Testosterone was the first successfully synthesized anabolic steroid. Testosterone propionate is a fast-acting, short-ester, oil-based injectable testosterone compound that is commonly prescribed for the treatment of hypogonadism – low testosterone levels and various related symptoms in males.
Testosterone propionate was first described in 1935 to increase synthetic testosterone’s therapeutic usefulness by slowing its release into the bloodstream. It was released for clinical use two years later by Schering AG in Germany, featured in a hybrid blend with testosterone enanthate under the brand name Testoviron. This was also the first commercially available version on the U.S. prescription drug market and remained the dominant form of testosterone globally prior to 1960.
Cells in the adrenal cortex, ovary, and testis produce endogenous testosterone, the most common androgen in the human body. The treatment of either congenital or acquired hypogonadism involves the use of testosterone. The best exogenous androgen for postmenopausal women to use in the palliative management of breast cancer is testosterone. 1938 saw the introduction of testosterone, which the FDA approved in 1939. Anabolic steroids, which are testosterone derivatives, have been used illegally and are now considered restricted substances. In 1991, testosterone was designated as a restricted substance along with numerous anabolic steroids. Both standard and delayed-release (depot) dose versions of testosterone are supplied parenterally. In September 1995, the FDA initially approved testosterone transdermal patches (Androderm); many transdermal forms and brands are now available including implants, gels, and topical solutions. A testosterone buccal system, Striant, was FDA approved in July 2003; the system is a mucoadhesive product that adheres to the buccal mucosa and provides a controlled and sustained release of testosterone. In May 2014, the FDA approved an intranasal gel formulation (Natesto). A transdermal patch (Intrinsa) for hormone replacement in women is under investigation; the daily dosages used in women are much lower than for products used in males. The FDA ruled in late 2004 that it would delay the approval of Intrinsa women's testosterone patch and has required more data regarding safety, especially in relation to cardiovascular and breast health.
The propionate ester is a type of chemical molecule that reacts with water to form alcohols and organic or inorganic acids. The majority of esters are made from carboxylic acids, and one or more esters are frequently supplied along with injectable testosterone. The testosterone molecule has an ester added to it, which affects how soluble it is after it enters the bloodstream. A large/long ester will have a longer half-life; the longer the carbon chain, the longer the ester, and the less soluble the drug. In contrast, short carbon chains, such as the propionate ester, act quickly on the body and expel waste products at a similar rate. The testosterone ester has the shortest half-life of all testosterone esters, at 4 days, thanks to its three-carbon chain.
Endogenous testosterone is responsible for sexual maturation at all stages of development throughout life. Synthetically, it is prepared from cholesterol. The function of androgens in male development begins in the fetus, is crucial during puberty, and continues to play an important role in the adult male. Women also secrete small amounts of testosterone from the ovaries. The secretion of androgens from the adrenal cortex is insufficient to maintain male sexuality.
Increased androgen plasma concentrations suppress gonadotropin-releasing hormone (reducing endogenous testosterone), luteinizing hormone, and follicle-stimulating hormone by a negative-feedback mechanism. Testosterone also affects the formation of erythropoietin, the balance of calcium, and blood glucose. Androgens have a high lipid solubility, enabling them to rapidly enter cells of target tissues. Within the cells, testosterone undergoes enzymatic conversion to 5-alpha-dihydrotestosterone and forms a loosely bound complex with cystolic receptors. Androgen action arises from the initiation of transcription and cellular changes in the nucleus brought about by this steroid-receptor complex.
Normally, endogenous androgens stimulate RNA polymerase, resulting in an increased protein production.These proteins are responsible for normal male sexual development, including the growth and maturation of the prostate, seminal vesicle, penis, and scrotum. During puberty, androgens cause a sudden increase in growth and development of muscle, with redistribution of body fat. Changes also take place in the larynx and vocal cords, deepening the voice. Puberty is completed with beard development and growth of body hair. Fusion of the epiphyses and termination of growth is also governed by the androgens, as is the maintenance of spermatogenesis. When endogenous androgens are unavailable, use of exogenous androgens are necessary for normal male growth and development.
Testosterone is injected into a muscle. The injection is usually given every 2 to 4 weeks.
Testosterone injections should be given only by a healthcare professional. Misuse can lead to serious side effects or death.
The length of treatment will depend on the condition being treated.
Testosterone will not enhance athletic performance and should not be used for that purpose.
While receiving this medicine, you will need frequent blood tests.
Testosterone can affect bone growth in boys who are treated for delayed puberty. Bone development may need to be checked with x-rays every 6 months during treatment.
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