Testosterone (medication)

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Testosterone is a naturally occurring drug and steroid hormone. It is used to treat male hypogonadism and some types of breast cancer. It can also be used to improve athletic ability in the form of doping. It is unclear whether the use of testosterone for low levels because of useful or harmful aging. Testosterone can be used as a gel or patch applied to the skin, injection into muscles, tablets placed on the cheeks, or tablets to drink.

Common side effects of testosterone include acne, swelling, and breast enlargement in men. Serious side effects may include liver toxicity, heart disease, and behavioral changes. Exposed women and children can develop masculinization. It is recommended that individuals with prostate cancer do not use drugs. May cause harm to infants if used during pregnancy or lactation. Testosterone is present in the androgen drug family.

Testosterone was first isolated in 1935. Usage levels have increased three times in the United States between 2001 and 2011. This is a List of Essential Medicines of the World Health Organization, the most effective and safe medicines needed in the health system. It is available as a generic drug. Price depends on the dose and shape of the product.

Video Testosterone (medication)

Medical use

The primary use of testosterone is the treatment of men with too little or no natural testosterone production, also called hypogonadism or hypoandrogenism (androgen deficiency). This treatment is referred to as hormone replacement therapy (HRT), or alternatively, and more specifically, as a replacement therapy for testosterone (TRT) or androgen replacement therapy (ART). This is used to maintain serum testosterone levels in the normal male range. Decreased production of testosterone with age has led to interest in testosterone supplementation.

Disadvantages

Lack of testosterone (also called hypotestosteronism or hypotestosteronemia) is an abnormally low production of testosterone. This may be due to testicular dysfunction (primary hypogonadism) or hypothalamus-pituitary dysfunction (secondary hypogonadism) and may be congenital or acquired.

Low due to age

Testosterone levels may decrease gradually with age. The United States Food and Drug Administration (FDA) stated in 2015 that both the benefits and safety of testosterone supplements have been established for low testosterone levels due to aging. The FDA has required labels on testosterone including warnings about an increased risk of heart attack and stroke.

Transgender men

To harness the virilizing effect, testosterone is given to transgender men as part of the masculinizing hormone therapy, titrated for clinical effects with "target levels" of the average male testosterone level.

Female

Low-dose effective low-dose testosterone supplementation for hypoactive sexual desire disruption in women. However, its long-term security is unclear. Treating low androgen levels with testosterone is generally not recommended in women when caused by hypopituitarism, adrenal insufficiency, or after ovarian removal surgery. It is also not usually recommended to improve cognition, risk of heart disease, bone strength, or for general wellbeing.

A 2014 systematic review and meta-analysis of 35 studies comprising more than 5,000 postmenopausal women with normal adrenal gland function found that testosterone was associated with a significant increase in various sexual function domains. Such domains include the frequency of sexual activity, orgasm, arousal, and sexual satisfaction among others. Women who experience menopause due to ovariectomy show a significant increase in sexual function with testosterone relative to those who experience normal menopause. In addition to beneficial effects on sexual function, testosterone is associated with changes in blood lipids including decreased total cholesterol levels, triglycerides, and high density lipoproteins and elevated levels of low-density lipoproteins. However, these changes are small in magnitude, and their long-term effects on cardiovascular outcomes are unclear. Clearer changes with oral undecanoate testosterone compared with parenteral testosterone (eg, transdermal). Testosterone does not show any significant effects on depressed mood or anxiety, anthropomorphic measures such as weight or body mass index, or bone mineral density. In contrast, it was associated with significant incidence of androgenic side effects including acne and hirsutism, and other androgenic side effects such as weight loss, hair loss patterns and deepening of sounds were also reported in some experiments but excluded from the meta-analysis because of insufficient data. The overall quality of evidence is low and considered inconclusive in certain areas, such as long-term security.

Systematic review and meta-analysis performed on more than 3,000 postmenopausal women found that transdermal testosterone was effective in improving several sexual function domains in the short-term treatment of hypoactive sexual desire disorder (also known as sexual interference/female sexual arousal). Androgenic side effects such as acne and increased hair growth were significantly greater in incidence, while there was no significant difference in "increased facial hair, alopecia, deepening of voice, urinary symptoms, breast pain, headache, site reaction to patches, total adverse events, serious side effects, reason for withdrawal from the study, and the number of women completing the study "were seen relative to controls.

Although testosterone is effective in improving sexual function in postmenopausal women, it does not look like in premenopausal women. A 2016 review reported that studies have not found a significant correlation between libido and testosterone levels circulating in premenopausal women and that treatment of premenopausal women with low-dose testosterone has not been found to significantly improve sexual functioning in most studies.

Maps Testosterone (medication)

Non-medical use

Athletics

Testosterone is used as a form of doping among athletes to improve performance. Testosterone is classified as an anabolic agent and is on the World Anti-Doping Agent (WADA) List of Substances and Prohibited Methods. Hormone supplements cause the endocrine system to adjust production and decrease natural hormone production, so that when the supplement is stopped, natural hormone production is lower than before.

Anabolic-androgenic steroids (AAS), including testosterone and ester, have also been taken to promote muscle development, strength, or endurance. They do so directly by increasing the synthesis of muscle proteins. As a result, muscle fibers become larger and improve faster than the average person.

After a series of scandals and publicity in the 1980s (such as Ben Johnson's increasing performance at the 1988 Summer Olympics), the ban on the use of the AAS was updated or reinforced by many sports organizations. Testosterone and other AAS were defined as "substances controlled" by the United States Congress in 1990, with the Anabolic Steroid Control Act . Its use is seen as a problem in modern sport, especially given the length of athletes and professional laboratories in trying to hide the use of sports regulators. The use of steroids has once again been highlighted recently as a result of the suicide of Chris Benoit's double professional suicide in the Netherlands in 2007; However, there is no evidence to suggest the use of steroids as a factor in the incident.

Some female athletes may have higher levels of testosterone naturally than others, and may be asked to agree to gender verification and surgery or drugs to lower testosterone levels. This has proven controversial, with the Court of Arbitration for Sport suspending the IAAF policy because there is insufficient evidence of a link between high androgen levels and increased athletic performance.

Abuse detection

A number of methods for detecting testosterone use by athletes have been used, largely based on urine testing. These include the ratio of testosterone/epitestosterone (usually less than 6), the ratio of testosterone/luteinizing hormone and the carbon-13/carbon-12 ratio (pharmaceutical testosterone contains less carbon-13 than endogenous testosterone). In some test programs, an individual's historical results can serve as a reference interval for the interpretation of suspicious findings. Another approach under investigation is the detection of a given form of testosterone, usually an ester, in the hair.

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Contraindications

Absolute contraindications to testosterone include prostate cancer, increased hematocrit (& gt; 54%), uncontrolled congestive heart failure, other cardiovascular diseases, and uncontrolled obstructive sleep apnea. Breast cancer is said by some sources to be the absolute contraindication of testosterone therapy, but androgens including testosterone have actually been used to treat breast cancer. The relative contraindications of testosterone include increased prostate-specific antigen (PSA) in men with high prostate cancer risk due to ethnicity or family history, severe lower urinary tract symptoms, and an increase in hematocrit (& gt; 50%).

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Side effects

Side effects may also include mild side effects such as oily skin, acne, and seborrhea, as well as the loss of scalp hair, which can be prevented or reduced by 5-reductase inhibitors. In women, testosterone can produce hirsutism (excessive facial/body hair growth), deepening of the voice, and other signs of virilization. Exogenous testosterone can lead to suppression of spermatogenesis in men, which causes, in some cases, reversible infertility. Gynecomastia and breast tenderness can occur with high doses of testosterone because peripheral conversion of testosterone by aromatase to estrogen estradiol in excessive amounts. Testosterone treatment, especially in high doses, can also be associated with mood swings, increased aggression, increased sex drive, spontaneous erection, and nocturnal emission.

Other side effects include an increase in hematocrit, which may require venipuncture to treat, and exacerbations of sleep apnea.

The FDA states by 2015 that neither the benefits nor the safety of testosterone has been established for low testosterone levels due to aging. The FDA has required testosterone pharmaceutical labels including warning information about the possible increased risk of heart attacks and strokes. They also need labels including concerns about harassment and dependence.

Long term harmful effects

Cardiovascular Disease

The adverse effects of testosterone supplementation may include increased cardiovascular events (including stroke and heart attack) and deaths based on three studies conducted by colleagues involving men taking testosterone replacement. In addition, an increase of 30% of deaths and heart attacks in older men has been reported. Due to the increased incidence of adverse cardiovascular events compared with the placebo group, Testosterone in older men with the National Institute of Aging randomized trials was stopped earlier by the Safety and Data Monitoring Committee. On January 31, 2014, reports of strokes, heart attacks, and deaths in men who used FDA approved testosterone replacements made the FDA announce that they would investigate the issue. Then, in September 2014, the FDA announced, as a result of "potentially adverse cardiovascular outcomes", a review of the suitability and safety of Testosterone Replacement Therapy (TRT). The FDA now requires warnings in drug labels of all approved testosterone products regarding deep vein thrombosis and pulmonary embolism.

Until 2010, the study did not show any effect on the risk of death, prostate cancer or cardiovascular disease; Newer studies, however, do cause concerns. A 2013 study, published in the Journal of the American Medical Association, reported "the use of testosterone therapy was significantly associated with an increased risk of adverse outcomes." The study began after previous, randomized clinical trials, testosterone therapy in men was prematurely terminated "because adverse cardiovascular events raised concerns about the safety of testosterone therapy."

Prostate cancer

Testosterone in the presence of slow-growing prostate cancer is assumed to increase its growth rate. However, the relationship between testosterone supplementation and prostate cancer progression has not been proven. Nevertheless, doctors are warned about the risk of cancer associated with testosterone supplementation.

This can accelerate the growth of prostate cancer that already exists in individuals who have experienced androgen reduction. It is recommended that doctors screen prostate cancer by rectal examination and specific prostate antigen level (PSA) before starting therapy, and monitor the PSA and hematocrit levels closely during therapy.

Ethnic groups have different rates of prostate cancer. Differences in sex hormones, including testosterone, have been suggested as an explanation for this difference. This real paradox can be overcome by noting that prostate cancer is very common. In an autopsy, 80% of 80-year-old men suffer from prostate cancer.

Pregnancy and breastfeeding

Testosterone is contraindicated in pregnancy and is not recommended during breastfeeding. Androgens such as testosterone are teratogens and are known to cause fetal damage, such as producing virilization and ambiguous genitals.

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Interactions

5? -Reductase inhibitor

5? -Reductase inhibitors such as finasteride and dutasteride can slightly increase the amount of testosterone in circulation by inhibiting metabolism. However, these drugs do this through the prevention of conversion of testosterone into potent dihydrotestosterone (DHT) metabolites, and this results in a dramatically reduced decrease in DHT levels (which circulate at much lower relative concentrations). In addition, local DHT levels in so-called androgenic tissues (5 -reductase-expressing) are also greatly reduced, and this can have a strong impact on certain testosterone effects. For example, body and facial hair growth and penile growth induced by testosterone may be inhibited by a 5-uctase inhibitor, and this may be considered undesirable in context, for example, puberty induction. On the other hand, 5-reductase inhibitors can prevent or reduce adverse androgenic side effects of testosterone such as scalp hair loss, oily skin, acne, and seborrhea. In addition to preventing the conversion of testosterone into DHT, 5 -reductase inhibitors also prevent the formation of neurosteroids such as 3? -androstanediol from testosterone, and this may have neuropsychiatric consequences in some men.

Aromatase inhibitors

Aromatase inhibitors such as anastrozole prevent the conversion of testosterone to estradiol by aromatase. Since only a small part of testosterone is converted to estradiol, it does not affect testosterone levels, but it can prevent estrogenic side effects such as gynecomastia that can occur when testosterone is given at relatively high doses. However, estradiol provides negative feedback on the hypothalamus-pituitary-gonad axis and, for this reason, the prevention of its formation can reduce this feedback and inhibit the production of gonadal testosterone, which in turn can increase endogenous testosterone levels. Testosterone therapy is sometimes combined with aromatase inhibitors for men with secondary hypogonadism who wish to conceive children with their partners.

Cytochrome P450 Inhibitor

Inhibitors and inducers of cytochrome P450 enzymes such as CYP3A4 have been associated with little or no effect on circulating testosterone levels.

Antiandrogen and estrogen

Antiandrogens such as cyproterone acetate, spironolactone, and bicalutamide can block the androgenic and anabolic effects of testosterone. Estrogens can reduce the effects of testosterone by increasing liver production and in turn circulating levels of sex hormone binding globulin (SHBG), carrier proteins that bind and occupy androgens such as testosterone and DHT, and thereby reduce these androgen free concentrations.

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Pharmacology

Pharmacodynamics

Testosterone is a high affinity ligand for nuclear androgen receptor agonists (AR). In addition, testosterone binds and activates membrane androgen receptors (mars) such as GPRC6A and ZIP9. Testosterone is also strengthened by transformation by 5-conversion into more potent DHT androgens in so-called androgenic tissues such as prostate gland, seminal vesicles, skin, and hair follicles. In contrast to the case of testosterone, such potentiation occurs at a reduced or absent rate with most synthetic AAS (as well as with DHT), and is primarily responsible for the dissociation of anabolic and androgenic effects with these agents. In addition to DHT, testosterone is converted at a rate of about 0.3% into estrogen estradiol through aromatase. This occurs in many tissues, especially adipose tissue, liver, and brain, but especially in adipose tissue. Testosterone, once converted to DHT, is also metabolized to 3? -androstanediol, neurosteroids and strong positive allosteric modulators of GABA receptors _A , and 3? -androstanediol, a powerful and special agonist from ER? This metabolite, together with estradiol, may be involved in a number of testosterone effects in the brain, including antidepressant, anxiolytic, stress-relieving, beneficial, and pro-sexual effects.

Effects on body and brain

ARS is widely expressed throughout the body, including the penis, testes, epididymides, prostate gland, seminal vesicles, fat, skin, bone, bone marrow, muscle, larynx, heart, liver, kidney, pituitary gland, hypothalamus, and elsewhere. throughout the brain. Through ARS activation (as well as mars), testosterone has many effects, including the following:

• Increases growth, function and maintenance of the prostate gland, seminal vesicles, and penis during puberty and subsequently
• Increases muscle growth and maintenance, especially in upper body
• Causes subcutaneous fat deposited in a masculine pattern and decreases overall body fat
• Suppressing estrogen-induced breast development, but can also continue to produce gynecomastia through over-conversion to estradiol if levels are too high
• Maintain skin health, integrity, appearance, and hydration and slow the rate of skin aging, but it can also cause oily skin, pimples, and seborrhea
• Increases facial and body hair growth, but can also cause hair loss and hirsutism on the scalp
• Contribute to bone growth and cause shoulder width during puberty
• Integrates the synthesis of liver proteins, such as the production of sex hormone binding globulin and many other proteins
• Increases the production of erythropoietin in the kidneys and thus stimulates the production of red blood cells in the bone marrow and elevates the hematocrit
• Provide negative feedback on the hypothalamus-pituitary-gonad axis by suppressing the secretion of the follicle gonadotropin (FSH) hormone and luteinizing hormone (LH) from the pituitary gland, thus inhibiting the production of gonad sex hormones and spermatogenesis and fertility
• Set the vasomotor system and body temperature through the hypothalamus, thus preventing hot flashes
• Modulate brain function, with effects on mood, emotion, aggression, and sexuality, and cognition and memory
• Increases sex drive and erection capacity and causes spontaneous erections and nocturnal emissions
• Increases the risk of benign prostatic hyperplasia and prostate cancer and accelerates prostate cancer progression
• Reduces breast proliferation and breast cancer risk

Pharmacokinetics

Testosterone is not orally active except in very high doses due to poor absorption and extensive first-track metabolism. In addition, steroidal androgens including testosterone are hepatotoxic and there is potential for liver injury with high doses of oral testosterone because of local concentrations of supraphysiological drug concentrations in the liver. Instead of taking oral, testosterone is administered parenterally in topical gels and creams, transdermal patches, buccal tablets, and subdermal implants. In addition, it is administered by intramuscular depot injection in the form of a long-acting prodrug ester such as testosterone cypionate, testosterone enanthate, and testosterone propionate, and highly durable undeservano testosterone. Buciclate testosterone is a long-acting testosterone tester that has been developed, but has not been approved for medical use.

Although testosterone itself is not used orally, undecanoate testosterone is approved and used orally. Due to the unique chemical properties provided by very long ester chains, undecanoate testosterone partially passes the heart's first-pass metabolism through the uptake of the gastrointestinal tract directly into the lymphatic system and then into the circulation. Of the oral undecanoate testosterone that reaches the circulation, 90 to 100% is transported by lymphatics. These esters are not hepatotoxic at the doses used. However, undecanoate oral testosterone has variable pharmacokinetics and should be taken two to four times daily with food. In addition to undecanoate testosterone, a combination of testosterone with a 5-ductasease inhibitor such as dutasteride can make the testosterone active orally when administered in the form of a capsule containing oil. This is through the reduction of the metabolism of the first liver testosterone hormone.

Absorption

Oral bioavailability testosterone is very low and almost meaningless. Oral undecanoate testosterone bioavailability is 3 to 7%. Topical testosterone gel has a 10% bioavailability when administered to recommended skin sites including stomach, arms, shoulders, and thighs. The bioavailability of testosterone through implants is nearly 100%, while the bioavailability of intramuscularly administered drugs is generally almost 95%.

Distribution

In circulation, 97.0 to 99.5% of testosterone is bound to a plasma protein, with 0.5 to 3.0% unbound. It is tightly bound to SHBG and weak on albumin. Of circulating testosterone, 30 to 44% is bound to SHBG while 54 to 68% is bound to albumin. Unbound testosterone is referred to as free testosterone and testosterone bound to albumin is referred to as bioavailable testosterone . Unlike testosterone bound to SHBG, testosterone bioavailable bound to plasma proteins is weak enough that, as with free testosterone, it may be biologically active, at least to some extent. When referred collectively (ie, free, bioavailable, and SHBG-bound), the circulating testosterone is referred to as total testosterone .

Metabolism

Testosterone is metabolized primarily in the liver especially (90%) by reduction through 5? - and 5? -reductase and conjugation through glucuronidation and sulfation. The main urine metabolism of testosterone is androsterone glucuronide and etiocholanolone glucuronide.

The half-life of testosterone elimination varies depending on the route of administration and formulation and whether or not it is esterified. Oral undecanoate testosterone (in the oil capsule) has a half-life of terminal 1.6 hours. Because of the very short half-life of the terminal, oral undecanoate testosterone is taken two to four times per day. In contrast to oral testosterone, other testosterone forms including gels and topical solutions, transdermal patches, and buccal tablets have an extended discharge effect and can be administered less frequently, at intervals, depending on the route/formulation, once daily, twice daily, or every two days once.

While the half-life of the unesterified testosterone terminal given by intramuscular injection is very short in only about 10 minutes, the terminal half of the intramuscular testosterone ester is much longer. Given in the form of an oil solution, the half-life terminal is 0.8 days for testosterone propionate, 4.5 days for testosterone enanthate, 20.9 days (in tea seed oil) and 33.9 days (in caster oil) for undecanoate testosterone , and 29.5 days for buciclate testosterone. Although precise values ​​are not available for intramuscular cypionate testosterone, the pharmacokinetics are said to be the same as testosterone enanthate, with a "very comparable" testosterone release. Because of their varying and different terminal half-lives, different intramuscular testosterone esters are administered with different frequencies. Testosterone propionate is injected two to three times per week, testosterone enanthate and testosterone cypionate are injected every two to four weeks, and testosterone undecanoate and testosterone buciclate are injected every 10 to 14 weeks. Because of its relatively short duration, testosterone propionate is now relatively little used and undeservano testosterone is the preferred testosterone ester for intramuscular use. Testosterone undecanoate and testosterone buciclate can be injected intramuscularly at least four times per year.

The half-life of the subdermal testosterone implant is 2.5 months. Interval replacement every four to five months.

Elimination

Testosterone and its metabolites are removed in the urine. It is excreted primarily as androsterone glucuronide and etiocholanolone glucuronide. It is also excreted to a small extent like other conjugates such as glucuronide testosterone (1%), testosterone sulfate (0.03%), and androstanediol glucuronides. Only a small amount of testosterone (less than 0.01%) is found to be unchanged in the urine.

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Chemistry

Testosterone is a natural androstane steroid and is also known by the chemical name androst-4-en-17? -ol-3-one. It has a double bond between the position of C4 and C5 (making it androstene), ketone group at position C3, and hydroxyl group (alcohol) at C17? position.

Derivatives

Testosterone esters replaced in C17? position with the lipophilic fatty acid ester part of various long chains. The major testosterone esters include testosterone cypionate, testosterone enanthate, testosterone propionate, and undecanoate testosterone. A C17? ether prodrug testosterone, cloxotestosterone acetate, has also been marketed, although little known and used very rarely or no longer. Another C17? ether prodrug testosterone, silandrone, also exist but never marketed, and famous for being orally active. In addition to esters and ether prodrugs, androgen progenies or testosterone precursors, such as dehydroepiandrosterone (DHEA), androstenediol, and androstenedione, are also present, and converted to testosterone with variable extents after oral ingestion. Unlike testosterone ester and ether prodrugs, these prohormones are just weak androgenic/anabolic.

All synthetic AAS is a derivative of testosterone. Prominent examples include nandrolone (19-nortestosterone), metandienone (17? -metil -? ¹ -testosterone), and stanozolol (17? Derivated Derivative DHT). Unlike testosterone, the 17-alkylated AAS, such as metandienone and stanozolol, is actively orally administered. This is due to steric disruption of C17 metabolism-the position during the first pass through the liver. In contrast, most of the non-alkylated AAS, such as nandrolone, is inactive orally, and must be administered by intramuscular injection. This is almost always in the form of esters; for example, in the case of nandrolone, such as nandrolone decanoate or nandrolone phenylpropionate.

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History

Testosterone was first isolated and synthesized in 1935. Shortly thereafter, in 1937, the first testosterone became commercially available as a pharmaceutical drug in pellet form and then in ester form for intramuscular injection as a relatively short propionate testosterone. Methyltestosterone, one of the first synthetic AAS and orally active androgens, was introduced in 1935, but was associated with hepatotoxicity and eventually became largely medically obsolete. In the mid-1950s, testosterone of estrogen ester-esters was longer and testosterone enosterat was introduced. They largely replaced testosterone propionate and became the main testosterone ester used medically for more than half a century. In the 1970s, undecanoate testosterone was introduced for oral use in Europe, although intramuscular undetanoate testosterone has been used in China for several years. Intramuscular testosterone undecanoate was not introduced in Europe and the United States until some time later (in the early to mid 2000s and 2014).

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Society and culture

Usage

In the US in the 2000s, companies and figures in popular media had the idea of ​​"andropause" being heavily marketed as something parallel to the menopause; these ideas have been rejected by the medical community. In addition, advertising from drug companies that sell testosterone and human growth hormone, as well as food supplement companies that sell all kinds of "boosters" for older men, has emphasized the "need" of middle-aged or aging men for testosterone. There is a medical condition called slow-onset hypogonadism; according to Thomas Perls and David J. Handelsman, writing in an editorial in 2015 at the Journal of the American Geriatrics Society, it seems that the condition is overly diagnosed and overdone. Perls and Handelsman noted that in the US, "testosterone sales increased from $ 324 million in 2002 to $ 2 billion in 2012, and the number of prescribed testosterone doses rose from 100 million in 2007 to half a billion by 2012, excluding additional contributions from pharmacy compounding , internet, and direct clinic sales to patients. "

Common names

Testosterone is a generic name of testosterone in both English and Italian and INN , USAN , USP , BAN , and DCIT of the drug, while testostÃÆ' Â © rone is the French name and DCF . It is also referred to in Latin as testosteronum in Spanish and Portuguese as testosterone, and in German, Dutch and Russian and other Slavic languages ​​as testosterone me. The Cyrillic script of testosterone is ??????????? .

Brand name

Testosterone is marketed under a large number of brand names worldwide. The major brand names of testosterone and/or ester include Andriol, Androderm, Androgel, Axiron, Delatestryl, Depo-Testosterone, Intrinsa, Nebido, Omnadren, Primoteston, Sustanon, Testim, Testogel, Testopatch, Testoviron, and Tostran.

Availability

United States

In November 2016, unmodified (non-esterified) testosterone was available in the United States in the following formulations:

• Topical gel: Androgel, Fortesta, Testim, Testosterone (generic)
• Topical solutions: Axiron, Testosterone (generic)
• Transdermal filling: Androderm, Testoderm (discontinued), Testoderm TTS (discontinued), Testosterone (generic)
• Intranasal Gel: Natesto
• Buccal Tablet: Striant
• Pellet implants: Testopel

And the following testosterone ester prodrugs are available in the United States in oil solutions for intramuscular injection:

• Testosterone cypionate: Depo-Testosterone, Testosterone Cypionate (generic)
• Testosterone enanthate: Delatestryl, Testosterone Enanthate (generic)
• Testosterone propionate: Testosterone Propionate (generic)
• Testosterone undecanoate: Scheduled

Unmodified testosterone was also previously available for intramuscular injection but was not continued.

Testosterone cypionate and testosterone enanthate were previously available in combination with estradiol cypionate and estradiol valerate, respectively, under the brand name Depo-Testadiol and Ditate-DS, respectively, as an oil solution for intramuscular injection, but this formulation has been discontinued.

Unlike in Europe, Canada, and many other parts of the world, oral undecanoate testosterone is not available in the United States.

Canada

In November 2016, testosterone is available in Canada in topical gel (Androgel, Testim), topical solution (Axiron), transdermal patch (Androderm), and intranasal gel (Natesto). Testosterone cypionate (Depo-Testosterone, Testosterone Cypionate (generic)), testosterone enanthate (Delatestryl, PMS-Testosterone Enanthate), and testosterone propionate (Testosteron Propionate (generic)) are available as an oil solution for intramuscular injection and undecanoate testosterone (Andriol, PMS- Testosterone, Taro-Testosterone) is available in the form of oral capsules. Buccal tablets of testosterone and pellet implants do not appear to be available in Canada.

Other countries

Testosterone and/or ester are widely available in countries around the world in various formulations.

Legal status

Testosterone and its ester, along with other AASs, are prescription-controlled substances in many countries around the world. In the United States, they are drug Schedule III under the Controlled Substance Act, in Canada, they are drug Schedule IV under the Drug and Controlled Medicines Act, and in the UK, they are Class C drugs under the Abuse Act Drug.

Litigation

In 2014, a number of lawsuits are being made against testosterone producers, accusing a significant increase in stroke rates and heart attacks in elderly men taking testosterone supplements.

Doping in sports

There are many known doping cases in sports with testosterone and esters by professional athletes.

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Research

Depression

Testosterone has been used to treat depression in middle-aged men with low testosterone. However, the 2014 review shows no benefit in a men's mood with normal testosterone levels or in older men's moods with low testosterone.

Heart failure

Testosterone replacement can significantly increase exercise capacity, muscle strength and reduce QT interval in men with chronic heart failure (CHF). During the 3 to 6 months of the study under review, testosterone therapy seemed safe and generally effective, and (excluding prostate cancer) the authors found no justification for actually limiting its use in men with CHF. A similar review in 2012 also found increased training capacity and reasoned benefits provided to women. However, both reviews advocate for larger, longer, and randomized controlled trials.

Male contraception

Testosterone, as an ester such as testosterone undecanoate or testosterone buciclate, has been studied and promoted as male contraceptives analogous to estrogen-based contraceptives in women. If it is not considered a bad effect of testosterone, reduced spermatogenesis can be further suppressed by the addition of progestin such as norethisterone enanthate or levonorgestrel butanoate, enhancing the effects of contraception.

Testosterone is under development in low-dose intranasal formulations for the treatment of anorgasmia in women.

Porous hair loss

A study found that of 76 pre and postmenopausal women with hair thinning, 63% experienced hair regrowth when treated with subcutaneous testosterone implants that produced an average testosterone level over 300 ng/dL for 12 months. No woman reported hair loss or thinning during testosterone treatment.

Miscellaneous

Testosterone therapy can improve the management of type 2 diabetes. Low testosterone has been associated with the progression of Alzheimer's disease.

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References

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External links

• Testosterone (drug) in Curlie (based on DMOZ)
• Androderm (transdermal testosterone patch) - William Llewellyn's Anabolic.org
• AndroGel (transdermal testosterone gel) - William Llewellyn's Anabolic.org
• Testosterone Suspension - William Llewellyn's Anabolic.org

Source of the article : Wikipedia