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.

Each package contains 28 tables. area: 24 tabl. pink, each containing 3 mg drospirenone and 0.02 mg ethinylestradiol; 4 tables white (placebo) that does not contain active substances. 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. After oral administration, drospirenone is rapidly and almost completely absorbed. The maximum serum concentration is reached approximately 1-2 hours after a single dose. Bioavailability is 76-85%. Final T_0,5 is 31 h. Drospirenone binds to serum albumin, does not bind to sex hormone binding globulin (SHBG) or to corticosteroid binding globulin (CBG). Only 3-5% of the total amount of this active substance in the serum is in the form of an unrelated steroid. Increases in ethinyl estradiol induced SHBG levels do not affect the binding of drospirenone to serum proteins. Drospirenone after oral administration is subject to rapid metabolism. The main metabolites are formed without the involvement of the cytochrome P450 system. Drospirenone is metabolised to a lesser extent by CYP3A4 and has the ability to inhibit this enzyme and CYP1A1, CYP2C9 and CYP2C19 under conditionsin vitro. Only traces of drospirenone are excreted unchanged. Drospirenone metabolites are excreted in the faeces and urine in a ratio of approximately 1.2 to 1.4. T_0,5 metabolites in the urine and faeces is about 40 hours. After oral administration, ethinyl estradiol is rapidly and completely absorbed. Maximum plasma concentration occurs within 1-2 h after a single dose. The total bioavailability is about 60% due to the first-pass effect and the coupling phenomenon before the substance goes into circulation. Plasma ethinyl estradiol concentration is reduced in two phases; in the final phase of the elimination of T_0,5 is about 24 h. Ethinylestradiol is subject to strong, non-specific binding by serum albumin (around 98.5%) and induces an increase in SHBG and corticosteroid binding globulin (CBG) in serum. Before penetration into the systemic circulation ethinylestradiol is coupled in the mucous membrane of the small intestine and in the liver. Ethinyl estradiol in unchanged form is not excreted in significant amounts. Ethinyl estradiol metabolites are excreted in urine and bile at a ratio of 4: 6. T_0,5 excretion of metabolites is about 1 day.

Hypersensitivity to the active substances or to any of the excipients. Current or past venous thrombosis (deep vein thrombosis, pulmonary embolism). Current or past arterial thrombosis (eg myocardial infarction) or prodromal conditions (e.g. angina pectoris and transient ischemic attack). Current or past cerebrovascular incident. The presence of severe or complex risk factors for arterial thrombosis: diabetes with vascular lesions, severe hypertension, severe dyslipoproteinaemia. Inherited or acquired predisposition to venous or arterial thrombosis, eg resistance to activated C protein (APC), antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia and the presence of anti-phospholipid antibodies (anti-cardiolipin antibodies, lupus anticoagulant). Current or previous pancreatitis if severe hypertriglyceridemia has occurred. Current or past severe liver disease, unless the liver function parameters have returned to normal. Severe or acute renal failure. Current or past liver tumors (benign or malignant). Presence or suspicion of malignant tumors dependent on sex hormones (e.g., genital or breast cancer). Bleeding from the genital tract of undetermined etiology.Migraine with focal neurological symptoms in an interview.

The use of combined oral contraceptives carries an increased risk of venous thromboembolism (VTE). The increased risk of VTE is the highest in the first year of application. The use of combined oral contraceptives is associated with an increased risk of arterial thromboembolic events (myocardial infarction, transient cerebral ischemic attack). The occurrence of thrombosis of other blood vessels, such as hepatic, mesenteric, renal, cerebral or retinal arteries, has been reported rarely. The risk of complications of venous thromboembolic events in patients taking oral combined oral contraceptives increases with: age; positive family history (presence of venous thromboembolism in siblings or parents at a relatively young age) - if genetic predisposition is suspected, a woman should be referred for specialist consultation before deciding whether to use any combined oral contraceptive; long-term immobilization, major surgery, any operation in the lower limbs or severe trauma - in these situations, it is recommended to stop using a combined oral contraceptive (at least 4 weeks before the planned surgery) and resume taking it no sooner than after 2 weeks after the patient regains full mobility, you should consider introducing anticoagulant therapy, if you do not stop using the tablets before; obesity (body mass index above 30 kg / m²pc.); It was not determined what role the presence of varicose veins and superficial vein inflammation in the early stages and progression of venous thrombosis play. The risk of complications of thromboembolic disorders of the arteries or cerebrovascular accident in patients taking combined oral contraceptives increases with: age; smoking (women over the age of 35 should be strongly advised to stop smoking); dyslipoproteinemia; hypertension; migraine; obesity (body mass index above 30 kg / m²pc.); positive family history (occurrence of arterial thromboembolic disorders in siblings or parents at a relatively young age) - if genetic predisposition is suspected, a woman should be referred for specialist consultation before deciding whether to use any combined oral contraceptive; valvular heart disease; atrial fibrillation. The presence of one serious or several risk factors for venous or arterial disease, respectively, may be another contraindication. In such cases, the possibility of anticoagulation should also be considered. If thrombosis is suspected or diagnosed, discontinue use. Increasing the risk of thromboembolic events during the postpartum period should be considered. Other disorders that promote cardiovascular side effects include diabetes mellitus, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic enteritis (Crohn's disease or ulcerative colitis) and sickle cell anemia. Increased incidence and severity of migraine headaches when taking combined oral contraceptives (may be a prodromal sign of stroke) and may require immediate cessation of use. Long-term use of combined oral contraceptives (over 5 years) may increase the risk of cervical cancer. However, the importance of additional factors such as sexual and other behaviors such as human papillomavirus (HPV) infection has still not been resolved. There is a slightly increased relative risk of diagnosing breast cancer in women who are currently using combined oral contraceptives. This increased risk gradually disappears within 10 years after the end of treatment. In case of severe upper abdominal pain, hepatomegaly or symptoms of abdominal haemorrhage in women taking combined oral contraceptives in differential diagnosis, liver cancer should be considered. The progestogen contained in the preparation is an aldosterone antagonist with potassium-sparing properties.In most cases, you should not expect an increase in potassium. In some patients with mild or moderate renal impairment and those taking concomitant other potassium sparing therapies in combination therapy, a small, insignificant increase in serum potassium has been observed while taking drospirenone - monitoring of serum potassium during the first cycle of treatment in patients with renal failure and starting serum potassium at the upper limit of normal, especially when concomitant use of potassium-sparing drugs. In women with hypertriglyceridemia or family history of hypertriglyceridemia, the risk of pancreatitis may be increased when taking combined oral contraceptives. If the use of a combined oral contraceptive in a woman with pre-existing hypertension is accompanied by persistently elevated blood pressure or a significant increase in blood pressure not responding to antihypertensive therapy, it is necessary to discontinue using the combined oral contraceptive. If warranted, the use of a combined oral contraceptive can be restarted after restoring blood pressure to the normal range as a result of antihypertensive treatment. The occurrence or worsening of the following conditions has been reported both during pregnancy and during the use of combined oral contraceptives, but evidence of their association with the use of these preparations is not conclusive: jaundice and / or pruritus associated with cholestasis, cholelithiasis, porphyria, lupus systemic lupus erythematosus, haemolytic-uremic syndrome, Sydenham chorea, herpes of pregnant women, hearing loss associated with otosclerosis. In women with hereditary angioedema, exogenous estrogens may induce or exacerbate the symptoms of angioneurotic edema. Acute or chronic liver problems may require discontinuation of the combined oral contraceptive until the functional parameters of the liver return to normal. Recurrence of cholestatic jaundice and / or pruritus associated with cholestasis which occurred during pregnancy or prior sex hormone replacement requires discontinuation of combined oral contraceptives. Although combined oral contraceptives may affect peripheral tissue insulin resistance and Glucose tolerance, there is no evidence of a need to change the diabetes therapy regimen. However, the condition of diabetic patients should be carefully monitored, especially in the initial period of use of combined oral contraceptives. There have been reports of worsening of the course of endogenous depression, epilepsy, Crohn's disease and ulcerative colitis in women taking combined oral contraceptives. Chloasma may occur occasionally, especially in women who have had chloasma during pregnancy. Women prone to chloasma should avoid exposure to solar and ultraviolet light during the use of combined 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 may be reduced, for example, by skipping a tablet containing active substances, stomach and intestinal disorders when tablets containing active substances are used or when other medicines are concomitantly administered. Irregular bleeding (spotting or intracycular bleeding) may occur with the use of combined oral contraceptives, especially in the first months of use. Therefore, the assessment of irregular bleeding can only be meaningful after the adaptation period lasting about 3 cycles. If the intercyclical bleeding persists or occurs in a woman who has had regular bleeding, non-hormonal reasons should be considered and appropriate diagnosis should be made to exclude malignancy or the possibility of pregnancy. This diagnosis may include curettage of the uterine cavity.In some women, withdrawal bleeding may not occur during the placebo-taking phase.

The preparation is not indicated for use during pregnancy. If a woman becomes pregnant while using the preparation, her use should be discontinued immediately. Epidemiological studies did not show an increased risk of congenital malformations in children of women who used combined oral contraceptives prior to pregnancy or a teratogenic effect due to miscarriage of these preparations during pregnancy. Available data on the use of the preparation in pregnant women are too limited to confirm its negative impact on pregnancy and the state of health of the fetus or newborn. At the moment, there is no relevant epidemiological data. Combined oral contraceptives may affect lactation, reducing the amount and changing the composition of the food - they are not recommended until complete breastfeeding. Small amounts of steroid contraceptives and / or their metabolites may pass into the milk of women taking combined oral contraceptives. Such amounts may affect the child.

Common: emotional instability, headache, nausea, breast pain, uterine haemorrhage (irregular bleeding usually disappears during further use), lack of menstruation. Uncommon: depression, nervousness, insomnia, dizziness, paresthesia, migraine, varicose veins, hypertension, abdominal pain, vomiting, dyspepsia, flatulence, gastritis, diarrhea, acne, pruritus, rash, back pain, pain in the limbs, painful muscle cramps, vaginal candidiasis, pelvic pain, breast enlargement, fibrocystic cysts, uterine and / or vaginal bleeding (usually subside during continued use), vaginal discharge, hot flushes, vaginitis, menstrual disorders, painful menstruation, scanty and short-lasting menstruation, menorrhagia, vaginal dryness, abnormal cytology of the smear (Papanicolaou classification), decreased sex drive, weakness, excessive sweating, edema (generalized edema, peripheral edema, facial edema), weight gain. Rare: candidosis, anemia, thrombocytosis, allergic reactions, endocrine disorders, increased appetite, anorexia, hyperkalemia, hyponatremia, lack of orgasm, insomnia, diarrhoeas, tremor, conjunctivitis, dry eye syndrome, eye disorders, tachycardia, phlebitis, vascular disorders, epistaxis, fainting, abdominal distension, gastrointestinal disorders, a feeling of fullness in the stomach and intestines, hiatal hernia, candidiasis of the mouth, constipation, dry mouth, pain in the gallbladder area, cholecystitis, chloasma , eczema, alopecia, acne-like dermatitis, dry skin, erythema nodosum, hypertrichosis, skin disorders, stretch marks, contact dermatitis, photosensitive dermatitis, skin nodule, painful intercourse, vulvovaginal inflammation, non-menstrual bleeding . withdrawal bleeding, breast cyst, breast tissue growth, breast cancer, cervical polyps, endometrium atrophy, ovarian cyst, enlarged uterus, malaise, weight loss. Not known: hypersensitivity, erythema multiforme.
In women taking combined oral contraceptives, the following serious side effects have been reported: venous thromboembolic events; arterial thromboembolic disorders; hypertension; liver cancer; there are conflicting data on the association of combined oral contraceptives with induction or severity: Crohn's disease, ulcerative colitis, epilepsy, uterine fibroids, porphyria, systemic lupus erythematosus, herpes simplex, Sydenhama chorea, haemolytic-uremic syndrome, cholestatic jaundice; chloasma; acute or chronic liver problems that sometimes require discontinuation of the combined oral contraceptive until liver function values ​​return to normal; in women with congenital angioneurotic edema, exogenous oestrogens may cause or worsen the symptoms of angioneurotic edema.Breast cancer is diagnosed slightly more frequently in a group of women using oral contraceptives (a causal relationship with the use of combined oral contraceptives is not known).

Orally. The tablets should be taken daily at approximately the same time of the day, if necessary with a small amount of liquid in the order indicated on the blister. The tablets are taken continuously. Take 1 tabl. daily for 28 consecutive days. Each Next blister should be started the day after taking the last tablet from the previous blister. The withdrawal bleed usually starts after 2-3. days after starting placebo tablets (the last row of tablets) and may not end until the next blister 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).Change from a combined hormonal contraceptive (oral combined contraceptive, vaginal or transdermal system)A woman should start taking the medicine the day after the last tablet containing the active ingredients of the previous combined oral contraceptive, but no later than the day after the end of the pause or after taking the placebo tablets of the previous combined contraceptive. If a vaginal or transdermal patch system is used, the preparation should be started on the day the system is removed, but no later than on the day when the next system should be used.Change from a preparation containing only progestagen (mini-tablet, injection, implant) or an intrauterine-releasing system: women taking a minitablete can switch to the use of the preparation on any day of the cycle (women using an implant or an intrauterine system can start using the preparation on the day of removal and women who use the injection - on the day of the next injection). However, in all these cases, a mechanical method of contraception should be used for the first 7 days of taking tablets.After a miscarriage in the first trimester of pregnancy: a woman can start using the preparation right away. In this case, it is not necessary to use additional methods of contraception.After delivery or miscarriage in the second trimester of pregnancy: The patient should be informed that tablets should be started between the 21st to 28th day after delivery or abortion in the second trimester of pregnancy. If you start using the tablets later, you should inform the patient about the need for additional mechanical contraception during the first 7 days of taking the tablets. If a relationship has occurred before taking the preparation, pregnancy should be ruled out or the first menstrual bleeding should be allowed to occur.Proceeding in case of skipping tablets. The following recommendations only concern the omission of tablets containing active substances. If less than 12 hours have elapsed since the planned tablet was taken, the effectiveness of contraceptive protection is not reduced. The woman should take the tablet as soon as possible after remembering to skip the tablet, and the next tablet should be taken at the usual time. If more than 12 hours have passed since the planned adoption of the tablet, the effectiveness of contraceptive protection may be reduced. In this case, you must follow the following two basic principles: 1. never stop using the tablets for more than 4 days. 2. adequate inhibition of the hypothalamo-pituitary-ovary axis occurs after 7 days of continuous taking of tablets. According to the aforementioned principles, the following information can be provided in daily medical practice.If you miss a tablet on days 1-7.: The patient should take the last forgotten tablet as soon as she remembers it, even if it means taking 2 tablets at the same time. The next tablets should be taken at the usual time. In addition, for the next 7 days you should additionally use a mechanical method of contraception, e.g. condoms. If there has been a relationship within the 7 previous days, the possibility of pregnancy should be taken into account. The more tablets are missed and the less time has passed since the placebo tablets were used, the greater the risk of getting pregnant.If you miss the tablet on days 8-14.: the patient should take the last forgotten tablet as soon as she remembers it, even if it means taking 2 tablets at the same time. The next tablets should be taken at the usual time. If the correct dosage has been used within 7 days prior to skipping the tablet, no additional contraceptive measures are required. However, if the patient omitted more than 1 tablet, an additional method of contraception should be used for 7 days.If you miss the tablet on days 15-24.: there is a significant risk of reducing the effectiveness of contraception due to the approaching use of placebo tablets. However, by adjusting the dosage regimen, the contraceptive effectiveness may be reduced. The use of one of the two options below makes it unnecessary to use additional contraceptive methods, provided that the correct dosage has been used for 7 days prior to skipping the tablet. Otherwise, the woman should follow the first of the two options and for the next 7 days, use an additional method of contraception. 1. The patient should take the last forgotten tablet as soon as she remembers, even if it means taking 2 tablets at the same time. Continue to take your tablets at the usual time until you stop taking tablets containing active substances. Throw 4 placebo tablets from the last row and start taking the tablets from the next blister immediately. Until the end of use of tablets containing active substances from the second blister, there is usually no withdrawal bleeding, but spotting or intermenstrual bleeding may occur. 2. You may also be advised to stop taking tablets containing active ingredients from the current blister. The woman should then start taking placebo tablets from the last row for up to 4 days, including the days she missed taking the tablets, and then start a new blister pack. If a woman has missed the tablets and there is no withdrawal bleeding during the use of the placebo tablets, the possibility of pregnancy should be considered.Proceedings in the case of gastrointestinal disorders. In the case of severe gastrointestinal disturbances (eg, vomiting, diarrhea), absorption may be reduced and additional contraceptive methods should be used. If vomiting occurs within 3-4 hours after taking the tablet containing active substances, take the new (additional) tablet as soon as possible. An additional tablet should be taken as much as possible within 12 hours of the usual time of tablet use. If more than 12 hours have elapsed, recommendations on missed doses should be considered. If a woman does not want to change her current dose schedule, she should take an additional (additional) tablet (s) from the new blister.Proceedings to delay withdrawal bleeding. To delay the onset of withdrawal bleeds, skip the placebo tablets from the current blister pack and proceed immediately to the tablets from the next blister pack. The duration of the bleeding delay can be extended by taking further tablets, even until the tablets containing the active ingredients from the second blister are discontinued. During the extended cycle, there may be some intermenstrual bleeding or spotting. Then, after the use of placebo tablets, the preparation should be resumed. For women who want to move their withdrawal bleed to a different day of the week than the current dosing regimen, we recommend that you shorten the next placebo tablet period for any number of days. The shorter the break, the greater the likelihood that no withdrawal bleeding will occur, while interstitial bleeding or spotting may occur when taking tablets from another blister pack (similar to a delayed bleeding).