In connection with the establishment of the key role of androgens in the development of common baldness and manifestations of hyperandrogenism syndrome, substances with antiandrogenic properties are used in the treatment of these diseases. The mechanism of action of antiandrogens is different. Suppression of the effect of androgens is achieved either by inhibiting the activity of the enzyme 5a-reductase, or by blocking androgen receptors in target tissues, or by increasing the production of sex hormone binding globulin.
Antiandrogens with steroid structure
At a daily dose of 5 mg, finasteride (Proscar) is used in the treatment of prostate adenoma.
For the treatment of common male pattern baldness, finasteride is recommended at a dose of 1 mg per day (Propecia). Propecia prevents the progression of baldness and promotes new hair growth. The drug is intended for long-term (12-24 months) use. The therapeutic effect is noticeable after 3-6 months of general treatment, but significant clinical improvement is observed by the end of the first year of therapy in 48% of patients and by the end of the second year in 80%. The drug is indicated for the treatment of androgenic alopecia only in men: it is most effective for initial and moderately severe baldness (types I-III according to J. Hamilton); does not affect hair growth in the area of bitemporal bald patches.
Contraindications:
Cautions: Prescribe with caution to patients with functional liver disorders, since it is in the liver that finasteride is most actively metabolized.
Side effects: 1.2% of patients develop impotence, decreased libido, decreased ejaculate volume, and gynecomastia. These complications go away when you stop taking the drug and do not require additional treatment.
Dosage: 1 mg (1 tablet) 1 time per day, regardless of meals. Long-term use is recommended. Discontinuation of treatment returns the patient to the starting state of baldness approximately one year after discontinuation of the drug.
The optimal dose of cyproterone acetate (CPA) for the treatment of common alopecia has not yet been established. Good results were obtained when high doses of CPA were prescribed (50-100 mg daily from days 5 to 14 of the menstrual cycle) in combination with 0.050 mg ethinyl estradiol from days 5 to 25 of the cycle. Efficiency control, carried out a year later to avoid possible seasonal fluctuations, objectively showed an increase in hair diameter and the number of hairs in the anagen phase. It was noted that optimal results are achieved in women with normal serum levels of vitamin B12 and iron.
According to another point of view, low doses of CPA are more effective for normal hair loss than high doses. In this regard, the contraceptive drug Diane-3 5 (Diane-3 5), 1 tablet of which contains 2 mg of CPA and 0.035 mg of ethinyl estradiol, deserves attention. The drug is taken 1 tablet per day from the 1st day of the menstrual cycle according to the scheme indicated on the package. The duration of treatment for normal baldness is 6-12 months.
At a dose of 100 mg per day and above, CPA is hepatotoxic. In recent years, there have been reports of an increased risk of developing liver malignancies while taking CPA. The prescription of the drug must be agreed with a gynecologist-endocrinologist.
For many years, combined oral contraceptives containing estrogens and gestagens have been used to treat androgenic alopecia and other manifestations of hyperandrogenism syndrome in women. Estrogens increase the production of sex hormone binding globulin; as a result, there is a decrease in serum testosterone levels. Gestagens inhibit 5a-reductase and also bind cytosolic androgen receptors. Currently, preference is given to third-generation gestagens that are devoid of antiestrogenic side effects (desogestrel, norgestimate, gestaden). Good results have been achieved with the use of the drug Silest, containing norgestimate and ethinyl estre diol. Unfortunately, long-term (more than 5 years) use of these drugs causes dysmenorrhea. The prescription of oral contraceptives must be agreed with a gynecologist-endocrinologist.
Local use of estrogens and gestagens, separately or in combination, has proven to be ineffective in both women and men.
Prescribed to women over 30 years of age for 6 months. At a daily dose of 200 mg, spironolactone has been tested as a treatment for common baldness in 6 women; a good cosmetic result was achieved. Side effects include swelling of the mammary glands and dysmenorrhea. Since the drug causes feminization of the male fetus, the prescription of oral contraceptives is necessary. Long-term use of spironolactone increases the risk of breast tumors.
In men, spironolactone causes decreased libido and gynecomastia. The drug is contraindicated in acute renal failure, the nephrotic stage of chronic nephritis. Caution should be exercised when prescribing the drug to patients with incomplete atrioventricular block.
Nonsteroidal antiandrogens
Drugs with a very strong antiandrogenic effect; block androgen receptors of target cells, preventing the development of the biological effects of endogenous androgens. Used for palliative treatment of prostate cancer. There is no information on systemic use for the treatment of common baldness. Experience has been reported with the topical use of flutamide in small doses in combination with minoxidil. This combination gave more noticeable results than minoxidil monotherapy.
Antiandrogens of plant origin.
The fruits of the dwarf palm contain a number of fatty acids (capric, caprylic, lauric, oleic and palmitic), a large amount of phytosterols (beta-sitosterol, cycloartenol, stigmasterol, lupeol, etc.), as well as resins and tannins. The red berries of the dwarf palm have long been used in folk medicine to treat prostatitis, enuresis, testicular atrophy, and impotence.
Serenoa repens extract is the active substance of the drugs Prostaseren, Permixon, Prostamol-uno, Tricoxen. The mechanism of the antiandrogenic action of the extract has not yet been fully elucidated. Its inhibitory effect was revealed at the level of estrogen and androgen receptors in the nucleus. The drugs are recommended for the treatment of benign prostatic hyperplasia; they do not affect the levels of T, FSH and LH in the blood plasma of men. There is not yet enough data on the effect of dwarf palm fruit extract on the process of baldness for it to be recommended for the treatment of androgenetic alopecia, although positive results have already been published, in women. When used in recommended doses, the drugs are well tolerated by patients and do not affect sexual activity, appetite, body weight, blood pressure, heart rate; no cases of overdose have been reported. To date, no clinically significant interactions of these drugs with other drugs have been identified.
A lipophilic extract from the fruits of the Sabal palm tree inhibits the enzymes 5a-reductase and aromatase, thereby inhibiting the formation of dihydrotestosterone and 17-estradiol from testosterone; is the active substance of the herbal medicine Prostaplant. The drug is used for the treatment of benign prostatic hyperplasia in adult men and has no contraindications. Cases of overdose of the drug Prostaplant have not been reported, drug interactions have not been described.
There is currently no information on the use of Prostaplant for the treatment of androgenetic alopecia, but in the future Prostaplant, like other herbal remedies, may seriously compete with finasteride, which has a number of serious side effects.
Thus, systemic use of antiandrogens is effective in the prevention and treatment of common baldness, but the need for long-term (possibly lifelong) use of these drugs is disappointing.
Other drugs
Cimetidine belongs to the first generation of histamine H2 receptor blockers and is used in the treatment of peptic ulcers; is also a DTS inhibitor. As a treatment for common baldness, the drug was tested on 10 women who received 300 mg of cimetidine 5 times a day for 9 months. The results of therapy were assessed as good and excellent. At the same time, there is a publication describing alopecia caused by taking cimetidine.
Antiandrogen drugs for women are used quite widely.
They help female representatives to remain healthy and attractive, to maintain a share of feminine charm even in situations when male hormones take over.
Currently, increase has become a real problem, because many girls are forced to resort to the use of drugs that have an antiandrogenic effect.
They are male steroid hormones. They are responsible for the functioning of the genital organs and the manifestation of special sexual characteristics in men.
The broad group of androgens includes the following elements:
Androgens are present in the blood not only in men, but also in girls. They are normally produced in small quantities by the adrenal glands and ovaries.
It is these substances that are responsible for normal hair growth in the pubic area and a normal menstrual cycle.
Androgens are involved in the regulation of the sweat and sebaceous glands. Therefore, women with an excess of these hormones often experience skin and hair problems.
Development is possible. In this case, hair loss follows the male pattern. Bald patches appear on the temporal region.
With an excess of such hormones, a woman takes on the appearance of a man, and the manifestation of external characteristic signs is possible:
The appearance of vegetation is not the most dangerous consequence of the riot of androgenic hormones in a woman’s body. As a result of the activity of these hormones, a number of pathologies can appear:
A characteristic manifestation of excess male hormones is the absence of menstruation. The development of infertility is possible.
If symptoms are present, drugs with the ability to have an antiandrogenic effect should be selected.
These drugs include combined oral contraceptives (COCs), which are selected by a gynecologist depending on the results.
Women whose ovaries and adrenal glands overproduce male sex hormones are forced to select contraceptives with an antiandrogenic effect.
Such medications have a special effect on the body of girls and allow them to get rid of the manifestations characteristic of excess male hormones.
An excess of male hormones negatively affects a woman’s psycho-emotional state; this is primarily due to the appearance of excess hair on the face and body. Even barely noticeable hairs above the lip cause the development of stable complexes.
Among the list of main factors that separate the manifestation of male hormones in excess quantities, the following pathologies are distinguished:
To eliminate the causes that caused the manifestations of androgenization, hormonal contraceptives with antiandrogenic action are often used.
Some herbs have antiandrogenic activity, but it is important to consider that plant substances under no circumstances is it possible used in combination with synthetic hormones.
The latter neutralize the healing effect of herbs. If a doctor has prescribed COCs to normalize hormonal levels, you should not give preference to herbal stabilizers.
Among the advantages of consuming herbal antiandrogens are the following factors:
Plant antiandrogens do not have a contraceptive effect. Among them healing abilities special provisions are highlighted:
The antiandrogenic properties of herbs have not been fully studied. They can be used, like any other drugs, after prior consultation with a doctor.
Only the specialist will be able to determine the required dosage and frequency of administration, which will benefit and not harm the patient’s body.
(COCs) contain a combination of two main female sex hormones:
Progestins are included in COCs in significant concentrations. These drugs consist of a special type of substance that has the ability to bind to andorene receptors.
It is these elements that are responsible for the production of testosterone in the body. Under the influence of contraceptives, the production of male sex hormones is reduced.
Among the list of popular combined oral contraceptives with antiandrogenic effects, the following popular drugs stand out:
The elements ethyl estradiol and progestogen are contained in sufficient quantities in these medications. They are presented as the main component of successful therapy.
Monophasic oral contraceptive with antiandrogenic properties - a drug containing hormones called Jazz.
The drug has a number of contraindications and in some cases causes side effects. In addition, the remedy not recommended for girls under 35 years of age.
In any case, the possibility of using such a component should be discussed with your gynecologist.
The activity of COCs that have an antiandrogenic effect is aimed primarily at several elements that ensure the production of sex hormones:
Contraceptive drugs containing antiandrogens, when taken for a long time, normalize a woman’s hormonal levels.
In most situations, girls are selected for a drug that has the lowest risk of side effects, because it is necessary to use the drug for six months to normalize hormonal levels.
The effect of use appears much earlier - within 2-3 months from the start of use.
Oral contraceptives have a beneficial effect on menstruation, lead to the appearance of menstruation “on schedule,” and remove rashes from the facial skin.
Hormonal drugs with antiadrogenic effects are used not only to prevent unwanted pregnancy.
Often such drugs are prescribed to normalize the hormonal levels of female representatives. The drugs reduce the intensity of production of male steroid hormones.
Among the list of indications for taking drugs with an antiandrogenic effect, the following types are distinguished:
Combined oral contraceptives, which have an antiandrogenic effect, have contraindications indistinguishable from the use of other hormonal drugs.
Several years ago, the World Health Association prohibited the use of this type of medication for girls who are not sexually active.
Not so long ago, low-dose drugs were included in the drugs approved for use in these cases.
This decision was pleasant due to the fact that the safety of the effects of drugs of this kind on the female body has been proven.
Birth control pills are a discovery of modern medicine. They help many women not only prevent unwanted pregnancy, but also, on the contrary, promote fertilization. These COCs (combined oral contraceptives) include tablets with an androgenic effect. They are designed to regulate the level of sex hormones related to males - androgens. Sometimes, due to hormonal imbalance, the patient experiences pain, the inability to conceive and bear a child, and skin pathologies. Then gynecologists include contraceptive pills with an androgenic effect in the complex of therapy.
Antiandrogenic from the word “androgen”, meaning male hormone. It is responsible for the manifestation of external and internal sexual characteristics of the stronger sex. Sometimes a woman may have a predominance of androgens over estrogens, which significantly affects her life functions. In such a situation, doctors may prescribe birth control pills with an antiandrogenic effect. This helps to regulate the imbalance and remove the main manifestations of the disease.
A woman can take COCs (combined oral contraceptives) with an antiandrogenic effect after consulting an endocrinologist and gynecologist. It is necessary to check hormone levels before starting pill therapy or using them for contraception. A specialist should select a specific type of COC.
When a patient’s test results show an increased level of androgens, we can talk about a diagnosis of “hyperandrogenism.” It can manifest itself in the following symptoms. Their presence is considered an indication for the use of contraceptive pills with an antiandrogenic effect:
As a rule, women who first encounter the use of COCs do not know that they have a wide spectrum of action. Birth control pills can be prescribed not only to prevent unwanted pregnancy. The drugs successfully cope with the treatment of infertility, hormonal imbalance, and skin pathologies.
In reviews you can often find enthusiastic responses about the effects of contraceptives on the skin of the face. It becomes clear, the rash goes away on its own. In fact, gynecologists and endocrinologists advise paying attention to this criterion when using COCs.
If, during therapy or contraception with pills with an antiandrogenic effect, a woman has an increase in the number of skin rashes or acne begins to develop more often, she should stop taking this type of medication. We are talking about incompatibility. On the contrary, when the skin condition improves while taking COCs, we can talk about the right choice of tablets.
Hormonal birth control pills, despite their effectiveness and versatility, have a number of side effects and can cause health problems if used incorrectly. Before you start taking medications, you should familiarize yourself with the contraindications.
If a woman can apply to herself at least one of the points listed below, using COCs is not recommended:
Please note - smoking and taking birth control pills are incompatible!
This increases the risk of adverse reactions. It has been proven that almost 60% of patients who took COCs for a long time and consumed nicotine subsequently have cardiovascular problems: thrombosis, varicose veins, arrhythmia.
Today, the pharmacological market is replete with a selection of birth control pills with an antiandrogenic effect. Women sometimes find it difficult to make a choice. Many people do not know what to pay attention to, what are the pros and cons of each product. The table below will help you consider the most popular and effective antiandrogen pills and make the right choice.
| Name | Pros | Cons | Average cost |
|---|---|---|---|
| Diana is 35 | Regulation of hormonal levels and the menstrual cycle. Helps in the complex treatment of gynecological problems. | Large list of side effects. Pot reviews are not suitable for all women with hyperandrogenism. High cost. | 850 rub. |
| Logest | Ease of use, suitable for most women, a small list of contraindications and side effects. | Excess weight, decreased sexual activity, decreased libido. | 720 rub. |
| Yarina | Normalizes the menstrual cycle, acne goes away quickly, skin rashes stop, ease of use. Used in the treatment of polycystic ovary syndrome, dysmenorrhea, endometriosis. | High cost, frequent side effects such as headaches and mood swings. | 800 rub. |
| Janine | They are used in the complex treatment of polycystic ovary syndrome, dysmenorrhea, endometriosis, and infertility. Help regulate and restore the menstrual cycle. | Side effects often occur in the form of excess weight gain and depression. High cost. | 800 rub. |
| Jess | Convenient packaging, which makes it easy to take, detailed instructions for use. They restore the menstrual cycle and relieve inflammatory processes in complex therapy. | High cost. List of contraindications. | 900 rub. |
| Marvelon | It is used as a complex therapy for inflammatory processes in the ovaries and uterus. Helps restore the menstrual cycle. | A large list of adverse reactions, which often manifest themselves according to reviews in the form of headaches, stool problems, and chest pain. | 640 rub. |
| Tri-Mercy | The menstrual cycle is restored and skin rashes go away. Average cost. | Adverse reactions often occur. Many women note enlarged mammary glands, weight gain, and decreased libido. | 650 rub. |
How to take oral contraceptives correctly? The table shows birth control pills that have shown high effectiveness in relation to hyperandrogenism over the past 5 years. These names of COCs with an antiandrogenic effect are worth remembering if a woman has signs of hormonal imbalance. Together with a gynecologist, it will be possible to select a specific medication after tests and examination.
When a woman starts taking pills on her own for the first time, she has a lot of questions about the best time of day to take them, what to do if she misses them, etc. The instructions for use should provide answers to these questions. If for some reason it is unavailable, you can rely on standard recommendations for taking COCs. They are as follows:
If you follow all the recommendations of specialists, birth control pills with a cosmetic effect will become a real salvation. Consulting a specialist will help prevent the risk of adverse reactions and complications. Gynecologists and endocrinologists have extensive experience; they prescribe pills based on the patient’s body weight, individual characteristics, concomitant pathologies, and age.
Probably no acne treatment has caused as much controversy, hope, and disappointment as antiandrogens. Every now and then, reports appear in the press, on television and on the World Wide Web about both the miraculous results of their use and their complete ineffectiveness. It is difficult to figure out who is telling the truth, and mainly because the disputing parties prefer not to discuss the mechanism of action of these drugs, the peculiarities of their use by specific patients and other important details that are decisive in assessing the effectiveness of the drug. Basically there is a pointless discussion on the principle “I tried it, it didn’t help me, and therefore it’s nonsense!”
But what can we talk about if it is unknown how a particular patient used this drug, what concomitant diseases he has, etc.?
It’s even more strange (in my opinion) to take any drug (even on the recommendation of a doctor!) without knowing how it works. After all, health is the personal value of every person, and to preserve it, it is worth thinking about what is being taken, how to reduce the possibility of adverse consequences, and whether it is even possible to get by with a safer drug.
So, hormonal treatment, accompanied by the intake of sebosuppressors-antiandrogens, affects only seborrhea. And nothing else: antiandrogens themselves do not reduce the number of rashes, do not kill bacteria, and do not have an anti-inflammatory effect.
Accordingly, you should not expect a quick and comprehensive result from these drugs: their action is similar to the action of retinoids, which does not appear immediately, but over time gives a very noticeable effect. The most effective drug from this group is, without a doubt, cyproteronacetate, or CPA for short.
This substance has the ability to bind to the receptors of male sex hormones (androgens), which are always formed in the body of women, although not in such large quantities as in men. And the sebaceous glands are very sensitive to an increase in the level of androgens in the blood, and react to it quite definitely - by increasing the amount of sebum synthesized.
CPA “turns off” the receptors of male sex hormones, making them less sensitive to even large amounts of them, after which the receptors almost do not respond to them, and the synthesis of sebum decreases. As a result, the formation of comedones stops (or is greatly weakened), which means that inflammation is deprived of the basis for its occurrence. As you can see, at first glance, the effect of this substance on the body is very attractive, since it is aimed at the root cause of acne - seborrhea. For this reason, CPA is widely used in the pharmaceutical industry, thanks to which a number of drugs with a fairly high content of CPA are now widely available, among which are Androkur and Diane-35.
"Androkur" contains 50 milligrams (mg) of the active substance (SPA), that is, an amount sufficient for a single dose. It is usually recommended to take it from the 5th to the 14th day of the monthly cycle (cyclicity and dosage are selected individually by the attending physician!).
It should be taken into account that the first results from its use in the form of a decrease in skin oiliness appear no earlier than after 1 month (and then very rarely), usually only after 6 or more months of regular use. But the resulting result is very stable and lasts a long time.
Take Androkur orally in tablet form after meals, always with a liquid that does not contain alcohol; Usually prescribed 1 tablet (50 mg) 2 times a day. The current release form of "Androkur" is a tablet of 0.05 g (50 mg), usually 50 pieces in a package.
There are contraindications to the use of this antiandrogen drug, and quite significant ones: first of all, all liver diseases (including tumors), hepatitis, chronic depression, severe forms of diabetes, sickle cell anemia, pregnancy, lactation, hypersensitivity to the drug.
It is especially worth dwelling on depression, especially its severe forms: when taking Androcur, patients often experience a pronounced decrease in mood, causeless anxiety, etc., which gradually worsen and develop into real depression.
It is clear that with acne, the state of mind leaves much to be desired, so against this background, taking Androcur may be undesirable.
In addition, the side effect of this antiandrogen drug is a decrease in attention and an increasing inability to concentrate. Accordingly, if you take it, your studies (work) may suffer somewhat. Also, caution is required when taking it for those who drive a car themselves or for other reasons are required to have a quick reaction. If your doctor approves of taking this drug, I strongly recommend that from the first week of taking Androcur you carefully monitor your mood, and track changes in your mood daily in a simple diary.
How people don’t like this! The vast majority of patients do not want to track changes in their mood, well-being, and health in the form of written records. But they are practically invaluable for any doctor: the dynamics of many processes are immediately visible, and you can reduce the likelihood of an error several times, as well as increase the effectiveness of treatment.
Without records, it is not only difficult to achieve a stable result, but the doctor’s work is repeatedly hampered: after all, his usual question is “How are you feeling?” not just a sign of politeness! The doctor needs to get information from you, but usually he hears “Fine”, “So-so”, etc. Agree, there is no information at all in such “standard answers”!
Therefore, I strongly recommend keeping notes and reviewing them periodically: as soon as you begin to notice at least one of the above symptoms of depression, you should immediately inform your doctor about this, discussing with him compensatory measures (usually changing the dosage of the drug or eliminating anxiety factors - driving a car, unnecessary stress, tension, etc.).
An antiandrogen drug such as Diane-35, which, in addition to CPA, also contains ethinyl estradiol in an amount of 35 micrograms (mcg), has a similar effect. This drug is usually prescribed for a period of 24 months (maximum), after which the synthesis of sebum in almost all cases is significantly reduced: this combination causes an even greater suppression of excess activity of the sebaceous glands.
By the way, women taking it note that after 1-2 months of therapy, not only the oiliness of the skin decreases, but also the growth of hair on the head improves, while simultaneously reducing the amount of hair on other parts of the body. This is normal, since this drug has an antiandrogenic effect (like Androcur).
It is possible that after reading these lines, some of my readers saw these andandrogens as a panacea for acne. This is not true: any hormonal drugs are potentially dangerous to the body, and their uncontrolled administration can significantly upset the hormonal balance. There is no need to explain what consequences this is fraught with.
In addition, despite such a high attractiveness of drugs based on CPA, which solve two such different but important problems as reliable contraception and seborrhea, one must remember that these drugs, like any other hormonal drugs, are utilized in the liver. And, most likely, those researchers are right who associate an increased number of cases of tumor development in the liver with long-term use of SPA drugs.
It is an indisputable fact that almost always, while taking these drugs, some cycle disturbances are observed (irregularity, increased pain, etc.).
How to minimize the risk of side effects?
1) Do not take CPA medications without a doctor’s prescription. The rule is simple, but for some reason unpopular in Russia.
2) Observe some dietary restrictions: it is advisable to limit the consumption of heavy foods (fried in oil, smoked meats, etc.), as well as alcohol (the liver will utilize the drug taken daily, so its excess load is simply harmful).
Please note: we are not talking about completely excluding these foods from the diet, but about limiting their quantity - for example, by half or at least a third.
3) Regularly take hepaprotectors (Karsil, Essentiale or Liv.52).
Their high hepaprotective and antitoxic effectiveness has been reliably confirmed, and their ability to stimulate the regeneration of damaged liver cells
more than valuable when taking the above medications.
4) Perform tubage periodically.
The resulting effect of draining excess bile, preventing its stagnation in the ducts and improving metabolic processes allows you to prevent many problems; This procedure is carried out once every week or two, depending on how you feel.
5) Do not forget that the hormonal drugs listed above are not intended to be taken throughout life: it is necessary to take breaks periodically, since over time not only the effectiveness of these drugs decreases, but at the same time the risk of developing liver diseases and hormonal imbalances increases.
Therefore, be sure to take breaks from taking hormonal drugs for at least 1-2 months, having agreed with the gynecologist on the transition to non-hormonal contraceptives.
Following the above rules will not only help prevent hormonal imbalances in the body, but will also help put the liver in order, and, accordingly, reliably maintain your health for many years.
