Microgynon 150 mcg+30 mcg 21 pcs 21 pcs, 150 mcg+30 mcg 21 pcs

Microgynon is a contraceptive, estrogen-gestagenic.

Pharmacokinetics

Levonorgestrel

Absorption

. After oral administration, levonorgestrel is rapidly and completely absorbed; its C_max in serum, equal to 3-4 ng/mL, is reached after about 1 hour. The bioavailability of levonorgsstrel is almost complete with oral administration.

Distribution

Levonorgestrel is bound by serum albumin and sex hormone-binding globulin (hGBS). Only 1.3% of total serum concentrations are free; whereas 64% are specifically bound to HSPH and about 35% are not specifically bound to albumin. As a result of the induction of hGH synthesis by ethinylestradiol, the hGH-bound fraction increases while the albumin-bound fraction decreases. The apparent volume of distribution of levonorgestrel is approximately 184 L after a single dose.

Metabolism

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

Elevation

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

The equilibrium concentration. The pharmacokinetics of levonorgestrel are affected by serum hGH levels, which increase about 1.7-fold over a 21-day course of Microgynon. As a result of daily administration of the drug, serum levels of the substance increase by about 3-4 times, and the equilibrium concentration is reached in the second half of the cycle of administration. When the equilibrium concentration is reached, the clearance rate decreases accordingly to 0.7 ml/min/kg.

Ethinylestradiol

Absorption After oral administration, ethinylestradiol is absorbed rapidly and completely. C_max in blood serum, equal to about 95 pg/ml, is reached in 1-2 hours. During absorption and the first passage through the liver, ethinylestradiol is metabolized, resulting in an average bioavailability of about 45% when taken orally, with significant individual differences ranging from 20-65%.

Distribution

Ethinylestradiol is almost completely (98%), although non-specific, bound by albumin. Ethinylestradiol induces the synthesis of HSPC. The apparent volume of distribution of ethinylestradiol is 2.8-8.6 L/kg.

Metabolism

Ethinylestradiol undergoes presystemic conjugation both in the small intestinal mucosa and in the liver. The main metabolic pathway is aromatic hydroxylation. The metabolic clearance rate from plasma is 2.3-7 ml/min/kg.

Elimination

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

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

Indications

Active ingredient

Composition

1 dragee contains:

Active substance:

levonorgestrel micro 20 – 0.15 mg,

ethinylestradiol micro 20 – 0.03 mg,

Associates:

Lactose, 32.97 mg;

Corn starch, 18 mg;

Polividone 25000, 2.1 mg;

Talc – 1.65 mg;

Magnesium stearate – 0.1 mg

Covering:

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

How to take, the dosage

The tablets should be taken orally in the order given on the package, at approximately the same time each day, with a little water. One tablet per day is taken continuously for 21 days. The next package is taken after a 7-day break in the intake of tablets, during which you usually have a bleeding withdrawal. Bleeding usually begins 2 to 3 days after taking the last dose and may not end until a new dose is taken.

How to start taking Microgynon

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

The intake of Microgynon begins on the first day of the menstrual cycle (i.e., the first day of menstrual bleeding). It is allowed to start taking it on the 2nd-5th menstrual cycle, but in this case it is recommended to use an additional barrier method of contraception during the first 7 days of taking pills from the first package.

– When switching from other combined oral contraceptives.

Preferably, start Microgynon the day after taking the last active dragee from the previous package, but in no case later than the day after the usual 7-day break (for products containing 21 drages) or after taking the last inactive dragee (for products containing 28 drages per package).

– When switching from gestagen-only contraceptives (“mini-pills,” injectable forms, implant) or from a gestagen-releasing intrauterine contraceptive (Mirena).

A woman can switch from the mini-pill to Microgynon on any day (without a break), from the implant or intrauterine contraceptive with gestagen – on the day of its removal, from the 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 the pills.

– After an abortion in the first trimester of pregnancy.

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

– After childbirth or an abortion in the second trimester of pregnancy. It is recommended that the drug be started 21-28 days after childbirth or a second trimester abortion. If intake is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the dragee. However, if a woman has already been sexually active, before taking Microgynon, pregnancy must be ruled out or the first menstrual period must be waited for.

Taking missed pills

If there is a delay of less than 12 hours in taking the medication, contraceptive protection is not reduced. The woman should take the pills as soon as possible, the next one is taken at the usual time.

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

– Taking the drug should never be interrupted, for more than 7 days.

– 7 days of continuous administration of the dragee is required to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

The following advice may be given accordingly if the delay in taking the dragee is more than 12 hours (the interval since the last dragee was taken is more than 36 hours):

– First week of taking the drug

The woman should take the last missed dragee as soon as she remembers (even if that means taking two dragees at the same time). The next pill 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 the pills, the possibility of pregnancy should be taken into account.

The more the pills are missed, and the closer they are to a break in the active ingredient, the greater the chance of pregnancy.

– Second week of taking the drug

The woman should take the last missed dragee as soon as she remembers (even if that means taking two dragees at the same time). The next one is taken at the usual time.

As long as the woman has taken the dragee correctly in the 7 days preceding the first missed dragee, no additional contraceptive measures are necessary. Otherwise, and if two or more pills are missed, additional barrier contraceptive methods (e.g., a condom) should be used for 7 days.

– The third week of taking the drug

The risk of decreased reliability is inevitable because of the impending interruption in taking the pills.

The woman must strictly adhere to one of the following two options. In this case, if all the pills were taken correctly in the 7 days preceding the first missed pills, there is no need to use additional contraceptive methods.

1. The woman should take the last missed pills as soon as she remembers (even if that means taking two pills at the same time). Take the next pill at the usual time until the pills from the current package are finished. The next pack should be started immediately. Bleeding cancellation is unlikely until the second pack is finished, but there may be oozing and breakthrough bleeding while taking the pills.

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

If a woman misses a dose and then has no bleeding cancellation during a break in the dragee, pregnancy must be ruled out.

Recommendations for vomiting and diarrhea

If a woman has had vomiting or diarrhea within 4 hours of taking active pills, absorption may not be complete and additional contraceptive measures must be taken. In these cases, the recommendations for skipping the dragee should be followed.

Changing the start day of the menstrual cycle

In order to delay the start of a period, women should continue any new pack of Microgynon immediately after taking all the pills from the previous day, without interruption. This new pack can be taken as long as the woman wishes (until the pack runs out). While taking the product from the second package, a woman may experience mucous discharge or breakthrough uterine bleeding. You should resume taking Microgynon from the new package after the usual 7-day break.

In order to postpone the day her period starts to another day of the week, a woman should be advised to shorten her immediate break from taking the dragee by as many days as she wants. The shorter the interval, the greater the risk that she won’t have a bleeding withdrawal and will subsequently have oozing and breakthrough bleeding while taking the second pack (just as she would if she wanted to delay the start of her period).

Interaction

Sulfonamides, pyrazolone derivatives can increase the metabolism of the steroid hormones in the drug.
Prolonged treatment with drugs that induce liver enzymes, resulting in increased clearance of sex hormones, may lead to breakthrough bleeding and/or decrease the contraceptive efficacy of Microgynon.
These medications include: phenytoin, barbiturates, primidone, carbamazepine, and rifampicin; there is also speculation about oxcarbazepine, topiramate, felbamate, ritonavir and griseofulvin, and St John’s wort medications.

Contraceptive protection is reduced when taking antibiotics (such as ampicillins and tetracyclines) because some evidence suggests that some antibiotics may reduce intrahepatic circulation of estrogen, thereby lowering the concentration of ethinylestradiol.
Preterm combined contraceptives may affect the metabolism of other drugs (including cyclosporine), resulting in changes in their plasma and tissue concentrations.
When taking estrogen-gestagen drugs, dosing regimens of hypoglycemic drugs and indirect anticoagulants may need to be adjusted.

Special Instructions

If surgery is planned, it is recommended to discontinue the drug at least 4 weeks prior to surgery and not to resume it for 2 weeks after the end of immobilization.

When taking drugs that affect microsomal enzymes and for 28 days after their withdrawal, an additional barrier method of contraception should be used.

When taking antibiotics (such as ampicillins and tetracyclines) and for 7 days after their withdrawal, an additional barrier method of contraception should be used.

If the period of barrier method of contraception ends later than the pills in the package, you should proceed to the next package of Microgynon without the usual break in taking the pills.

If any of the conditions/risk factors listed below are currently present, the potential risks and expected benefits of Microgynon 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 worsen, intensify, or first appear, the woman should consult her physician, who may decide if the drug should be discontinued.

Cardiovascular disease

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

However, the incidence of venous thromboembolism (VTE) developing while taking combined oral contraceptives is lower than that associated with pregnancy (6 per 10,000 pregnant women per year).

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

The woman should discontinue the drug and consult a physician if she develops symptoms of venous or arterial thrombosis or cerebrovascular disorders, which may include: unilateral leg pain and/or swelling; sudden severe chest pain, with or without irrigation to the left arm; sudden shortness of breath; sudden cough attack; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia slurred speech or aphasia; dizziness; loss of consciousness with or without a seizure; weakness or very marked loss of sensation, suddenly on one side or in one part of the body; motor disturbances; “acute abdominal symptoms. The risk of thrombosis (venous and/or arterial) and thromboembolism increases:

– with age

– in smokers (with more cigarettes or increased age, the risk further increases, especially in women over 35);

if there is:

– a family history (i.e. venous or arterial thromboembolism ever in a close relative or parent at a relatively young age; if there is a hereditary predisposition, the woman should be seen by an appropriate specialist to decide whether to take OCs;

– obesity (body mass index greater than 30 kg/m2);

– dyslipoproteinemia;

– arterial hypertension;

– migraine;

– heart valve disease;

p> – atrial fibrillation;

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

The increased risk of thromboembolism in the postpartum period should be considered.

Circulatory disturbances may also be noted in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn’s disease or nonspecific ulcerative colitis) and sickle cell anemia.

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

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

Tumors

There have been reports of an increased risk of cervical cancer with long-term use of combined oral contraceptives. Its association with taking combined oral contraceptives has not been proven. There remains controversy about the extent to which these findings relate to patterns of sexual behavior and other factors, such as human papillomavirus (HPV).

It has also been found that there is a slightly increased relative risk of breast cancer diagnosed in women who have used combined oral contraceptives. Its connection with the use of combined oral contraceptives has not been proved. The observed increase in risk may be a consequence of earlier diagnosis of breast cancer in women who used combined oral contraceptives.

In rare cases, the development of liver tumors has been observed during the use of combined oral contraceptives. If severe abdominal pain, liver enlargement, or signs of intra-abdominal bleeding occur, this should be considered in making a differential diagnosis.

Other conditions

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

While small increases in blood pressure have been described in many women taking combined oral contraceptives, clinically significant increases have rarely been reported. However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, the medications should be stopped and treatment for arterial hypertension should be initiated. The combined oral contraceptives may be continued if normal blood pressure values are achieved with hypotensive therapy.

The following conditions have been reported to develop or worsen both during pregnancy and while taking combined oral contraceptives, but their association with taking 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. Cases of Crohn’s disease and nonspecific ulcerative colitis have also been described with combined oral contraceptives.

Acute or chronic liver dysfunction may require discontinuation of combined oral contraceptives until liver function returns 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.

While combined oral contraceptives may affect 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 ethinylestradiol). However, women with diabetes should be closely monitored while taking combined oral contraceptives.

Women who are prone to chloasma should avoid prolonged sun exposure and exposure to ultraviolet radiation while taking combined oral contraceptives.

Laboratory tests

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

The effect on the menstrual cycle

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

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

Some women may not develop withdrawal bleeding during a break in the drags. If the combined oral contraceptives have been taken as directed, it is unlikely that the woman is pregnant. However, if the combined oral contraceptives have been taken irregularly before, or if there have not been two consecutive bleeding withdrawals, pregnancy must be ruled out before continuing the medication.

Medical examinations

Before starting Microgynon, it is recommended that a woman undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), to rule out pregnancy. In addition, disorders of the blood clotting system should be excluded.

In case of long-term use of the drug, follow-up examinations should be performed every 6 months.

Warn women that drugs like Microgynon do not protect against HIV infection (AIDS) or other sexually transmitted diseases!

The effect on the ability to drive and operate machinery

No effect has been found.

Contraindications

Side effects

Pain and tightness in the mammary glands, breast enlargement, mammary discharge; oozing and breakthrough uterine bleeding; headache; migraine; change in libido; decrease/change in mood; poor tolerance of contact lenses; visual disturbances; nausea; vomiting; abdominal pain; changes in vaginal secretion; skin rash; erythema nodosum; erythema multiforme; generalized itching; cholestatic jaundice; fluid retention; weight changes; allergic reactions. Rarely, increased fatigue and diarrhea.

Sometimes chloasma may develop, especially in women with a history of pregnancy chloasma.

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

Overdose

Symptoms that may occur in case of overdose: nausea, vomiting, mucous bloody discharge or metrorrhagia.

There is no specific antidote, symptomatic treatment should be carried out.

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