Human Growth Hormone (somatropin)
人類生長激素(生長激素)
Description:
As its name suggests, human growth hormone is an important mediator of the human growth process. This hormone is produced endogenously by the anterior pituitary gland, and exists at especially high levels during childhood. Its growth promoting effects are broad, and can be separated into three distinct areas: bone, skeletal muscle, and internal organs. It also supports protein, carbohydrate, lipid, and mineral metabolism, and can stimulate the growth of connective tissues. Although vital to early development, human growth hormone is produced throughout adulthood. Its levels and biological role decline with age, but continue to support metabolism, muscle tissue growth/maintenance, and the
management (reduction) of adipose tissue throughout life.
描述:
顧名思義，人類生長激素是人類生長過程的重要調節者。這種激素是由腦垂體前葉內 源性產生的，在童年時期的量特別高。其生長促進作用廣泛，可以分為三個不同的領 域:骨骼，骨骼肌和內臟。它還支持蛋白質，碳水化合物，脂質和礦物質代謝，並可 刺激結締組織的生長。雖然對早期發育至關重要，但人類生長激素在整個成年期間仍 可產生。其水平和生物學作用隨年齡而下降，但在一生中繼續支持新陳代謝，肌肉組 織生長/維持脂肪組織的管理(減少)。
Somatropin specifically describes pharmaceutical human growth hormone that was synthesized with the use of recombinant DNA technology. Somatropin (rhGH) is biologically equivalent to human growth hormone (hGH) of pituitary origin. In a medical setting, somatropin is used to help treat a variety of health conditions. It is most notably prescribed in cases of childhood growth disorders that are characterized by insufficient growth hormone production. While usually not fully corrective, somatropin use is often capable of substantially increasing the linear growth rate and overall height before further growth is halted in adolescence.
Somatropin 是特異性地描述了使用重組 DNA 技術合成的人類生長激素藥物。Somatropin(rhGH)是在生物學上，相當於腦垂體來源的人類生長激素(hGH)。在醫療環境中，生長激素用於幫助治療各種健康狀況。在兒童生長障礙的情況下，特 別是對於生長激素生產不足的特徵是最明顯的。雖然通常不能完全糾正，但在青春期 停止進一步生長之前，生長激素的使用通常能夠顯著增加線性生長速率和總體身高。
This medication is also used to accelerate growth in children that were born small and failed to catch up by the age of two. Other uses include the treatment of short bowel syndrome, growth failure due to renal insufficiency, muscle wasting associated with HIV infection, and adult growth hormone deficiency. Somatropin is also sometimes prescribed to healthy men and women who are aging. Growth hormone levels tend to decline as we get older, and many physicians believe that its supplementation to more youthful levels can help slow some of the damage of aging. Given its beneficial metabolic effects on muscle mass, strength, energy, cell regeneration, and fat loss, there are many supporters of this use, even if hGH may not specifically retard the aging process.
這種藥物也用於加速二歲前生長遲緩兒童的生長。其他用途包括治療短腸症候群，由 於腎功能不全引起的生長失敗，與 HIV 感染相關的肌肉消瘦，以及成人的生長激素缺乏。生長激素有時也被用於正在老化的健康男性和女性。隨著年齡的增長，生長激素水平往往會下降，許多醫生認為補充至更年輕的水平，有助於減緩老化的一些損害。鑑於其對肌肉質量，力量，能量，細胞再生和脂肪減少的有益的代謝作用，即使人類生長激素也許不能特異性地推遲衰老過程，這種使用方式仍有許多支持者。
Note that in order to prescribe hGH for adult hormone deficiency in the U.S., the patient must have a diagnosed pituitary disease or history of childhood GH deficiency. It is specifically illegal according to Federal law to prescribe growth hormone for any off- label use, which includes anti-aging and bodybuilding purposes.717 Somatropin may be given by either subcutaneous or intramuscular injection. During clinical studies, the pharmacokinetic properties of somatropin following both methods of use were determined. When given by subcutaneous injection, somatropin has a similar but moderately higher level of bioavailability (75% vs. 63%).
注意，在美國為了開立成人激素缺乏症所需的人類生長激素，患者必須被診斷有垂體 疾病或童年生長激素缺乏症的病史。根據聯邦法律，對於任何藥品仿單標示外用途 (包括抗衰老和健美用途)，開立生長激素特別是違法的.717 Somatropin 可以通過皮 下或肌內注射給予。在臨床研究中，確立了兩種使用方法使用後，somatropin 的藥物 動力學性質。當通過皮下注射給予時，somatropin 具有相似，但略微較高水平的生體 可用率(75%vs. 63%)。
The rate of drug metabolism following both routes was also very similar, with somatropin displaying a half-life of approximately 3.8 hours and 4.9 hours after subcutaneous and intramuscular injection, respectively. Baseline hormone levels are usually reached between 12 hours and 18 hours following injection, with the slower times seen with intramuscular use. Given the delayed rise in IGF-1 levels, however, which can remain elevated 24 hours after hGH injection, the metabolic activity of human growth hormone will outlast its actual levels in the body. Although drug absorption is acceptable by both methods of use, daily subcutaneous administration is generally regarded as the preferred method of using somatropin.
兩種途徑後藥物代謝率也非常相似，somatropin 在皮下和肌肉注射，顯示約 3.8 小時 和 4.9 小時的半衰期。基線激素水平通常在注射後 12 小時至 18 小時之間達到，其中 較慢的時間在肌肉注射見到。然而，鑑於 IGF-1 水平的延遲升高性質，它可以在人類 生長激素注射後 24 小時內保持升高，人類生長激素的代謝活性將超過其在體內的實際 水平。儘管兩種使用方法都可以接受藥物吸收，但是每日皮下給藥通常被認為是使用 somatropin 的首選方法。
A specific analysis of somatropin activity shows a hormone with a diverse set of effects. It is anabolic to skeletal muscle, shown to increase both the size and number of cells (processes referred to as hypertrophy and hyperplasia, respectively). The hormone also seems to have growthpromoting effects on all organs of the body excluding the eyes and brain. Somatropin has a diabetogenic effect on carbohydrate metabolism, which means that it causes blood sugar levels to rise (a process normally associated with diabetes). Excessive administration of somatropin over time may induce a state of type-2 (insulin resistant) diabetes. This hormone also supports triglyceride hydrolysis in adipose tissue, and may reduce body fat stores. Coinciding with this tends to be a reduction in serum cholesterol. The drug also tends to reduce levels of potassium, phosphorous, and sodium, and may cause a decrease in levels of the thyroid hormone triiodothyronine (T3). The latter effect marks a reduction in thyroid-supported metabolism, and can interfere with the effectiveness of extended therapy with somatropin.
一個對 somatropin 活性的特殊分析，顯示一個激素會有多種效應。它對骨骼肌的效果 是合成代謝，顯示增加細胞的大小和數量(分別稱為肥大和增生的過程)。這個激素 也似乎對身體的所有器官具有生長促進作用，除了眼睛和大腦之外。Somatropin 對碳 水化合物代謝具有致糖尿病作用，這意味著它會導致血糖水平升高(通常與糖尿病有 關)。隨著時間的推移，somatropin 的過量給藥可能引起 2 型(胰島素抵抗)糖尿病。這種激素也支持脂肪組織中的三酸甘油酯水解，並可能減少體脂肪的儲存。與此有關， 往往是降低血清膽固醇。該藥物也傾向於降低鉀，磷和鈉的水平，並可能導致甲狀腺 激素 - 三碘甲狀腺原氨酸(T3)水平的降低。而後的效應顯示甲狀腺支持代謝的減少， 並且可能干擾 somatropin 延伸治療的有效性。
Growth hormone has both direct and indirect effects. On the direct side, the hGH protein attaches to receptors in muscle, bone, and adipose tissues, sending messages to support anabolism and lipolysis (fat loss). Growth hormone also directly increases glucose synthesis (gluconeogenesis) in the liver, and induces insulin resistance by blocking its activity in target cells. The indirect effects of growth hormone are largely mediated by IGF-1 (insulin-like growth factor), which is produced in the liver and virtually all other tissues in response to growth hormone. IGF-1 is also anabolic to both muscle and bone, augmenting growth hormone’s activity. IGF-1, however, also has effects that are strongly antagonistic to growth hormone. This includes increased lipogenesis (fat retention), increased glucose consumption, and decreased gluconeogenesis. The synergistic and antagonists effects of these two hormones combine to form the character of hGH. Likewise, they also dictate the effects of somatropin administration, which include the support lipolysis, increased serum glucose levels, and reduced insulin sensitivity. 生長激素具有直接和間接的作用。在直接方面，hGH 蛋白附著於肌肉，骨骼和脂肪組 織中的受體，發送信息以支持合成代謝和脂肪分解(脂肪減少)。生長激素也直接增 加肝臟中的葡萄糖合成(糖質新生)，並通過阻斷其在靶細胞中的活性，來誘導胰島 素抵抗。生長激素的間接作用主要由 IGF-1(胰島素樣生長因子)介導，它在肝臟中 和實質上所有其他對生長激素有反應的組織中產生。IGF-1 也對肌肉和骨骼有合成代謝作用，並增強生長激素的活性。然而，IGF-1 也具有強烈拮抗生長激素的作用。這 包括增加脂肪生成(脂肪保留)，增加葡萄糖消耗和降低的糖質新生。這兩種激素的 協同作用和拮抗作用相結合，形成了 hGH 的特徵。同樣地，它們還決定了 somatropin 給藥的作用，包括支持脂肪分解，增加血清中葡萄糖水平和降低胰島素敏 感性。Somatropin is considered to be a controversial anabolic and performance-enhancing drug in the realm of bodybuilding and athletics. The main issue of debate is the exact level of potential benefit this substance carries. While studies with HIV+ patients in a wasting state tend to support potentially strong anabolic and anticatabolic properties, studies demonstrating these same effects in healthy adults and athletes are lacking. During the 1980s, a large body of myth surrounded discussions of hGH in bodybuilding circles, which may have been fueled by the high cost of the drug and its very name (「growth hormone」). It was once thought to be the most powerful anabolic substance you could buy.Somatropin 被認為是在健身和運動領域中，有爭議的合成代謝和性能增強藥物。爭辯 的主要問題是這種物質所具有的潛在利益的確切水平。雖然對於處於耗損狀態的 HIV 陽性患者的研究，傾向於支持潛在的強力合成代謝和反分解代謝特性，但是在健康成 年人和運動員中，證明具有相同效果的研究則是缺乏的。在 1980 年代，大量的神話包 圍了健身圈中關於 hGH 的討論，這可能是由於藥物的高花費及其名稱(「生長激素」) 所推動的。它曾被認為是您可以買到的最強大的合成代謝物質。Today, recombinant human growth hormone is much more affordable and readily obtained. Most experienced individuals now tend to agree that it is the fat-loss- promoting properties of somatropin that are most obvious. The drug can support muscle growth, strength gains, and increased athletic performance, but its effects are generally milder than those of anabolic/androgenic steroids. For a highly advanced athlete or bodybuilder, however, somatropin can help push body and performance further than might have been possible with steroids alone. 今天，重組人類生長激素更容易負擔得起並且容易獲得。大多數有經驗的人現在傾向 於同意，somatropin 的促脂肪流失性質是最明顯的。該藥物可以支持肌肉生長，強度 增加和運動表現增加，但其作用通常比合成代謝/雄激素類固醇更溫和。然而，對於高 度進階的運動員或健美運動員，somatropin 可以有助於推進身體和性能，比單獨使用 類固醇可能更有可能。History:The first human growth hormone preparations to be used in medicine were made from pituitary extracts of human origin. These are now commonly referred to as cadaver growth hormone preparations. Approximately 1 mg of hGH (a 1 day dose) could be obtained from each cadaver. The first successful treatment with human cadaver GH was reported in 1958.718 Soon after these medicines were introduced to market, and were sold in the U.S. until 1985. The Food and Drug Administration banned them that year after they had been linked to the development of Creutzfeldt-Jakob’s disease (CJD), a highly degenerative and ultimately fatal brain disorder, in a number of patients. The disease can be transmitted from one person to another under exceptional circumstances (usually blood transfusion or organ implantation are involved), and was likely caused by the extraction of hGH from infected cadavers. CJD has a very slow incubation period, and has been diagnosed anywhere from 4 to 30 years after therapy with growth hormone of cadaver origin. As of 2004 estimates, at least 26 patients that received cadaver GH drugs in the United States have been diagnosed with the disease.719 歷史:用於醫學上的第一種人類生長激素製劑是由人類垂體提取物製成的。這些現在通常被 稱為屍體生長激素製劑。每具屍體可以獲得約 1 毫克的 hGH(1 天劑量)。在 1958 年 首度報導了人類屍體生長激素的首例成功治療.718。這些藥物不久之後進入市場，在 美國銷售直到 1985 年。食品和藥物管理局在人類屍體生長激素被連結至 Creutzfeldt- Jakob 病(CJD)的進展有關後，來年禁止了它們，這是在一些病人當中，一種高度 退行性和最終致命的腦部疾患。這種疾病在特殊情況下(通常是輸血或器官移植)可 以從一個人傳播到另一個人，並且可能是由從感染的屍體中提取 hGH 造成的。CJD 的潛伏期非常緩慢，在屍體來源的生長激素治療後 4〜30 年被診斷。截至 2004 年的估 計，至少有 26 例在美國接受屍體生長激素藥物的患者，已被診斷患有這種疾病。The overall incidence of this disease is less than 1%, as approximately 6,000 patients are documented to have received the medication. The FDA approved the first synthetic human growth hormone drug in 1985. Synthesis produced a pure hormone without biological contamination, eliminating the possibility of CJD transmission. The drug approved was called somatrem (Protropin), and was based on a manufacturing technology developed by Genentech in 1979.720 Somatrem came at an important time given the removal of cadaver GH by the FDA that same year. This hormone is actually a slight variant of the hGH protein, but displays the same biological properties of the natural hormone.這種疾病的整體發病率低於 1%，大約 6000 名患者被記錄曾接受這個藥物治療。食品 和藥物管理局於 1985 年批准了第一種合成的人類生長激素藥物。人工合成產了沒有生 物汙染的純激素，消除了 CJD 傳播的可能性。該藥物被稱為 somatrem(Protropin)， 是基於 Genentech 公司於 1979 年開發的製造技術。722 Somatrem 在一個重要的時間 點到來，就是食品和藥物管理局下架屍體生長激素的同一年。這種激素實際上是 hGH 蛋白的一個輕微變體，但顯示出與天然激素相同的生物學特性。Protropin was initially very successful being it was the first synthetic GH product. By 1987, however, Kabi Vitrum (Sweden) had published methods for the production of pure synthetic somatropin with the exact amino acid sequence of endogenous growth hormone.721 It was also discovered that the unnatural structure of somatrem causes a much higher incidence of antibody reactions in patients, which can reduce drug efficacy.722 Somatropin would come to be viewed as a more reliable drug, and would dominate the global market within several years. Today, although somatrem products are still sold, somatropin retains the vast majority of hGH sales worldwide. Protropin 最初是非常成功的，因為它是第一個合成的生長激素產品。然而，到 1987 年，Kabi Vitrum(瑞典)公司發表了生產純粹合成生長激素的方法，其具有內生性生 長激素精確的胺基酸序列。7221 還發現 somatrem 的非天然結構，在患者體內導致抗體反應發生率高得多，降低 了藥物的療效.722 Somatropin 被認為是更可靠的藥物，並且在幾年內主宰全球市場。今天，儘管 somatrem 產品仍然在銷售，但 Somatropin 仍然佔有了全世界絕大多數 hGH 銷售市場。How Supplied:Somatropin is most commonly supplied in multi-dose vials containing a white lyophilized powder that requires reconstitution with sterile or bacteriostatic water before use. Dosage may vary widely from 1mg to 24mg or more per vial. Somatropin is also available as a stabile pre-mixed solution (Nutropin AQ) that is biologically equivalent to reconstituted somatropin. 如何提供:
施用:
Somatropin 被設計用於皮下或肌內給藥。一毫克生長激素相當於約 3 個國際單位 (3IU)。當用於治療成人發病的生長激素缺乏症時，該藥物通常以每天 0.005 毫克/公 斤至 0.01 毫克/公斤的劑量施用。對體重約 180-220 磅的人來說，粗估大約每天 1 IU 至
3 IU。在回顧患者的 IGF-1 水平和隨著時間的臨床反應之後，長期維持劑量被建立了。當用於體格或表現增強的目的時，生長激素通常以每天 1 IU 至 6 IU 的劑量施用(2-4
IU 是最常見的)。
The drug is commonly cycled in a similar manner to anabolic/androgenic steroids, with the length of intake generally being between 6 weeks and 24 weeks. The anabolic effects of this drug are less apparent than its lipolytic (fat loss) properties, and generally take longer periods of time and higher doses to manifest themselves. Other drugs are commonly used in conjunction with somatropin in order to elicit a stronger response. Thyroid drugs (usually T3) are particularly common given the known effects of somatropin on thyroid levels, and may significantly enhance fat loss during therapy. Insulin is also commonly used with somatropin.
該藥物通常以與合成代謝/雄激素類固醇類似的方式循環，其使用的時間長度通常在 6 周至 24 周之間。這種藥物的合成代謝作用，比起其脂肪分解(脂肪減少)性質來的較 不明顯，通常需要更長的時間和更高的劑量來彰顯它的效果。其他藥物通常與 somatropin 聯合使用，以引起更強烈的反應。鑑於 somatropin 對甲狀腺水平的已知作 用，甲狀腺藥物(通常為 T3)是特別常見會給予的，並且可能顯著增強治療期間的脂 肪減少。胰島素也常與 somatropin 並用。
Aside from countering some of the effects somatropin has on glucose tolerance, insulin can increase receptor sensitivity to IGF-1, and reduce levels of IGF binding protein-1, allowing for more IGF-1 activity 723 (growth hormone itself also lowers IGF binding protein levels).724 Anabolic/androgenic steroids are also commonly taken with somatropin, in an effort to maximize potential muscle-building effects. Anabolic steroids may also further increase free IGF-1 levels via a lowering of IGF binding proteins.725 Note that the stacking of somatropin with thyroid drugs and/or insulin is usually approached with great care and caution, given that these are particularly strong medications with potentially serious or life threatening acute side effects.
除了 somatropin 對葡萄糖耐受性的一些反面作用外，胰島素可增加對 IGF-1 的受體敏 感性，並降低 IGF 結合蛋白-1 的水平，從而允許更多的 IGF-1 活性 723(生長激素本 身也會降低 IGF 結合蛋白的水平).724 合成代謝/雄激素類固醇通常與生長激素一起使 用，以努力去最大化潛在的肌肉建構效應。合成代謝類固醇還可以通過降低 IGF 結合
X.Talent 科技團隊。vx 1328892949
蛋白，進一步增加游離 IGF-1 的水平.72 注意，生長激素與甲狀腺藥物和/或胰島素的 堆棧，通常要非常小心和謹慎地處理，因為這些是特別強力的藥物，有著潛在的嚴重 或危及生命的急性副作用。
Availability:
Somatropin is produced by many different drug companies, and is distributed in virtually all developed countries. The most common brand names include Serostim (Serono),
Saizen (Serono), Humatrope (Eli Lilly), Norditropin (novo nodisk), Omnitrope (Sandoz), and Genotropin (Pharmacia).
可得性:
Somatropin 由許多不同的藥物公司生產，分布在幾乎所有的開發中國家。最常見的品 牌包括 Serostim(Serono)，Saizen(Serono)，Humatrope(禮來)，Norditropin (Novo nodisk)，Omnitrope(Sandoz)和 Genotropin(Pharmacia)等。
Somatropin products are high value targets for drug counterfeiting operations. Many counterfeits are highly deceptive in nature, and have been found in both illicit and legitimate drug distribution channels. Some counterfeit growth hormone products are made by relabeling vials of hCG, which bear a very close visual resemblance to somatropin. A home pregnancy test is sometimes used to help determine if hCG has been used to make a counterfeit hGH product. This test works by detecting hCG in the urine.
Somatropin 產品是藥物假冒作業的高價值目標。許多假冒質量實上是高度欺騙性質的， 並且在非法和非法合法藥物分銷渠道都有被發現。一些假冒生長激素的產品，通過重 新標記 hCG(人類絨毛膜性腺激素)小瓶製成，hCG 與 somatropin 具有非常接近的 外觀相似性。家庭妊娠試驗有時用於幫助確定 hCG 是否已被用於製造假冒的人類生長 激素產品。該試驗通過檢測尿液中的 hCG 起作用。
A few days into a cycle with somatropin, the individual will take a 3-4 IU injection prior to bed. Upon rising, the pregnancy test will be used, and a positive result will indicate that an hCG counterfeit has been used. The powder in the vial of somatropin should also be in the form of a solid (lyophilized) disc. Do not take any product that contains loose powder.
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