Hormone therapy for menopause: contraindications and side effects

At a certain period in a woman's life, the reproductive system fades away, when the ovaries stop producing hormones. Women's hormonal levels change, and these changes cause many inconveniences and problems: hot flashes, dryness and a burning sensation in the genitals, pain during intimacy, urinary incontinence, dry skin, wrinkles on the face, and the development of osteoporosis (a decrease in the calcium level in the bones, which makes the bones brittle). Hormone replacement therapy is designed to overcome discomfort during menopause. Hormone replacement therapy is also designed to soften the transition period during menopause, and reduce the manifestation of symptoms to a minimum. Drugs intended for replacement therapy should compensate for the lack of estrogens in the female body, and, in certain cases, the lack of progestogens.

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Release form

Hormones used for replacement therapy can be prescribed in the form of tablets, injections for intramuscular administration, skin hormonal medicinal patches, as well as subcutaneous medicinal implants, medicinal suppositories for invaginal use. The drugs and dosage are selected by the doctor individually for each woman, and depend on what symptoms she has, how long her period has been absent, as well as on what diseases she has suffered and the presence of surgical interventions in the anamnesis.

What medications are used to treat the problems that arise?

We will provide a list of the most popular and frequently used hormone replacement therapy drugs in medical practice.

• Tablets and dragees: Hormoplex, Premarin, Klimonorm, Femoston, Klimen, Proginova, Cyclo-proginova, Trisequence.
• Injections for intramuscular administration during menopause: Gynodiane-depot.
• Hormonal skin patches for menopause: Estraderm, Menorest, Klimara.
• External skin gels for menopause: Divigel, Estrogel
• Intrauterine device (IUD) for menopause: Mirena.
• Vaginal suppositories during menopause: Ovestin.
• Medicinal herbs and infusions: oregano, red clover, sage, hawthorn, peony, calendula, lemon balm and mint, St. John's wort, hop cones.

Next, we will consider in more detail how the best hormonal drugs work and how they are used during the climacteric period. First of all, we will analyze the drugs with estradiol used for manifestations of the pathological course of the perimenopausal period.

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Premarin

Indications: severe symptoms of climacteric syndrome, insufficient estrogen levels during menopause, development of osteoporosis in postmenopause, bleeding from the uterine cavity, menstrual irregularities, amenorrhea (absence of menstruation).

Release form of Premarin: tablet preparation of 0.625 mg.

Pharmacodynamics of the drug: supports the development and maintenance of the functioning of the reproductive (childbearing) female system. Helps to alleviate or completely eliminate the symptoms of climacteric syndrome (fluctuations in blood pressure, anxiety, depression, atrophy of the vaginal mucosa). Stops the development of osteoporosis in postmenopause. Helps to increase the level of lipoproteins (HDL), lowers low-density lipoproteins (LDL), prevents the development of pathologies and diseases of the cardiovascular system.

Pharmacokinetics of the drug: the ingredients of the drug have the property of dissolving well in water and are easily absorbed into the gastrointestinal tract, have the ability to penetrate into the tissues of the mucous membrane of the female genital organs, the mammary gland, into bone tissue, into the hypothalamus and pituitary gland, into the cytoplasm of the cell and its nucleus, and, being there, contribute to the synthesis of ribonucleic acid (RNA) and the production of proteins. The metabolism of the drug occurs in the liver tissue, then estrogens enter the intestine with bile, then are reabsorbed from the intestine into the blood, and again the substances return to the blood supply system of the abdominal organs. The ingredients of the drug, which have the property of dissolving in water, are ionized in the human body and will be excreted by the kidneys.

Use of Premarin during pregnancy: contraindicated for use at any stage of pregnancy.

Contraindications Premarin: Malignant and benign neoplasms of the mammary gland, uterine bleeding of unknown etiology, as well as disorders of the hemocoagulation function (blood clotting), thromboembolism, thrombophlebitis, in severe forms of damage and pathologies of the cardiovascular system, in severe disorders in the functioning of the kidneys, as well as the liver; various anemias, congenital hearing impairment, condition after immobilization for a long time.

Side effects of the drug Premarin: nausea, up to vomiting, severe headaches, weight gain, swelling, gynecological bleeding, pigment spots on the skin of the face, inflammation of the subcutaneous vessels (erythema), increased levels of liver enzymes, allergic rash, benign and malignant tumors of the inner layer of the uterus (endometrium).

Method of administration of Premarin and dosage of the drug: orally, the drug should be used in cycles - 625 mcg - 1.25 mg during the day, the duration of taking the drug is 3 weeks, a break is 1 week. In case of gynecological bleeding, the drug is prescribed on the 5th day of the menstrual cycle, gestagens are additionally prescribed, starting from the 15th day of the cycle and up to the 21st day. If necessary, the doctor increases the daily dosage to no more than 3.75 mg from the 5th - 7th day of the cycle, with a gradual decrease to 1.25 mg throughout the day.

Overdose: nausea and vomiting, prolonged bleeding from the uterine cavity.

Interaction of Premarin with a number of other medications: the effectiveness of Premarin can be reduced by barbiturates, anticonvulsants, Butadion, Rifampicin.

Storage conditions for Premarin: List B drug, store at a temperature of 15–25 C in a dark place.

The shelf life of this medicine is 60 months.

Hormoplex

Indications for the use of Gormoplex: for acute symptoms of the pathological course of the perimenopausal period, symptoms of the development of postmenopausal osteoporosis, lack of estrogens in the female body, cancerous formations of the prostate gland in men, neoplasms, tumors of the mammary glands in women.

Release form of Gormoplex: 1.25 mg dragee No. 20. One dragee contains 1.25 mg of bound estrogen in the form of sodium salt.

Pharmacodynamics: replenish the deficiency of estrogens in the body, bind to receptors of affected organs, increase the production of enzymes, as well as protein synthesis, participate in the regulation of fat metabolism, prevent the development of hormone-dependent neoplasms.

Pharmacokinetics: the components of the drug dissolve well in water, then are quickly absorbed into the gastrointestinal tract, have the property of penetrating into tissues and cells of target organs, are introduced into the cytoplasm of the cell and its nucleus, increasing the production of ribonucleic acid and protein production. The metabolism of the drug, as a rule, occurs in the liver tissues, then estrogens enter the intestine with bile, after which they are reabsorbed in the intestine and again return to the blood supply system of the abdominal organs. The ingredients of the drug, which have the property of dissolving in water, are ionized in the human body and will be excreted by the kidneys.

Contraindications: malignant estrogen-dependent tumors in the organs and tissues of the genitourinary system and mammary gland, thromboembolic disease, liver failure, with endometrial proliferation (endometriosis), benign tumors of the uterus.

Side effects: nausea, vomiting, depression, headaches (like migraines), swelling of the mammary glands, bleeding from the uterine cavity, liver dysfunction, various types of jaundice, increased body weight, allergic rashes on the skin, increases the possibility of developing cancerous tumors of the uterus and mammary glands.

Method of administration and dosage: orally. Individual dosage selection.

For symptoms of severe menopause and development of climacteric osteoporosis, the therapeutic average daily dose is 1.25 mg for 20 days, or for 29 days with a one-week break; it is possible to increase the dosage to 2.5-3.75 mg during the day, but not longer than 7 days.

Pathological bleeding from the uterine cavity - 2.5-7.5 mg per day 2-3 times a day for 2-5 days; the doctor may increase the therapeutic dose and continue therapy after the bleeding has stopped.

If menstruation is absent for a long period of time - 1.25-3.75 mg per day for 20 days; in case of climacteric syndrome with a regular cycle, amenorrhea, or, on the contrary, in case of bleeding from the uterine cavity, it is combined with a gestagenic agent for 15 to 21 days of the menstrual cycle.

For cancer - 3.75-7.5 mg throughout the day.

Overdose of the drug Gormoplex: severe nausea, repeated vomiting, bleeding from the uterine cavity.

Interaction of Gormoplex with other drugs: reduces the effect of anticholinesterase drugs, anticoagulants, antidepressants, drugs aimed at treating diabetes. The drug Rifampicin, barbiturate derivatives, the drug Butadion enhance the effect of estrogen metabolism.

Storage conditions for Gormoplex: store in a place inaccessible to children.

Shelf life: 5 years.

Klimonorm

Indications: used in hormone replacement therapy for women with severe symptoms of menopause, suffering from dryness and atrophy of the mucous membrane of the genitals, osteoporosis, etc.

The drug Klimonorm is available in the form of 21 dragees in a package (9 yellow and 12 turquoise dragees).

Pharmacodynamics: estradiol valeriate contained in the drug Klimonorm is transformed into natural free estradiol in the human body. Levonorgestrel, which is part of this drug, compensates for the lack of progesterone and prevents the proliferation of the inner layer of the uterus (endometrium) into neoplasms of various etiologies. If the patient's uterus has not been removed, then, thanks to the components of the drug, the menstrual cycle is restored in women. Estradiol increases the level of estrogen in the body of women after menopause, and contributes to the effective treatment of perimenopausal pathology: hot flashes, hyperhidrosis, psychoemotional disorders, pain in the heart, atrophy of the mucous membrane of the genitals, urinary incontinence, muscle and joint pain. Estradiol prevents a decrease in bone mass concentration and with constant and controlled use of HRT, the risk of bone fractures is reduced. The components of Klimonorm lead to a decrease in cholesterol levels, create an optimal balance of low-density lipoproteins and high-density lipoproteins in the body.

The drug helps to increase the content of elastic substance - collagen in the skin, which slows down the development of deep wrinkles on the skin of the face.

Pharmacokinetics: estradiol valerate and levonorgestrel have the property of being well absorbed in the gastrointestinal tract. Estradiol valerate enters into metabolism and forms natural estradiol and estrone, which further participate in metabolic processes. Estradiol valerate is excreted from the body in the form of metabolic products with urine and bile. Levonorgestrel is also excreted with urine and bile in the form of bile acids.

Use during pregnancy: the drug is contraindicated during various periods of pregnancy and during lactation.

Contraindications: individual intolerance to the components of the drug, liver dysfunction, congenital pathologies of lipid metabolism, thromboembolism, condition during myocardial infarction, strokes, hormone-dependent neoplasms in the uterus and mammary glands, as well as suspicion of them, endometriosis and intrauterine bleeding, severe diabetes mellitus in severe forms of manifestation, pregnancy at different stages, breastfeeding period.

Side effects: rare. May include nausea, repeated vomiting, vaginal bleeding, skin hyperpigmentation, breast tenderness, decreased libido.

Method of administration of Klimonorm and dosage: this drug is taken orally, recommended at a certain time of day, if treatment is interrupted, vaginal bleeding may occur.

If there is a regular menstrual cycle, the drug is prescribed on the 5th day of the menstrual cycle. In case of symptoms of dysmenorrhea, amenorrhea and during postmenopause, this drug is prescribed regardless of the day of the cycle, excluding pregnancy.

During the seven-day break in taking the medicinal product Klimonorm, the drug should be taken from a new package. The 1st pill from the new package should be taken on the same day of the week when the 1st tablet from the previous package was taken.

Overdose of Klimonorm: severe or mild nausea, single or multiple vomiting, gynecological bleeding. Symptomatic treatment is prescribed for overdose.

Interaction of Klimonorm with other drugs: when prescribing hormone replacement therapy, it is necessary to stop using hormonal contraceptives. The effectiveness of the components of the drug is reduced when treating with antibiotics, when prescribing anticonvulsants, when using Rifampicin, barbiturates, Griseofulvin. The level of estradiol decreases when taking Tetracycline and Penicillin. For patients with diabetes mellitus - control the dosage of insulin. Alcoholic beverages increase the level of estradiol in the body.

Storage conditions for the medicinal product: list B. Storage at a temperature not exceeding 25C.

Shelf life: 60 months.

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Gynodiane Depot

Indications: climacteric syndrome, as well as symptoms of estrogen deficiency in the body in women (removal or irradiation of the ovaries), depression, hot flashes, hyperhidrosis, involuntary urination, atrophy of the mucous membrane of the genitourinary system, sleep disorders. Prevents the development of osteoporosis in perimenopause.

Release form: oil solution for intramuscular injections. 1 ml of solution contains 4 estradiol valerate, as well as prasterone enanthate 200 mg.

Pharmacodynamics: estradiol is involved in the regulation of metabolic processes of proteins, fats and carbohydrates, water-salt balance; causes proliferation of the endometrium. Prasterone enanthate is involved in the regulation of gonadotropin production, which regulates sexual desire (libido), the intensity of the creation of new cells, affecting the functioning of the glands - sebaceous and sweat. Both ingredients of the drug are involved in the regulation, generation and functional activity of bone tissue. This drug is designed to replenish the body's insufficient amount of female sex hormones during perimenopause and in the state after removal of the ovaries. Suppresses the development of perimenopausal pathology. Prevents bone dystrophy and prevents the development of osteoporosis.

Contraindications: pregnancy at any stage, liver tumors, thromboembolism, hormone-dependent tumors of the uterus, ovaries and mammary glands, congenital pathologies of lipid metabolism, otospongiosis.

Use of the drug during pregnancy: contraindicated at any stage of pregnancy.

Side effects: are rare. Increased libido, breast engorgement, increased body weight, uterine bleeding, increased production of male hormones in women may be observed.

Method of administration and dosage: intramuscularly, 1 ml every 4-6 weeks.

When interacting with other drugs: during the period of use of this drug, it is necessary to adjust the doses of insulin or other antidiabetic drugs.

Storage conditions for this product: the drug should be stored in a cool, dark place, out of the reach of children.

Shelf life: no more than 5 years. Do not use after the expiration date.

Estraderm - hormonal patch for menopause

Indications: absence of menstruation for a long period of time, infantilism of female genital organs and lack of full development of secondary sexual characteristics, signs of climacteric disorders, condition after surgical removal of the ovaries, infertility, insufficient labor force.

Release form: patch, with a contact surface of 5, 10 and 20 square centimeters and 20, 50 and 100 mcg of estradiol per day. The package contains 6 patches.

Contraindications: malignant tumors of the mammary glands, the inner and muscular layer of the uterus, pathological proliferation of the endometrium, bleeding from the uterine cavity of unknown origin, severe liver dysfunction, thromboembolism, pregnancy at any stage. It is prescribed with caution in case of heart failure, hypertension, liver and kidney dysfunction, epilepsy.

Use during pregnancy: contraindicated.

Side effects: breast tenderness, gynecological bleeding, endometrial cancer, local application – skin hyperemia and itching.

Method of application: the Estraderm patch is applied to a clean, dry, undamaged area of skin on the lower back or abdomen. The Estraderm external application system is applied twice a week, the dosage is adjusted depending on the therapeutic effect of the drug. After 6 applications, a 7-day break is required. After removal of the uterus, the drug is administered continuously. Before prescribing the drug, a thorough medical examination is required. A combination of the drug with gastagens is recommended.

Interaction with other drugs: increases the effect of drugs that reduce lipid concentration. Weakens the effect of male sex hormones, sugar-lowering drugs, diuretics, as well as blood pressure-lowering drugs, anticoagulants. Anesthetics, analgesics (narcotic), tranquilizers, barbiturates, antiepileptic drugs accelerate metabolic processes involving estradiol. Phenylbutazone, Rifampicin, antibiotic Ampicillin reduce estradiol levels. Vitamin B9 (folic acid) and thyroid hormone preparations increase the effect of estradiol.

Storage conditions: Store the drug from List B in a dark place.

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Divigel - hormonal gel for menopause

Indications: ovarian failure (estrogen deficiency), symptoms of pathological perimenopause, both natural (fading of female ovarian function) and artificial (due to removal of patients' ovaries). Prevention of bone tissue dystrophy in the postmenopausal period.

Release form: 0.1% gel for topical application. In 1g sachets. There are 28 sachets in a pack.

Pharmacodynamics: the active component is synthesized estradiol. Promotes the effeminaton of the female body, has a beneficial effect on the rejection of the inner layer of the uterus and regular menstrual bleeding. Stimulates blood clotting. Increases the content of copper, iron, and thyroxine hormone in the blood.

Pharmacokinetics: When rubbing the gel into the skin, most of it quickly enters the bloodstream, the rest is absorbed into the blood later. It enters the liver, where the active substance is broken down into components. It is excreted with bile into the intestine, where it is again absorbed into the bloodstream.

Contraindications: patients with hypersensitivity to the ingredients of the gel, patients with cancerous tumors of various organs, blockage of blood vessels, dysfunction of the liver, kidneys, acute and chronic diseases of the cardiovascular system, strokes, edema of various tissues and organs, epilepsy, bronchial asthma, bleeding, including gynecological.

Contraindicated for use during pregnancy and breastfeeding.

Observed side effects: high blood pressure, headaches, nausea, risk of blood clots, accelerated tumor growth, gynecological bleeding, enlargement of the mammary glands and body weight, allergic skin rashes.

Method of application: the dosage and day of the cycle are selected by the doctor individually for each patient, as a rule, they start with 1 g per day. It is possible to increase the dosage according to indications, as well as additionally prescribe gestagenic drugs. The gel is applied to clean skin, an area of 1-2 palms. Let it dry for 2-3 minutes, do not wash off for an hour. The areas to which the gel is applied are alternated. For example: one day apply to the buttocks, the next - to the abdomen, then to the shoulder area.

In drug interactions, it is an antagonist of male sex hormones, glucose-lowering agents, diuretics and blood pressure lowering agents, and blood clotting agents. Metabolic processes with estradiol are accelerated by taking barbiturates, tranquilizers, antiepileptics, and general anesthetics. The level of estradiol in the blood can be reduced by antibiotics and antiviral agents. Estradiol enhances its action under the influence of vitamin B9 (folic acid) and thyroid hormones.

Store the drug in places inaccessible to children, at a temperature of no more than 25C.

The shelf life of the drug is limited to 36 months.

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Mirena - hormonal intrauterine device for menopause

Indications for the use of this medicine may be: as a local therapeutic agent in hormonal replacement therapy for symptoms of pathological perimenopause, as a contraceptive, for the prevention of pathological proliferation of the inner layer of the uterus, for heavy menstruation.

The release form of this product: a therapeutic intrauterine system (IUD) consists of a medicinal (hormonal) core and a special membrane that doses the flow of the medicinal product into the body. One system contains levonorgestrel in the amount of 52 mg.

Pharmacodynamics of the IUD: the progestogen has a local therapeutic effect in the uterine cavity. The concentration and thickness of mucus in the cervix increases, which prevents sperm from entering the uterine cavity and has a contraceptive (birth control) effect. In some cases, the development of the egg is suppressed. During replacement therapy, it prevents heavy bleeding and inhibits the growth of the mucous membrane of the inner layer of the uterus.

The pharmacodynamics of the drug is due to the local use of this agent, levonorgestrel is absorbed into the endometrial mucosa, and the concentration in the blood is very small. Due to the low concentration in the blood plasma, the therapeutic effect of the drug is minimal. The coil is designed for 5 years. Levonorgestrel is actively involved in the metabolic process and is excreted from the body through the kidneys and intestines with urine and feces.

The drug is contraindicated in the following cases: individual intolerance to the ingredients of the drug, pregnancy at any stage, infectious diseases of the reproductive system, tumors, inflammatory processes of the inner layer of the uterus, metrorrhagia of unknown etiology, pathologies of the structure of the uterus.

The following side effects of the drug are observed: dysmenorrhea, changes in menstrual discharge, ovarian cysts, allergic skin rashes, severe migraine-type headaches, increased blood pressure.

When using hemoproteins that participate in metabolic processes when using antibiotics and anticonvulsants, the metabolic properties of gestagens are enhanced.

It is recommended to store the drug in a dry, cool place protected from light, where children cannot access the drug.

Do not use after 36 months from the date of manufacture of the medicinal product.

Ovestin - hormonal suppositories for menopause

The use of the drug is indicated for: dystrophy of the vaginal mucosa associated with estrogen deficiency in the body, as a result of which patients complain of dryness and pain in the vagina, especially during sexual intercourse, frequent and painful urination, urinary incontinence, for the treatment of the cervix in infertility.

Release form: vaginal suppositories (candles). 1 suppository contains 500 micrograms of micronized estriol.

Pharmacodynamics of the drug: the components of the drug interact with the cells of the inner layer. Replenishes the lack of estrogens in the female body and relieves the symptoms of perimenopausal syndrome. It has a beneficial effect on the epithelium and microflora of the vagina, eliminating discomfort and dryness in the vagina, relieves painful urination and reduces its frequency.

Pharmacokinetics: estriol is absorbed in the vagina and enters the bloodstream. In blood plasma, it forms a bond with albumin. Estriol is metabolized in the liver. It is excreted from the body with feces and urine.

The use of the drug is contraindicated in the following cases: intolerance to the components of the drug, tumors of various organs, proliferation of the inner layer of the uterus, vaginal bleeding, vascular occlusions, liver damage, heart attacks, diabetes mellitus, epilepsy.

Side effects that are possible when using this drug: swelling and soreness of the mammary glands, itching in the vagina, sometimes nausea, headaches, hypertension.

Use of the drug is contraindicated during pregnancy.

Application and dosage: vaginal suppositories are used 1 suppository per day for 1 month. Then the dosage can be reduced to 2 suppositories per week.

Interactions with other drugs have not been established during clinical studies.

Store the drug at a temperature not exceeding 30C. The storage place for the drug should be inaccessible to children.

Stop using the drug if its expiration date exceeds 36 months from the date of manufacture.