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Active ingredients
Levonorgestrel + Ethinyl Estradiol
Release form
Dragee
Composition
Active ingredient: 0.15 mg of levonorgestrel and 0.03 mg of ethinyl estradiol. Auxiliary substances: lactose monohydrate, corn starch, povidone 25 Ltd., talc, magnesium stearate, sucrose, povidone 700 000, macrogol 6000, calcium carbonate, glycerol 85%, titanium dioxide, iron oxide pigment yellow, montan glycolic wax. Concentration of active ingredient (mg): 0.18 mg
Pharmacological effect
Microgynon - a low-dose monophasic oral combined estrogen-gestagenic contraceptive drug. Mikoginon contraceptive effect is carried out through three complementary mechanisms: - suppression of ovulation at the level of the hypothalamic-pituitary regulation; which makes implantation of a fertilized egg impossible. In women taking combined oral contraceptives ratseptivy, the menstrual cycle becomes more regular, less frequent painful menstruation, decreases the intensity of bleeding, resulting in reduced risk of iron deficiency anemia.
Pharmacokinetics
LevonorgestrelAbsorptionAfter oral administration, the levonorgestrel is rapidly and completely absorbed, its Cmax in serum, equal to 3-4 ng / ml, is reached after about 1 hour. When administered orally, the bioavailability of levonorgsstrela is almost complete. DistributionLevonorgestrel is bound by serum albumin and a sex hormone-binding globulin (SHBG). In free form is only 1.3% of the total serum concentration; while 64% are specifically associated with SHBG and about 35% are not specifically associated with albumin. As a result of the induction of ethylene estradiol synthesis of HSPG, the fraction associated with HSPG increases, while the fraction associated with albumin 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 about 1.3–1.6 ml / min / kg. Injection The content of levonorgestrel in serum decreases in two phases.T1 / 2 of the terminal phase is about 20-23 hours. Levonorgestrel is not excreted in unchanged form, but only in the form of metabolites (T1 / 2 - 24 h), which are excreted in urine and bile in a ratio of approximately 1: 1 Equilibrium concentration. The pharmacokinetics of levonorgestrel is influenced by the level of SHBG in blood serum, which increases approximately 1.7 times over the 21-day course of administration of Mikolinon. As a result of the daily intake of the drug, the level of the substance in the serum increases by about 3-4 times, and the equilibrium concentration is reached in the second half of the intake cycle. When the equilibrium concentration is reached, the rate of clearance is reduced accordingly to 0.7 ml / min / kg. Ethinyl estradiol Absorption After oral administration, ethinyl estradiol is absorbed quickly and completely. Cmax in serum, equal to about 95 pg / ml, is achieved in 1-2 hours. During absorption and the first passage through the liver, ethinyl estradiol is metabolized, resulting in its bioavailability when administered orally averages about 45%, with significant individual differences within 20-65%. The distribution of ethynyl estradiol is almost completely (98%), although it is not specific, binds albumin. Ethinyl estradiol induces synthesis of SHBG. The apparent volume of distribution of ethinyl estradiol is 2.8–8.6 l / kg. Metabolism Ethinyl estradiol undergoes systemic conjugation in both the mucosa of the small intestine and in the liver. The main metabolic pathway is aromatic hydroxylation. The rate of metabolic clearance from blood plasma is 2.3-7 ml / min / kg. WithdrawalThe decrease in the concentration of ethinyl estradiol in serum is biphasic; The first phase is characterized by T1 / 2 about 1 hour, the second - 10-20 hours. Unchanged from the body is not displayed. Ethinyl estradiol metabolites are excreted by the kidneys and liver in a 4: 6 ratio with a T1 / 2 of about 24 hours. Equilibrium concentration. Equilibrium concentration is reached in one week.
Indications
Contraception
Contraindications
Microgynon should not be applied in the presence of any of the conditions listed below. If any of these conditions develop for the first time while receiving, the drug should be immediately discontinued. Thrombosis (venous and arterial) and thromboembolism at present or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders). Pre-thrombosis states (including transient ischemic attacks,Angina pectoris) currently or in history. Migraine with focal neurological symptoms in the history hearts; uncontrolled arterial hypertension. Pancreatitis with severe hypertriglyceridemia now or in history. Hepatic failure and severe liver disease (until liver tests return to normal). Tumors of the liver (benign or malignant) now or in anamnesome. hormone-dependent malignant diseases (including the genitals or mammary glands) or suspicion of them. Vaginal bleeding of unknown origin. Pregnancy or suspicion of it. The period is fed I am breastfeeding. Increased sensitivity to any of the components of Microgynone previous pregnancy, migraine, congenital hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndromes), diabetes mellitus, systemic lupus erythematosus ; hemolytic uremic syndrome; Crohn's disease; sickle cell anemia; arterial hypertension.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Microgynon is not prescribed during pregnancy and during breastfeeding. If pregnancy is detected while taking Microgynon, the drug is immediately canceled. However, extensive epidemiological studies have not revealed any increased risk of developmental defects in children born to women who received sex hormones before pregnancy or teratogenic effects, when sex hormones were taken by negligence in the early stages of pregnancy. , so,their use is contraindicated during lactation. A small amount of sex steroids and / or their metabolites may be excreted in milk, but there is no evidence of their negative impact on the health of the newborn.
Dosage and administration
Drops should be taken orally in the order indicated on the packaging, every day at about the same time, with a small amount of water. Take one dragee per day continuously for 21 days. Receiving the next pack begins after a 7-day break in taking the dragee, during which withdrawal bleeding usually occurs. Bleeding, as a rule, begins 2-3 days after taking the last dragee and may not end before the start of taking a new package.
Side effects
Soreness and tension of the mammary glands, an increase in the mammary glands, discharge from the mammary glands; spotting and breakthrough uterine bleeding; headache; migraine; libido change; decrease / change of mood; poor tolerance to contact lenses; visual impairment; nausea; vomiting; stomach ache; changes in vaginal secretion; skin rash; erythema nodosum; erythema multiforme; generalized itching; cholestatic jaundice; fluid retention; change in body weight; allergic reactions. Rarely - increased fatigue, diarrhea. Chloasma can sometimes develop, especially in women with a history of pregnant chloasma. As with other combined oral contraceptives, in rare cases thrombosis and thromboembolism may occur.
Overdose
Symptoms that may occur with an overdose: nausea, vomiting, spotting or metrorrhagia. There is no specific antidote, symptomatic treatment should be carried out.
Interaction with other drugs
Sulfonamides, derivatives of pyrazolone, are able to increase the metabolism of steroid hormones that make up the drug. Long-term treatment with drugs that induce liver enzymes, which increase the clearance of sex hormones, can lead to breakthrough bleeding and / or a decrease in the contraceptive efficacy 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), since, according to some information, some antibiotics can reduce intrabiotic circulation, such as ampicillins and tetracyclines), since, according to some information, some antibiotics can reduce intrahepatic circulation. most, lowering the concentration of ethinyl estradiol. Predictive combination contraceptives can affect the metabolism of other drugs (including cyclosporine), which leads to a change in their concentration concentrations in plasma and tissues. When taking estrogen-progestin drugs, correction of the dosage regimen of hypoglycemic drugs and indirect anticoagulants may be required.
special instructions
In the case of the planned operation, it is recommended to stop taking the drug at least 4 weeks before it and not to resume taking it within 2 weeks after the end of immobilization. During the time of taking drugs that affect microsomal enzymes, and within 28 days after their cancellation, it should be further use a barrier method of contraception. While taking antibiotics (such as ampicillins and tetracyclines) and within 7 days after their cancellation, you should additionally use a barrier method of contraception. If the period of use is barrier If one of the conditions / risk factors listed below are presently present, then the potential risk and the expected risk should be carefully weighed. benefit of Microgynon treatment in each individual case and discuss it with a woman before she decides to start taking the drug. In case of worsening, intensifying or first manifestation of any of these conditions or risk factors, the woman should consult with her doctor, who may decide to discontinue the drug. Cardiovascular diseases There is evidence of an increased incidence of venous and arterial thrombosis and thromboembolism during admission combined oral contraceptives. However, the frequency of venous thromboembolism (VTE),developing when taking combined oral contraceptives, less than the frequency associated with pregnancy (6 per 10,000 pregnant women per year). Women taking combined oral contraceptives described extremely rare cases of thrombosis of other blood vessels, for example, hepatic, mesenteric, renal arteries and veins, central vein of the retina and its branches. The relationship with taking oral oral contraceptives has not been proven. Women should stop taking the drug and consult a doctor if they develop symptoms of venous or arterial thrombosis or cerebrovascular disorders, which may include: unilateral pain in the leg and / or edema; sudden severe chest pain, with or without irradiation to the left hand; sudden shortness of breath; sudden coughing attack; any unusual, severe, prolonged headache; sudden partial or complete loss of vision; diplopia; inarticulate speech or aphasia; dizziness; loss of consciousness with / or without convulsive seizure; weakness or a very significant loss of sensitivity, suddenly appearing 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 further increases, especially in women over 35 years old), if there is: - a family history (ie venous or arterial thromboembolism ever with close relatives or parents at a relatively young age); in case of hereditary predisposition, the woman should be examined by an appropriate specialist to decide on the possibility of taking COCs - obesity (body mass index more than 30 kg / m2); - dyslipoproteinemia; - arterial hypertension; - migraine; - valvular heart disease; atrial - prolonged immobilization, serious surgery, any surgery on the legs or extensive trauma. In these situations, it is advisable to stop using combined oral contraceptives (in the case of the planned operation, at least four weeks before it) and not to resume reception within two weeks after the end of immobilization. The increased risk of thromboembolism in the postpartum period should be taken into account. noted in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome,chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. Increasing the frequency and severity of migraine while using combined oral contraceptives (which may precede cerebrovascular disorders) may be grounds for immediate discontinuation of these drugs. Biochemical parameters that may be indicators of hereditary or acquired susceptibility to venous or arterial thrombosis, include resist ntnost to activated protein C, hyperhomocysteinemia, deficiency of antithrombin-IIl, protein C deficiency, protein deficit S, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant) .OpuholiImeyutsya reports of increased risk of developing cervical cancer with long-term use of combined oral contraceptives. His connection with the reception of combined oral contraceptives has not been proven. Controversy persists regarding the extent to which these findings relate to sexual behavior and other factors, such as human papillomavirus (HPV). It was also found that there is a slightly increased relative risk of developing breast cancer diagnosed in women who used the combined oral contraceptives. His connection with the reception of combined oral contraceptives has not been proven. The observed increase in risk may be a consequence of an earlier diagnosis of breast cancer in women using combined oral contraceptives. In rare cases, the development of liver tumors was observed during the use of combined oral contraceptives. If you experience severe abdominal pain, enlarged liver, or signs of intra-abdominal bleeding, this should be considered when making a differential diagnosis. Other conditions a slight increase in blood pressure has been described in many women taking combined oral contraceptives, clinically significant improve search were rare.However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, these drugs should be canceled and treatment of hypertension should begin. Reception of combined oral contraceptives can be continued if normal blood pressure values are achieved using antihypertensive therapy. The following conditions have been reported to develop or worsen both during pregnancy and when combined oral contraceptives are taken, but they are associated with combined oral contraceptives not proven: jaundice and / or itching associated with cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; chorea; herpes pregnant; hearing loss associated with otosclerosis. Also described are cases of Crohn's disease and ulcerative colitis associated with the use of combined oral contraceptives. Acute or chronic liver dysfunction may require discontinuation of the use of combined oral contraceptives until the liver function returns to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous sex hormones, requires the discontinuation of combined oral contraceptives. Although combined oral contraceptives may affect insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetic patients who low-dose combined oral contraceptives (<0.05 mg ethinyl estradiol). However, women with diabetes should be carefully monitored while taking combined oral contraceptives. Women who have a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation. laboratory tests, including indicators of liver, kidney, thyroid, adrenal glands, transport proteins in plasma, carbohydrate metabolism, coagulation and fibrinolysis parameters.Changes usually do not go beyond the normal range. Influence on the menstrual cycleIn a 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 adaptation period of approximately three cycles. If irregular bleeding recurs or develops after previous regular cycles, a thorough examination should be carried out to rule out malignant neoplasms or pregnancy. Some women may have do not develop withdrawal bleeding. If combined oral contraceptives were taken as directed, it is unlikely that the woman is pregnant. However, if previously combined oral contraceptives were taken irregularly or, if there are no two withdrawal bleedings in a row, pregnancy should be ruled out before continuing to take the drug. Medical examinations examination of cervical mucus), 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 tests every 6 months. A woman should be warned that drugs of Microgynon do not protect against HIV infection (AIDS) and other sexually transmitted diseases! on the ability to drive a car and equipmentNo detected.