Hormone replacement therapy for men with age-related androgen deficiency

• November 12, 2018
• Sports nutrition
• Tatyana Andreeva

The process of getting rid of excess subcutaneous fat in a professional sports environment is called body drying. If you don't take the matter seriously, you can lose muscle mass instead of fat cells. Therefore, it is very important to choose the right cutting course that will help minimize muscle loss, but at the same time burn fat deposits to the maximum. It is also very important to understand that in addition to medications, it is necessary to adjust the diet and maintain a special regimen. In this article, we will take a closer look at the steroids that are most often used for drying the body in professional and amateur bodybuilding.

"Stanozolol"

This is perhaps the most popular steroid for cutting the body among beginners in bodybuilding. Its reputation is largely due to its rather low cost and the absence of negative manifestations both during the drying course itself and after it.

The advantage of Stanozolol is that it perfectly removes excess fluid from the body, making the muscles more prominent. At the same time, the drug increases anabolic processes and reduces muscle loss during a low-carbohydrate diet.

Beginners use the steroid alone, and professional athletes combine Stanozolol with other drugs, thus achieving the best effect.

Dosages of Stanozolol for drying the body are different and depend on experience and goals: the starting dosage starts from 40 milligrams per day and reaches 100 milligrams. The duration of drying courses can range from six to twelve weeks.

It is important to know that Stanozolol greatly dries out the joints, so when using this steroid you should be careful when working with heavy weights during exercise. Using the drug in a solo course carries the risk of injury.

Solo courses for drying[edit | edit code]

• Anavar (Anavar)
  .
  Synonyms:
  Oxandrolone, Oxandrin, Anatrophyll, Lipidex, Lonavar, Vasorome. Take Anavar 3 times a day: 20 mg: in the morning, 20 mg at lunch and 10 mg in the evening (before 18:00). Do not use steroid drugs for 3 months after the cycle. For an additional fat-burning effect, Yu. Bombela recommends including Clenbuterol or other fat burners in the course.
• Tamoxifen
  - despite the fact that anavar slightly suppresses its own hormonal levels, post-cycle recovery is advisable. Taking tamoxifen begins 2 days after the end of the course.

• Winstrol (stanozolol)
  . It is more accessible and significantly less expensive than the previous drug. The course is structured in a similar way. To reduce toxicity to the liver, you can use the injection form (50 mg / day), since when taken orally, the entire drug passes through it, while the suspension only partially (from the systemic circulation). Although, on the other hand, the indicated oral dosage is not dangerous to health, while injections are very painful and abscesses develop relatively often.

Tablets of Winstrol can be taken in 2-3 doses (most of them in the first half of the day) on an empty stomach. Optionally, after the cycle you can take hepatoprotectors to restore the liver.

"Testosterone propionate"

No competent drying of the body can do without this drug. According to experts, it is “Propionate” that should form the basis of any course aimed at burning subcutaneous fat. Also, professionals recommend using it, and not Testosterone Enanthate, when cutting. This is due to the fact that the latter drug has a strong aromatization, which will interfere with effective fat burning.

The strong androgenic and anabolic effect of Testosterone Propionate helps not only to maintain the gained muscles during drying, but also to gain a few extra kilograms of dry mass during the cycle. And the versatility of the drug allows you to effectively combine the steroid with other drugs.

“Propionate” is given in the course every other day, in a dosage of 50 mg for beginners to 100 mg for professionals. The duration of the courses may also vary. The shortest is six weeks. If the duration of use is more than eight weeks, it is recommended to additionally inject Gonadotropin to restore body functions.

"Turinabol"

Based on reviews of Turinabol, we can say that it is the leader of this review. The steroid is very popular in bodybuilding. Athletes use it to gain high-quality lean muscles, as well as during drying.

It does not retain fluid in the muscles, does not cause side effects associated with aromatization, and does not aromatize. The use of Turinabol during drying allows you to preserve both muscles and strength indicators. And with the right diet, you can gain several kilograms of muscle.

The dosage of the steroid when used solo, both for a cutting course and for muscle gain, is practically the same - 40-50 milligrams is enough to obtain the desired effect.

The duration of use is from six to eight weeks. During post-course therapy, Clomid or Tamoxifen is used. The first drug is more expensive, but it is less toxic, which will ensure good health during recovery.

Main goals of post-cycle therapy

While taking androgenic anabolic steroids (AAS), the athlete's body experiences a number of negative effects, especially on the hormonal system, and not only. The main goals of PCT after anabolic steroids are:

• Restoring hormonal levels and natural hormone production.
• Minimizing rebound to maintain muscle gains.
• Prevention of the appearance of secondary sexual characteristics (gynecomastia) caused by estrogenic activity.
• Prevention of testicular atrophy.
• Restoring libido (sexual desire).
• Restoring normal liver function.
• Bringing blood composition back to normal.
• Reduced cortisol levels.

PCT after the cycle will also help in preventing a number of other side effects from anabolic steroids.

"Masteron"

The drug is considered a safe and effective replacement for injection Stanozolol in any course of muscle building and body drying. Masteron is a powerful androgen and aromatase inhibitor. A steroid that does not retain fluid and does not cause estrogen negative effects. On the contrary, the drug is a diuretic and removes water from the muscles, making them prominent and stiff.

The product has a fat burning effect. That is why, in combination with a diet, the Masteron drying course is considered particularly effective. It allows you to reduce fat mass by 5-7% when used solo. The dosage in this case is 100 mg every other day.

"Clenbuterol"

This weight loss drug is used in medicine to treat bronchial asthma. Recently, Clenbuterol has found wide use in fitness and bodybuilding. The fact is that this drug has the ability to burn fat cells. That is why the drug is often used by athletes for weight loss. Clenbuterol courses for cutting often include ketotifen and thyroxine. This speeds up the fat burning process.

This product is not related to anabolic steroids. The drug belongs to the group of adrenergic agonists, which affect the body by activating the sympathetic system.

The course of "Clenbuterol" for drying should last no more than 1.5 months. With longer use, the effect of the drug decreases. In order to avoid this, you should use Ketotifen. It prevents a decrease in effectiveness and makes it easier to endure the first days of the course, when negative effects appear. The daily dosage of Ketotifen is 1 or 2 micrograms.

Start using Clenbuterol with small dosages, increasing the dose by 20 mcg every day until the optimal dosage is determined. It is not necessary to reach the maximum dose. You can stop at 80 mcg. In this case, you should focus on your own feelings.

Who is tibolone for?

Changes in the demographic structure of society in recent decades have led to an increase in the proportion of women in the older age group in the population. Currently, the developed countries of the world are facing a serious social and medical problem - the inversion of the age “pyramid”, which is associated with an increase in life expectancy. A modern woman spends more than a third of her life in a state of deficiency of female sex hormones. According to WHO, the number of women entering postmenopause is increasing every year (by 2030 their number will reach 1.2 billion people). Menopause, although not a disease, leads to a disruption of the endocrine balance in a woman’s body, causing hot flashes, irritability, insomnia, and subsequently possible urogenital disorders, increasing the risk of developing osteoporosis and cardiovascular diseases. All these data indicate the need to develop a range of medical and social measures to protect the health, maintain productivity and a decent quality of life for peri- and postmenopausal women.

A new stage in the development of menopausal hormone therapy (MHT) was data on the possibility of effective use of special groups of drugs as an alternative to traditional estradiol-containing hormone replacement therapy (HRT) [1]. One such drug is tibolone, which is classified as G3H - other sex hormones and drugs used to treat menopausal disorders. Tibolone is a synthetic steroid, a tissue-selective regulator of estrogenic activity. In the human body, it is metabolized into three isomers: 3 alpha-hydroxytibolone, 3 beta-hydroxytibolone and 4 delta metabolite, which have a tissue-selective affinity for estrogen receptors. Hydroxymetabolites circulate in the blood plasma in a bound inactive state in the form of sulfated forms. Once in target tissues (bones, central nervous system, genitourinary organs, cardiovascular system), tibolone metabolites are reactivated under the influence of sulfatase, which provides their estrogen-like effect. In the mammary gland and endometrium, the 4 delta isomer blocks sulfatase, preventing the formation of active metabolites that can interact with estrogen receptors. This isomer also has gestagenic and weak androgenic properties. As a result, beneficial estrogenic effects are achieved in the central nervous system, bones and genitourinary tract in the absence of undesirable effects in the endometrium and mammary glands.

Tibolone has appeared on the pharmaceutical market since 1988. It is registered in 89 countries for the treatment of menopausal syndrome, and in 45 countries for the prevention of osteoporosis. The drug Ledibon is registered in the Russian Federation - tibolone 2.5 mg, which is used once a day, preferably at the same time. Indications for use: treatment of symptoms of estrogen deficiency in women 1 year after the last natural menstruation; prevention of osteoporosis in postmenopausal women at high risk of fractures, and with intolerance to other drugs used to prevent osteoporosis. Beginning of treatment: natural menopause - treatment can begin 12 months after the last natural menstruation; surgical menopause - treatment begins immediately. Missing a pill: less than 12 hours - take immediately; more than 12 hours - skip taking the tablet, take the next tablet at the usual time. General tolerability: Ladybon is well tolerated, there is no significant effect on body weight.

In randomized, placebo-controlled trials, tibolone has been shown to control hot flashes, sweating, and other common symptoms such as insomnia, headache, and fatigue. It appears to be as effective as numerous estrogen-progestogen combination and estrogen-only therapy (EPT/ET) regimens in relieving menopausal symptoms [8–10], although it may have a slightly slower onset of action, but may also be used as “coverage therapy” to relieve symptoms of estrogen deficiency in women treated with gonadotropin-releasing hormone agonists (GnRH agonists) for uterine fibroids and endometriosis [11, 12].

It has been shown that tibolone promotes the reverse development of vaginal atrophy (increases the karyopyknotic index and cell maturation index) and improves the quality of cervical mucus [13]. Women treated with tibolone report significant improvements in vaginal dryness, dyspareunia, and urinary symptoms.

The effects of tibolone on circulating androgens differ from those of standard oral MHT regimens (EPT/ET). With tibolone, sex steroid binding globulin (SHBG) levels are reduced rather than increased, resulting in an increase in free testosterone concentrations, whereas with standard MHT (EPT/ET) there is a decrease. It has been shown that the concentration of dehydroepiandrosterone sulfate (DEAS) also increases [14]. In addition, the 4 delta isomer of tibolone also has some androgenic effects. These properties of tibolone contribute to its beneficial effects on sexual well-being, which include increased sexual desire, arousal, stimulation of sexual fantasies and increased vaginal hydration [15–17]. Compared to standard EPT regimens, tibolone significantly increases the frequency of coitus and increases the degree of pleasure and satisfaction with sexual intercourse [18]. Regarding the frequency of orgasm and sexual sensitivity, when using tibolone or a combination of estrogens and androgens, a more pronounced effect is observed than when using ET or in the control group [19].

It is assumed that the significant beneficial effect of tibolone on mood levels is due to the normalization of endorphin levels and its androgenic properties [15, 20]. In a comparative study using EBT, tibolone was more effective in reducing the severity of mood disorders [21]. In addition, its effect may be synergistic with the effects of psychoactive drugs, which is accompanied by faster improvement in women suffering from depression and psychosis. Since the use of antidepressants is often associated with sexual dysfunction, the effect of tibolone on sexuality in these women is accompanied by additional benefits.

Randomized controlled trials have shown that tibolone causes an increase in bone mineral density (BMD) and prevents bone loss [23, 24]. Beneficial effects of tibolone were observed in both the femoral neck and spine. These beneficial effects were observed with long-term (10-year) treatment [25] in both early and late postmenopausal women with established osteoporosis and in women treated with GnRH agonists [11, 12, 26–28].

Tibolone therapy is significantly less likely to cause breast tenderness and mastalgia than EPT; this reason is much less likely than in the case of EPT to lead to discontinuation of tibolone treatment [8, 9, 23, 29]. Women with breast tenderness or mastalgia due to EPT appear to benefit from switching to tibolone [30].

Tibolone does not cause an increase in tissue density on the mammogram [29, 31]. Spontaneously occurring increased radiographic density of the mammary glands is considered an independent risk factor for breast cancer. It is currently unclear whether EPT-induced breast density is a surrogate marker of increased breast cancer risk, however, increased mammographic density may mask breast tumors on screening mammography, leading to delayed diagnosis [32]. In addition, increased mammographic density leads to an increase in the frequency of repeat patient calls, which causes fear among women [33, 34]. The effect of tibolone on the mammary glands differs from the effects of EPT. Unlike EPT, tibolone does not increase the risk of breast tissue proliferation, but stimulates apoptosis [31, 35]. In pooled data from all phase III/IV studies of tibolone, tibolone did not increase the risk of breast cancer compared with placebo (relative risk (RR) 0.50; 95% confidence interval 0.11–2.54) [36]. The Million Women Study (MWS) reported an increased RR for breast cancer with tibolone treatment (RR 1.45; 95% CI 1.25–1.67), although the increase was significant (p < 0.0001). less than against the background of EPT [5]. Another epidemiological study using the UK General Practice Research Database (GPRD) found no increased risk with tibolone (RR 1.02; 95% CI 0.78–1.33) [37]. However, the data from this study were published only as an abstract and not as a full-text article.

Although the best evidence currently available for the effect of tibolone on breast cancer development comes from MWS, the risks described in this observational study are likely to be overestimated [3, 4]. Evidence from prospective studies [2, 33] suggests that the absolute increase in breast cancer risk is lower than reported in the MWS study and that the risk of tibolone and ET is likely lower than the risk of EPT.

Bottom line: who is Ladybon for?

Postmenopausal patients with vasomotor symptoms in whom Ladybon may be of particular importance:

• women with low levels of sexual desire or so-called female sexual dysfunction;
• women with mood disorders and women receiving psychoactive drugs;
• women at risk of accelerated bone loss;
• women with menopausal mastalgia;
• women with increased X-ray density of the mammary glands;
• women with uterine fibroids;
• women with urogenital complaints.

Patients who may benefit from switching from EPT/ET to Ladybon:

• women who have increased pain in the mammary glands;
• women who experience an increase in breast density, which leads to frequent false calls for examinations or unreadable mammograms;
• women with low sex drive;
• women with mood swings;
• women with bleeding (provided there is no histopathological reason for bleeding).

Patients without menopausal symptoms to keep in mind (some postmenopausal women without menopausal symptoms or with mild symptoms may benefit from treatment with Ladybon):

• women with low sex drive;
• women with mood swings;
• women with osteopenia.

Literature

1. Smith CL, O'Malley BW Coregulator function: a key to understanding tissue specificity of selective receptor modulators // Endocr Rev. 2004; 25: 45–71.
2. Anderson GL, Limacher M, Assaf AR et al. Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women's Health Initiative randomized controlled trial // J Am Med Assoc. 2004; 291:1701–1712.
3. Shapiro S. The Million Women Study: potential biases do not allow uncritical acceptance of the data // Climacteric. 2004; 7:3–7.1
4. Whitehead M., Farmer R. The MillionWomen Study: a critique // Endocrine. 2004; 24: 187–194.
5. Million Women Study Collaborators. Breast cancer and hormone replacement therapy in the MillionWomen Study // Lancet. 2003; 362:419–427.
6. EMAS Revised Statement // Maturitas. 2005; 51:8–14.
7. IMS Revised Position Paper // Climacteric. 2004; 7:333–337.
8. Hammar M., Christau S., Nathorst-B¨o¨os J., Rud T., Garre K. A double-blind randomized trial comparing the effects of tibolone and continuous combined hormone replacement therapy in postmenopausal women with menopausal symptoms // Br J Obstet Gynaecol. 1998; 105:904–911.
9. Huber J., Palacios S., Berglund L. et al. The effect of tibolone compared with conjugated equine oestrogens continuously combined with medroxyprogesterone acetate on bleeding rates, quality of life and tolerability in postmenopausal women // Br J Obstet Gynaecol. 2002; 109:886–893.
10. Baracat EC, Barbosa IC, Giordano MG et al. A randomized, open-label study of conjugated equine estrogens plus medroxyprogesterone acetate versus tibolone: ​​effects on symptom control, bleeding pattern, lipid profile and tolerance // Climacteric. 2002; 5:60–69.
11. Lindsay PC, Shaw RW, Coelingh Bennink HJ, Kovic P. The effect of add back treatment with tibolone (Livial®) on patients treated with the gonadotrophin-releasing hormone agonist triptorelin (Decapeptyl) // Fertil Steril. 1996; 65:342–348.
12. Palomba S., Affinito P., Di Carlo C., Bifulco G., Nappi C. Longterm administration of tibolone plus gonadotrophin-releasing hormone agonist for the treatment of uterine leiomyomas: effectiveness and effects on vasomotor symptoms, bone mass and lipid profile / / Fertil Steril. 1999; 72:889–895.
13. Morris EP, Wilson POG, Robinson J., Rymer JM Long-term effects of tibolone on the genital tract in postmenopausal women // Br J Obstet Gynaecol. 1999; 106:954–959.
14. Doren M., Rubig A., Coelingh Bennink HJ, Holzgreve W. Differential effects on the androgen status of postmenopausal women treated with tibolone and continuous combined estradiol and norethindrone acetate replacement therapy // Fertil Steril. 2001; 75:554–559.
15. Davis SR The effects of tibolone on mood and libido // Menopause. 2002; 9: 162–170.
16. Palacios S., Menendez C., Jurado R., Castano JC, Vargas JC Changes in sex behavior after menopause: effects of tibolone // Maturitas. 1995; 22: 155–161.
17. Laan E., van Lunsen RHW, Everaerd W. The effects of tibolone on vaginal blood flow, sexual desire and arousability in postmenopausal women // Climacteric. 2001; 4:28–41.
18. Nathorst-Boos J., Hammar M. Effect on sexual life—a comparison between tibolone and a continuous estradiol-norethisterone acetate regimen // Maturitas. 1997; 26: 15–20.
19. Castelo-Branco C., Vicente J., Figueras F. et al. Comparative effects of estrogens plus androgens and tibolone on bone, lipid pattern and sexuality in postmenopausal women // Maturitas. 2000; 34: 161–168.
20. Genazzani AR, Petraglia F., Facchinetti F. et al. Effects of Org OD 14 on pituitary and peripheral-endorphin in castrated rats and in postmenopausal women // Maturitas. 1987; 1:35–48.
21. Egarter Ch., Huber J., Leikermoser R. et al. Tibolone versus conjugated estrogens and sequential progestogen in the treatment of climacteric complaints // Maturitas. 1996; 23:55–62.
22. Meeuwsen IB, Samson MM, Duursma SA, Verhaar HJ The influence of tibolone on quality of life in postmenopausal women // Maturitas. 2002; 41: 35–43.
23. Roux C., Pelissier C., Fechtenbaum J., Loiseau-Peres S., Benhamou CL Randomized, double-blind, 2-year comparison of tibolone with 17-estradiol and norethindrone acetate in preventing postmenopausal bone loss // Osteoporosis Int. 2002; 13: 241–248.
24. Lippuner K., Haenggi W., Birkhauser M.H., Casez J.-P., Jaeger P. Prevention of postmenopausal bone loss using tibolone or conventional oral or transdermal hormone replacement therapy with 17-oestradiol and dydrogesterone // J Bone Min Res. 1997; 12:806–812.
25. Rymer J., Robinson J., Fogelman I. Ten years of treatment with tibolone 2.5 mg daily: effects on bone loss in postmenopausal women // Climacteric. 2002; 5:390–398.
26. Berning B., Kuijk CV, Kuiper JW, Coelingh Bennink HJT, Kicovic PM, Fauser BCJM Effects of two doses of tibolone on trabecular and cortical bone loss in early postmenopausal women: a two-year randomized, placebo-controlled study // Bone. 1996; 19: 395–399.
27. Bjarnason NH, Bjarnason K., Haarbo J., Rosenquist C., Christiansen C. Tibolone: ​​prevention of bone loss in late postmenopausal women // J Clin Endocrinol Metab. 1996; 81:2419–2422.
28. Pavlov PW, Ginsburg J., Kicovic PM, van der Schaaf DB, Prelevic G., Coelingh Bennink HJT Double-blind, placebo controlled study of the effects of tibolone on bone mineral density in postmenopausal osteoporotic women with and without previous fractures // Gynecol Endocrinol. 1999; 13: 230–237.
29. Lundstrom E., Christow A., Svane G. et al. Effects of tibolone and a continuous combined HRT regimen on mammographic breast density // Am J Obstet Gynecol. 2002; 186:717–722.
30. Palomba S., Di Carlo C., Morelli M. et al. Effect of tibolone on breast symptoms resulting from postmenopausal hormone replacement therapy // Maturitas. 2003; 45: 267–273.
31. Valdivia I., Campodonico I., Tapia A. et al. Effects of tibolone and continuous combined hormone therapy on mammographic breast density and breast histochemical markers in postmenopausal women // Fertil Steril. 2004; 81:617–623.
32. Thurfjell E. Breast density and the risk of breast cancer // N Engl J Med. 2002; 347:866.
33. Chlebowski RT, Hendrix SL, Langer RD et al. Influence of estrogen plus progestin on breast cancer and mammography in healthy postmenopausal women: theWomen's Health Initiative Randomized Trial // J Am Med Assoc. 2003; 289:3243–3253.
34. Banks E., Reeves G., Beral V. et al. Impact of use of hormone replacement therapy on false positive recall in the NHS breast screening program: results from the Million Women Study // Br Med J. 2004; 328:1291–1292.
35. Conner P., Christow A., Kersemaekerc W. Acomparative study of breast cell proliferation during hormone replacement therapy: effect of tibolone and continuous combined estrogen progestogen therapy // Climacteric. 2004; 7:50–58.
36. Helmond FA, Kloosterboer HJ Safety and tolerance profile of Livial. In: Genazzani AR, editor. Hormone replacement therapy and cancer. The current status of research and practice. Boca Raton: The Parthenon Publishing Group; 2002. P. 252–256.
37. Allen DS, de Vries CS, Farmer RDT Pharmaceutical content and regimen of hormone replacement therapy and risk of breast cancer // Pharmacoepidemiol Drug Saf. 2002; 11 (Suppl 1): 296.

A. L. Tikhomirov1, Doctor of Medical Sciences, Professor I. B. Manukhin, Doctor of Medical Sciences, Professor E. I. Manukhina, Doctor of Medical Sciences, Professor V. V. Kazenashev, Candidate of Medical Sciences

GBOU VPO MGMSU im. A. I. Evdokimova Ministry of Health of the Russian Federation, Moscow

1 Contact information