Composition, form of production and packaging
The tablets covered with a cover of white color, the round form.
ethinylestradiol 30 Ојg
gestodene 75 mcg
Excipients: lactose monohydrate - 37.43 mg, corn starch - 15.5 mg, povidone 25,000 - 1.7 mg, sodium calcium edetate - 0.065 mg, magnesium stearate - 0.2 mg.
Sheath composition: sucrose - 19.66 mg, povidone 700,000 - 0.171 mg, macrogol 6000 - 2.18 mg, calcium carbonate - 8.697 mg, talc - 4.242 mg, wax mountain glycolide - 0.05 mg.
21 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
Low-dose monophasic oral contraceptive.
The contraceptive effect of Femodena is based on the interaction of various factors, the most important of which are inhibition of ovulation and a change 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 painful menstruation is observed less often. the intensity of bleeding decreases, resulting in a reduced risk of iron deficiency anemia.
Accepted orally gestoden quickly and completely absorbed. C max Gestodene in serum, equal to 4 ng / ml, is achieved through 1.0 h after ingestion. Absolute bioavailability of Gestodene is about 99% of the dose.
Gestodene is bound by serum albumin and globulin, which binds sex steroids (GSPC). Only about 1-2% of the total serum level of Gestodene is in free form, approximately 50-70% are specifically associated with the GSP. The relative distribution of fractions (free Gestodene, bound with albumin, associated with the GSPC) depends on the concentration of the GHS in the serum. Following the induction of the binding protein, the fraction associated with the GHS is increased, while the free and albumin bound fraction is reduced.
The subsequent biotransformation is similar to the known metabolism of steroids. For Gestodene, the apparent volume of distribution is 0.7 l / kg and the rate of metabolic clearance from serum is about 0.8 ml / min / kg. There was no interaction with simultaneous administration of ethinylestradiol.
There is a two-phase decrease in the serum Gestodene level. The terminal phase of the distribution is characterized by a half-life of about 12-15 hours. Gestodene is not excreted unchanged, only in the form of metabolites, which are eliminated with a half-life of about 1 day. Metabolites Gestodene excreted in urine and bile in a ratio of about 6: 4. Pharmacologically active metabolites of Gestodene are not known.
The pharmacokinetics of Gestodene is influenced by the serum level of GSH, which increases approximately 3-fold under the action of ethinyl estradiol. With daily intake of the drug, an increase in the concentration of Gestodene in the blood serum is observed. Mean serum levels are approximately 4 times higher when equilibrium concentration is reached (usually achieved during the second half of the cycle).
After ingestion, ethinylestradiol is rapidly and completely absorbed. C max ethinyl estradiol in plasma, about 80 pg / ml is achieved after 1-2 hours. During absorption and the first passage through the liver, a significant portion of ethinylestradiol is metabolized. Absolute bioavailability is about 60%.
About 98.5% of the serum level of ethinyl estradiol binds non-specifically to serum albumins. Ethinyl estradiol increases the hepatic synthesis of GSPC (globulin, binding sex steroids). For ethinylestradiol, the apparent volume of distribution is approximately 5 l / kg.
During absorption and the first passage through the liver, a significant portion of ethinyl estradiol is metabolized (mainly by hydroxylation). Metabolites are 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 plasma, with T 1/2 of the final phase about 24 hours. In unchanged form it is not excreted from the body. Metabolites of ethinyl estradiol are excreted in urine and bile in a ratio of 4: 6 with T 1/2 about 1 day. The equilibrium concentration reached after 3-4 days of admission was 40-60% higher than the concentration of ethinyl estradiol after a single dose.
In nursing mothers, about 0.02% of the daily dose of ethinylestradiol can enter the body of a child with breast milk.
Before applying Femodena, a woman should undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), and exclude pregnancy. In addition, violations of the blood coagulation system should be avoided.
Control examinations should be conducted at least once a year.
A woman should be warned that preparations of the type of Femodena do not protect against HIV infection (AIDS) and other sexually transmitted diseases!
Dragee should be taken in the order indicated on the package, every day at about the same time with a small amount of water. Take one pills a day continuously for 21 days. The admission of each next package begins after a 7-day break, during which withdrawal bleeding (menstrual-like bleeding) is observed. It usually begins on day 2-3 from the reception of the last dragee and may not end before the start of taking a new package.
If there is no reception of any hormonal contraceptives in the previous month, the use of Femodena begins on the first day of the menstrual cycle (ie on the first day of menstrual bleeding). It is acceptable to start taking the menstrual cycle on the 2nd-5th day, but in this case it is recommended to use the barrier method of contraception during the first 7 days of taking the pills from the first package.
When switching from combined oral contraceptives, it is preferable to start taking Femodena the day after receiving the last active pills from the previous package, but in no case later than the day after the usual 7-day suspension (for preparations containing 21 tablets) or after taking the last inactive dragee (for preparations containing 28 dragees in a package).
When switching from contraceptives containing only gestagens (minipillins, injection molds, implants), a woman can switch from a mini-drink to Femoden on any day (without interruption), from an implant - on the day of removal, from the injection form - from the day. when the next injection would be 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, a woman can start taking the medicine immediately. If this condition is met, the woman does not need additional contraceptive protection.
After childbirth or abortion in the second trimester of pregnancy, a woman should be recommended to start taking the medication on the 21-28th day after childbirth 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 the pills. However, if a woman already had sex, prior to the start of taking Femodena, pregnancy should be excluded or it is necessary to wait for the first menstruation.
Acceptance of missed pills
If the delay in taking the pills is less than 12 hours, the contraceptive protection does not decrease. The woman should take the pills as soon as possible, the next dragee is taken at the usual time.
If the delay r is more than 12 hours, contraceptive protection may be reduced. In this case, you can follow the following two basic rules:
- the reception of a dragee should never be interrupted, for more than 7 days;
- 7 days of continuous reception of pills are required to achieve adequate suppression of the hypothalamic-pituitary-ovarian axis.
Accordingly, the following tips can be given if the delay in taking the dragees was more than 12 hours (the interval from the last dragee was more than 36 hours):
The first and second week of taking the drug
The woman should take the last missed dragee as soon as possible, as soon as she remembers (even if it means taking two pills simultaneously). The next dragee is taken at the usual time. In addition, a barrier method of contraception (for example, a condom) should be used for the next 7 days. If sexual intercourse took place within a week before skipping the dragees, the probability of pregnancy should be taken into account. The more pills are missed, and the closer this pass to the 7-day break in taking the pills, the higher the risk of pregnancy.
The third week of taking the drug
The woman should take the last missed dragee as soon as possible, as soon as she remembers (even if it means taking two pills simultaneously). The next dragee is taken at the usual time. In addition, a barrier method of contraception (for example, a condom) should be used for the next 7 days. In addition, the reception of a dragee from a new package should be started as soon as the current packaging is finished, i. E. nonstop. Most likely, the woman will not have withdrawal bleeding until the end of the second package, but she may have spotting spotting or breakthrough uterine bleeding on the days of taking the pills.
If the woman missed taking the pills, and then in the first normal drug-free interval, she does not have withdrawal bleeding, it is necessary to exclude pregnancy.
If a woman had vomiting within 3 to 4 hours after taking the Femodena pellet, the absorption may be incomplete. In this case, it is necessary to be guided by the advice on skipping the dragees. If a woman does not want to change the normal mode of taking the drug, she should take, if necessary, an additional pellet (or several pills) from another package.
In order to delay the onset of menstruation , a woman should continue taking the dragee from a new package of Femodena immediately after taking all the pills from the previous one, without interruption in admission. Dragee from this new package can be taken for as long as the woman wishes (until the packaging is finished). Against the background of taking the drug from the second package, a woman may have spotting or breakthrough uterine bleeding. To resume taking Femodena from the new package follows the usual 7-day break.
In order to transfer the day of the onset of menstruation on the next day of the week , the woman should shorten the nearest break in taking the dragees for as many days as she wants. The shorter the interval, the greater the risk that it will not have withdrawal bleeding and, in the future, there will be macular bleeding and breakthrough bleeding at the time of taking the second package (as well as in the case where she would like to delay the onset of menstruation).
The following undesirable effects were described in women taking Femoden, and their relationship with the drug was neither confirmed nor disproved: engorgement, tenderness of the mammary glands, secretion of secretions from them; headache; migraine; change in libido; decreased mood; poor tolerance of contact lenses; nausea; vomiting; changes in vaginal secretion; various skin reactions; fluid retention; change in body weight; hypersensitivity reactions.
Sometimes chloasma can develop, especially in women with a history of pregnancy chloasma.
Combined oral contraceptives should not be used in the presence of any of the conditions listed below. If any of these conditions develop for the first time against the background of the drug, the drug should be immediately withdrawn.
- presence of thromboses (venous and arterial) at present or in the anamnesis (for example, thrombosis of deep veins, thromboembolism of the lungs, myocardial infarction, cerebrovascular disorders);
- Availability at present, or in the history of conditions preceding thrombosis (eg, transient ischemic attacks, angina pectoris);
- diabetes mellitus with vascular complications;
- the presence of severe or multiple risk factors for venous or arterial thrombosis may also be considered a contraindication;
- the present or a history of jaundice or severe forms of liver disease (until liver tests are normal);
- the presence, at present or in the past, of liver tumors (benign or malignant);
- identified hormone-dependent malignant diseases of genital organs or mammary glands or suspected of them;
- vaginal bleeding of unknown origin;
- Pregnancy or suspicion of it;
- hypersensitivity to any of the components of Femodena.
PREGNANCY AND LACTATION
Contraindication: pregnancy or suspicion of it, lactation period.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: severe forms of liver disease (until liver tests are normal).
When taking an estrogen / progestogen combination, irregular bleeding (spotting or breakthrough bleeding) can 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 is repeated or develops after previous regular cycles, then nonhormonal causes should be considered and adequate diagnostic measures taken to exclude malignant neoplasms or pregnancy. These can include diagnostic scraping.
In some women, bleeding cancellations may not develop during a break in taking a dragee. If the drug was taken as directed, it is unlikely that a woman is pregnant. Nevertheless, if before this, the pills were taken irregularly or, if there are no consecutive menstrual bleeding, the pregnancy should be excluded before the drug is continued.
If any of the conditions / risk factors outlined below are present, carefully weigh the potential risk and expected benefits of using Femodena in each individual case and discuss it with the woman before she decides to start taking the drug. In case of weighting, strengthening or the first manifestation of any of the died down states or risk factors, a woman should consult her doctor who can decide whether to cancel the drug.
Diseases of the cardiovascular system
A number of epidemiological studies have revealed a slight increase in the incidence of venous and arterial thrombosis and thromboembolism in the use of combined oral contraceptives.
Venous thromboembolism (VTE), in the form of deep vein thrombosis and / or pulmonary thromboembolism, can develop during use of all combined oral contraceptives. The estimated incidence of VTE in women taking oral contraceptives with a low estrogen dose (less than 50 Ојg ethinylestradiol) 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 OC. However, the frequency of VTE developing with combined oral contraceptives is less than the frequency associated with pregnancy (6 per 10 000 pregnant women per year).
Women receiving combined oral contraceptives describe extremely rare cases of thrombosis of other blood vessels, for example, renal, hepatic, mesenteric; veins and arteries of the retina. The relationship 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 when developing symptoms of venous or arterial thrombosis, which may include: unilateral leg pain and / or swelling; sudden severe pain in the chest, with irradiation in the left arm or without irradiation; sudden shortness of breath; a sudden attack of coughing; any unusual, strong, prolonged headache; increased frequency and severity of migraine; sudden partial or complete loss of vision; Diplomacy; slurred speech or aphasia; dizziness; collapse with or without partial seizure; weakness or very significant loss of sensitivity, suddenly appeared on one side or in one part of the body; motor disorders; "sharp" abdomen.
The risk of thrombosis (venous and / or arterial) and thromboembolism increases:
- with age;
- for smokers (with an increase in the number of cigarettes or an increase in age, the risk further increases, especially in women older than 35 years);
in the presence of:
- family history (ie venous or arterial thromboembolism ever in close relatives or parents at a relatively young age);
- obesity (body mass index more than 30 kg / m 2 );
- arterial hypertension;
- heart valve diseases:
- Atrial fibrillation;
- prolonged immobilization, serious surgical intervention, any foot surgery or extensive trauma. In these situations, it is desirable to discontinue the use of combined oral contraceptives (in case the intended operation of at least four weeks prior to it) and not to resume reception at 2 weeks after the immobilization.
It should take into account the increased risk of thromboembolism during the postpartum period.
Circulatory disorders as may occur in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis nsspetsificheskom, sickle-cell anemia. Adequate treatment of these diseases can reduce the associated risks of thrombosis.
Biochemical parameters that may indicate a predisposition to thrombosis include resistance to activated protein C (APC), hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein deficit S, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).
It should be borne in mind that the risk of thrombosis during pregnancy is higher than when taking combined oral contraceptives.
An increased risk of cervical cancer in long-term use of combined oral contraceptives has been reported in some epidemiological studies. His connection with the reception of combined oral contraceptives has not been proved. Saved controversy as to the extent to which these cases are related to the characteristics of sexual behavior and other factors such as human papilloma virus (HPV).
A 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 are at the time of the study have used combined oral contraceptives. His connection with the reception of combined oral contraceptives has not been proved. The observed increase in risk may be due to early diagnosis of breast cancer in women using oral contraceptives combined.
In rare cases, against application of sex steroids observed the development of liver tumors. In case of severe pain in the abdomen, liver enlargement or signs of intra-abdominal bleeding it should be considered in the differential diagnosis.
Although small increases in blood pressure have been reported in many women taking COCs, clinically relevant increases were rare. The relationship between the reception of combined oral contraceptives and hypertension has not been established. However, if at the time of their admission develops resistant hypertension, suitable cancellation peroralnyh combined contraceptives and treatment of hypertension. The reception can be continued, if using antihypertensive therapy achieved normal blood pressure values.
The following states are broken or worsen both during pregnancy and when taking combined oral contraceptives, but their connection with the reception of combined oral contraceptives has not been proven: jaundice and / or pruritus related to cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; chorea (Sydenham's disease); herpes gestationis; hearing loss associated with otosclerosis.
Acute or chronic disturbances of liver function may require discontinuation of combined oral contraceptives, as long as liver function tests have not returned to normal. Recurrent cholestatic jaundice that develops for the first time during pregnancy or previous use of sex steroids, requires discontinuation of COCs.
Although COCs affect the tissues to insulin resistance and glucose tolerance, usually not necessary to correct dose of antidiabetic drugs in diabetics taking these drugs. However, these women should be under close medical supervision.
Women with hypertriglyceridemia, or a family history of it, we can not exclude an increased risk of developing pancreatitis while taking combined oral contraceptives.
Women with a tendency to hloazms while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation.
Sang in women suffering from hirsutism, symptoms, or developed recently increased significantly, in the differential diagnosis should take into account other factors such as au core gene producing tumor, congenital adrenal hyperplasia.
Receiving COCs can affect the results of some laboratory tests including liver function tests, renal, thyroid, adrenal gland, the level of transport proteins in plasma, carbohydrate metabolism, coagulation parameters and fibrinolysis. Changes do not usually go beyond the normal range.
Impact on the ability to drive vehicles and manage mechanisms
There were no effects.
No serious side effects have been reported with overdose.
Symptoms that may occur in this case: nausea, vomiting and, in young girls, slight vaginal bleeding.
There is no specific antidote; should be symptomatic treatment.
Drug interactions that result in increased clearance of sex hormones can lead to breakthrough uterine bleeding or reduce the contraceptive reliability. It was established in respect of hydantoins. barbiturates, primidone, carbamazepine and rifampicin; also there is a suspicion in respect of oxcarbazepine, topiramate, felbamate and griseofulvin. The mechanism of this interaction is based on the induction of these preparations of liver enzymes.
Contraceptive reliability is reduced when taking antibiotics such as ampicillin and tetracycline. This mechanism of action has not been elucidated.
Women treated with any of the above classes of drugs short course, in addition to Femodenu must temporarily use a barrier method of contraception during the concomitant drug administration and for 7 days after their withdrawal. While receiving rifampicin and 28 days after its cancellation in addition to Femodenu should be used a barrier method of contraception (e.g., condom). If the application of these drugs was started in the receiving end Femoden package next pack should be started without a normal break in reception.
Women receiving long course these drugs to recommend other (hormonal) contraceptive methods (such as a condom).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children. Shelf life - 5 years.