Midiana - official instructions for use. The hormone drospirenone in various drugs Drospirenone instructions for use

What is drospirenone? It is a synthetic hormone similar in properties to natural progesterone. The agent is a derivative of spirinolactone.

This substance is from the group of oral contraceptives. It is usually used in combination with other hormones. Has a therapeutic effect on androgen-dependent diseases (acne, sulfur), removes sodium ions and excess fluid from the body. In this regard, it normalizes blood pressure, edema subsides, body weight decreases, pain in the mammary glands disappears. Also, in the course of treatment, the drug reduces the level of cholesterol in the blood and LDL, slightly increases the concentration of triglycerides.

For women: During menopause, the likelihood of colon cancer, hyperplasia and endometrial cancer is significantly reduced.

Drospirenone fights sleep disturbances, irritability with premenstrual syndrome, depression.

And, of course, the remedy is used to prevent unwanted pregnancy.

IMPORTANT! Preparations with drospirenone are prescribed by a doctor. Don't practice self-medication!

Indications for use

Drospirenone has multidirectional properties: gestagenic, antiandrogenic, antigonadotropic, antimineralocorticoid.

It is prescribed for:

Contraception (in combination with other hormones)
Complex therapy for the prevention of postmenopausal osteoporosis
Climacteric disorders (elimination of hot flashes, sweating)
Severe PMS symptoms
Treating acne, blackheads
Folate deficiency
Fluid retention in the body
Involutional changes in the genitourinary tract (in women with an unremoved uterus)

Contraindications

Allergic reactions to drospirenone
Porphyria
Tendency to form blood clots
Liver failure
Lactation (breastfeeding period)
Vaginal bleeding of unknown origin
Breast (or genital) cancer
Pregnancy
Thromboembolism or thrombophlebitis

Side effects

Allergy
Dizziness, headaches
Arterial hypertension
Puffiness
Thrombophlebitis, blood clots in the retinal veins, thromboembolism of the pulmonary artery or cerebral vessels
Calculous cholecystitis
Depression, apathy, drowsiness, insomnia
Vomiting, nausea
Weight jumps
Decreased visual acuity
Vaginal discharge (bloody or unusual consistency)
Decreased libido
Chloasma
Varicose veins, convulsions
Galactorrhea
Alopecia
Breast pain and swelling

Overdose: symptoms

Nausea
Vomit
Vaginal bleeding

Instruction (method of administration and dosage)

Drospirenone is prescribed according to different treatment regimens, which depend on the combination of the hormone in the drug.

Usually hormones are taken once a day at exactly the same time.

IMPORTANT! Therapy is prescribed by a doctor.

The duration and nuances of treatment should also be discussed by your doctor.

Drospirenone is available from pharmacies only with a prescription.

Interaction

Drospirenone reduces the effectiveness of anabolic steroids and drugs that stimulate the smooth muscles of the uterus.

Reduces the effectiveness of drugs that enhance liver enzymes (barbiturates, carbamazepine, oscarbazepine, hydantoin derivatives, primidone, rifampicin, topiramate, griseofulvin, felbamate).

Some antibiotics can interfere with the metabolism of drospirenone.

Contraceptives with drospirenone (analogs, cost)

The most common question about this tool on the Internet is: "What contraceptives contain?" Here is a list of drugs:

Angelique(Drospirenone + Estradiol) 28 pcs., 2 mg - 1160-1280 RUB.

Dailla

(Drospirenone + Ethinylestradiol) 28 pcs. - 900-1000 rubles.

Modelle Pro(Drospirenone + Ethinylestradiol)

Simizia(Drospirenone + Ethinylestradiol)

Modell Trend(Drospirenone + Ethinylestradiol)

Midiana(Drospirenone + Ethinylestradiol) Midiana, 21 pcs. - 680-700 RUB.

(Drospirenone + Ethinylestradiol) 21 pcs. - 1000-1300 RUB.

Vidora(Drospirenone + Ethinylestradiol)

Zentiva(Drospirenone + Ethinylestradiol)

Jess Plus

(Drospirenone + Ethinylestradiol with the addition of calcium levomefolicate)

Dimia, 28 pcs. - 980-990 RUB.

KOC composition

Hormonal contraceptives from the category of COCs (combined oral contraceptives) are a combination of two hormones (estrogen + progestogen).

Estrogen is always the same in all drugs and is presented as ethinyl estradiol. But as progesterone, both droperinone and another active substance can be used.

Distinctive features of drospirenone

Good anti-mineral corticoid activity
Helps block the binding of steroid hormone to mineralocorticoid receptors

Gestodene or Drospirenone?

Both synthetic hormones are effective. Side effects from taking them are minimized. Differences:

Preparations with gestodene are prescribed for dysmenorrhea, as well as for setting a regular menstrual cycle.

Drospirenone reduces the severity of PMS, relieves acne and removes excess fluid from the body. However, there is a risk of thromboembolism and hyperkalemia with prolonged use of drugs with this substance.

Desogestrel or Drospirenone?

Desogestrel is used to eliminate dysmenorrhea.

While taking drugs with drospirenone, the risk of weight gain is slightly higher.

BUT! In any case, only a qualified specialist should decide what is more suitable for you. Hormonal treatment is no joke.

Formula: C24H30O3, chemical name: (6R, 7R, 8R, 9S, 10R, 13S, 14S, 15S, 16S, 17S) -1,3 ", 4", 6,6a, 7,8,9,10,11,12 , 13,14,15,15a, 16-hexadecahydro-10,13-dimethylspiro-cyclopenta [a] phenanthrine-17.2 "(5H) -furan] -3.5" (2H) -dione).
Pharmacological group: hormones and their antagonists / estrogens, gestagens; their homologues and antagonists.
Pharmachologic effect: gestagenic, antiandrogenic, antigonadotropic, antimineralocorticoid.

Pharmacological properties

Drospirenone is a derivative of spironolactone. Drospirenone has a therapeutic effect on androgen-dependent diseases: seborrhea, acne, androgenic alopecia. Drospirenone increases the excretion of water and sodium ions, which can prevent an increase in body weight, blood pressure, breast tenderness, edema and other symptoms associated with fluid retention. Drospirenone does not have androgenic, estrogenic, antiglucocorticosteroid, glucocorticosteroid activity, does not affect insulin resistance and glucose tolerance, which, together with antiandrogenic and antimineralocorticoid effects, provides it with a pharmacological and biochemical profile that is similar to natural progesterone. Drospirenone attenuates the rise in triglyceride levels caused by estradiol. The mechanism of action of drospirenone is still unclear. When taken orally, drospirenone is completely and rapidly absorbed. The bioavailability of drospirenone is 76 - 85%. Food intake does not affect bioavailability. The maximum concentration is reached after 1 hour and is 22 ng / ml with multiple and single doses of 2 mg drospirenone. This is followed by a two-phase decrease in the plasma level of drospirenone with a terminal half-life of about 35 to 39 hours. After about 10 days of daily intake of drospirenone, an equilibrium concentration is reached. Due to the long half-life of drospirenone, the equilibrium concentration is 2 to 3 times higher than the concentration with a single dose. Drospirenone binds to plasma albumin and does not bind to corticoid-binding globulin and globulin, which binds sex hormones. Approximately 3-5% of drospirenone does not bind to proteins. The main metabolites of drospirenone are 4,5-dihydrospirenone-3-sulfate and the acidic form of drospirenone, which are formed without the participation of the cytochrome P450 system. The clearance of drospirenone is 1.2 - 1.5 ml / min / kg. Drospirenone is excreted mainly as metabolites in feces and urine in a ratio of 1.4: 1.2, with a half-life of approximately 40 hours; a small part of drospirenone is excreted unchanged.

Indications

As part of the combined treatment: prevention of postmenopausal osteoporosis; hormone replacement treatment for menopausal disorders in the postmenopausal period, including vasomotor symptoms (increased sweating, hot flashes), depressive conditions, sleep disturbances, irritability, involutional changes in the genitourinary tract and skin in women with an unremoved uterus; contraception; contraception and therapy for severe premenstrual syndrome; contraception and therapy for moderate acne); contraception for women with folate deficiency; contraception for women with symptoms of hormone-dependent fluid retention.

Drospirenone dosage and administration

The method of administration and doses are set individually by the doctor, depending on the indications and the dosage form used.

Contraindications for use

Hypersensitivity, porphyria, a tendency to thrombosis, severe violations of the functional state of the liver, acute forms of thromboembolic diseases or phlebitis, vaginal bleeding of unknown origin, cancer of the breast and genital organs, pregnancy, breastfeeding.

Restrictions on use

Pathology of the circulatory system, including arterial hypertension, severe disorders of the functional state of the kidneys, bronchial asthma, diabetes mellitus, pathology of the central nervous system, including depression, epilepsy, migraine.

Application during pregnancy and lactation

Drospirenone is contraindicated in pregnancy and lactation.

Side effects of drospirenone

Allergic reactions, thromboembolism (including cerebral and pulmonary artery vessels), retinal vein thrombosis, thrombophlebitis, dizziness, increased blood pressure, calculous cholecystitis, edema, cholestatic hepatitis, headache, drowsiness, depression, dysphoria, apathy, blurred vision, nausea, decreased appetite, vomiting, galactorrhea, changes in body weight, alopecia, hirsutism, increase, tension and pain in the mammary glands, disorders of the menstrual cycle (intermediate bleeding, contraction), decreased libido, spotting spotting, breakthrough uterine bleeding, changes in the nature of vaginal discharge, a condition similar to premenstrual syndrome, an increase in the size of fibroids, benign mammary glands, pruritus, skin rash, chloasma, erythema multiforme, erythema nodosum, migraine, anxiety, increased fatigue, insomnia, heart palpitations, edema, varicose veins, muscle intolerance contact lenses.

Interaction of drospirenone with other substances

Long-term therapy with drugs that induce liver enzymes (including barbiturates, hydantoin derivatives, primidone, rifampicin, carbamazepine, oxcarbazepine, felbamate, topiramate, griseofulvin) can increase the clearance of sex hormones and reduce their effectiveness. Drospirenone can reduce the effectiveness of anabolic steroids and drugs that stimulate uterine smooth muscle.

Overdose

In case of an overdose of drospirenone, nausea, vomiting, and vaginal bleeding are possible. Symptomatic treatment is necessary, there is no antidote.

Trade names of drugs with active ingredient drospirenone

Used in combination preparations:
Drospirenone + Estradiol: Angelique®;
Drospirenone + Ethinylestradiol: Dailla®, Jess®, Midiana®, Yarina®;
Drospirenone + Ethinylestradiol + [Calcium levomefolinate]: Jess® Plus, Yarina® Plus;
Ethinylestradiol + Drospirenone: Dimia®, Yarina®.

Clinical and pharmacological group: & nbsp

Part of preparations

ATX:

G.03.A.A.12 Drospirenone and ethinyl estradiol

Pharmacodynamics:

Combined oral contraceptive containing drospirenone. At a therapeutic dose, drospirenone also has antiandrogenic and weak antimineralocorticoid properties. It lacks any estrogenic, glucocorticoid and antiglucocorticoid activity. This provides drospirenone with a pharmacological profile similar to natural progesterone.

There is evidence of a reduction in the risk of developing endometrial and ovarian cancer with the use of combined oral contraceptives.

Pharmacokinetics:

Drospirenone

Suction... After oral administration, drospirenone is rapidly 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, C max in serum is reached after 1 hour and is about 22 ng / ml. After this, there is a two-phase decrease in the concentration of drospirenone in the serum with a final half-life of about 35-39 hours. Drospirenone binds to albumin and does not bind to globulin that binds sex steroids and corticoid-binding globulin; about 3-5% - free fraction.

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

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

Withdrawal... The clearance of drospirenone from serum is 1.2-1.5 ml / min / kg. Some of the dose received 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; the half-life is about 40 hours.

Ethinylestradiol

Suction. When taken orally, it is absorbed quickly and completely. C max in serum - about 33 pkg / ml, is achieved within 1-2 hours after a single oral administration. The absolute bioavailability as a result of presystemic conjugation and first-pass metabolism is approximately 60%. Concomitant food intake reduced the bioavailability of ethinyl estradiol in about 25% of the patients surveyed; the others did not.

Distribution. Serum concentrations of ethinyl estradiol decrease in two phases, in the terminal distribution phase the elimination half-life is approximately 24 hours.It binds well but not specifically to serum albumin (approximately 98.5%) and induces an increase in serum concentrations sex steroid binding globulin... V d - about 5 l / kg.

Metabolism. Ethinylestradiol is a substrate for presystemic conjugation in the mucous membrane of the small intestine and in the liver. is primarily metabolized by aromatic hydroxylation, with the formation of a wide range of hydroxylated and methylated metabolites, which are present both in free form and in the form of conjugates with glucuronic acid. The renal clearance of ethinylestradiol metabolites is approximately 5 ml / min / kg.

Excretion. Unchanged is practically not excreted from the body. Ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6. The half-life of metabolites is about 24 hours.

C ss occurs in the second half of the treatment cycle, and the serum concentration of ethinyl estradiol increases 2-2.3 times.

Special patient groups

In case of impaired renal function. C ss of drospirenone in blood plasma in women with mild renal insufficiency (creatinine clearance - 50-80 ml / min) was comparable to those in women with normal renal function (creatinine clearance> 80 ml / min). In women with moderate renal insufficiency (creatinine clearance from 30 ml / min to 50 ml / min), the concentration of drospirenone in blood plasma was on average 37% higher than in women with normal renal function. Drospirenone was well tolerated in all groups. Taking drospirenone did not have a clinically significant effect on the serum potassium content. Pharmacokinetics in severe renal failure have not been studied.

In case of impaired liver function. Drospirenone is well tolerated by patients with mild to moderate hepatic impairment (Child-Pugh class B). Pharmacokinetics in severe hepatic impairment have not been studied.

Indications:

Contraception.

XXI.Z30-Z39.Z30.0 General advice and advice on contraception

XXI.Z30-Z39.Z30 Monitoring contraceptive use

Contraindications:

The drug, like other combined oral contraceptives, is contraindicated in any of the conditions listed below:

Hypersensitivity to the drug or any of the components of the drug;

Thrombosis (arterial and venous) and thromboembolism currently or in history (including thrombosis, deep vein thrombophlebitis, pulmonary embolism, myocardial infarction, stroke, cerebrovascular disorders). Conditions preceding thrombosis (including transient ischemic attacks, angina pectoris), currently or in history;

Multiple or severe risk factors for venous or arterial thrombosis, including complicated lesions of the valvular apparatus of the heart, atrial fibrillation, diseases of the vessels of the brain or coronary arteries; uncontrolled arterial hypertension, volumetric surgery with prolonged immobilization, smoking over the age of 35, obesity with a body mass index> 30;

Hereditary or acquired predisposition to venous or arterial thrombosis, for example, resistance to activated protein C, antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia, and anti-phospholipid antibodies (presence of antibodies to phospholipids - antibodies to cardiolipin, lupus); anticoagulant

Pregnancy and suspicion of it;

Lactation period;

Pancreatitis with severe hypertriglyceridemia at present or in history;

Existing (or history) severe liver disease, provided that liver function is not currently normalized;

Severe chronic or acute renal failure;

A liver tumor (benign or malignant), currently or in history;

Hormone-dependent malignant neoplasms of the genitals or mammary gland, currently or in history;

Vaginal bleeding of unknown origin;

Migraine with a history of focal neurological symptoms;

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption, Lapp lactase deficiency.

Carefully:

Risk factors for the development of thrombosis and thromboembolism are smoking under the age of 35, obesity, dyslipoproteinemia, controlled arterial hypertension, migraine without focal neurological symptoms, uncomplicated heart valve defects, hereditary predisposition to thrombosis (thrombosis, myocardial infarction or cerebrovascular accident) any of the next of kin); diseases in which peripheral circulation disorders may occur (diabetes mellitus without vascular complications, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia, phlebitis of superficial veins); hereditary angioedema; hypertriglyceridemia; severe liver disease (before normalization of liver function tests); diseases that first appeared or worsened during pregnancy or against the background of previous use of sex hormones (including jaundice and / or itching associated with cholestasis, cholelithiasis, otosclerosis with hearing impairment, porphyria, herpes during pregnancy in history, chorea Sidengama); chloasma; postpartum period.

Pregnancy and lactation:

The drug is contraindicated during pregnancy. If pregnancy occurs while using the drug, it should be stopped immediately. Extensive epidemiological studies have found neither an increased risk of birth defects in children born to women who took before pregnancy, nor teratogenic effects when taken unintentionally during pregnancy. According to the data of preclinical studies, it is impossible to exclude undesirable effects that affect the course of pregnancy and fetal development, due to the hormonal action of the active components.

The drug can affect lactation: reduce the amount of milk and change its composition. Small amounts of contraceptive steroids and / or their metabolites may be excreted in milk during administration combined oral contraceptives... These amounts can affect the baby. The use of the drug during breastfeeding is contraindicated.

Method of administration and dosage:

Every day, at about the same time, with a little water, in the order indicated on the blister pack. The tablets are taken continuously for 28 days, 1 tablet per day. Taking pills from the next package begins after taking the last tablet from the previous package. Withdrawal bleeding usually begins 2–3 days after starting the placebo pill (last row) and does not necessarily end by the start of the next pack.

The procedure for taking the drug

Hormonal contraceptives have not been used in the last month. Taking the drug begins on the 1st day of the menstrual cycle (that is, on the 1st day of menstrual bleeding). It is also possible to start taking the pills on the 2-5th day of the menstrual cycle, in this case, additional use of the barrier method of contraception is required during the first 7 days of taking the pills from the first package.

Switching from other combined contraceptives (pill, vaginal ring, or transdermal patch). It is necessary to start taking the drug the next day after taking the last inactive tablet (for drugs containing 28 tablets) or the next day after taking the last active tablet from the previous package (possibly the next day after the end of the usual 7-day break) - for drugs, containing 21 tablets per pack. If a woman uses a vaginal ring or a transdermal patch, it is preferable to start taking the drug on the day they are removed or, at the latest, on the day when a new ring or patch is planned to be inserted.

Switching from contraceptives containing only progestogens (mini-pills, injections, implants), or from an intrauterine system that secretes progestogens. A woman can switch from taking a mini-pill to taking a drug on any day (from an implant or from the intrauterine system - on the day of their removal, from injectable forms of drugs - on the day when the next injection was to be made), but in all cases it is necessary to use additionally a barrier method of contraception during the first 7 days of taking the pills.

After an abortion in the first trimester of pregnancy. Taking the drug can be started as directed by a doctor on the day of termination of pregnancy. In this case, the woman does not need to take additional contraceptive measures.

After childbirth or abortion in the second trimester of pregnancy. A woman is recommended to start taking the drug on the 21-28th day after childbirth (provided that she is not breastfeeding) or an abortion in the second trimester of pregnancy. If the reception is started later, the woman should use an additional barrier method of contraception within the first 7 days after starting the drug. With the resumption of sexual activity (before the start of taking the drug), pregnancy should be excluded.

Taking missed pills

Skipping placebo pills from the last (4th) row of the blister can be ignored. However, they should be discarded to avoid unintentionally prolonging the placebo phase. The instructions below only apply to missed tablets containing active ingredients.

If the delay in taking the pill is less than 12 hours, contraceptive protection is not reduced. The woman should take the missed pill as soon as possible (as soon as she remembers), and the next pill at the usual time.

If the delay exceeds 12 hours, contraceptive protection may be reduced. In this case, you can be guided by two basic rules:

1.Pill-taking should never be interrupted for more than 7 days.

2.To achieve adequate suppression of the hypothalamic-pituitary-ovarian system, 7 days of continuous pill intake are required.

In accordance with this, women can be given the following recommendations:

Days 1-7. A woman should take the missed pill as soon as she remembers it, even if that means taking two pills at the same time. Then she should take the pills at the usual time. In addition, a barrier method, such as a condom, should be used for the next 7 days. If intercourse has occurred in the previous 7 days, the possibility of pregnancy should be taken into account. The more tablets are missed and the closer this pass is to the 7-day break in taking the drug, the higher the risk of pregnancy.

Days 8-14. A woman should take the missed pill as soon as she remembers it, even if it means taking two pills at the same time. Then she should take the pills at the usual time. If during the 7 days preceding the first missed pill, the woman took the pills as expected, there is no need for additional contraceptive measures. However, if she missed more than 1 tablet, an additional method of contraception (barrier, such as a condom) is needed for 7 days.

Days 15-24. The reliability of the method inevitably diminishes as the placebo pill phase approaches. However, adjusting the pill regimen can still help prevent pregnancy. When performing one of the two schemes described below, and if in the previous 7 days before skipping the pill, the woman adhered to the regimen of taking the drug, there will be no need to use additional contraceptive measures. If this is not the case, she should follow the first of the two regimens and use additional precautions for the next 7 days.

1. A woman should take the last missed pill as soon as she remembers it, even if that means taking two pills at the same time. She should then take the pills at the usual time until the active pills run out. 4 placebo tablets from the last row should not be taken, you should immediately start taking the tablets from the next blister pack. Most likely, withdrawal bleeding will not occur until the end of the second pack, but spotting spotting or withdrawal bleeding may occur on the days of taking the drug from the second pack.

2. The woman can also stop taking active tablets from the started package. Instead, she must take the last row of placebo pills for 4 days, including skipped days, and then start taking the next pack of pills. If a woman misses a pill and does not subsequently experience withdrawal bleeding in the placebo pill phase, pregnancy should be considered.

Use of the drug for gastrointestinal upset

In the case of severe gastrointestinal disorders (for example, vomiting or diarrhea), the absorption of the drug will be incomplete, and additional contraceptive measures will be required. If vomiting occurs within 3-4 hours after taking the active pill, it is necessary to take a new (replacement) pill as soon as possible. If possible, the next tablet should be taken within 12 hours of the usual tablet-taking time. If more than 12 hours have passed, it is recommended to act as directed when skipping tablets. If the woman does not want to change her usual pill regimen, she must take an additional pill from a different package.

Delaying menstrual bleeding with withdrawal

To delay bleeding, a woman should skip taking placebo pills from the started package and start taking pills from a new package. The delay can be extended until the active tablets in the second pack run out. During a delay, a woman may experience acyclic profuse or spotting bleeding from the vagina. Regular use of the drug is resumed after the placebo phase. To shift the bleeding to another day of the week, it is recommended to shorten the upcoming phase of taking the placebo tablets by the desired number of days. With a shortening of the cycle, it is more likely that the woman will not have menstrual withdrawal bleeding, but will have acyclic profuse or spotting bleeding from the vagina when taking the next pack (just like when lengthening the cycle).

Side effects:

The most commonly reported adverse reactions to the drug are nausea and breast pain. They occurred in more than 6% of women using this drug.

Arterial and venous thromboembolism are serious adverse reactions.

Listed below are adverse reactions with a very rare incidence or with delayed symptoms, which are believed to be associated with the use of drugs from the group of combined oral contraceptives.

The frequency of diagnosing breast cancer in women taking combined oral contraceptives is slightly increased. Due to the fact that breast cancer is rare in women under 40, the increase in the number of breast cancer diagnoses in women taking combined oral contraceptives is insignificant in relation to the overall risk of this disease.

Liver tumors (benign and malignant).

Other conditions:

Erythema nodosum;

Women with hypertriglyceridemia (increased risk of pancreatitis while taking combined oral contraceptives);

Increased blood pressure;

Conditions that develop or worsen while taking combined oral contraceptives, but their relationship with taking the drug has not been proven (jaundice and / or pruritus associated with cholestasis; formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Sydenham's chorea ; herpes during pregnancy; hearing loss associated with otosclerosis);

In women with hereditary angioedema, estrogen intake can cause or worsen its symptoms;

Liver dysfunction;

Impaired glucose tolerance or impact on insulin resistance;

Crohn's disease, ulcerative colitis;

Chloasma;

Hypersensitivity (including symptoms such as rash, hives).

Overdose:

Cases of drug overdose have not yet been described.

Based on general application experience combined oral contraceptives potential symptoms of an overdose may be: nausea, vomiting, mild vaginal bleeding.

Treatment: no antidotes. Further treatment should be symptomatic.

Interaction:

Interaction between oral contraceptives and other medicinal products can lead to acyclic bleeding and / or contraceptive ineffectiveness. The interactions described below are reflected in the scientific literature.

The mechanism of interaction with hydantoin, barbiturates, primidone, carbamazepine and rifampicin; oxcarbazepine, topiramate, felbamate, ritonavir, griseofulvin and St. John's wort preparations is based on the ability of these active substances to induce liver microsomal enzymes. The maximum induction of liver microsomal enzymes is not achieved within 2-3 weeks, but after that it persists for at least 4 weeks after discontinuation of drug therapy.

Contraceptive ineffectiveness has also been reported with antibiotics such as ampicillin and tetracycline. The mechanism of this phenomenon is unclear. Women with short-term treatment (up to one week) with any of the above groups of drugs or mono-drugs should temporarily use (during the period of simultaneous administration of other drugs and for another 7 days after its end), in addition to combined oral contraceptives, barrier methods of contraception.

Women receiving rifampicin therapy other than taking combined oral contraceptives must use a barrier method of contraception and continue using it for 28 days after stopping rifampicin treatment. If taking concomitant medications lasts longer than the expiration date of the active tablets in the package, you should stop taking the inactive tablets and immediately start taking the tablets from the next package.

If a woman is constantly taking inducers of liver microsomal enzymes, she should use other reliable non-hormonal methods of contraception.

The main metabolites of drospirenone in human plasma are formed without the participation of the cytochrome P450 system. Inhibitors of cytochrome P450 are therefore unlikely to interfere with the metabolism of drospirenone.

Oral contraceptives can affect the metabolism of some other active ingredients. Accordingly, the concentrations of these substances in blood plasma or tissues can either increase (for example) or decrease (for example). Based on inhibition studies in vitro and interactions in vivo in female volunteers who took, and as a substrate, the effect of drospirenone at a dose of 3 mg on the metabolism of other active substances is unlikely.

In patients without renal failure, concomitant administration of drospirenone and ACE inhibitors or non-steroidal anti-inflammatory drugs does not significantly affect the serum potassium content. Nevertheless, the simultaneous use of the drug with aldosterone antagonists or potassium-sparing diuretics has not been studied. In this case, during the first cycle of treatment, it is necessary to monitor the concentration of serum potassium.

Special instructions:

If there are any of the conditions / risk factors listed below, the benefits of taking combined oral contraceptives should be assessed individually for each woman and discussed with her before starting use. In case of an exacerbation of an undesirable phenomenon or in the event of any of these conditions or risk factors, a woman should contact her doctor. The doctor must decide whether to interrupt the appointment combined oral contraceptives.

Circulatory disorders

Reception of any combined oral contraceptive increases the risk of venous thromboembolism. The increased risk of venous thromboembolism is most pronounced in the first year of use by a woman. combined oral contraceptives.

Epidemiological studies have shown that the incidence of venous thromboembolism in women with no risk factors who took low doses of estrogen (< 0,05 мг этинилэстрадиола) в составе combined oral contraceptives, is approximately 20 cases per 100,000 women-years (for levonorgestrel-releasing combined oral contraceptives second generation) or 40 cases per 100,000 women-years (for desogestrel / gestodene-containing combined oral contraceptives third generation). In women who do not use combined oral contraceptives, 5-10 venous thromboembolism occurs and 60 pregnancies per 100,000 women-years. Venous thromboembolism is fatal in 1–2% of cases.

Data from a large, prospective, 3-pronged study showed that the incidence of venous thromboembolism in women with or without other risk factors for venous thromboembolism, who used a combination of ethinylestradiol and drospirenone, 0.03 + 3 mg, coincides with the incidence of venous thromboembolism in women who used levonorgestrel. oral contraceptives and others combined oral contraceptives... The degree of risk of venous thromboembolism while taking the drug is currently not established.

Epidemiological studies have also shown a link between intake combined oral contraceptives with an increased risk of arterial thromboembolism (myocardial infarction, transient ischemic disorders).

Very rarely, women taking oral contraceptives have thrombosis of other blood vessels, such as veins and arteries in the liver, mesentery, kidney, brain, or retina. There is no consensus regarding the relationship of these phenomena with the use of hormonal contraceptives.

Symptoms of venous or arterial thrombotic / thromboembolic events or acute cerebrovascular accidents:

Unusual one-sided pain and / or swelling of the lower extremities;

Sudden severe chest pain, whether it radiates to the left arm or not;

Sudden shortness of breath;

Sudden onset of cough;

Any unusual severe, prolonged headache;

Sudden partial or complete loss of vision;

Diplopia;

Impaired speech or aphasia;

Vertigo;

Collapse with or without partial seizures;

Weakness or very noticeable numbness that suddenly affects one side or one part of the body;

Movement disorders;

Sharp abdomen.

Before you start combined oral contraceptives a woman should consult a specialist. Risk of venous thromboembolic disorders when taken combined oral contraceptives increases:

With increasing age;

Hereditary predisposition;

Prolonged immobilization, extended surgery, any surgery on the lower extremities or major trauma. In such situations, it is recommended to stop taking the drug (in the case of planned surgery, at least 4 weeks) and not resume until two weeks after the full recovery of mobility. If the drug has not been discontinued early, anticoagulant treatment should be considered;

There is no consensus on the possible role of varicose veins and superficial thrombophlebitis in the onset or exacerbation of venous thrombosis.

Risk of arterial thromboembolic complications or acute cerebrovascular accident when taken combined oral contraceptives increases with:

Increasing age;

Smoking (women over 35 are strongly advised to quit smoking if they want to take combined oral contraceptives);

Dyslipoproteinemia;

Arterial hypertension;

Migraines without focal neurological symptoms;

Obesity (body mass index over 30);

Hereditary predisposition (arterial thromboembolism ever in siblings or parents at a relatively early age). If a hereditary predisposition is possible, the woman should consult with a specialist before taking combined oral contraceptives;

Damage to the valves of the heart;

Atrial fibrillation.

Having one major risk factor for vein disease or multiple risk factors for arterial disease may also be a contraindication. Anticoagulant therapy should also be considered. Women receiving combined oral contraceptives should be properly instructed on the need to inform the attending physician in case of suspicion of symptoms of thrombosis. If thrombosis is suspected or confirmed, taking combined oral contraceptives should stop. It is necessary to start an adequate alternative contraception due to the teratogenicity of anticoagulant therapy with indirect anticoagulants - coumarin derivatives.

Consideration should be given to the increased risk of thromboembolism in the postpartum period.

Other medical conditions associated with adverse vascular events include diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis), and sickle cell disease.

Increased frequency or severity of migraines while taking combined oral contraceptives may be an indication for their immediate cancellation.

Tumors

The most significant risk factor for cervical cancer is human papillomavirus infection. Some epidemiological studies have reported an increased risk of cervical cancer with long-term use combined oral contraceptives however, conflicting views persist as to the extent to which these findings are related to co-factors, such as testing for cervical cancer or the use of barrier methods of contraception.

A meta-analysis of 54 epidemiological studies found a small increase in the relative risk of breast cancer in women who are currently taking combined oral contraceptives... The risk gradually decreases over 10 years after you stop taking combined oral contraceptives... Since breast cancer rarely develops in women under 40 years of age, an increase in the number of diagnosed cases of breast cancer in those using combined oral contraceptives has little effect on the overall likelihood of breast cancer. These studies did not find sufficient evidence for a causal relationship. The increased risk may be due to the earlier diagnosis of breast cancer in those using combined oral contraceptives, biological action combined oral contraceptives or a combination of both. Diagnosed breast cancer in women who have ever taken combined oral contraceptives, was clinically less severe due to the early diagnosis of the disease.

Rarely in women taking combined oral contraceptives, there were benign liver tumors and, even more rarely, malignant liver tumors. In some cases, these tumors were life-threatening (due to intra-abdominal bleeding). This should be taken into account when making a differential diagnosis in case of severe pain in the abdomen, enlarged liver, or signs of intra-abdominal bleeding.

Other

The progestogen component of the drug is an aldosterone antagonist that retains potassium in the body. In most cases, an increase in potassium is not expected. However, in a clinical study in some patients with mild to moderate kidney disease who took potassium-sparing drugs, the serum potassium content slightly increases while taking drospirenone. Therefore, it is recommended to monitor serum potassium during the first cycle of treatment in patients with renal insufficiency in whom the serum potassium concentration was at the upper normal limit before treatment, and especially while taking potassium-sparing drugs. In women with hypertriglyceridemia or a hereditary predisposition to it, the risk of pancreatitis may be increased when taking combined oral contraceptives... Although a small increase in blood pressure has been observed in many women, a clinically significant increase was rare. Only in these rare cases is it justified to immediately stop taking combined oral contraceptives... If when receiving combined oral contraceptives in patients with concomitant arterial hypertension, blood pressure constantly increases or significantly increased pressure cannot be corrected with antihypertensive drugs, intake combined oral contraceptives should stop. After normalizing blood pressure with antihypertensive drugs, taking combined oral contraceptives can be resumed.

The following diseases appeared or worsened during pregnancy and when taking combined oral contraceptives: jaundice and / or pruritus associated with cholestasis, gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; rheumatic chorea (Sydenham's chorea); herpes during pregnancy; otosclerosis with hearing loss. However, evidence of their relationship with the reception combined oral contraceptives unconvincing.

In women with hereditary angioedema, exogenous estrogens can induce or exacerbate symptoms of edema.

Acute or chronic liver disease may be an indication for discontinuation combined oral contraceptives before normalization of liver function indicators. Recurrence of cholestatic jaundice and / or itching associated with cholestasis, which developed during a previous pregnancy or with earlier use of sex hormones, serve as an indication for discontinuation combined oral contraceptives.

Though combined oral contraceptives may affect peripheral insulin resistance and glucose tolerance, change in the treatment regimen in patients with diabetes mellitus while taking combined oral contraceptives low in hormones (containing< 0,05 мг этинилэстрадиола) не показано. Однако следует внимательно наблюдать женщин с сахарным диабетом, особенно на ранних стадиях приема combined oral contraceptives.

During the reception combined oral contraceptives exacerbation of endogenous depression, epilepsy, Crohn's disease and ulcerative colitis was observed.

Chloasma may occur from time to time, especially in women who have had a history of chloasma during pregnancy. Women with a tendency to chloasma should avoid exposure to the sun or ultraviolet light when taking combined oral contraceptives.

Coated tablets contain 48.53 mg of lactose monohydrate, placebo tablets contain 37.26 mg of anhydrous lactose per tablet. Patients with rare hereditary diseases (such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption) who are on a lactose-free diet should not take this drug.

Women who are allergic to soy lecithin may experience allergic reactions.

The effectiveness and safety of the drug as a contraceptive have been studied in women of reproductive age. It is assumed that in the post-pubertal period up to 18 years, the efficacy and safety of the drug are similar to those in women after 18 years.

Medical examinations

Before starting or re-using the drug, a complete medical history (including family history) should be collected and pregnancy should be ruled out. It is necessary to measure blood pressure, conduct a medical examination, guided by contraindications and precautions. The woman needs to be reminded of the need to carefully read the instructions for use and adhere to the recommendations indicated in it. The frequency and content of the survey should be based on existing practice guidelines. The frequency of medical examinations is individual for each woman, but should be carried out at least once every 6 months.

Decreased efficiency

Efficiency combined oral contraceptives may decrease, for example, when you skip taking pills, gastrointestinal disorders while taking the pills, or while taking other medications.

Insufficient cycle control

As with others combined oral contraceptives, a woman may experience acyclic bleeding (spotting or withdrawal bleeding), especially in the first months of admission. Therefore, any irregular bleeding should be assessed after a three-month adaptation period.

Instructions

A substance called drospirenone is a chemical compound belonging to the progestogens used to create hormonal contraceptive drugs. This chemical compound can only be used in combination with estrogens, and cannot be prescribed in its pure form for contraceptive purposes.

In addition to contraceptive activity, drospirenone in contraceptives has a therapeutic effect in diseases such as seborrhea and acne.

Properties and differences from other hormones

The distinctive properties of the hormone drospirenone are that this chemical compound has a therapeutic effect in the so-called androgen-dependent diseases. Such diseases include oily seborrhea and acne. In addition, this substance helps to remove excess interstitial fluid from the body, thereby eliminating edema, normalizing blood pressure indicators, reducing body weight and relieving pain in the mammary glands.

Women with severe premenstrual syndrome know firsthand about each of these symptoms. Also, throughout the hormone replacement therapy, drospirenone tablets reduce the level of low-density lipoproteins in the female body and increase the triglyceride content.

Important! Oral contraceptives based on drospirenone, during menopause, significantly reduce the likelihood of developing cancer and endometrial hyperplasia, as well as colon cancer in women.

Drospirenone or Gestodene

Both chemical compounds belong to the latest generation of synthetic hormones. Gestodene and drospirenone have a high level of efficacy and a minimal risk of adverse reactions. If we talk about the differences between the hormone drospirenone and the hormone gestodene, then drugs based on gestodene are more often prescribed to patients with pronounced signs of dysmenorrhea in order to restore the regularity of the menstrual cycle. It is advisable to prescribe drugs based on drospirenone in order to protect against the onset of unwanted pregnancy, as well as to reduce the severity of premenstrual syndrome. It is important to remember that therapy with drospirenone drugs can cause hyperkalemia and thromboembolic complications.

Drospirenone or dienogest

These biologically active compounds belong to the category of progestins that are part of combined oral contraceptives. The key difference between the hormone drospirenone and dienogest is that dienogest combines not only the effect of progesterone, but also the effect of testosterone. Also, dienogest is the only progesterone analog capable of suppressing the effect of 17-beta-estradiol at the peripheral level, without significantly affecting the level of follicle-stimulating and luteinizing hormones.

Drospirenone or desogestrel

Both biologically active compounds are new generation hormonal contraceptives. By analogy with gestodene, desogestrel is used to eliminate the clinical signs of dysmenorrhea.

It cannot be said unequivocally that drospirenone or the hormone desogestrel is better, since both substances differ in contraceptive and therapeutic efficacy.

The only difference is that, compared to drospirenone, desogestrel does not increase the risk of gaining extra pounds.

Dosage and rules for taking the hormone

Contraceptive contraceptives with drospirenone can be prescribed for taking according to various schemes, which are selected by the attending physician on an individual basis. As a rule, the standard regimen for taking such drugs requires the use of a contraceptive 1 tablet, 1 time per day, at a strictly designated time. Regardless of the name, preparations based on drospirenone are dispensed in pharmacies only with medical prescriptions.

Drug interactions

Contraceptives based on drospirenone significantly inhibit the effects of uterotonics and anabolic steroids.

Also, drospirenone negatively affects the level of effectiveness of drugs such as Primidone, Oscarbazepine, Carbamazepine, barbiturate derivatives, Rifampicin, Felbamat.

Contraceptives with drospirenone

All contraceptive drugs with drospirenone are combined into a general list, which includes the following names:

Each of the above drugs contains a combination of drospirenone and ethinyl estradiol. The drugs Jess Plus and Yarina Plus, in addition to these components, include calcium levomefolicate.

Indications

Given the anti-mineralocorticoid, antigonadotropic, antiandrogenic and gestagenic properties of drospirenone, this type of contraception can be prescribed if there are such indications:

Folate deficiency.
Oily seborrhea and acne.
As part of the complex therapy of postmenopausal osteoporosis.
Severe manifestations of premenstrual syndrome.
Chronic stagnation of fluid in the body.
Pronounced manifestations of menopause.
To protect against unwanted pregnancy.

Contraindications

Hormonal contraceptives containing drospirenone cannot be used if there are such contraindications:

Side effects of contraceptives with drospirenone

Taking a contraceptive consisting of drospirenone and estradiol, you can encounter a list of such adverse reactions from the body:

Headache and dizziness.
Skin and systemic allergic reactions.
Bloody discharge from the genital tract in the intermenstrual period.
Chloasma.
Alopecia.
Varicose veins.
Increase or decrease in body weight.
Insomnia, drowsiness, depressive disorders and apathy.
Formation of stones in the gallbladder.
Nausea and vomiting.
Decreased visual acuity.
Galactorrhea.

If the contraceptive dosing regimen is violated, complications such as uterine bleeding, vomiting and nausea may occur.

Important notes

Before starting a course of therapy with contraceptive pills containing drospirenone, you should pay attention to the following recommendations:

In addition, the pharmacological effect of biphasic hormonal COCs based on drospirenone is significantly reduced when interacting with antibacterial drugs of the penicillin and tetracycline series.

In order to avoid the development of serious complications, the choice of the names of contraceptives and their dosages should be performed by the attending physician gynecologist on an individual basis.

Chemical properties

Drospirenone - what is it? This substance belongs to the group of oral contraceptives. Most often it is used in combination with other hormones. The medicine can have a therapeutic effect on androgen-dependent diseases .

Drospirenone - what is this hormone? Drospirenone is a synthetic hormone with properties close to natural progesterone , derivative spironolactone ... Molecular weight of a chemical compound = 366.5 grams per mole. The density of the substance = 1.26 grams per cm3, the melting point is approximately 200 degrees Celsius.

Drospirenone on Wikipedia is mentioned in articles on hormonal contraception and the effect of drugs on human sexual function.

pharmachologic effect

Gestagenic , antigonadotropic , antimineralocorticoid , antiandrogenic .

Pharmacodynamics and pharmacokinetics

Due to the fact that this substance has pronounced antiandrogenic properties, it has a beneficial effect on the flow androgen-dependent diseases , such as acne , alopecia and seborrhea ... Drospirenone stimulates excretion sodium ions and other fluids from the body, as a result of which blood pressure normalizes, swelling and soreness in the mammary glands decreases, and body weight decreases.

Clinical studies have shown that after 4 months of using the drug, the systolic pressure decreases by an average of 2-4 mm Hg, and the diastolic pressure - by 1-3 mm Hg. Art., the weight is reduced by 1-2 kg. In women during menopause, the likelihood of developing colon cancer , hyperplasia and endometrial cancer .

The synthetic hormone does not possess estrogenic , androgenic and glucocorticosteroid activity , does not change insulin resistance and the body's response to glucose ... During treatment with the drug, the patient's level of cholesterol in blood and LDL , the concentration increases slightly triglycerides .

After taking tablets containing drospirenone, the active substance is quickly and almost completely absorbed by the body. The biological availability of the substance is about 75-85%. Parallel food intake has no effect on pharmacokinetics of the drug ... The concentration of the drug in the blood plasma decreases in two phases, the half-life is 35-40 hours. With a systematic, daily intake, the equilibrium concentration of the agent is observed after 10 days.

The agent has a high degree of binding to plasma proteins (serum albumen ) - about 95-97%. The main metabolites of the hormone are formed without affecting cytochrome P450 system ... The drug is excreted in the form of metabolites with feces and urine, a small part is excreted unchanged.

Indications for use

as part of complex therapy for the prevention of postmenopausal osteoporosis ;
if necessary, hormonal contraception in women with deficiency folate or fluid retention in the body;
as a hormone replacement treatment for menopausal disorders to eliminate tides , sweating and other vasomotor symptoms;
with involutional changes in the genitourinary tract in women with an unremoved uterus;
in combination with other synthetic hormones for contraception;
for contraception in severe PMS ;
in severe and moderate form eels for contraception.

Contraindications

patients with allergies on Drospirenone;
at porphyrias ;
persons with a tendency to education blood clots ;
with severe liver failure;
during lactation;
at thromboembolism or thrombophlebitis in severe form;
if the patient has vaginal bleeding of unknown origin;
at breast cancer or other genital organs;
pregnant women.

Side effects

During treatment with the drug, the following may develop:

allergic reactions of varying severity, dizziness;
thromboembolism pulmonary artery or cerebral vessels;
thrombophlebitis , blood clots in the veins of the retina;
arterial hypertension , swelling, headaches;
calculous cholecystitis ;
drowsiness ,apathy , depressive states ;
decreased visual acuity, vomiting, growth or weight loss;
galactorrhea , nausea, hirsutism ;
alopecia , painful sensations and swelling of the mammary glands;
bloody or unusual vaginal discharge;
decreased sex drive, chloasma ;
insomnia , lowering the convulsive threshold, varicose veins .

Drospirenone, application instruction (Way and dosage)

Depending on the combination in which this hormone is in the pill, it is prescribed according to various treatment regimens. According to the instructions for Drospirenone in tablets, it is taken once a day at the same time.

Therapy begins after the previous hormonal agent has been canceled, in accordance with the doctor's recommendations. The duration of treatment is also set on an individual basis and often depends on the effectiveness of the therapy.

Overdose

In case of an overdose, nausea, vaginal bleeding, and vomiting may occur. Due to the fact that the drug has no specific antidote , then the treatment is symptomatic.

Interaction

With long-term treatment with drugs that induce liver enzymes ( barbiturates , carbamazepine , oscarbazepine , hydantoin derivatives , primidone , rifampicin , topiramate , griseofulvin , felbamat ) increases the clearance of a given substance and reduces their effectiveness. As a rule, this effect manifests itself in 2-3 weeks after the start of therapy and persists for a month after stopping the drug intake.

The medicine reduces the effectiveness of drugs that stimulate the smooth muscles of the uterus and anabolic steroids .

Terms of sale

special instructions

A number of uncontrolled randomized trials have shown an increased risk of developing venous thromboembolism during treatment with the agent. It is necessary to prescribe the drug with extreme caution to women who have a predisposition to the occurrence of venous thromboembolism (heredity, obesity , age). It is necessary to carefully correlate the indicators "risk - benefit".

Rarely, during treatment, there were benign, and even less often - malignant liver tumors ... If the patient has any signs of this disease, pain in the area under the ribs, enlargement of the organ and intra-abdominal bleeding, then the treatment must be interrupted.

In patients with moderate to mild renal impairment, intake of this synthetic hormone may affect concentration potassium ions in the blood serum. There is a small risk of developing hyperkalemia , especially if the patient additionally takes potassium-sparing drugs .

Before starting treatment with the drug, it is recommended to undergo a gynecological and general medical examination, it is recommended to pay special attention cytological examination of church mucus and mammary glands, blood coagulation system, exclude pregnancy. During therapy, these studies should be repeated periodically.

With antibiotics

It is likely that some antibiotics can interfere with the metabolism of the drug.

Instructions from Listel.Ru tablets

Only the most current official instructions for the use of medicines! Instructions for medicines on our website are published unchanged, in which they are attached to the medicines.

PRESCRIPTION MEDICINES ARE APPOINTED TO THE PATIENT BY A DOCTOR ONLY. THIS INSTRUCTION IS FOR MEDICAL PROVIDERS ONLY.

Description of the active substance Drospirenone / Drospirenone.

Formula: C24H30O3, chemical name: (6R, 7R, 8R, 9S, 10R, 13S, 14S, 15S, 16S, 17S) -1,3 ′, 4 ′, 6.6a, 7,8,9,10,11,12 , 13,14,15,15a, 16-hexadecahydro-10,13-dimethylspiro-cyclopenta [a] phenanthrine-17.2 ′ (5H) -furan] -3.5 ′ (2H) -dione).
Pharmacological group: hormones and their antagonists / estrogens, gestagens; their homologues and antagonists.
Pharmachologic effect: gestagenic, antiandrogenic, antigonadotropic, antimineralocorticoid.

Pharmacological properties

Indications

Drospirenone dosage and administration

The method of administration and doses are set individually by the doctor, depending on the indications and the dosage form used.

Contraindications for use

Restrictions on use

Application during pregnancy and lactation

Drospirenone is contraindicated in pregnancy and lactation.

Side effects of drospirenone

Interaction of drospirenone with other substances

Overdose

In case of an overdose of drospirenone, nausea, vomiting, and vaginal bleeding are possible. Symptomatic treatment is necessary, there is no antidote.

Trade names of drugs with active ingredient drospirenone

Pharmaceutical group:

Reviews and comments

Good evening! I read that

Inna Sun, 21/09/2014 - 23:12

Good evening! I read that the drug JES is effectively used to treat acne in adolescence. I would like to know the dosage and contraindications. A 14-year-old girl has no menstrual cycle, the rash is very profuse, is it possible to use the drug?

It's too early for the girl Jess,

It's too early for Jess's girl, it is advisable to wait for a regular cycle.

Drospirenone is a hormone included in the group of oral contraceptives. On its basis, a large number of contraceptive drugs are manufactured, as well as medicines 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 belongs to synthetic hormones 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 temperature - 200 degrees Celsius;
density - 1.26 g / cubic centimeter.

The hormone is able to affect the sexual function of a person, as well as to have an antigonadotropic, gestagenic, antiandrogenic and antimineralocorticoid effect.

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

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

Yarina. This medication is available in the form of film-coated tablets. It is only used to prevent unwanted pregnancies. The drug has many contraindications, so it should be taken with extreme caution. At the same time, it is important to follow all the prescriptions of doctors and limit the number of pills taken.
Angelique. This medicine is also available in film-coated tablets, which may vary in color. It is used for the prevention of postmenopausal osteoporosis, as well as for menopausal disorders in women with an unremoved uterus. The drug practically does not have a negative effect on the body, but has several features of its use. If you follow all of them, then 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.

In all these drugs and their analogues, Ethinylestradiol, Estradiol, Dienogest, Chlormadinone, Cyproterone acetate act as an additional active ingredient.

Indications for use

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

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

The main contraindications

Drospirenone has several contraindications. They must be taken into account before buying medicines and starting to use them. Otherwise, various problems can be formed, which will develop into a full-fledged disease.

It is forbidden to use drugs with the hormone Drospirenone in such situations:

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

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

Drospirenone is taken with caution in such cases:

diabetes.

arterial hypertension (prolonged increase in blood pressure);
cholestatic jaundice (a pathological process in the patient's body, in which bile does not enter the duodenum through the liver, but accumulates in the blood);
cholestatic pruritus that occurs 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 pigmented hepatosis);
Dubin-Johnson syndrome (pigmentary hepatosis, characterized by impaired excretion of bound bilirubin from hepatocytes into bile capillaries);
endometriosis (a disease characterized by the proliferation of endometrial cells);
diabetes.

Instructions for use

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

Dosages and rules

All preparations containing Drospirenone are available in the form of tablets intended for oral administration. They must 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. It is forbidden to crush the tablets in any way, as this may lead to a loss of their effectiveness.

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

Side effects

If it is wrong to take contraceptives containing the hormone Drospirenone, then you may encounter side effects. Because of them, health conditions can deteriorate.

Circulatory system. In rare cases, patients may experience thrombocytosis and anemia.
The immune system. The drug can cause various allergic reactions. There are negative consequences from the increased sensitivity of the body to the hormone.
Metabolism. Women taking Drospirenone may develop hyponatremia and hyperkalemia.
Nervous system. Patients often complain of severe headaches and dizziness. Migraine develops, nervousness, drowsiness and depression appear. In case of large overdoses, tremor, vertigo and anorgasmia may occur.
Organs of vision. Drospirenone can affect visual acuity as well as dry eye syndrome and conjunctivitis.
The cardiovascular system. In case of errors in taking pills, tachycardia and arterial hypertension may develop. Rarely, arterial and venous thromboembolism, varicose veins, epistaxis and phlebitis are formed.
Digestive system. Women suffer from pain in the abdomen, exacerbation of gastritis, severe diarrhea, bouts of nausea and vomiting. Much less common are gastrointestinal disorders, oral candidiasis, and a feeling of fullness in the abdomen.
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.
Musculoskeletal system. The hormone can cause pain in the back, limbs and muscles.
The reproductive system. In women, there are pains in the mammary glands, amenorrhea and metrorrhagia. With excessive dosages, vaginal and uterine bleeding, menstrual irregularities, hypomenorrhea and dysmenorrhea may occur.
General disorders. Patients may experience increased sweating, weight gain, weakness, asthenia.

special instructions

During clinical trials, some of the features of Drospirenone were discovered. Thanks to them, errors in application can be avoided and dosages can be accurately calculated.

Studies have shown that the use of the hormone increases the risk of developing venous thromboembolism. Because of this, one should carefully monitor changes in the health status of women predisposed to this disease.
Patients with mild to moderate renal impairment should regularly monitor the concentration of potassium ions in the blood.
It is possible to use contraceptives containing Drospirenone only after passing a full examination and passing all tests.
Women suffering from chronic liver diseases should periodically monitor the indicators of the functionality of this organ.
With moderate hypertriglyceridemia, it is necessary to monitor the amount of triglycerides in the blood.
Patients with diabetes mellitus of varying severity can use Drospirenone only under medical supervision.
The hormone does not combine well with alcohol, therefore, during the period of therapy, one should refrain from drinking alcoholic beverages.
Drospirenone causes drowsiness and slows down the reaction rate. Because of this feature, it is prohibited to drive a car or any other vehicle. It is not recommended to perform work requiring special accuracy and increased concentration of attention.

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 can cause the development of side effects and reduce the therapeutic effect.

The main combinations and their consequences for the body:

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

Cost and comparison with other hormones

All medicines containing Drospirenone are included in the register of medicines (RLS), therefore they 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 the capital, and in neighboring states - higher.

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

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

Drospirenone is one of the most popular hormones found in oral contraceptives. With its correct application and adherence to all the recommendations of doctors, you can achieve the desired result and avoid any complications.