Index of drugs

Oral contraception.

1 tabl powl. contains 3 mg drospirenone and 0.02 mg ethinyl estradiol. The product contains lactose and soy lecithin.

A complex oral contraceptive. The contraceptive effect of the preparation is based on the interaction of several factors, the most important of which is inhibition of ovulation and changes in the endometrium. Following oral administration, drospirenone is rapidly and almost completely absorbed. After a single administration, the maximum serum concentration occurs after 1-2 h. The bioavailability is 76-85%. Final T_0,5 is 31 h. Drospirenone binds to blood serum albumin, but does not bind to sex hormone binding globulins (SGHB) and corticoid binding globulin (CBG). Only 3-5% of the total active substance concentration in the serum is free. The increase in serum SHGB concentration due to ethinylestradiol does not affect the binding of drospirenone to proteins. After oral administration, drospirenone undergoes rapid metabolism. Both main metabolites of drospirenone are formed without the involvement of the cytochrome P450 system. Drospirenone is slightly metabolised by cytochrome P450 3A4; in conditionsin vitro demonstrated the ability of drospirenone to inhibit this enzyme and the following cytochromes: CYP1A1, CYP2C9 and CYP2C19. Only trace amounts of drospirenone are excreted unchanged. Drospirenone metabolites are excreted in the faeces and urine in a ratio of approximately 1.2-1.4. T_0,5 metabolite excretion is about 40 h. Ethinylestradiol is rapidly and completely absorbed after oral administration. After a single dose of the drug, the maximum concentration of the drug occurs after about 1-2 hours. Ethinyl oestradiol is subject to the first-pass effect, which shows high individual variability. The absolute bioavailability is about 60%. Plasma protein binding is approximately 98%. Ethinylestradiol induces hepatic synthesis of SHBG, is completely metabolised. There is virtually no excretion of ethinyl estradiol unchanged. Metabolites are excreted with urine and bile in a ratio of 4: 6. T_0,5 metabolites in the phase of excretion is about 1 day.

Hypersensitivity to the active substances or to any of the excipients. Venous thrombosis currently or in history (deep vein thrombosis, pulmonary embolism). Arterial thrombosis presently or historically present (eg myocardial infarction) or prodromal symptoms (eg angina pectoris, transient seizures of cerebral ischemia). Vascular stroke now or in an interview. The presence of a serious risk factor or many risk factors for arterial thrombosis: diabetes with vascular lesions, severe hypertension, severe dyslipoproteinaemia. Inherited or acquired predisposition to venous or arterial thrombosis, such as resistance to activated C protein, antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia, antiphospholipid antibodies (anti-cardiolipin antibodies, lupus anticoagulant). Pancreatitis associated with severe hypertriglyceridemia, present or in history. Severe liver disease now or in history until the results of liver function tests return to normal. Severe or acute renal failure. Current or past liver cancer (benign or malignant). Occurrence or suspicion of a malignant tumor dependent on sex hormones (e.g., reproductive organs or breasts). Bleeding from the vagina of undetermined etiology. Migraine with focal neurological symptoms in an interview.

The use of a combined oral contraceptive carries an increased risk of venous thromboembolism (VTE). The highest risk of VTE occurring during the first year of application. There is a connection between the use of combined oral contraceptives and an increased risk of arterial thromboembolism (myocardial infarction, transient ischemic attack). Extremely rarely reported is the occurrence of thrombosis in other blood vessels, for example in the vessels of the liver, mesentery, kidney, cerebral or veins and retinal arteries.The risk of venous thromboembolism in women using combined oral contraceptives increases with: age; a positive family history (VTE with siblings or parents at a relatively young age) - if genetic predisposition is suspected, a woman should be referred to a specialist before consulting the use of oral contraceptives; prolonged immobilization, large surgical procedures, any lower extremity surgery or severe trauma - in these cases it is recommended to discontinue the use of tablets (in the case of planned surgery it is recommended to stop contraception for 4 weeks before the procedure), re-use can start at the earliest 2 weeks after the patient regains her ability to move, if taking oral contraceptives is not interrupted, anticoagulation should be considered; obesity (body mass index above 30 kg / m²); lack of unanimity regarding the role of varicose veins and thrombophlebitis of superficial veins in the initial stage or development of venous thrombosis. The risk of arterial complications of thromboembolism or cerebrovascular accident in women using combined oral contraceptives increases with: age; smoking (cigarette smoking is strongly discouraged for women over 35 years of age); dyslipoproteinemia; hypertension; migraine; obesity (body mass index above 30 kg / m²); positive family history (arterial thromboembolism in siblings or parents at a relatively young age) - if genetic predisposition is suspected, the woman should be referred to a specialist before consultation with the oral contraceptive. valvular heart disease; atrial fibrillation. The presence of one serious or several risk factors for venous or arterial disease may also be a contraindication. Anticoagulation should be considered. If a thrombosis is suspected or diagnosed, the use of a combined oral contraceptive should be discontinued. The increased risk of thromboembolic events during the postpartum period should be considered. Other medical conditions that have been associated with vascular adverse events are: diabetes, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic enteritis (Crohn's disease or ulcerative colitis) and sickle cell disease. Increasing the frequency or severity of migraine attacks during the use of combined oral contraceptives (which may be a prodromal symptom of cerebrovascular events) may be the reason for immediate withdrawal of combined oral contraceptives. In some epidemiological studies, an increased risk of cervical cancer has been observed in women over a long time (over 5 years) using combined oral contraceptives, but it is not known to what extent these effects are influenced by sexual behavior and other factors such as human papillomavirus (HPV). There is a slightly increased risk of breast cancer in women taking combined oral contraceptives. This risk gradually disappears within 10 years after discontinuation of combined oral contraceptives. If there is a severe epigastric pain, enlargement of the liver or symptoms of abdominal bleeding in women taking combined oral contraceptives, the possibility of liver cancer should be considered in the differential diagnosis. The progestogen component in the preparation is an aldosterone antagonist with potassium-sparing properties. In most cases, an increase in potassium in the blood should not be expected. In some patients with mild to moderate renal impairment who were also taking potassium-sparing drugs, a slight but insignificant increase in serum potassium was observed when taking drospirenone - monitoring of serum potassium during the first course of treatment in patients with renal insufficiency and potassium starting to use the product near the upper limit of normal, especially when concomitant use of potassium-sparing drugs.In women with hypertriglyceridemia or a positive family history of hypertriglyceridemia, there may be an increased risk of pancreatitis when taking combined oral contraceptives. If the use of combined oral contraceptives in women with pre-existing hypertension has a continuous or significant increase in blood pressure not responding to antihypertensive therapy, discontinuation of combined oral contraceptives is necessary. In justified cases, if the blood pressure value has been normalized during antihypertensive therapy, the use of combined oral contraceptives can be restarted. The following conditions have been reported or worsening both during pregnancy and during the use of combined oral contraceptives, however their relationship with the use of combined oral contraceptives has not been confirmed: jaundice and / or pruritus associated with cholestasis; cholelithiasis; porphyria; systemic lupus erythematosus; haemolytic-uremic syndrome; Sydham's chorea; herpes of pregnant women; hearing loss associated with otosclerosis. In women with hereditary angioedema, exogenous estrogens may cause or exacerbate the symptoms of angioedema. Acute or chronic liver problems may necessitate discontinuation of combined oral contraceptives until liver function parameters return to normal. Recurrence of cholestatic jaundice and / or pruritus associated with bile stasis, which previously occurred earlier during pregnancy or during earlier use of sex hormones requires discontinuation of combined oral contraceptives. Although combined oral contraceptives may have an effect on insulin resistance of peripheral tissues or on Glucose tolerance, there is no evidence of a need to change the treatment regimen for the treatment of diabetes. Diabetic patients should be monitored constantly, especially during the initial period of using oral contraceptives. Combinations of endogenous depression, epilepsy, Leśniowski-Crohn's disease and ulcerative colitis have been reported with the use of combined oral contraceptives. Chloasma may occur occasionally, especially in women who have had chloasma gravid in the past. Women with a tendency to chloasma should avoid exposure to sunlight or ultraviolet light when using oral contraceptives. The preparation contains lactose - should not be used by patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. The product contains lactose - should not be used by patients with hypersensitivity to peanut or soya. The efficacy of combined oral contraceptives can be reduced in the case of eg omission of the tablet, gastrointestinal disorders or concomitant use of other drugs. When using a combined oral contraceptive, irregular bleeding (spotting or bleeding) may occur, especially in the first months of using the tablets. Therefore, the assessment of irregular bleeding is of significance only after the adaptation period lasting about 3 cycles. If irregular bleeding persists or occurs after previous regular cycles, non-hormonal reasons should be considered and appropriate diagnostic tests performed to exclude malignancy or pregnancy. These tests may include curettage of the uterine cavity. In some women, withdrawal bleeding may not occur during tablet interruption.

The preparation is not indicated for use during pregnancy. If a woman becomes pregnant while using the preparation, it should be immediately discontinued. The results of epidemiological studies show neither an increased risk of congenital malformations in children born by women using COCs before pregnancy, nor a teratogenic effect if they are unintentionally administered during pregnancy. Combined oral contraceptives can affect lactation, reducing the amount and changing the composition of breast milk. Therefore, generally, they should not be prescribed until the child is completely withdrawn from the breast.Small quantities of contraceptive steroids and / or their metabolites may be secreted in breast milk of women using combined oral contraceptives. Such amounts can affect the child.

Common: emotional instability, headache, abdominal pain, acne, breast pain, breast enlargement, breast tenderness, dysmenorrhea, bleeding unrelated to the menstrual cycle, weight gain. Uncommon: candidosis, herpes infection, allergic reactions, increased appetite, depression, nervousness, sleep disorders, paresthesia, dizziness, visual disturbances, additional spasms, tachycardia, pulmonary embolism, hypertension, migraine, varicose veins, pharyngitis, nausea, vomiting, gastroenteritis, diarrhea, constipation, gastrointestinal disorders, angioedema, alopecia, eczema, pruritus, rash, dry skin, seborrhea, skin disorders, neck pain, limb pain, muscle spasms, breast cancer, fibrous dysplasia cystic breast, mycotoxicity, ovarian cyst, hot flushes, menstrual disorders, amenorrhoea, excessive menstrual bleeding, vaginal candidiasis, vaginitis, vaginal discharge, diseases of the vulva and vagina, vaginal dryness, pelvic pain, abnormal cytological picture of the smear in the classification Papanicolaou, decreased libido, edema, weakness No, pain, excessive thirst, increased perspiration, weight loss. Rare: asthma, hearing loss, thromboembolism, erythema nodosum, erythema multiforme. In women taking combined oral contraceptives, the following serious adverse reactions have been reported: venous and arterial thromboembolism, hypertension, liver cancer, chloasma, acute or chronic hepatic impairment (requiring discontinuation of a combined oral contraceptive in some cases until the parameters return liver to normal). The occurrence or deterioration of disease states for which the connection with the use of combined oral contraceptives is not clear: Crohn's disease, ulcerative colitis, epilepsy, myoma, porphyria, systemic lupus erythematosus, herpes simplex, Sydenhama chorea, haemolytic-uremic syndrome , cholestatic jaundice. In women with an inherited propensity to angioneurotic edema, exogenous oestrogens may cause or worsen symptoms of angioedema. In women who take hormonal contraceptives, breast cancer is diagnosed slightly more often (however, the causal relationship with the use of combined oral contraceptives is unknown).

Orally. The tablets should be taken daily, at about the same time, in the order indicated on the blister, with a small amount of liquid if necessary. For 21 consecutive days, one table should be accepted. per day. Each subsequent pack should be started after a 7-day tablet-free break, during which time the withdrawal bleed usually occurs. The withdrawal bleed usually starts in 2 -3. the day after taking the last tablet and may not finish before the Next packet begins.Beginning of the preparation. No hormonal contraception last month: taking tablets should begin on the first day of the natural menstrual cycle (ie on day 1 of menstrual bleeding).A change from a combined hormonal contraceptive (combined oral contraceptive, therapeutic vaginal system or transdermal patch, patch): the woman should start the treatment, preferably on the day following the last active tablet (the last tablet containing active substances) of the previous combined oral contraceptive, but no later than the following day after the usual break in taking the tablets or after taking the placebo tablets of the previously used combined oral contraceptive. If a therapeutic vaginal system or patch is used, a patch should be started on the day the previous contraceptive is removed, but at the latest on the next day of use of the previously used preparation.Change from the progestagen only method (tablets containing only progestin, injections, implants or an IAS): a woman can start using the product after using progestin-only pills on any day (if she used the implant or IUS on the day of removal and if injections) the day on which the next injection should be administered). In all these cases, however, the patient should be advised to additionally use a mechanical method of contraception during the first 7 days of taking the tablets.After a miscarriage in the first trimester of pregnancy: the woman can start taking the tablets immediately; no additional contraceptive methods are necessary.After delivery or after a miscarriage in the second trimester of pregnancy: the patient should be advised to start using the product from day 21 to day 28 after childbirth or abortion in the second trimester of pregnancy. If the patient starts using the product later, it should be advised to use additional mechanical contraception during the first 7 days of taking the tablets. If you have already had a relationship before taking a combined oral contraceptive, you must either have a pregnancy or wait for your first menstrual bleeding.Proceeding in case of skipping tablets. If less than 12 hours have passed since the planned adoption of any of the tablets, contraceptive protection is not reduced. The woman should take the missed tablet as soon as she remembers it and take the next tablet at the usual time. If more than 12 hours have passed since the planned adoption of any tablet, contraceptive protection may be reduced. If you miss the tablets, you must follow the following two basic principles: 1. Never stop using the tablets for more than 7 days. 2. Appropriate inhibition of the hypothalamo-pituitary-ovary axis is obtained after 7 days of continuous taking of tablets.If you miss a tablet in the first week: the woman should take the last missed tablet as soon as she remembers it, even if it means taking 2 tablets at the same time. Then, continue taking your tablets at the usual time. In addition, she should use a mechanical method of contraception, e.g. a condom, for the next 7 days. If there has been a relationship within the previous 7 days, the possibility of pregnancy should be considered. The more tablets are missed and the shorter the time between their omission and the regular tablet-free interval, the greater the risk of getting pregnant.If you miss a tablet in the 2nd week: the woman should take the last missed tablet as soon as she remembers it, even if it means taking 2 tablets at the same time. Then, continue taking your tablets at the usual time. If within 7 days before skipping the first tablet, the woman took the tablets correctly, no additional contraceptive measures are necessary. However, if the patient forgot to take more than 1 tablet, it should be advised to use an additional method of contraception for 7 days.If you miss a tablet in the third week. There is a high risk of contraception being reduced due to the upcoming 7-day tableting interval. However, by adjusting the tablet intake regimen, it is possible to prevent the contraceptive effect from being reduced. Using one of the following two options means that you do not need to use additional methods of contraception, provided that all tablets were taken correctly for 7 days before skipping the first tablet. Otherwise, the patient should be advised to use the first of the two options and that for the next 7 days she should use an additional method of contraception. 1. A woman should take her last missed tablet as soon as she remembers, even if it means taking 2 tablets at the same time. Then, she should continue taking the tablets at the usual time. You should immediately start taking the tablets from the next blister pack without taking a break between the packages. Until the end of the use of the tablets from the second pack, withdrawal bleeding should not occur, however, during the days when the woman takes the tablets, spotting or bleeding may occur. 2.You can also advise a woman to stop taking the tablets from the current packaging. She should stop taking the tablets for 7 days, including the days she missed the tablets, and then continue taking the tablets from the next pack. If the patient has missed several tablets and there is no withdrawal bleeding during the first normal tableting interruption, the possibility of pregnancy should be considered.Recommendations in the case of gastrointestinal disorders. In case of severe gastrointestinal disturbances (eg vomiting and diarrhea), the absorption of the preparation may not be complete and additional contraceptive methods should be used. If vomiting occurs within 3-4 hours after taking the tablet, immediately take a new (additional) tablet. If possible, take a new tablet within 12 hours of the usual time of taking the tablet. If more than 12 hours have elapsed, recommendations for omitting the tablet should be taken. If a woman does not want to change her current tablet schedule, she should take the additional tablet (s) from another pack.Proceedings to delay the withdrawal bleeding. To delay the onset of menstruation, the woman should start using the tablets from the next pack of the product, without interruption in taking the tablets. The use of tablets can continue for as long as necessary until the end of the second package. During the extended cycle, intracyclic bleeding or spotting may occur. You should return to regular use after a normal 7-day break without tablets. If a woman wants to change her day of bleeding to a different day of the week than the current one, she can be advised to shorten the next break without tablets for any number of days. The shorter the break, the greater the risk that there will be no withdrawal bleeding and there will be bleeding or staining during the use of the tablets from the next pack (just as in the case of delaying the menstrual period).