Taking HRT: pros and cons. Modern pharmacological market of hormone replacement therapy drugs

Despite the fact that menopause is a physiological process, many women need medication correction to make it easier to survive this period of life. Changes in hormonal levels during menopause, which are based on stopping the synthesis of estrogen, negatively affect the ability to work, appearance, physical health and the psycho-emotional state of the lady. Then special medications for menopause can help.

Experts prescribe to many women menopausal age drug therapy, giving preference to homeopathic remedies, antidepressants, dietary supplements and other drugs that do not contain hormones. Limiting the use of hormonal drugs is justified by the fact that they have a large amount side effects.

In this topic, we want to tell you how and when experts recommend taking non-hormonal medications during menopause for hot flashes, depression, fluctuations in blood pressure and other unpleasant symptoms that a woman may experience during this period of life. We will also look at in what cases and what hormonal medications a gynecologist can prescribe, as well as how to take them correctly to avoid unwanted health consequences.

Hormone replacement therapy for relief menopausal symptoms used by specialists in many European countries, since its high effectiveness and safety have been proven. But domestic gynecologists are afraid to alleviate menopause in women with the help of hormone replacement drugs, since they have an impressive list of side effects.

But in the process of clinical observations, European doctors established a number of conditions to minimize the risk of side effects, namely:

• timely prescription and withdrawal of hormonal drugs during menopause;
• presence of indications for hormone therapy;
• the use of microdoses of drugs that will not cause undesirable effects;
• selection of drugs and its dosage, based on the results of a blood test for sex hormones;
• prescribing medications that contain exclusively natural hormones;
• strict adherence by the patient to the recommendations of the treating doctor.

But many patients still refuse hormonal medications for the following reasons:

• consider the use of hormone therapy unnatural, since menopause is a physiological process;
• do not want to take hormonal drugs because they consider them unnatural;
• afraid to gain weight;
• afraid of addiction;
• are afraid of hair appearing in unwanted places;
• think that hormonal drugs damage the gastric mucosa;
• believe that taking drugs with sex hormones increases the risk of developing malignant tumors in the female body.

But these are all just prejudices, because by observing the conditions that we talked about earlier, you can avoid negative health consequences.

Thus, if the body does not have enough of its own sex hormones, then it needs foreign hormones, since hormonal imbalance leads to disruption of the functioning of all organs and systems.

Indications for the use of hormonal drugs during menopause

Hormonal drugs are prescribed in the following situations:

• pathological menopause, which developed as a result of removal of the uterus, taking chemotherapy drugs or radiation treatment;
• menopause occurring in women under 40 years of age;
• too pronounced signs of menopause;
• the development of complications and diseases that appeared against the background of menopause (hypertension, atherosclerosis, polycystic ovary syndrome, dry vaginal mucosa, urinary incontinence and others);
• the patient's desire to eliminate unpleasant symptoms.

Hormonal drugs for menopause in women: side effects and contraindications

• increased fatigue;
• emotional lability;
• swelling;
• weight gain;
• flatulence;
• mastopathy;
• breast tumors;
• severe symptoms of premenstrual syndrome;
• painful menstruation;
• anovulatory menstrual cycle;
• development of benign tumors in the uterus and appendages;
• uterine bleeding;
• increased risk.

The correct selection of the dose, strict adherence to the specialist’s prescriptions, regularity of administration and the combination of estrogens with allows you to avoid the above-mentioned side effects.

The following conditions are absolute contraindications to hormonal drugs:

• allergy to the components of the hormonal drug;
• malignant neoplasms of the mammary glands and female genital organs, including a history of;
• metrorrhagia;
• thrombophilia;
• stroke;
• myocardial infarction;
• varicose veins and blood clots in the veins of the lower extremities;
• increased blood coagulation;
• third stage hypertension;
• severe liver diseases (cirrhosis, liver failure, hepatitis);
• autoimmune diseases (scleroderma, red systemic lupus and others).

Relative contraindications include:

• endometriosis;
• uterine fibroids;
• migraine;
• epilepsy;
• precancerous diseases of the uterus and mammary glands;
• calculous cholecystitis and cholelithiasis.

The best drugs for menopause: list, description, price

The best reviews from gynecologists and patients about combined hormonal drugs latest generation, which contain both estrogen and progesterone.

HRT for menopause includes new generation drugs:

• Angelica – 1300 rubles;
• Klimen - 1280 rubles;
• Femoston – 940 rubles;
• Climinorm – 850 rubles;
• Divina – 760 rubles;
• Ovidon – the drug is not yet commercially available;
• Climodien – 2500 rubles;
• Activel - the drug is not commercially available;
• Cliogest – 1780 rubles.

The listed drugs perform the following tasks:

• eliminate anxiety, improve mood, activate memory and improve sleep;
• increase the tone of the bladder sphincter muscles;
• retain calcium in bone tissue;
• prevent the development of periodontal disease;
• restore the endometrium;
• eliminate dryness of the mucous membranes of the genital organs;
• normalize blood cholesterol levels.

These drugs are available in the form of dragees and tablets. One blister, where each tablet is numbered, is enough for 21 days of use. After a woman takes the last pill, she needs to take a break for seven days and only then start a new blister. Each tablet has its own dose of hormones, which corresponds to the day of the cycle.

Femoston, Aktivel, Kliogest, as well as the drug Angeliq are produced in 28 tablets in a blister, seven of which are pacifiers, that is, they do not contain hormones.

Estrogens

Preparations that contain only estrogens are produced mainly in the form of gels, creams, patches or implants that are placed under a woman’s skin.

The most effective for menopause are the following gels and ointments with estrogens:

• Divigel – 620 rubles;
• Estrogel – 780 rubles;
• Octodiol – the drug is not commercially available;
• Menorest - the drug is not commercially available;
• Proginova - 590 rubles.

Among estrogen patches, the following have performed well:

• Estraderm - the drug is not commercially available;
• Alora – 250 rubles;
• Klimara – 1214 rubles;
• Estramon – 5260 rubles;
• Menostar.

Gels and ointments are quite convenient to use, since they only need to be applied once a day to the skin of the shoulders, abdomen or lower back.

Hormonal patches are an even more convenient dosage form because they need to be changed once every seven days.

Implants that are sutured under the skin last six months, releasing a small dose of estrogen into the blood every day.

Gels, ointments, creams, patches and implants have a number of advantages over oral or injectable forms of hormonal drugs, namely:

• ease of dosage selection;
• gradual penetration of estrogen into the blood;
• the hormone enters directly into the blood without passing through the liver;
• maintaining balance different types estrogens;
• minimal risk of side effects;
• can be used even if there are contraindications to the use of estrogens.

Progestins

To avoid the development of side effects, estrogens are prescribed in combination with progesterone. But if hysterectomy was performed, then the patient is indicated for estrogen monotherapy.

Preparations with progesterone are mainly prescribed from days 14 to 25 menstrual cycle.

There are many progestins on the modern pharmaceutical market, but a number of drugs have the best effectiveness.

1. Tablets and dragees:

• Duphaston – 550 rubles;
• Utrozhestan – 4302 rubles;
• Norkolut – 130 rubles;
• Iprozhin - 380 rubles.

1. Gels and vaginal suppositories:

• Utrozhestan;
• Crinon – 2450 rubles;
• Progestogel – 900 rubles;
• Prajisan - 260 rubles;
• Progesterone gel.

1. Intrauterine hormonal systems:

• Mirena – 12,500 rubles.

IN Lately specialists and patients prefer the Mirena intrauterine device, which is not only a contraceptive, but also contains progesterone and gradually releases it into the uterus.

Instructions for the use of hormonal agents

The choice of hormone therapy regimen, selection of the drug and its dosage should be handled exclusively by a gynecologist. Medicines are prescribed based on the results of a study of a woman’s hormonal levels, as well as taking into account her overall health status. Self-medication can lead to irreversible consequences!

Treatment for menopause begins when the first signs of a lack of sex hormones appear. The duration of treatment depends on the severity of menopause symptoms and can take from one to three years, and sometimes up to ten years.

Most experts believe that taking hormonal drugs should be stopped by the age of sixty, as cancer may develop.

Rules for taking hormonal drugs:

• vaginal suppositories and tablets should be taken at the same time of day, as prescribed by the treating doctor.
• basically all hormones are prescribed daily or cyclically, that is, 21 days with seven-day breaks;
• if the patient forgot to take the drug, then the usual dose should be taken within the next 12 hours, and the next tablet at the appointed time;
• It is strictly forbidden to change the dose of the drug or the drug itself;
• You cannot take the hormone for life;
• During hormone therapy, you need to regularly visit a gynecologist - once every six months.

Treatment of menopause with non-hormonal drugs

Experts today have differing opinions about the advisability of hormone therapy. In addition, many women refuse to take hormone-containing drugs because they are afraid of their side effects, do not have the financial ability to constantly buy them, or for other reasons.

In such cases, you can use treatment for menopause without hormones, which consists of the use of phytohormones, homeopathic medicines, dietary supplements, etc.

Homeopathic remedies for menopause

Homeopathy for menopause is very popular. The effect of homeopathic remedies is based on the activation of the body’s natural mechanisms. Patients are prescribed small doses of substances that, in large doses, can lead to negative consequences.

Homeopathic medicines will help eliminate symptoms of menopause such as:

• hyperhidrosis (increased sweating);
• menopausal vertigo (dizziness);
• hot flashes during menopause;
• dryness of the vaginal mucous membranes;
• mood swings;
• and others.

The benefits of homeopathy for menopause include the following:

• natural origin of components;
• relatively low cost;
• there are practically no side effects, only allergies to the components of the product;
• safety of use in the elderly.

Let's look at the most effective homeopathic remedies, used for menopause.

• Remens – 580 rubles. The drug consists of soybean phytohormones, which activate the synthesis of sex hormones at the level of the hypothalamus and pituitary gland. Remens effectively relieves a woman of hot flashes during menopause and prevents the appearance of vaginitis. In addition, with the help of Remens you can prevent urinary incontinence and cystitis during menopause.
• Estrovel - 385 rubles. This drug contains phytoestrogens from soy and wild yam, as well as a complex of vitamins and microelements. Estrovel allows you to reduce the number and intensity of hot flashes and sweating.
• Feminal – 670 rubles. This drug contains liquid extracts of nettle, oregano, celandine, hawthorn, shepherd's purse herb, centaury, St. John's wort, thyme, celandine and calendula. Feminal helps get rid of hot flashes, excessive sweating, psycho-emotional lability and dizziness during menopause, and women do not recover from this medicine.
• Climaxin – 120 rubles. This preparation consists of sepia, lachesis and black cohosh. The action of Climaxin is aimed mainly at regulating vegetative-vascular disorders (insomnia, irritability, palpitations, increased sweating, dizziness) during menopause.
• Klimakt-Hel – 400 rubles. This drug perfectly eliminates the symptoms caused by menopause.

Herbal remedies for menopause

Herbal preparations for menopause contain phytoestrogens - substances that can perform the function of female sex hormones and eliminate the symptoms of aging in the female body.

Plant estrogens are analogs of female sex hormones obtained from soy products. For example, the innovative Italian formula Flavia Night contains phytoestrogens - genistein and daidzein, which have a mild substitutive effect during menopause and menopause and help a woman cope with hot flashes, sweating and poor health.

Flavia Night also contains melatonin to normalize sleep, vitamin D and calcium to strengthen bone tissue, vitamins B6, B9 and B12 to normalize metabolism and alpha-linolenic acid for antioxidant protection.

Flavia Night is a unique Italian formula designed specifically for active women who want to lead a vibrant life rather than experience the symptoms of menopause. Just one capsule before bed will help a woman get through this difficult time. Flavia Night - works while you rest.

Another effective and popular drug for menopause symptoms is Inoclim, which is biological additive based on phytoestrogens.

Inoclim effectively fights such menopausal symptoms as a feeling of heat in the body, vaginal dryness, increased sweating, and also prevents the development of complications.

The drug has virtually no contraindications or side effects. Inoclim is not prescribed only to those who are allergic to the substances that make up its composition.

Thus, we have looked at what medications to take during menopause to alleviate its symptoms. But drug therapy can and should be supplemented with the correct and balanced diet, drinking enough fluids, playing sports, taking vitamins and mineral complexes. Also, do not forget about the positive emotions that communication with loved ones, hobbies or handicrafts can give you.

Watch a video about medications for menopause.

Having reached the age of forty, many women notice changes in their appearance and health. This happens because this period is dangerous due to a decrease in the level of female sex hormones, and this is reflected in general well-being. Hormono replacement therapy solves many problems - from eliminating depression to prolonging youth for many years. Having mastered the necessary information, women can easily survive menopause with its unpleasant symptoms without any threat to their health.

Benefits of hormone replacement therapy

Many women feel the need to take additional hormones, but not all resort to their help, fearing side effects. Gynecologists claim that modern hormonal drugs for women do not pose a threat, and fears are inspired by myths about the dangers of HRT. Doctors note many benefits of therapy with medications containing hormones. Through experiments it has been proven that cases of cardiac vascular diseases are less common in women taking modern hormonal medications than in those who do not accept such treatment.

During menopause

During menopause in women, estrogen levels for a long time remains extremely low, which has consequences that worsen the quality of life:

1. Depression becomes a frequent visitor during menopause.
2. Headaches often occur in women after 45 years of age.
3. Women complain of weakening memory with the onset of menopause.
4. The condition of the skin worsens: it becomes less elastic, unwanted wrinkles appear.
5. Increased sweating and a feeling of heat appear at the most inopportune moment.

The following positive effects are observed with hormone replacement therapy:

1. The risk of vascular diseases that can occur in women after forty is reduced. Estrogen protects blood vessels from cholesterol plaques; when its level decreases, problems with the cardiovascular system begin.
2. The risk of thrombosis is reduced.
3. The body receives protection from osteoporosis because the mineral density of bone tissue increases.
4. Modern hormone therapy can stabilize weight, the excess of which women suffer during menopause.

For breast cancer

With such a terrible disease, taking hormones is prerequisite for a speedy recovery and maintaining the woman’s health during this difficult period. This treatment is only relevant after surgical intervention, with amputation of the mammary gland. HRT has the following effects:

1. Reducing the risk of developing metastases, both to nearby organs and tissues and to distant ones.
2. Relief during menopause: complete or partial relief of symptoms.
3. Extending lifespan by decades.

After removal of the uterus and ovaries

Apoplexy (rupture of an ovarian cyst), fibroids, malignant tumors of the uterus and appendages can become the reason for a very important step - removal of these organs. After surgery, even young women experience all the unpleasant symptoms of menopause:

• irritability;
• depression;
• frequent headaches;
• lack of libido;
• vaginal dryness;
• hot flashes, feeling of heat, redness of the face and hands.

To prolong a woman’s youth and improve her quality of life, therapy with sex hormones is prescribed, which, after removal of the uterus and ovaries, are secreted by the adrenal glands, but in insufficient quantities. Some patients refuse such treatment, taking menopause for granted. By making choices in favor of proper nutrition, exercise and positive thoughts, a girl can live a long and happy life!

What examinations need to be completed before prescribing hormones?

The selection of hormonal therapy is individual and cannot be prescribed independently. To exclude contraindications, a number of examinations must be carried out before taking hormones. So, you need to write down in your plan:

1. Visit a gynecologist who will conduct a visual and palpation examination in a medical chair.
2. Take a smear from the cervix to examine the flora and exclude tumor markers.
3. Examination of blood in expanded form.
4. Blood test for hormones (reproductive, thyroid, and so-called sugar hormones).
5. Tests demonstrating the condition of the liver.
6. Ultrasound examination of the pelvic organs to exclude tumors.
7. Visiting a mammologist to diagnose the mammary glands.
8. Thyroid examination.

Forms of hormonal drugs

Modern medications for menopause are available in different forms:

1. Oral tablets are the most popular and frequently used among this type of medicine. It contains not only estrogens, but also gestagens.
2. External form: a gel or patch containing estrogen is prescribed to women who have undergone surgery to remove the ovaries and uterus, because. they are allowed to take this hormone in its pure form.
3. Form for local application in the form of creams or suppositories. This medicine for menopause is used if a woman has hypertrophy of the mucous membrane of the genitourinary system.
4. The hormonal implant is prescribed to women for whom estrogen is contraindicated. It is installed through simple surgery under the skin for 3 years, but can be easily removed if desired. This type of medicine contains progesterone, which can protect against unwanted pregnancy during menopause.

Hormone replacement therapy drugs after 40 years

Modern pharmacology provides a large selection of medications containing hormones for women after forty years. The most popular drugs for menopause, which have only good reviews from patients:

1. “Klimonorm” is available in the form of tablets containing estradiol (one of the types of female hormone estrogen), prescribed for the removal of internal genital organs: ovaries and uterus, to relieve symptoms during menopause. Contraindicated in diabetes mellitus, jaundice and peptic ulcer stomach. Apply once a day, 21 days. Then a seven-day break is taken and the new packaging. The tablets are designed for long-term use: from 5 to 10 years. This drug does not protect against pregnancy.
2. Trisequence is a pill consisting of estrogen and progesterone. Prescribed by gynecologists to relieve painful symptoms upon the onset of menopause in women after forty years. Contraindicated for internal bleeding and malignant tumors. The medication is taken once every 12 hours for 28 days, then a new package begins. Sometimes side effects occur in the form of vaginal itching, frequent headaches, and swelling of the legs. In such cases, you must stop taking the drug.
3. "Cliogest" is a drug for the prevention of osteoporosis, hot flashes, high blood pressure in women after forty. It is allowed to take for a long time if there are no side effects: migraine, hepatic colic, internal bleeding.
4. "Estrofem". Estrogen in this drug is represented by estradiol plant origin. Prescribed to relieve climatic symptoms and prevent cardiovascular diseases in women. Contraindicated in case of impaired renal function or peptic ulcer.
5. "Proginova" is prescribed to replenish the necessary female hormones. The estrogen contained in the tablets completely compensates for the lack of this component after removal of the appendages in women. Side effects may occur: skin allergies, itching all over the body. In case of such manifestations, this drug should be replaced with a more suitable one.
6. "Livial" - female hormones in tablets, which are prescribed for the prevention of osteoporosis and high blood pressure. The medicine relieves unpleasant symptoms during menopause. Doctors recommend taking the drug for no longer than five years, after which a six-month break is taken. Contraindicated during pregnancy.
7. Femoston is available in the form of tablets containing the hormone estradiol. Prescribed to increase bone density when a woman reaches menopause. This drug is also used to treat the prostate in men. Reduces the risk of heart attack in women during menopause. Long-term use of such hormones is dangerous due to unwanted sensations from the gastrointestinal tract. If a woman discovers side effects, she should consult a doctor.

Contraindications for use

Not all women will benefit from hormone replacement therapy; there are contraindications for use:

• malignant breast tumors;
• uterine bleeding;
• diabetes 2 types;
• jaundice.

Video about hormone replacement therapy for menopause

For clarity and a better understanding of the processes that occur in the female body, watch the video. A practicing obstetrician-gynecologist with many years of experience in a well-known clinic will talk about the role of estrogens for female beauty, the causes and signs of deficiency of sex hormones in the blood. Every woman will benefit from watching this video: the doctor will explain whether homeopathy is effective for menopause, what studies and tests should be done so that the prescription is correct and beneficial.

Attention! The information presented in the article is for informational purposes only. The materials in the article do not encourage self-treatment. Only a qualified doctor can make a diagnosis and make treatment recommendations based on individual characteristics specific patient.

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Discuss

Hormone replacement therapy

It does not require treatment, because this is a normal physiological process, not a pathology. But menopause is a difficult “stage” in the life of every woman, affecting absolutely all areas of a woman’s life. The lack of sex hormones affects health, psycho-emotional state, appearance and self-confidence, sex life, relationships with loved ones and even labor activity, on the quality of life in general. Therefore, any woman during this period requires help both from professional doctors and reliable support and support from her closest relatives.

How to alleviate the condition during menopause?

What can a woman do to ease menopause?

• Do not withdraw into yourself, accept the fact that menopause is not a vice or a shame, this is the norm for all women;
• lead a healthy lifestyle ;
• have a good rest;
• review your diet in favor of plant-based and low-calorie foods;
• move more;
• do not give in to negative emotions, receive positivity even from the smallest things;
• take care of your skin;
• follow all the rules intimate hygiene;
• consult a doctor promptly for preventive examination and if there are complaints;
• Follow your doctor’s orders and do not skip taking recommended medications.

What can doctors do?

• Monitor the condition of the body, identify and prevent the development of diseases associated with menopause;
• if necessary, prescribe treatment with sex hormones - hormone replacement therapy;
• Assess symptoms and recommend medications to relieve them.

What can family members do?

• Show patience with a woman’s emotional outbursts;
• do not leave alone with the problems that have piled up;
• the attention and care of loved ones works wonders;
• give positive emotions;
• support with words: “I understand”, “all this is temporary”, “you are so beautiful and attractive”, “we love you”, “we need you” and everything in that mood;
• lighten the household load;
• protect from stress and troubles;
• participate in trips to doctors and other manifestations of care and love.

Treatment of menopause - hormone replacement therapy (HRT)

Modern medicine believes that, despite physiology, menopause must be treated in many women. And the most effective and adequate treatment hormonal disorders is hormone replacement therapy. That is, the lack of one’s own sex hormones is compensated for with hormonal medications.

Hormone replacement therapy has already been successfully used on a large scale throughout the world. Thus, in European countries, more than half of women entering menopause receive it. And in our country only 1 in 50 women receives such treatment. And all this is not because our medicine is lagging behind in some way, but because of many prejudices that force women to refuse the proposed hormonal treatment. But many studies have proven that such therapy for menopause is not only effective, but also absolutely safe.
Factors on which the effectiveness and safety of hormonal drugs for the treatment of menopause depend:

• Timely administration and withdrawal of hormones;
• usually use small doses of hormones;
• correctly selected drugs and their doses, under the control of laboratory tests;
• the use of drugs containing natural sex hormones identical to those produced by the ovaries, and not their analogues, only similar in their chemical structure;
• adequate assessment of indications and contraindications;
• taking medications regularly.

Hormone therapy for menopause: pros and cons

Most people are unjustifiably wary of treatment with any hormones; everyone has their own arguments and fears about this. But for many diseases, hormonal treatment is the only way out. The basic principle is that if the body lacks something, it must be replenished by ingestion. So, with a deficiency of vitamins, microelements and other useful substances, a person consciously or even at the subconscious level tries to eat food with a high content of the missing substances, or takes dosage forms of vitamins and microelements. It’s the same with hormones: if the body does not produce its own hormones for any reason, they must be replenished with foreign hormones, because with any hormonal shift, more than one organ and process in the body suffers.

The most common prejudices regarding the treatment of menopause with female hormones:
1. "Menopause is normal, but its treatment is unnatural" , supposedly all our ancestors experienced it - and I will survive it. Until recently, the problems of menopause were a closed and “shameful” topic for women, almost like venereal diseases, so its treatment was out of the question. But women have always suffered during menopause. And we should not forget that women of those times were noticeably different from modern women. The previous generation aged much earlier, and most people took this fact for granted. Nowadays, all ladies strive to look as good and young as possible. Taking female hormones will not only ease the symptoms of menopause, but will also prolong youth both in appearance and in the internal state of the body.
2. "Hormonal drugs are unnatural." New trends against “synthetics”, for a healthy lifestyle and herbal preparations. So, hormonal drugs taken to treat menopause, although produced by synthesis, are natural, since their chemical structure is absolutely identical to estrogen and progesterone, which are produced by the ovaries of a young woman. At the same time, natural hormones that are extracted from plants and animal blood, although similar to human estrogen, are still poorly absorbed due to differences in structure.
3. “Hormonal treatment always means excess weight.” Menopause is often manifested by excess weight, so by correcting hormonal levels, weight gain can be avoided. To do this, it is important to take not only estrogens, but also progesterone in a balanced dose. In addition, many studies have proven that sex hormones do not increase the risk of obesity, but vice versa. While plant hormones (phytoestrogens) will not fight excess weight.
4. “After hormonal therapy, addiction develops.” Hormones are not drugs. Sooner or later, a decrease in sex hormones occurs in a woman’s body; she will still have to live without them. And hormonal therapy with sex hormones only slows down and facilitates the onset of menopause, but does not exclude it, that is, menopause will occur in any case.
5. “Hormones will cause hair to grow in unwanted places.” Facial hair grows in many women after menopause, and this is due to a lack of female sex hormones, so taking HRT will prevent and delay this process.
6. "Hormones kill the liver and stomach." Among the side effects of estrogen and progesterone drugs, there are indeed points regarding liver toxicity. But microdoses of hormones used for HRT usually do not affect liver function; problems can arise when taking drugs against the background of liver pathologies. You can bypass the toxic effect on the liver by replacing tablets with gels, ointments and other dosage forms applied to the skin. HRT has no irritating effect on the stomach.
7. “Hormonal replacement therapy with sex hormones increases the risk of cancer.” The deficiency of sex hormones itself increases the risk oncological diseases, as well as their excess. Properly selected doses of female sex hormones normalize hormonal levels, thereby reducing this risk. It is very important not to use estrogen-only therapy - progesterone neutralizes many of the negative effects of estrogen. It is also important to stop HRT in time; such therapy after 60 years is really dangerous for the uterus and mammary glands.
8. “If I tolerate menopause well, why do I need HRT?” A logical question, but the main goal of hormonal treatment of menopause is not so much the relief of hot flashes as the prevention of the development of diseases associated with menopause, such as osteoporosis, mental disorders, hypertension and atherosclerosis. It is these pathologies that are more undesirable and dangerous.

There are still some disadvantages to hormonal therapy for menopause. Incorrectly selected, namely high doses of estrogen drugs, can really do harm.

Possible side effects from taking high doses of estrogen:

• development of mastopathy and increased risk of breast cancer;
• painful menstruation and severe premenstrual syndrome, lack of ovulation;
• may contribute to the development of benign tumors of the uterus and appendages;
• fatigue and emotional instability;
• increased risk of developing cholelithiasis;
• uterine bleeding due to the development of uterine hyperplasia;
• increased risk of developing hemorrhagic strokes.

Other possible side effects HRT not associated with high doses of estrogen:

1. Intimate hygiene products for menopause are very important not only for eliminating dryness, but also for the daily prevention of various inflammatory processes of the vagina. There are also quite a lot of them on the shelves of stores and pharmacies. These are gels, panty liners, wipes. A woman in menopause should wash herself at least twice a day, as well as after sexual intercourse.

Basic requirements for intimate hygiene products:

• the product must contain lactic acid, which is normally found in vaginal mucus and determines the acid-base balance;
• should not contain alkalis and soap solutions;
• must include antibacterial and anti-inflammatory components;
• the gel for washing should not contain preservatives, dyes, or aggressive fragrances;
• the gel should not cause irritation or itching in a woman;
• Panty liners should not be colored or scented, should not consist of synthetic materials and should not injure the delicate intimate area.

2. Correct selection of underwear:

• it should be comfortable, not narrow;
• consist of natural fabrics;
• should not shed or stain the skin;
• must always be clean;
• It should be washed with laundry soap or fragrance-free powder, after which the laundry should be rinsed well.

3. Prevention sexually transmitted diseases : monogamy, use of condoms and chemical methods of contraception (Pharmatex, etc.).

Vitamins for menopause

During menopause, changes occur in many systems, organs and processes in a woman’s body. A lack of sex hormones always leads to a slowdown in metabolism. Vitamins and microelements are catalysts for many biochemical processes in the body of every person. That is, they speed up metabolic processes, also participate in the synthesis of their own sex hormones and increase defenses, alleviate the symptoms of menopause, hot flashes and improve the tolerance of hormonal therapy. Therefore, a woman after 30, and especially after 50 years, simply needs to replenish her reserves with useful substances.

Yes, many vitamins and microelements come to us with food, they are the most useful and are better absorbed. But in the menopause this is not enough, so it is necessary to obtain vitamins in other ways - these are medications and biologically active additives(dietary supplements).

In most cases, a woman is prescribed multivitamin complexes, which contain all groups of vitamins and essential microelements at once, and all this is balanced for the daily requirement. The choice of such drugs and biological active substances is very large, for every taste and budget, they can be in the form of capsules, tablets, syrups, solutions. Some of them designed specifically for women over 40 years of age:

• Hypotrilon;
• Doppel Hertz Active Menopause;
• Woman 40 Plus;
• Orthomol Femin;
• Qi-klim;
• Hypotrilon;
• Feminal;
• Estrovel;
• Klimadinon Uno and others.

Vitamins are constantly necessary for a woman during menopause, so they must be used regularly or in courses throughout the entire period of menopause.

What vitamins and microelements are most important during menopause?

1. Vitamin E (tocopherol) – vitamin of youth and beauty. Promotes the production of your own estrogens. It also improves the condition of skin, hair and nails. In addition to oral intake, vitamin E should be included in skin care products.
2. Vitamin A (retinol) – is also indispensable for any woman. It has many positive effects on the body:

• antioxidant effect, frees body tissues from harmful free radicals;
• simulates the ovaries and the production of their own estrogens;
• positive effect on the skin: prevents the development

Fatigue, aging skin, insomnia - this is not the whole bouquet of what a woman can feel during menopause.

“You have to endure this, it happens to everyone, you don’t die from it,” our mothers and grandmothers and, unfortunately, many gynecologists assure.

“If I hadn’t started taking hormones on time, I would have lost my youth,” Madonna boldly states in one interview.

Why are our compatriots so afraid of hormone replacement therapy (HRT) during menopause, and why are women abroad during menopause in mandatory turn to doctors for help so that they can prescribe a hormonal drug that will help them survive menopause?

We’ll talk about this on the women’s website “Beautiful and Successful”.

How does menopause occur?

After 40 years, the female body rises to a new level. The new “stage” is quite medical name– menopause (by the way, “menopause” is literally translated as “step”). This period is directly related to the process of production of sex hormones, or more precisely, with a decrease in the production of these hormones - estrogen and progesterone. Due to their lack, significant changes begin to occur in the female body.

The restructuring of the body for menopause begins at 40-45 years old and ends at 51-53 years old - the time of the last menstruation.

After this age, hormonal changes continue to occur in a woman’s body, and she constantly feels all the delights of menopause. Is it worth enduring the ebbs and flows, depression and headaches all these years if hormonal therapy can help? What should women do with?

Why does menopause have so many symptoms?

The functioning of the mammary glands, genital organs, brain, cardiovascular system, the condition of the skin and hair, the functioning of the liver, large intestine and genitourinary system depend on estrogen, the female sex hormone. The lack of this hormone, which occurs during menopause, immediately affects all systems in the body.

There are more than 30 symptoms that women experience due to menopause after 40 years.

The most common mistake of modern women is that they are accustomed to letting everything take its course, especially if the symptoms are not pronounced. Like, this will pass. But at this time, a woman just needs to undergo the first diagnosis in order to start helping her body in a timely manner.

Why are women afraid of HRT?

In our country there is a “widespread hormone phobia”. Doctors often prescribe hormones for early menopause or after surgery, but, having no experience in using these drugs during menopause, they refuse to use them. Many of our compatriots are afraid of hormones, believing that they:

1. Total chemistry;
2. Contrary to feminine nature and cause cancer;
3. They make you fat and masculine;
4. Affects the liver and stomach;
5. Cause addiction;

So it turns out that there is a mutual responsibility: doctors don’t prescribe – women endure. But why be afraid of what has been practiced abroad for several decades?

How does HRT work?

The work of the female body can be conditionally divided into 2 periods: the first, when it has enough hormones, and the second, when hormones cease to be produced and there is a deficiency. The second period is called menopause (menopause).

Hormone production stops when the ovaries stop producing eggs, or after the female organs are removed surgically. Lack of hormones manifests itself in different ways:

• Hot flashes in women during menopause indicate that she lacks estrogen.
• Weakness and malaise in women during menopause occur due to a lack of another hormone - progesterone.

Operating principle HRT drugs During menopause it is quite simple - the body is given a certain dose of hormones so that this deficiency is not felt. That is, the body receives what nature took from it. New generation drugs cope well with this. Only the drug must be prescribed in a timely manner after mandatory diagnosis.

When should you start taking hormones?

It is better to prescribe hormonal therapy as soon as a lack of estrogen begins, so you need to go for diagnosis at 40–45 years old - at the beginning of the premenopausal period.

It is also mandatory to prescribe HRT for early menopause - the drugs are selected strictly by the doctor after a preliminary examination, and for artificial menopause.

If 5 years have passed since menopause, then it is already too late to prescribe hormones - it is almost impossible to stop the aging process of the female body and help it.

Is it possible to do without hormonal drugs?

Let us remember that the main goal of hormonal therapy is to alleviate a woman’s condition during menopause. Therefore, you can not take hormones, but begin to fight each symptom of menopause separately: take medications for headaches, antidepressants, medications to improve the functioning of the gastrointestinal tract, antipyretics for hot flashes, for osteoporosis, medications for blood pressure, etc. Note that such therapy is also effective, but in comparison with hormonal it is:

• expensive
• troublesome
• not always effective
• psychologically difficult (“do I really need so much medication at this age to feel good?”)

Why take each drug separately if HRT has a complex effect on the cause and does not remove individual symptoms?

Prescribing new generation HRT drugs during menopause will help prevent many problems associated with a woman’s health: reduce the risk of diabetes and Alzheimer’s disease, obesity and skin aging.

Of course, you can go through menopause without HRT. There are alternative options for how to do without hormones during this period.

• First, you need to seriously think about healthy way life: stop smoking, eat a balanced diet, monitor your sleep and wakefulness, limit exposure to the sun.
• Secondly, you need to constantly use the services of modern cosmetology, including expensive skin tightening operations and rejuvenation sessions.
• Well, and, of course, we must not forget about homeopathic medicines and dietary supplements, which are so widely popular in the modern world.

New generation HRT drugs

HRT drugs for menopause have always caused controversy for and against. Let's dispel several myths about the unnaturalness and danger of HRT for women's health.

• HRT drugs have gone through a long journey of testing and research. We can consider ourselves lucky - only new generation drugs reach our shelves, which can only be produced by serious pharmacological companies.
• Hormone replacement drugs of the modern generation are completely natural - they have a composition of hormones identical to those produced by the female body.
• The dosage of hormones in the drug is minimal. There is no addiction to hormonal drugs. This is just a remedy that helps a woman survive hormonal changes. After discussing with your doctor, medications can be stopped at any time.
• During menopause, the body does not stop producing male hormones. Natural estrogens, which are included in the main composition of all HRT preparations, are female. It is their production that stops during menopause. Taking female hormones neutralizes the effect of male hormones: it will stop hair growth in unnecessary places, allow you to maintain female shapes and proportions, improve the condition of your skin, and prevent snoring.
• The hormones that make up HRT do not lead to obesity. On the contrary, they stop the production of estrogen in adipose tissue. It is not the use of HRT that leads to obesity during menopause, but the age-related prerequisites for this: it decreases physical activity, metabolism slows down.
• Many people are afraid to take HRT, believing that they have a bad effect on the gastrointestinal tract. Modern hormonal drugs do not affect the gastrointestinal tract in any way, and for those who are very afraid for their stomach, alternative forms of the drug have been released - patches, gels, ointments and suppositories, which are absorbed through the skin.
• HRT contains components that prevent cancer, rather than provoke it. The hormonal cause of cancer due to HRT use has not been proven.

A woman who takes hormonal medications during menopause must be observed by a doctor: monitor the condition of the endometrium and vaginal mucosa, mammary glands, hormone levels, etc.

The best HRT drugs

If yesterday doctors considered menopause to be a period in a woman’s life that needs to be overcome, today menopause is considered to be a period of lack of hormones that can be given to the body. A doctor should prescribe HRT after preliminary diagnosis, so the site will only introduce its readers to the list of modern drugs, but we will not recommend them for use. All new generation drugs have a low dosage, which allows you to select the optimal safe dose for each woman. It can be lowered or raised.

• We have received good reviews about the drugs “Femoston”, “Angelik”, “Atarax”, “Grandaxin”, “Sigetin”, etc.

Of course, there are many among us who consider themselves to be opponents of everything hormonal. Homeopathic and herbal remedies will come to the aid of such women, although they are less effective than modern HRT drugs.

Of course, menopause is natural process in our body. And it’s very good that modern women have the opportunity to choose products that help improve their quality of life during this period.

The scope of indications for their use is constantly expanding. To date modern medicine has a fairly wide selection good drugs for HRT, experience in the use of drugs for HRT, indicating a noticeable predominance of benefits over the risks of HRT, good diagnostic capabilities, which allows monitoring both positive and negative effects of treatment.

Although there is all the evidence indicating the positive effect of taking HRT on health, in general the risks and benefits of this therapy, according to many authors, can be considered comparable. In many cases, the benefits of long-term use of HRT will outweigh the risks; in others, possible risk outweigh the benefits. Therefore, the use of HRT must meet the needs and demands of a particular patient, be individual and permanent. When selecting a dose, it is necessary to take into account both the age and weight of the patient, as well as the characteristics of the medical history, as well as the relative risk and contraindications for use, which will ensure the best treatment result.

An integrated and differentiated approach to prescribing HRT, as well as knowledge about the features and properties of the components that make up most drugs, will avoid possible undesirable consequences and side effects and will lead to the successful achievement of intended goals.

It must be remembered that the use of HRT is not prolongation of life, but an improvement in its quality, which may decrease under the influence of the adverse consequences of estrogen deficiency. And a timely solution to the problems of menopause is a real path to good health and well-being, maintaining working capacity and improving the quality of life of an ever-increasing number of women entering this “autumn” period.

Various classes of estrogens are used to carry out hormone replacement therapy, which alleviates the problems of menopause and the difficulties of the transition period for most women.

• The first group includes native estrogens - estradiol, estrone and estriol.
• The second group includes conjugated estrogens, mainly sulfates - estrone, equilin and 17-beta-dihydroequilin, which are obtained from the urine of pregnant mares.

As is known, the most active estrogen is ethinyl estradiol, used in drugs for oral contraception. Its doses, which are necessary to relieve menopausal symptoms, are 5-10 mcg/day, orally. However, due to the narrow range of therapeutic doses, the high likelihood of developing side effects and not such a beneficial effect on metabolic processes as natural estrogens, it is not advisable to use this hormone for HRT purposes.

Currently, the following types of estrogens are most widely used for HRT:

1. ORAL DRUGS
   • Estradiol esters [show] .

     Estradiol esters include

     • Estradiol valerate
     • Estradiol benzoate.
     • Estriol succinate.
     • Estradiol hemihydrate.

     Estradiol valerate is an ester of the crystalline form of 17-beta-estradiol, which, when administered orally, is well absorbed from the gastrointestinal tract (GIT). For oral administration, the crystalline form of 17-beta-estradiol cannot be used, since in this case it is practically not absorbed into the gastrointestinal tract. Estradiol valerate is rapidly metabolized to 17-beta-estradiol, so it can be considered a natural estrogen precursor drug. Estradiol is not a metabolite or end product of estrogen metabolism, but is the main circulating estrogen in premenopausal women. Estradiol valerate therefore appears to be an ideal estrogen for oral hormone replacement therapy, given that its goal is to restore hormonal balance to pre-ovarian failure levels.

     Regardless of the form of estrogen used, its dosage should be sufficient to both relieve the most severe menopausal disorders and prevent chronic pathology. In particular, effective prevention osteoporosis involves taking 2 mg of estradiol valerate per day.

     Estradiol valerate has a positive effect on lipid metabolism, manifested by an increase in the level of high-density lipoproteins and a decrease in the level of low-density lipoproteins. Along with this, the drug does not have a pronounced effect on protein synthesis in the liver.

     Among the oral drugs for HRT doctors(especially in Europe), drugs containing estradiol valerate, a prodrug of endogenous 17-beta-estradiol, are most often prescribed. At a dose of 12 mg of estradiol, valerate for oral administration as monotherapy or in combination with gestagens has shown high effectiveness in the treatment of menopausal disorders (drugs Climodien, Klimen, Klimonorm, CycloProginova, Proginova, Divina, Divitren, Indivina).

     However, drugs containing micronized 17-beta-estradiol (Femoston 2/10, Femoston 1/5) are no less popular.

   • Conjugated estrogens [show] .

     The composition of conjugated equiestrogens obtained from the urine of pregnant mares includes a mixture of sodium sulfates and estrone sulfate (they make up about 50%). Most of the other components of the hormones or their metabolites are specific to horses - equilin sulfate - 25% and alphadihydroequilin sulfate - 15%. The remaining 15% is inactive estrogen sulfates. Equilin has high activity; it is deposited in adipose tissue and continues to act even after the drug is stopped.

     Horse urine estrogens and their synthesized analogues have a more dramatic effect on the synthesis of the substrate renin and hormone-binding globulins compared to estradiol valerate.

     No less significant factor is the biological half-life medicinal product. Estrogens in horse urine are not metabolized in the liver and other organs, whereas estradiol is rapidly metabolized with a half-life of 90 minutes. This explains the very slow elimination of equilin from the body, which is evidenced by the persistence of its elevated level in the blood serum, noted even three months after cessation of therapy.

   • Micronized forms of estradiol.
2. DRUGS FOR INTRAMUSCULAR ADMINISTRATION [show]

   For parenteral administration, there are preparations of estradiol for subcutaneous administration (the classic form is depot - the drug Gynodian Depot, which is administered once a month).

   • Estradiol valerate.
3. DRUGS FOR INTRAVAGINAL ADMINISTRATION
4. PREPARATIONS FOR TRANSDERMAL ADMINISTRATION [show]

   The most physiological way to create the required concentration of estrogen in the blood of women should be recognized as the transdermal route of administration of estradiol, for which preparations of skin patches and gel were developed. The Klimara patch is used once a week and ensures a constant level of estradiol in the blood. Divigel and Estrogel gel are used once a day. The pharmacokinetics of estradiol when administered transdermally differs from that which occurs after oral administration. This difference consists primarily of the elimination of extensive initial metabolism of estradiol in the liver and significantly less effect on the liver. When administered transdermally, estradiol is converted less into estrone, which, after oral administration of estradiol preparations, exceeds the level of the latter in the blood plasma. In addition, after oral administration of estrogens, they are largely subject to enterohepatic recirculation. As a result, when using a patch or gel, the estrone/estradiol ratio in the blood is close to normal and the effect of the primary passage of estradiol through the liver disappears, but the beneficial effect of the hormone on vasmotor symptoms and protection of bone tissue from osteoporosis remains. Transdermal estradiol, compared to oral estradiol, has approximately 2 times less effect on lipid metabolism in the liver; does not increase the level of sexsteroid-binding globulin in serum and the cholesterol content in bile.

   Gel for external use 1 g of gel contains: estradiol 1.0 mg, excipients q.s. up to 1.0 g DIVIGEL- this is a 0.1% alcohol-based gel, active substance which is estradiol hemihydrate. Divigel is packaged in aluminum foil sachets containing 0.5 mg or 1.0 mg estradiol, corresponding to 0.5 g or 1.0 g of gel. The package contains 28 sachets. Pharmacotherapeutic group Hormone replacement therapy. Pharmacodynamics The pharmacodynamics and clinical effectiveness of Divigel are similar to those of oral estrogens. Pharmacokinetics When the gel is applied to the skin, estradiol penetrates directly into circulatory system, which avoids the first stage of hepatic metabolism. For this reason, fluctuations in plasma estrogen concentrations when using Divigel are significantly less pronounced than when using oral estrogens. Transdermal application of estradiol at a dose of 1.5 mg (1.5 g of Divigel) creates a plasma concentration of approximately 340 pmol/l, which corresponds to the level of the early follicle stage in premenopausal women. During treatment with Divigel, the estradiol/estrone ratio remains at 0.7; whereas with oral estrogen it usually drops to less than 0.2. Metabolism and excretion of transdermal estradiol occurs in the same way as natural estrogens. Indications for use Divigel is prescribed for the treatment of menopausal syndrome associated with natural or artificial menopause that develops as a result of surgical intervention, as well as for the prevention of osteoporosis. Divigel should be used strictly as prescribed by your doctor. Contraindications Pregnancy and lactation. Severe thromboembolic disorders or acute thrombophlebitis. Uterine bleeding of unknown etiology. C-strogen-dependent cancer (breast, ovarian or uterine). Severe liver diseases, Dubin-Johnson syndrome, Rotor syndrome. Hypersensitivity to the constituent components of the drug. Directions for use and doses Divigel is intended for long-term or cyclic treatment. Doses are selected by the doctor taking into account the individual characteristics of the patients (from 0.5 to 1.5 g per day, which corresponds to 0.5-1.5 mg of estradiol per day, the dose can be adjusted in the future). Typically, treatment begins with the appointment of 1 mg of estradiol (1.0 g of gel) per day. For patients with an “intact” uterus, during treatment with Divigel it is recommended to prescribe a gestagen, for example, medroxyprogesterone acetate, norethisterone, norethisterone acetate or dydrogestron for 10-12 days in each cycle. In postmenopausal patients, the cycle duration can be increased to 3 months. A dose of Divigel is applied once a day to the skin of the lower part of the anterior abdominal wall, or alternately to the right or left buttocks. The application area is equal in size to 1-2 palms. Divigel should not be applied to the mammary glands, face, genital area, or to irritated areas of the skin. After applying the drug, you should wait a few minutes until the gel dries. Accidental contact of Divigel with the eyes should be avoided. You should wash your hands immediately after applying the gel. If the patient has forgotten to apply the gel, this should be done as soon as possible, but no later than within 12 hours from the date of application of the drug as scheduled. If more than 12 hours have passed, the application of Divigel should be postponed until the next time. If the drug is not used regularly, menstrual-like uterine “breakthrough” bleeding may occur. Before starting therapy with Divigel, you should undergo a thorough medical examination and during the treatment process, visit a gynecologist at least once a year. Patients suffering from endometriosis, endometrial hyperplasia, diseases of the cardiovascular system, as well as cerebrovascular disorders, arterial hypertension, a history of thromboembolism, disorders of lipid metabolism, renal failure, a history of breast cancer or a family history should be under special supervision. During treatment with estrogen, as well as during pregnancy, some diseases may worsen. These include: migraines and severe headaches, benign breast tumors, liver dysfunction, cholestasis, cholelithiasis, porphyria, uterine fibroids, diabetes mellitus, epilepsy, bronchial asthma, otosclerosis, multiple sclerosis. Such patients should be under medical supervision if they are treated with Divigel. Drug interactions There is no evidence of probable cross-interaction Divigel with other medications. Side effect Side effects are usually mild and very rarely lead to cessation of treatment. If they do occur, it is usually only in the first months of treatment. Sometimes observed: engorgement of the mammary glands, headaches, swelling, irregular menstruation. Overdose As a rule, estrogens are well tolerated even in very large doses. Possible signs of overdose are the symptoms listed in the “Side Effects” section. Their treatment is symptomatic. Shelf life: 3 years. The drug should not be used after the date indicated on the package. Store at room temperature out of the reach of children. The drug is registered in the Russian Federation. Literature 1. Hirvonen et al. Transdermal estradiol gel in the treatment of the climacterium: a comparison with oral therapy. Br J of Ob and Gyn 1997, Vol 104; Suppl. 16: 19-25. 2. Karjalainen et al. Metabolic changes induced by oral oestrogen and transdermatjfylktradiol gel therapy. Br J of Ob and Gyn 1997, Vol 104; Suppl. 16:38-43. 3. Hirvonen et al. Effects of transdermal oestrogen therapy in postmenopausal women: a comparative study of an oestradiol gel and an oestradiol delivering patch. Br J of Ob and Gyn 1997, Vol 104; Suppl. 16:26-31. 4. Marketing research 1995, Data on tile, Orion Pharma. 5. JArvinen et al. Steady-state pharmacokinetics of oestradiol gel in postmenopausal women: effects of application area and washing. Br J of Ob and Gyn 1997, Vol 104; Suppl. 16:14-18.

   

   • Estradiol.

Existing data on pharmacological properties ax different estrogens indicate the preference for using mainly drugs containing estradiol for HRT purposes.

For 2/3 of all women, the optimal doses of estrogen are 2 mg estradiol (orally) and 50 mcg estradiol (transdermal). However, in each case, during the process of HRT, women should be examined in a clinic to adjust these doses. In women over 65 years of age, there is a decrease in renal and especially hepatic clearance of hormones, which requires special caution in prescribing estrogens in high doses.

There is evidence that lower doses of estradiol (25 mcg/day) may be sufficient for the prevention of osteoporosis.

Currently, there is evidence indicating the presence of pronounced differences in the effects of conjugated and natural estrogen preparations on cardiovascular system and the hemostasis system. In the work of C.E. Bonduki et al. (1998) compared conjugated estrogens (0.625 mg/day orally, continuous regimen) and 17-beta-estradiol (transdermal 50 μg/day) in menopausal women. All women took medroxyprogesterone acetate (5 mg/day orally) monthly for 14 days. It was found that conjugated estrogens, unlike estradiol, cause a statistically significant decrease in antithrombin III in plasma 3, 6, 9 and 12 months after the start of therapy. However, both types of estrogens did not affect prothrombin time, factor V, fibrinogen, platelet count and euglobulin lysis time. Over 12 months, no thromboembolic complications occurred among study participants. According to these results, conjugated estrogens reduce antithrombin III levels, while HRT with 17-beta-estradiol does not affect this indicator. The level of antithrombin III is of key importance in the development of myocardial infarction and thromboembolism.

Antithrombin III deficiency can be congenital or acquired. The lack of ability of conjugated estrogens to have a protective effect in women with myocardial infarction may be due precisely to their effect on the content of antithrombin III in the blood. Therefore, natural estrogens are preferable to oral therapy with conjugated estrogens when prescribing HRT to patients with risk factors for thrombosis.

In this regard, it should be noted that the historically widespread use of conjugated estrogens in the United States until recent years cannot be considered as the best and recommended in all cases. These obvious facts might not have been discussed if statements in favor of the use of conjugated estrogen preparations had not appeared in the literature, based only on their widespread use in the United States and the existence of a sufficiently large number of studies on their properties. In addition, it is impossible to agree with the statements about the best properties among the gestagens included in various combinations of HRT, medroxyprogesterone acetate with regard to their effect on lipid metabolism. Existing data show that among the gestagens on the market, along with progesterone, there are both its derivatives - 20-alpha and 20-beta-dihydrosterone, 17-alpha-hydroxyprogesterone, and derivatives of 19-nortestosterone, the use of which allows you to obtain the desired effect .

Hydroxyprogesterone derivatives (C21-gestagens) are chlormadinone acetate, cyproterone acetate, medroxyprogesterone acetate, dydrogesterone, etc., and 19-nortestosterone derivatives are norethisterone acetate, norgestrel, levonorgestrel, norgestimate, dienogest, etc.

The choice of a drug from the group of combined estrogen-gestagen agents is determined by the period of age-related hormonal changes in a woman.

Specially designed to increase the effectiveness of hormone replacement therapy and prophylactic use, taking into account the requirements for maximum safety of the drug. This drug, characterized by an optimal ratio of hormones, not only has a positive effect on lipid profile, but also helps to quickly reduce menopausal symptoms. It has not only a preventive, but also a therapeutic effect on osteoporosis.

Klimonorm is highly effective for atrophic disorders of the genitourinary system and atrophic skin disorders, as well as for the treatment of psychosomatic disorders: irritability, depression, sleep disorders, forgetfulness. Klimonorm is well tolerated: more than 93% of all women taking Klimonorm note only positive changes in their well-being (Czekanоwski R. et al., 1995).

Klimonorm is a combination of estradiol valerate (2 mg) and levonorgestrel (0.15 mg), providing the following advantages of this drug:

• quick and effective reduction in the severity of menopausal symptoms;
• prevention and treatment of postmenopausal osteoporosis;
• maintaining the positive effect of estrogen on the atherogenic index;
• the antiatrophogenic properties of levonorgestrel have a positive effect on changes in the mucous membranes of the genitourinary system and weakness of the sphincters;
• While taking Klimonorm, the cycle was well controlled and no signs of endometrial hyperplasia were observed.

Klimonorm should be considered the drug of choice for HRT purposes during pre- and perimenopause in most women with osteoporosis, psychosomatic disorders, atrophic changes in the mucous membranes of the genitourinary system, hypercholesterolemia, hypertriglyceridemia, with high risk development of colon cancer, Alzheimer's disease.

The dose of levonorgestrel included in Klimonorm provides good cycle control, sufficient protection of the endometrium from the hyperplastic effect of estrogens and at the same time maintaining the beneficial effect of estrogens on lipid metabolism, the cardiovascular system, prevention and treatment of osteoporosis.

It has been shown that the use of Klimonorm in women from 40 to 74 years of age for 12 months leads to an increase in the density of cancellous and cortical bone tissue by 7 and 12%, respectively (Hempel, Wisser, 1994). The mineral density of the lumbar vertebrae in women aged 43 to 63 years when using Klimonorm for 12 and 24 months increases from 1.0 to 2.0 and 3.8 g/cm2, respectively. Treatment with Klimonorm for 1 year in premenopausal women with removed ovaries is accompanied by restoration of bone mineral density and markers of bone metabolism to normal levels. In this parameter, Klimonorm is superior to Femoston. The additional androgenic activity of levonorgestrel, apparently, is also very significant for the formation of a state of mental comfort. While Klimonorm eliminates or reduces symptoms of depression, Femoston increases symptoms of depressive mood in 510% of patients, which requires interruption of therapy.

An important advantage of levonorgestrel as a gestagen is its almost 100% bioavailability, which ensures the stability of its effects, the severity of which is practically independent of the woman’s diet, the presence of gastrointestinal diseases and activity hepatic system, metabolizing xenobiotics during their initial passage. Note that the bioavailability of dydrogesterone is only 28%, and its effects are therefore subject to marked differences, both interindividual and interindividual.

In addition, it should be noted that cyclic (with a seven-day break) use of Klimonorm provides excellent cycle control and a low frequency of intermenstrual bleeding. Femoston, used continuously, has less control over the cycle in this regard, which may be due to the lower progestogenic activity of dydrogesterone compared to levonorgestrel. If, when taking Klimonorm, the regularity of menstrual bleeding is observed in 92% of all cycles and the number of cases of intermenstrual bleeding is 0.6%, then when using Femoston these values ​​are 85 and 4.39.8%, respectively. At the same time, the nature and regularity of menstrual bleeding reflect the state of the endometrium and the risk of developing its hyperplasia. Therefore, the use of Klimonorm from the point of view of preventing possible hyperplastic changes in the endometrium is preferable to Femoston.

It should be noted that Klimonorm has pronounced activity in the treatment of menopausal syndrome. When analyzing its effect in 116 women over 6 months, a decrease in the Kupperm index was revealed from 28.38 to 5.47 (after 3 months it decreased to 11.6) with no effect on blood pressure and body weight (Czekanowski R. et al ., 1995).

At the same time, it should be noted that Klimonorm compares favorably with drugs containing other 19-nortestosterone derivatives (norethisterone) with more pronounced androgenic properties as a gestagen. Norethisterone acetate (1 mg) counteracts the beneficial effects of estrogens on HDL cholesterol concentrations and may also increase low-density lipoprotein levels, thereby increasing the risk of cardiovascular disease.

For women who need additional protection from hyperplastic processes in the endometrium, it is better to prescribe the drug Cyclo-Proginova, in which the activity of the gestagenic component (norgestrel) is 2 times higher than Klimonorm.

Combined estrogen-progestogen drug. The action is due to the estrogenic and gestagen components included in the drug. The estrogenic component - estradiol is a substance of natural origin and, after entering the body, quickly turns into estradiol, which is identical to the hormone produced by the ovaries and has its own effects: it activates the proliferation of organ epithelium reproductive system, including regeneration and growth of the endometrium in the first phase of the menstrual cycle, preparation of the endometrium for the action of progesterone, increased libido in the middle of the cycle, affects the metabolism of fats, proteins, carbohydrates and electrolytes, stimulates the liver's production of globulins that bind sex hormones, renin, TG and coagulation factors blood. Due to its participation in the implementation of positive and negative feedback in the hypothalamic-pituitary-ovarian system, estradiol is capable of causing moderately pronounced central effects. He plays important role in the development of bone tissue and the formation of bone structure.

The second component of the drug Cyclo-Proginova is an active synthetic gestagen - norgestrel, which is superior in potency to the natural hormone corpus luteum progesterone. Promotes the transition of the uterine mucosa from the proliferation stage to the secretory phase. Reduces excitability and contractility of the uterine muscles and fallopian tubes, stimulates the development of the end elements of the mammary glands. Blocks the secretion of hypothalamic factors releasing LH and FSH, inhibits the formation of gonadotropic hormones, inhibits ovulation, and has minor androgenic properties.

Climen is a combination drug containing natural estrogen estradiol (in the form of valerate) and a synthetic gestagen with an antiandrogenic effect, cyproterone (in the form of acetate). Estradiol, which is part of Clymene, replenishes estrogen deficiency that occurs during natural menopause and after surgical removal of the ovaries (surgical menopause), eliminates menopausal disorders, improves the blood lipid profile and ensures the prevention of osteoporosis. Cyproterone is a synthetic gestagen that protects the endometrium from hyperplasia, preventing the development of cancer of the uterine mucosa.

In addition, cyproterone is a strong antiandrogen, blocks testosterone receptors and prevents the effect of male sex hormones on target organs. Cyproterone enhances the beneficial effect of estradiol on the blood lipid profile. Thanks to its antiandrogenic effect, Klimen eliminates or reduces such manifestations of hyperandrogenism in women as excess facial hair growth ("lady's mustache"), acne (blackheads), and hair loss on the head.

Clymene prevents the formation of male-type obesity in women (accumulation of fat in the waist and abdomen) and the development of metabolic disorders. When taking Klimene during a 7-day break, a regular menstrual-like reaction is observed, and therefore the drug is recommended for premenopausal women.

It is a combined, modern, low-dose hormonal drug, the therapeutic effects of which are due to the constituent estradiol and dydrogesterone.

Currently, three varieties of the drug Femoston are produced - these are Femoston 1/10, Femoston 2/10 and Femoston 1/5 (Conti). All three varieties are available in a single dosage form - tablets for oral administration (28 tablets per package), and differ from each other only in the dosage of the active ingredients. The numbers in the name of the drug indicate the hormone content in mg: the first is the content of estradiol, the second is dydrogesterone.

All varieties of Femoston have the same therapeutic effect, and different dosages of active hormones allow you to choose the optimal drug for each woman that best suits her.

Indications for use for all three varieties of Femoston (1/10, 2/10 and 1/5) are the same:

1. Hormone replacement therapy for natural or artificial (surgical) menopause in women, manifested by hot flashes, sweating, palpitations, sleep disturbances, excitability, nervousness, vaginal dryness and other symptoms of estrogen deficiency. Femoston 1/10 and 2/10 can be started to be used six months after the last menstruation, and Femoston 1/5 - only a year later;
2. Prevention of osteoporosis and increased bone fragility in women during menopause with intolerance to other drugs intended to maintain normal bone mineralization, prevent calcium deficiency and treat this pathology.

Femoston is not indicated for the treatment of infertility, however, in practice, some gynecologists prescribe it to women experiencing problems conceiving to increase endometrial growth, which significantly increases the likelihood of implantation of a fertilized egg and pregnancy. In such situations, doctors use the pharmacological properties of the drug to achieve a certain effect in conditions that are not an indication for use. This practice of using drugs for other purposes is found all over the world and is called off-label prescriptions.

Femoston replenishes the deficiency of sex hormones in a woman’s body, thereby eliminating various disorders (vegetative, psycho-emotional) and sexual disorders, and also prevents the development of osteoporosis.

Estradiol, which is part of Femoston, is identical to the natural one normally produced by a woman’s ovaries. That is why it replenishes the deficiency of estrogen in the body and ensures smoothness, elasticity and slow aging of the skin, slows down hair loss, eliminates dry mucous membranes and discomfort during sexual intercourse, and also prevents atherosclerosis and osteoporosis. In addition, estradiol eliminates such manifestations of menopausal syndrome as hot flashes, sweating, sleep disturbances, excitability, dizziness, headaches, atrophy of the skin and mucous membranes, etc.

Dydrogesterone is a progesterone hormone that reduces the risk of developing endometrial hyperplasia or cancer. This progesterone hormone does not have any other effects, and is included in Femoston specifically to reduce the risk of endometrial hyperplasia and cancer, which increases due to estradiol intake.

During the postmenopausal period, medications intended for continuous use should be used. Of these, Climodien has additional advantages associated with good tolerability, since the dienogest included in its composition has moderate antiandrogenic activity and optimal pharmacokinetics.

Contains 2 mg estradiol valerate and 2 mg dienogest in one tablet. The first component is well known and described, the second is new and should be described in more detail. Dienogest combines the properties of modern 19-norprogestogens and progesterone derivatives in one molecule with almost 100% bioavailability. Dienogest - 17-alpha-cyanomethyl-17-beta-hydroxy-estra-4.9(10)diene-3-one (C 20 H 25 NO 2) - differs from other norethisterone derivatives in that it contains a 17-cyanomethyl group (-CH 2 CM) instead of the 17 (alpha)-ethynyl group. As a result, the size of the molecule, its hydrophobic properties and polarity changed, which, in turn, affected the absorption, distribution and metabolism of the compound and gave dienogest, as a hybrid gestagen, a unique range of effects.

The progestogenic activity of dienogest is especially high due to the presence of a double bond at position 9. Since dienogest has no affinity for plasma globulins, approximately 90% of its total amount is associated with albumin, and it is in a free state in fairly high concentrations.

Dienogest is metabolized through several pathways - mainly by hydroxylation, but also by hydrogenation, conjugation and aromatization into completely inactive metabolites. Unlike other nortestosterone derivatives that contain an ethynyl group, dienogest does not inhibit the activity of enzymes containing cytochrome P450. Due to this, dienogest does not affect the metabolic activity of the liver, which is its undoubted advantage.

The half-life of dienogest in the terminal phase is quite short compared to other progestogens, similar to that of norethisterone acetate and ranges between 6.5 and 12.0 hours. This makes it convenient to use daily in a single dose. However, unlike other progestogens, the accumulation of dienogest with daily oral administration is insignificant. Compared with other progestogens, when taken orally, dienogest has a high kidney/fecal excretion ratio (6.7:1). About 87% of the administered dose of dienogest is eliminated after 5 days (mainly in the urine in the first 24 hours).

As a result of the fact that mainly metabolites are found in the urine, and unchanged dienogest is detected in small quantities, a fairly high amount of unchanged substance remains in the blood plasma until elimination.

The lack of androgenic properties of dienogest makes it the drug of choice for use in combination with estrogens in a continuous regimen of hormone replacement therapy.

In studies using molecular models, it was shown that, unlike other 19-norprogestins, dienogest not only did not have androgenic activity, but became the first 19-norprogestogen, which has a certain antiandrogenic activity. Unlike most nortestosterone derivatives (eg, levonorgestrel and norethinodrone), dienogest does not compete with testosterone for binding to sex steroid binding globulin and therefore does not increase the free fraction of endogenous testosterone.

Because the estrogen component of hormone replacement therapy stimulates the synthesis of this globulin in the liver, a progestogen with partially androgenic activity may counteract this effect. In contrast to most nortestosterone derivatives, which reduce plasma globulin levels, dienogest does not affect the estrogen-induced increase in its level. Consequently, the use of Climodien leads to a decrease in serum free testosterone levels.

It has been shown that dienogest is also capable of altering the biosynthesis of endogenous steroids. In in vitro studies, it has been demonstrated to reduce the synthesis of ovarian steroids by inhibiting the activity of 3-beta-hydroxysteroid dehydrogenase. Moreover, like progesterone, dienogest has been found to locally reduce the conversion of testosterone to the more active form, dihydrotestosterone, by competitively inhibiting 5-alpha reductase in the skin.

Dienogest is well tolerated and has a low incidence of side effects. In contrast to the estrogen-dependent increase in renin levels during the control cycle, no increase in renin was observed with dienogest.

In addition, dienogest causes less platelet aggregation than medroxyprogesterone acetate and also has an antiproliferative effect on breast cancer cells.

Thus, dienogest is a strong oral progestogen that is ideal for combined use with estradiol valerate as part of the drug Climodien for hormone replacement therapy. Its chemical structure determines the combination of the positive properties of 19-norprogestins with those of C21 progestogens (Table 2).

Table 2. Pharmacokinetic and pharmacodynamic properties of dienogest

Properties and characteristics	19-Nor-progestogens	C21-Progesta- genes	Dieno-gest
High bioavailability when taken orally	+	+
Short half-life in plasma	+	+
Strong progestogenic effect on the endometrium	+	+
No toxic or genotoxic effects	+	+
Low antigonadotropic activity		+	+
Antiandrogenic activity		+	+
Antiproliferative effects		+	+
Relatively low skin penetration		+	+
With the exception of progesterone receptors, does not bind to any other steroid receptors			+
Does not bind to specific steroid-binding transport proteins			+
No adverse effects on the liver			+
A significant portion of the steroid is in the free state in plasma			+
In combination with estradiol valerate, weak accumulation when taken daily			+

Climodien effectively relieves the manifestations and symptoms of menopause associated with a decrease in hormone levels after menopause. When taking Climodien for 48 weeks, the Kupperm index decreased from 17.9 to 3.8, improved verbal and visual memory, and eliminated insomnia and sleep-disordered breathing. Compared with estradiol valerate monotherapy, the combination of estradiol valerate with dienogest had a more pronounced positive effect on atrophic changes in the genitourinary tract, manifested by vaginal dryness, dysuria, frequent urges to urination, etc.

Taking Climodien was accompanied by favorable changes in lipid metabolism, which, firstly, are useful for preventing atherosclerosis, and, secondly, contribute to the redistribution of fat according to the female type, making the figure more feminine.

Specific markers of bone metabolism (alkaline phosphatase, pyridinoline, deoxypyridinoline) when taking Climodien changed in a characteristic way, indicating inhibition of osteoclast activity and a pronounced suppression of bone resorption, which indicates a reduced risk of osteoporosis.

A description of the pharmacological properties of Climodien will be incomplete without noting its ability to increase in postmenopausal women the content of endogenous mediators that mediate vasodilation - cGMP, serotonin, prostacyclin, relaxin, which allows us to classify this drug as a drug with vasorelaxing activity that can improve blood circulation.

The use of Climodien leads to atrophic changes in the endometrium in 90.8% of women, and therefore prevents the development of endometrial hyperplasia. Bloody discharge, which is relatively common in the first months of therapy, decreases with increasing duration of treatment. The incidence of adverse effects and side effects is similar when treating postmenopausal women with other similar drugs. At the same time, no adverse effects were detected on chemical laboratory parameters, which is especially important, on hemostasis and carbohydrate metabolism.

Thus, we can conclude that for postmenopausal women, the drug of choice for a continuous combined regimen of hormone replacement therapy is Climodien, which, meeting all the necessary standards of effectiveness and tolerability, helps preserve femininity after menopause.

• provides quick and effective relief of menopausal symptoms;
• provides reliable “protection” of the endometrium and better controls breakthrough bleeding, compared to Cliogest, without reducing the beneficial effects of estrogens;
• contains a dienogest-progestogen component that does not bind to sex steroid-binding globulin, as a result of which the endogenous steroids testosterone and cortisol are not displaced from the sites of their binding to transport proteins;
• reduces testosterone levels in women;
• contains dienogest, which has a partial antiandrogenic effect;
• according to the study of bone metabolism indicators, it exhibits an inhibitory effect of estradiol on bone resorption. Dienogest does not counteract this effect of estradiol;
• according to the results of a study of endothelial markers during the treatment period, there is a vasodilating effect of estradiol and nitric oxide on the vascular network;
• does not have an adverse effect on the lipid profile;
• does not change blood pressure, coagulation factors or body weight;
• improves mood, cognitive function, eliminates insomnia and normalizes sleep in patients with sleep disorders, if they are associated with menopause.

Climodien is a highly effective, well-tolerated and easy-to-use combination drug for hormone replacement therapy, which is designed for long-term use. It stops all manifestations of menopausal syndrome and causes amenorrhea after 6 months from the start of use.

Climodien is indicated for a continuous combination regimen for the treatment of climacteric disorders in postmenopausal women. Additional advantages of Climodien include the antiandrogenic properties of the progestogen included in its composition - dienogest.

Of great interest today is the emergence of a new monophasic combination drug Pauzogest for the treatment of postmenopausal patients.

Pauzogest is the drug of choice for long-term treatment of women undergoing longer than a year postmenopausal and preferring HRT without periodic bleeding.

Pauzogest is a combination of estrogen and progesterone. One tablet of Pauzogest contains 2 mg of estradiol (2.07 mg as estradiol hemihydrate) and 1 mg of norethisterone acetate. The drug is available in packaging - 1 or 3 blisters of 28 tablets. The tablets are film-coated. Daily dose is 1 tablet and is taken daily continuously. The drug compensates for the lack of female sex hormones during the postmenopausal period. Pauzogest relieves vegetative-vascular, psycho-emotional and other climacteric estrogen-dependent symptoms during the postmenopausal period, prevents bone loss and osteoporosis. The combination of estrogen with progestogen helps protect the endometrium from hyperplasia and at the same time prevent unwanted bleeding. Active substances The drugs are well absorbed when taken orally and are actively metabolized in the intestinal mucosa and when passing through the liver.

Similar to endogenous estradiol, exogenous estradiol hemihydrate, which is part of Pauzogest, affects a number of processes in the reproductive system, the hypothalamic-pituitary system and other organs; it stimulates bone mineralization.

Taking estradiol hemihydrate once a day ensures a stable, constant concentration of the drug in the blood. It is excreted completely within 72 hours after entering the body, mainly with urine, in the form of metabolites and, partially, unchanged.

Research in recent years has shown that the role of the progestin component in HRT is not limited to protecting the endometrium. Progestins can weaken or enhance some of the effects of estradiol, for example, in relation to the cardiovascular and skeletal systems, and also have their own biological effects, in particular psychotropic effects. Side effects and tolerability of the drug for HRT are also largely determined by the gestagenic component. The properties of the gestagenic component in the composition of continuous combination therapy, since the duration of administration and the total dose of gestagen with this regimen are greater than with cyclic regimens.

Norethisterone acetate, which is part of Pauzogest, belongs to testosterone derivatives (C19-gestagens). In addition to the general property of derivatives of C21-gestagens and C19-gestagens to cause transformation of the endometrium, norethisterone acetate has various additional “characteristics” that determine their use in therapeutic practice. It has a pronounced anti-estrogenic effect, reducing the concentration of estrogen receptors in target organs and inhibiting the action of estrogens at the molecular level (“down-reg-ulation”). On the other hand, the moderate mineralocorticoid activity of norethisterone acetate can be successfully used in the treatment of menopausal syndrome in women with primary chronic adrenal insufficiency, and androgenic activity can be used both to achieve a positive anabolic effect and to compensate for androgen deficiency in menopause, leading to a decrease in sexual desire.

Row unwanted effects norethisterone acetate manifests itself during its passage through the liver and is most likely due to the presence of the same residual androgenic activity. Oral administration of norethisterone acetate interferes with estrogen-dependent synthesis of lipoprotein apoproteins in the liver and therefore reduces the beneficial effect of estradiol on the blood lipid profile, as well as worsens glucose tolerance and increases blood insulin levels.

Norethisterone acetate is well absorbed when taken orally. It is excreted mainly in the urine. With simultaneous administration of estradiol hemihydrate, the characteristics of norethisterone acetate do not change.

Thus, the drug Pauzogest has a positive effect on all symptoms of peri- and postmenopause. Clinical evidence suggests that Pauzogest reduces bone destruction and prevents bone loss in postmenopause, thereby reducing the risk of fractures caused by osteoporosis. Endometrial proliferation, which occurs under the influence of estrogen, is effectively inhibited by continuous use of norethisterone acetate. This minimizes the risk of developing endometrial hyperplasia and cancer. Most women who take Pausogest in monophasic mode do not experience uterine bleeding, which is preferable for postmenopausal patients. Long-term use of Pauzogest (less than 5 years) does not increase the risk of developing breast cancer. The drug is well tolerated. Side effects include engorgement of the mammary glands, mild nausea, and rarely - headache, peripheral edema.

Thus, the results of many clinical trials indicate that the arsenal of drugs for HRT in postmenopause has been replenished with another worthy drug, which is highly effective, safe, well tolerated, acceptable and easy to use.

Conclusion

When choosing a drug for HRT in women, you must consider:

• age and weight of patients
• features of the anamnesis
• relative risk and contraindications for use

Oral drugs	It is better to take for women with atrophic skin changes, hypercholesterolemia, it is possible to use smoking women and women at high risk of developing colon cancer.
Transdermal drugs	Preferably used in women with medical conditions gastrointestinal tract, gallbladder, diabetes, hypertriglyceridemia, and possibly in women after cholecystectomy.
Estrogen monotherapy	Indicated for women with a removed uterus and possibly elderly women suffering from vascular heart disease or Alzheimer's disease.
Combined estrogen-progestin therapy	Indicated for women with a non-removed uterus, as well as women with a removed uterus with a history of hypertriglyceridemia or endometriosis.

The choice of HRT regimen depends on the severity of the menopausal syndrome and its period.

• During perimenopause, it is preferable to use two-phase combination drugs in a cyclic mode.
• In postmenopause, it is advisable to constantly use a combination of estrogen and gestagen; Since at this age women, as a rule, have increased insulin resistance and hypercholesterolemia, it is better for them to use Climodien - the only drug for continuous use that contains a gestagen with antiandrogenic activity.