What is the hormone drospirenone responsible for? The hormone drospirenone in various medications. Contraindications for the use of combined oral contraceptives

Preparations based on drospirenone (drospirenone) in combination with estradiol are used in hormone replacement therapy, as a contraceptive and in the treatment of androgen-dependent conditions (hirsutism, seborrhea, acne, seborrhea). Drospirenone is the main active ingredient with antiandrogenic activity, which is prescribed by gynecologists for hirsutism. Trade names of drugs containing drospirenone: Yarina/ Yarina, Jess/ Yaz, Simicia / Symicia, Dailla / Dailla, Midiana / Midiana, Dimia / Dimia, Leia, Anabella, Vidora (drospirenone + ethinyl estradiol), Angelique/ Angeliq (drospirenone + estradiol hemihydrate).

Drospirenone is a 17α-spirolactone derivative with progestogenic, antimineralocorticoid and antiandrogenic activity, presumably does not have estrogenic, androgenic, glucocorticosteroid and antiglucocorticosteroid activity, does not affect glucose tolerance and insulin resistance, which, in combination with antimineralocorticoid and antiandrogenic action, provides drospirenone with biochemical and macological profile, similar to natural progesterone.

Antiandrogenic activity is due to two mechanisms: on the one hand, the drug reduces the secretion of testosterone in the adrenal glands and ovaries due to its antigonadotropic effect, and on the other, it competes with androgens for space on their receptors. At the same time, drospirenone does not interfere with the process of converting free testosterone into dehydrotestosterone and does not in any way affect the activity of the 5α-reductase enzyme.

Like cyproterone, drospirenone-based drugs should not be taken in case of adrenal insufficiency due to antimineralocorticoid activity. However, unlike cyproterone, drospirinone has a diuretic effect: by increasing the excretion of sodium and water, the drug can prevent an increase in blood pressure, body weight, swelling, tenderness of the mammary glands and other symptoms associated with fluid retention.

The effectiveness of Yarina in the treatment of hirsutism was observed for a year in 52 young women (25±6 years). The results were assessed once every 3-6-12 months using hormonal blood tests (LH, FSH, androstenedione, testosterone, estradiol, SHBG, DHEA-S; blood sampling on days 3-6 from the onset of bleeding). Results in the picture:

We see that on the Ferriman-Galloway scale, women on average have become half as hairy. The hormonal profile shows a significant increase in SHBG (sex hormone binding globulin) and an associated decrease in free testosterone. The remaining hormones remained virtually unchanged. The authors conclude that the use of drugs based on drospirenone is promising in the treatment of hirsutism, since in addition to reducing free testosterone, the drug helps eliminate excess fluid and does not have a negative effect on metabolism, which is especially important for. However, the authors warn about the risks of thromboembolism associated with taking drospirenone.

In another study of 15 women with PCOS, hormonal changes in the blood showed much more significant changes after starting to take Yarina tablets. We see that in addition to an increase in sex hormone binding globulin (SHBG), cortisol increases significantly, 17-OH-progesterone (17OHP) and dehydroepiandrosterone sulfate (DHEAS) decrease, estradiol and androstenedione (A) decrease. Glucose tolerance tests revealed no changes, but a trend toward increases in cholesterol, triglycerides, and high- and low-density lipoproteins.

A blind experiment over 12 months involving 91 women showed that drugs based on drospirinone and cyproterone are similar in effectiveness. The study authors, however, believe that due to their diuretic effect (and therefore blood pressure reduction), drospirinone-containing contraceptives are preferable. Below is a chart of the decline in hairiness scores on the Ferriman-Galloway scale in different areas of the body:


Like other hormone replacement drugs with progestogenic activity, taking drospirenone increases the risk of developing venous thromboembolism. Controlled randomized trials show that hormone replacement therapy increases the risks of the following diseases: endometrial hyperplasia or carcinoma, benign and malignant tumors liver, cholelithiasis, stroke, pancreatitis, jaundice, uterine bleeding, etc. Contraceptives are not used in the presence of any benign or malignant tumors. Full list For contraindications, see

Included in the preparations

ATX:

G.03.F.A.17 Drospirenone and estrogen

Pharmacodynamics:

Combined drug for continuous replacement hormone therapy, allowing you to avoid regular withdrawal bleeding that is observed with cyclic or phase hormone replacement therapy.

Contains 17β-estradiol, which is identical in chemical structure and biological properties to endogenous human estradiol, and a spironolactone derivative - drospirenone, which has a gestagenic, antigonadotropic and antiandrogenic, as well as antimineralocorticoid effect.

Estradiol compensates for estrogen deficiency in female body after the onset of menopause and provides effective treatment of psycho-emotional and vegetative menopausal symptoms (hot flashes, increased sweating, sleep disturbance, increased nervous excitability, irritability, palpitations, cardialgia, dizziness, headache, decreased libido, muscle and joint pain), involution of the skin and mucous membranes, especially the mucous membranes of the genitourinary system (urinary incontinence, dryness and irritation of the vaginal mucosa, pain during sexual intercourse).

Estradiol prevents bone loss caused by estrogen deficiency. This is mainly due to the suppression of osteoclast function and a shift in the process of bone remodeling towards bone formation. Long-term use of hormone replacement therapy has been shown to reduce the risk of peripheral bone fractures in women after menopause. When hormone replacement therapy is discontinued, the rate of bone mass decline is comparable to that characteristic of the period immediately after menopause.

Hormone replacement therapy also has a beneficial effect on the collagen content of the skin, as well as its density, and can also slow down the formation of wrinkles.

In addition, due to the antiandrogenic properties of drospirenone, it has a therapeutic effect on androgen-dependent diseases such as acne, seborrhea, and androgenetic alopecia.

Drospirenone has antimineralocorticoid activity, increases the excretion of sodium and water, which can prevent increases in blood pressure, body weight, swelling, breast tenderness and other symptoms associated with fluid retention. After 12 weeks of using the drug, a slight decrease in blood pressure is observed (systolic - on average by 2-4 mm Hg, diastolic - by 1-3 mm Hg). The effect on blood pressure is more pronounced in women with borderline arterial hypertension. After 12 months of using the drug, the average body weight remains unchanged or decreases by 1.1-1.2 kg.

Drospirenone does not have androgenic, estrogenic, glucocorticoid and antiglucocorticoid activity, does not affect glucose tolerance and insulin resistance. This, combined with its antimineralocorticoid and antiandrogenic effects, gives drospirenone a biochemical and pharmacological profile similar to natural progesterone.

Taking the drug leads to a decrease in the level of total cholesterol and cholesterol low density lipoproteins. Drospirenone attenuates the increase in triglyceride concentrations caused by estradiol.

The addition of drospirenone prevents the development of endometrial hyperplasia and cancer.

Observational studies suggest that postmenopausal women use hormone replacement therapy to reduce the incidence of colon cancer.

Pharmacokinetics:

Estradiol

Suction. After taking the drug orally, it is quickly and completely absorbed from the gastrointestinal tract. Subjects to a “first pass” effect with the formation of estrone, estriol and estrone sulfate. Bioavailability when taken orally is about 5% and is independent of food intake. Cmax of estradiol in serum is approximately 22 pg/ml and is achieved after 6-8 hours. Food intake does not affect the bioavailability of estradiol.

Distribution. Binds to albumin and sex steroid binding globulin. The free fraction of estradiol in serum is approximately 1-12%, and that bound to sex steroid binding globulin is 40-45%. The apparent Vd after a single intravenous injection is about 1 l/kg.

After repeated use, the concentration of estradiol is approximately 2 times higher than after a single dose, while C ss varies from 20 pg/ml to 43 pg/ml. After discontinuation of use, levels of estradiol and estrone return to baseline values ​​within approximately 5 days.

Metabolism. metabolized predominantly in the liver, partially in the intestines, kidneys, skeletal muscles and in target organs with the formation of estrone, estriol, catechol estrogens, as well as sulfate and glucuronide conjugates of these compounds, which have significantly less estrogenic activity compared to estradiol or are generally inactive.

Removal. Serum clearance of estradiol is about 30 ml/min/kg. Estradiol metabolites are excreted in urine and bile. The half-life is approximately 24 hours.

Drospirenone

Suction. After oral administration, drospirenone is quickly and completely absorbed from the gastrointestinal tract. Bioavailability is 76-85% and does not depend on food intake. Food intake does not affect the bioavailability of drospirenone.

Distribution. After a single or multiple dose of 2 mg, Cmax in serum is reached after 1 hour and is about 22 ng/ml. After this, a biphasic decrease in the concentration of drospirenone in the serum is observed with a final half-life of about 35-39 hours. Drospirenone binds to albumin and does not bind to sex steroid-binding globulin and corticoid-binding globulin; about 3-5% is the free fraction.

Due to the long half-life, C ss is achieved after 10 days of daily dosing and exceeds the concentration after a single dose by 2-3 times.

Metabolism. The main metabolites are the acid form of drospirenone and 4,5-dihydro-drospirenone-3-sulfate, which are formed without the participation of isoenzymes of the cytochrome P450 system.

Removal. The serum clearance of drospirenone is 1.2-1.5 ml/min/kg. Some part of the received dose is excreted unchanged. Most of the dose is excreted by the kidneys and through the intestines in the form of metabolites in a ratio of 1.2:1.4; half-life is about 40 hours.

Indications:

Hormone replacement therapy for menopausal disorders in postmenopause; prevention of postmenopausal osteoporosis.

XIV.N80-N98.N95.1 Menopause and menopause in women

XIV.N80-N98.N95.2 Postmenopausal atrophic vaginitis

XIII.M80-M85.M81.0 Postmenopausal osteoporosis

XIV.N80-N98.N95.9 Menopausal and premenopausal disorders, unspecified

XVIII.R20-R23.R23.4 Changes in skin structure

Contraindications:

Hypersensitivity, vaginal bleeding of unknown origin, established or suspected breast cancer, established or suspected hormone-dependent precancerous diseases or hormone-dependent malignant tumors, benign or malignant liver tumors (including a history), severe liver disease, severe kidney disease, including history (until normalization of renal function indicators), acute arterial thrombosis or thromboembolism (including myocardial infarction, stroke), deep vein thrombosis in the acute stage, venous thromboembolism (including a history), severe hypertriglyceridemia, pregnancy, lactation.

Carefully:

Arterial hypertension, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndrome), cholestatic jaundice or cholestatic pruritus during pregnancy, endometriosis, uterine fibroids, diabetes.

When prescribing hormone replacement therapy to women who have several risk factors for the development of thrombosis or a high degree of severity of one of the risk factors, the possibility of mutually enhancing the effect of risk factors and the prescribed treatment on the development of thrombosis should be taken into account. In such cases, the total value of the existing risk factors increases. If there is a high risk, the drug is contraindicated.

Pregnancy and lactation:

FDA Category X Advisory. No violations reported. If there are no two subsequent cycles in a row, it is necessary to discontinue use and exclude pregnancy; if the dosage regimen is violated, exclude pregnancy after the first missing cycle. To try to get pregnant, you should wait 1-2 months after stopping the drug or wait for regular menstruation.

Directions for use and dosage:

Orally, 1 tablet daily; swallow whole with a small amount of liquid. If you are not taking estrogen or switching from another combination hormonal drug for continuous use, treatment is started at any time. Patients switching from a combination drug to cyclic hormone replacement therapy should begin taking the drug after the end of withdrawal bleeding.

After finishing taking 28 tablets from the current pack, you must start a new pack, taking the first tablet on the same day of the week as from the previous pack.

If you miss several tablets, vaginal bleeding may develop.

Side effects:

The most common adverse drug reactions observed when using the drug were breast tenderness, bleeding from the genital tract, gastrointestinal pain and abdominal pain. Irregular bleeding usually disappears with long-term therapy. The frequency of bleeding decreases with increasing duration of treatment.

Serious adverse reactions include arterial and venous thromboembolic complications and breast cancer.

Mental disorders: often - emotional lability.

From the side of the central nervous system: often - migraine.

From the outside of cardio-vascular system: infrequently - venous and arterial thromboembolic complications (occlusion of peripheral deep veins, thrombosis and embolism/occlusion of pulmonary vessels, thrombosis, embolism and infarction/myocardial infarction/cerebral infarction and stroke, with the exception of hemorrhagic).

From the digestive system: often - gastrointestinal pain, abdominal pain.

From the reproductive system: very often - pain in the mammary glands (including discomfort in the mammary glands), bleeding from the genital tract; often - cervical polyp; infrequently - breast cancer.

In women with hereditary angioedema, exogenous estrogens may exacerbate symptoms.

Hypersensitivity reactions (including symptoms such as rash and urticaria) have also been observed.

Overdose:

Acute toxicity studies have not revealed a risk of acute side effects when accidentally taking the drug in quantities many times higher than the daily therapeutic dose. In clinical studies, the use of drospirenone up to 100 mg or combined estrogen/progestin drugs containing 4 mg estradiol was well tolerated.

Symptoms that may occur in case of overdose: nausea, vomiting, bleeding from the vagina.

Treatment: there is no specific antidote; if necessary, symptomatic therapy is carried out.

Interaction:

Anticoagulants, derivatives of coumarin and indanedione - multidirectional changes in the activity of anticoagulants are possible.

Ascorbic acid, - increased estrogen concentrations, possibly associated with inhibition of conjugation.

Atorvastatin - increases the concentration of estrogen.

Benzodiazepines - inhibition of their metabolism.

Hepatotoxic drugs - increased toxicity due to activation of hepatic blood flow by estrogens.

Glucocorticoids - decreased metabolism, increased synthesis of transcortin.

Clofibrate - decrease in its effectiveness.

Tobacco smoking - a possible decrease in estrogen concentration due to the induction of microsomal liver enzymes, increasing the risk of cardiovascular diseases.

Ritonavir - decreases the concentration of estrogen.

Antidiabetic agents taken orally and insulin - when used together, the effectiveness of insulin and hypoglycemic agents may decrease due to increased glucose tolerance, especially in persons with diabetes mellitus.

Drugs that induce microsomal liver enzymes (especially barbiturates) - reduce the activity of oral contraceptives.

Tamoxifen - a decrease in its antiestrogenic activity.

Tricyclic antidepressants, neuroleptics - increased risk of developing movement disorders, increased concentration of antidepressants, chorea.

Cyclosporine - an increase in its plasma concentration.

Special instructions:

Not used for contraception. If contraception is necessary, non-hormonal methods should be used (with the exception of calendar and temperature methods). If you suspect pregnancy, you should stop taking the pills until pregnancy has been ruled out.

With long-term estrogen monotherapy, the risk of developing endometrial hyperplasia or carcinoma increases. Studies have confirmed that the addition of gestagens reduces the risk of endometrial hyperplasia and cancer.

Clinical trial data and observational studies have found an increase in the relative risk of developing breast cancer in women using hormone replacement therapy for several years. This may be due to earlier diagnosis, accelerated growth of an existing tumor during hormone replacement therapy, or a combination of both factors.

The relative risk increases with duration of therapy but may be absent or reduced with estrogen-only treatment. This increase is comparable to the increased risk of breast cancer in women with a later onset of natural menopause, as well as with obesity and alcohol abuse. Increased risk gradually decreases to normal levels for several (but most of five) years after stopping hormone replacement therapy.

The increased risk of breast cancer has been suggested based on the results of more than 50 epidemiological studies (risk ranges from 1 to 2).

Hormone replacement therapy increases mammographic breast density, which in some cases may have a negative effect on X-ray detection of breast cancer.

During the use of sex steroids, which also include drugs for hormone replacement therapy, benign, and even more rarely, malignant liver tumors have been observed in rare cases. IN in some cases these tumors resulted in life-threatening intra-abdominal bleeding. If there is pain in the upper abdomen, an enlarged liver, or signs of intra-abdominal bleeding, the differential diagnosis should take into account the possibility of a liver tumor.

It is known that estrogens increase the lithogenicity of bile. Some women are predisposed to developing gallstones when treated with estrogen.

There is limited clinical trial data on a possible increased risk of dementia in women who start taking medications containing . As observed in studies, the risk may be reduced if hormone replacement therapy drugs containing conjugated equine estrogens, started in early menopause. It is not known whether this applies to other hormone replacement therapy products.

Treatment should be stopped immediately if migraine-like or frequent and unusually severe headaches appear for the first time, as well as if other symptoms appear - possible precursors of a thrombotic stroke of the brain.

The relationship between hormone replacement therapy and the development of clinically significant arterial hypertension has not been established. A slight increase in blood pressure has been described in women taking hormone replacement therapy; clinically significant increases are rare. However, in some cases, if persistent clinically significant arterial hypertension develops while taking hormone replacement therapy, discontinuation of hormone replacement therapy may be considered. In women with high blood pressure, there may be a slight decrease in blood pressure while taking the drug. In women with normal blood pressure, no significant changes in blood pressure are expected.

In renal failure, the ability to excrete potassium may be reduced. Taking drospirenone does not affect serum potassium concentrations in patients with mild to moderate forms of renal failure. The risk of developing hyperkalemia cannot theoretically be excluded only in the group of patients whose serum potassium concentration before treatment was determined to be at the upper limit of normal, and who additionally take potassium-sparing drugs.

For mild liver dysfunction, including various forms Hyperbilirubinemia, such as Dubin-Johnson syndrome or Rotor syndrome, requires medical supervision, as well as periodic liver function tests. If liver function indicators deteriorate, the drug should be discontinued.

In case of recurrence of cholestatic jaundice or cholestatic itching, which was observed for the first time during pregnancy or previous treatment with sex steroid hormones, the drug should be stopped immediately.

Special monitoring of women is necessary when triglyceride concentrations increase. In such cases, the use of hormone replacement therapy may cause a further increase in the concentration of triglycerides in the blood, which increases the risk acute pancreatitis.

Although hormone replacement therapy may affect peripheral insulin resistance and glucose tolerance, there is usually no need to change the treatment regimen of patients with diabetes mellitus while undergoing hormone replacement therapy. However, women with diabetes should be monitored when undergoing hormone replacement therapy.

Some patients under the influence of hormone replacement therapy may develop undesirable manifestations of estrogen stimulation, for example, pathological uterine bleeding. Frequent or persistent pathological uterine bleeding during treatment is an indication for examination of the endometrium in order to exclude an organic disease.

Under the influence of estrogens, uterine fibroids can increase in size. In this case, treatment should be stopped.

If prolactinoma is suspected, this disease should be excluded before starting treatment. If prolactinoma is detected, the patient should be under close medical supervision (including periodic assessment of drug concentrations).

In some cases, chloasma may occur, especially in women with a history of chloasma during pregnancy. During drug therapy, women with a tendency to develop chloasma should avoid prolonged exposure to the sun or ultraviolet radiation.

The following conditions may occur or be aggravated by hormone replacement therapy, and women with these conditions should be under medical supervision while undergoing hormone replacement therapy: epilepsy, benign breast tumor, bronchial asthma, migraine, porphyria, otosclerosis, systemic lupus erythematosus, chorea minor .

In women with hereditary forms of angioedema, exogenous estrogens may cause or worsen symptoms of angioedema.

Drospirenone is well tolerated in women with mild or moderate hepatic impairment. In women with mild to moderate renal impairment, a slight slowdown in the elimination of drospirenone was observed, which was not clinically significant.

Instructions

Drospirenone is a hormone that is part of the group of oral contraceptives. On its basis, a large number of contraceptive drugs are manufactured, as well as medications that have a therapeutic effect on androgen-dependent diseases. You can buy the substance in any city, but only with a prescription. The low cost allows you to use the hormone even in the absence of financial resources.

General information

Before you start using various oral contraceptives, you need to understand in detail what kind of hormone Drospirenone is. Its properties allow the substance to be used in combination with other hormones, which maximizes the therapeutic effect.

Substance information

Drospirenone is a synthetic hormone and is a derivative of Spironolactone - a potassium-sparing diuretic, a competitive antagonist of aldosterone and other mineralocorticoids. In its pharmacological properties, it is very similar to natural Progesterone - an endogenous steroid and progestogenic sex hormone that affects the menstrual cycle, pregnancy and embryonic development in humans.

Basic chemical and physical parameters:

  • molecular weight - 366.5 μg/mol;
  • melting point - 200 degrees Celsius;
  • density - 1.26 g/cubic centimeter.

The hormone can influence human sexual function, as well as have antigonadotropic, progestogenic, antiandrogenic and antimineralocorticoid effects.

To find out which contraceptives contain Drospirenone, you should consult your doctor. Only he can accurately determine the most effective option, which will perform its functions efficiently and not render negative impact to your health.

Drospirenone is often used in various combined contraceptive contraceptives (COCs) as active substance. In its pure form, the hormone is contained only in two medicines:

  1. Yarina. This medication is available in the form of film-coated tablets. It is used only to prevent unwanted pregnancy. The drug has many contraindications, so it should be taken with extreme caution. It is important to follow all doctor’s instructions and limit the number of pills taken.
  2. Angelique. This medicine is also available in film-coated tablets that may vary in color. It is used for the prevention of postmenopausal osteoporosis, as well as for menopausal disorders in women with a non-removed uterus. The drug has virtually no negative effect on the body, but has several features of use. If you follow all of them, you can avoid any side effects.

In all other contraceptives, Drospirenone is used as one of the components. In the right proportions, it complements other chemical compounds and allows you to achieve the desired therapeutic effect.

List of medications:

  • Jess;
  • Dailla;
  • Midiana;
  • Dydrogesterone;
  • Zentiva;
  • Vidor.

In all of these drugs and their analogues, Ethinyl estradiol, Estradiol, Dienogest, Chlormadinone, and Cyproterone acetate act as additional active ingredients.

Indications for use

Most drugs based on Drospirenone have the same indications, so they are often considered together. Doctors recommend using the hormone only for its intended purpose. Otherwise, you may cause harm to your health.

  • prevention of postmenopausal osteoporosis (as part of complex therapy);
  • hormonal contraception in women with fluid retention in the body or with folate deficiency (vital vitamins);
  • hot flashes, sweating and other vasomotor symptoms during menopausal disorders;
  • involutional changes in the genitourinary tract (only in patients with a non-removed uterus);
  • prevention of pregnancy (in combination with other synthetic hormonal agents);
  • contraception for severe premenstrual syndrome.

Main contraindications

Drospirenone has several contraindications. They must be taken into account before purchasing medications and starting to use them. Otherwise, various problems can form that will develop into a full-fledged disease.

It is prohibited to use drugs with the hormone Drospirenone in the following situations:

  • porphyrin disease (hereditary disorder of pigment metabolism with an increased content of porphyrins in the blood and tissues, as well as their increased release);
  • tendency to thrombosis;
  • severe form of thrombophlebitis and thromboembolism;
  • acute liver failure;
  • the presence of vaginal bleeding of unknown etiology;
  • all trimesters of pregnancy;
  • breastfeeding period;
  • individual intolerance to the hormone.

In some cases, Drospirenone is considered relatively prohibited. In such a situation, it should be used with extreme caution. During the treatment period, it is important not only to comply with the prescribed dosages, but also to limit the duration of the course of taking the drugs. If you detect the slightest negative changes in your health, you should immediately stop therapy and seek help from the nearest medical facility.

Drospirenone is taken with caution in the following cases:

  • diabetes.

  • arterial hypertension (prolonged increase in blood pressure);
  • cholestatic jaundice (a pathological process in the patient’s body in which bile does not flow through the liver into the duodenum, but accumulates in the blood);
  • cholestatic itching that appears during pregnancy;
  • Gilbert's syndrome (a hereditary disease characterized by episodes of jaundice, which develops as a result of an increase in indirect bilirubin in the blood serum);
  • Rotor syndrome (hereditary pigmentary hepatosis);
  • Dubin-Johnson syndrome (pigmentary hepatosis, characterized by impaired excretion of conjugated bilirubin from hepatocytes into the bile capillaries);
  • endometriosis (a disease characterized by the proliferation of endometrial cells);
  • diabetes.

Instructions for use

For Drospirenone to have the most effective effect, it must be taken correctly. To do this, you must accurately calculate the dosage and determine the permissible duration of use. Only in this case can you achieve the desired therapeutic effect and avoid any negative consequences.

Dosages and rules

Dosages and rules

All drugs containing Drospirenone are available in the form of tablets intended for oral administration. They should be swallowed whole and washed down with plenty of clean, still water (at least 200 ml). In this case, the liquid must be heated to room temperature. Do not crush the tablets in any way as this may render them ineffective.

  1. It is forbidden to use more than 1 tablet per day, as this can negatively affect the female body.
  2. You can take Drospirenone at any time of the day. It is important to take the tablets at the same time every day (for example, before going to bed or after waking up).
  3. If you miss a dose, it is forbidden to compensate for forgetfulness and take 2 tablets at once.
  4. If a long-term suspension of the course is necessary, the treatment regimen should be adjusted. This work should be entrusted to a highly qualified doctor, who will take into account all the nuances of the current situation and find the optimal solution.

Side effects

If you take contraceptives containing the hormone Drospirenone incorrectly, you may experience side effects. Because of them, your health condition may worsen.

Possible complications:

  1. Circulatory system. In rare cases, patients may experience thrombocytosis and anemia.
  2. The immune system. The drug can cause various allergic reactions. There are negative consequences from the body's increased sensitivity to the hormone.
  3. Metabolism. Women taking Drospirenone may develop hyponatremia and hyperkalemia.
  4. Nervous system. Patients often complain of severe headaches and dizziness. Migraine develops, nervousness, drowsiness and depression appear. With large overdoses, tremor, vertigo and anorgasmia may occur.
  5. Organs of vision. Drospirenone may affect visual acuity and may also cause dry eye syndrome and conjunctivitis.
  6. The cardiovascular system. If you make mistakes in taking pills, tachycardia and arterial hypertension may develop. Rarely, arterial and venous thromboembolism, varicose veins, nosebleeds and phlebitis occur.
  7. Digestive system. Women suffer from pain in the abdominal area, exacerbation of gastritis, severe diarrhea, attacks of nausea and vomiting. Much less common gastrointestinal disorders, candidiasis oral cavity and a feeling of fullness in the abdomen.
  8. Skin. A common side effect is a rash on the surface of the skin accompanied by severe itching. In addition, acne dermatitis, eczema, erythema, hypertrichosis and dry skin occur.
  9. Musculoskeletal system. The hormone can cause pain in the back, limbs and muscles.
  10. Reproductive system. Women experience breast pain, amenorrhea and metrorrhagia. With excessive dosages, vaginal and uterine bleeding, menstrual irregularities, hypomenorrhea and dysmenorrhea may occur.
  11. General disorders. Patients may experience increased sweating, weight gain, weakness, and asthenia.

special instructions

During clinical trials, some features of Drospirenone were discovered. Thanks to them, you can avoid errors in use and accurately calculate dosages.

Basic instructions:

  1. Studies have found that the use of the hormone increases the risk of developing venous thromboembolism. Because of this, changes in the health status of women predisposed to this disease should be closely monitored.
  2. Patients with mild to moderate renal failure should regularly monitor the concentration of potassium ions in the blood.
  3. You can use contraceptives containing Drospirenone only after undergoing full examination and passing all tests.
  4. Women suffering from chronic liver diseases should periodically monitor the functionality of this organ.
  5. With moderate hypertriglyceridemia, it is necessary to monitor the amount of triglycerides in the blood.
  6. Patients with diabetes mellitus varying degrees severity can use Drospirenone only under medical supervision.
  7. The hormone does not combine well with alcohol, so you should refrain from drinking alcohol during the period of therapy.
  8. Drospirenone causes drowsiness and reduces reaction time. Because of this feature, it is prohibited to drive a car or any other vehicle. It is not recommended to perform work that requires special care and increased concentration.

Pharmacological interactions

Before taking drugs containing Drospirenone, it is necessary to take into account not only their characteristics, but also interactions with other drugs. Some combinations may cause side effects and reduce the therapeutic effect.

Main combinations and their consequences for the body:

  1. When taken simultaneously with drugs that induce liver enzymes (Carbamazepine, Primidone, Topiramate), their effectiveness decreases.
  2. Drospirenone reduces the therapeutic effect of taking anabolic steroids and drugs that stimulate the smooth muscles of the uterus.
  3. The concentration of the hormone in the blood is significantly reduced due to interaction with antibiotics of the tetracycline and penicillin groups.
  4. Combination with paracetamol may increase bioavailability.
  5. Some nonsteroidal anti-inflammatory drugs may affect serum potassium concentrations.
  6. Drospirenone increases the activity of Aldosterone and Renin.

Cost and comparison with other hormones

All medications containing Drospirenone are included in the Register of Medicines (RLS), and therefore can be sold throughout Russia. You can buy them not only in large settlements, but also in smaller ones. The cost of drugs in Moscow can vary from 1 to 5 thousand rubles. In other cities and regions of the country the price is slightly lower than in the capital, and in neighboring countries it is higher.

To determine which is better, Drospirenone, Desogestrel or any similar hormone, it is necessary to study in detail all the available information. Thanks to it, you can find out the main differences and choose best option, which will not have a negative impact on the patient.

It is best to take Drospirenone or Gestodene only after consulting a doctor and undergoing various tests. Otherwise, each of these hormones can cause a worsening of the condition and the development of side effects.

Drospirenone is one of the most popular hormones included in oral contraceptives. If you use it correctly and follow all doctor’s recommendations, you can achieve the desired result and avoid any complications.

There are many types of contraceptives to protect against unwanted pregnancy. They come in different groups and compositions, and also have different dosage and admission rules. The active component of many drugs is drospirenone. What kind of hormone is this? You can find out all the necessary information from the article.

Properties

Drospirenone belongs to the hormonal group of substances. These are estrogens, gestagens. The product is a derivative of spirinolactone. This hormone has a therapeutic effect in androgen-dependent diseases such as seborrhea and acne. Drospirenone also helps remove excess fluid and sodium ions from the body, which cause weight gain, increased blood pressure, and swelling of the mammary gland.

In general, all those unpleasant conditions that are observed during the premenstrual period can be eliminated by the hormone. Therefore, women who take drospirenone-based drugs rarely suffer from PMS. When ingested, the substance is quickly absorbed. Do all women need drospirenone? What kind of hormone is this? Both endometriosis and menstrual irregularities - hormonal treatment is indicated for all these disorders.

Where else is drospirenone used?

The hormone is prescribed for the combined treatment of osteoporosis in the postmenopausal period. The substance is used as replacement therapy for all symptoms of postmenopausal syndrome, which are accompanied by increased sweating and fever.

The product copes well with sleep disturbances, depression, and irritability in women before menstruation and at the beginning of menopause. In pharmacies you can find the drug "Drospirenone" (suppresses ovulation). This remedy is widely used to prevent pregnancy. The hormone is prescribed by a doctor in individually. It is not recommended to use drospirenone-based drugs on your own.

Contraindications

This hormone should not be prescribed if you are hypersensitive. Also for thrombosis, vaginal bleeding of unknown etiology, thromboembolism. Do not take during pregnancy and lactation, for cancer of the female genital organs and breast. Caution should be used when prescribing the drug for circulatory problems, high blood pressure, bronchial asthma, and diabetes mellitus.

It should not be used for pathologies of the liver or central nervous system, which are accompanied by depression and epilepsy. Drospirenone - what kind of hormone is it? Why shouldn't you take it uncontrollably? Experts say that unpleasant symptoms may develop.

Side effects

The hormone can cause an allergic reaction, which manifests itself as a rash and itchy skin. The substance can cause dizziness, headache, thromboembolism, increased blood pressure, blurred vision, vomiting, nausea, stomach pain, and diarrhea. can lead to such unpleasant consequences as changes in body weight, sleep disturbances, and apathy.

On the part of the reproductive system, irregularities in the menstrual cycle, intermediate bleeding, and enlarged mammary glands are observed. Benign tumors may appear in the breast and uterus, changes in the vaginal smear, and an increase in fibroids. In rare cases, intolerance may occur contact lenses, swelling, increased heart rate, thrombophlebitis. Drospirenone suppresses ovulation. Women who are planning a pregnancy should avoid hormone-based medications.

If we consider contraceptives with drospirenone, the most popular is Yarina. The features of its use will be described below.

The drug "Yarina"

It is monophasic and has antiandrogenic properties. Available in tablet form yellow color. The drug contains drospirenone and enylestradiol. Available in blisters.

The main effect of the drug is based on suppressing ovulation and increasing viscosity. Women taking the combined contraceptive normalize their periods, reduce pain, and bleeding becomes less pronounced, which reduces the risk of anemia. After many studies, scientists announced that the hormone that is part of birth control pills, prevents the development of ovarian and endometrial cancer. Drospirenone prevents the formation of edema, increased blood pressure, and the indication for taking the pills is contraception.

The drug should not be prescribed for thrombosis in the acute or chronic period. If there is a history of migraine, diabetes mellitus, or a risk of venous and arterial thrombosis, the medication is also not used.

The tablets must be taken daily. The medicine should be swallowed whole and washed down with a small amount of water. The appointment lasts 21 days. Then you need to take a break of seven days and start taking the medicine from another package. It is better to take the pills at the same time of day.

Should I use drugs that contain drospirenone?

We managed to figure out what kind of hormone this is. Its main purpose is to suppress ovulation. Therefore, women who are not planning a pregnancy should use the drugs. However, it is worth remembering that side effects has drospirenone. Which contraceptives contain the hormone? Enough in many. Before using birth control pills, you should carefully study the instructions.


For quotation: Tarasova M.A., Lekareva T.M. What will drospirenone change in contraception and hormone replacement therapy? // RMJ. 2005. No. 17. S. 1139

One of the most important extragenital effects of endogenous progesterone is its antimineralcorticoid effect as a natural aldosterone antagonist. Aldosterone, supporting the active absorption of sodium and the excretion of potassium and hydrogen ions in the urine in the distal renal tubules, performs biological function regulator of extracellular metabolism and water metabolism. In the luteal phase of the menstrual cycle, against the background of increased secretion of progesterone, natriuresis increases.

Estradiol and synthetic estrogens have a sodium-sparing effect opposite to progesterone, which is mainly due to an increase in the synthesis of angiotensinogen in the liver and, accordingly, an increase in the level of angiotensin, the main stimulator of aldosterone production. Synthetic progestogens, derivatives of 17a-hydroxyprogesterone and 19-nortestosterone, do not have an antimineralkorticoid effect and do not counteract the stimulating effect of estrogen on the renin-angiotensin-aldosterone system (RAAS). The result of sodium and fluid retention in women taking estrogen-containing drugs for contraception and hormone replacement therapy (HRT) may be weight gain due to fluid retention, swelling and increased blood pressure in predisposed women.
Drospirenone is a new progestogen - a derivative of 17a-spironolactone, the spectrum of effects of which is progestogenic, antimineralocorticoid and antiandrogenic, characteristic of natural progesterone. The antimineralocorticoid activity of drospirenone is 8 times higher than that of spironolactone (a diuretic with antimineralocorticoid activity).
The results of this property of the drug are a decrease in body weight and a decrease in systolic and diastolic blood pressure. The loss of sodium in the body caused by drospirenone does not lead to clinical significant increase potassium concentration, which allows its use even in women with impaired renal function.
In a study by Oelkers et al. a significant increase in cumulative sodium excretion was established in the group of healthy women receiving 2 mg of drospirenone compared to the placebo group. It should also be noted that there is an increase in the level of aldosterone in plasma and its excretion in the urine, which, according to the authors, characterizes compensatory activation of the RAAS in response to changes in the electrolyte composition of the blood.
The same study showed that drospirenone significantly increases plasma renin activity, and this effect is independent of the dose of the drug. In addition, a slight decrease in body weight was detected in patients taking a drug containing 30 mcg ethinyl estradiol and 3 mg drospirenone (Yarina), in contrast to women taking a contraceptive containing 30 mcg ethinyl estradiol in combination with 150 mcg desogestrel, in whom, on the contrary, There was a slight increase in body weight.
These data indicate that drospirenone in COCs can effectively counteract estrogen-dependent sodium and fluid retention.
Drospirenone is also an androgen receptor antagonist. The antiandrogenic activity of drospirenone is 5–10 times stronger than that of progesterone, but lower than that of cyproterone acetate.
Combined oral contraceptives (COCs), by inhibiting the secretion of androgens by the ovaries, have a positive effect on acne and seborrhea. In addition, ethinyl estradiol (EE) causes an increase in the concentration of sex steroid binding globulin (SHBG), which reduces the free fraction of androgens in the blood plasma. The severity of the androgenic effect of the progestogen included in the combination drugs significantly affects the effects of EE, such as an increase in GSPC and antiatherogenic changes in the spectrum of lipoproteins. Drospirenone does not reduce the level of SHBG and has an antiatherogenic effect on lipid metabolism.
The use of combined estrogen-progestogen preparations containing drospirenone for contraception and hormone replacement therapy allows for additional benefits associated with the pharmacological and clinical characteristics of this progestogen.
Contraception with drospirenone
Modern hormonal contraceptives provide real opportunity regulate the timing of pregnancy and thus reduce the risk of abortion-related maternal mortality. However, their impact on reproductive health is not limited to this. Estrogen-gestagen contraceptives have numerous non-contraceptive preventive and therapeutic effects: they reduce the abundance, duration and pain of menstrual blood loss, have a positive effect on the condition of the skin, reduce the risk of anemia, ectopic pregnancy, pelvic inflammatory diseases, benign and malignant ovarian tumors, endometrial cancer.
Currently, according to WHO (2001), about 100 million women use hormonal methods of contraception. There is no doubt that the relevance of hormonal contraception will continue to increase in the future.
The new progestogen drospirenone is part of the combined low-dose monophasic contraceptive Yarin (Schering AG, Germany), containing 30 μg of EE and 3 mg of drospirenone.
As is known, the effectiveness of contraceptive methods is determined by the number of pregnancies occurring in 100 women in the first 12 months of using a contraceptive (Pearl index). For Yarina, this figure is 0.07, which meets the criteria for a highly effective contraceptive.
Studies of the duration of COC use have shown that about 30% of women stop using the drugs within the first year. The main reason for discontinuing COCs is side effects. Side effects such as weight gain, breast engorgement and tenderness, and increased blood pressure are associated with the effect of EE on the RAAS.
Due to its antimineralkorticoid activity, drospirenone prevents sodium and fluid retention in the body, which maintains stability of body weight and blood pressure levels and prevents engorgement of the mammary glands when taking Yarina. During the first month of use, headache, tension in the mammary glands, decreased libido, and depression occur in 3.1–4.6%; nausea – in 4.6–6.2% of cases. By the sixth month of treatment, all of the above symptoms are mostly relieved.
Medicinal properties of COCs
with drospirenone
Drospirenone, which has an effect on the RAAS similar to spironolactone, opens up new therapeutic possibilities for the use of COCs.
This primarily applies to the treatment of premenstrual syndrome (PMS). At least 95% of women of reproductive age, to one degree or another, a few days before menstruation, experience symptoms such as irritability (93.8%), engorgement and tenderness of the mammary glands (87.5%), flatulence (75%), headache (56.3%), mood changes with a tendency towards depression (56.3%), swelling (50%).
The use of COCs is the most common therapeutic strategy for PMS. However, the severity of PMS symptoms does not always decrease, and may even worsen, which is associated with a deficiency of natural progesterone.
Numerous clinical studies have shown the positive effect of the drug Yarina on the somatic and psycho-emotional symptoms of PMS.
In an open, uncontrolled study conducted by Apter D. et al. . The effectiveness of the drug was assessed in 336 women aged 18 to 42 years using the health questionnaire The Psychological General Well-Being Index (PGWBI), which includes indicators such as anxiety, low mood, general well-being, ability to control one’s emotions, and overall health , activity. After three cycles of treatment, there was a trend toward improvement, and after six cycles, a statistically significant increase in overall well-being was detected. In addition, the severity of somatic symptoms was assessed. A decrease in the symptoms of bloating and engorgement of the mammary glands occurred by the 6th cycle of taking the drug in 77.3 and 69% of women, respectively. In addition, in 52% of cases, patients noted a decrease in swelling of the extremities. Body weight remained stable or even decreased slightly. Although this study did not include a placebo group, this shortcoming was compensated for by the duration of treatment (12 months), because It is known that after 3–6 months the placebo effect is leveled out.
In another study conducted in the USA in 2002, Borenstein J. et al. assessed the effect of the drug on premenstrual symptoms and quality of life in more than a thousand women suffering from PMS. Premenstrual symptoms and quality of life were assessed before treatment and after two cycles of treatment. The use of Yarina led to an improvement in the physical and psycho-emotional symptoms of PMS, as well as overall well-being and quality of life.
Boschitsch E. et al. studied the effectiveness of using Yarina and a drug containing 30 mcg of EE and 150 mcg of desogestrel in the treatment of PMS. In the group of women receiving Yarina, a significant decrease in body weight was noted. In addition, there was a statistically significant decrease in severity premenstrual symptoms, such as depressed mood, fluid retention, increased appetite. The drug had a positive effect on skin manifestations. The number of acne elements decreased by 62.5%, seborrhea decreased by 25.1%. After the end of the study, 75.6% of women expressed a desire to continue taking the drug.
In a study by Brown C. et al. 326 women aged 18 to 35 years filled out the 23-component Women’s Health Assessment Questionnaire at the beginning of observation and after completing the 6th cycle of taking Yarina. At the end of cycle 6, there was an improvement in scores on scales characterizing fluid retention and emotional status. It should be especially noted that the results were similar in the groups of patients who had not previously used oral contraceptives and used OCs that did not contain drospirenone.
In a randomized placebo-controlled study, Freeman E.W. et al. The effectiveness of the drug Yarina was studied during 3 menstrual cycles in 82 women with severe PMS, the so-called premenstrual dysphoric syndrome. Patients treated with a drug containing EE and drospirenone showed significantly greater improvement in all 22 items on the Calendar of Premenstrual Experiences (COPE) questionnaire. A significant difference between the groups was obtained for factor 3 – constant increased appetite, acne.
In all of the studies described above, a standard dosage regimen was used: taking 21 tablets followed by a seven-day break. It is known that it is during this period of time that PMS symptoms more often recur in women taking oral contraceptives.
The use of an extended COC regimen, when the patient receives the drug daily for 9–12 weeks and only then takes a break, increases the effectiveness of PMS therapy. A decrease in symptoms in this case is noted by 74% of women. When using this regimen, breakthrough bleeding is quite rare; a menstrual-like reaction occurs when the pills are discontinued.
Taking these data into account, a study was conducted on the use of Yarina in an extended regimen. It involved 1,433 women, 175 of whom received the drug continuously for 42–126 days. It was shown that swelling of the extremities decreased by 49% in patients taking the drug in an extended regimen compared to 34% in patients using the standard 21-day regimen. Soreness of the mammary glands decreased by 50 and 40%, respectively, and the feeling of bloating by 37 and 29%. An extended regimen is also more effective in women with acne. The incidence of breakthrough bleeding was 15% at the beginning of therapy and tended to decrease as the drug was continued. There was no increase in the incidence of other side effects.
Thus, an extended regimen can be used to increase the therapeutic effectiveness of Yarina.
The antiandrogenic properties of COCs with drospirenone are due to several mechanisms: suppression of ovulation, the ability of drospirenone to block androgen receptors and the absence of a decrease in the concentration of sex steroid binding globulin.
The use of the drug Yarina is pathogenetically justified in women with excess body weight or increased blood pressure when taking combined contraceptives, as well as those requiring therapy due to premenstrual syndrome, acne, mild arterial hypertension or “idiopathic edema”.
Hormone replacement therapy with drospirenone
Termination of the estrogen-producing function of the ovaries, leading to the development of vasomotor symptoms, sleep disturbances, decreased resistance to psychological and emotional stress, urogenital and sexual disorders, changes in appearance, osteoporosis, back pain and fractures, significantly reduces the quality of life of older women. Correction of all these manifestations is the goal of hormone replacement therapy in peri- and postmenopausal women.
Drospirenone is part of a combination drug for continuous HRT in postmenopause Angelique (Schering AG, Germany), containing 17b-estradiol and 2 mg of drospirenone.
The use of drospirenone in a combination drug for HRT, similar to Yarina, reduces the incidence of side effects (such as mastodynia, swelling, weight gain due to fluid retention) and improves tolerability of therapy. Increasing the acceptability of therapy (“compliance”) is the most important condition for its maximum effectiveness, since preventive effects are achieved only with a sufficient duration of estrogen therapy. In addition, the antialdosterone effect of drospirenone is especially important for older women. age groups, having a higher frequency hypertension And coronary disease hearts.
It is known that the renin–angiotensin–aldosterone system has a multicomponent effect on the function of the cardiovascular system. Angiotensin II has a strong direct vasoconstrictor effect on arteries and a less strong vasoconstrictor effect on veins. In addition, angiotensin II serves as the main stimulator of aldosterone production, the main regulator of water and electrolyte balance, acting through mineralocorticoid receptors in the distal tubules of the kidneys.
At the same time, it was recently discovered that aldosterone receptors are also located in other organs, including the brain, blood vessels and heart. This indicates the role of aldosterone in the physiology and pathology of the cardiovascular system. Excessive synthesis of aldosterone, which always accompanies the course of heart failure, leads to stimulation of fibroblasts, which, in turn, causes an increase in collagen synthesis, the development of interstitial fibrosis, and disruption of the functional activity of the myocardium with the development of left ventricular diastolic dysfunction. In addition, excessive synthesis of aldosterone promotes increased sodium reabsorption, loss of potassium, retention of water in the renal tubules, which, in turn, leads to an increase in the volume of circulating blood and, as a consequence, to overload of the left ventricle of the heart with volume and pressure, which also leads to progression heart failure.
The influence of aldosterone on the development of cardiovascular pathology includes effects on cardiac and vascular fibrosis, hypertension, endothelial dysfunction, suppression of fibrinolysis, impaired heart rate. It has been shown that the use of the aldosterone receptor blocker spironolactone reduces blood pressure, improves endothelial function, reduces left ventricular hypertrophy, reduces the incidence of fatal arrhythmia and, as a result, leads to a 30% reduction in mortality among patients with severe cardiac pathology.
Large cohorts of patients have shown that circulatory levels of norepinephrine, renin, angiotensin II, aldosterone, endothelin-1 and adrenomedulin correlate with both the severity and prognosis of chronic heart failure. In particular, there is a complex relationship between the activity of the renin–angiotensin–aldosterone system and the overproduction of endothelin-1. As the Framingham Offspring Study (Framingham, Massachusetts) showed, even in normotensive individuals, a single measurement of aldosterone in the morning predicted the likelihood of increased blood pressure several years later.
A multicenter study examined serum potassium levels and blood pressure levels in postmenopausal women 45–70 years old with and without diabetes mellitus receiving Angeliq and angiotensin-converting enzyme inhibitors or angiotensin II receptor blockers. The women examined showed a hypotensive effect of HRT. In addition, hyperkalemia was not detected in any of the observed groups.
The hypotensive effect was also confirmed by the results of a 12-week multicenter, randomized, double-blind, placebo-controlled study of the effect of Angeliq on blood pressure in 212 postmenopausal women with moderate hypertension (BP in the range of 140/90–159/99 mmHg). Compared with the placebo group, women who used Angeliq showed a significant decrease in blood pressure and no significant changes in the potassium content in the blood serum.
The presented research results indicate new possibilities for combined estrogen-progestogen drugs containing drospirenone as a progestogen component. The contraceptive drug "Yarina", due to the antimineral corticoid and antiandrogenic effect of drospirenone, is well tolerated, associated with maintaining stable weight, no increase in blood pressure, improvement in skin condition, and effectiveness in relieving premenstrual symptoms. In addition, data have been obtained indicating the potential of HRT with drospirenone to reduce the risk of cardiovascular pathology in postmenopausal women.

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