Index of drugs

Oral contraception.

1 tabl friction contains 0.03 mg ethinyl estradiol and 0.075 mg gestodene. The product contains lactose and sucrose.

A complex oral contraceptive. The contraceptive effect is achieved thanks to the interaction of several different factors, the most important of which is inhibition of ovulation and cervical secretion. Following oral administration, Gestodene is rapidly and completely absorbed. After a single dose, it reaches the maximum concentration within 1 hour in the serum. Biological availability is about 99%. Gestodene is bound in the blood by albumin and by sex hormone binding globulin (SHBG). Only 1-2% of the total amount of Gestodene is in free serum, while 50-70% is specifically associated with SHBG. Under the influence of ethinylestradiol, the distribution of blood proteins changes as the concentration of SHBG increases. This leads to an increase in the fraction associated with SHBG and the reduction of the albumin-related fraction. Gestodene is completely metabolised by the known pathways of steroid metabolism. The decrease in the concentration of Gestodene in blood serum is two-fold. T_0,5 in the final elimination phase it is 12-15 h. Gestodene is not excreted unchanged. Its metabolites are excreted in urine and bile in a ratio of 6: 4. T_0,5 metabolites is about 1 day. Ethinylestradiol, taken orally, is rapidly and completely absorbed. The maximum serum concentration is reached within 1-2 hours. The total bioavailability resulting from pre-system conjugation and first pass effect is approximately 60%. Ethinylestradiol is mainly bound in a non-specific manner by albumin (around 98.5%) and causes an increase in serum SHBG. It is subject to pre-systemic conjugation in the mucosa of the small intestine and in the liver. Ethinyl estradiol is primarily metabolized by aromatic hydroxylation, but a variety of hydroxylated and methylated metabolites are formed that can be present in free form or in combination with a disulfonate or sulphate residue. The reduction of ethinyl estradiol concentration in the blood proceeds in a two-phase manner. T_0,5 drug in the final phase of elimination is 24 h. Ethinyl estradiol in unchanged form is not excreted, but its metabolites are excreted in the urine and bile in a ratio of 4: 6. T_0,5 metabolites is about 1 day.

Hypersensitivity to the active substances or to any of the excipients. Venous thromboembolism currently or in the past (deep vein thrombosis, pulmonary embolism), both in the absence and in the presence of risk factors. Arterial thromboembolic disorders present or in the past (myocardial infarction, cerebral circulation disorders) or prodromal symptoms (angina pectoris, transient ischemic attacks). Hereditary or acquired predisposition to venous or arterial thrombosis, such as: antithrombin deficiency, protein C deficiency, protein S deficiency, resistance to activated C protein, anti-phospholipid antibodies (anticardiolipid, lupus anticoagulant), hyperhomocysteinemia. Significant or numerous risk factors for arterial thrombosis. Severe hypertension. Diabetes complicated by micro- or macroangiopathy. Severe dyslipoproteinemia. Established or presumed hormone-dependent malignant tumors (e.g., genital organs, breast). At present or in the past severe liver dysfunction until normalization of liver function parameters. Mild or malignant liver cancer present or in the past. Bleeding from the genital tract of unknown cause. Migraine with focal neurological disorders.

The use of combined oral contraceptives increases the risk of venous thromboembolism. The risk is the highest in the first year of use in women who have not previously used combined oral contraceptives. Several epidemiological studies have found that the risk of venous thromboembolism is higher in women using ethinylestradiol-containing combined oral contraceptives, most commonly 30 μg, and progestagen as gestodene compared with women taking ethinyloestradiol-containing combined oral contraceptives at a dose below 50 μg and progestagen in the form of levonorgestrel. In women taking combined oral contraceptives, thrombosis in other vessels such as hepatic, mesenteric, renal or retinal vessels has been reported rarely; venous and arterial. It has not been unequivocally confirmed whether the occurrence of these cases is associated with the use of combined oral contraceptives.The risk of developing venous thromboembolism increases with: age; positive family history (eg venous thromboembolism in siblings or parents at a relatively young age) - if a hereditary propensity is suspected, refer to a specialist before using oral contraception; obesity (factor of over 30 kg / m)²); prolonged immobilization, major surgery, surgery involving lower limbs or severe trauma - in this case, use of oral contraceptives should be discontinued (in the case of elective surgery at least 4 weeks before surgery) and not introduced until at least 2 weeks after fully returning to moss activities; there is no unambiguous opinion on the possible relationship between varicose veins and superficial vein thrombosis and venous thromboembolism. The use of combined oral contraceptives is associated with an increased risk of heart attack or stroke. The risk of arterial thromboembolic disorders increases with: age; smoking cigarettes (this risk increases further with the amount of cigarettes smoked and with age, in particular in women over 35 years of age); dyslipoproteinemia; obesity (factor of over 30 kg / m)²); hypertension; the presence of a valvular heart defect; atrial fibrillation; positive family history (ie occurrence of arterial thrombosis in siblings or parents at a relatively young age) - in the case of suspected hereditary propensity, before making a decision about the use of any hormonal contraceptives, refer the patient to a specialist. The increased risk of venous thromboembolism during puerperium should be considered. Other illnesses associated with circulatory disorders include diabetes mellitus, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic inflammatory bowel diseases (Crohn's disease or ulcerative colitis) and sickle cell disease. Increasing the frequency or severity of migraine pain (which may be a symptom that heralds a cerebrovascular incident) may be an indication for immediate withdrawal of oral contraceptives. Biochemical indicators of congenital or acquired propensity to venous or arterial thrombosis are: resistance to activated protein C (APC), factor V (Leiden) mutations, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (anticardiolipin antibodies) , lupus anticoagulant). When considering the risk / benefit ratio, it should be taken into account that proper treatment of these disorders can reduce the risk of clotting and that the risk of pregnancy-related thrombosis is higher than that associated with the use of combined oral contraceptives. Some epidemiological studies have shown an increased risk of cervical cancer in women who have been using combined oral contraceptives for a long time, but it is still unclear to what extent this risk can be increased by sexual behavior and other factors such as human papillomavirus (HPV). In women taking combined oral contraceptives, there is a slightly increased relative risk of developing breast cancer, which gradually disappears within 10 years of stopping these preparations. In case of a woman taking a combined oral contraceptive, severe epigastric problems, enlargement of the liver or symptoms of bleeding within the abdominal cavity should be considered in the differential diagnosis of the possibility of liver cancer. In women with hypertriglyceridemia or a positive family history of taking combined oral contraceptives, the risk of pancreatitis may increase. In the case of acute or chronic liver failure, treatment should be discontinued until liver function is normalized. Patients with hepatic impairment may be compromised by the metabolism of steroid hormones. If persistent, clinically significant hypertension develops during the use of a combined oral contraceptive, discontinue administration and initiate antihypertensive therapy. Combined oral contraceptives can be re-included if this is indicated when the antihypertensive effect of the blood pressure is within normal limits.During pregnancy and during the use of combined oral contraceptives, the following diseases may develop or worsen (however, there is no clear association between their occurrence and the use of oral contraceptives): jaundice and / or pruritus in combination with cholestasis; development of gallstones, porphyria, systemic lupus erythematosus, haemolytic-uremic syndrome, Sydenhama chorea, herpes of pregnant women; hearing loss due to otosclerosis. Combined oral contraceptives can affect insulin resistance and Glucose tolerance - women with diabetes taking combined oral contraceptives should be under special control. The preparation contains lactose and sucrose - it should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption or rare hereditary fructose intolerance. Degradation of endogenous depression, epilepsy, Crohn's disease and ulcerative colitis has been observed with the use of combined oral contraceptives. Chloasma may occur when taking oral contraceptives, especially in women who have it during pregnancy. Women with this type of predisposition should avoid exposure to sunlight and ultraviolet radiation when using complex oral contraceptives. During the use of the preparation, herbal preparations containing St. John's wort should not be taken because of the risk of reducing the effectiveness of the preparation. The effectiveness of oral contraceptives can be reduced if tablets are missed, severe diarrhea or vomiting occurs, or when other medicines are taken simultaneously. When using all combined oral contraceptives, irregular bleeding (spotting or breakthrough bleeding) may occur, especially during the first months. Therefore, it is only after an adaptation period of about 3 cycles that the necessity to diagnose irregular bleeding may be considered. If irregular bleeding persists, the need for a combined oral contraceptive that contains higher doses of hormones should be considered. If irregular bleeding occurs after previous regular cycles, consider outside hormonal causes and perform appropriate diagnostic tests to exclude cancer or pregnancy. Occasionally, there may be no withdrawal bleeding during the tablet-free period.

It is not recommended to use the product during pregnancy. If pregnancy occurs while taking the preparation, the preparation should be stopped immediately. Epidemiological studies have not shown an increase in the risk of birth defects in children born to mothers taking combined oral contraceptives prior to pregnancy and have not demonstrated the teratogenic effect of combined oral contraceptives, which are unintentionally taken during pregnancy. Hormonal contraceptives can reduce the amount and change the composition of breast milk. Small amounts of contraceptive hormones and / or their metabolites can be excreted into human milk - hormonal contraceptives are not recommended during breastfeeding.

Common: headache, nervousness, eye irritation in people wearing contact lenses, blurred vision, nausea, acne, migraine, weight gain, fluid retention, irregular bleeding, lack of menstruation or skimpy periods, breast tenderness, libido changes, depression, irritability. Uncommon: vomiting, hyperlipidemia, hypertension. Rare: otosclerosis, cholelithiasis, chloasma, venous thromboembolism (deep veins or pelvis veins thrombosis and pulmonary embolism), lupus erythematosus, thromboembolic disorders of the arteries, changes in vaginal secretions. Very rare: chorea, pancreatitis. In women taking combined oral contraceptives, the following serious side effects have been reported: venous thromboembolism, i.e. deep vein thrombosis or pelvic thrombosis, and pulmonary embolism; thromboembolic disease of the arteries; liver cancer; chloasma. In women taking combined oral contraceptives, the incidence of breast cancer is slightly increased.

Oral: Tablets should be taken according to the order shown on the blister pack, daily, at the same time each day. You should take 1 tablet for 21 days. per day. Each subsequent blister pack should be started after a 7-day tablet-free interval during which the withdrawal bleed appears. This bleeding usually occurs on the 2nd or 3rd day after the last tablet has been taken and may last until the Next packet begins.Beginning of the preparation. No use of oral contraceptives in the last month: tablets should be started on the first day of the woman's natural menstrual cycle (ie on the 1st day of menstrual bleeding). You can also start taking tablets between the 2nd and 5th day of the cycle, but in this case it is recommended to use additional mechanical contraception for the first 7 days of taking the tablets during the first cycle.A change from another previously used combined oral contraceptive: the preparation should be started the day after the last tablet containing active substances from the previous packet of contraceptive pills - but no later than the day after the end of the break or the period of taking placebo tablets of the previous contraceptive.Change from previously used preparation containing only progestogen (tablets containing only progestogen, injections, implants, IOP system): changes from progestin-only tablets can be made each day. Take the first tablet the day after you take any of the progestagen tablets from the pack. When changing from an implant or IUS, the preparation should be started on the day the implant is removed. When changing from injections, the preparation should be taken on the day on which the next injection was to be made. In all these cases, it is recommended to use additional mechanical contraception for the first 7 days of taking tablets.After a miscarriage in the first trimester of pregnancy: taking tablets can be started immediately. In this case, no other contraceptive measures are necessary.After delivery or miscarriage in the second trimester of pregnancy: tablets should be started within 21-28 days after delivery, for women who are not breastfeeding or who have had a miscarriage in the second trimester. If the preparation is introduced later, it is recommended to use additional mechanical contraception for the first 7 days of taking tablets. If the patient has an intercourse before taking the tablets, pregnancy should be ruled out or the first menstrual bleeding should be expected.Proceeding in case of skipping tablets. If less than 12 hours have passed since the tablet was missed, the contraceptive effectiveness is maintained. Discard the missed tablet as soon as possible and continue taking the remaining tablets as usual. If it has been more than 12 hours since you missed the tablet, the contraceptive effectiveness may be reduced. You should then follow two rules: 1. The interval in taking tablets can not be more than 7 days. 2. The tablets should be taken continuously for 7 days in order to properly inhibit the hypothalamic-pituitary-cannabino axis.Skipping the tablet in the first week: take the missed tablet as soon as possible, even if it means taking 2 tablets at the same time. From now on, take the remaining tablets at the usual time. At the same time, mechanical contraceptive methods should be used for 7 consecutive days. If you have had sexual intercourse during the last 7 days, you should consider the possibility of pregnancy. The more tablets were missed and the closer to the 7-day interval in taking tablets, the higher the risk of getting pregnant.Skipping the tablet in the 2nd week: take the missed tablet as soon as possible, even if it means taking 2 tablets at the same time. From now on, take the remaining tablets at the usual time. If before the period of 7 days preceding the omission of the tablet were taken as directed, no additional contraceptive methods are necessary. Otherwise, or if more than one tablet is left out, the barrier method of contraception should be recommended for 7 days.Skipping the tablet in the third week: the risk of decreasing the effectiveness of contraception increases due to the impending break in taking tablets. However, reducing the effectiveness of contraception can be prevented by the appropriate dosage of tablets. If you choose one of the recommendations described below, there is no need for any additional contraceptive methods, provided that during the 7 days preceding the omission of the tablet, the preparation was taken correctly. If, however, within 7 days before skipping the tablet, the preparation was not taken correctly, you should follow recommendation No. 1 and use barrier methods of contraception for 7 days. 1. Take the missed tablet as soon as possible, even if it means taking 2 tablets at the same time. From now on, take the remaining tablets at the usual time. After taking the last tablet from the current package, start the next pack immediately, without taking a break in taking the tablets. Most likely, no withdrawal bleeding will occur until the next pack is completed. However, spotting or bleeding may occur during tablet taking. 2. You can also stop taking the tablets from the current pack. In this case, take a break for a period of 7 days (including days of skipping tablets) and then start taking the tablets from the new packaging. If, after skipping the tablet, you do not experience withdrawal bleeding during the first normal period of tableting, the possibility of pregnancy should be taken into account.Proceedings in cases of vomiting and / or diarrhea. If vomiting occurs within 3-4 hours of taking the tablet, the tablet may not be completely absorbed. In this case, the same recommendations as for omitting the tablets, described above, should be applied. If diarrhea is not extremely severe, it does not affect the absorption of combined oral contraceptives and there is no need for additional contraception. If severe diarrhea persists for 2 or more days, recommendations such as when tablets are missed are recommended. If a woman does not want to change the normal rhythm of taking tablets, she should take an extra tablet / tablet from another package.Proceedings to accelerate or delay the withdrawal bleeding. In order to delay the withdrawal bleeding, the next pack of the product should be started without a break in taking the tablets. You can delay the withdrawal bleeding for as long as necessary until the end of the second pack, but no longer. If you delay the onset of withdrawal bleeding, you may get spotting or bleeding. Regular use of the preparation should be restarted after maintaining the correct 7-day tablet-free interval. In order to move the withdrawal bleed to a different day of the week than it usually occurs using the current tablet intake regimen, it may be advisable to shorten the next tablet-free interval for as long as the withdrawal bleed is to be postponed. The shorter the break, the higher the risk that no withdrawal bleeding will occur, and bleeding in the middle of the cycle or spotting when taking the tablets from the next pack (as in the case of delaying the withdrawal bleeding).