Microgynon, 21 pcs., 150 mcg+30 mcg, film-coated tablets

Pharmacological properties of the drug Microgynon

The contraceptive effect of combined oral contraceptives (COCs) is based on the interaction of various factors, important among which are suppression of ovulation and changes in cervical secretion. In addition to preventing pregnancy, PDAs have a number of positive properties that can be used when choosing a method of contraception. The menstrual cycle becomes regular, menstruation is usually less painful, blood loss decreases (thereby reducing the incidence of iron deficiency anemia). There is evidence of a reduced risk of endometrial and ovarian cancer. In addition, when using high-dose COCs (50 mcg ethinyl estradiol), the risk of ovarian cysts, pelvic inflammatory diseases, benign breast diseases and ectopic pregnancy is reduced. Standard preclinical studies of repeated dose toxicity, genotoxicity, carcinogenicity and reproductive toxicity do not indicate any specific risk to humans. However, it should be noted that sex steroids can promote the growth of certain hormone-dependent tissues and pre-existing tumors. Levonorgestrel After oral administration, levonorgestrel is rapidly and completely absorbed. The peak concentration of the substance in the blood serum is about 3-4 ng/ml and is achieved approximately 1 hour after a single dose. The bioavailability of levonorgestrel after oral administration is almost complete. Levonorgestrel binds to plasma albumin and sex steroid binding globulin (SGBS). Only 1.3% of the total serum concentration is present as a free steroid, while about 64% is specifically bound to SHB and 35% is nonspecifically bound to albumin. Ethinyl estradiol-induced increase in SHPS levels affects the distribution between blood plasma proteins, causing an increase in the SHPS-bound fraction and a decrease in the albumin-bound fraction. The expected volume of distribution of levonorgestrel is 184 L after a single dose. Levonorgestrel is completely metabolized. Serum clearance is 1.3–1.6 ml/min/kg. The level of levonorgestrel in the blood serum decreases in 2 phases. Distribution in the final phase is characterized by a half-life of almost 20–23 hours. Levonorgestrel is not excreted in unchanged form. Metabolites are excreted in urine and bile in a 1:1 ratio. The half-life of metabolites is about 1 day. After daily use, the level of the drug in the blood serum increases approximately 3-4 times, reaching a state of equilibrium in the second half of the course of administration. The pharmacokinetics of levonorgestrel is affected by the level of SHPS, which increases approximately 1.7 times after oral administration of the drug Microgynon. This results in a decrease in clearance to approximately 0.7 ml/min/kg when equilibrium is reached. Ethinyl estradiol When administered orally, ethinyl estradiol is rapidly and completely absorbed. The maximum concentration is almost 95 pkg/ml and is achieved within 1–2 hours. During absorption and initial passage through the liver, ethinyl estradiol is significantly metabolized, resulting in an average oral bioavailability of about 45%. Ethinyl estradiol binds strongly and nonspecifically to plasma albumin (about 98%) and causes an increase in the concentration of GSPC. The volume of distribution is approximately 2.8–8.6 l/kg. Ethinyl estradiol is metabolized mainly by aromatic hydroxylation, however, a large number of hydroxyl and methyl metabolites are additionally formed, among which there are both free metabolites and conjugates with glucuronides and sulfates. Clearance is 2.3–7 ml/min/kg. Serum ethinyl estradiol levels decrease in 2 phases with half-lives of about an hour and 10–20 hours, respectively. The drug is not excreted from the body unchanged; ethinyl estradiol metabolites are excreted in urine and bile in a ratio of 4:6. The half-life of metabolites is about 1 day. Serum concentrations of ethinyl estradiol increase slightly after oral administration. The maximum concentration is about 114 pg/ml and is determined at the end of the cycle. Based on the variable serum half-life and daily dosing, the steady-state concentration of ethinyl estradiol in the serum is achieved in approximately one week.

Composition and release form

The drug Microgynon is produced in the form of tablets with a contraceptive effect.

The main components of the composition are ethinyl estradiol in the amount of 0.03 mg and levonorgestrel - 0.15 mg

In the production of birth control pills, other substances are also used as auxiliary substances.:

1. Lactose;
2. Corn starch;
3. Talc;
4. Polyvidone 25000;
5. Magnesium stearate.

The drug is packaged in 21 tablets , which is 1 cycle for use.

Use of the drug Microgynon

The pills should be taken every day according to the order indicated on the blister, at approximately the same time, with a small amount of liquid. The drug is taken 1 tablet per day for 21 days. Taking pills from each subsequent package should be started after the end of a 7-day break from taking the drug, during which menstrual-like bleeding usually occurs. As a rule, it begins on the 3rd day after taking the last pill and may not end by the time you start taking the pill from the next package. How to start taking Microgynon

1. No hormonal contraceptive drug was used in the previous period (last month). Taking the pills should begin on the 1st day of the patient’s menstrual cycle. You can start taking it from the 5th day, but in this case, during the first cycle, it is recommended to additionally use a barrier method of contraception in the first 7 days of using the drug.
2. Transfer from another combined PDA. It is advisable to start taking Microgynon the day after taking the last active pill of the previous COC, at least no later than the next day after a break in taking the pill or after taking the placebo pill of the patient's previous COC.
3. Transitioning from a progestogen-only method (mini-pills, injections, implants) or a progestogen-containing intrauterine system. You can start taking Microgynon any day after you stop taking the mini-pill (in the case of an implant or intrauterine system - on the day of their removal, in the case of an injection - instead of the next injection). However, in all cases it is recommended to additionally use a barrier method of contraception during the first 7 days of taking 1 tablet.
4. After an abortion in the first trimester of pregnancy. You can start taking Microgynon immediately after an abortion. In this case, there is no need to use additional contraception.
5. After childbirth or abortion in the second trimester of pregnancy. If you are breastfeeding, see the subsection Pregnancy and lactation.

It is recommended to start taking the drug Microgynon from the 21st to 28th day after childbirth or abortion in the second trimester of pregnancy. If you start taking the pill later, you must additionally use a barrier method of contraception during the first 7 days of taking the drug. However, if sexual intercourse has already taken place, then before starting to use the PDA, you need to exclude a possible pregnancy or wait for menstruation. What to do if you miss taking the pills If the delay in taking the pills does not exceed 12 hours, the contraceptive effect of the drug is not reduced. The missed pill should be taken as soon as possible. The next pill from this package should be taken at the usual time. If the delay in taking the missed pill exceeds 12 hours, contraceptive protection may decrease. In this case, you can follow two basic rules:

• a break in taking pills should never exceed 7 days;
• Adequate suppression of the hypothalamus-pituitary-ovarian system is achieved by continuously taking the pills for 7 days.

According to this, you must follow the recommendations below: 1st week You need to take the last missed pill as soon as possible, even if you have to take two pills at the same time. After this, continue to take the pills at the usual time. In addition, over the next 7 days you need to use a barrier method of contraception, such as a condom. If sexual intercourse took place in the previous 7 days, the possibility of pregnancy must be taken into account. The more pills you miss and the closer the break in taking the drug, the higher the risk of pregnancy. Week 2 You need to take the last missed pill as soon as possible, even if you have to take 2 pills at the same time. After this, continue to take the pills at the usual time. Provided you take the tablets correctly for 7 days before the first missed period, there is no need to use additional contraceptives. Otherwise, or if more than one pill is missed, it is recommended to additionally use a barrier method of contraception for 7 days. Week 3 The risk of decreased reliability increases as the break in taking the pill approaches. However, if you follow the regimen for taking pills, you can avoid a decrease in contraceptive protection. If you adhere to one of the following options, there will be no need to use additional contraceptives, provided you take the tablets correctly for 7 days before the missed period. If this is not the case, you need to stick to the first of the following options and use additional methods of contraception for the next 7 days.

1. It is advisable to take the last missed pill as soon as possible, even if you need to take 2 pills at the same time. After this, continue to take the pills at the usual time. The pills from the next package should be taken immediately after the end of the previous one, that is, there should be no break. It is unlikely that a woman will experience menstrual-like bleeding before finishing the second pack, although spotting or breakthrough bleeding may occur while taking the tablets.
2. You may also be advised to stop using the pills from the current package. In this case, the break in using the drug should be up to 7 days, including days of missing pills; You should start taking the drug from the next package.

If a tablet dose is missed and there is no menstrual bleeding during the first usual break in taking the drug, the possibility of pregnancy should be considered. Recommendations in case of gastrointestinal disorders In case of severe dysfunction, incomplete absorption of the drug is possible; in this case, you need to use additional contraception. If vomiting occurs within 3-4 hours after taking the pills, it is advisable to use the recommendations regarding skipping pills. If the patient does not want to change her usual regimen of using the drug, she needs to take additional tablet(s) from a different package. To delay the onset of menstruation, you need to continue taking Microgynon tablets from a new package and not take a break from taking the drug. If desired, the period of administration can be continued until the end of the second package. In this case, breakthrough bleeding or spotting cannot be ruled out. The usual use of the drug Microgynon continues after a 7-day break from taking the tablets. To shift the onset of menstruation to another day of the week, it is recommended to shorten the break in taking the pills by the required number of days. The shorter the break, the more often the absence of menstrual-like bleeding and breakthrough bleeding or spotting is noted while taking the pills from the second package (as in the case of a delay in the onset of menstruation).

Reviews from gynecologists

Beletskaya Oksana Anatolyevna, gynecologist:

“I am a woman myself and I prefer COCs. The contraceptive drug Microgynon is used along with the others. It is of the same quality as more well-known similar products.”

Maslyukova Veronika Andreevna, gynecologist:

“I don’t prescribe these pills often, not because they are bad, but I just don’t have much experience with them. But those patients who use them are satisfied.”

Contraindications to the use of the drug Microgynon

The PDA should not be used if you have one of the following conditions or diseases. If any of these conditions or diseases occurs for the first time while using the COC, then the drug should be stopped immediately:

• venous or arterial thrombotic/thromboembolic events (eg deep vein thrombosis, pulmonary embolism, myocardial infarction) or cerebrovascular disorders, including a history;
• prodromal symptoms of thrombosis (for example, transient ischemic attack, angina), including a history;
• history of migraine with focal neurological symptoms;
• diabetes mellitus with vascular damage;
• the presence of severe or multiple risk factors for venous or arterial thrombosis may also be a contraindication (see section PECULIARITIES OF APPLICATION);
• pancreatitis (including a history) associated with severe hypertriglyceridemia;
• severe liver disease (until normalization of liver function indicators);
• liver tumors (benign or malignant), including history;
• known or suspected hormone-dependent malignant tumors (for example, genitals or mammary glands);
• vaginal bleeding of unknown etiology;
• pregnancy;
• hypersensitivity to the active substances or to any of the components of the drug.

Side effects of the drug Microgynon

Adverse effects have been reported with the use of COCs, but their relationship with the use of COCs has not been confirmed:

Special instructions for the use of Microgynon

If any of the following conditions/risk factors are present, it is necessary to weigh the benefits of using a COC against the possible risks, taking into account the individual characteristics of each patient, before prescribing a COC. If any of the following conditions or risk factors become worse, worse, or occur for the first time, it is recommended that you consult your doctor. The doctor must decide to stop using the COC. Based on the results of epidemiological studies, there is a possible connection between the use of COCs and an increased risk of venous and arterial thrombotic and thromboembolic diseases, such as myocardial infarction, stroke, deep vein thrombosis and pulmonary embolism. The above conditions occur rarely. 1. Venous thromboembolism (VTE) - acute venous thrombosis and/or pulmonary embolism can occur when using any COC. The risk of VTE is very high during the first year of using COCs. The incidence of VTE in patients taking oral contraceptives with a low dose of estrogens (≤0.05 mg ethinyl estradiol) is up to 4 cases per 10,000 women/year compared with women not using oral contraceptives - 0.5–3 cases per 10,000 women/year The incidence of VTE associated with pregnancy is 6 cases per 10,000 women/year. Thrombosis of other blood vessels, such as arteries and veins of the liver, kidneys, mesenteric vessels, cerebral or retinal vessels, has been extremely rarely reported in women using COCs. There is no general conclusion regarding the connection of these complications with the use of PDAs. Symptoms of venous or arterial thrombotic/thromboembolic events or cerebrovascular disorders may include: unilateral lower extremity pain or swelling; sudden severe chest pain that may radiate to the left arm; sudden shortness of breath; sudden onset of cough; any unusual, severe, prolonged headache; sudden decrease or complete loss of vision; diplopia; speech impairment or aphasia; vertigo; collapse with or without partial epileptic seizure; weakness or very severe sudden numbness of one side or one part of the body; motor impairment; "acute" stomach. Factors that increase the risk of venous or arterial thrombotic/thromboembolic events or cerebrovascular events: age; smoking (with heavy smoking, the risk increases with age, especially in women over 35 years of age); family history (for example, cases of venous or arterial thromboembolism in siblings or parents at a relatively early age); obesity (body mass index more than 30 kg/m2); dyslipoproteinemia; arterial hypertension; migraine; heart valve disease; atrial fibrillation; prolonged immobilization, radical surgical interventions, any surgical operations on the lower extremities, significant injuries. In these cases, it is recommended to stop using the PDA (for elective operations at least 4 weeks before the procedure) and not restore it until 2 weeks after complete remobilization. It is necessary to take into account the increased risk of thromboembolism in the postpartum period. Other diseases that may be associated with circulatory disorders include: diabetes mellitus; systemic lupus erythematosus; hemolytic uremic syndrome; chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. An increased incidence of migraine or its exacerbations during the use of COCs (which may predetermine cerebrovascular accidents) may require urgent cessation of COC use. Biochemical indicators that may be characteristic of a hereditary or acquired tendency to venous or arterial thrombosis include: activated protein C (APC) resistance, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (anticardiolipin antibodies). When analyzing the risk/benefit ratio, the physician should take into account the fact that adequate treatment of the conditions mentioned above may reduce the associated risk of thrombosis, and also that the risk of thrombosis associated with pregnancy is higher than with the use of low-dose COCs (≤0.05 mg ethinyl estradiol). 2. Tumors An important risk factor for the development of cervical cancer is the persistence of papillomavirus. Some epidemiological studies suggest an additional increase in this risk with long-term COC use, but this is controversial because the extent to which these data account for concomitant risk factors such as cervical screening and sexual behavior, including the use of barrier methods of contraception, is unclear. The results of 54 epidemiological studies indicate a slight increase in the risk (RR = 1.24) of developing breast cancer in women using COCs. The risk gradually decreases over 10 years after stopping taking COCs. Because breast cancer is rarely diagnosed in women under 40 years of age, the increase in breast cancer diagnosis among current or recent COC users is small relative to the overall risk of developing breast cancer. The results of these studies do not prove the existence of a causal relationship. The increased risk may be due to earlier diagnosis of breast cancer in women using COCs, the biological effects of COCs, or both. There was a tendency that breast cancer detected in patients who took COCs was clinically less severe than in those who never took COCs. In isolated cases, patients taking COCs were diagnosed with benign and, less frequently, malignant liver tumors, leading in some cases to life-threatening intra-abdominal bleeding. In case of complaints of severe pain in the epigastric region, enlarged liver size, or signs of intra-abdominal bleeding during differential diagnosis, the possibility of a liver tumor in women taking COCs should be taken into account. 3. Other conditions Women with hypertriglyceridemia (including a family history) are at risk of developing pancreatitis when using COCs. Slight increases in blood pressure have been reported in many women taking COCs, but clinically significant increases in blood pressure have been reported extremely rarely. However, if prolonged clinically significant hypertension (arterial hypertension) occurs while taking a COC, then it is necessary to discontinue the COC and direct treatment to the hypertension (arterial hypertension). If appropriate, the use of COCs can be resumed after normalization of blood pressure. The following diseases have been reported to occur or worsen during pregnancy and when using COCs, but their relationship is not completely clear: jaundice and/or skin itching associated with cholestasis, gallstone formation, porphyria, systemic lupus erythematosus, hemolytic-uremic syndrome, chorea Sydenham, herpes of pregnancy, hearing loss associated with otosclerosis. In case of acute or chronic liver dysfunction, it may be necessary to stop taking COCs until liver function tests normalize. If cholestatic jaundice relapses, which first occurred during pregnancy or previous use of sex hormones, the use of COCs should be discontinued. Although COCs may influence peripheral insulin resistance and glucose tolerance, there are no data regarding the need for changes in the therapeutic regimen in patients with diabetes mellitus taking low-dose COCs (≤0.05 mg ethinyl estradiol). However, patients with diabetes mellitus should be under medical supervision during the period of taking COCs. Crohn's disease and ulcerative colitis may be associated with COC use. Chloasma can sometimes occur, especially in patients with a history of chloasma during pregnancy. Patients predisposed to the development of chloasma should avoid exposure to direct sunlight or ultraviolet radiation while taking COCs. Medical examination Before starting or resuming taking the drug Microgynon, it is necessary to conduct a full medical examination and study the patient’s medical history in detail, taking into account contraindications (see CONTRAINDICATIONS) and warnings (see PECULIARITIES OF APPLICATION). When using COCs, it is recommended to conduct periodic examinations, since the conditions listed in the CONTRAINDICATIONS section (for example, transient circulatory disorders, etc.) or risk factors (for example, a family history of venous or arterial thrombosis) may appear for the first time while taking COCs. The frequency and nature of these examinations should be based on current standards of medical practice, taking into account the individual characteristics of each patient. Particular attention is paid to examination of the pelvic organs, including standard cytological analysis of the cervix, abdominal organs, mammary glands, and blood pressure control. The patient must be warned that oral contraceptives do not protect against HIV infection and other sexually transmitted diseases. Decreased effectiveness The effectiveness of combined oral contraceptives may be reduced if a pill is missed, gastrointestinal dysfunction or other medications are used. Monitoring your cycle When taking oral contraceptives, you may experience intermenstrual bleeding (spotting or breakthrough bleeding), especially during the first few months. Taking this into account, examination in the event of the appearance of any intermenstrual discharge should be carried out only after a period of adaptation of the body to the drug (about three cycles). If the cycle disorder continues or occurs after several normal cycles, non-hormonal causes of bleeding should be considered and appropriate examinations should be carried out to exclude the presence of tumors and pregnancy. Curettage can be included in the diagnosis. Some patients may not experience menstrual bleeding during a break in taking the drug. If you take your COC as directed, there is a low chance of pregnancy. However, if the contraceptive was taken irregularly, if menstrual-like bleeding is absent for two cycles, pregnancy must be excluded before continuing to take the COC. Pregnancy and lactation The drug is contraindicated for use during pregnancy. If pregnancy occurs while using the drug Microgynon, its use must be stopped. However, the results of epidemiological studies do not indicate an increased risk of congenital defects in children born to patients who took COCs before pregnancy, nor do they indicate the existence of a teratogenic effect when unintentionally taking COCs in early pregnancy. PDAs can affect lactation, since under their influence the amount of breast milk can decrease and also change its composition. Given this, COCs are not recommended for use during breastfeeding. The active substances included in the drug and/or their metabolites are excreted in small quantities into breast milk, although there is no evidence that this negatively affects the health of the infant. The drug does not affect the ability to drive vehicles or operate machinery.

Interactions of the drug Microgynon

With other drugs may lead to breakthrough bleeding and/or loss of contraceptive effectiveness. Interactions with drugs that induce microsomal enzymes may occur. These include, for example, phenytoin, barbiturates, primidone, carbamazepine, rifampicin and (possibly) oxcarbazepine, topiramate, felbamate, ritonavir, griseofulvin, as well as medicines containing St. John's wort. This interaction may cause an increase in the clearance of sex hormones. Some clinical studies suggest that ethinyl estradiol levels may be reduced by certain antibiotics (eg penicillin and tetracycline antibiotics). When treating with any of the above drugs, it is necessary to temporarily use a barrier method of contraception in addition to taking COCs or choose another method of contraception. When treating with drugs that induce microsomal enzymes, the barrier method should be used throughout the entire period of treatment with the corresponding drug and for another 28 days after stopping its use. When treating with an antibiotic (with the exception of rifampicin and griseofulvin), the barrier method should be used for another 7 days after its discontinuation. If the barrier method is still being used, and the tablets in the PDA package have already run out, taking the tablets from the next package should be started without the usual break. Oral contraceptives may affect the metabolism of other drugs. Taking this into account, the concentrations of active substances in blood plasma and tissues (for example, cyclosporine) may change. Note: to determine the potential for interaction with drugs that are taken concomitantly with COCs, it is recommended that you read the instructions for medical use of these drugs. Impact on laboratory results Taking contraceptives may affect the results of some laboratory tests, including biochemical parameters of liver, thyroid, adrenal and kidney function, plasma levels of proteins (carriers), such as sex hormone-binding globulin and fractions lipids/lipoproteins, parameters of carbohydrate metabolism, as well as parameters of coagulation and fibrinolysis. Usually such changes are within normal limits.

Analogues substitutes

Among the substitutes for Microgynon birth control pills, the most popular are:

• Rigevidon is available in tablets based on ethinyl estradiol and levonorgestrel. (Hungary).
• Triquilar is produced in tablet form. (Germany).
• Non-Ovlon is created in tablets based on norethisterone and ethinyl estradiol. (Germany).
• Tri-Regol is available in tablet form. (Hungary).
• Triziston is produced in tablets. (Germany).
• Ovidone is available in tablets. (Hungary).
• Miniziston is produced in the form of tablets. (Germany).

Photos of substitutes:

Miniziston

Triquilar

Rigevidon

Triziston

Tri-regol