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Active ingredients
Gestoden + Ethinyl Estradiol
Release form
Dragee
Composition
Active ingredient: 0, 075 mg of gestodene and 0, 03 mg of ethinyl estradiol. Auxiliary substances: lactose monohydrate, corn starch, povidone 25000, sodium calcium edetate, magnesium stearate, sucrose, povidone 700000, polyethylene glycol (macrogol) 6000, calcium carbonate, talc, montan glycolic wax. . Concentration of active ingredient (mg): 0, 105 mg
Pharmacological effect
Low-dose monophasic oral contraceptive. The femodene contraceptive effect is based on the interaction of various factors, the most important of which are inhibition of ovulation and changes in the secretion of cervical mucus. In addition to contraceptive action, combined oral contraceptives have a positive effect, which should be considered when choosing a method of birth control. the cycle becomes more regular, less frequent painful menstruation. decreases the intensity of bleeding, resulting in reduced risk of iron deficiency anemia.
Pharmacokinetics
Gestodene Orally taken gestodene is rapidly and completely absorbed. Cmax of gestodene in serum, equal to 4 ng / ml, is reached within 1.0 h after ingestion. The absolute bioavailability of gestodene is about 99% of the dose taken. Gestoden is bound by serum albumin and globulin that binds sex steroids (GSPS). Only about 1-2% of the total serum level of gestodene is in a free form, approximately 50-70% are specifically associated with GSPS. The relative distribution of fractions (free gestodene associated with albumin, associated with GSPS) depends on the concentration of GSPS in the serum. Following the induction of the binding protein, the fraction bound to the SHBG increases, while the free and bound albumin fraction decreases. The subsequent biotrapsformation is similar to the known metabolism of steroids. For gestodene, the apparent volume of distribution is 0.7 l / kg and the metabolic rate of serum clearance is about 0.8 ml / min / kg. There was no interaction when taking ethinyl estradiol. There is a two-phase decrease in the level of gestodene in serum. The terminal distribution phase is characterized by a half-life of about 12-15 hours.Gestodene is not excreted in unchanged form, only in the form of metabolites, which are eliminated with a half-life of about 1 day. Gestodene metabolites are excreted in urine and bile in a ratio of about 6: 4. The pharmacologically active metabolites of gestodene are not known. The serum level of SHBG, which increases about 3 times under the action of ethinyl estradiol, affects the pharmacokinetics of gestodene. With daily intake of the drug, an increase in the serum gestodene concentration is observed. Average serum levels are approximately 4 times higher when reaching an equilibrium concentration (usually reached during the second half of the cycle). Ethinyl estradiol After ingestion, ethinyl estradiol is rapidly and completely absorbed. Cmax of ethinyl estradiol in plasma, amounting to about 80 pg / ml is achieved in 1-2 hours. During the absorption and the first passage through the liver, a large part of ethinyl estradiol is metabolized. Absolute bioavailability is about 60%. About 98.5% of the serum level of ethinyl estradiol binds non-specifically to serum albumin. Ethinyl estradiol increases hepatic synthesis of SHBG (sex hormone binding globulin). For ethinyl estradiol, the apparent volume of distribution is approximately 5 l / kg. During absorption and the first passage through the liver, a large part of ethinyl estradiol is metabolized (mainly by hydroxylation). Metabolites are found both in free form and in the form of glucuronides and sulfates. The rate of metabolic clearance from plasma is about 5 ml / min / kg. There is a two-phase decrease in the level of ethinyl estradiol in the plasma, with a T1 / 2 final phase of about 24 hours. It is not excreted unchanged from the body. Ethinyl estradiol metabolites are excreted in the urine and bile in the ratio 4: 6 with T1 / 2 for about 1 day. The equilibrium concentration achieved after 3-4 days of intake was 40–60% higher than the concentration of ethinyl estradiol after a single dose. Nursing mothers have about 0.02% of the daily dose of ethinyl estradiol in the infant’s breast milk.
Indications
Contraception.
Contraindications
Femoden should not be applied in the presence of any of the conditions listed below. If any of these conditions develop for the first time in reception,the drug should be immediately canceled. 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 transit) ischemic attacks, angina pectoris) currently or in history. Migraine with focal neurological symptoms at present or in history of diabetes with vascular complications. Multiple or expressed risk factors th or arterial thrombosis, including valvular lesions, cardiac arrhythmia, cerebrovascular disease or coronary arteries of the heart; 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 grudyu.Povyshennaya sensitivity to any of the components of the drug Femoden
Precautionary measures
The drug should be kept out of the reach of children.
Use during pregnancy and lactation
Contraindication: pregnancy or suspicion of it, lactation.
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 usually starts 2-3 days after taking the last dragee and may not end before taking a new package. How to start taking Femoden If you are not taking any hormonal contraceptives in the previous month. Femoden starts on the first day of the menstrual cycle (t ae on the first day of menstrual bleeding).It is allowed to start taking on the 2-5 day 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 Femodene the next day after taking the last active drops from the previous package, but in no case later than the next day after the usual 7-day break (for preparations containing 21 pills) or after taking the last inactive One dragee (for preparations containing 28 pills in a package). When switching from contraceptives containing only gestagens (mini-drank, injection forms, implant), or from a progestogen releasing intrauterine contraceptive (Mirena). A woman can switch from mini- drank on Femoden any day (without a break), from the implant or intrauterine contraceptive with the progestogen - on the day of its removal, from the injection form - from the day when the next injection should be made. In all cases, you must 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 the drug immediately. If this condition is observed, the woman does not need additional contraceptive protection. After delivery or abortion in the second trimester of pregnancy. It is recommended to start taking the drug 21-28 days after delivery or abortion in the second trimester of pregnancy. If 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 lived sexually, pregnancy should be excluded before the start of Femodena, or it is necessary to wait for the first menstruation. Reception of missed dragees If the delay in taking the drug was less than 12 hours, contraceptive protection is not reduced. A woman should take dragee as soon as possible, the following is taken at the usual time. If the delay in taking the dragee is more than 12 hours, contraceptive protection can be reduced. In this case, you can follow the following two basic rules: The drug should never be interrupted,More than 7 days. 7 days of continuous receiving pills are required to achieve adequate suppression of the hypothalamic-pituitary-ovarian regulation. Accordingly, the following advice can be given if a delay in taking pills was more than 12 hours (the interval from the moment of taking the last tablet is more than 36 hours) : The first week of taking the drug A woman should take the last missed dragee as soon as possible, as soon as she remembers (even if it means taking two dragees at the same time). The following pills are taken at the usual time. Additionally, a barrier method of contraception (for example, a condom) should be used within the next 7 days. If sexual intercourse took place within a week before skipping dragees, it is necessary to take into account the probability of pregnancy. The more pills are missed, and the closer they are to a break in taking active substances, the greater the likelihood of pregnancy. The second week of taking the drug. A woman should take the last missed pill as soon as possible (even if it means taking two pills at the same time). The following pills are taken at the usual time. Provided that the woman took the pills correctly for 7 days preceding the first missed pills, there is no need to use additional contraceptive measures. Otherwise, as well as skipping 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 reducing the reliability of contraception is inevitable due to the upcoming break in taking the pills. A woman should strictly adhere to one of the following two options. Moreover, if in the 7 days preceding the first missed pills, all the pills were taken correctly, there is no need to use additional contraceptive methods. 1. A woman should take the last missed dragee as soon as possible, as soon as she remembers (even if it means taking two dragees at the same time). The next dragee is taken at the usual time until the dragee from the current package is finished. The next package should start immediately. Withdrawal bleeding is unlikely until the second package ends, but there may be spotting and breakthrough bleeding while taking pills. 2A woman can also interrupt the taking of pills from the current package. Then she should take a break for 7 days, including the day of skipping dragees, and then start taking a new package. If a woman misses pills, and then during a break in taking pills, she has no withdrawal bleeding, it is necessary to exclude pregnancy. Recommendations in case of vomiting and diarrhea. If the woman had vomiting or diarrhea within 4 hours after taking active pills, the absorption may not be complete and additional contraceptive measures should be taken. In these cases, you should focus on the recommendations when skipping dragees. Changing the day of the beginning of the menstrual cycle In order to delay the onset of menstruation, a woman must continue to take pills from the new Femoden package immediately after all pills from the previous one are taken, without interruption in reception. Drops from this new package can be taken as long as the woman wants (until the package ends). While taking the drug from the second package, a woman may have spotting or breakthrough uterine bleeding. Resume taking Femodena from the new pack should be after the usual 7-day break. In order to postpone the start of menstruation to another day of the week, a woman should be advised to speed up 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 in the future, there will be spotting and breakthrough bleeding while taking the second package (just as if she would like to delay the onset of menstruation).
Side effects
When taking combined oral contraceptives, irregular bleeding (spotting or breakthrough bleeding) may occur, especially during the first months of use. Against the background of combined oral contraceptive use, other adverse effects were observed in women. Organ system Often (> 1/100) Infrequently (> 1/1000 and <1/100) Rarely (<1/1000) Organ of vision contact lenses (discomfort with wearing them) Gastrointestinal nausea, abdominal pain vomiting, diarrhea Immune systems allergic reactionsGeneral symptoms weight gain weight lossMetabolism fluid retention Nervous system headache migraine Mental disorders mood decrease, mood swings Nia decreased libido increase libidoReproduktivnaya system and mammary gland breast pain,breast engorgement, breast hypertrophy, vaginal discharge, discharge from the breast, skin and subcutaneous tissues rash, urticaria, erythema nodosum, erythema multiformeAs with other combined oral contraceptives, thrombosis and thromboembolism may occur in rare cases
Overdose
No serious side effects from overdose have been reported. Symptoms that may occur in this case are: nausea, vomiting and, in young girls, slight vaginal bleeding. There is no specific antidote; symptomatic treatment should be carried out.
Interaction with other drugs
Drug interactions, which increase the clearance of sex hormones, can lead to breakthrough uterine bleeding or a decrease in contraceptive reliability. This has been established for hydantoins. barbiturates, primidone, carbamazepine and rifampicin; there is also a suspicion of oxcarbazepine, topiramate, felbamate and griseofulvin. The mechanism of this interaction is based on the induction of hepatic enzymes by these preparations. Contraceptive reliability is reduced when taking antibiotics such as ampicillins and tetracyclines. The mechanism of this action has not been elucidated. Women who receive any of the above short-course classes of drugs, in addition to Femoden, should temporarily use a barrier method of contraception during concomitant use of drugs and for 7 days after their withdrawal. When taking rifampicin and for 28 days after its cancellation, a barrier method of contraception (for example, a condom) should be used in addition to femoden. If the use of these drugs is started at the end of taking Femoden, the next pack should be started without the usual interruption in the reception. For women who receive these drugs for a long course, other (non-hormonal) methods of contraception should be recommended (for example, a condom).
special instructions
While taking an estrogen / gestagen combination, irregular bleeding (spotting or breakthrough bleeding) may occur, especially during the first months of use.Therefore, any irregular bleeding should be assessed only after an adaptation period of approximately three cycles. If irregular bleeding recurs or develops after previous regular cycles, non-hormonal causes should be considered and adequate diagnostic measures should be taken to exclude malignant neoplasms or pregnancy. They may include diagnostic curettage. In some women, withdrawal bleeding may not develop during a break in taking pills. If the drug was taken as directed, it is unlikely that the woman is pregnant. However, if pills were taken irregularly before or if there are no two menstrual bleeding in a row, pregnancy should be excluded before continuing to take the drug. If any of the conditions / risk factors listed below are present, then we should carefully weigh the potential risk and expected benefits of using Femoden in each individual case and discuss it with a woman before she decides to start taking the drug. In the case of weighting, amplification, or the first manifestation of any of the states or risk factors subsided, the woman should consult with her physician, who may decide on the need to discontinue the drug. when taking combined psroral contraceptives. Venous thromboembolism (VTE), in the form of deep vein thrombosis and / or pulmonary thromboembolism, can develop during the use of all combined psoral contraceptives. The approximate frequency of VTE in women taking moral contraceptives with a low dose of estrogen (less than 50 μg of ethinyl estradiol) is up to 4 per 10,000 women per year compared to 0.5–3 per 10,000 women per year in women who do not use OK. However, the incidence of VTE that develops when taking combined oral contraceptives is less than the frequency associated with pregnancy (6 per 10,000 pregnant women per year). For women taking combined oral contraceptives, extremely rare cases of thrombosis of other blood vessels are described, for example, renal, hepatic, mesenteric; veins and retinal arteries.The connection of these cases with the use of combined oral contraceptives has not been proven. A woman should stop taking the drug and consult a doctor if symptoms of venous or arterial thrombosis develop, which may include: unilateral pain in the leg and / or edema; sudden severe pain in the chest, with or without irradiation to the left hand; sudden shortness of breath; sudden coughing up any unusual, severe, prolonged headache; increased frequency and severity of migraine; sudden partial or complete loss of vision; diplopia; inarticulate speech or aphasia; dizziness; collapse with / or without partial seizure; weakness or a very significant loss of sensitivity, suddenly appearing on one side or in one part of the body; movement disorders; 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); (i.e., venous or arterial thromboembolism ever with close relatives or parents at a relatively young age); obesity (body mass index of more than 30 kg / m2); dyslipoproteinemia; arterial hypertension; valvular heart disease: - atrial fibrillation; - for 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 2 weeks after the end of immobilization. The increased risk of thromboembolism in the postpartum period should be considered. Circulatory disorders can also noted in diabetes, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, nonspecific ulcerative colitis, sickle cell anemia. Adequate treatment of these diseases can reduce the associated risk of thrombosis. Biochemical parameters that may indicate a predisposition to thrombosis include resistance to activated protein C (APC), hyperhomocysteinemia, antithrombin III deficiency, deficiency of protein C,Protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant). It should be noted that the risk of thrombosis during pregnancy is higher than when taking combined oral contraceptives. Tumors There was an increase in the risk of developing cervical cancer with prolonged use of combined oral contraceptives. research. His connection with the reception of combined oral contraceptives has not been proven. There are contradictions regarding the extent to which these cases are related to the characteristics of sexual behavior and other factors such as the human papillomavirus (HPV). Meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk (RR = 1.24) of breast cancer, diagnosed in women who at the time of the study used combined oral contraceptives. His connection with the reception of combined oral contraceptives has not been proven. The observed increase in risk may be due to an earlier diagnosis of breast cancer in women using combined oral contraceptives. In rare cases, against the background of the use of sex steroids, liver tumors developed. In case of severe abdominal pain, liver enlargement or signs of intra-abdominal bleeding, this should be taken into account when making a differential diagnosis. Other conditions Although a slight increase in blood pressure has been described in many women taking combined oral contraceptives, clinically significant increases were rarely observed. The relationship between taking combined oral contraceptives and arterial hypertension has not been established. However, if persistent arterial hypertension develops during their admission, it is advisable to cancel the combined oral contraceptives and to treat arterial hypertension. Reception can be continued if normal blood pressure values are achieved using antihypertensive therapy. The following conditions are broken down or worsened both during pregnancy and when taking combined oral contraceptives,but their association with the use of combined oral contraceptives has not been proven: jaundice and / or itching associated with cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; minor chorea (Sydengam disease); herpes pregnant; Hearing loss associated with otosclerosis. Acute or chronic abnormal liver function may require discontinuation of combined oral contraceptive use until the liver function returns to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous intake of sex steroids, requires discontinuation of combined oral contraceptives. Although combined oral contraceptives affect insulin resistance and glucose tolerance, it is usually not necessary to correct the dose of sugar-lowering drugs in patients with sugar patients, patients with sugar who do not have to correct sugar-lowering drugs in patients with sugar patients, patients who have sugar do not have to correct sugar-lowering drugs, glucose tolerance and glucose tolerance. taking these drugs. However, these women should be carefully monitored by a doctor. Women with hypertriglyceridemia, or a family history of her, cannot be ruled out by an increased risk of developing pancreatitis while taking combined oral contraceptives. Women with a tendency to chloasms while taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation. They sang in women suffering from hirsutism, the symptoms developed recently or significantly increased, managing differential diagnosis should take into account other causes, such as a tumor gene-producing nucleus, congenital adrenal cortex dysfunction. Laboratory tests Receiving combined oral contraceptives can affect the results of some laboratory tests, including indicators of liver function, kidney, thyroid, adrenal glands, the level of transport proteins in plasma, carbohydrate metabolism, coagulation parameters and fibrinolysis. Changes usually do not exceed the limits of normal values. Impact on the ability to drive vehicles and control mechanismsNo effects were observed.