Testosterone E 250

(Testosterone Enanthate 250 mg/mL 10mL Vial)
Pharmacologic Classifications: Hormone Modifiers, Androgens
Dosage strength of Testosterone Enanthate Injection: 250 mg/mL 10 mL vial

General Information: Testosterone was the first ever synthesized anabolic steroid. Testosterone enanthate is a slow-acting, long-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 enanthate first appeared in the U.S. prescription drug market during the early 1950’s, as Delatestryl by Squibb.  It changed hands several times over the years, most notably to Mead Johnson, BTG, Savient, and in December 2005, Indevus.  Testosterone enanthate’s was most prominently featured in a hybrid blend with testosterone propionate under the brand Testoviron, a drug that has seen uninterrupted production by Schering AG of Germany for more than 50 years.

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 1938 and approved by the FDA in 1939. 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 1991. Testosterone is administered parenterally in regular and delayed-release (depot) dosage forms. 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 Enanthate Ester: 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 addition of a carbon chain (ester) attached to the testosterone molecule controls how soluble it will be once inside the bloodstream.  The smaller the carbon chain, the shorter the ester, and the more soluble the medication.  A small/short ester will have a shorter half life – a repeating cycle of a medication’s time and activity within the body.  The inverse is true of long carbon chains, like enanthate, which both act slowly upon the body and evacuates the body at a similar rate. Specifically, testosterone enanthate contains the carboxylic acid ester (enanthoic acid), and a half-life is approximately 8-9 days; the longest half-life of all common ester based testosterones.  An uncommon testosterone such as Nebido (testosterone undecanoate) has a very long 3-month half-life.

Indications: Testosterone Enanthate 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.

Mechanism of Action: 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.

 

Indications: Testosterone Enanthate 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.

Breast-feeding: Testosterone topical solution, transdermal patches, and gels are contraindicated in lactating women who are breast-feeding. It is recommended that other testosterone formulations be avoided during breast-feeding as well.Testosterone distribution into breast milk has not been determined; it is unclear if exposure would increase above levels normally found in human milk. Significant exposure to this androgen via breast-feeding may have adverse androgenic effects on the infant and the drug may also interfere with proper establishment of lactation in the mother. Historically, testosterone/androgens have been used adjunctively for lactation suppression. Alternative methods to breast-feeding are recommended in lactating women receiving testosterone therapy.

Interactions: Possible interactions include: certain medicines for diabetes; certain medicines that treat or prevent blood clots like warfarin; oxyphenbutazone; propranolol; steroid medicines like prednisone or cortisone. This list may not describe all possible interactions.

How is this medication best taken? This medicine is for injection into a muscle. It is usually given by a health care professional in a hospital or clinic setting. Contact your pediatrician regarding the use of this medicine in children. While this medicine may be prescribed for children as young as 12 years of age for selected conditions, precautions do apply. Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

What do I do if I miss a dose? If you are given your dose at a clinic or doctor’s office, call to reschedule your appointment. If you give your own injections and you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

Storage: Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the expiration date. Do not flush unused medications or pour down a sink or drain.

General Statements: Do not share or take any one else’s medicine. Talk with your healthcare provider before starting any new medicine, including over-the-counter, natural products, or vitamins. This medication was compounded specifically for you. This patient information summarizes the most important information about your medication; if you would like more information, talk with your doctor.

Note: Patients using testosterone should seek medical attention immediately if symptoms of a heart attack or stroke are present, such as: chest pain, shortness of breath or trouble breathing, weakness in one part or one side of the body, slurred speech.

Abuse of testosterone, usually at doses higher than those typically prescribed and usually in conjunction with other AAS, is associated with serious safety risks affecting the heart, brain, liver, mental health, and endocrine system.  Reported serious adverse outcomes include heart attack, heart failure, stroke, depression, hostility, aggression, liver toxicity, and male infertility. Individuals abusing high doses of testosterone have also reported withdrawal symptoms, such as depression, fatigue, irritability, loss of appetite, decreased libido, and insomnia.

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