Index of drugs

Oral contraception. The decision to prescribe the preparation should be made on the basis of an individual assessment of risk factors in women, in particular the risk of venous thromboembolism and the risk of venous thromboembolism associated with the use of the preparation in relation to other combined hormonal contraceptives.

1 tabl contains 3 mg drospirenone and 0.03 mg ethinyl estradiol. The preparation contains lactose.

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 45%. 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. Occurrence or risk of venous thromboembolism (VTE): venous thromboembolism - active (treated with anticoagulants) or history of venous thromboembolism, e.g. deep vein thrombosis (DVT), pulmonary embolism (PE); known hereditary or acquired predisposition for venous thromboembolic disease, eg resistance to active C protein (APC) (including Leiden V factor) antithrombin III deficiency, protein C deficiency, protein S deficiency; extensive surgery associated with long-term immobilization; high risk of venous thromboembolism due to multiple risk factors. Occurrence or risk of arterial thromboembolism (ATE): arterial thromboembolic events - active (eg myocardial infarction) or prodromal symptoms (eg angina pectoris); cerebrovascular diseases - active stroke, previous stroke or prodromal symptoms (eg transient ischemic attack TIA); confirmed hereditary or acquired tendency to occur in arterial thromboembolic disorders, eg hyperhomocysteinemia and the presence of anti-phospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant); migraine with focal neurological symptoms in an interview; high risk of arterial thromboembolic events due to the presence of multiple risk factors or the presence of one of the major risk factors, such as: diabetes with vascular complications, severe hypertension, severe dyslipoproteinaemia. Cerebrovascular incident present or in the past.Pancreatitis or its presence in the past if associated with the occurrence of acute hypertriglyceridemia. Current or previous acute hepatic failure until the liver parameters return to normal. Severe or acute renal failure. A liver tumor (benign or malignant) present or present. Diagnosed or suspected malignant tumors (such as reproductive organs or breasts) dependent on sex hormones. Bleeding from the genital tract of undetermined etiology.

The use of combined hormonal contraceptives is associated with an increased risk of venous thromboembolism compared to when the therapy is not used. The use of preparations containing levonorgestrel, norgestimate or norethisterone is associated with the lowest risk of venous thromboembolism. The use of other preparations such as Asubtela may be associated with a 2-fold greater risk. The decision to use the preparation from outside the lowest risk of venous thromboembolism should only be made after talking to the patient to ensure that she understands the risk of venous thromboembolism associated with the preparation, how current risk factors affect this risk and that the risk of venous thromboembolism is the highest in the first year of use. There is also some evidence that the risk is increased when combined hormonal contraceptives are taken again after an interruption of 4 weeks or more. Epidemiological studies have shown that the risk of VTE for oral contraceptives containing drospirenone is greater than for levonorgestrel-containing contraceptives (so-called 2nd generation contraceptives) and may be similar to the risk for agents containing desogestrel / gestodene (so-called third generation contraceptives). In patients taking combined oral contraceptives, cases of thrombosis in other blood vessels such as the hepatic, mesenteric, renal or veins and retinal arteries have been reported very rarely. Risk factors for venous thromboembolism: obesity (BMI body mass index over 30 kg / m²) - the risk increases significantly with the increase in BMI, this is especially important for women who also have other risk factors; long-term immobilization, extensive surgery, any surgical operation in the lower limbs or pelvis, neurosurgical surgery or serious trauma - it is recommended to stop using the tablets for at least 4 weeks before the planned surgery and not to resume use within 2 weeks from the time of return for motor function (another method of contraception should be used), anticoagulant therapy should be considered if the preparation has not been discontinued early (temporary immobilization, including air travel> 4 h, may also be a risk factor for venous thromboembolism, especially in women with co-existing other risk factors); positive family history (occurrence of venous thromboembolism in siblings or parents, especially at a relatively young age, e.g. before 50) - if genetic predisposition is suspected, a woman should be referred for a decision to use a combined hormonal contraceptive consultation with a specialist; other diseases associated with venous thromboembolism (cancer, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic inflammatory bowel diseases (eg Crohn's disease or ulcerative colitis) and sickle-cell anemia); age - especially at the age of over 35 years. If the patient has several VTE risk factors at the same time, the use of the preparation is contraindicated. If a woman has more than one risk factor, it is possible that the risk increase is greater than the sum of single factors - in this case, the overall risk of venous thromboembolism should be assessed - if the benefit-risk assessment is negative, complex hormonal measures should not be prescribed contraceptives. Consensus was not reached as to the possible role of varicose veins and thrombophlebitis of surface veins on the occurrence or progression of venous thromboembolism. The increased risk of thromboembolism during pregnancy and in particular in the 6th week should be considered. postpartum period.Patients should be advised that if symptoms of venous thromboembolism occur, see a doctor immediately and tell the healthcare professional that they use a combined hormonal contraceptive. Risk factors for arterial thromboembolic events: age - especially those over 35 years of age; smoking - women should be carefully instructed not to smoke if they intend to use a combined hormonal contraceptive, women over the age of 35 who have not stopped smoking should be carefully instructed to use a different method of contraception; hypertension; obesity (body mass index BMI over 30 kg / m²) - the risk increases significantly with the increase in BMI, this is especially important for women who also have other risk factors; positive family history (occurrence of arterial thromboembolism in siblings or parents, especially at a relatively young age, eg before 50) - if genetic predisposition is suspected, before a decision to use a combined hormonal contraceptive is made, the woman should be referred for consultation with a specialist; migraine - an increase in the frequency or severity of migraine during use of combined hormonal contraceptives (which may indicate the occurrence of a cerebrovascular event) may be a reason to discontinue use immediately; other conditions associated with adverse events within the vessels (diabetes, hyperhomocysteinemia, valvular heart disease, atrial fibrillation, dyslipoproteinemia and systemic lupus erythematosus). The use of the preparation is contraindicated if the patient has one serious or several risk factors for arterial thromboembolic events that place the patient at high risk of arterial thrombosis. If a woman has more than one risk factor, it is possible that the risk increase is greater than the sum of individual factors - in this case, the total risk should be assessed - if the benefit-risk assessment is negative, the combined hormonal contraceptives should not be prescribed. Patients should be advised that if signs of arterial thromboembolism occur, immediately seek medical attention and tell the healthcare professional that they are using combined hormonal contraceptives. The increased risk of thromboembolic complications during the postpartum period should also be taken into account. Increasing the incidence or severity of migraine pain when using oral contraception (which may be a symptom of a cerebrovascular event) may be the reason for the immediate withdrawal of these tablets. There is an increased risk of developing cervical cancer during long-term use of combined oral contraceptives. However, it remains a matter of dispute as to whether this is due to specific sexual behaviors and other factors such as human papillomavirus (HPV) infection. There is a slightly increased risk of breast cancer in women taking combined oral contraceptives. This risk gradually decreases within 10 years after discontinuation of combined oral contraceptives. In differential diagnosis of severe epigastric pain, hepatomegaly or abdominal haemorrhage in women using COC, liver cancer should be considered. The progestogen component in the preparation is an aldosterone antagonist with potassium-sparing properties. In most cases, you should not expect an increase in potassium. Some patients with mild to moderate renal insufficiency who also used potassium-sparing drugs have had a modest increase in serum potassium while taking drospirenone - monitoring of serum potassium is recommended during the first cycle of treatment in patients with renal insufficiency and potassium prior to starting treatment preparation 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; gallstones; porphyria; systemic lupus erythematosus; haemolytic-uremic syndrome; Sydham's chorea; herpes of pregnant women; hearing loss associated with otosclerosis. In women with congenital 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 cholestasis which occurred earlier during pregnancy or during previous use of sex hormones requires discontinuation of combined oral contraceptives. Although combined oral contraceptives may have an effect on peripheral tissue insulin resistance or 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 efficacy of combined oral contraceptives can be reduced in the case of, for example, skipping a tablet, vomiting or severe diarrhea, or the simultaneous use of other medications. When using a combined oral contraceptive, irregular bleeding (spotting or breakthrough bleeding) may occur, especially in the first months of using the tablets. Therefore, the correct assessment of the occurrence of irregular bleeding is possible 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. In some women, withdrawal bleeding may not occur when using placebo tablets.

The use of the preparation during pregnancy is contraindicated. If during pregnancy the woman becomes pregnant, stop using it immediately. Epidemiological studies have not shown or increased the risk of birth defects in children of women who used oral contraceptives before pregnancy and no teratogenic effects when they were used in early pregnancy. Available data on the use of the preparation during pregnancy are too limited to draw conclusions about the harmful effects of the preparation on pregnancy, the health of the fetus or newborn baby. So far, there are no relevant epidemiological data.The risk of venous thromboembolism in women in the postpartum period should be taken into account when deciding whether to restart the treatment. Combined oral contraceptives may affect lactation because they can reduce the amount and modify the composition of food - the use of combined oral contraceptives is not recommended until breastfeeding is terminated. Small amounts of steroid contraceptives and / or their metabolites may be excreted in human milk. Such amounts may affect the child.

Common: menstrual disorders, intermenstrual bleeding, breast pain, headache, depressive mood, migraine, nausea, white vaginal discharge, vaginal candidiasis. Uncommon: libido changes, hypertension, hypotension, vomiting, acne, eczema, pruritus, vaginitis, fluid retention, changes in body weight. Rare: hypersensitivity, asthma, discharge from the breast, hearing loss, venous or arterial thromboembolism, erythema nodosum, erythema multiforme. The following serious adverse events have been reported in women using COC: venous and arterial thromboembolism, hypertension, liver cancer, chloasma, acute or chronic hepatic dysfunction (requiring in some cases discontinuation of COC until the liver parameters return to normal); occurrence or worsening of conditions, the relationship of which with the use of COC is uncertain: Leśniowski-Crohn's disease, ulcerative colitis, epilepsy, migraine, myoma, porphyria, systemic lupus erythematosus, herpes simplex, Sydenhama chorea, haemolytic-uremic syndrome, jaundice cholestatic; in women with hereditary angioedema, exogenous estrogens may provoke or exacerbate symptoms of angioedema. The incidence of breast cancer in women using COC is slightly increased (however, the causal relationship to the use of COC is unknown).

Orally. The tablets should be taken daily at about the same time, in the order shown on the blister, with a small amount of liquid if necessary. Take 1 tabl. daily for the Next 21 days. Each subsequent pack should be started after a 7-day break, during which usually withdrawal bleeding occurs. Bleeding usually starts on the 2nd or 3rd day after taking the last tablet and may not end before the next pack.Beginning of the preparation. No hormonal contraception last month: tablets should be started on day 1 of the menstrual cycle (on the day of menstrual bleeding).Change from another combined contraceptive (COC, oral vaginal system or transdermal patch): the preparation should be started the day after the last active tablet of the previously used COC, but no later than the day after the end of the interruption or after taking the placebo tablets of the previous COC. If a therapeutic intravaginal or transdermal patch system is used, the preparation should be started preferably on the day of removal, or at the latest when the next date is reached.Change from a contraceptive method based only on the use of progestagen (tablets, injection, implant) or the progestin releasing system (IUS): women can change the method of contraception from a progestogen-only tablet on any day of the cycle (from the implant or intrauterine system - on the day of removal, from the injection - on the day the next injection was to be made), but in each of them cases should be recommended additionally to the barrier method for the first 7 days of taking tablets.After a miscarriage in the first trimester of pregnancy: the patient can start taking the product immediately. There is no need to use additional methods of contraception.After delivery or after a miscarriage in the second trimester of pregnancy: start taking the preparation between the 21st and 28th day after giving birth or abortion in the second trimester of pregnancy. In the event of later initiation of the preparation, the patient should additionally use a barrier method of contraception for the first 7 days.However, in the event of a postpartum or miscarriage relationship, pregnancy should be ruled out before the first use of COC or wait until the first menstrual period.Proceeding in case of skipping tablets. If less than 12 hours have passed since you missed the tablet, contraceptive protection is not reduced. The patient should take the tablet as soon as she remembers to skip the dose, and the next tablet should take at usual times. If more than 12 hours have passed since you missed the tablet, contraceptive protection may be reduced. The procedure in the case of skipping tablets may follow two basic principles: 1. Taking tablets must never be interrupted for more than 7 consecutive days. 2. A 7-day, continuous tableting period is necessary for sufficient inhibition of the hypothalamo-pituitary-ovary axis.If you miss a tablet in the first week: take the last missed tablet immediately after remembering to skip the dose, even if it means taking 2 tablets once. Then continue to take the tablets at the usual time. In addition, for the next 7 days, an additional barrier method of contraception, eg a condom, should be used. If there has been sexual intercourse during the last 7 days, the possibility of pregnancy should be taken into account. The risk of pregnancy is the greater, the more tablets are missed and the less time remaining for a normal break in the use of tablets.If you miss a tablet in the 2nd week: take the last missed tablet immediately after remembering to skip the dose, even if it means taking 2 tablets once. Then continue to take the tablets at the usual time. If during the 7 days preceding the omission of the tablet, the preparation was used correctly, there is no need to use additional contraceptives. If, however, more than one tablet has been missed, additional contraception should be recommended for 7 days.If you miss a tablet in the third week: the risk of decreasing the effectiveness of the contraceptive is high due to the upcoming 7-day break in taking tablets. However, you can still prevent reducing the effectiveness of contraceptive protection by adjusting the pattern of tablets. Proceeding according to one of the two options below excludes the need for additional contraception, as long as all tablets were taken correctly within 7 days before skipping the tablet for the first time. Otherwise, follow the first option, and for additional 7 days apply additional security. 1. Take the last missed tablet immediately after remembering to skip the dose, even if it means taking 2 tablets at a time. The next tablets should be taken at the usual time. Taking the tablets from the next package should start immediately after finishing the currently used packaging, i.e. without a break between the packages. Until the end of taking the tablets containing the active substances from the second pack, there should be no withdrawal bleeding, but staining or breakthrough bleeding may occur during the use of the tablets. 2. The patient may also be advised to discontinue tablets from the currently used packaging. She should take a 7-day or shorter break in taking the tablets, including the days when the tablets were left out, and then continue taking the tablets from the next pack.Recommendations in the case of gastrointestinal disorders: in the case of severe gastrointestinal disturbances (eg, vomiting or severe diarrhea), the active substances in the preparation may not completely absorb and additional contraceptive methods should be used. If vomiting occurred within 3-4 hours after taking the tablet, take a new tablet as soon as possible. If possible, the new tablet should be taken within 12 hours of the usual time of taking the drug. If more than 12 hours have elapsed, follow the instructions for omitting the tablets. If you do not want to change your dosage regimen, take an extra tablet (tablet) from another pack.Proceedings to delay the withdrawal bleeding. To delay the occurrence of bleeding, after completing the current package, without interruption, begin taking the tablets from the next blister of the preparation.The tablets can be taken as long as the patient wants even while the second pack is empty. During this time, bleeding or spotting may occur. The next regular intake of the preparation should start after a 7-day break. In order to postpone the date of bleeding to a different day of the week than that resulting from the current pattern of taking the preparation, shorten the next break in taking tablets for as many days as you intend to postpone the date of bleeding. The shorter the break in taking the tablets, the more likely it is that the withdrawal bleed does not occur. When taking tablets from the next pack, spotting or breakthrough bleeding may occur (as in the case of delayed bleeding).