double-murder and suicide
- 5.4.2 David Jacobs
- 5.1 Abuse potential
- 6 Legal and sport restrictions
- 6.1 Legal status
- 6.1.1 United States
- 6.1.2 United Kingdom
- 6.2 Status in sports
- 6.3 Detection of use
- 6.1 Legal status
- 7 Illegal trade
- 8 History
- 8.1 Isolation of gonadal AAS
- 8.2 Development of synthetic AAS
- 9 See also
- 10 References
- 11 Further reading
- 12 External links
List of anabolic steroids
See also: List of steroid abbreviations
Exogenous anabolic androgenic steroids
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|
Endogenous anabolic androgenic steroids
- Androstenediol
- Androstenedione
- Dihydrotestosterone
- Prasterone (dehydroepiandrosterone DHEA)
- Testosterone
Metabolites and isomers
Metabolites and isomers of endogenous anabolic androgenic steroids, including, but not limited to:
|
|
Pharmacology
Routes of administrations
A vial of injectable testosterone cypionate
There are four common forms in which anabolic steroids are administered: oral pills; injectable steroids; creams/gels for topical application; and skin patches. Oral administration is the most convenient. Testosterone administered by mouth is rapidly absorbed, but it is largely converted to inactive metabolites, and only about 1/6 is available in active form. In order to be sufficiently active when given by mouth, testosterone derivatives are alkylated at the 17 position, e.g. methyltestosterone and fluoxymesterone. This modification reduces the liver's ability to break down these compounds before they reach the systemic circulation.
Testosterone can be administered parenterally, but it has more irregular prolonged absorption time and greater activity in muscle in enanthate, undecanoate, or cypionate ester form. These derivatives are hydrolyzed to release free testosterone at the site of injection; absorption rate (and thus injection schedule) varies among different esters, but medical injections are normally done anywhere between semi-weekly to once every 12 weeks. A more frequent schedule may be desirable in order to maintain a more constant level of hormone in the system.[7] Injectable steroids are typically administered into the muscle, not into the vein, to avoid sudden changes in the amount of the drug in the bloodstream. In addition, because estered testosterone is dissolved in oil, intravenous injection has the potential to cause a dangerous embolism (clot) in the bloodstream.
Transdermal patches (adhesive patches placed on the skin) may also be used to deliver a steady dose through the skin and into the bloodstream. Testosterone-containing creams and gels that are applied daily to the skin are also available, but absorption is inefficient (roughly 10%, varying between individuals) and these treatments tend to be more expensive. Individuals who are especially physically active and/or bathe often may not be good candidates, since the medication can be washed off and may take up to six hours to be fully absorbed. There is also the risk that an intimate partner or child may come in contact with the application site and inadvertently dose himself or herself; children and women are highly sensitive to testosterone and can suffer unintended masculinization and health effects, even from small doses. Injection is the most common method used by individuals administering anabolic steroids for non-medical purposes.[8]
The traditional routes of administration do not have differential effects on the efficacy of the drug. Studies indicate that the anabolic properties of anabolic steroids are relatively similar despite the differences in pharmacokinetic principles such as first-pass metabolism. However, the orally available forms of AAS may cause liver damage in high doses.[6][9]
Mechanism of action
See also: Steroid hormone
The human androgen receptor bound to testosterone[10] The protein is shown as a ribbon diagram in red, green, and blue, with the steroid shown in white.
The pharmacodynamics of anabolic steroids are unlike peptide hormones. Water-soluble peptide hormones cannot penetrate the fatty cell membrane and only indirectly affect the nucleus of target cells through their interaction with the cell’s surface receptors. However, as fat-soluble hormones, anabolic steroids are membrane-permeable and influence the nucleus of cells by direct action. The pharmacodynamic action of anabolic steroids begin when the exogenous hormone penetrates the membrane of the target cell and binds to an androgen receptor located in the cytoplasm of that cell. From there, the compound hormone-receptor diffuses into the nucleus, where it either alters the expression of genes[11] or activates processes that send signals to other parts of the cell.[12] Different types of anabolic steroids bind to the androgen receptor with different affinities, depending on their chemical structure.[5] Some anabolic steroids such as methandrostenolone bind weakly to this receptor in vitro, but still exhibit androgenic effects in vivo. The reason for this discrepancy is not known.[13]
The effect of anabolic steroids on muscle mass is caused in at least two ways:[14] first, they increase the production of proteins; second, they reduce recovery time by blocking the effects of stress hormone cortisol on muscle tissue, so that catabolism of muscle is greatly reduced. It has been hypothesized that this reduction in muscle breakdown may occur through anabolic steroids inhibiting the action of other steroid hormones called glucocorticoids that promote the breakdown of muscles.[15] Anabolic steroids also affect the number of cells that develop into fat-storage cells, by favouring cellular differentiation into muscle cells instead.[16] Anabolic steroids can also decrease fat by increasing basal metabolic rate (BMR), since an increase in muscle mass increases BMR.
Anabolic and androgenic effects
| Preparation | Ratio |
|---|---|
| Testosterone | 1:1 |
| Methyltestosterone | 1:1 |
| Fluoxymesterone | 1:2 |
| Oxymetholone | 1:3 |
| Oxandrolone | 1:3–1:13 |
| Nandrolone decanoate | 1:2.5–1:4 |
As the name suggests, anabolic-androgenic steroids have two different, but overlapping, types of effects: anabolic, meaning that they promote anabolism (cell growth), and androgenic (or virilising), meaning that they affect the development and maintenance of masculine characteristics.
Some examples of the anabolic effects of these hormones are increased protein synthesis from amino acids, increased appetite, increased bone remodeling and growth, and stimulation of bone marrow, which increases the production of red blood cells. Through a number of mechanisms anabolic steroids stimulate the formation of muscle cells and hence cause an increase in the size of skeletal muscles, leading to increased strength.[17][18][19]
The androgenic effects of AAS are numerous. Depending on the length of use, the side effects of the steroid can be irreversible. Processes affected include pubertal growth, sebaceous gland oil production, and sexuality (especially in fetal development). Some examples of virilizing effects are growth of the clitoris in females and the penis in male children (the adult penis size does not change due to steroids[medical citation needed] ), increased vocal cord size, increased libido, suppression of natural sex hormones, and impaired production of sperm.[20] Effects on women include deepening of the voice, facial hair growth, and possibly a decrease in breast size. Men may develop an enlargement of breast tissue, known as gynecomastia, testicular atrophy, and a reduced sperm count.[21]
The androgenic:anabolic ratio of an AAS is an important factor when determining the clinical application of these compounds. Compounds with a high ratio of androgenic to an anabolic effects are the drug of choice in androgen-replacement therapy (e.g., treating hypogonadism in males), whereas compounds with a reduced androgenic:anabolic ratio are preferred for anemia and osteoporosis, and to reverse protein loss following trauma, surgery, or prolonged immobilization. Determination of androgenic:anabolic ratio is typically performed in animal studies, which has led to the marketing of some compounds claimed to have anabolic activity with weak androgenic effects. This disassociation is less marked in humans, where all anabolic steroids have significant androgenic effects.[7]
A commonly used protocol for determining the androgenic:anabolic ratio, dating back to the 1950s, uses the relative weights of ventral prostate (VP) and levator ani muscle (LA) of male rats. The VP weight is an indicator of the androgenic effect, while the LA weight is an indicator of the anabolic effect. Two or more batches of rats are castrated and given no treatment and respectively some AAS of interest. The LA/VP ratio for an AAS is calculated as the ratio of LA/VP weight gains produced by the treatment with that compound using castrated but untreated rats as baseline: (LAc,t–LAc)/(VPc,t–VPc). The LA/VP weight gain ratio from rat experiments is not unitary for testosterone (typically 0.3–0.4), but it is normalized for presentation purposes, and used as basis of comparison for other AAS, which have their androgenic:anabolic ratios scaled accordingly (as shown in the table above).[13][22] In the early 2000s, this procedure was standardized and generalized throughout OECD in what is now known as the Hershberger assay.
Body composition and strength improvements
A review spanning more than three decades of experimental studies in men found that body weight may increase by 2–5 kg as a result of short-term (<10 weeks) AAS use, which may be attributed mainly to an increase of lean mass. Animal studies also found that fat mass was reduced, but most studies in humans failed to elucidate significant fat mass decrements. The effects on lean body mass have been shown to be dose-dependent. Both muscle hypertrophy and the formation of new muscle fibers have been observed. The hydration of lean mass remains unaffected by AAS use, although small increments of blood volume cannot be ruled out.[5]
The upper region of the body (thorax, neck, shoulders, and upper arm) seems to be more susceptible for AAS than other body regions because of predominance of androgen receptors in the upper body. The largest difference in muscle fiber size between AAS users and non-users was observed in type I muscle fibers of the vastus lateralis and the trapezius muscle as a result of long-term AAS self-administration. After drug withdrawal, the effects fade away slowly, but may persist for more than 6–12 weeks after cessation of AAS use.[5]
The same review observed strength improvements in the range of 5–20% of baseline strength, depending largely on the drugs and dose used as well as the administration period. Overall, the exercise where the most significant improvements were observed is the bench press.[5] For almost two decades, it was assumed that AAS exerted significant effects only in experienced strength athletes, particularly based on the studies of Hervey and coworkers.[23][24] In 1996, a randomized controlled trial published in the New England Journal of Medicine demonstrated, however, that even in novice athletes a 10-week strength training program accompanied by testosterone enanthate at 600 mg/week may improve strength more than training alone does.[5][25] The same study found that dose to be sufficient to significantly improve lean muscle mass relative to placebo even in subjects that did not exercise at all.[25] A 2001 study by the same first author, showed that the anabolic effects of testosterone enanthate were highly dose dependent.[5][26]
Medical and ergogenic uses
Medical uses
Various anabolic steroids and related compounds
Since the discovery and synthesis of testosterone in the 1930s, anabolic steroids have been used by physicians for many purposes, with varying degrees of success, for the treatment of:
- Bone marrow stimulation: For decades, anabolic steroids were the mainstay of therapy for hypoplastic anemias due to leukemia or kidney failure, especially aplastic anemia.[27] Anabolic steroids have largely been replaced in this setting by synthetic protein hormones (such as epoetin alfa) that selectively stimulate growth of blood cell precursors.
- Growth stimulation: Anabolic steroids can be used by pediatric endocrinologists to treat children with growth failure.[28] However, the availability of synthetic growth hormone, which has fewer side effects, makes this a secondary treatment.
- Stimulation of appetite and preservation and increase of muscle mass: Anabolic steroids have been given to people with chronic wasting conditions such as cancer and AIDS.[29][30]
- Induction of male puberty: Androgens are given to many boys distressed about extreme delay of puberty. Testosterone is now nearly the only androgen used for this purpose and has been shown to increase height, weight, and fat-free mass in boys with delayed puberty.[31]
- Male contraception, in the form of testosterone enanthate; potential for use in the near-future as a safe, reliable, and reversible male contraceptive.[32][33]
- Stimulation of lean body mass and prevention of bone loss in elderly men, as some studies indicate.[34][35][36] However, a 2006 placebo-controlled trial of low-dose testosterone supplementation in elderly men with low levels of testosterone found no benefit on body composition, physical performance, insulin sensitivity, or quality of life.[37]
- Hormone replacement for men with low levels of testosterone; also effective in improving libido for elderly males.[38][39][40][41]
- Gender Identity Disorder, by producing secondary male characteristics, such as a deeper voice, increased bone and muscle mass, facial hair, increased levels of red blood cells, and clitoral enlargement in female-to-male patients.[42]
Ergogenic use and abuse
See also: Ergogenic use of anabolic steroids
Numerous vials of injectable anabolic steroids
Most steroid users are not athletes.[43] Between 1 million and 3 million people (1% of the population) are thought to have misused AAS in the United States.[44] Studies in the United States have shown that anabolic steroid users tend to be mostly middle-class heterosexual men with a median age of about 25 who are noncompetitive bodybuilders and non-athletes and use the drugs for cosmetic purposes.[45] "Among 12- to 17-year-old boys, use of steroids and similar drugs jumped 25 percent from 1999 to 2000, with 20 percent saying they use them for looks rather than sports, a study by insurer Blue Cross Blue Shield found."(Eisenhauer) Another study found that non-medical use of AAS among college students was at or less than 1%.[46] According to a recent survey, 78.4% of steroid users were noncompetitive bodybuilders and non-athletes, while about 13% reported unsafe injection practices such as reusing needles, sharing needles, and sharing multidose vials,[47] though a 2007 study found that sharing of needles was extremely uncommon among individuals using anabolic steroids for non-medical purposes, less than 1%.[8] Another 2007 study found that 74% of non-medical anabolic steroid users had secondary college degrees and more had completed college and fewer had failed to complete high school than is expected from the general populace.[8] The same study found that individuals using anabolic steroids for non-medical purposes had a higher employment rate and a higher household income than the general population.[8] Anabolic steroid users tend to research the drugs they are taking more than other controlled-substance users; however, the major sources consulted by steroid users include friends, non-medical handbooks, internet-based forums, blogs, and fitness magazines, which can provide questionable or inaccurate information.[48]
Anabolic steroid users tend to be disillusioned by the portrayal of anabolic steroids as deadly in the media and in politics.[49] According to one study, AAS users also distrust their physicians and in the sample 56% had not disclosed their AAS use to their physicians.[50] Another 2007 study had similar findings, showing that, while 66% of individuals using anabolic steroids for non-medical purposes were willing to seek medical supervision for their steroid use, 58% lacked trust in their physicians, 92% felt that the medical community's knowledge of non-medical anabolic steroid use was lacking, and 99% felt that the public has an exaggerated view of the side-effects of anabolic steroid use.[8] A recent study has also shown that long term AAS users were more likely to have symptoms of muscle dysmorphia and also showed stronger endorsement of more conventional male roles.[51]
Anabolic steroids have been used by men and women in many different kinds of professional sports to attain a competitive edge or to assist in recovery from injury. These sports include bodybuilding, weightlifting, shot put and other track and field, cycling, baseball, wrestling, mixed martial arts, boxing, football, and cricket. Such use is prohibited by the rules of the governing bodies of most sports. Anabolic steroid use occurs among adolescents, especially by those participating in competitive sports. It has been suggested that the prevalence of use among high-school students in the U.S. may be as high as 2.7%.[52] Male students used anabolic steroids more frequently than female students and, on average, those that participated in sports used steroids more often than those that did not.
Adverse effects
Anabolic steroid use can cause many adverse effects.
Neuropsychiatric
A 2005 review in CNS Drugs determined that "significant psychiatric symptoms including aggression and violence, mania, and less frequently psychosis and suicide have been associated with steroid abuse. Long-term steroid abusers may develop symptoms of dependence and withdrawal on discontinuation of AAS".[53] High concentrations of AAS, comparable to those likely sustained by many recreational AAS users, produce apoptotic effects on neurons, raising the specter of possibly irreversible neuropsychiatric toxicity. Recreational AAS use appears to be associated with a range of potentially prolonged psychiatric effects, including dependence syndromes, mood disorders, and progression to other forms of substance abuse, but the prevalence and severity of these various effects remains poorly understood.[54] There is no evidence that steroid dependence develops from therapeutic use of anabolic steroids to treat medical disorders, but instances of AAS dependence have been reported among weightlifters and bodybuilders who chronically administered supraphysiologic doses.[55] Mood disturbances (e.g. depression, [hypo-]mania, psychotic features) are likely to be dose- and drug-dependent, but AAS dependence or withdrawal effects seem to occur only in a small number of AAS users.[5]
Large-scale long-term studies of psychiatric effects on AAS users are not currently available.[54] In 2003, the first naturalistic long-term study on ten users, seven of which having completed the study, found a high incidence of mood disorders and substance abuse, but few clinically relevant changes in physiological parameters or laboratory measures were noted throughout the study, and these changes were not clearly related to periods of reported AAS use.[56] A 13-month study, which was published in 2006 and which involved 320 body builders and athletes suggests that the wide range of psychiatric side-effects induced by the use of AAS is correlated to the severity of abuse.[57]
DSM assertion
DSM-IV lists General diagnostic criteria for a personality disorder guideline that "The pattern must not be better accounted for as a manifestation of another mental disorder, or to the direct physiological effects of a substance (e.g. drug or medication) or a general medical condition (e.g. head trauma).". As a result anabolic steroid users may get misdiagnosed by psychiatrist not told about their habit.[58]
Personality profiles
Cooper, Noakes, Dunne, Lambert, and Rochford identified that anabolic–androgenic steroid (AAS) using individuals are more likely to score higher on borderline (4.7 times), antisocial (3.8 times), paranoid (3.4 times), schizotypal (3.1 times), histrionic (2.9 times), passive-aggressive (2.4 times), and narcissistic (1.6 times) personality profiles than non-users.[59] Other studies have suggested that antisocial personality disorder is slightly more likely among anabolic steroid users than among non-users (Pope & Katz, 1994).[58] Bipolar dysfunction,[60] substance dependency, and conduct disorder have also been associated with AAS use.[61]
Mood and anxiety
Affective disorders have long been recognised as a complication of anabolic steroid use. Case reports describe both hypomania and mania, along with irritability, elation, recklessness, racing thoughts and feelings of power and invincibility that did not meet the criteria for mania/hypomania.[62] Of 53 bodybuilders who used anabolic steroids, 27 (51%) reported unspecified mood disturbance.[63]
Aggression and hypomania
From the mid-1980s onward, the media reported "roid rage" as a side-effect of AAS.[64]
A 2005 review determined that some, but not all, randomized controlled studies have found that anabolic steroid use correlates with hypomania and increased aggressiveness, but pointed out that attempts to determine whether AAS use triggers violent behavior have failed, primarily because of high rates of non-participation.[65] A 2008 study on a nationally representative sample of young adult males in the United States found an association between lifetime and past-year self-reported anabolic-androgenic steroid use and involvement in violent acts. Compared with individuals that did not use steroids, young adult males that used anabolic-androgenic steroids reported greater involvement in violent behaviors even after controlling for the effects of key demographic variables, previous violent behavior, and polydrug use.[66] A 1996 review examining the blind studies available at that time also found that these had demonstrated a link between aggression and steroid use, but pointed out that with estimates of over one million past or current steroid users in the United States at that time, an extremely small percentage of those using steroids appear to have experienced mental disturbance severe enough to result in clinical treatments or medical case reports.[67]
A 1996 randomized controlled trial, which involved 43 men, did not find an increase in the occurrence of angry behavior during 10 weeks of administration of testosterone enanthate at 600 mg/week, but this study screened out subjects that had previously abused steroids or had any psychiatric antecedents.[25][68] A trial conducted in 2000 using testosterone cypionate at 600 mg/week found that treatment significantly increased manic scores on the YMRS, and aggressive responses on several scales. The drug response was highly variable. However: 84% of subjects exhibited minimal psychiatric effects, 12% became mildly hypomanic, and 4% (2 subjects) became markedly hypomanic. The mechanism of these variable reactions could not be explained by demographic, psychological, laboratory, or physiological measures.[69]
A 2006 study of two pairs of identical twins, in which one twin used anabolic steroids and the other did not, found that in both cases the steroid-using twin exhibited high levels of aggressiveness, hostility, anxiety, and paranoid ideation not found in the "control" twin.[70] A small-scale study of 10 AAS users found that cluster B personality disorders were confounding factors for aggression.[71]
Androgenic steroids are known to increase aggression with greater likelihood when compared to more anabolic steroids. Trenbolone is frequently noted for its increases in aggression. Equipoise is known to increase anxiety in some users.
Depression and suicide
The relationship between AAS use and depression is inconclusive. There have been anecdotal reports of depression and suicide in teenage steroid users,[72] but little systematic evidence. A 1992 review found that anabolic-androgenic steroids may both relieve and cause depression, and that cessation or diminished use of anabolic-androgenic steroids may also result in depression, but called for additional studies due to disparate data.[73] In the case of suicide, 3.9% of a sample of 77 those classified as AAS users reported attempting suicide during withdrawal (Malone, Dimeff, Lombardo, & Sample, 1995).[74]
Physiological
Depending on the length of drug abuse, there is a chance that the immune system can be damaged. Most of these side-effects are dose-dependent, the most common being elevated blood pressure, especially in those with pre-existing hypertension,[75]
Anabolic steroids have been shown to alter fasting blood sugar and glucose tolerance tests.[76] Anabolic steroids such as testosterone also increase the risk of cardiovascular disease[2] or coronary artery disease.[77][78] Acne is fairly common among anabolic steroid users, mostly due to stimulation of the sebaceous glands by increased testosterone levels.[5][79] Conversion of testosterone to dihydrotestosterone (DHT) can accelerate the rate of premature baldness for males genetically predisposed, but testosterone itself can produce baldness in females.[80]
A number of severe side-effects can occur if adolescents use anabolic steroids.
For example, the steroids may prematurely stop the lengthening of bones (premature epiphyseal fusion through increased levels of estrogen metabolites), resulting in stunted growth. Other effects include, but are not limited to, accelerated bone maturation, increased frequency and duration of erections, and premature sexual development. Anabolic steroid use in adolescence is also correlated with poorer attitudes related to health.[81]
Cancer
WHO organization International Agency for Research on Cancer (IARC) list Androgenic (anabolic) steroids under Group 2A: Probably carcinogenic to humans.[82]
Cardiovascular
Other side-effects can include alterations in the structure of the heart, such as enlargement and thickening of the left ventricle, which impairs its contraction and relaxation.[4] Possible effects of these alterations in the heart are hypertension, cardiac arrhythmias, congestive heart failure, heart attacks, and sudden cardiac death.[83] These changes are also seen in non-drug-using athletes, but steroid use may accelerate this process.[84][85] However, both the connection between changes in the structure of the left ventricle and decreased cardiac function, as well as the connection to steroid use have been disputed.[86][87]
AAS use can cause harmful changes in cholesterol levels: Some steroids cause an increase in LDL "bad" cholesterol and a decrease in HDL "good" cholesterol.[88] In addition, steroids provoke a rapid increase in body weight and an accompanying rise in blood pressure, both of which leave users more vulnerable to a cardiovascular event.[89]
Growth defects
An important side effect to mention for high school athletes because steroids can cause the premature closure of the growth plate, leading to stunted growth.[89]
Feminization
Male with gynecomastia
See also: Feminization (biology)
There are also sex-specific side effects of anabolic steroids. Development of breast tissue in males, a condition called gynecomastia (which is usually caused by high levels of circulating estradiol), may arise because of increased conversion of testosterone to estradiol by the enzyme aromatase.[90] Reduced sexual function and temporary infertility can also occur in males.[32][91][92] Another male-specific side-effect that can occur is testicular atrophy, caused by the suppression of natural testosterone levels, which inhibits production of sperm (most of the mass of the testes is developing sperm). This side-effect is temporary: The size of the testicles usually returns to normal within a few weeks of discontinuing anabolic steroid use as normal production of sperm resumes.[93]
Masculinization
See also: Virilization
Female-specific side effects include increases in body hair, permanent deepening of the voice, enlarged clitoris, and temporary decreases in menstrual cycles. When taken during pregnancy, anabolic steroids can affect fetal development by causing the development of male features in the female fetus and female features in the male fetus.[94]
Kidney problems
Kidney tests revealed that nine of the ten bodybuilders developed a condition called focal segmental glomerulosclerosis, a type of scarring within the kidneys. The kidney damage in the bodybuilders has similarities to that seen in morbidly obese patients, but appears to be even more severe.[95]
Liver problems
High doses of oral anabolic steroid compounds can cause liver damage, as the steroids are metabolized (17α-alkylated) in the digestive system to increase their bioavailability and stability.[3] Peliosis hepatis has been increasingly recognised with the use of anabolic steroids.
AAS abuse
Anabolic steroids are not psychoactive and cannot be detected by stimuli devices like a pupilometer which makes them hard to spot as a source of neuropsychological imbalaces in some AAS users.
Research data indicates that steroids affect the serotonin and dopamine neurotransmitter systems of the brain.[96] In an animal study, male rats developed a conditioned place preference to testosterone injections into the nucleus accumbens, an effect blocked by dopamine antagonists, which suggests that androgen reinforcement is mediated by the brain. Moreover, testosterone appears to act through the mesolimbic dopamine system, a common substrate for drugs of abuse. Nonetheless, androgen reinforcement is not comparable to that of cocaine, nicotine, or heroin. Instead, testosterone resembles other mild reinforcers, such as caffeine, or benzodiazepines. The potential for androgen addiction remains to be determined.[97] However, abuse of steroids is rivalling heroin use in Britain.[98]
Abuse potential
The Diagnostic Statistical Manual IV (DSM IV) and the International Classification of Diseases, Volume 10 (ICD 10) differ in the way they regard Anabolic-Androgenic Steroids' (AAS) potential for producing dependence. DSM IV regards AAS as potentially dependence producing. ICD 10 however regards them as non-dependence producing.[99] Anabolic steroids are not physically addictive but users can develop a psychological dependence on the physical result.[100]
DSM
For DSM-IV, anabolic-androgenic steroid dependency is found in the “other substance-related disorder” (include inhalants, anabolic steroids, medications) section and can be coded, depending on which diagnostic criteria are met.[101]
ICD
ICD–10 criteria for dependence include experience of at least three of the following during the past year:[58]
- a strong desire to take steroids
- difficulty in controlling use
- withdrawal syndrome when use is reduced
- evidence of tolerance
- neglect of other interests and persistent use despite harmful consequences
However, the following ICD-10-CM Index entries contain back-references to ICD-10-CM F55.3:[102]
- Abuse
- hormones F55.5
- steroids F55.5
- drug NEC (non-dependent) F19.10
- hormones F55.5
- steroids F55.5
- non-psychoactive substance NEC F55.8
- hormones F55.5
- steroids F55.5
ICD-10 goes on to state that “although it is usually clear that the patient has a strong motivation to take the substance, there is no development of dependence or withdrawal symptoms as in the case of the psychoactive substances.”[101]
ICD-9-CM will be replaced by ICD-10-CM beginning October 1, 2014, therefore, F55.3 and all other ICD-10-CM diagnosis codes should only be used for training or planning purposes until then.
National Institute on Drug Abuse
The National Institute on Drug Abuse (NIDA) says that "even though anabolic steroids do not cause the same high as other drugs, steroids are reinforcing and can lead to addiction. Studies have shown that animals will self-administer steroids when given the opportunity, just as they do with other addictive drugs. People may persist in abusing steroids despite physical problems and negative effects on social relationships, reflecting these drugs’ addictive potential. Also, steroid abusers typically spend large amounts of time and money obtaining the drug; another indication of addiction. Individuals who abuse steroids can experience withdrawal symptoms when they stop taking them, including mood swings, fatigue, restlessness, loss of appetite, insomnia, reduced sex drive, and steroid cravings, all of which may contribute to continued abuse. One of the most dangerous withdrawal symptoms is depression. When depression is persistent, it can sometimes lead to suicidal thoughts. Research has found that some steroid abusers turn to other drugs such as opioid to counteract the negative effects of steroids."[103]
Causes and treatment
Male anabolic-androgenic steroid abusers often have a troubled social background.[104]
Childhood trauma
25% of male weightlifters reported memories of childhood physical or sexual abuse in an interview. Anabolic steroids are sometimes used by people with muscle dysmorphia (a very specific type of body dysmorphic disorder (BDD)) as a defense mechanism.[105] Interestingly, yohimbine, while it was originally considered a flop of a supplement, because it did not increase testosterone levels as first suspected, have at higher doses been discovered to be useful to facilitate recall of traumatic memories in the treatment of post traumatic stress disorder (PTSD).[106] Also, Tabernanthe iboga and ibogaine have been used to treat PTSD and/or addiction to anabolic steroids.
Illicit use by groups
Criminals
Anabolic steroid use has been associated with an antisocial lifestyle involving various types of criminality.[107]
Governments
Law enforcement
Steroid abuse among law enforcement is considered a problem by some. "It's a big problem, and from the number of cases, it's something we shouldn't ignore. It's not that we set out to target cops, but when we're in the middle of an active investigation into steroids, there have been quite a few cases that have led back to police officers," says Lawrence Payne, a spokesman for the United States Drug Enforcement Administration.[108] The FBI Law Enforcement Bulletin stated that “Anabolic steroid abuse by police officers is a serious problem that merits greater awareness by departments across the country".[109] It is also believed that police officers across the United Kingdom "are using criminals to buy steroids and abuse their power for sexual gratification" which he claims to be a top risk factor for police corruption.[110]
Sports
Professional wrestling
Main article: WWE § Wellness Program
Following the murder-suicide of Chris Benoit in 2007, the Oversight and Government Reform Committee investigated steroid usage in the wrestling industry.[111] The Committee investigated WWE and Total Nonstop Action Wrestling (TNA), asking for documentation of their companies' drug policies. WWE CEO and Chairman, Linda and Vince McMahon respectively, both testified. The documents stated that 75 wrestlers—roughly 40 percent—had tested positive for drug use since 2006, most commonly for steroids.[112][113]
Tragedies involving AAS abuse
Chris Benoit double-murder and suicide
Main article: Chris Benoit double-murder and suicide
Chris Benoit committed suicide after he killed his wife Nancy Benoit and strangled their seven-year-old son Daniel, led to numerous media accounts, and federal investigation into steroid abuse in professional wrestling.
David Jacobs
Main article: David Jacobs (steroid dealer)
On June 5, 2008, police discovered Jacobs, along with his "on-again, off-again" girlfriend,[114] prominent fitness model Amanda Earhart-Savell, both dead of multiple gunshot wounds from a .40 caliber Glock handgun.[115] Police shortly thereafter began characterizing their investigation as consistent with a murder-suicide. Police had been alerted to possible foul play after friends of Savell had reported she had been missing for several days, and officers were sent to check on their welfare at Jacobs' house located in Plano, Texas.[116] Also found in Jacobs's house were "146 vials of steroids, 10 syringes, scales, bags with steroids and marijuana, a computer, and a .22 semi-automatic gun with ammunition."[117]
Legal and sport restrictions
See also: Legality of anabolic steroids
Legal status
Various compounds with anabolic and androgenic effects, their relation with anabolic steroids
The legal status of anabolic steroids varies from country to country: some have stricter controls on their use or prescription than others though in many countries they are not illegal. In the U.S., anabolic steroids are currently listed as Schedule III controlled substances under the Controlled Substances Act, which makes simply possessing of such substances without a prescription, first offense, a federal crime punishable by up to one year in prison. Unlawful distribution or possession with intent to distribute anabolic steroids punishable as a first offense is punished by up to ten years in prison.[118] In Canada, anabolic steroids and their derivatives are part of the Controlled drugs and substances act and are Schedule IV substances, meaning that it is illegal to obtain or sell them without a prescription; however, possession is not punishable, a consequence reserved for schedule I, II, or III substances. Those guilty of buying or selling anabolic steroids in Canada can be imprisoned for up to 18 months.[119] Import and export also carry similar penalties. In Canada, researchers have concluded that steroid use among student athletes is extremely widespread. A study conducted in 1993 by the Canadian Centre for Drug-Free Sport found that nearly 83,000 Canadians between the ages of 11 and 18 use steroids.[120] Anabolic steroids are also illegal without prescription in Australia,[121] Argentina, Brazil and Portugal,[122] and are listed as Class C Controlled Drugs in the United Kingdom. Anabolic steroids are readily available without a prescription in some countries such as Mexico and Thailand.
United States
Steroid pills intercepted by the US Drug Enforcement Administration during the "Operation raw deal" bust in September 2007.
The history of the U.S. legislation on anabolic steroids goes back to the late 1980s, when the U.S. Congress considered placing anabolic steroids under the Controlled Substances Act following the controversy over Ben Johnson's victory at the 1988 Summer Olympics in Seoul. During deliberations, the American Medical Association (AMA), Drug Enforcement Administration (DEA), Food and Drug Administration (FDA) as well as the National Institute on Drug Abuse (NIDA) all opposed listing anabolic steroids as controlled substances,[citation needed] citing the fact that use of these hormones does not lead to the physical or psychological dependence required for such scheduling under the Controlled Substance Act. Nevertheless, anabolic steroids were added to Schedule III of the Controlled Substances Act in the Anabolic Steroids Control Act of 1990.[123]
The same act also introduced more stringent controls with higher criminal penalties for offenses involving the illegal distribution of anabolic steroids and human growth hormone. By the early 1990s, after anabolic steroids were scheduled in the U.S., several pharmaceutical companies stopped manufacturing or marketing the products in the U.S., including Ciba, Searle, Syntex, and others. In the Controlled Substances Act, anabolic steroids are defined to be any drug or hormonal substance chemically and pharmacologically related to testosterone (other than estrogens, progestins, and corticosteroids) that promote muscle growth. The act was amended by the Anabolic Steroid Control Act of 2004, which added prohormones to the list of controlled substances, with effect from January 20, 2005.[124]
United Kingdom
In the United Kingdom, anabolic steroids are classified as class C drugs for their illegal abuse potential, which puts them in the same class as benzodiazepines. Anabolic steroids are in Schedule 4, which is divided in 2 parts; Part 1 contains most of the benzodiazepines and Part 2 contains the anabolic and androgenic steroids.
Part 1 drugs are subject to full import and export controls with possession being an offence without an appropriate prescription. There is no restriction on the possession when it is part of a medicinal product. Part 2 drugs require a Home Office licence for importation and export unless the substance is in the form of a medicinal product and is for self-administration by a person.[125]
Status in sports
See also: Use of performance-enhancing drugs in sport
Legal status of anabolic steroids and other compounds with anabolic effects in Western countries
Anabolic steroids are banned by all major sports bodies including Association of Tennis Professionals, Major League Baseball, Fédération Internationale de Football Association[126] the Olympics,[127] the National Basketball Association,[128] the National Hockey League,[129] and the National Football League.[130] The World Anti-Doping Agency (WADA) maintains the list of performance-enhancing substances used by many major sports bodies and includes all anabolic agents, which includes all anabolic steroids and precursors as well as all hormones and related substances.[131][132] Spain has passed an anti-doping law creating a national anti-doping agency.[133] Italy passed a law in 2000 where penalties range up to three years in prison if an athlete has tested positive for banned substances.[134] In 2006, Russian President Vladimir Putin signed into law ratification of the International Convention Against Doping in Sport which would encourage cooperation with WADA. Many other countries have similar legislation prohibiting anabolic steroids in sports including Denmark,[135] France,[136] the Netherlands[137] and Sweden.[138]
Detection of use
The most commonly employed human physiological specimen for detecting anabolic steroid usage is urine, although both blood and hair have been investigated for this purpose. The anabolic steroids, whether of endogenous or exogenous origin, are subject to extensive hepatic biotransformation by a variety of enzymatic pathways. The primary urinary metabolites may be detectable for up to 30 days after the last use, depending on the specific agent, dose and route of administration. A number of the drugs have common metabolic pathways, and their excretion profiles may overlap those of the endogenous steroids, making interpretation of testing results a very significant challenge to the analytical chemist. Methods for detection of the substances or their excretion products in urine specimens usually involve gas chromatography–mass spectrometry or liquid chromatography-mass spectrometry.[139][140][141][142]
Illegal trade
Main article: Illegal trade in anabolic steroids
Several large buckets containing tens of thousands of anabolic steroid vials confiscated by the DEA during "Operation Raw Deal" in 2007.
Anabolic steroids are frequently produced in pharmaceutical laboratories, but, in nations where stricter laws are present, they are also produced in small home-made underground laboratories, usually from raw substances imported from abroad.[143] In these countries, the majority of steroids are obtained illegally through black market trade.[144][145] These steroids are usually manufactured in other countries, and therefore must be smuggled across international borders. As with most significant smuggling operations, organized crime is involved.[146]
In the late 2000s, the worldwide trade in illicit AAS increased significantly, and authorities announced record captures on three continents. In 2006, Finnish authorities announced a record seizure of 11.8 million AAS tablets. A year later, the DEA seized 11.4 million units of AAS in the largest U.S seizure ever. In the first three months of 2008, Australian customs reported a record 300 seizures of AAS shipments.[147]
In the U.S., Canada, and Europe, illegal steroids are sometimes purchased just as any other illegal drug, through dealers who are able to obtain the drugs from a number of sources. Illegal anabolic steroids are sometimes sold at gyms and competitions, and through the mail, but may also be obtained through pharmacists, veterinarians, and physicians.[148] In addition, a significant number of counterfeit products are sold as anabolic steroids, in particular via mail order from websites posing as overseas pharmacies. In the U.S., black-market importation continues from Mexico, Thailand, and other countries where steroids are more easily available, as they are legal.[149]
History
Isolation of gonadal AAS
The use of gonadal steroids pre-dates their identification and isolation. Medical use of testicle extract began in the late 19th century while its effects on strength were still being studied.[20] The isolation of gonadal steroids can be traced back to 1931, when Adolf Butenandt, a chemist in Marburg, purified 15 milligrams of the male hormone androstenone from tens of thousands of litres of urine. This steroid was subsequently synthesized in 1934 by Leopold Ruzicka, a chemist in Zurich.[150]
In the 1930s, it was already known that the testes contain a more powerful androgen than androstenone, and three groups of scientists, funded by competing pharmaceutical companies in the Netherlands, Germany, and Switzerland, raced to isolate it.[150][151] This hormone was first identified by Karoly Gyula David, E. Dingemanse, J. Freud and Ernst Laqueur in a May 1935 paper "On Crystalline Male Hormone from Testicles (Testosterone)."[152] They named the hormone testosterone, from the stems of testicle and sterol, and the suffix of ketone. The chemical synthesis of testosterone was achieved in August that year, when Butenandt and G. Hanisch published a paper describing "A Method for Preparing Testosterone from Cholesterol."[153] Only a week later, the third group, Ruzicka and A. Wettstein, announced a patent application in a paper "On the Artificial Preparation of the Testicular Hormone Testosterone (Androsten-3-one-17-ol)."[154] Ruzicka and Butenandt were offered the 1939 Nobel Prize in Chemistry for their work, but the Nazi government forced Butenandt to decline the honor, although he accepted the prize after the end of World War II.[150][151]
Clinical trials on humans, involving either oral doses of methyltestosterone or injections of testosterone propionate, began as early as 1937.[150] Testosterone propionate is mentioned in a letter to the editor of Strength and Health magazine in 1938; this is the earliest known reference to an anabolic steroid in a U.S. weightlifting or bodybuilding magazine.[150] There are often reported rumors that German soldiers were administered anabolic steroids during the Second World War, the aim being to increase their aggression and stamina, but these are, as yet, unproven.[155] Adolf Hitler himself, according to his physician, was injected with testosterone derivatives to treat various ailments.[156] AAS were used in experiments conducted by the Nazis on concentration camp inmates,[156] and later by the allies attempting to treat the malnourished victims that survived Nazi camps.[155] President John F. Kennedy was administered steroids both before and during his presidency.[157]
Development of synthetic AAS
The development of muscle-building properties of testosterone was pursued in the 1940s, in the Soviet Union and in Eastern Bloc countries such as East Germany, where steroid programs were used to enhance the performance of Olympic and other amateur weight lifters. In response to the success of Russian weightlifters, the U.S. Olympic Team physician John Ziegler worked with synthetic chemists to develop an anabolic steroid with reduced androgenic effects.[158] Ziegler's work resulted in the production of methandrostenolone, which Ciba Pharmaceuticals marketed as Dianabol. The new steroid was approved for use in the U.S. by the Food and Drug Administration (FDA) in 1958. It was most commonly administered to burn victims and the elderly. The drug's off-label users were mostly bodybuilders and weight lifters. Although Ziegler prescribed only small doses to athletes, he soon discovered that those having abused Dianabol suffered from enlarged prostates and atrophied testes.[159] AAS were placed on the list of banned substances of the IOC in 1976, and a decade later the committee introduced 'out-of-competition' doping tests because many athletes used AAS in their training period rather than during competition.[5]
Three major ideas governed modifications of testosterone into a multitude of AAS: Alkylation at 17-alpha position with methyl or ethyl group created orally active compounds because it slows the degradation of the drug by the liver; esterification of testosterone and nortestosterone at the 17-beta position allows the substance to be administered parenterally and increases the duration of effectiveness because agents soluble in oily liquids may be present in the body for several months; and alterations of the ring structure were applied for both oral and parenteral agents to seeking to obtain different anabolic to androgenic effect ratios.[5]
See also
| Pharmacy and Pharmacology portal |
- Antiandrogen
- Androgen insensitivity syndrome
- Steroid rosacea
- Steroid use in Bollywood
- Bigger, Stronger, Faster*
- Juiced: Wild Times, Rampant 'Roids, Smash Hits & How Baseball Got Big
- Selective androgen receptor modulator
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Further reading
- Yesalis CE (2000). Anabolic Steroids in Sport and Exercise. Human Kinetics. ISBN 0-88011-786-9.
- Daniels RC (February 1, 2003). The Anabolic Steroid Handbook. RCD Books. p. 80. ISBN 0-9548227-0-6.
- Gallaway S (January 15, 1997). The Steroid Bible (3rd Sprl ed.). Belle Intl. p. 125. ISBN 1-890342-00-9.
- Llewellyn W (January 28, 2007). ANABOLICS 2007 : Anabolic Steroid Reference Manual (6th ed.). Body of Science. p. 988. ISBN 978-0-9679304-6-6.
- Roberts A, Clapp B (January 2006). Anabolic Steroids: Ultimate Research Guide. Anabolic Books, LLC. p. 394. ISBN 1-59975-100-3.
- Tygart TT (December 2009). "Steroids, the Media, and Youth". Prevention Researcher Integrated Research Services, Inc., (SIRS Researcher) 16 (7–9).
- Eisenhauer L (Nov 7, 2005). "Do I Look OK?". St. Louis Post-Dispatch (St. Louis, MO). Retrieved 25 Oct 2010.
External links
- Dmoz Directory of websites on anabolic steroids
- National Institute on Drug Abuse: "NIDA for Teens: Anabolic Steroids".
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UpToDate Contents
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- 1. 運動能力の向上を目的としたアンドロゲンおよびその他のホルモンの使用 use of androgens and other hormones to enhance athletic performance
- 2. 性腺機能低下を呈する男性に対するテストステロン治療 testosterone treatment of male hypogonadism
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- 5. 結腸直腸癌長期生存患者へのアプローチ approach to the long term survivor of colorectal cancer
English Journal
- Aggression Is Associated With Increased Anabolic-Androgenic Steroid Use Contemplation Among Adolescents.
- Sagoe D1, Mentzoni RA1,2, Hanss D1,3, Pallesen S1.
- Substance use & misuse.Subst Use Misuse.2016 Sep 18;51(11):1462-9. doi: 10.1080/10826084.2016.1186696. Epub 2016 Jun 29.
- We investigated the relationship between aggression and anabolic-androgenic steroid (AAS) use intent among adolescents. A nationally representative sample of Norwegian 18-year-olds (N = 1,334, females = 58.7%) took part in a survey in 2013 (response rate = 64.9%). Participants completed the physical
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- Muscle-bone interactions: From experimental models to the clinic? A critical update.
- Laurent MR1, Dubois V2, Claessens F2, Verschueren SM3, Vanderschueren D4, Gielen E5, Jardí F4.
- Molecular and cellular endocrinology.Mol Cell Endocrinol.2016 Sep 5;432:14-36. doi: 10.1016/j.mce.2015.10.017. Epub 2015 Oct 23.
- Bone is a biomechanical tissue shaped by forces from muscles and gravitation. Simultaneous bone and muscle decay and dysfunction (osteosarcopenia or sarco-osteoporosis) is seen in ageing, numerous clinical situations including after stroke or paralysis, in neuromuscular dystrophies, glucocorticoid e
- PMID 26506009
- Inherited antithrombin deficiency and anabolic steroids: a risky combination.
- Choe H1, Elfil M, DeSancho MT.
- Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis.Blood Coagul Fibrinolysis.2016 Sep;27(6):717-9. doi: 10.1097/MBC.0000000000000454.
- A 20-year-old male with asymptomatic inherited type 1 antithrombin deficiency and a family history of thrombosis started injecting himself with testosterone 250 mg intramuscularly twice weekly for 5 weeks. He presented to the hospital with progressive dyspnea on exertion, chest pain and hemoptys
- PMID 26588446
Japanese Journal
- 骨髄不全症候群におけるテロメア制御異常
- 日本医科大学医学会雑誌 11(3), 136-144, 2015
- NAID 130005087586
- 一次性骨髄異形成症候群に合併した原発性肺癌の1手術例
- 日本呼吸器外科学会雑誌 28(4), 451-455, 2014
- NAID 130004495387
- MDSに対する蛋白同化ステロイド (特集 低リスク骨髄異形成症候群(MDS)のマネジメント)
- 血液内科 67(3), 333-336, 2013-09
- NAID 40019830344
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★リンクテーブル★
| リンク元 | 「蛋白同化ステロイド薬」「タンパク質同化ステロイド」「タンパク質同化ステロイド薬」「蛋白同化ステロイド」 |
| 拡張検索 | 「anabolic steroids」 |
| 関連記事 | 「anabolic」 |
「蛋白同化ステロイド薬」
「タンパク質同化ステロイド」
「タンパク質同化ステロイド薬」
「蛋白同化ステロイド」
- 英
- anabolic steroid
- 関
「anabolic steroids」
「anabolic」
- adj.
- 同化の、蛋白同化の、タンパク同化の、アナボリック、タンパク同化性の、蛋白同化性の