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Hormonal therapy with menopause: contraindications and side effects
Last reviewed: 23.04.2024
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At a certain period in the life of women, the reproductive system disappears when the ovaries stop producing hormones. Women change the hormonal background and these changes bring a lot of inconveniences and problems: tides, dryness and burning sensation in the genitals, pain during intimate proximity, urinary incontinence, dry skin, wrinkles on the face, development of osteoporosis (decrease in calcium in Bones, because of what the bones become brittle). Overcome discomfort during menopause is called hormone replacement therapy. Also, hormone replacement therapy is designed to alleviate the transition period during menopause, to reduce the manifestation of symptoms to a minimum. Drugs intended for substitution therapy should compensate for the lack of estrogen in the female body, as well as, in certain cases, the lack of progestogens.
[Release form
Hormones used for substitution therapy can be prescribed in the form of tablets, injections for intramuscular injection, cutaneous hormonal medicinal patches, as well as subcutaneous medicinal implants, medicinal suppositories of invaginal application. Preparations and dosage are selected by the doctor individually for each woman, and depend on which of the symptoms she has manifested, how long menstruation is absent, and also on what diseases have been transferred and from the presence of surgical interventions in the anamnesis.
What medications are used in case of problems?
We will provide a list of the most popular and often used in medical practice hormone replacement therapy.
- Tablets and pills: Hormoplex, Premarin, Klimonorm, Femoston, Klimen, Proginova, Cyclo-proginova, Triksevensom.
- Injections for intramuscular injection with menopause: Gynodian Depot.
- Skin hormonal patches with menopause: Estraderm, Menorest, Klimara.
- External dermal gels with menopause: Divigel, Estrogel
- Intrauterine spiral (IUD) with menopause: Mirena.
- Vaginal suppository in menopause: Ovestin.
- Medicinal herbs and dues: oregano, red clover, sage, hawthorn, peony, calendula, lemon balm and mint, St. John's wort, cones of hops.
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 medicines with estradiol, used for the manifestations of the pathological course of the perimenopausal period.
Premarin
Indications: severe symptoms of climacteric syndrome, insufficient levels of estrogen during menopause, postmenopausal osteoporosis, bleeding from the uterine cavity, malfunctions of the menstrual cycle, amenorrhea (no monthly).
The form of the release of Premarin: a tablet preparation of 0.625 mg.
Pharmacodynamics of the drug: supports the development, as well as the safety of the functioning of the reproductive (genital) female system. They help to alleviate or completely eliminate symptoms in menopausal syndrome (blood pressure changes, anxiety, depressive state, atrophy of the vaginal mucosa). They stop the development of osteoporosis in postmenopausal women. They help to increase the level of lipoproteins (HDL), lower low density lipoproteins (LDL), prevent the development of pathologies and diseases of the cardiovascular system.
Pharmacokinetics of the drug: the ingredients of the drug have a good dissolving ability in water and are easily absorbed into the gastrointestinal tract, have the ability to penetrate into the mucous membrane of the genital female organs, the breast, bone tissue, the hypothalamus and the pituitary, into the cytoplasm of the cell and its nucleus , and, while there, contribute to the synthesis of ribonucleic acid (RNA) and the production of proteins. Metabolism of the drug occurs in the liver tissues, then the estrogens enter the intestine with bile, then they are re-absorbed from the intestine into the blood, and again the substances return to the blood supply system of the abdominal organs. 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 the drug Premarin during pregnancy: it is contraindicated to apply at any time of pregnancy.
Contraindications Premarin: Malignant and benign neoplasms of the breast, bleeding of the uterus of undefined etiology, as well as violations of the function of hemocoagulation (coagulation), thromboembolism, thrombophlebitis, with severe forms of lesions and pathologies of the cardiovascular system, with severe violations in kidney function, and so the same liver; various anemia, congenital hearing loss, condition after immobilization for a long time.
Side effects of the drug Premarin: a feeling of nausea, up to vomiting, severe headaches, weight gain, the appearance of swelling, gynecological bleedings, the appearance of pigment spots on the skin of the face, inflammation of the subcutaneous vessels (cutaneous erythema), increased levels of hepatic enzymes, an allergic rash, benign, as well as malignant tumors of the inner layer of the uterus (endometrium).
The way of using Premarin and the dosage of the drug: oral, the drug should be administered in cycles of 625 μg-1.25 mg during the day, the duration of the drug intake is 3 weeks, the break is 1 week. With gynecological bleeding the appointment of the drug occurs on the 5th day of the menstrual cycle, additionally prescribed gestagens, starting from the 15th day of the cycle and 21 days in advance. If necessary, the doctor increases the daily dosage no more than 3.75 mg from 5 to 7 days of the cycle, with a gradual decrease to a level of 1.25 mg throughout the day.
Overdose: nausea and vomiting, prolonged bleeding from the uterine cavity.
Interaction of Premarin with a number of other medicinal preparations: the effectiveness of Premarin may reduce barbiturates, anticonvulsants, Butadion, Rifampicin.
Storage conditions Premarin: the preparation of list B, stored at a temperature of 15-25 C in a dark place.
Shelf life of this medicine: 60 months.
Hormoplex
Indications for use of the Hormoplex: with acute symptoms of the pathological course of the perimenopausal period, symptoms of postmenopausal osteoporosis, lack of estrogen in the female body, cancer of the prostate gland of men, neoplasms, breast tumors in women.
The form of the release of the Hormoplex: dragees is 1.25 mg No. 20. In one pellet contains bound estrogen-shaped sodium salt of 1.25 mg.
Pharmacodynamics: fill the deficiency in the body of estrogens, bind to the receptors of the affected organs, increase the production of enzymes, as well as protein synthesis, participate in regulation regulate fat metabolism, inhibit the development of hormone-dependent neoplasms.
Pharmacokinetics: the components of the drug dissolve well in water, then quickly absorbed into the gastrointestinal tract, have the property of penetrating into the 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 usually occurs in the liver tissues, then the estrogens enter the intestines with bile, then they are absorbed back into the intestine and returned to the blood supply system of the abdominal organs. 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 organs and tissues of the genitourinary system and breast, thromboembolic disease, hepatic insufficiency, with the growth of the endometrium (endometriosis), benign uterine tumors.
Side effects: nausea, vomiting, depressive conditions, headaches (as migraine), swelling of the mammary glands, bleeding from the uterine cavity, liver dysfunction, various jaundices, increased body weight, allergic skin rashes, increases the possibility of cancer of the uterus and breast glands.
Dosage and administration: orally. Individual selection of dosage.
With symptoms of severe climacteric and climacteric osteoporosis, the therapeutic average daily dose is 1.25 mg for 20 days, or for 29 days with a break of one week; it is possible to increase the dosage of 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; it is possible that the doctor will increase the therapeutic dose and continue the therapy after the bleeding ends.
If menstruation is absent for a long period of time-1,25-3,75 mg during the day for 20 days; with climacteric syndrome with a regular cycle, amenorrhea, or, on the contrary, with bleeding from the uterine cavity is combined with a gestagenic remedy on the extent of 15 to 21 days of the menocycle.
With cancer - 3.75-7.5 mg throughout the day.
Overdose with preperatom Hormoplex: severe nausea, multiple vomiting, discharge of blood from the uterine cavity.
Interaction of the hormone with other drugs: reduce the effect of anticholinesterase drugs, anticoagulants, antidepressants, drugs directed to treat diabetes. The drug Rifampicin, derivatives of barbiturate, drug Butadion strengthen the effect of the exchange of estrogenic substances.
Storage conditions of the Hormoplex: store in a place that will be inaccessible to children.
Shelf life: 5 years.
Climonorm
Indication: used for hormone replacement therapy in women with severe symptoms of menopause, suffering from dryness and atrophy of the mucous of the genital organs, osteoporosis, etc.
The form of release of a medicinal product Climonorm: dragees in a package of 21 pieces (9 dragees of yellow and 12 turquoise).
Pharmacodynamics: estadiol valeriate, contained in the drug Klimonorm, in the human body is transformed into a natural free estradiol. Levonorgestrel, part of this medication, compensates for the lack of progesterone and prevents the growth of the inner layer of the uterus (endometrium) into tumors of various etologies. If the uterus has not been removed from the patients, then, due 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 the onset of menopause, and contributes to the effective treatment of perimenopausal pathology: hot flashes, hyperhidrosis, psychoemotional disorders, heart pain, mucosal atrophy, urinary incontinence, muscle and joint pain. Estradiol prevents the reduction of bone mass concentration and with the constant and controlled use of HRT reduces the risk of bone fractures. Components of the drug Climonorm lead to a decrease in the level of cholesterol, create an optimal balance of lipoprotein content of low, as well as high-density lipoproteins in the body.
The drug helps to increase the content of collagen in the skin, which slows the development of deep wrinkles on the skin of the face.
Pharmacokinetics: estradiol valerate and levonorgestrel have a property to be well absorbed into the gastrointestinal tract. Estradiol valerate is metabolized and forms a natural estradiol and estrone, which continue to participate in metabolic processes. Estradiol valerate is excreted from the body in the form of metabolic products with urine and bile. Levonorgestrel is excreted in the same way with urine and bile in the form of bile acids.
Application in pregnancy: during various periods of pregnancy and during lactation, the drug is contraindicated.
Contraindications: individual intolerance of drug components, liver dysfunction, congenital abnormalities of fat metabolism, thromboembolism, condition with 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 times, the period of breastfeeding.
Manifestations of side effects: are rare. There may be nausea, multiple vomiting, vaginal bleeding, hyperpigmentation of the skin, breast engorgement, decreased libido.
Method of application of the Clinonorm and dose: take this drug (orally) inside, it is recommended at certain times of the day, with the interruption of treatment, the occurrence of vaginal bleeding.
In the presence of a menstrual regular cycle, the drug is prescribed on day 5 of the menocycle. With symptoms of dysmenorrhea, amenorrhea and during postmenopause, the appointment of this remedy takes place regardless of the day of the cycle, excluding pregnancy.
During the seven-day break in taking the drug Climonorm, the drug should be taken with a new package. 1-d dragee from the new packaging to take on the same day of the week, when the first pill from the previous package was taken.
Overdose of the drug Climonorm: strong or slight nausea, single or multiple vomiting, gynecological bleeding. Treatment is prescribed in case of an overdose symptomatic.
Interaction of the Clinmon with other medicinal preparations: when hormone replacement therapy is prescribed, it is necessary to stop the use of hormonal contraceptives. The effectiveness of the components of the drug in the treatment of antibiotics, with the appointment of anticonvulsants, with the use of Rifampicin, barbiturates, Griseofulvin. The level of estradiol decreases with the admission of tetracycline and penicillin. Patients with diabetes mellitus - insulin dosage control. Alcoholic drinks increase the level of estradiol in the body.
Conditions for storage of the medicinal product: list B. Storage at a temperature not exceeding 25 ° C.
Shelf life: 60 months.
Gynodian depot
Indication: climacteric syndrome, as well as symptoms with insufficient estrogen in the body in women (removal or irradiation of the ovaries), depression, hot flushes, hyperhidrosis, involuntary discharge of urine, mucosal atrophy of the genitourinary system, sleep disturbance. Prevents the development of osteoporosis in the perimenopause.
Form release: oily solution for intramuscular injection. In 1 ml of the 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 the growth of the endometrium. Prasterone enanthate takes part in the regulation of the development of gonadotropin regulating sexual desire (libido), the intensity of the creation of new cells that affect the functioning of glandular 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 inadequate amount of female sex hormones in the perimenopause and in the condition after removal of the ovaries. Suppresses the development of the pathology of the perimenopausal period. It hinders the dystrophy of bone tissue and prevents the development of osteoporosis.
Contraindications: pregnancy at any time, neoplasms in the liver, thromboembolism, hormone-dependent formations of the uterus, ovaries and mammary glands, congenital pathologies of lipid metabolism, otosposgio.
Use of the drug during pregnancy: contraindicated at any time of pregnancy.
Side effects: are rare. There may be increased libido, breast engorgement, increased body weight, bleeding from the uterine cavity, increased production of male hormones in women.
Dosing and Administration: intramuscularly 1 ml every 4-6 weeks.
When interacting with other drugs: during the period of application of this drug, adjustments of doses of insulin or other antidiabetic drugs are necessary.
Conditions of storage of this product: the drug should be stored in a cool, protected from the rays of light, a place inaccessible to children.
Shelf life: not more than 5 years. Do not use after the expiration date.
Estraderm - hormonal patch with menopause
Indication: the absence of a long period of menstruation, infantile sexual organs of the sexes and the lack of full development of secondary sexual characteristics, symptoms of menopausal disorders, the condition after surgical removal of the ovaries, infertility, inadequate generic forces.
Form release: plaster, with a contact surface of 5,10 and 20 square centimeters and 20, 50 and 100 μg of estradiol per day. The package contains 6 patches.
Contraindications: malignant tumors of the mammary glands, inner and muscular layers of the uterus, pathological proliferation of the endometrium, bleeding from the uterine cavity of unknown origin, severe liver dysfunction, thromboembolism, pregnancy at any time. With caution is prescribed for heart failure, hypertension, with liver and kidney dysfunction, with epilepsy.
Use during pregnancy: contraindicated.
Side effects: tension of the mammary glands, gynecological bleeding, endometrial cancer, topically when applied - skin hyperemia and itching.
Method of application: Estraderm plaster is applied to the skin area, cleaned, dried, undamaged, on the lower back or on the abdomen. The external application system Estraderm is applied twice a week, the dosage is adjusted, depending on the therapeutic effect of the drug. After 6 overlaps, you need to take a break for 7 days. After removal of the uterus, the drug is administered continuously. Before the appointment of a medicinal product, a thorough medical examination is necessary. It is recommended that the drug be combined with gastagens.
Interaction with other drugs: increases the effect of drugs that reduce the concentration of lipids. Weaken the effect of male sex hormones, drugs that reduce the level of sugar, diuretics, as well as funds that reduce blood pressure, anticoagulant drugs. Anesthetics, analgesics (narcotic), tranquilizers, barbiturates, antiepileptic drugs accelerate metabolic processes involving estradiol. Phenylbutazone, Rifampicin, antibiotic Ampicillin reduce the level of estradiol. Vitamin B9 (folic acid) and drugs of thyroid hormones - increase the effect of estradiol.
Storage conditions: Store List B. Store in a dark place.
Divigel - hormonal gel with menopause
Indications: insufficiency of ovarian function (estrogen insufficiency), symptoms of pathological perimenopause, both natural (extinction of the function of female ovaries), and artificial (due to removal of ovaries in patients). Prophylaxis of bone tissue dystrophy in the postmenopausal period.
Product: 0.1% gel for cutaneous application. In bags of 1g. In the pack of 28 packets.
Pharmacodynamics: active ingredient-synthesized estradiol. Promotes the effemination of the female body, has a beneficial effect on the rejection of the inner layer of the uterus and regular menstrual bleeding. Stimulate blood clotting. Increases the content in the blood of copper, iron, hormone thyroxine.
Pharmacokinetics: During the rubbing of the gel into the skin, most of it quickly enters the circulatory system, the rest is absorbed into the blood later. It enters the liver where the active substance decomposes into components. It is excreted with bile into the intestine, where the absorption occurs again in the circulatory system.
Contraindications: patients with hypersensitivity to gel ingredients, patients with cancer tumors of various organs, blood vessel blockage, liver, kidney, acute and chronic diseases of the cardiovascular system, strokes, edema of various tissues and organs, epilepsy, bronchial asthma , with bleeding, including gynecological.
During pregnancy and breast-feeding, it is contraindicated.
The observed side effects: high blood pressure, headaches, nausea, the threat of blood clots, accelerated growth of tumors, gynecological bleeding, enlargement of mammary glands and body weight, rashes on the skin of an allergic nature.
Usage: the dosage and the day of the cycle are selected by the doctor individually for each patient, as a rule, begin with 1g per day. It is possible to increase the dosage according to the indications, and additionally the administration of gestagenic preparations. The gel is applied to clean skin, with an area of 1-2 palms. Let dry for 2-3 minutes, do not rinse for an hour. Sites to which the gel is applied alternate. For example: one day to put on the buttocks, the other - on the abdomen, then on the shoulder area.
In drug interactions, it is an antagonist of male sex hormones, glucose lowering agents, diuretics and blood pressure lowering drugs that reduce blood clotting. Exchange processes with estradiol are accelerated by taking barbiturates, tranquilizers, antiepileptic drugs, and for general anesthesia. The level of estradiol in the blood can lower antibiotics and antiviral agents. Estradiol intensifies its action under the influence of vitamin B9 (folic acid) and thyroid hormones.
Storage of the drug in places inaccessible to children, with a temperature regime of not more than 25C.
Shelf life of the drug is limited to 36 months.
Mirena - hormonal intrauterine device with climax
Indications for the use of this medicine can be: as a local therapeutic agent for hormonal replacement therapy with symptoms of the pathological perimenopause, as a contraceptive, for the prevention of pathological proliferation of the inner layer of the uterus, with profuse menstruation.
The form of release of this drug: therapeutic intrauterine system (spiral) consists of a drug (hormonal) core and a special membrane that doses the intake of the drug into the body. In the same system - levonorgestrel in the amount of 52 mg.
Farmakodimanika IUS: progestagen has a local therapeutic effect in the uterine cavity. Increases the concentration and density of mucus in the cervix, which prevents the penetration of sperm into the uterine cavity and has a contraceptive (contraceptive) effect. In some cases, the development of the egg is suppressed. When substitution therapy prevents excessive bleeding and depresses the growth of the mucosa of the inner layer of the uterus.
Pharmacodynamics of the drug is due to the local application of this drug, levonorgestrel is absorbed into the endometrial mucosa, and the concentration in the blood is very small. In connection with a small concentration in the blood plasma - is the minimum therapeutic effect of the drug. The spiral is designed for 5 years. Levonorgestrel actively participates in the process of metabolism 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 time, infectious diseases of the genital system, tumors, inflammatory processes of the inner layer of the uterus, metrorrhagia of unclear etiology, pathology of the uterine structure.
The following side effects of the drug are observed: dysmenorrhea, changes in discharge during menstruation, ovarian cysts, allergic skin rashes, severe migraine headaches, and increased blood pressure.
When using hemoproteins, which are involved in metabolic processes using antibiotics and anticonvulsants, the metabolic properties of gestagens are enhanced.
Storage of the drug is recommended in a dry, protected from light cool place where there is no access of children to the drug.
Do not use after 36 months from the date of release.
Ovestin - hormonal suppository with menopause
The use of the drug is indicated for: dystrophy of the vaginal mucosa associated with insufficient estrogen 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 cervical infertility.
The form of release: suppositories (suppositories) vaginal. 1 suppository contains 5o micrograms of estriol micronised.
Pharmacodynamics of the drug: the components of the drug interact with the cells of the inner layer. Replenishes the lack of estrogen in the female body and relieves the symptoms of perimenopausal syndrome. Favorably affects the epithelium and the microflora of the vagina, eliminating discomfort and dryness in the vagina, relieves the soreness of urination and reduces their frequency.
Pharmacokinetics: Estriol is absorbed into the vagina and enters the circulatory system. In the blood plasma forms a bond with albumin. Metabolism of estriol occurs in the liver. It is excreted from the body with feces and urine.
The drug is contraindicated for: intolerance to the components of the drug, tumors of various organs, proliferation of the inner layer of the uterus, vaginal bleeding, blockage of blood vessels, liver damage, heart attacks, diabetes, epilepsy.
Side effects that are possible with this drug: swelling and tenderness of the mammary glands, itching in the vagina, sometimes - nausea, headaches, hypertension.
Use of the drug is contraindicated in pregnancy.
Usage and dosage: vaginal suppositories are used for 1 suppository per day for 1 month. Then it is possible to reduce the dosage to 2 suppositories per week.
Interactions with other drugs have not been established in clinical trials.
Store the drug at a temperature of not more than 30C. The place of storage of the drug should be inaccessible to children.
Stop the use of the drug, the expiration date of which exceeds 36 months from the date of release.
Attention!
To simplify the perception of information, this instruction for use of the drug "Hormonal therapy with menopause: contraindications and side effects" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.