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Overview of Testosterone Cypionate Injection

General Information

Testosterone was the first ever synthesized anabolic steroid, and testosterone cypionate 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. Buy 1-Testosterone Cypionate Online In Australia

Testosterone cypionate first appeared on the U.S. prescription drug market during the early 1950’s, as Depo-Testosterone by Upjohn, now Pharmacia & Upjohn. Due to testosterone cypionate’s vast similarity to the earlier released and slightly longer testosterone enanthate, it has received only limited global availability and is often identified as an American medication.

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. Buy 1-Testosterone Cypionate Online In Australia

The Cypionate 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 will have a shorter half life – a repeating cycle of a medication’s time within the body. The inverse is true of long carbon chains, like cypionate, which both act slowly upon the body and evacuates the body at a similar rate. Buy 1-Testosterone Cypionate Online In Australia

 

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.Buy 1-Testosterone Cypionate Online In Australia

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.Buy 1-Testosterone Cypionate Online In Australia

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. Buy 1-Testosterone Cypionate Online In Australia

 

Pharmacokinetics

Testosterone is administered intramuscularly (IM), 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.

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. The active metabolite DHT has a greater affinity for SHBG than testosterone. Elimination half-life is 10—100 minutes and is dependent on the amount of free testosterone in the plasma.

Testosterone is metabolized primarily in the liver to various 17-keto steroids. It is a substrate for hepatic cytochrome P450 (CYP) 3A4 isoenzyme.1 Estradiol and dihydrotestosterone (DHT) are the major active metabolites, and DHT undergoes further metabolism. Testosterone activity appears to depend on formation of DHT, which binds to cytosol receptor proteins. Further metabolism of DHT takes place in reproductive tissues. About 90% of an intramuscular testosterone dose is excreted in the urine as conjugates of glucuronic and sulfuric acids. About 6% is excreted in the feces, largely unconjugated. There is considerable variation in the half-life of testosterone as reported in the literature, ranging from 10 to 100 minutes.2

Affected cytochrome P450 isoenzymes and drug transporters: CYP3A4, P-gp

Testosterone is a substrate for CYP3A4 and is also both transported by and an inhibitor of P-glycoprotein (P-gp) transport.13

Route-Specific Pharmacokinetics:

Intramuscular Route: 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.

Contraindications/Precautions

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: breast cancer; breathing problems while sleeping; diabetes; heart disease; if a female partner is pregnant or trying to get pregnant; kidney disease; liver disease; lung disease; prostate cancer, enlargement; any unusual or allergic reactions to testosterone or other products; pregnant or trying to get pregnant; breast-feeding. Your healthcare provider will need to have regular bloodwork drawn while on testosterone. This medication is banned from use in athltes by most athletic organizations.. Buy 1-Testosterone Cypionate Online In Australia

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: breast cancer; breathing problems while sleeping; diabetes; heart disease; if a female partner is pregnant or trying to get pregnant; kidney disease; liver disease; lung disease; prostate cancer, enlargement; any unusual or allergic reactions to testosterone or other products; pregnant or trying to get pregnant; breast-feeding. 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.4

Because some testosterone transdermal systems (e.g., Androderm) contain aluminum or other metal components, patients should be instructed to remove the patch before undergoing magnetic resonance imaging (MRI). 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.4

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.5 Additionally, the efficacy and long-term safety of testosterone topical solution in patients over 65 years of age has not been determined due to an insufficient number of geriatric patients involved in controlled trials.6 According to the Beers Criteria, testosterone is considered a potentially inappropriate medication (PIM) for use in geriatric patients and should be avoided due to the potential for cardiac problems and its contraindication in prostate cancer. The Beers expert panel considers use for moderate to severe hypogonadism to be acceptable.Buy 1-Testosterone Cypionate Online In Australia7  . 

1-Testosterone Cypionate is an injectable steroid which contains 100 mg of the Dihydroboldenone Cypionate.

Dihydroboldenone, most commonly known as 1-testosterone, is a 5alpha reduced form of the steroid Boldenone. This lack of 5alpha reduction with the compound allows users to administer it without suffering the negative side effects associated with this chemical reaction but also eliminates the benefits as well. Boldenone is not the only steroid that shares similarities with Dihydroboldenone. In fact Dihydroboldenone is chemically identical to the drug Methenolone except for the 1-methylation that is apart of Methenolone. 1-methylation was of course added to Methenolone to make it more available when taken orally and thus Dihydroboldenone is not efficiently utilized when administered orally, although it was once sold over the counter in tablet and pill form. Some of these over the counter preparations of the drug were done utilizing a delivery system similar to Andriol, i.e. producing an oil-solubilized product with Dihydroboldenone. This would still not be a relatively worthwhile system of delivery to use however if one wanted to maximize the potential of the compound. Intramuscular injection is by far the most efficient method of administration to use as with most anabolic steroids. Buy 1-Testosterone Cypionate Online In Australia

As mentioned above, Dihydroboldenone is structurally similar to Methenolone and Boldenone and less so to testosterone despite the commonly used name for it, 1-testosterone. For this reason some female athletes may be inclined to use 1-Testosterone Cypionate as well. The potential for development of symptoms of virilization still remain but are not as severe as with synthetic testosterone or other harsher drugs. This is not to say however that 1-Testosterone Cypionate is a mild drug. To simplify the explanation of exactly what the drug is, it is to Boldenone as Dihydrotestosterone (DHT) is to testosterone. This would explain why the effects of the drug, both positive and negative, are so dissimilar to those of Boldenone. Like testosterone and Dihydrotestosterone, a portion of the Boldenone that a user administers converts to Dihydroboldenone. Also similarly, Dihydroboldenone like Dihydrotestosterone does not convert to anything else past that compound.

The frequency of dosing with 1-Testosterone Cypionate depends on the ester used with the compound. Seemingly the most popular current ester to produce the drug with is Cypionate. Typcially, males would use a dosage of 200-400 mg 1-Testosterone Cypionate a week. For womens, the cycle starts at a low dose of 25 mg per week, and it gradually increases until it reaches a maximum dose of 75 mg per week.