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Anabolic Steroid - Testosterone Propionate
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. 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. Testosterone is the primary androgen found in the body. Endogenous testosterone is synthesized by cells in the testis, ovary, and adrenal cortex.
Therapeutically, testosterone is used in the management of hypogonadism, either congenital or acquired. Testosterone is also the most effective exogenous androgen for the palliative treatment of carcinoma of the breast in postmenopausal women.
Testosterone was in use in and approved by the FDA in Anabolic steroids, derivatives of testosterone, have been used illicitly and are now controlled substances.
Testosterone, like many anabolic steroids, was classified as a controlled substance in Testosterone is administered parenterally in regular and delayed-release depot dosage forms. In September , 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 ; the system is a mucoadhesive product that adheres to the buccal mucosa and provides a controlled and sustained release of testosterone.
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 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. An ester is any of a class of organic compounds that react with water to produce alcohols and organic or inorganic acids.
Most esters are derived from carboxylic acids, and injectable testosterone is typically administered along with one or multiple esters. The inverse is true of short carbon chains, like the propionate ester, which acts rapidly upon the body and evacuates the body at a similar rate. With a three-carbon chain, the testosterone ester possesses the shortest half life of all testosterone esters at 4 days.
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 administered intramuscularly IM ; via subcutaneous injection; to the skin as a topical gel, solution, ointment or transdermal systems for transdermal absorption; by implantation of long-acting pellets, or; via buccal systems.
In serum, testosterone is bound to protein. It has a high affinity for sex hormone binding globulin SHBG and a low affinity for albumin. The albumin-bound portion freely dissociates. The affinity for SHBG changes throughout life. It is high during prepuberty, declines during adolescence and adult life, then rises again in old age. Elimination half-life is 10— minutes and is dependent on the amount of free testosterone in the plasma.
Testosterone is metabolized primarily in the liver to various keto steroids. Testosterone activity appears to depend on formation of DHT, which binds to cytosol receptor proteins. Further metabolism of DHT takes place in reproductive tissues. There is considerable variation in the half-life of testosterone as reported in the literature, ranging from 10 to minutes. Testosterone is a substrate for CYP3A4 and is also both transported by and an inhibitor of P-glycoprotein P-gp transport.
Parenteral testosterone formulations have been developed that reduce the rate of testosterone secretion, with esters being less polar and slowly absorbed from intramuscular sites. Esters have a duration of action of 2—4 weeks following IM administration.
The esters are hydrolyzed to free testosterone, which is inactivated in the liver. The duration of action of testosterone subcutaneous implantable pellets Testopel is usually 3—4 months, but may last as long as 6 months. Testosterone Propionate injections are primarily used I men who do not make enough testosterone naturally hypogonadism , as well as in specific adolescent cases to induce puberty in those with delayed puberty.
Who should not take this medication? Children should not use testosterone unless directed otherwise by a physician. Your health care provider needs to know if you have any of these conditions: Your healthcare provider will need to have regular bloodwork drawn while on testosterone.
This medication is banned from use in athletes by most athletic organizations. The manufacturers of AndroGel and Striant state that their products are contraindicated in patients with soybean, soy, or soya lecithin hypersensitivity because they are derived partially from soy plants.
Topical gels and solutions are typically flammable, therefore exposure to fire, flame, and tobacco smoking should be avoided while using any topical gel or solution formulation of testosterone.
Testosterone undecanoate Aveed oil for injection contains benzyl benzoate, the ester of benzyl alcohol and benzoic acid, and refined castor oil. Therefore, testosterone undecanoate use is contraindicated in patients with polyoxyethylated castor oil hypersensitivity, benzoic acid hypersensitivity, or benzyl alcohol hypersensitivity. Because some testosterone transdermal systems e. Metal components contained in the backing of some transdermal systems can overheat during an MRI scan and cause skin burns in the area where the patch is adhered.
Testosterone injections are administered intramuscularly. Do not inject via intravenous administration. Respiratory adverse events have been reported immediately after intramuscular administration of testosterone enanthate and testosterone undecanoate. Care should be taken to ensure slow and deep gluteal muscle injection of testosterone. Testosterone can stimulate the growth of cancerous tissue and is contraindicated in male patients with prostate cancer or breast cancer.
Patients with prostatic hypertrophy should be treated with caution because androgen therapy may cause a worsening of the signs and symptoms of benign prostatic hypertrophy and may increase the risk for development of malignancy.
Elderly patients and other patients with clinical or demographic characteristics that are recognized to be associated with an increased risk of prostate cancer should be evaluated for the presence of prostate cancer prior to initiation of testosterone replacement therapy. In patients receiving testosterone therapy, surveillance for prostate cancer should be consistent with current practices for eugonadal men.
Testosterone replacement is not indicated in geriatric patients who have age-related hypogonadism only or andropause because there is insufficient safety and efficacy information to support such use. The Beers expert panel considers use for moderate to severe hypogonadism to be acceptable.
Because of reduced drug clearance and an increased risk of drug accumulation, patients with hepatic disease or hepatic dysfunction should be prescribed testosterone with caution. In addition, edema secondary to water and sodium retention may occur during treatment with androgens. Use testosterone with caution in patients with hepatic disease; renal disease, including nephritis and nephrosis; preexisting edema; or cardiac disease, including heart failure, coronary artery disease, and myocardial infarction MI , as fluid retention may aggravate these conditions.
Further, the possible association between testosterone use and the increased risk of severe cardiovascular events, irrespective of pre-existing cardiac disease, is currently under investigation. An observational study in the U. Veteran Affairs health system included adult male patients of an average age of 60 years.
Within the larger cohort, testosterone therapy was initiated in males after a median of days following coronary angiography; males did not receive testosterone therapy. Three years after coronary angiography, The incidence rate of MI occurring within 90 days following the initial testosterone prescription was compared to the incidence rate of MI occurring in the one year leading-up to the first prescription. Among older males, a 2-fold increase in the risk of MI was observed within the 90 day window; among younger males with a pre-existing history of cardiac disease, a 2- to 3-fold increased risk of MI was observed.
In contrast, no increased risk was observed in younger males without a history of cardiac disease. However, health care professionals are urged to carefully consider whether the benefits of treatment are likely to exceed the potential risks. The FDA will communicate their final conclusions and recommendations when the evaluation is complete. The treatment of hypogonadal men with testosterone esters may potentiate sleep apnea, especially in patients that have risk factors for apnea such as obesity or chronic pulmonary disease.
Patients receiving high doses of testosterone are at risk for polycythemia. Periodically, patients receiving testosterone should have their hemoglobin and hematocrit concentrations measured to detect polycythemia. Testosterone is contraindicated during pregnancy because of probable adverse effects on the fetus FDA pregnancy risk category X. Women of childbearing potential who are receiving testosterone treatments should utilize adequate contraception.
Because testosterone is not used during pregnancy, there should be no particular reason to administer the products to women during labor or obstetric delivery; safety and efficacy in these settings have not been established.
Testim testosterone gel is specifically contraindicated in females; the drug is for males only; the dosage form supplies testosterone in excess of what should be prescribed to females under certain endocrine situations. At high doses, virilization is common and is not prevented by concomitant use of estrogens. Some virilization may be judged to be acceptable during treatment for breast carcinoma; however, if mild virilism is evident, discontinuation of drug therapy is necessary to prevent long term virilization.
When clothing covered the treated site on the male, the transfer of testosterone to the female was avoided. Accidental exposure to topical testosterone gel has also occurred in pediatric patients after contact between the child and the application site in treated individuals.