Microgynon, dragee, 21pcs

Composition

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of 1 tablet contains:

Active ingredient:

levonorgestrel micro 20-0.15 mg,

ethinyl estradiol micro 20-0.03 mg,

Auxiliary substances:

lactose-32.97 mg;

corn starch-18 mg;

polyvidone 25000-2.1 mg;

talc-1.65 mg;

magnesium stearate-0.1 mg

Shell:

sucrose-19.371 mg; polyvidone 700000-0.189 mg; polyethylene glycol 6000-2.148 mg; calcium carbonate-8.606 mg; talc — 4.198 mg; titanium dioxide-0.274 mg; glycerol 85% – 0.137 mg; mountain glycol wax-0.05 mg; iron oxide yellow pigment-0.027 mg

Pharmacological action

Microgynone is a contraceptive, estrogen is a progestogen.

Pharmacokinetics

Levonorgestrel

Absorption rate

Levonorgestrel is rapidly and completely absorbed after oral use, and itsserum cmax of 3-4 ng / ml is reached in approximately 1 hour. When taken orally, the bioavailability of levonorgestrel is almost complete.

Distribution

Levonorgestrel binds to serum albumins and sex hormone-binding globulin (SHBG). Only 1.3% of the total serum concentration is free, while 64% is specifically bound to SHBG and about 35% is not specifically bound to albumin. As a result of ethinylestradiol induction of SHBG synthesis, the SHBG-bound fraction increases, while the albumin-bound fraction decreases. The apparent volume of distribution of levonorgestrel is approximately 184 liters after a single dose.

Metabolism

Levonorgestrel is completely metabolized. The rate of serum clearance is approximately 1.3-1.6 ml / min / kg.

Deduction

The levonorgestrel content in the blood serum decreases biphasically. T_1/2 of the terminal phase is about 20-23 hours. Levonorgestrel is not excreted unchanged, but only in the form of metabolites (T_1/2-24 hours), which are excreted in the urine and bile in a ratio of approximately 1: 1

Equilibrium concentration. The pharmacokinetics of levonorgestrel are affected by the level of SHBG in the blood serum, which increases approximately 1.7 times over the 21-day course of Microgynone use. As a result of daily use of the drug, the level of the substance in the serum increases approximately 3-4 times, and the equilibrium concentration is reached in the second half of the intake cycle. When the equilibrium concentration is reached, the clearance rate decreases to 0.7 ml/min/kg, respectively.

Ethinyl Estradiol

Absorption After oral use, ethinyl estradiol is rapidly and completely absorbed. _Cmax in blood serum, equal to approximately 95 pg / ml, is reached in 1-2 hours. During absorption and the first passage through the liver, ethinyl estradiol is metabolized, resulting in an average oral bioavailability of about 45%, with significant individual differences in the range of 20-65%.

Distribution

Ethinyl estradiol binds almost completely (98%), although not specifically, to albumin. Ethinyl estradiol induces the synthesis of SHBPS. The apparent volume of distribution of ethinyl estradiol is 2.8-8.6 l / kg.

Metabolism

Ethinyl estradiol undergoes presystemic conjugation, both in the mucosa of the small intestine and in the liver. The main pathway of metabolism is aromatic hydroxylation. The rate of metabolic clearance from blood plasma is 2.3-7 ml / min / kg.

Deduction

The decrease in the concentration of ethinyl estradiol in the blood serum is biphasic; the first phase is characterized by T_1/2 of about 1 hour, the second-10-20 hours. It is not excreted unchanged from the body. Metabolites of ethinyl estradiol are excreted by the kidneys and liver in a ratio of 4: 6 with T_1/2 for about 24 hours.

Equilibrium concentration. The equilibrium concentration is reached after one week.

Indications

Contraception.

Contraindications

• hypertension (systemic arterial pressure 160/100 or higher);
• thrombophlebitis any location, thromboembolic disease (including cured);
• severe violations of cerebral circulation stroke; complicated valvular heart disease;
• high risk of cardiovascular lesions (ischemic heart disease, myocardial infarction);
• surgery with prolonged immobilization (high probability of thromboembolic complications), hereditary thrombogenic diseases;
• migraine with severe neurological symptoms;
• severe acute and chronic liver disease (acute hepatitis, cirrhosis, decompensation, cancer);
• diabetes duration more than 20 years, or diabetes mellitus with severe vascular complications, regardless of length of disease;
• breast cancer;
• uterine bleeding of unknown etiology;
• Smoking at the age of 35 years and older; 
• hypersensitivity to the drug; 
• pregnancy.

Side effects

Soreness and tightness of the mammary glands, breast enlargement, discharge from the mammary glands; spotting spotting and breakthrough uterine bleeding; headache; migraine; changes in libido; decreased/altered mood; poor contact lens tolerance; visual impairment; nausea; vomiting; abdominal pain; changes in vaginal secretion; skin rash; erythema nodosum; erythema multiforme; generalized pruritus; cholestatic jaundice; fluid retention; weight change; allergic reactions. Rarely – increased fatigue, diarrhea.

Sometimes chloasma can develop, especially in women with a history of chloasma in pregnant women.

As with other combined oral contraceptives, thrombosis and thromboembolism may occur in rare cases.

Interaction

Sulfonamides, pyrazolone derivatives can enhance the metabolism of the steroid hormones included in the preparation. Long-term treatment with drugs that induce liver enzymes, which increases the clearance of sex hormones, may lead to breakthrough bleeding and / or a decrease in the contraceptive effectiveness of Microgynon. These drugs include: phenytoin, barbiturates, primidone, carbamazepine and rifampicin; there are also suggestions for oxcarbazepine, topiramate, felbamate, ritonavir and griseofulvin and preparations containing St. John’s wort.

Contraceptive protection is reduced when taking antibiotics (such as ampicillins and tetracyclines), as, according to some reports, some antibiotics can reduce the intrahepatic circulation of estrogens, thereby lowering the concentration of ethinyl estradiol. Oral combined contraceptives can affect the metabolism of other drugs (including cyclosporine), which leads to changes in their concentration in plasma and tissues. When taking estrogen-progestogenic drugs, it may be necessary to adjust the dosage regimen of hypoglycemic drugs and indirect anticoagulants.

How to take, course of use and dosage

Pills should be taken orally in the order indicated on the package, every day at about the same time, with a small amount of water. Take one tablet a day continuously for 21 days. Taking the next package begins after a 7-day break in taking pills, during which withdrawal bleeding usually occurs. Bleeding usually begins 2-3 days after taking the last tablet and may not end until the start of taking a new package.

How to start taking Microgynone

— If you have not taken any hormonal contraceptives in the previous month.

Microgynone is taken on the first day of the menstrual cycle (i. e., on the first day of menstrual bleeding). It is allowed to start taking pills for 2-5 of the menstrual cycle, but in this case it is recommended to additionally use a barrier method of contraception during the first 7 days of taking pills from the first package.

— When switching from other combined oral contraceptives.

It is preferable to start taking Microgynone the next day after taking the last active tablet from the previous package, but in no case later than the next day after the usual 7-day break (for drugs containing 21 tablets) or after taking the last inactive tablet (for drugs containing 28 tablets in a package).

— When switching from progestogen-only contraceptives (mini-pills, injectable forms, implants) or from a progestogen-releasing intrauterine contraceptive (Mirena).

A woman can switch from a mini-pill to Microgynone on any day (without a break), from an implant or intrauterine contraceptive with a progestogen-on the day of its removal, from an injectable form-from the day when the next injection should have been made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking pills.

– After an abortion in the first trimester of pregnancy.

A woman can start taking medication immediately. If this condition is met, the woman does not need additional contraceptive protection.

– After giving birth or having an abortion in the second trimester of pregnancy. It is recommended to start taking the drug on 21-28 days after delivery or abortion in the second trimester of pregnancy. If the reception is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking pills. However, if a woman has already had sexual activity, pregnancy should be excluded before taking Microgynone or it is necessary to wait for the first menstruation.

Taking missed pills

If the delay in taking the drug is less than 12 hours, the contraceptive protection is not reduced. A woman should take a tablet as soon as possible, the next one is taken at the usual time.

If the delay in taking pills is more than 12 hours, the contraceptive protection may be reduced. In this case, you can follow the following two basic rules::

– The drug should never be interrupted for more than 7 days.

– 7 days of continuous intake of pills are required to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

Accordingly, the following tips can be given if the delay in taking pills is more than 12 hours (the interval from the moment of taking the last pill is more than 36 hours)::

– First week of taking the drug

A woman should take the last missed tablet as soon as she remembers (even if it means taking two pills at the same time). The next tablet is taken at the usual time. Additionally, a barrier method of contraception (such as a condom) should be used for the next 7 days. If sexual intercourse took place during the week before skipping pills, it is necessary to take into account the probability of pregnancy.

The more pills missed, and the closer they are to a break in taking active substances, the more likely pregnancy is.

– The second week of taking the drug

, a woman should take the last missed tablet as soon as possible, as soon as she remembers (even if this means taking two pills at the same time). The next tablet is taken at the usual time.

Provided that the woman took the pills correctly during the 7 days preceding the first missed pill, there is no need to use additional contraceptive measures. Otherwise, as well as if you miss two or more pills, you must additionally use barrier methods of contraception (for example, a condom) for 7 days.

– The third week of taking the drug

The risk of reduced reliability is inevitable due to the upcoming break in taking pills.

A woman should strictly adhere to one of the following two options. However, if all pills were taken correctly in the 7 days preceding the first missed pill, there is no need to use additional contraceptive methods.

1. A woman should take the last missed pill as soon as she remembers (even if it means taking two pills at the same time). The next tablet is taken at the usual time, until the pills from the current package run out. The next package should be started immediately. Withdrawal bleeding is unlikely until the second pack is finished, but there may be spotting and breakthrough bleeding while taking pills.

2. A woman can also stop taking pills from the current package. Then she should take a break for 7 days, including the day of skipping pills and then start taking a new package.

If a woman has missed taking pills, and then during a break in taking pills, she does not have withdrawal bleeding, it is necessary to exclude pregnancy.

Recommendations for vomiting and diarrhea

If a woman has had vomiting or diarrhea for up to 4 hours after taking active pills, absorption may not be complete and additional contraceptive measures should be taken. In these cases, you should follow the recommendations when skipping pills.

Changing the day when your menstrual cycle starts

In order to delay the onset of menstruation, a woman should continue taking pills from the new package of Microgynone immediately after taking all the pills from the previous one, without a break in reception. Pills from this new package can be taken as long as the woman wants (until the package is finished). Against the background of taking the drug from the second package, a woman may experience spotting or breakthrough uterine bleeding. Resume taking Microgynone from a new package after the usual 7-day break.

In order to move the day of the beginning of menstruation to another day of the week, a woman should be advised to shorten the next break in taking pills for as many days as she wants. The shorter the interval, the higher the risk that she will not have withdrawal bleeding, and will continue to have spotting and breakthrough bleeding while taking the second package (as well as in the case when she would like to delay the onset of menstruation).

Overdose

Symptoms that may occur with an overdose: nausea, vomiting, spotting or metrorrhagia.

There is no specific antidote, and symptomatic treatment should be performed.

Special instructions

In the case of planned surgery, it is recommended to stop taking the drug at least 4 weeks before it and not resume taking it for 2 weeks after the end of immobilization.

When taking medications that affect microsomal enzymes, and for 28 days after their withdrawal, you should additionally use a barrier method of contraception.

When taking antibiotics (such as ampicillins and tetracyclines) and for 7 days after their withdrawal, you should additionally use a barrier method of contraception.

If the period of using the barrier method of protection ends later than the pills in the package, you need to move on to the next package of Microgynone without the usual break in taking pills.

If any of the conditions / risk factors listed below are currently present, then the potential risk and expected benefit of Microgynone treatment should be carefully weighed on a case-by-case basis and discussed with the woman before she decides to start taking the drug. If any of these conditions or risk factors become more severe, worsen, or first appear, a woman should consult with her doctor, who may decide whether to discontinue the medication.

Diseases of the cardiovascular system

There is evidence of an increased incidence of venous and arterial thrombosis and thromboembolism when taking combined oral contraceptives.

However, the rate of venous thromboembolism (VTE) that develops when taking combined oral contraceptives is less than the rate associated with pregnancy (6 per 10,000 pregnant women per year).

Extremely rare cases of thrombosis of other blood vessels, such as hepatic, mesenteric, renal arteries and veins, central retinal vein and its branches, have been described in women taking combined oral contraceptives. The association with the use of combined oral contraceptives has not been proven.

Women need to stop taking the drug and consult a doctor if you develop symptoms of venous or arterial thrombosis or cerebrovascular disorders, which can include: unilateral leg pain and/or swelling; sudden severe pain in the chest, with or without radiating to the left arm; sudden breathlessness; sudden attack of coughing; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia; slurred speech or aphasia; vertigo; loss of consciousness with or without convulsive seizure; weakness or very significant loss of sensitivity suddenly appeared on one side or in one part of the body; movement disorders; symptoms of “acute abdomen”. The risk of thrombosis (venous and/or arterial) and thromboembolism increases:

– with age

-in smokers (with an increase in the number of cigarettes or an increase in age, the risk increases further, especially in women over 35 years of age);

in the presence of:

– family history (i. e. venous or arterial thromboembolism ever in close relatives or parents at a relatively young age); in the case of hereditary predisposition, the woman should be assessed appropriately skilled for the solution of the question about the possibility of receiving KOK;

– obesity (body mass index more than 30 kg/m 2);

– dyslipoproteinemia;

– arterial hypertension;

– migraine;

– diseases of heart valves;

– atrial fibrillation;

– prolonged immobilization, major surgery, any surgery to the legs or extensive trauma. In these situations, it is advisable to stop using combined oral contraceptives (in the case of planned surgery, at least four weeks before it) and not resume taking them for two weeks after the end of immobilization.

An increased risk of postpartum thromboembolism should be considered.

Circulatory disorders can also occur in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel diseases (Crohn’s disease or ulcerative colitis) and sickle cell anemia.

An increase in the frequency and severity of migraines during the use of combined oral contraceptives (which may precede cerebrovascular disorders) may be a reason for immediate discontinuation of these medications.

Biochemical parameters that can be indicators of hereditary or acquired predisposition to venous or arterial thrombosis include resistance to activated protein C, hyperhomocysteinemia, antithrombin-IIl deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (cardiolipin antibodies, lupus anticoagulant).

Tumors

There are reports of an increased risk of cervical cancer with prolonged use of combined oral contraceptives. Its association with the use of combined oral contraceptives has not been proven. Controversy persists as to the extent to which these findings relate to sexual behaviors and other factors such as human papillomavirus (HPV).

It also found that there was a slightly increased relative risk of developing breast cancer diagnosed in women who used combined oral contraceptives. Its association with the use of combined oral contraceptives has not been proven.The observed increased risk may be due to earlier breast cancer diagnosis in women using combined oral contraceptives.

In rare cases, the development of liver tumors was observed against the background of the use of combined oral contraceptives. If there is severe abdominal pain, enlarged liver, or signs of intra-abdominal bleeding, this should be taken into account when making a differential diagnosis.

Other states

Women with hypertriglyceridemia (or a family history of this condition) may have an increased risk of developing pancreatitis while taking combined oral contraceptives.

Although a small increase in blood pressure has been reported in many women taking combined oral contraceptives, clinically significant increases have rarely been observed. However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, these medications should be discontinued and treatment for hypertension should be initiated. The use of combined oral contraceptives can be continued if normal blood pressure values are achieved with the help of antihypertensive therapy.

The following conditions have been reported to develop or worsen both during pregnancy and with combined oral contraceptives, but their association with combined oral contraceptives has not been proven: jaundice and/or pruritus associated with cholestasis; gallstone formation; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Sydenham’s chorea; herpes of pregnancy; hearing loss associated with otosclerosis. There are also cases of Crohn’s disease and ulcerative colitis associated with the use of combined oral contraceptives.

Acute or chronic liver function disorders may require discontinuation of combined oral contraceptives until liver function indicators return to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous use of sex hormones, requires discontinuation of combined oral contraceptives.

Although combined oral contraceptives may have an effect on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients using low-dose combined oral contraceptives (less than 0.05 mg of ethinyl estradiol). However, women with diabetes should be carefully monitored while taking combined oral contraceptives.

Women with a tendency to chloasma should avoid prolonged exposure to the sun and exposure to ultraviolet radiation while taking combined oral contraceptives.

Laboratory tests

The use of combined oral contraceptives may affect the results of certain laboratory tests, including liver, kidney, thyroid, and adrenal function, plasma transport protein levels, carbohydrate metabolism, and coagulation and fibrinolysis parameters. Changes usually do not exceed the limits of normal values.

Effects on the menstrual cycle

While taking combined oral contraceptives, irregular bleeding (spotting spotting or breakthrough bleeding) may occur, especially during the first months of use. Therefore, any irregular bleeding should only be evaluated after an adjustment period of approximately three cycles.

If irregular bleeding recurs or develops after previous regular cycles, a thorough examination should be performed to rule out malignancies or pregnancy.

Some women may not develop withdrawal bleeding during a break from taking pills. If combined oral contraceptives were taken as directed, it is unlikely that the woman is pregnant. However, if previously combined oral contraceptives were taken on an irregular basis or if there are no consecutive withdrawal bleeds, pregnancy should be excluded before continuing the drug.

Medical examinations

Before starting the use of Microgynone, a woman is recommended to undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), to exclude pregnancy. In addition, violations of the blood coagulation system should be excluded.

In case of long-term use of the drug, it is necessary to conduct control examinations every 6 months.

A woman should be warned that drugs such as Microquinone do not protect against HIV infection (AIDS) and other sexually transmitted diseases!

Influence on the ability to drive a car and machinery

Not detected.

Form of production

Dragees

Storage conditions

Store under normal conditions, out of the reach of children.

Shelf

life is 5 years.

Active ingredient

Ethinyl Estradiol, Levonorgestrel

Conditions of release from pharmacies

By prescription

Dosage form

dragees

Purpose

For adults as prescribed by a doctor, For women of childbearing age

Indications

Contraception