Testosterone enanthate is an injectable testosterone supplement that is usually administered to treat low testosterone and other symptoms of hypogonadism in males. It is a slow-release oil-based ester that can be administered either intramuscularly or subcutaneously, depending on the health care provider's preference or the individual receiving the injection. It was first used clinically as a treatment of low testosterone in , and its use by men has since then significantly increased in popularity.
Testosterone exerts its actions in the body primarily by means of its binding to and interaction with androgen receptors. In tissues within the body, the testosterone secreted by the testes is converted into a more potent metabolite known as dihydrotestosterone DHT ; this conversion of testosterone to its more active form is facilitated by the cytoplasmic enzyme known as 5 alpha-reductase.
DHT then binds to the androgen receptors inside the cytoplasm of the target cells and forms a DHT-receptor complex.
After the formation of the DHT complex, it passes into the nucleus of the target cells, where it binds to the relevant nucleotide sequences on the chromosomal DNA, which then results in the synthesis of the relevant proteins by nuclear transcription.
A second pathway by which testosterone also acts in the body is through its conversion into estradiol; the amount of testosterone that follows this pathway is considerably less than when involving DHT synthesis. In this pathway, free testosterone is converted by the cytochrome P enzyme aromatase into estradiol. The estradiol that is produced then interacts with the estrogen receptors within the cells and then begins to exert its effects in the development and maintenance of bone density.
Testosterone may be exogenously administered by injection, topically as a gel, ointment, or patch, or by implantation of long-acting pellets. Testosterone enanthate, however, is typically administered as an injection either through the intramuscular route, or subcutaneously.
It has a long half-life of 7 to 9 days and may persist in the body at therapeutic levels for up to 3 or 4 weeks after administration. After administration, testosterone enanthate circulates in the bloodstream by binding to plasma proteins.
One of the most important plasma proteins that testosterone enanthate binds to is sex hormone-binding globulin SHBG ; of the various plasma proteins in the body, testosterone has the most affinity for SHBG. Other plasma proteins that testosterone enanthate binds to in lesser amounts are albumin, corticosteroid-binding globulin, and alpha-1 acid glycoprotein. After binding to the plasma proteins, testosterone is then transported around the body until it reaches the cells in the targeted tissues.
Testosterone is passively transferred across the cell membranes into the cytoplasm at the target tissues, where it is converted into DHT as previously discussed. The metabolism and inactivation of testosterone occur mainly in the liver; it undergoes both phases I and phases II hepatic metabolism to be readily excreted.
However, testosterone can also be metabolized in the kidneys, gut, muscles, and adipose tissue. Testosterone is oxidized in the liver by the cytochrome P 3A family of hepatic oxidases during phase I hepatic metabolism. Following its oxidation by cytochrome PA, testosterone is then conjugated with glucuronic acid to make it water-soluble so that the kidneys can readily excrete it.
The process by which the oxidized testosterone becomes conjugated with glucuronic acid is facilitated by the enzyme uridine diphospho glucuronosyl transferase UGT. The testosterone that is excreted in the stool is unconjugated for that which has bound glucuronic acid. Several medical conditions may indicate the need for exogenous testosterone administration.
Some of these medical conditions are: 12 There are several circumstances in which testosterone injections should not be administered or administered with extra caution:. This means that research has demonstrated significant fetal abnormalities when used in pregnant women. As such, testosterone injections are absolutely contraindicated in pregnancy, and the risks of its use far outweigh any potential benefits that may be gained from its administration.
Testosterone injections are also contraindicated in women who are breastfeeding as studies have shown that it is expressed in breast milk to a significant degree. Some side effects that may arise from exogenous administration of testosterone enanthate injections are:. Testosterone Enanthate Injection. Generic Name: Testosterone Enanthate. Some of these functions include: Skeletal muscle : Testosterone has a hypertrophic and hyperplastic effect on the muscle fibers within the skeletal muscular system.
There is a significant increase in muscle growth during puberty due to the hypertrophic effects of testosterone. In men experiencing muscle loss due to aging, testosterone administration has been shown to aid in reversing this condition. It is converted to estradiol by means of the enzyme aromatase; estradiol minimizes the breakdown of bone by inhibiting the resorption of bone by osteoclasts.
Additionally, testosterone is converted into dihydrotestosterone DHT by the enzyme 5-alpha reductase; DHT stimulates bone osteoblasts and the laying down of bone. This is one of the reasons that males generally tend to have higher red blood cell levels compared to females. The process by which testosterone stimulates red blood cell production is not yet fully understood and is undergoing research. These studies indicate that most men suffering from hypogonadism due to low testosterone may experience some degree of memory impairment as well as impaired verbal and visual performance.
There is an association between hypogonadism in men and depressive moods. Research performed revealed an improvement in moods in men with hypogonadism after treatment with testosterone supplements. Some of these medical conditions are: 12 13 Male hypogonadism: This may occur at birth or later in the life of males. In this condition, there are decreased levels of testosterone due to failure of the testicles for a variety of reasons such as orchitis, orchidectomy, testicular torsion, or aging, among others.
Older cis men with symptoms of andropause, including the loss of vigor and a lower sex drive, will often benefit from TRT. This drug can also be used for hormone therapy in transgender masculine people. Other uses include treatment for delayed puberty in cis boys, and in metastatic breast cancer when it has spread in those who are postmenopausal.
The drug is also sometimes used, controversially, as an anti-aging therapy in older cis men. Testosterone enanthate is a clear or yellowish fluid that comes in a 5-milliliter ml glass vial. It is injected into a buttock muscle every one to four weeks. To avoid large changes in hormone levels, and the mood swings that may come with them, lower doses are often used over shorter intervals. The active drug, which is suspended in sesame oil, has a sustained release period of two to three weeks.
The dosage may vary by individual but it is typically used as follows:. While testosterone enanthate is sometimes used interchangeably with testosterone cypionate depo testosterone , the latter is approved only for treating hypogonadism. Testosterone enanthate is a steroid with both anabolic and androgenic properties. It is used to treat low testosterone levels, whether as TRT in cisgender men or as hormone therapy in transgender people, among other uses.
It is given by intramuscular injection in the buttocks. This drug is designed to alter hormone levels, and has both clear benefits and risks. The side effects can range from mild to intolerable. The most serious side effects are associated with testosterone abuse, an increasing problem in the United States. According to the FDA, the most common side effects associated with testosterone enanthate use include:. The severity of the side effects usually depends on the dose.
The side effects may improve if the dose is reduced. Less common but potentially more serious side effects are associated with the long-term use or overuse of this drug. Some are related to its androgenic effects. Others can affect the heart and liver. Call a healthcare provider if you have any of the following while using testosterone enanthate:.
Some androgenic effects seen in those assigned female at birth, such as clitoral enlargement and a deepening voice, are permanent once they happen. A low sperm count can reduce fertility in cis men. The excessive use of testosterone also may increase the risk of some medical conditions, especially in cis men. They include:. Severe liver injury also may occur. Symptoms of such injury include fatigue, abdominal pain, nausea, vomiting, dark urine, and the yellowing of the eyes and skin jaundice.
Call or seek emergency care if you have signs of a cardiovascular event, such as heart attack or stroke. Heart attack signs include chest pain, shortness of breath, profuse sweating, and pain in the left arm or jaw.
Stroke symptoms include severe headache, weakness on one the side of the body, and trouble speaking. There are certain drugs that interact with testosterone enanthate. Some may need to be changed or adjusted. Or, other forms of therapy can be explored, including lower-dose testosterone patches. The possible drug interactions include:.
There are conditions in which this drug should not be used under any circumstances. This includes the use of testosterone in untreated prostate cancer or breast cancer , and in pregnancy. The drug should also be avoided if you are allergic to sesame oil or any components of the drug. The prostate gland is an organ in those assigned male at birth. Its role is to secrete prostate fluid, one of the elements of semen. The gland depends on androgens to function and if their level falls too low, the body will make less prostate fluid.
Along with this decrease is a higher risk of prostate gland enlargement, known as benign prostatic hyperplasia BPH. The condition limits the flow of urine, and may lead to bladder stones and reduced kidney function. Moreover, it appears to do so without increasing the risk of prostate cancer. The same may not be true for those assigned male at birth who are diagnosed with a prostate malignancy. The link between testosterone use and prostate cancer remains highly controversial, but there have been reports that testosterone use in older men with untreated prostate cancer led to the cancer's spread.
With that being said, a study from Harvard Medical School found there was no link between disease progression and testosterone use in 13 cis men with untreated prostate cancer who were on TRT for an average of 2. Other studies have reached a similar conclusion.
Despite the ongoing controversy, the FDA strongly advises against the use of testosterone in cis men with untreated prostate cancer. Even for cis men without cancer, any elevation in the prostate-specific antigen PSA test within the first three to six months of starting testosterone would mean ending treatment until a complete cancer investigation can be done.
The mechanism for this link is poorly understood and some don't believe it exists. For cis men with untreated breast cancer, however, the FDA remains firm. The use of testosterone poses a potential threat and should be avoided without exception.
Testosterone enanthate should not be used in those who are pregnant. When given during pregnancy, testosterone can affect a female fetus. This condition causes physical characteristics typically associated with those assigned male at birth to be present in a fetus assigned female.
Some of the symptoms may be seen at birth, while others may only become apparent during puberty or later in life. The risk of virilism, the medical term for this condition, in the baby is higher in pregnant women who themselves are experiencing virilism as a result of testosterone use.
Testosterone therapy must be stopped if a pregnancy is suspected. This is especially true during the first trimester as fetal cells are still specializing.
If the pregnancy is confirmed, the parents need to be advised about the potential hazards to the baby. Testosterone use does not appear to pose any risk to a breastfeeding baby. The components of the drug are largely broken down before they reach the bloodstream, breast milk, or other body fluids. Similarly, testosterone use in cis men does not pose any risk to a pregnancy, either during conception or gestation.
Testosterone enanthate offers clear benefits when treating cis men with low testosterone levels. It also may be used to treat other conditions, including hormone therapy in transgender masculine people.
But it also carries with it many potential side effects and health risks. Some are quite serious, including the risk of heart attack and stroke in cis men. Drug interactions are a potential problem too, so it's important tell your healthcare provider your complete health history before starting its use. Whether you're thinking of TRT or considering testosterone enanthate for another reason, it's important to discuss all the possibilities with your healthcare provider.
It's the best way to ensure that your decision to use the drug leads to a positive outcome. Sign up for our Health Tip of the Day newsletter, and receive daily tips that will help you live your healthiest life. Endo Pharmaceuticals Solutions Inc. Updated October Testosterone therapy: What we have learned from trials.
0コメント