Drugs to increase testosterone: TOP 10 best

What are hormones and where are they produced?

Hormones are substances that are produced in the body in special glands in very small quantities, but have a significant impact on the functioning and interaction of all organs.
Not a single biological process can occur without their participation. Testosterone is a hormone that is produced in the testicles, in special Leydig cells. In the testicles, sperm production also occurs in another type of cell - Sertoli cells. The coordinated work of these two types of cells ensures normal sexual and reproductive function in men.

The process of formation of testosterone (as well as other hormones) is under the control of the central nervous system, namely the pituitary gland - an organ the size of a pea, but whose role is enormous - it is a kind of conductor of the hormonal orchestra of the whole body. The production of testosterone is regulated by the so-called luteinizing hormone (doctors simply call it LH).

Stimulant therapy

Stimulant therapy is aimed at increasing the production of a man's own testosterone in the testicles. For this purpose, human chorionic gonadotropin preparations obtained from the pituitary gland of cattle are used. They are analogues of male luteinizing hormone, produced in the pituitary gland of the male brain.

This group of drugs includes:

• domestic Chorionic Gonadotropin (produced by the Federal State Unitary Enterprise "Moscow Endocrine Plant")
• imported drug Horagon (manufactured by Ferring, Germany).

The dose and frequency of administration of the drug depend on the age, weight of the patient and the initial level of male testosterone.

Prescription drugs, dispensed according to a doctor's prescription.

What effect does testosterone have on the male body?

The man has not yet been born, and in the seventh week of his stay in the womb, the male sex glands - the testes - are already forming. Another two weeks - and the testes begin to produce testosterone. During the transition period (13-17 years), the boy's testosterone secretion increases sharply, and he gradually turns into a man. How does this happen?

Firstly, under the influence of testosterone, the normal development of a man’s genital organs occurs - the penis, testicles, prostate gland (which, in fact, distinguishes him from a woman) as well as the appearance of so-called secondary sexual characteristics - hair growth on the face and body, characteristic hair growth pubic area.

Body structure: Testosterone promotes the formation of protein in body tissues, primarily in muscles, the growth and development of strength of which is proportional to the amount of testosterone (think about athletes who take “anabolic steroids” in order to have developed muscles). Testosterone is involved in the normal distribution of fat in the body.

In addition, this hormone affects the formation and normal maturation of bone tissue; thanks to testosterone, bone growth zones close in time. The condition of the skin is also directly related to testosterone, since the sebaceous glands function under its influence. Thus, a man’s appearance depends entirely on the amount of testosterone.

The lower timbre of a man’s voice is also the result of testosterone; it is with its participation that the vocal cords thicken during puberty.

Another extremely important function of testosterone is its influence on sexual activity and sexual behavior . Testosterone affects certain areas of the brain, leading to the appearance of sexual desire (libido), not only in men, but also in women.

Normal erection is also ensured with the active participation of testosterone: it has been proven that under its action, complete relaxation of the corpora cavernosa occurs, testosterone contributes to normal blood supply to the vessels of the penis.

Undoubtedly, sexual function and physical development determine a man’s well-being and attitude. However, the role of testosterone is not limited to this. In fact, there is not a single organ system that is not influenced to some extent by testosterone.

The cardiovascular system:

• promotes dilation of coronary vessels
• slows down the process of atherosclerosis
• prevents the development of cardiac hypertrophy in arterial hypertension
• reduces symptoms of coronary heart disease

Urinary system:

• prostate condition

Hematopoiesis: Testosterone affects the maturation of red blood cells (erythrocytes) in the bone marrow.

Central nervous system: Testosterone affects the following processes:

• attention, memory and speed of thinking
• mood (a large amount of testosterone promotes aggressive behavior, a low amount - on the contrary, causes depression)
• spatial orientation
• pronounced antidepressant effect

So testosterone “is what really differentiates men and women, testosterone literally shapes our creativity, intelligence, way of thinking, energy, desire to understand things. It influences and controls not only the potential we possess, but also the benefit we derive from it. It controls our sexual and communicative behavior” (Anna Moir “The Brain of the Sexes”).

What you need to know about using testosterone supplements?

Testosterone injections are a hormonal treatment.

This hormone is present in both men and women, but levels are naturally higher in men.

Its main use is to treat sexual dysfunction in men and postmenopausal symptoms in women with testosterone deficiency.

Transgender men can also use testosterone injections as a masculinizing therapy.

Testosterone injections are safe for many people, but may have side effects that vary depending on the reason a person is using the injections.

Before recommending long-term testosterone therapy, you should make sure you understand and evaluate the risks and benefits.

Therapy for low testosterone levels in men

Low production of testosterone by the testes is called hypogonadism.

Low testosterone levels can have negative consequences.

Symptoms of low testosterone in men include decreased sperm count, decreased bone or muscle mass, increased body fat, and erectile dysfunction.

The normal blood level of total testosterone in healthy adult men is > 17 nmol/L.

When treating hypogonadism, testosterone therapy may have the following benefits:

• improved sexual function
• increase muscle mass and strength
• improved mood
• better cognitive function
• possible reduction of osteoporosis

It is important to note that this therapy treats the symptoms of low testosterone, not the underlying cause.

Anyone who suspects they may have low testosterone levels can see their doctor for a diagnosis.

However, symptoms are quite common and can be caused by other conditions or lifestyle factors.

Not all men with low testosterone need treatment, and it is not always safe.

For more detailed information, you can contact Evgeniy Viktorovich for an in-person or online consultation.

Testosterone therapy in women

The use of testosterone in women is a more controversial topic than its use in men.

Normal levels of total testosterone in healthy adult women are 0.29–1.67 nmol/L.

Low testosterone levels in women can cause fertility problems, irregular periods, vaginal dryness and low sex drive. Despite this, doctors do not often recommend testosterone injections to treat low testosterone levels in women because they may have a masculinizing effect.

However, doctors may recommend testosterone therapy to help with hypoactive sexual desire disorder in postmenopausal women.

Research has not supported their use for other signs and symptoms that people may experience after menopause, including anxiety, mood changes, weight gain and decreased bone density.

Masculinizing hormone therapy

Testosterone therapy allows people to develop a more masculine appearance.

Transgender men may use testosterone injections as part of their gender transition.

Testosterone therapy helps a person develop masculine sexual characteristics and reduce feminine characteristics, and this may result in any of the following changes:

• changes in emotional and social functioning
• facial hair grows
• increase in body hair
• increase in acne
• deeper voice
• receding hairline with male pattern baldness
• changes in fat location
• increase in muscle mass
• absence of menstrual periods

Testosterone treatment regimens are similar to those used to treat hypogonadism in men.

Taking testosterone injections once a week may be the best way to maintain levels of this hormone.

Injectable testosterone preparations can be of several types.

These include:

• Testosterone cypionate (depot testosterone)
• testosterone enanthate (shorter-acting form)
• Testosterone undecanoate (long-acting drug)

How to use them?

When you receive an injection of testosterone, the hormone enters the body directly through the muscle bloodstream or through slow release from intramuscular stores.

You can choose between two methods of using the drug:

• self-administration of the drug at home (administration of short- and medium-acting drugs)
• injection of the drug into the gluteal muscle during a doctor's visit (injection of long-acting drugs)

When receiving testosterone injections, people usually visit their doctor every 2-3 months to monitor testosterone levels and prevent complications.

Treatment can be lifelong or short-term, depending on the patient's condition and treatment goals.

It is safe?

Testosterone injections can be safe if the patient follows the doctor's instructions. However, research has linked testosterone therapy to several side effects and possible complications.

Possible negative effects of testosterone therapy may include:

• increased risk of cardiovascular complications (if therapy is started for existing diseases of the cardiovascular system)
• worsening of symptoms in the lower urinary tract (growth of prostate adenoma, if the transformation of testosterone into dihydrotestosterone is not prevented)
• polycythemia, a rare type of blood cancer
• increased risk of venous thrombosis

Some people may have an allergic reaction to testosterone injections.

For example, testosterone undecanoate may cause a severe allergic reaction or breathing problems after injection. Symptoms may include breathing problems, dizziness and skin rashes.

Other forms of testosterone, including testosterone enanthate, may increase blood pressure, which may increase the risk of stroke or heart attack.

People who have had a stroke, heart attack, heart disease or high blood pressure should tell their doctor before starting testosterone injections as they may be at higher risk of complications.

If someone experiences any of the following symptoms after a testosterone injection, they should seek emergency medical attention:

• dyspnea
• slow or difficult speech
• chest pain
• weakness or numbness in an arm or leg
• pain in the arms, neck, back or jaw
• dizziness
• pallor

If a doctor prescribes testosterone injections for a teenager to treat constitutional delays in growth and puberty, the goal will be to achieve an accelerated growth spurt during puberty.

Summary

You may be given testosterone injections to restore your testosterone levels. It does not cure the underlying condition, but may help relieve some symptoms.

Women can also use these injections to treat sexual dysfunction that occurs as a result of body changes after menopause.

You should be aware of the possible serious complications of testosterone use, both in the short and long term.

It is important to always follow your doctor's instructions to reduce your risk.

How does testosterone deficiency manifest?

The effects of testosterone on the body are described above, respectively, deficiency can manifest itself in various symptoms, the most common are:

• depression
• decrease in concentration
• fatigue
• decreased muscle mass and strength
• decreased sexual desire
• erectile dysfunction - problems with developing and maintaining an erection
• infertility caused by a decrease in sperm count
• osteoporosis (cause of brittle bones)
• tides
• reduction in size and soft consistency of the testicles
• anemia (low red blood cell count)
• reduction in prostate size

Why can a man's testosterone levels be reduced in adulthood?

It has been established that testosterone levels in men begin to gradually decline from about the age of 30, by 1-2% every year. As a result, by the age of 50-55 (and in some cases even earlier), the testosterone content can be only about 1/2 of its amount at a young age. In addition, with age, the amount of a special protein in the blood that binds sex hormones increases, which also leads to a decrease in biologically active testosterone. A condition called age-related hypogonadism .

The amount of testosterone in adulthood and old age also depends on genetic (congenital) factors, such as the sensitivity of body tissues to the action of testosterone.

Various diseases of internal organs have an important impact on testosterone levels.

Hormone replacement therapy

Androgen hormone replacement therapy involves replenishing testosterone deficiency with various dosage forms of artificial testosterone.

Short-acting testosterone preparations:

• Sustanon-250 (manufactured by Organon , the Netherlands) – 1.0 ml. an oil solution of four testosterone esters, differing in the rate of delivery and duration of action.
• Omnadren-250 (manufactured by Jelfa , Poland) – 1.0 ml. oil solution of two testosterone esters, differing in the rate of entry into the blood and duration of action

After a single intramuscular injection, a sufficient concentration of testosterone in the blood is maintained for no more than 14 days.

Long-acting testosterone preparation:

• Nebido (manufactured by Bayer , Germany). Available in 4.0 ml bottles. testosterone undecanoate oil solution

After a single intramuscular injection, it maintains the physiological concentration of testosterone in the blood for 10 to 14 weeks.

Cutaneous form of testosterone

• Cutaneous form of testosterone in the form of Androgel gel (manufactured by Besins International Belgigue, Belgium). Available in the form of a gel in 5.0 gram bags. It is applied to certain areas of the skin and provides a stable physiological concentration of the hormone in the blood for 24 hours.

All dosage forms of testosterone are prescription drugs and are available only with a doctor's prescription.

Today, drugs with a questionable effect on testosterone levels include numerous dietary supplements - dietary supplements based on plant raw materials.

The most well-known plants for their production are: Tribulus terrestris, Ginseng, Eleutherococcus, African creeping palm root, etc. They are produced under different brand names and have more of a general tonic effect than an androgenic one.

What diseases can lead to testosterone deficiency?

In addition to physiological factors, acute and chronic diseases and medications can lead to hypogonadism, which ultimately increases the age-related decrease in testosterone levels.

Among diseases of internal organs, low testosterone levels can be caused by:

• chronic obstructive pulmonary disease, bronchial asthma
• cardiac ischemia
• arterial hypertension
• diabetes
• obesity
• cirrhosis of the liver
• chronic alcoholism

How do medications affect testosterone and sexual function?

Medicines taken for various diseases can negatively affect the level of testosterone in the blood. Therefore, self-administration of medications is unacceptable; only a doctor can prescribe treatment for you, taking into account possible adverse effects on sexual function.

What kind of medicines are these:

1. used for high blood pressure:

• methyldopa
• clonidine
• reserpine
• β-blockers (atenolol, anaprilin)
• prazosin

2. diuretics:

• veroshpiron
• hypotazid
• chlorthalidone

3. affecting the heart:

• digoxin
• verapamil
• antiarrhythmic drugs

4. affecting the central nervous system:

• antidepressants
• sleeping pills
• amphetamines

5. affecting the gastrointestinal tract:

• cerucal
• ranitidine

Publications in the media

(Testosteroni proplorras)

Synonyms. Oreton F.

Composition and release form. 1% and 5% oil solutions of testosterone propionate in 1 ml ampoules.

Indications. Sexual underdevelopment in men, delayed puberty, functional disorders in the genital area; breast and ovarian cancer in women; dysfunctional uterine bleeding; acromegaly.

Pharmachologic effect. Testosterone propionate is a synthetic analogue of the male sex (androgenic) hormone. Androgen secretion is regulated by gonadotropins. Androgens are responsible for stimulating spermatogenesis, the development of secondary sexual characteristics in men and the completion of puberty. Androgens are highly lipid soluble and penetrate target cells by passive diffusion. Under the influence of the enzyme 5-alpha reductase, testosterone in target cells is converted into 5-alpha-dihydrotestosterone. Testosterone and 5-alpha-dihydrotestosterone, through binding to cytosolic androgen receptors, initiate transcription in the cell nucleus, resulting in increased protein synthesis. Testosterone propionate, in addition to its specific androgenic effect, affects nitrogen and phosphorus metabolism. Thus, the drug has an anabolic effect.

Pharmacokinetics. Testosterone propionate is slowly absorbed from the injection site, but is more persistent in the body than testosterone. The connection with plasma proteins is high - 90-98%. Metabolized in the liver, excreted mainly in the urine in the form of metabolites.

Side effects. Women only: amenorrhea or oligomenorrhea, virilism; only in men: bladder irritation, urinary tract infections, breast tenderness, gynecomastia; swelling; erythrocytosis or polycythemia; nausea, vomiting, liver dysfunction.

Contraindications. Breast cancer in women; prostate cancer; increased sensitivity to androgens.

Adverse reactions when interacting with other drugs. When used together, indirect anticoagulants and testosterone propionate may increase the anticoagulant effect by reducing the concentration of the procoagulant factor in the blood. Androgens can reduce blood glucose concentrations, so to avoid hypoglycemia, it is necessary to adjust the dose of insulin when administered simultaneously. Androgens increase plasma concentrations of cyclosporine when used together, increasing the risk of nephrotoxicity.

Information for the patient. Oily solutions of testosterone propionate are administered intramuscularly or subcutaneously, the dose is selected individually taking into account the nature of the disease. Treatment is usually carried out over a long period of time; when the clinical picture improves, switch to maintenance doses.

How is testosterone level determined?

To find out what kind of testosterone you have, you need to take a blood test in the morning (preferably between 7 and 11 o'clock), since it is in the morning that the testosterone content in the blood is maximum. In addition, other special tests are needed - determination of the level of LH, protein that binds sex hormones, as well as a number of other tests that the doctor will prescribe based on the results of the examination.

At the same time, testosterone deficiency can be suspected by clinical symptoms. Several special questionnaires and scales have been developed for this purpose. By answering a few questions, you can guess whether testosterone is low or not.

Long-acting forms of testosterone in the treatment of hypogonadism

Definition and classification

Hypogonadism is a clinical syndrome caused by the inability to provide a physiological level of testosterone associated with dysfunction of one of the links of the hypothalamic-pituitary-gonadal (HPG) system with a normal sperm count.

There are primary and secondary testicular failure.

Primary testicular failure is a testicular disease manifested by low testosterone levels, impaired spermatogenesis and increased levels of gonadotropic hormones.

Secondary testicular failure is a disorder at the central level in the hypothalamus and pituitary gland, characterized by low or normal levels of gonadotropins and low testosterone levels.

This classification is important for the choice of treatment tactics, since with secondary hypogonadism, unlike primary, fertility can be restored with appropriate hormonal stimulation. In men with primary testicular failure, childbearing is most often impossible. Further evaluation of patients with secondary hypogonadism reveals pituitary tumors or systemic diseases.

Late-onset hypogonadism is an age-related syndrome characterized by typical clinical symptoms caused by low levels of testosterone in the blood. The presence of late hypogonadism worsens the patient’s quality of life and leads to dysfunction of many organs and systems. This term includes concepts such as andropause, androgen deficiency in old age, partial androgen deficiency in aging men. An age-related decline in testosterone levels is associated with dysfunction of both the testicles and the hypothalamic-pituitary axis. At the same time, testosterone levels decrease with age in men by an average of 1-2 per year, although a lower testosterone concentration compared to the lower limit of normal for a healthy young man is observed only in some elderly patients.

Less commonly, hypogonadism can serve as one of the manifestations of the pathology of the HGG system in men with a mutation of the DAX-1 gene, hemochromatosis, sickle cell anemia, thalassemia, during treatment with glucocorticosteroids, and alcoholism.

Clinical picture of hypogonadism

Diagnosing androgen deficiency in men presents certain difficulties. Clinical symptoms of hypogonadism are nonspecific and depend on age, comorbidities, severity and duration of the disorder, varying sensitivity to androgens, and previous testosterone therapy.

We list the symptoms and signs indicating the presence of androgen deficiency in men.

• Incomplete sexual development, eunuchoidity, aspermia.
• Decreased sexual desire (libido) and activity.
• Decreased frequency of spontaneous erections.
• Feeling of discomfort in the mammary glands, gynecomastia.
• Reduced amount of body hair (axillary and pubic), slow hair growth, particularly on the face.
• Reduced testicles.
• Infertility, absence or low sperm count in semen.
• Decreased height, fractures due to minor injuries, low bone mineral density.
• Reduced muscle mass and strength.
• Hot flashes, increased sweating.

The above clinical symptoms and signs were established based on a study by doctors of a population of patients being treated in the clinic, who are likely to have a more pronounced androgen deficiency; There have been no observations of men with classical androgen deficiency in the general population.

The threshold testosterone concentration below which symptoms of androgen deficiency occur and adverse health effects develop remains unknown and may be age dependent. Moreover, the testosterone concentration at which the drug is effective remains unknown and may vary depending on the individual patient and target organ.

Less specific symptoms and signs that occur with androgen deficiency include the following.

• Decreased energy, motivation, initiative, self-confidence; aggressiveness.
• Feeling sad, depressed, depressed mood.
• Decreased concentration and memory.
• Sleep disturbances, increased drowsiness.
• Mild anemia (normochromic, normocytic, within the range typical for women).
• Decreased physical activity and performance.

Thus, the data available today indicate that there is no clear threshold testosterone level at which lower levels would indicate clinical symptoms of androgen deficiency and which would be a criterion for diagnosing hypogonadism in all patients.

Laboratory diagnostics

Determination of testosterone levels. It should be noted that determination of testosterone levels is indicated only for patients with clinical signs of androgen deficiency. The most important parameters in identifying hypogonadism are total and estimated free testosterone, which is determined by calculating the level of total testosterone and sex hormone binding globulin (SHBG). It is important to determine testosterone between 7 and 11 am, when its level is highest.

It is believed that the minimum testosterone threshold level is not constant and depends on geographical and ethnic factors. However, the minimum level of testosterone at which hormone replacement therapy is not required has now been officially determined. Thus, the lower limit of normal is the level of total testosterone 12 nmol/l (346 ng/dl) and free testosterone 250 pmol/l (72 pg/ml). It was also determined that when the level of total testosterone is 8 nmol/l (231 pg/ml) and free testosterone is 180 pmol/l (52 pg/ml), hormone replacement therapy is indicated. With intermediate testosterone levels and the presence of symptoms of hypogonadism, the indication for hormonal therapy is to exclude other causes of the disease.

It must be remembered that in 30% of cases, a repeat test reveals a normal testosterone level. In addition, 15% of healthy young men may experience a decrease in testosterone levels compared to normal values ​​within 24 hours. Therefore, if a discrepancy between the clinical picture and laboratory diagnostic data is detected, it is better to repeat the tests.

The evaluation of a patient with androgen deficiency should include a general health assessment to rule out systemic diseases, the use of certain medications (eg, opiates or high-dose glucocorticoids) and recreational drugs that affect testosterone production and metabolism, eating disorders and excessive exercise, such as how these conditions may cause a transient decrease in testosterone levels. The diagnosis of androgen deficiency should not be made during the acute phase of a viral respiratory illness.

The following are groups of patients who are often found to have low testosterone levels. All of them are indicated for determination of androgen levels.

Conditions in which it is recommended to determine testosterone levels in the blood:

• Mass formation in the area of ​​the sella turcica, exposure to radiation in the area of ​​the sella turcica or other diseases of the sella area.
• The use of drugs that affect the production and metabolism of testosterone, such as glucocorticoids, ketoconazole and opioids.
• Weight loss during HIV infection.
• End-stage renal failure and hemodialysis.
• Moderate and severe chronic obstructive pulmonary diseases.
• Infertility.
• Osteoporosis or fractures due to minor injuries, especially in young men.
• Diabetes mellitus type 2.

Thus, diagnosing androgen deficiency in certain groups of patients makes it possible to identify patients with diseases that may seem unrelated to androgen deficiency. For them, testosterone therapy is also indicated and may be useful in treating the underlying disease.

Determination of FSH, LH and additional examinations. After identifying androgen deficiency, for the differential diagnosis of primary (testicular) and secondary (hypothalamic-pituitary) hypogonadism, determination of the level of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in the blood plasma is indicated. In men with primary testicular failure of unknown etiology, we recommend a karyotype study to exclude Klinefelter syndrome. In patients with suspected secondary hypogonadism, additional examinations are necessary to exclude pituitary tumors, hyperprolactinemia, hemochromatosis and other infiltrative processes, obstructive sleep apnea syndrome and genetic disorders associated with gonadotropin deficiency.

Imaging of the pituitary gland is recommended using magnetic resonance imaging (MRI) to exclude tumor, infiltrative processes, severe secondary hypogonadism (plasma testosterone level < 150 ng/dL), panhypopituitarism, persistent hyperprolactinemia, symptoms or signs of tumor compression, such as headaches, visual impairment, visual field defects.

Testosterone stimulates bone formation and prevents bone resorption. Numerous mechanisms underlie this effect of testosterone, including processes regulated by estrogen and androgen receptors.

It is recommended to determine bone density using dual-energy x-ray absorptiometry in men with severe androgen deficiency and with fractures due to minor injuries.

Treatment

The presence of clinical symptoms of hypogonadism and low testosterone levels confirmed by laboratory testing are an indication for hormone replacement therapy. Testosterone preparations can be used either as monotherapy or in combination with other drugs. Testosterone monotherapy may be effective in treating erectile dysfunction in men with hypogonadism. However, treatment with testosterone alone has a more pronounced effect on libido than on erectile function. During testosterone therapy, men with hypogonadism report improved ratings of sexual activity, more frequent thoughts and fantasies related to sex, increased attention to erotic stimuli, and an increase in the frequency and duration of nocturnal erections. There is an improvement in hair growth in some androgen-dependent areas, in addition, with testosterone therapy in healthy men with hypogonadism, muscle mass and strength increase, the volume of adipose tissue decreases, and an increase in bone mineral density is noted.

The use of testosterone improves mood. Uncontrolled studies have shown increased feelings of alertness and well-being after testosterone use. The effects of testosterone on cognitive function have been poorly studied, with some studies finding small effects on visual spatial perception, verbal memory, and fluent speech.

Thus, the use of testosterone is aimed at preserving secondary sexual characteristics in men, improving sexual function, maintaining good health and maintaining bone mineral density, i.e., correcting the main symptoms of hypogonadism.

When prescribing testosterone therapy, one should strive to increase its content to an average level within normal values.

Characteristics of testosterone preparations

Currently, there are various dosage forms of testosterone available that have proven effectiveness and safety. These include drugs for intramuscular administration, subdermal and transdermal use, and tablet forms. To successfully carry out hormone therapy, the doctor must clearly understand the pharmacokinetics of testosterone drugs, although the choice of one form or another of the drug depends on the patient’s preferences.

There is a risk of complications due to testosterone therapy. In this case, rapid withdrawal of the drug's effect may be required, which is only possible with treatment with short-acting forms of testosterone (transdermal, tablet and buccal preparations). Therefore, in late hypogonadism, short-acting drugs have an advantage over deposited forms (intramuscular, subcutaneous).

Preparations for oral use. Testosterone undecanoate (Andriol) is well absorbed when administered orally, but due to rapid breakdown in the liver, it does not adequately maintain sufficient levels of testosterone in the blood. 17-α-alkylated testosterone derivatives (especially methyltestosterone) are resistant to liver enzymes, but their use is currently limited due to proven hepatotoxicity.

Long-acting injectable forms of testosterone: thanks to the effect of esterification, a hydrophobic testosterone molecule was obtained, allowing the drug to prolong its effect. When the oil depot of hydrophobic testosterone is administered intramuscularly, it is slowly released, causing a prolonged effect.

Testosterone enanthate and testosterone cypionate (Testred Cypionate) have similar pharmacokinetic properties. In case of an overdose of these drugs, the levels of estradiol and dihydrotestosterone in the blood may exceed normal values. The usual daily dose of the drugs is 100 mg per week. 200–300 mg of testosterone enanthate is administered every 2–3 weeks. The maximum level of testosterone in the blood is achieved 5 days after administration of the drug, the initial level is achieved after 10–14 days. The advantage of these drugs is the low cost of treatment and the possibility of obtaining high concentrations of testosterone in the blood. Disadvantages include pain at the injection site and the need for frequent visits to the doctor to re-inject the drug.

Currently, a new parenteral form of testosterone undecanoate (Nebido) has been developed, which allows for a long-term, sustainable increase in testosterone levels in the blood. After two introductory doses of 1000 mg of the drug with an interval of 6 weeks, subsequent injections are made every 12 weeks, which allows maintaining normal testosterone levels in the blood in the vast majority of patients with hypogonadism. In some cases, the intervals between injections can be increased to 14 weeks.

Transdermal testosterone preparations. Transdermal forms of testosterone are available in the form of patches and gels. To achieve the best effect, their daily use is recommended. The daily dose of testosterone with this method of administration is 5–10 mg. The advantage of transdermal drugs is the ability to obtain stable testosterone levels throughout the entire duration of action. The most common side effect when using patches is skin irritation at the application site, which is not typical for the gel form. Individual characteristics of skin absorption may require doubling the daily dose.

Recommended testosterone replacement therapy regimens:

• IM administration of 75-100 mg of testosterone enanthate or testosterone cypionate (Testred Cypionate) weekly or 150 to 200 mg every 2 weeks.
• IM administration of Nebido once every 3 months or first 2 times after 6 weeks, then after 12 weeks.
• Application at night of one or two non-genital 5 mg testosterone patches to the skin of the back, thigh or shoulder, away from contact areas.
• Application of 5-10 g/day of gel containing testosterone to those areas of the skin that are covered by clothing.
• Use of buccal bioadhesive tablets at a dose of 30 mg 2 times a day.

This regimen should be considered as recommended for initiating testosterone replacement therapy; then the dose should be adjusted based on data on the concentration of testosterone in the blood plasma of each patient.

Men receiving testosterone supplements should be monitored according to a standard monitoring regimen. This allows side effects of therapy to be identified as early as possible. When monitoring men with hypogonadism receiving testosterone therapy, it is difficult to determine the indications for prostate biopsy. According to systematic reviews, after the initiation of testosterone therapy, PSA levels increased on average by 0.3 ng/ml in young hypogonadal men and by 0.44 ng/ml in older men. An increase in PSA levels after 3-6 months during testosterone therapy in men with androgen deficiency of more than 1.4 ng/ml is not typical. If this indicator is exceeded, you should pay attention to the condition of the prostate gland, perform TRUS; if questionable areas are identified along the periphery of the gland, a prostate biopsy is indicated. If the rate of increase in PSA exceeds 0.4 ng/ml over a period of less than 3 years, a detailed examination should be carried out and the patient should be monitored more closely.

Possible side effects

Undesirable effects that have been proven to be associated with testosterone use are the following:

• erythrocytosis;
• acne and oily skin;
• the appearance of subclinical prostate cancer;
• growth of metastatic prostate cancer;
• decreased sperm production and fertility.

Rare effects, the connection with the use of testosterone is not so obvious:

• gynecomastia;
• baldness (hereditary);
• progression of symptoms of benign prostatic hyperplasia;
• breast tumor growth;
• the appearance or progression of obstructive sleep apnea syndrome.

Specific undesirable effects of various forms of testosterone preparations:

• for tablets for oral use - effect on liver function and cholesterol levels (methyltestosterone);
• for implanted granules - infectious complications, expulsion of implanted granules;
• for intramuscular injections of testosterone enanthate or testosterone cypionate (Testred Cypionate) - fluctuations in mood and libido, pain at the injection sites, severe erythrocytosis (especially in older men);
• for a skin patch - skin reactions at the site of application;
• for skin gel - the potential risk of transferring testosterone to the skin of another person (the patient must be warned about the need to cover the areas of skin to which the gel is applied with clothing and to wash these areas of skin and hands with soap before close contact with another person);
• for buccal tablets - changes in taste sensations, irritation of the gum mucosa.

Risk factors and contraindications. Hormone replacement therapy has been used in women for a long time. Available indications of an increased risk of developing hormone-dependent diseases force us to pay attention to the possible consequences of hormone replacement therapy in men.

Conditions in which the use of testosterone is contraindicated:

• metastatic prostate cancer;
• mammary cancer;
• undiagnosed nodular formations or indurative process in the prostate gland;
• increased PSA levels of unknown etiology;
• erythrocytosis (hematocrit >50%);
• severe symptoms of lower urinary tract obstruction associated with benign prostatic hyperplasia, more than 19 points on the AUA/IPSS scale;
• severe course of heart failure (III and IV functional class).

Testosterone therapy may be associated with an increased risk of serious adverse effects in men for a number of conditions. Metastatic prostate cancer and breast cancer are hormonally dependent tumors, the growth of which can be stimulated by testosterone therapy; Testosterone should not be prescribed to men with these types of tumors. There is an opinion about the possibility of prescribing testosterone replacement therapy on the basis of an individual approach to patients with low testosterone levels after radical prostatectomy in the absence of signs of the disease for two or more years and if it is impossible to detect PSA in the blood, however, due to the lack of randomized trials, such an approach should not be considered as a recommendation for all patients.

The presence of a nodular formation or inducing process in the prostate gland, as well as an increase in PSA levels, sometimes indicate undetected prostate cancer. In addition, testosterone therapy may worsen the condition in men with erythrocytosis, untreated obstructive sleep apnea syndrome, severe symptoms of lower urinary tract obstruction, and severe heart failure.

Open studies in young hypogonadal men have shown a low incidence of side effects with testosterone replacement therapy. Frequent specific side effects of testosterone are increased hematocrit levels, acne, increased skin oiliness, and a feeling of tension in the mammary glands.

Literature

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I. A. Danilov, Candidate of Medical Sciences P. A. Shcheplev, Doctor of Medical Sciences, Professor of the KB of the Administration of the President of the Russian Federation, Moscow/p>

Androgen level rating scale

1. Do you notice a decrease in sexual desire (decreased pleasure from sex, lack of desire for sexual contact)? 2. Have you become less energetic? 3. Have you noticed a decrease in physical strength and endurance? 4. Has your height decreased? 5. Are you about (the feeling that the peak of life has been passed)? 6. Have you become sad and/or irritable? 7. Do you notice a decrease in the quality of erections? 8. Have you noticed a recent decline in your ability to participate in sports? 9. Do you fall asleep after lunch? 10. Has your performance decreased?

Testosterone deficiency is possible if the answer to questions 1.7 or any three other questions is positive.