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. 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 ofchildhood growth disorders that are characterized by in sufficient 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 adole scence. 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 eficiency.

Somatropin is also sometimes prescribed to healthy men and women who are aging. Growth hormone levels tend todecline 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 effectson muscle mass, strength, energy, cell regeneration, and fatloss, there are many supporters of this use, even if hGH maynot specifically retard the aging process. 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 accordingto Federal law to prescribe growth hormone for any off-labeluse, 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 bio availability (75% vs. 63%).The rate of drug metabolism following both routes was alsovery 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 hoursfollowing injection, with the slower times seen within tramuscular 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.

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 growth promoting effects on all organs of the body excluding theeyes and brain. Somatropin has a diabetogenic effect on carbohydrate metabolism, which means that it causes bloodsugar levels to rise (a process normally associated with diabetes). Excessive administration of somatropin over timemay induce a state of type-2 (insulin resistant) diabetes. This hormone also supports triglyceride hydrolysis in adipose tissue, and may reduce body fat stores. Coin ciding 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 are duction in thyroid-supported metabolism, and can interfere with the effectiveness of extended therapy with somatropin.

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’sactivity. IGF-1, however, also has effects that are strongly antagonistic to growth hormone. This includes increased lipogenesis (fat retention), increased glucose consumption and decreased gluconeo genesis. The synergistic and antagonists effects of these two hormones combine to form the character of HGH. Like wise, they also dictate the effects of somatropin administration, which include the support lipolysis, increased serum glucose levels, and reduced insulin sensitivity.

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 anti catabolic 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. Today, recombinant human growth hormone is much more afford able 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.

History:

The first human growth hormone preparations to be used inmedicine were made from pituitary extracts of human origin.These are now commonly referred to as cadaver growthhormone preparations. Approximately 1 mg of hGH (a 1 daydose) could be obtained from each cadaver. The firstsuccessful treatment with human cadaver GH was reported in1958.718 Soon after these medicines were introduced tomarket, and were sold in the U.S. until 1985. The Food andDrug Administration banned them that year after they hadbeen linked to the development of Creutzfeldt-Jakob’sdisease (CJD), a highly degenerative and ultimately fatalbrain disorder, in a number of patients. The disease can betransmitted from one person to another under exceptionalcircumstances (usually blood transfusion or organimplantation are involved), and was likely caused by theextraction of hGH from infected cadavers. CJD has a veryslow incubation period, and has been diagnosed anywherefrom 4 to 30 years after therapy with growth hormone ofcadaver origin. As of 2004 estimates, at least 26 patients thatreceived cadaver GH drugs in the United States have beendiagnosed with the disease.719 The overall incidence of thisdisease is less than 1%, as approximately 6,000 patients aredocumented to have received the medication.

The FDA approved the first synthetic human growth hormonedrug in 1985. Synthesis produced a pure hormone withoutbiological contamination, eliminating the possibility of CJDtransmission. The drug approved was called somatrem(Protropin), and was based on a manufacturing technologydeveloped by Genentech in 1979.720 Somatrem came at animportant time given the removal of cadaver GH by the FDAthat same year. This hormone is actually a slight variant ofthe hGH protein, but displays the same biological propertiesof the natural hormone. Protropin was initially verysuccessful being it was the first synthetic GH product. By1987, however, Kabi Vitrum (Sweden) had publishedmethods for the production of pure synthetic somatropin withthe exact amino acid sequence of endogenous growthhormone.721 It was also discovered that the unnaturalstructure of somatrem causes a much higher incidence ofantibody reactions in patients, which can reduce drugefficacy.722 Somatropin would come to be viewed as a morereliable drug, and would dominate the global market withinseveral years. Today, although somatrem products are stillsold, somatropin retains the vast majority of hGH salesworldwide.

How Supplied:

Somatropin is most commonly supplied in multi-dose vials containing a white lyophilized powder that requires re constitution 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 recon stituted somatropin.

Structural Characteristics:

Somatropin is human growth hormone protein manufactured by recombinant DNA technology. It has 191 amino acid residues and a molecular weight of 22,125 dal tons. It is identical in structure to human growth hormone of pituitary origin.

Storage:

Do not freeze. Follow package insert for storage information. Refrigeration (2º to 8ºC, 35º to 46º F) may be required before and after reconstitution.

Side Effects (General):

The most common adverse reactions to somatropin therapy are joint pain, headache, flu-like symptoms, peripheraledema (water retention), and back pain. Less common adverse reactions include inflammation of mucousmembranes in the nose (rhinitis), dizziness, upper respiratory infection, bronchitis, tingling or numbness on the skin, reduced sensitivity to touch, general edema, nausea, sorebones, carpal tunnel syndrome, chest pain, depression,gynecomastia, hypothyroidism, and insomnia. The abuse of somatropin may cause diabetes, acromegaly (a visible thickening of the bones, most notably the feet, forehead,hands, jaw, and elbows), and enlargement of the internalorgans. Due to the growth promotion effects of human growth hormone, this drug should not be used by individuals with active or recurring cancer.

Side Effects (Impaired glucose tolerance):

Somatropin may reduce sensitivity to insulin and raise blood sugar levels. This may occur in individuals without pre-existing diabetes or impaired glucose tolerance.

Side Effects (Injection site):

The subcutaneous administration of somatropin may cause redness, itching, or lumps at the site of injection. It may also cause a localized decrease of adipose tissue, which may be compounded by the repeated administration at the same site of injection.

Administration:

Somatropin is designed for subcutaneous or intramuscular administration. One milligram of somatropin is equivalent to approximately 3 International Units (3 IU).

When used to treat adult onset growth hormone deficiency, the drug is commonly applied at a dosage of .005/mg/kg per day to.01mg/kg per day. This equates to roughly 1 IU to 3 IU per day for person of approximately 180-220 lbs. A long-term maintenance dosage is established after reviewing the patient’s IGF-1 levels and clinical response over time. When used for physique- or performance-enhancing purposes, somatropin is usually administered at a dosage between 1 IU and 6 IU per day (2-4 IU being most common).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. 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 activity723(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 a cute side effects.