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

Short story

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

The first popular synthetic testosterone preparations were sold in the form of tablets (methyltestosterone, fluoxymesterone, etc.). Oral administration metabolized testosterone 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 testosterone derivatives are banned for use, giving way to modern analogues.

A great influence on the development of synthetic forms of testosterone plays its role in sports. Despite the fact that the use of anabolic steroids is prohibited, incidents with doping control continue to boom at the Olympic Games and other major competitions.

Testosterone Administration Forms

Methods of introducing androgens are divided 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 DRUGS CHEMICAL NAME TRADENAME DOSAGE
Injection Forms Testosterone cypionate Depot Testosterone Cypionate 200-400 mg every 3-4 weeks
Testosterone enanthate Delasteryl
Testosterone Depot
200-400 mg every 2-4 weeks
A mixture of testosterone esters Sustanol-250
Omnadren 250
250 mg every 2–3 weeks
Testosterone undecanoate Nebido 1000 mg once every 3 months
Oral form Fluoxymesterone * Halotestin 5-20 mg daily
Methyltestosterone * Metadren 10-30 mg daily
Testosterone undecanoate Andriol 120-200 mg daily
Mesterolone *** Proviron
Vistinon
Vistimon
25-75 mg daily
Buccal pills 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
Patches with testosterone (scrotal and cutaneous) ** Androderm
Testoderm
2.5-7.5 mg daily
Testosterone cream Andromen 10-15 mg daily
Dihydrotestosterone Gel (DHT Gel) Andraktim Individually

Notes: * - hepatoxic and banned in a number of countries; ** - not registered in Russia; *** - discontinued.

Drug selection

Доля андрогенных препаратов

Fig. 1 - The share of various forms of androgenic drugs on the pharmaceutical market of Russia (2007) (source “Practical Andrology”, S. Yu. Kalinchenko I. A. Tyuzikov, 2009).

Intramuscular injections of testosterone are the most commonly used replacement therapy. The most famous testosterone esters - testosterone cypionate and testosterone enanthate have their own characteristics: getting into the bloodstream, the level of testosterone 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. “Roller coaster effect”, when mood, well-being and libido increase along with the level of androgens in the blood, and also abruptly goes down when the level of testosterone is at its lowest 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 mixture have been successfully used so far because of their low cost, availability and effectiveness. In particular, testosterone esters are loved by power athletes and bodybuilders for their anabolic properties and for the possibility of creating a high concentration of testosterone in the blood.

The injection drug of choice for hormone replacement therapy (HRT) today is testosterone undecanoate (Nebido). Its difference from other testosterone esters is the prolonged action (1 injection in 10-12 weeks) and the absence of pathological jumps in the level of androgens. The drug Nebido has a full spectrum of testosterone and does not cause hepatotoxic and hepatocarcinogenic effects.

Oral drugs have a mild effect compared to injectable forms, even when using high doses. Therefore, it is advisable to use oral forms of testosterone in cases where there is a slight decrease in androgens. The drug of choice for HRT is Andriol. Compared with old analogues (methyltestosterone, fluoxymesterolone), when Andriol is used, most of the testosterone bypasses the metabolism in the liver, and enters directly into the systemic circulation, which contributes to the rapid achievement of the required concentration of the hormone. However, this also determines the fast half-life of the drug (3-4 hours), which forces the patient to re-take (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 they do not undergo hepatic metabolism as oral preparations, and at the same time they do not create the supraphysiological level of testosterone, as is the case with 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 to the patient, evenly releasing the hormone for 6 months. In Russia, testosterone implants are not registered.

Фармакокинетика препаратов тестостерона

Fig. 2 - Pharmacokinetics of various testosterone preparations.

Table 2 - Characteristics of various forms of testosterone preparations

INJECTION ORAL Transdermal SUBCUTANEOUS
Therapy efficacy +

Highly effective. The ability to create high concentrations of the hormone in the blood

-

Effective only with mild androgen deficiency

+

Effective enough to overcome various degrees of androgen deficiency

+

Effective

Availability +

The availability of a wide selection of different testosterone esters

+

Prescription Availability

+/-

The availability of only testosterone gel (AndroGel). Testosterone patches not registered in Russia

-

In Russia, testosterone implants are not registered

Action duration +

The drug Nebido has the longest duration of action among all testosterone preparations (1 injection every 3 months.)

-

Daily from 2-4 times a day (Andriol)

-

Daily once a day

+

The duration of one implant is 6 months.

The possibility of an emergency stop of therapy - + + -
Sudden fluctuations in hormone levels +

Not detected, with Nebido-It is noted with the use of testosterone propionate, testosterone enanthate and a mixture of esters

-

Have a fast half-life

+

Evenly absorbed throughout the day, keeping hormone levels within normal limits

+

Uniform release of testosterone over the duration of the implant

Possibility of independent use +/-

The procedure is performed by a specialist, however, the possibility of independent use is not excluded

+ + -

Requires surgery

Side effects Depending on dosage Some liver toxicity, especially older drugs May cause skin reactions at the site of skin contact Surgical Complications

Contraindications for replacement therapy

Absolute:

  • Prostate cancer Androgen therapy can stimulate the growth of an existing tumor;
  • Breast Cancer (rare). Androgen therapy can lead to an increase in estrogen levels, which can trigger further tumor growth.
To exclude prostate cancer, prior to replacement therapy, it is necessary to conduct a digital examination of the prostate gland and determine the level of prostate-specific antigen (PSA).

Relative:

  • Sleep apnea;
  • Polycythemia;
  • Gynecomastia ;
  • Fluid retention;
  • Swelling;
  • Enlarged prostate;
  • Violation of spermatogenesis.

Relative contraindications mean that with HRT androgens, the course of the condition may worsen.

Possible indications for replacement therapy

  1. Primary and secondary hypogonadism .
  2. Cryptorchidism.
  3. Decreased libido and erectile dysfunction due to androgen deficiency.
  4. Age-related androgen deficiency .
  5. Gynecomastia
  6. Obesity is difficult to treat.

Side effects of hormone therapy

Side effects of testosterone occur only when using large doses of the drug in excess of normal physiological parameters. The use of androgens in physiological doses does not lead to side effects.

Possible side effects caused by large doses of androgens:

  • suppression of the production of own testosterone;
  • swelling, water retention;
  • acne, seborrhea;
  • gynecomastia;
  • inhibition of spermatogenesis;
  • baldness;
  • testicular atrophy.

Read more "Side effects of testosterone in replacement therapy . "

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