After 40 years of age, men experience hormonal changes that significantly suppress physical and sexual activity, mental abilities. Outwardly, this is manifested by obesity in the abdominal region, a decrease muscle mass, deterioration of general health, sometimes depressive syndrome develops. For treatment, HRT for men is prescribed - testosterone replacement therapy. Preparations based on hormonal components help restore testosterone levels in the blood, thus avoiding harmful effects. Consider what hormone therapy is, to whom is it recommended, and what are its contraindications?

What is testosterone therapy?

Hormonal disorders in the body lead to serious complications from all organs and systems, without exception. Therefore, hormone replacement therapy after 40 years for men is often the only treatment that can significantly improve the quality of life and avoid health problems.

Hormonal drugs are prescribed not only to men over 40, but also at a young age, since testosterone deficiency is not always caused by age-related changes in the body. The cause may be trauma to the spermatic cord, cancer, genetic pathologies, etc.

It is worth knowing: symptoms of testosterone deficiency include a decrease / lack of libido, chronic fatigue, depression, aggressiveness and irritability for no reason, erectile dysfunction, obesity against the background of a previous diet, an increase in mammary glands. If there are 3 or more signs, it is recommended to consult a doctor and take a blood test for the level of androgens in the blood.

Testosterone replacement therapy was carried out at the dawn of the last century. But its beneficial effects were only confirmed 40 years ago. Moreover, there is still no unequivocal opinion whether such a method of treatment is needed or not, which is due to the most severe side effects, sometimes of an irreversible nature.

Previously, hormone therapy was carried out using tablets that included artificial testosterone. After taking them, metabolism took place in the man's liver, where most of the active substance was destroyed. As a result, the liver "suffered" from the negative effects of carcinogenic and toxic components. This resulted in a broken functionality internal organ, which became the reason for the prohibition of such treatment in many countries of the world.

However, when similar drugs appeared that were not characterized by such adverse reactions, the ban was lifted. Often these medicines are used by men who are professionally involved in sports, although it is prohibited.

HRT with testosterone has strict medical indications:

• Natural andropause, due to which there is a pronounced deficiency of testosterone in the blood;
• Pathological conditions, regardless of the age group of a man, are accompanied by hormonal disorders. For example, diseases of the pituitary gland, gynecomastia, cryptorchidism, obesity, which cannot be treated with traditional methods.

Hormone therapy for men is carried out only on the basis of laboratory test results. When prescribing drugs with synthetic testosterone, all risks are necessarily assessed.

Methods for administering androgens

In modern medical practice, the introduction of androgens is carried out different ways... Each method is characterized by its own advantages and disadvantages, therefore the choice is always made on an individual basis, taking into account the condition of the man, concomitant diseases, clinical manifestations, and other factors.

Oral

Oral hormone replacement therapy for men involves the use of tablets / capsules by mouth. They contain the active ingredient in the required dosage. Pills are the very first form of hormonal drugs.

The advantages of the method:

1. Ease of use.
2. Possibility of urgent withdrawal of the drug.
3. Independent use without visiting the clinic.
4. Relatively low cost.

Important: tablets / capsules are effective only for mild androgen deficiency in the male body.

The tablet / capsule form is sold by prescription only. It is not recommended to buy online and in questionable stores, since this form of the drug is easiest to counterfeit. The replacement process is carried out with the help of such drugs:

• Andriol. The dosage is 150-200 mg per day;
• Streant is taken at 30 mg three times a day;
• Proviron. The dose will vary depending on the level of androgens in the blood. Assign from 30 to 80 mg per day.

The tablets must be taken in the dosage prescribed by a medical professional. During treatment, you should constantly monitor the concentration of hormones in the blood.

Injectable

According to many doctors, it is necessary to "harmonize" by the injection method, since this is the only way testosterone enters the body smoothly and naturally. Most clinical pictures use cypionate and enanthate for testosterone therapy. Literally 100 mg of the drug provides a weekly supply of androgens for the male body. The dose is always individual - some men need less, others much more.

The weekly dose is divided into two applications, administered at regular intervals, which ensures a stable concentration of hormonal substances in the body. The following drugs are used:

1. Delasteril. The dose ranges from 200 to 400 mg.
2. Nebido. Enter once every three months.
3. Sustanol. The introduction of 250 mg is carried out every 1-2 weeks.

Fact: Among all hormonal medicines, it is Nebido that is characterized by the most prolonged effect - one injection every 90 days and the minimum list of side effects.

The advantages of injection include the ability to create a high concentration of hormones in the blood; a wide range of new generation drugs.

Transdermal

There are other ways to "replace" the hormone in men. For this, plasters, creams and gels are used. Local agents provide a gradual intake of the active component into the male body, which reduces the risk of side effects. Nevertheless, according to medical experts, the therapeutic effectiveness of this method is the lowest.

HRT in men by the transdermal method is carried out using drugs:

• Androderm or Testoderm - plasters. They are used every day in a maximum dose of 7.5 mg of the hormonal substance;
• Andromen is a hormonal cream. The daily dosage is 15 mg;
• Andractim is a drug in the form of a gel, the dose is always determined individually.

During hormone therapy with gels and creams, do not swim after applying medications. It is strictly forbidden for women and children to touch the treated area of \u200b\u200bthe skin, as this poses a health hazard. A significant disadvantage is that it must be applied several times a day, which significantly reduces the quality of life and the usual way.

Subcutaneous

Subcutaneous hormone therapy involves the use of an implant. The method is quite effective, however, testosterone implants are not registered in Russia, which does not allow many representatives of the stronger sex to use this option.

For your information, the main advantage of the method is the uniform release of testosterone throughout the entire period of the implant's operation - 6 months.

The disadvantage of the method is surgical intervention, since the operation appears to be the only way to install the implant. Therefore, the risk of complications after surgery is added to the side effects of hormonal treatment.

Contraindications for substitution therapy

Hormone replacement treatment is a serious step, so before prescribing drugs, you need to make sure that there are no medical contraindications. In addition, the doctor must tell the man about the likely side effects. Contraindications are relative - the use of hormonal drugs is allowed, but with caution and absolute - such treatment is strictly prohibited.

Testosterone replacement therapy is not performed if a man is diagnosed with breast cancer (this is rare). The use of androgens can provoke an increase in the concentration of estrogens, which leads to the progression of the oncological process.

Important: testosterone replacement therapy is prohibited against the background of cancer of the glandular organ in men. Oncology must be excluded before treatment. For this, a rectal examination of the organ is performed, the level of PSA - prostate specific antigen - is determined.

The use of hormones is carried out with caution in the following pathological conditions and diseases:

1. Sleep apnea.
2. Gynecomastia.
3. Retention of fluid in the body.
4. Puffiness.
5. Polycythemia.
6. Hyperplasia of the prostate.

In the presence of relative contraindications, constant monitoring by a medical specialist is required. The introduction of hormonal drugs can lead to serious complications - suppression of the production of own testosterone, inhibition of spermatogenesis, alopecia, atrophic changes in the testicles, etc.

The final choice of the method of hormone replacement treatment depends on the general condition of the patient, concomitant diseases and individual tolerance of certain medications. Testosterone in any form should be prescribed exclusively by a doctor, independent use is fraught with serious consequences.

Prevention of testosterone reduction is the correct lifestyle (quitting smoking, alcohol, drugs), consuming organic products, controlling your own weight, and timely treatment of any diseases.

For young androgen-deficient men, testosterone treatment has many benefits and is associated with a low risk of serious adverse effects. In a systematic review of most open-label studies in healthy androgen-deficient men, testosterone treatment was associated with significant beneficial effects on muscle tissue, maximum voluntary strength, and vertebral bone mineral density, as well as significant reductions in whole body fat mass.

Testosterone treatment improves performance and sex drive. The purpose of this hormone affects many areas of sexual function: it increases the frequency of spontaneous sexual thoughts, improves responsiveness to erotic stimuli, and increases the frequency and duration of nocturnal penile erections. Therapy does not alter the erectile response to visual erotic stimulus or the frequency of orgasms in hypogonadal men, although it does increase ejaculate volume. Open-label studies have shown that therapy improves the positive and decreases the negative aspects of mood; data from randomized clinical trials on the effect of therapy on mood are limited and do not show significantly greater improvement in mood compared to placebo.

However, androgen-deficient men report improved feelings of health and energy after starting testosterone treatment. Some studies describe small and inconsistent effects on visuospatial recognition, auditory memory, and fluency. Studies of the effects of therapy on insulin sensitivity have produced conflicting results. Most of the studies were open-label, with patient selection based on low testosterone concentrations.

Testosterone preparations

Substitution therapy can be prescribed using one of several available dosage forms.

Testosterone esters given by injection

Esterification of testosterone in the 17-p-hydroxyl position makes the molecule hydrophobic and increases the duration of its action. The slow release from the oil depot in the muscle explains its extended duration of action. More side chain, more hydrophobicity of the ester and longer duration of action. Thus, testosterone enanthate and cypionate with longer side chains have a longer duration of action than propionate. De-esterification of esters occurs quickly in plasma, is not limited in speed and cannot explain the long duration of action.

Within 24 hours after intramuscular administration of 200 mg of testosterone enanthate or cypionate, serum hormone levels rise to the upper normal range or to the supraphysiological range and then gradually decline to the hypogonadal range over the next 2 weeks. The twice-monthly regimen of enanthate or cypionate results in peaks and troughs in serum testosterone levels, which can be associated with changes in the patient's mood, sexual desire, activity level, and alertness. With appropriate monitoring, adequate tolerated doses of injectable testosterone formulations can be selected (they are the least expensive drugs available).

Percutaneous Testosterone Gel

There are two testosterone gels available on the market. Pharmacokinetic studies have confirmed that 5-10 gram doses applied daily to the skin can increase and maintain serum total and free testosterone concentrations in the mid-normal range in hypogonadal men, although significant variations are possible throughout the day in individual patients. Currently, it is recommended to start at 5 g and adjust the dose based on serum levels of the hormone.

The advantages of testosterone gel are ease of application, its invisibility after application and flexibility in dosage. The main feature of using the gel is the potential for its transfer to a sexual partner or child who comes into close contact with the patient. Skin tolerance is good, skin irritations are rare.

Transdermal Testosterone Patch

One or two 5 mg extra-sex testosterone patches may be applied to the skin outside the scrotum. Testosterone and estradiol levels are in the mid-normal range for 4-12 hours after patch application. Extra-sex patches provide physiological serum testosterone levels. One 5 mg patch may not be sufficient to increase serum hormone concentrations to the mid-normal range in all hypogonadal men, and some patients may require two 5 mg patches daily to achieve the target level. In some patients, skin irritation is associated with the use of extra-sex patches.

Bioadhesive testosterone tablets

Bioadhesive 30 mg testosterone controlled release tablets applied every 12 hours to the buccal mucosa normalize serum hormone levels in hypogonadal men. In 16% of treated men, the use of cheek pills was associated with gum problems.

Crystalline testosterone implants are inserted into the subcutaneous tissue using a trocar through a small skin incision. The hormone is released by surface erosion of the implant and is absorbed into the systemic circulation. Four to six 200 mg implants can maintain serum concentrations in the mid-normal and high-normal range for 6 months. The need for a skin incision for insertion and removal, spontaneous extrusion and fibrosis at the site of implant insertion are potential drawbacks of this dosage form.

The intramuscular form of testosterone undecanoate in the form of an oily solution can maintain serum hormone levels in the normal range for 10-12 weeks after intramuscular injection. The usual regimen of testosterone undecanoate administration includes an initial injection of 1000 mg of the drug intramuscularly, a second injection of 1000 mg after 6 weeks, and then intramuscular injections of 1000 mg every 12 weeks. The relative advantage of this injectable form is its long-lasting effect and weaker fluctuations in serum hormone levels. However, undecanoate is prescribed in a large volume of oil, which causes discomfort in the patient.

Orally administered testosterone derivatives

Testosterone is well absorbed after oral administration, but rapidly undergoes first pass metabolism. This is why it is impossible to achieve stable blood levels after ingestion of a crystalline preparation. Alkylated derivatives are relatively resistant to hepatic degradation and can be administered orally, however, due to the potential hepatotoxicity and the availability of alternative and safer dosage forms, alkylated testosterone derivatives are not recommended for replacement therapy.

The latest androgenic dosage forms

A number of newer dosage forms of androgens with better pharmacinetics or more selective activity profiles are under development. The dosage form of biodegradable testosterone microspheres provides physiological levels of the hormone for 10-11 weeks. Long-acting esters - bucyclate and undecanoate when injected intramuscularly can maintain circulating testosterone concentrations in the male range for 7-12 weeks. Initial clinical trials have shown that testosterone can be administered by the sublingual or buccal route.

Contraindications to testosterone treatment

Testosterone therapy should not be used in men with metastatic prostate cancer, breast cancer, as it can promote the growth of these tumors. Therapy can worsen preexisting erythrocytosis, untreated severe obstructive sleep apnea, and severe congestive heart failure. Because a prostate lump, induration, or elevated PSA levels can be indicators of unrecognized prostate cancer, men with these conditions should have a urologic evaluation before considering testosterone treatment.

It is not known how safe testosterone treatment is for men who have undergone radical prostatectomy for localized prostate cancer and appear to be cured; some experts believe that therapy can be prescribed on an individual basis to such men, if they have not found PSA for more than 2 years. However, there is insufficient data to recommend this approach.

Testosterone side effects

The incidence of adverse effects associated with testosterone treatment in open-label studies in young hypogonadal men was low. The most common T-linked adverse effects are erythrocytosis, acne, oily skin and breast tenderness. Although there are reports of gynecomastia and induction or worsening of obstructive sleep apnea, the incidence of these adverse effects during therapy is low.

The widespread belief that testosterone treatment increases the risk of atherosclerotic heart disease is not supported by the available evidence. The long-term implications for the risk of heart disease remain unknown. Although supraphysiological doses of androgens commonly used by bodybuilders and athletes reduce plasma HDL levels, physiological testosterone replacement in older men has been associated with only moderate or no plasma HDL reductions. Profile studies of middle-aged men have revealed a direct rather than inverse relationship between serum hormone levels and HDL plasma concentrations and an inverse correlation between testosterone levels and visceral fat volume.

Open-label studies of testosterone use mainly in young hypogonadal men have shown small reductions in total cholesterol, HDL cholesterol, and LDL cholesterol in plasma. Placebo-controlled studies in older men have not found significant changes in blood HDL levels with long-term testosterone administration.

Spontaneous and experimentally induced androgen deficiency is associated with increased adipose tissue mass. Testosterone treatment reduces adipose tissue mass in older men who have low levels hormone. There have been reports of a decrease in visceral fat volume, serum glucose concentration and blood pressure, and an increase in insulin sensitivity with testosterone supplementation in middle-aged men.

Effects of testosterone on the risk of atherosclerotic heart disease

Research data suggest that both supraphysiologic and subphysiologic circulating testosterone concentrations are associated with increased cardiovascular risk, although the evidence for this is far from conclusive. The effects of testosterone treatment on the progression of atherosclerosis and the incidence of cardiovascular events have not been studied in men in randomized clinical trials, but they are important because even small changes in the incidence of cardiovascular disease can have a significant impact on the health of the population.

Testosterone and prostate cancer risk

There is no proven evidence that testosterone treatment is a cause of prostate cancer. There is also no consistent relationship between endogenous serum hormone levels and prostate cancer risk. However, there are a number of concerns.

Many older men have microscopic foci of cancer in their prostate gland. It is not known if the therapy will increase these subclinical cancer loci and make them clinically apparent.

Prostate cancer is a typical androgen-dependent tumor, and androgen therapy can promote its growth. That is why therapy is contraindicated in men with metastatic prostate cancer.

An increase in PSA levels during testosterone therapy may trigger examination and biopsy in some patients. More intensive PSA screening and follow-up of men on T-therapy can lead to an increased number of prostate biopsies and detections of subclinical prostate cancer that would otherwise go unnoticed.

Testosterone replacement therapy can be safely prescribed for men with benign prostatic hyperplasia who have mild to moderate symptom scores. Androgen deficiency is associated with reduced prostate volume, and androgen replacement increases prostate volume to levels in age-matched controls. In patients with pre-existing severe symptoms of adenoma, even a small increase in prostate volume can increase the symptoms of obstruction. For these men, testosterone should either not be used or given with close monitoring of obstruction symptoms.

Testosterone treatment and erythrocytosis

Testosterone preparations dose-dependently increase erythrocyte mass, apparently through effects on erythropoietin and stem cell proliferation. That is why testosterone replacement is not indicated for men with a baseline hematocrit of 50% or higher without appropriate examination and treatment of erythrocytosis. The administration of the hormone to young men with androgen deficiency is usually associated with a slight increase in hematocrit. Clinically significant erythrocytosis is uncommon in young hypogonadal men during treatment, but it can occur in men with severe smoking or COPD sleep apnea.

The increase in hemoglobin during therapy is higher in the elderly than in younger men. Erythrocytosis is the most common drug-induced adverse effect and also the most common reason for discontinuing therapy. Treatment with transdermal systems has been found to cause less increases in hemoglobin levels.

Testosterone treatment should be discontinued when the hematocrit level exceeds 54%, and therapy should be abstained from until the hematocrit drops to less than 50%, after which therapy can be restarted at a lower dose.

Testosterone is converted by aromatization to estradiol in many peripheral tissues and can exacerbate, so it should not be given to men with breast cancer.

Testosterone can induce sleep apnea syndrome or exacerbate existing sleep apnea syndrome due to its neuromuscular effects on the upper respiratory tract, and it should not be given to men with severe obstructive sleep apnea syndrome without appropriate evaluation and treatment. Men with sleep apnea syndrome may have low levels of this hormone.

Testosterone administration can transiently induce sodium and water retention and should therefore not be given (or given with great caution) to patients with severe congestive heart failure and Class 4 symptoms.

Monitoring testosterone therapy

According to the recommendations of the Endocrinological Society, men receiving testosterone treatment should be evaluated 3 months after the start of therapy and then annually using a standard monitoring plan for the effective correction of symptoms and signs associated with this hormone deficiency, and to facilitate early detection of adverse effects. Therapy should be aimed at raising serum hormone levels to the mid-normal range. Even in primary testicular failure, serum luteinizing hormone (LH) levels are not normalized by doses of testosterone that restore sexual function and induce clinical improvement. This is why serum LH levels have not been used to monitor the adequacy of treatment in men with androgen deficiency. Determinations of hemoglobin, hematocrit, PSA concentration and digital prostate examinations should be performed at regular intervals in addition to general health examinations, as recommended by local standards.

Medicinal	Therapy regimen	Pharmacokinetic	Dihydrotestosterone and estradiol	Benefits	disadvantages
T-enanthate or cypionate	10 and mg / week or 20 and mg at 2 weeks intramuscularly	After one intramuscular injection, serum testosterone levels rise above the physiological range and then gradually decline to the hypogonadal range towards the end of the dosing interval	Dihydrotestosterone and estradiol levels rise in proportion to the increase in testosterone concentrations	Corrects symptoms of androgen deficiency; relatively inexpensive if administered alone: dosage flexibility	Requires intramuscular injection, peaks and troughs in serum hormone levels
Extrasexual percutaneous system	One or two patches, nominally delivering 5-10 mg testosterone over a 24 hour period, applied daily to non-pressurized areas	Restores serum testosterone and estradiol levels to physiological levels in men	Levels are in the physiological range for men	Ease of use, corrects symptoms of androgen deficiency and mimics the normal daily rhythm of secretion; increases hemoglobin less than esters given by injection	Serum testosterone levels in some men with androgen deficiency may be in the lower normal range; these men may need to apply two patches daily, skin irritation at the site of attachment can be a problem for some patients
Testosterone	5-10 g of gel containing 50-100 mg testosterone should be applied daily	Restores serum testosterone and estradiol levels to physiological levels in men	Serum DHT levels are higher and the T: DHT ratio is lower in hypogonadal men treated with the gel than in healthy men with normal sex gland function	Corrects symptoms of androgen deficiency, provides dosing flexibility. ease of use, well tolerated by the skin	Potential transfer to a female partner or child through direct skin-to-skin contact; moderately high levels of DHT
17- methyl testosterone	This 17a alkylated derivative should not be used due to the potential for liver toxicity	Actively when taken orally			Clinical responses are variable; potentially toxic to the liver; should not be used to treat androgen deficiency

Table continuation

Cheek bio- adhesive testosterone tablets	30 mg bioadhesive controlled release tablets, used twice daily	Absorbed through the buccal mucosa	Normalizes serum testosterone concentrations in hypogonadal men	Corrects symptoms of androgen deficiency in healthy hypogonadal men	In 16% of patients, adverse effects associated with the gums
	40-80 mg orally 2-3 times a day with meals	When given in oleic acid, T-undecanoate is absorbed through the lymphatic vessels of the portal system significant variability in the same patient on different days and among different patients	High DHT: T ratio	Convenience of ingestion	Not permitted in the United States; variable clinical responses, variable serum testosterone levels, high DHT: T ratio
Injectable, long acting T-undecanoate in oil	1000 mg, injected intramuscularly, followed by 1000 mg after 6 weeks and then 1000 mg every 12 weeks	When given at a dose of 1000 mg intramuscularly, serum levels are maintained within the normal range in most men	DHT and estradiol levels rise in proportion to the increase in testosterone concentrations; ratios T: DHT and T: E 2 do not change	Corrects symptoms of androgen deficiency; requires infrequent appointments	Requires high volume intramuscular injection (4 ml)
Testosterone implants	4-6 implants 200 mg subcutaneously	Serum testosterone peaks at 1 mo and is then maintained in the normal range for 4-6 mo	T: DHT ratios do not change	Corrects symptoms of androgen deficiency	Requires a surgical incision for insertion; spontaneous extrusions

The form	Dosing
T-enanthate or cypiopath	75-100 mg / week or 150-200 mg every 2 weeks given intramuscularly
Extra-Sexual Testosterone Patches	One or two 5 mg patches applied at night to the skin of the back, thigh, or upper shoulder, away from areas of pressure
Testosterone gel	5-10 g applied to the covered areas of the skin
Bioadhesive cheek testosterone tablets'	30 mg tablets superimposed on the buccal mucosa 2 times a day
T-undecanoate for oral administration	Usually 40-80 mg by mouth 2 or 3 times a day with meals
T-undecanoate for injection	Usually 1000 mg intramuscularly at the beginning and after 6 weeks and then 1000 mg every 12 weeks
Testosterone implants	4-5 implants 200 mg subcutaneously every 4-6 months

The article was prepared and edited by: surgeon

Currently, the most popular form of therapy for androgen deficiency is testosterone replacement therapy.

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The first reports on the successful treatment of androgen deficiency were dated back to the 40s of the last century. However, the drugs of that time had many side effects and did not have the full spectrum of action of natural testosterone.

The first popular synthetic testosterone preparations were sold in the form of tablets (methyltestosterone, fluoxymesterone, etc.). Oral administration exposed testosterone to metabolism in the liver, as a result of which most of it was destroyed, while exerting a strong toxic and carcinogenic effect on the liver. In this regard, in most countries, drugs based on these derivatives of testosterone are prohibited for use, giving way to modern analogues.

A great influence on the development of synthetic forms of testosterone is played by its role in sports. Despite the fact that the use of anabolic steroids is prohibited, drug control incidents continue to rage at the Olympic Games and other major events.

Forms of administration of testosterone preparations

The methods of administration of androgens are subdivided into the following:

• oral (tablets, capsules);
• injection (injection);
• transdermal (patches, gels, creams);
• subcutaneous (implant).

Table 1 - Exogenous testosterone preparations (S. Yu. Kalinchenko, I. A. Tyuzikov, 2009)

GROUP OF PREPARATIONS	CHEMICAL NAME	TRADENAME	DOSAGE
Injection forms	Testosterone Cypionate	Depot testosterone cypionate	200-400 mg every 3-4 weeks
	Testosterone Enanthate	Delasteril Testosterone Depot	200-400 mg every 2-4 weeks
	Testosterone Ester Blend	Sustanol-250 Omnadren-250	250 mg every 2-3 weeks
	Testosterone Undecanoate	Nebido	1000 mg every 3 months
Oral forms	Fluoxymesterone *	Halotestin	5-20 mg daily
	Methyltestosterone *	Metadrene	10-30 mg daily
	Testosterone undecanoate	Andriol	120-200 mg daily
	Mesterolone ***	Proviron Vistinone Vistimon	25-75 mg daily
	Buccal tablets	Striant	30 mg 3 times a day
Subcutaneous forms	Implants	Testosterone implants	1200 mg every 6 months
Transdermal forms	Testosterone gel	Androgel	25-75-100 mg daily
	Testosterone patches (scrotal and cutaneous) **	Androderm Testoderm	2.5-7.5 mg daily
	Testosterone cream	Andromenes	10-15 mg daily
	Dihydrotestosterone Gel (DHT Gel)	Andractim	Individually

Notes: * - hepatotoxic and prohibited in some countries; ** - not registered in Russia; *** - out of production.

Choosing a drug

Figure: 1 - The share of various forms of androgenic drugs in the pharmaceutical market of Russia (2007) (source "Practical Andrology", S. Yu. Kalinchenko IA Tyuzikov, 2009).

Intramuscular testosterone injections are the most commonly used replacement therapy method. The most famous testosterone esters - testosterone cypionate and testosterone enanthate have their own characteristic features: getting into the bloodstream, the testosterone level reaches its maximum value 2-3 days after injection, after which it gradually decreases over 2 weeks and reaches its minimum. This causes the so-called. The roller-coaster effect, when mood, well-being and libido rise along with the level of androgens in the blood, and just as sharply declines when it is at the minimum level. The same properties are possessed by preparations containing a mixture of testosterone esters (Sustanol, Omnadren).

A sharp change in the concentration of androgens in the blood, often felt by the patient himself, is an undesirable effect when using testosterone preparations.

Nevertheless, both individual testosterone esters and their mixtures are still successfully used due to their low cost, availability and effectiveness. In particular, testosterone esters are loved by strength athletes and bodybuilders for their anabolic properties and for their ability to create high concentrations of testosterone in the blood.

Testosterone undecanoate (Nebido) is currently the injectable drug of choice for hormone replacement therapy (HRT). It differs from other testosterone esters in its prolonged action (1 injection every 10-12 weeks) and the absence of pathological surges in the level of androgens. The drug Nebido has the full spectrum of testosterone action and does not cause hepatotoxic and hepatocarcinogenic effects.

Oral drugs have little effect compared to injectables, even at high doses. Therefore, it is advisable to use oral testosterone in cases where there is a slight decrease in androgens. The drug of choice for HRT is Andriol. Compared with the old analogues (methyltestosterone, fluoxymesterolone), when using Andriol, most of the testosterone bypasses the metabolism in the liver and enters the systemic circulation directly, which contributes to the rapid achievement of the required hormone concentration. However, this also causes a fast half-life of the drug (3-4 hours), which forces the patient to take it again (3-4 times a day).

Transdermal forms of testosterone preparations (gels, patches) are gaining more and more popularity. They quickly create the necessary level of androgens in the blood, but at the same time they do not undergo hepatic metabolism like oral drugs, and at the same time do not create a supraphysiological level of testosterone, as is the case with the use of testosterone esters (cypionate, enanthate) and a mixture of esters (Sustanol, Omnadren) ... The advantage of transdermal forms is their non-invasiveness, the possibility of independent use, and the absence of pronounced side effects.

In some countries, implants are a common treatment for androgen deficiency. With the help of surgical intervention, the implant is placed subcutaneously in the patient, releasing the hormone evenly for 6 months. Testosterone implants are not registered in Russia.

Figure: 2 - Pharmacokinetics of various testosterone preparations.

Table 2 - Characteristics of various forms of testosterone preparations

	INJECTION	ORAL	TRANSDERMAL	SUBCUTANEOUS
The effectiveness of therapy	+ Highly effective. The ability to create high concentrations of the hormone in the blood	— Effective only for mild androgen deficiency	+ Effective enough to overcome varying degrees of androgen deficiency	+ Effective
Availability	+ A wide variety of testosterone esters available on the market	+ Availability by prescription	+/- Availability of only testosterone gel (AndroGel) on sale. Testosterone patches are not registered in Russia	— Testosterone implants are not registered in Russia
Duration of action	+ Nebido has the longest duration of action of all testosterone preparations (1 injection every 3 months)	— Daily from 2-4 times a day (Andriol)	— Daily, once a day	+ The duration of action of one implant is 6 months.
Possibility of urgent stopping of therapy	—	+	+	—
Sharp fluctuations in hormone levels	+ Not detected when using Nebido-It is noted when using testosterone propionate, testosterone enanthate and a mixture of esters	— Have a fast half-life	+ Absorbs evenly throughout the day, keeping hormone levels within normal limits	+ Uniform release of testosterone over the life of the implant
The possibility of independent use	+/- The procedure is performed by a specialist, but the possibility of independent use is not excluded	+	+	— Requires surgical intervention
Feature of side effects	Depending on the dosage	Have some liver toxicity, especially older drugs	May cause skin reactions where the drug comes in contact with the skin	Complications caused by surgery

With age, a man's body changes hormonal levels. As a rule, this starts at the age of 35–40, but in each case the process proceeds individually, and the terms may be different, both upward and downward.

The main male hormone is testosterone, which is responsible for sex, temperament, reproductive function and sexual performance. Starting from the age of 25, the amount of androgen produced gradually decreases, and by the age of 40, its concentration decreases by 25%.

The main symptoms of testosterone deficiency in men are:

• irritability, aggressiveness;
• decreased sex drive;
• erectile disfunction;
• fast fatiguability;
• decrease in muscle mass;
• hair loss on the head and body;
• weight gain, deposition of adipose tissue on the abdomen, thighs, breasts.

With a significant deficiency of testosterone, the size of the testicles decreases, gynecomastia develops, the figure changes according to the female type.

When hormonal drugs are prescribed

You can increase testosterone levels with the help of active physical activity, lifestyle changes, proper, balanced nutrition, and rejection of bad habits. If these methods do not help to normalize androgen levels, male hormones are prescribed as replacement therapy.

Are registered medications based on the results of a blood test, examination and questioning of the patient. The doctor selects the dosage and treatment regimen individually for each patient. Indications for taking hormonal drugs may be impotence, weak erection or infertility.

Types of hormonal drugs

Hormones for men used for replacement therapy are available in the form of capsules, solution for injection, patches, subcutaneous implants and gels for external use.

Gel preparations are considered to be the most effective; they are applied to the skin and ensure uniform absorption of the active substance within a short period of time. The disadvantages include local irritation of the epidermis, allergic reactions and discomfort while wearing clothes and bathing.

The main advantages of the drug are:

• no negative effect on the liver;
• aromatization of testosterone does not occur;
• own production of the sex hormone is not suppressed;
• there are fewer side effects.

The disadvantages include low bioavailability, the need for constant intake and high cost.

Patch Androderm

Another means for carrying out hormone replacement therapy is the Androderm pectoral patch. This is a transdermal preparation that ensures a uniform flow of the hormone into a man's body for 24 hours. During treatment, there are no sharp jumps in testosterone levels, the patch does not cause difficulties during application, has fewer side effects than drugs for oral administration.

The patch is fixed to the shoulders, hips, abdomen, or back. The only drawbacks are the possibility of skin irritation, the need for daily replacement, difficulties during hygiene procedures.

Injection therapy

The drugs for intramuscular injection are Nebido and Sustanon-250. The main active ingredient is a testosterone ester, additionally castor oil is present in the composition of the drug.

An injection of Nebido is given once every 10-14 weeks, Sustanon-250 - once every 3 weeks. The oily substance, getting into the body, is gradually released from the reserve depot, maintaining the testosterone concentration at the required level without sudden jumps. Treatment is carried out under constant monitoring of the concentration of androgen in the blood.

Based on the results of the analysis, the doctor adjusts the dosage, can increase or decrease the interval between injections.

Side effects of hormone replacement therapy

Hormonal drugs for men can cause the following side effects:

• aggressiveness, nervousness;
• muscle weakness, fatigue;
• acne on the face and body;
• increased sex drive;
• alopecia;

• in adolescents, early puberty;
• nausea, vomiting, diarrhea;
• suppression of the production of your own hormones;
• withdrawal syndrome;
• testicular atrophy;
• increased blood pressure;
• body swelling;
• prostate cancer.

To exclude the possibility of side effects, it is necessary to undergo a course of treatment under the supervision of a doctor, strictly adhere to the prescribed dosage of drugs, and do a control blood test for testosterone levels every 2 months.

Bibliography

1. Ivanova N.A. Syndromic pathology, differential diagnosis and pharmacotherapy.
2. Internal diseases in 2 volumes. Ed. A.I. Martynova M .: GEOTARD, 2004. (stamp UMO)
3. A guide for emergency medical doctors. help. Edited by V.A. Mikhailovich, A.G. Miroshnichenko. 3rd edition. SPb, 2005.
4. Clinical guidelines. Rheumatology. Ed. E.L. Nasonov- M.: GEOTARD-Media, 2006.
5. Kugaevskaya A.A. Modern principles of diagnosis and treatment arterial hypertension. Tutorial... Yakutsk: YSU Publishing House. 2007

Failure in the production of androgens leads to serious complications in the male body, which is why hormone replacement therapy for men can be a salvation for them. But for many, this issue is considered controversial, because the artificial administration of hormones can be dangerous. To hormone therapy for men was not so scary, you need to understand it in detail.

Hormone deficiency: causes and when therapy is indispensable

Hormone therapy for men over 40 is almost a natural process, but sometimes younger people may need such treatment. Aging is not always the reason for a decrease in testosterone production by the endocrine glands. Any injury to the testis can lead to such a deficiency. This is facilitated by oncological pathologies and / or a number of genetic diseases. An excess of iron in the body, which will suppress testosterone, is no less dangerous. Incorrect work of the pituitary gland, row medicines, chronic diseases, including alcoholism and tobacco smoking, inhibit the production of vital androgens.

Important! In the presence of symptoms of androgen deficiency, men under 40 should undergo an appropriate examination, and after 40 - do it regularly, even if there is no clinical picture of testosterone deficiency.

Hormone replacement therapy for men can be prescribed only after diagnosing the amount of hormones in their blood. This analysis is true and accurate. When will he confirm androgen deficiency and the absence of oncological neoplasms in the prostate gland, treatment will be prescribed to increase their level. The exclusion of oncology is imperative, since often androgen deficiency is the beginning of the development of carcinoma. And if testosterone therapy is carried out, the patient may become worse.

The following signs of testosterone deficiency in the body should become alarm bells for men:

• sexual desire is reduced or completely absent;
• frequent manifestations of loss of strength;
• depressive state;
• decreased growth;
• aggression and irritability, which did not exist before;
• erection problems;
• gaining excess weight;
• a constant desire to sleep after dinner;
• an increase in the mammary glands;
• osteoporosis and anemia;
• cholesterol plaques.

Any of the symptoms is dangerous, but if 3 or more are found, then a visit to the doctor should become an obligatory item for a man's plan for tomorrow. Often, such therapy is resorted to when it is diagnosed:

1. Primary and secondary hypogonadism.
2. Cryptorchidism.
3. Decrease in erictile function, libido.
4. Androgen deficiency associated with age-related changes.
5. Gynecomastia.
6. Obesity that cannot be cured with traditional methods.

Testosterone therapy: a brief historical background

Testosterone therapy in men it was carried out at the dawn of the last century. But its positive results were confirmed only 40 years later. Wherein side effects such therapy was much worse than its positive effect. Synthetic testosterone of those times had only a tablet form. After taking them, androgen metabolism took place in the liver, where most of it was destroyed. This led to the strongest effect on the liver of carcinogens and toxins. The organ was irrevocably destroyed, which was the reason for the prohibition of such treatment in many countries. But with the advent of analogues of the drug, but without such terrible side effects, this ban was lifted. Often, these drugs are used by athletes, which is prohibited by a number of prestigious competitions, and this is what causes public scandals and showdowns.

The introduction of androgens into a man's body: methods

Nowadays, there are the following forms of introducing androgens into the male body:

Oral

Where is a tablet or capsule with an active ingredient used? The tablet form is the very first form in the treatment of testosterone deficiency. It is appreciated by many for its ease of use and relatively low cost when compared to other modes of administration of androgens. It is the tablet form of testosterone that is most often counterfeited or produced in clandestine factories, which leads to serious health problems. Frequently used licensed drugs:

• Andriol 150-200 mg every day;
• Striant 30 mg three times a day;
• Proviron or Vistimon, 30–80 mg every day.

Yinginjection

Doctors believe that thanks to her, testosterone enters the body naturally and smoothly. There are two types of testosterone most commonly used: enanthate and cypionate. Literally 100 mg of these drugs provide a man's weekly supply of androgen. This number is individual, so someone will need a higher dosage, and someone lower. Anything above 200 mg from substitution therapy, becomes a bodybuilder's steroid course. Usually, the weekly dosage is divided into 2 equal parts and administered at regular intervals, which allows maintaining a stable level of the hormone in the blood. Injections are given subcutaneously, not intravenously. Frequently used injections:

• Delasteril 200-400 mg once a month, divided into equal doses;
• Nebido 1000 mg once every 90 days;
• Sustanol 250 mg every 7-14 days.

Transdermal

Presented by plasters, gels and creams. Gels and creams make the flow of testosterone into the body smooth and gradual. However, doctors say that the effectiveness of this form of its administration is less effective. Difficulties may arise with the application, because the skin must be clean (preferably immediately after bathing), it is forbidden to train for some time after that so as not to sweat or swim. The lubricated area of \u200b\u200bthe skin should not be touched by others, especially children and women, since the androgen is dangerous for them. To be effective, the skin must be lubricated at least 2-3 times a day, which significantly complicates the usual alignment of life. Apply the cream and gel without rubbing. Most often, the drug "Androgel" is used in Russia, since it is sold in pharmacies without a prescription and you need it from 25 to 100 mg every day. Other transdermal products:

• plasters Androderm and Testoderm should be applied every day at a maximum dosage of 7.5 mg;
• andromen cream is used daily at 15 mg;
• andractim gel, its dosage is determined personally.

Subcutaneous

Where is the implant used for these purposes? Few decide to insert an implant, and doctors do not consider it appropriate. But in a number of cases, especially with secondary hypogonadism, this cannot be avoided. More often hormone replacement therapy for men over 50, and the drugs for its solution are a testosterone implant at a dosage of 1200 mg, which is put on for six months.

Androgen administration: which to choose?

It is recommended to use tablets if the deviation level androgens from the norm is insignificant. In case of serious pathologies, even a large dose of the drug will be ineffective. It is recommended to give preference to Andriol, since with it the main metabolism of testosterone passes outside the liver, thereby not affecting it in any way. The drug as quickly as possible penetrates the bloodstream and raises androgens to the proper level. But because of this, it also quickly leaves the body, which causes it to be taken 3-4 times a day.

The man is diagnosed with low testosterone. Substitution therapy should not only raise its level, but also not harm the body. Therefore, many doctors prefer to use the injection method of drug administration. Testosterone ester, like Omnadren or Sustanol, when it enters the circulatory system, will reach its maximum concentration on the second day. Within a couple of weeks, its level will gradually decrease, reaching a minimum.

A man will feel an incredible rise in both well-being and mood, as well as sexual desire. But the lower the concentration testosterone in the blood, the worse the condition, therefore, by the end of the injection period, a decline will be observed. It is because of these declines that patients do not want to use this form of androgen administration. However, their availability and low cost, with excellent efficiency, often tilt the scales of choosing a product in their favor.

With the release of the drug Nebido on the market, it was possible to avoid frequent surges, since this is an injection with a prolonged effect. One dose of the drug is enough for 3-4 months, which means that the decrease will be gradual and without an acute difference in sensations. It has been clinically proven that this drug does not evoke hepatotoxic and hepatocarcinogenic effects in the body.

All more men prefer to use testosterone patches or gels. With them, hormones in the blood quickly reach the required level, and the liver is not exposed to their harmful effects. There is no need to change them several times a day, and you can also adjust them yourself. Side effects are not pronounced, but the price is higher than average. It is impossible to place an implant in our country, since certification for not one of them has not been passed.

When is substitution therapy prohibited?

Doctors share contraindications hormone therapy for men into absolute and relative.

The first are:

1. Oncological neoplasm in the prostate gland, because hello to its growth.
2. Cancer in the mammary gland, which is rare in men, but hormonal treatment will also provoke tumor growth.

Relative contraindications:

• snore;
• gynecomastia;
• polycythemia;
• problems with the removal of fluid from the body;
• swelling;
• an enlarged prostate;
• failure in spermogenesis.

According to relative contraindications, the doctor will determine the degree of deterioration of the patient's condition with the effectiveness of hormone treatment. Usually, these states can be moderated by acting on them in a complex manner.

Complications

Not worth to hormone therapy treat negligently, because if the dosage shown to the patient is exceeded, side effects will not be long in coming. The physiological indicators of the whole organism will be disrupted, which will lead to:

• the inability of the body to produce androgens on its own;
• swelling and delayed excretion of fluid;
• covering the skin with acne and seborrhea;
• baldness and hair loss all over the body;
• testicular atrophy;
• inhibition of sperm production.

Problems with excessive androgen levels most often occur with young people who are keen on sports and physical ideality of the body. They are the ones who abuse testosterone-containing drugs, which negatively affects their health. This is not a joke, and the selection of such a remedy should only be carried out by a doctor and strictly for medical reasons.