Antiandrogen drugs for acne. Treatment of acne with antiandrogen drugs. Contraindications for the use of combined oral contraceptives

With the introduction of hormonal contraception into clinical practice, new opportunities have emerged not only in the prevention of abortions and related complications, but also in the treatment of a number of gynecological diseases.

This is due to a number of non-contraceptive properties of drugs in this group and their diverse effects on various parts of the reproductive system. Having the ability to temporarily block ovulation, inhibit hypothalamic-pituitary-ovarian secretion, suppress proliferative processes in target organs, due to their pronounced gestagenic activity, contraceptive hormones have long occupied a prominent place in clinical practice in the treatment of dysfunctional uterine bleeding, endocrine infertility, premenstrual syndrome, dysmenorrhea, endometriosis and a number of other gynecological and extragenital diseases.

Every year the pharmacological properties of drugs are improved, new compounds appear that have good acceptability, fewer adverse reactions, and a selective effect on the pathogenesis of certain pathological conditions.

The synthesis of new drugs, the differences between certain drugs are mainly associated with a different progestogen component. For example, the unfavorable effects of hormonal contraception may be due to the androgenic and glucocorticoid activity inherent in some progestogens, while the favorable effects may be due to the antiandrogenic and antimineralcorticoid effects. In this regard, drugs with these beneficial properties are very promising from the standpoint of therapeutic use. Among the many trade names of hormonal contraceptives in general, there are not so many drugs with proven antiandrogenic properties. These include: “Diane-35”, “Zhanine”, “Belara”, “Yarina”. There are reports of some antiandrogenic properties of triphasic compounds, in particular Tri-Mercy, and effective use for acne in young women.

From the early 80s to the present day, the leader in the group of antiandrogenic contraceptives is Diane-35, which can rightfully be called the “gold standard” in the treatment of hyperandrogenic conditions. Cyproterone acetate, which is part of Diane-35, is capable of blocking androgen receptors in target organs, suppressing the secretion of gonadotropins and, consequently, the synthesis of androgens in the ovaries. Cyproterone acetate is practically the only antiandrogen that affects all parts of the pathogenesis of hyperandrogenism, so the range of its use is very wide. It is successfully used in gynecological, endocrinological, therapeutic, and dermatological practice. In particular, in gynecological practice it is used for various diseases accompanied by hyperandrogenism, hirsutism, alopecia, acne vulgaris, and polycystic ovary syndrome for contraception in women with hyperandrogenism and preserved fertility; in the treatment of infertility caused by hyperandrogenism, etc.

Diana-35 is prescribed according to the standard regimen: 21 days of admission - 7 days break, etc. The duration of treatment is individual.

The drug "Zhanine" also has antiandrogenic activity, but less than "Diane-35". At the same time, as clinical practice shows, its effect on hyperandrogenic skin manifestations is also very significant and in terms of its effect on skin manifestations it is close to Diana-35.

Dienogest, which is part of Zhanina, belongs to a new class of gestagens that have pronounced antiproliferative properties and the ability to suppress the growth of endometriotic heterotopias. Among the contraceptive hormones used to treat endometriosis, it can certainly be called the drug of choice (according to S. Moore et al.). The effectiveness of treatment of endometriosis with dienogest is comparable to the effectiveness of danazol and GnRH analogues.

In recent years, the drug “Yarina”, containing a qualitatively new progestogen - drospirenone, has been introduced into clinical practice. Drospirenone is a derivative of spironolactone, which has not only antiandrogenic but also antialdosterone activity. This combination of properties allows it to be used for hirsutism, in particular acne, seborrhea, and for conditions accompanied by fluid retention in the body. In particular, numerous studies indicate its effectiveness in women with premenstrual syndrome. It should be emphasized that drospirenone has biological properties close to those of endogenous progesterone.

The clinical significance of the antimineralkorticoid effect of “Yarina” lies in the fewer side effects caused by fluid retention (breast engorgement, swelling, weight gain, risk of hypertension, headaches) and the therapeutic effect in premenstrual syndrome, which is expressed in a decrease in psychoneurological disorders, weight loss, reducing increased appetite, mastodynia, headaches and other symptoms of premenstrual syndrome.

Drospirenone can be used in the usual contraceptive mode (21 days - 7 days break - 21 days, etc.) or according to a prolonged regimen without a seven-day break (from 6 to 18 or more weeks) as prescribed by a doctor, depending on the specific situation.

One of the drugs with an antiandrogenic, although weaker, effect is Belara, which contains the progestogen chlormadinone acetate. It can be used in women with mild acne.

Thus, the progress of contraception has made it possible to synthesize a number of drugs with medicinal, including antiandrogenic and antimineralkorticoid properties, which significantly expands the capabilities of practicing physicians.

Many girls and women are faced with such a problem as hyperandrogenism. This hormonal state indicates that an excess amount of male sex hormones (androgens) is present in the female body. They introduce an imbalance in the functioning of various organs and systems and cause many unpleasant and painful manifestations. Since 2000, endocrinologists and gynecologists have been using birth control pills with an antiandrogenic effect to correct these disorders.

Hyperandrogenism in women

Excess androgens can be observed in representatives of the fair sex of different ages: girls, women over 20 and even 40-45 years old. Hyperandrogenism is expressed as follows:

  1. acceleration of growth rate in girls;
  2. Excessive hair growth on the face, inner thighs and abdomen;
  3. excessive oily skin;
  4. the appearance of acne;
  5. hair loss in the crown and temples;
  6. gaining muscle mass;
  7. menstrual irregularities;
  8. infertility and miscarriage.

This condition forces one to resort to various treatment methods, and both non-hormonal drugs and hormonal-based contraceptives (including antiandrogenic contraceptives) can be used for its treatment.

Composition of contraceptives antiandrogens

Antiandrogen contraceptives consist of a combination of two female sex hormones: ethinyl estradiol and progestogen. The progestins that are part of these combined contraceptives consist of a special type of 19-nortes-tesorone, which is able to bind to androgen receptors that produce testorone and reduce the synthesis of this male sex hormone in the body. Oral contraceptives with an antiandrogenic effect, which include third-generation estrogens and progestogens (desogestrel, norgestimate and gestodene), are more effective for correcting hyperandrogenism in women, since these substances are able to bind more effectively to progesterone receptors.

Hormonal contraceptives with antiandrogenic action, which have shown the best results in the correction of hyperandrogenic conditions:

  • Diana-35;
  • Janine;
  • Marvelon;
  • Logest;
  • Belara;
  • Jazz;
  • Tri-Mercy;
  • Yarina.

The dosage of ethyl estradiol and progestogen in such oral contraceptives is the most important component of successful therapy.

Mechanism of action of antiandrogenic OCs

The mechanism of action of oral contraceptives with antiandrogenic action is aimed at several components that influence the synthesis of the sex hormone:

  1. estrogens stimulate the production of globulin in the liver - this helps to reduce the level of testosterone in the blood, since globulin is able to bind to free testosterone in the blood;
  2. estrogens and progestogens help reduce testosterone production in the ovaries, because they suppress the secretion of gonadotropic hormones;
  3. progestogens contribute to the inhibition of 5-alpha reductase, an enzyme that promotes the conversion of testosterone to its active state.

Thus, contraceptives with antiandrogens, used over a long period, help stabilize hormonal levels. As a rule, these contraceptive drugs are prescribed for at least 5-6 menstrual cycles, and their gestagenic effect becomes noticeable after 2-3 cycles, and the contraceptive effect is observed already in the first month of use.

Indications and contraindications for the use of antiandrogenic contraceptives

Antiandrogenic contraceptives, the list of which is given above, can be successfully used to protect against unwanted pregnancy in women with manifestations of hyperandrogenism and to treat diseases associated with hormonal imbalances observed in them. Most gynecologists do not recommend using antiandrogenic birth control pills for contraception unless there are signs of elevated testosterone levels. Indications for the use of these contraceptives may include:

  1. acne;
  2. menstrual irregularities;
  3. uterine bleeding associated with puberty and disturbances in the regulation of the menstrual cycle;
  4. dysmenorrhea associated with adolescence and not burdened by pathologies of the genital organs;
  5. ovarian cancer;
  6. hyperandrogenism.

Contraceptives with an antiandrogenic effect have the same contraindications as other hormonal contraceptives. Previously, contraceptive pills with antiandrogens were not prescribed to adolescent girls, but in 1997, WHO began recommending low-dose COCs for use in this age category. Modern contraceptives with an antiandrogenic effect, which include third-generation progestogens (gestodene, norgestimate or desogestrel), have minimal side effects and can be used for long courses of treatment of various disorders associated with changes in hormonal levels.

Side effects and risk factors

In most cases, contraceptives with antiandrogenic action rarely have side effects, which can be expressed in various manifestations. As a rule, after 1-2 months of use they disappear and do not require discontinuation of the drug.

Side effects:

  • intermenstrual bleeding;
  • tension and pain in the mammary glands;
  • headache;
  • frequent mood changes;
  • decreased or increased libido;
  • visual impairment;
  • increased sensitivity to contact lenses;
  • dyspeptic disorders;
  • skin rash and skin pigmentation disorders;
  • bile stagnation and jaundice;
  • changes in body weight;
  • swelling;
  • allergic reactions.

Risk factors and possible side effects when taking any birth control pills:

  • obesity;
  • nicotine or alcohol addiction;
  • vascular pathologies and predisposition to them.

Prescribing oral contraceptive pills with an antiandrogenic effect after a detailed examination, following all the rules for taking the drug and following all the doctor’s recommendations - all this not only guarantees the safety of using these contraceptives, but also promotes recovery from many diseases that can significantly worsen the quality of life.

The female body contains small amounts of male hormones androgens, which are responsible for normalizing the menstrual cycle and hair growth in intimate areas. With high production of the hormone, women begin to develop bald patches in the temple area, and hair growth in other parts of the body also increases. Antiandrogenic drugs for women, which we will consider below, are designed to combat this process.

For androgenetic alopecia, special medications are prescribed

"Androcur"

This drug is available in tablet form. Its main purpose is to block androgen receptors. For female representatives, it has the following indications for use:

Androkur leads to a weakening of the influence of androgen on the female body

  • the appearance of facial and body hair;
  • seborrhea;
  • acne disease.

"Androkur" leads to a weakening of the influence of androgen on the female body, and also helps to eliminate pathological changes in the form of increased vegetation.

The dosage and duration of drug treatment should be determined strictly by a doctor. The drug is prohibited for use in persons suffering from the following pathologies:

  • prolonged depression;
  • thrombosis;
  • liver pathologies;
  • diabetes.

Taking the drug is also contraindicated during pregnancy and breastfeeding in women.

Among the side effects that are observed while taking the drug, allergic reactions accompanied by a rash, pain in the abdomen, a feeling of nausea, and apathetic state should be highlighted. Since the medication can lead to a decrease in concentration, during the period of treatment they should refrain from driving vehicles, as well as engaging in activities that require quick reaction and concentration.

"Visanne"

Visanne should only be prescribed by a doctor

The medication has indications for use such as endometriosis. It is also prescribed for cases of increased body hair, which is caused by the production of large quantities of androgens in the female body.

This is a fairly serious drug with a large list of contraindications, so it is not used without a doctor’s prescription. "Visanne" is contraindicated in the presence of pathologies such as pathologies of the cardiovascular system, liver, internal bleeding, and jaundice. Also, the drug is not prescribed in the presence of diabetes mellitus, thrombophlebitis, or lactase deficiency.

Usually the drug is taken once a day with an equal amount of time between doses. The duration of treatment should be determined strictly by the doctor.

The drug can lead to complications such as vaginal bleeding, headaches, and depression.

"Marvelon"

Marvelon has a large list of contraindications and side effects

This medication is a contraceptive that can be used in therapy in women with the appearance of increased vegetation against the background of hyperproduction of androgens in the body. The duration of use and dosage of the medication should be determined exclusively by a specialist.

Marvelon has a large list of contraindications and side effects. The drug should not be taken in the following cases:

  • vaginal bleeding;
  • diabetes;
  • frequent, severe headaches;
  • severe liver pathologies;
  • pancreatitis;
  • nicotine addiction in persons over 35 years of age;
  • lactase deficiency;
  • pathologies of the cardiovascular system.

While taking the medicine, it is possible to develop such negative phenomena as the development of pathologies of the gastrointestinal tract, the appearance of autoimmune diseases, in particular lupus erythematosus, the development of depressive conditions, etc.

It is worth considering that the medication is incompatible with many groups of drugs, so before you start taking it you should carefully read the instructions for use.

"Diana is 35"

Diane 35 suppresses increased production of androgens in a woman’s body

This drug suppresses the increased production of androgens in a woman’s body, thereby eliminating the pathological process that leads to the appearance of excess vegetation in unwanted places. The drug is also prescribed for this type of dermatitis, such as seborrhea of ​​the scalp.

Under the influence of the drug, the body’s production of sebaceous glands decreases, hair follicles become stronger, which prevents premature hair loss. The drug also helps eliminate excessive facial hair. To obtain results, long-term therapy will be required over several months. The doctor should decide exactly how much medicine to take.

The medication cannot be used in therapy in patients suffering from various types of thrombosis, diabetes mellitus, jaundice, liver pathologies and vaginal bleeding.

Among the adverse reactions provoked by the drug, the development of migraines, decreased libido, and allergic rashes should be highlighted. After discontinuation of the drug, adverse events usually disappear.

"Janine"

Janine refers to contraceptives

The drug belongs to the category of contraceptives, the use of which is permissible in case of increased vegetation in females against the background of increased production of male hormones by the body.

The drug is taken over several weeks. It is up to the doctor to decide when to stop taking the medication. It is recommended to use the pills at regular intervals for better therapeutic effects.

“Janine” has a lot of contraindications, including various thromboses, liver pathologies, and the period after childbirth. Also, the drug should not be taken by a certain group of diabetics, as well as by patients suffering from migraines. If there is bleeding, the product should also not be used.

“Janine” is incompatible with many medications, so you should carefully read the instructions before taking it.

Side effects that the drug can cause include vaginitis, cystitis, anemia, weight loss, etc.

"Logest"

Logest is prescribed only by a doctor

This medication is an oral contraceptive prescribed for women with increased body hair and baldness on the head.

The dosage and duration of therapy are determined purely by a specialist. The appearance of the first positive results should not be expected quickly. Effectiveness of therapy occurs within a few months.

For any type of thrombosis, as well as in the presence of pathologies such as diabetes, tumors, liver pathologies, severe headaches and vaginal bleeding, the drug is not prescribed. If the dosage is exceeded, there is a high risk of uterine bleeding.

The drug has poor compatibility with antibiotics of the tetracycline and penicillin groups. Also, the drug is not recommended for use simultaneously with medications that contain carbamazepine and phenobarbital.

In some cases, the drug may cause undesirable reactions such as migraines, apathy, decreased libido, decreased body weight, allergies, etc.

"Spironolactone"

Spironolactone is prescribed for severe types of acne and seborrhea

A medication from the antiadrogen group is prescribed for severe types of acne and seborrhea. It is also used to reduce hair growth on unwanted areas of the body. It helps normalize the functioning of the sebaceous glands and strengthens the hair follicles.

The drug is also a strong diuretic, so it is often prescribed during pregnancy in the presence of severe edema.

The drug should not be used in cases of liver failure, diabetes mellitus, or thrombophlebitis.

Usually the medication is prescribed to be taken three times a day. The duration of therapy will depend largely on the severity of the pathological process.

Long-term use of the drug can lead to the development of gastritis, bleeding in the gastrointestinal tract, drowsiness, etc.

Spironolactone can reduce concentration, for this reason it is prohibited to drive vehicles during treatment.

"Cyproterone Teva"

Cyproterone Teva is one of the most effective drugs


For quotation: Nikitin S.V. The influence of various progestogens on the antiandrogenic effect of modern combined oral contraceptives // RMZh. 2002. No. 18. P. 823

IN have been used for over 40 years combined oral contraceptives (COCs). Considering the significant superiority of the advantages of modern COCs over side effects and rare complications, currently more than 150 million women in the world prefer them. Although there is a persistent downward trend in abortions in Russia (their absolute number in 2000 decreased by 20% compared to 1995), the frequency of use of modern highly effective methods of contraception remains insufficient. According to the Russian Ministry of Health, in 2000, the number of women using hormonal methods of contraception was 2.8 million (3% of the number of women of fertile age), intrauterine devices - 6.3 million (16.3%).

A decrease in estrogen content and the emergence of highly selective progestogens with low androgenic activity in modern COCs have made it possible to minimize the effect on metabolic parameters. In combination with the ease of use and rapid reversibility of the contraceptive effect, the positive non-contraceptive effects of COCs (control of the menstrual cycle; reduction in the number of cases of menopause and metrorrhagia, functional anemia; positive effect on vegetative-vascular and psycho-emotional reactions; correction of premenstrual syndrome; prevention and treatment of uterine fibroids and endometriosis; prevention and reduction of functional ovarian cysts; antiandrogenic effect) make them especially attractive for young nulliparous women planning pregnancy. Considering the pronounced antiandrogenic effect of some modern COCs, their use is recommended for the treatment of skin manifestations of hyperandrogenism.

Sex steroids, and most of all androgens, play an important role in determining hair type and distribution. Androgens stimulate the growth of terminal hair (Chieffi M., 1949; Hamilton J.B., 1950; Reynolds E.L., 1951; Futterweit W. et al., 1986), increase the size of the hair follicle, hair thickness and the time of the growth phase (anagen) in the development cycle of terminal hairs. hair (Ebling F.J.G., 1986; Messenger A.G., 1993; Randall V.A., 1994). Androgens influence the nature and volume of secretion of the sweat and sebaceous glands (Hay J. and Hodjins M., 1978; Takayasu S. et al., 1980; Itami S. and Takayasu S., 1981; Rosenfield R.L. et al., 1984; Lucky A.W. et al., 1994). Increased sebum volume during early puberty (adrenarche or “adrenal puberty”) and acne vulgaris in girls during puberty is associated with an increase in androgen levels (Stewart M.E. et al., 1992; Lucky A.W. et al., 1994; Lucky A.W. et al., 1997). The main site of testosterone formation in women is the skin (Table 1), which contains all the necessary enzymes for converting the prohormones dehydroepiandrosterone and androstenedione into testosterone and the most powerful androgen dihydrotestosterone (Rosenfield R.L., 1986; Djikstra A.C. et al., 1987; Itami S. et al. al., 1988; Sawaya M.E. et al., 1991; Rosenfield R.L. and Lucky A.W., 1993).

Most authors (Mowszowicz I. et al., 1983; George F. et al., 1991; Normington K. and Russell D.W., 1992; Andersson S. et al., 1993; Beckmann M.W. et al., 1993; Wilson J.D. et al., 1993; Russell D.W. et al., 1994) associate the activity of androgens in relation to the sweat and sebaceous glands with the presence of 5a-reductase, which is a microsomal NADP-H-dependent enzyme (Table 2). Androgen receptors on the skin are mostly localized in the dermal papilla and sebaceous gland epithelium (Choudhry R. et al., 1992; Blauer M. et al., 1991; Liang T. et al., 1993; Randall V.A. et al., 1993 ; Itami S. et al., 1991).

R.L. Rosenfield and D. Deplewski (1995) modeled the interaction of androgen receptor sensitivity and androgen levels in the development of cutaneous manifestations of androgen excess. With normal testosterone concentrations, only a small percentage of women with high skin sensitivity to androgens will have hirsutism or acne vulgaris(idiopathic in nature). With a moderate increase in testosterone levels, most women will have these skin manifestations. With a significant increase in testosterone levels, almost all women will have hirsutism or acne vulgaris. It remains unclear what regulates the nature of the response (excessive male-pattern hair growth and/or acne and/or alopecia). Hirsutism, acne, and alopecia are all manifestations of androgen excess. The sebaceous gland and hair follicle form a single morphological unit. What causes the differences in the expression of androgenic action? Possibly due to differences in androgen metabolism or genetic changes in factors modulating the effects of androgens.

Thus, the use of modern COCs for the treatment of acne and seborrhea is pathogenetically justified , which suppress the secretion of gonadotropins, stimulate the synthesis of sex steroid binding globulin and reduce the activity of 5a-reductase.

According to WHO recommendations (Improving Access to Quality Care in Family Planning, 2002) and the International Family Planning Federation (IMAP Statement on Steroidal Oral Contraception, 1998), the ethinyl estradiol content in COCs should not exceed 35 mcg. In studies by E. Spitzer et al. (1996), O. Lidegaard et al. (1998), M.A. Lewis et al. (1999) provides the following COC classification:

  • first generation - containing i50 mcg ethinyl estradiol and progestogen;
  • second generation - containing Ј35 mcg ethinyl estradiol and progestogen, including norgestimate, but not gestodene or desogestrel;
  • third generation - containing 20-30 mcg ethinyl estradiol and gestodene or desogestrel.

The main differences in the clinical and metabolic effects of COCs are determined by their progestogen component . Progestogens included in contraceptive drugs are derivatives of progesterone and testosterone.

Nortestosteroid compounds are characterized by the following features of their chemical structure - the absence of a methyl group at position 19 and the presence at C 17 of an ethynyl (17a-ethynyl gonans) or methyl group (17a -methyl gonans), which explains the pronounced antigonadotropic and progestogenic effect. All 19-nortestosterone derivatives, to a greater or lesser extent, have residual androgenic and anabolic activity, which actually determines the frequency of side effects.

Among modern progestogens, of particular interest is desogestrel (active metabolite 3-keto-desogestrel). Numerous studies (Kloosterboer H. et al., 1988; Pollow K., Jichem M., 1989; Phillips A. et al., 1990; Fuchrman U. et al., 1995; Kuhl H., 1996) confirmed the highest the selectivity of its action - with high antigonadotropic and progestogenic activity, desogestrel has the lowest androgenic activity (Table 3). Modified by D. Upmalis, A. Phillips (1991) selectivity index, presented as a ratio:

SELECTIVITY INDEX = A/B, where

A- The concentration of progestogen required to displace 50% of the reference steroid from its connection with androgen receptors,
B- The concentration of progestogen required to displace 50% of the reference steroid from its connection with progesterone receptors,

is 33 for 3-keto-desogestrel, 28 for gestodene, 11 for levonorgestrel. The glucocorticoid and mineralocorticoid effects of desogestrel are comparable to the effects of natural progesterone. Despite the fact that the actual biological activity of progestogen in vivo does not always fully correlate with the received in vitro receptor characteristics, the latter are used to substantiate pharmacological effects and therapeutic indications.

In combination with ethinyl estradiol, desogestrel has a pronounced antiandrogenic effect and can be used for acne and seborrhea. Desogestrel has a low affinity for globulins that transport sex steroids (Table 4), which allows it not to interfere with the estrogen-induced increase in the level of sex steroid-binding globulin (SHBG) and the decrease in the concentration of active androgens in the blood serum.

Recently, the special use of a new “hybrid” (structurally related to progesterone and testosterone) progestogen has been increasingly discussed in domestic and foreign literature. dienogest . Like all 19-nortestosterone derivatives, dienogest has some antiprogestogenic, low estrogenic and antiestrogenic effects. In addition, an antiandrogenic effect is indicated, amounting to about 30% of the activity of cyproterone acetate (i.e., comparable to the antiandrogenic effect of desogestrel). The moderately expressed antigonadotropic activity of dienogest explains its predominant use for hormone replacement therapy.

An important property of progestogen, which determines the advisability of its use, is its biological activity.

Adequate transformation of the endometrium caused by progestogens in doses:

3-keto-desogestrel - 2 mg/cycle

gestodene - 3 mg/cycle

levonorgestrel - 4 mg/cycle

dienogest - 6 mg/cycle

cyproterone acetate - 20 mg/cycle.

Ovulation blocking dose is:

gestodene - 40 mcg/day

3-keto-desogestrel - 60 mcg/day

levonorgestrel - 60 mcg/day

dienogest - 1000 mcg/day

cyproterone acetate - 1000 mcg/day.

In a study by D. Mango et al. (1996) showed a more pronounced increase in SHPS content when taking a COC containing 30 mcg ethinyl estradiol and 150 mcg desogestrel than when taking a COC containing 30 mcg ethinyl estradiol and 75 mcg gestodene. M. Levrier et al. (1988), R. Erkkola et al. (1991), C. Charoenvisal (1996) did not reveal significant differences in women with acne and seborrhea who used COCs with 150 mcg of desogestrel and 2 mg of cyproterone acetate.

In order to study the clinical effectiveness of the modern three-phase combined oral contraceptive Tri-Mercy with desogestrel in women with acne and seborrhea, a study was conducted in which 1873 patients were included by random sampling. Before your appointment Tri-Mercy and after 3 months of taking COCs, a survey was conducted. The study examined the effect on skin cleanliness, drug tolerability, and the frequency of side effects.

Statistical processing of the obtained results was carried out using generally accepted methods of nonparametric statistics. Sampling variability in the reported study results was described by the median and interquartile range (indicated as the 25% and 75% percentiles, i.e., the upper limit of the 1st quartile and the lower limit of the 4th quartile). The critical level of significance of the null hypothesis (about the absence of differences and influences) was taken equal to 0.05. Calculations were performed using the statistical analysis application package Statistica®5.1 (StatSoft, USA). Statistical data analysis was not performed for women who completed the questionnaires incorrectly or incompletely. In 200 cases (10.7%), the results of the repeated survey were presented on primary forms, which lacked information about the presence and nature of side effects observed while taking COCs. 145 questionnaires (7.7%) contained incomplete information (i.e. one or more items were missing). The dropout rate was 18.4% (345 women). The group of women with correctly completed questionnaires was comparable to the group of all respondents. Patients with correctly and incorrectly filled out questionnaires did not differ from each other in age, skin type, or use of contraceptives in the past (Table 5). The age characteristics of the women who took part in the study are presented in Table. 6.

The work assessed the frequency of use of various methods of contraception in the past. 656 (42.9%) women took COCs. Of these, 128 (19.5%) women took modern microdose drugs (containing 20 mcg ethinyl estradiol and gestodene, desogestrel), modern low-dose COCs (containing 30-35 mcg ethinyl estradiol and gestodene, desogestrel, norgestimate) - 170 (25.9%) women. 19 (2.9%) women used drugs with high (more than 35 mcg) ethinyl estradiol content. The postcoital drug Postinor was used by 8 (1.2%) women.

151 (22.4%) women had skin type I, 1004 (65.6%) women had type II, and 373 (24.4%) women had type III (Fig. 1).

Rice. 1. Distribution of women in the studied sample by skin type

While taking the drug, there was a statistically significant decrease in skin oiliness and acne (Fig. 2,3).

Rice. 2. Reduction of acne while taking Tri-Mercy

Rice. 3. Reducing skin oiliness while taking Tri-Mercy

While taking Tri-Mercy, a decrease in hair oiliness was noted. If at the beginning of the study 295 (19.3%) women complained that their hair became oily very quickly, then after three months of taking Tri-Mercy only 53 (3.5%) women complained (Fig. 4).

Rice. 4. Reducing oily hair while taking Tri-Mercy

At the beginning of the study, 1198 (78.4%) women experienced difficulties with hair styling (Fig. 5). While taking Tri-Mercy, their number decreased to 473 (31.0%) women, of whom only 53 (3.5%) women noted that it was very difficult to style their hair.

Rice. 5. Conditions of scalp hair when taking Tri-Mercy

Side effects while taking Tri-Mercy were noted by 308 (20.2%) women. The main ones are nausea, which was noted by 109 (7.1%) women, scanty bleeding - 87 (5.7%), engorgement of the mammary glands - 35 (2.3%), weight gain - 32 (2.1%). %) women.

1453 (95.1%) women noted their satisfaction with taking Tri-Mercy (Fig. 6). Moreover, 1430 (93.6%) women expressed a desire to recommend using Tri-Mercy to their friends.

Rice. 6. Results of taking Tri-Mercy

The highest selectivity and low androgenic activity of desogestrel, its optimal combination with ethinyl estradiol (allowing it not to interfere with the ethinyl estradiol-induced increase in the level of sex steroid binding globulin), and the low cyclic content of desogestrel distinguish Tri-Mercy from other modern COCs. Taking Tri-Mercy for 3 months significantly reduces skin manifestations of hyperandrogenism , which, combined with high contraceptive effectiveness and good tolerability, allows us to consider it the first choice contraceptive, especially for young women with skin manifestations of hyperandrogenism. Literature:

1. Andersson S., Chan H.K., Einstein M., Geissler W.M., Patel S. The molecular genetics of steroid 5(-reductase) // J. Endocrinol. - 1993. - Vol. 139, Suppl. - P. 17.

2. Beckmann M.W., Wieacker P., Dereser M.M., Flecken U., Breckwoldt M. Influence of steroid hormones on 5(-reductase activity in female and male genital skin fibroblasts in culture // Acta Endocrinol. (Copenh.). - 1993 - Vol. 128. - P. 161-167.

3. Blauer M., Vaalasti A., Pauli S.L., Ylikomi T., Joensuu T., Tuohimaa P. Location of androgen receptor in human skin // J. Invest. Dermatol. - 1991. - Vol. 97. - P. 264-268.

4. Charoenvisal C., Thaipisuttikul Y., Pinjaroen S., Krisanapan O., Benjawang W., Koster A., ​​Doesburg W. Effects on acne of two oral contraceptives containing desogestrel and cyproterone acetate // Int. J. Fertil. Menopausal. Stud. - 1996. - Vol. 41. - P. 423-429.

5. Chieffi M. Effect of testosterone administration on the beard growth of elderly males // J. Gerontol. - 1949. - Vol. 4. - P. 200-204.

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For health, it is necessary to maintain normal levels of hormones in the human body. Testosterone, produced by the adrenal glands and genital appendages, plays a major role in both men and women. It is also called a steroidal androgen. As soon as this hormone deviates from the norm, serious health problems begin. Here you can’t do without antiandrogen drugs.

Male steroid

It is androgens that contribute to the development of sexual characteristics in both representatives of humanity. Only in each organism it acts differently:

  • The main “factories” for the production of steroid hormones in men are located in the testes and adrenal cortex. A sufficient amount of androgenic enzyme in the blood determines the appearance of a beard and the growth of a mustache, developed muscles, and a voice with a low timbre;
  • In women, the male enzyme is produced according to the same principle and by the same organs. But in their body, steroids are responsible for regulating the menstrual cycle, the appearance of hair in the bikini area and the development of a female figure.

Androgens are also related to the production of other enzymes, influence the formation of the bone skeleton, and also regulate the production of sebum and the functioning of the sweat glands.

Note! When the level of this androgen in a woman’s blood begins to go off scale, her figure changes, becoming more masculine. Hairs above the upper lip and the appearance of a beard may also appear.


Hair begins to grow where women usually don’t have it: on the back, stomach, breasts, hips, face. The glands that produce sebum fail, and immediately problems with the epidermal layer begin - seborrhea develops, acne appears, etc.

If you do not pay attention to these symptoms and do not carry out treatment on time, then hormonal imbalance will lead to various pathologies: endocrine diseases (in particular, inflammation of the thyroid gland), tumors of the adrenal glands and reproductive organs. As a result, women experience disruptions in the menstrual cycle, miscarriages in pregnant women, and infertility.

Antiandrogens

To correct the situation and return the hormone balance to normal, doctors recommend antiandrogen drugs for women. They will not only help reduce the level of male enzymes, but also bring them to the optimal level. All antiandrogenic drugs inhibit testosterone into another active hormone, which is harmless for women.


Indications for the use of androgenic drugs in men are seborrheic and other types of alopecia, hirsutism, and prostate cancer. It is prescribed to women for the treatment of infertility, endometriosis, and uterine fibroids. But treatment with such drugs is also fraught with negative consequences:

  • in the stronger half of humanity, changes in the prostate gland are observed, the ability to produce full-fledged semen decreases, libido decreases, and impotence develops;
  • in women, hair disappears not only on the body, but also the development of alopecia on the head is observed; the function of the sebaceous glands decreases, and at the same time the work of the ovaries is inhibited.

But these side effects are observed only during the period when hormonal pills with an antiandrogenic effect are taken. Under the influence of the drugs, steroid androgens break down into their components and are quickly eliminated from the body, without having time to seriously affect the functioning of the main organs.

COCs

All oral contraceptives of combined action basically contain antiandrogens - the female sex hormones ethinyl estradiol and progestogen. They are able to bind to androgen receptors that produce testosterone. COCs are excellent at reducing the level of male enzymes in the female body.


Among drugs with similar effects, “Zhanin”, “Logest”, “Yarina”, “Belara” and others are considered popular. But no matter how good birth control pills are, girls should take them with caution.

Properties of oral contraceptives:

  • estrogen entering the liver stimulates the production of globulin, which leads to a decrease in testosterone in the blood;
  • progestogens prevent testosterone from going into its active form;
  • the drug reduces the production of male hormone in the ovaries;
  • COCs are antagonists of gonadotropic enzymes.

Important! For girls, contraceptive pills should be selected taking into account individual characteristics and only after a hormonal examination. In this case, you should be prepared for long-term use of COCs, since the first effect can be observed no earlier than after 3 months.

All drugs prescribed for hormonal imbalance are divided into 2 types: steroidal and non-steroidal. Such products are available in various forms: tablets, dragees, capsules, sprays and injection solutions. Which one to choose is decided only by the attending physician, based on the individual characteristics of the developed disease.

Steroid drugs

Steroid drugs are based on synthetic progesterones: dienogest, spironolactone, chlormadenone acetate, but the so-called CPA (cyproterone acetate) is most often used in practice.


Features of some drugs are given in the table below.

Steroid antiandrogens

NameRelease formDescriptionContraindications
"Androcur"Tablets, solutionsPrescribed to women for:
hair growth on the face and body (hirsutism);
development of androgenic type baldness;
for various forms of acne, accompanied by scars, nodules, inflammation;
with persistent seborrhea
with predispositions to thrombosis;
anemia;
diabetes mellitus;
liver problems;
meningomyomas;
with prolonged depressive states;
when carrying a child and during lactation
"Diana-35"DrageeThe drug belongs to the category of antiandrogenic contraceptives, which are prescribed to prevent pregnancy in the following cases:
with male pattern hair growth or baldness;
acne
in case of disturbances in the synthesis of fat production;
for liver diseases;
dermatoses;
breast oncology;
pregnancy
"Klymen"DrageeHelps prevent the premature onset of menopause, while eliminating all its symptoms (profuse sweating, dizziness, palpitations, hot flashes, sleep disturbance, increased nervous excitability, etc.).
The product is recommended for women of reproductive age to eliminate bleeding from the uterus and regulate the cyclicity of menstruation.
It also helps reduce vaginal dryness.
It is also prescribed for those with a predisposition to oncological diseases such as hyperplasia and endometrial cancer.
The product stimulates the production of collagen in tissues, thereby slowing down the aging process
Cannot be prescribed for:
thromboembolism and thrombosis;
pathologies affecting the liver;
blood loss of unknown etiology;
tumors in the mammary glands;
pregnancy
"Chloe"Birth control pillsIn addition to antiandrogenic, it also has a gestagenic effect.
Recommendations for use:
with mild hirsutism;
acne;
profuse baldness
Cannot be prescribed for:
thrombosis and embolism;
various cardiovascular diseases;
bleeding from the uterus;
oncologies with hormonal dependence;
neurological migraines;
pregnancy;
women over 40

When taking these drugs, it is worth taking into account that their synthetic base has a detrimental effect on the functioning of the gastrointestinal tract, leading to various disorders of this system.

Non-steroidal drugs

Nonsteroidal drugs are considered better than steroidal ones, as they are “pure” antiandrogens with high activity. They are not endowed with the properties of androgens and are selective when binding to hormones.

Among such drugs, the drugs presented in the table below are especially distinguished.

Nonsteroidal antiandrogens

NameIndicationsContraindications
"Flutafarm"Prescribed for varying degrees of hirsutism, disruptions in the menstrual cycleRestrictions on intake exist for cardiovascular diseases.
Contraindicated for use in pathologies of the kidneys, liver and thyroid gland
"Flutamide"Available in the form of an ointment and recommended for facial and body hair growth in women.Prescribe with caution if you are prone to thrombosis and other problems of the circulatory system, as well as with heart pathologies.
Do not take if you have kidney disease or if you are pregnant
"Dutasteride"Inhibits the enzyme responsible for converting testosterone to DHT. Refers to drugs with narrowly targeted action and does not affect other hormonesAs with any antiandrogenic drug, use with caution.
Prohibited for pregnant and lactating women
"Metmorphine"Prescribed for obesity, metabolic disorders, diabetes. A decrease in insulin levels also leads to a decrease in the production of active DHTIt is considered safe in small doses, but if taken frequently it can cause persistent diarrhea. Therefore, it should be taken with caution and only after meals.
For liver and heart diseases, this drug is either not prescribed, or it is taken strictly under the supervision of a doctor.

Non-steroidal drugs not only help regulate hormonal levels, but are also involved in combination therapy for infertility, as well as the treatment of a number of oncological diseases.

Herbal preparations

Separately, we can highlight herbal products that give an antiandrogenic effect. True, they do not have contraceptive properties, but they help restore hormonal levels well, acting more gently on the body than COCs. A list of these drugs is given in the table below.

NamePeculiarities
LicoriceReduces testosterone levels in women, but this requires large dosages of the drug. With long-term use, side effects may occur: hypertension, increased cortisol
CinnamonBy affecting the production of insulin, it also reduces the male hormone. Can be used as a seasoning for carbohydrate foods or as part of dietary supplements
Flax seedsThey have a narrowly targeted effect - they reduce free and total testosterone, but have no effect on estradiol
Chinese peonyPromotes the production of estrogen and reduces testosterone levels in the female body

For your information. You can find many other antiandrogenic drugs in the pharmacy, but you should not purchase them yourself without consulting your doctor. Allergic reactions to each herbal remedy must also be taken into account.

Side effects

Any of the drugs described (especially birth control pills), along with restoring hormonal levels, has side effects that occur not only with long-term use:

  • nausea and vomiting accompanied by diarrhea;
  • true or false gynecomastia;
  • liver dysfunction and increased appetite;
  • fatigue and insomnia;
  • dizziness and headaches;
  • in some cases, cataracts may develop.

It should be taken into account that drugs that have an antiandrogenic effect reduce libido and reproductive ability in men, and also cause anxiety and lead to depression.

Important! Girls who do not have sexual intercourse should not take birth control pills to avoid a number of consequences.


These drugs also affect psychomotor perception, reducing its speed. Therefore, while taking antiandrogen drugs, it is necessary to refrain from any activity related to concentration. You should not prescribe these medications yourself, especially if you are taking other medications with which androgens may be incompatible.

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