Index of drugs

Oral contraception.

Each blister contains 28 tables. area: 24 tabl. white, each containing 3 mg drospirenone and 0.02 mg ethinyl estradiol; 4 tables green (placebo) that do not contain active substances. The preparation contains lactose.

A combined oral contraceptive containing ethinyl estradiol and progestin drospirenone. The main mechanism of the contraceptive effect of the preparation is inhibition of ovulation and induction of changes in the endometrium. At therapeutic doses, drospirenone also shows antiandrogenic activity and low antimineralocorticoid activity. It has no estrogenic, glucocorticoid and anti-glycocorticoid properties (the pharmacological profile of drospirenone is very similar to that of natural progesterone). Drospirenone is rapidly and almost completely absorbed after oral administration, reaching C_max after 1-2 h. Bioavailability is 76-85%, food does not affect bioavailability. It binds to albumin, is not associated with SGBH and CBG. It is rapidly metabolised, metabolites are excreted in faeces and urine. T_0,5 is about 40 hours. Ethinyl estradiol is rapidly and completely absorbed after oral administration, reaching C_max after 1-2 h. Is subject to the first-pass effect, which is characterized by high individual variability. Bioavailability is about 60%. It binds to plasma proteins in 98.5% and induces hepatic synthesis of SHBG. It is completely metabolized, metabolites are excreted in the bile and urine. T_0,5 is about 24 hours.

Hypersensitivity to the active substances or auxiliary substances of the preparation. 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, transient ischemic attack). Current or previous cerebral vascular stroke. 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: resistance to activated C protein (APC), deficiency of antithrombin III, protein C deficiency, protein S deficiency, hyperhemocysteinemia, presence of anti-phospholipid antibodies (anticardiolipid, lupus anticoagulant). Current or previous pancreatitis, if progressing with severe hypertriglyceridemia. Current or past severe liver disease, until the liver parameters return to normal. Severe or acute renal failure. Current or past liver tumors (benign or malignant). Identified or suspected malignant tumors that are sex hormone dependent (eg, tumors of reproductive organs or breasts). Bleeding from the genital tract of undetermined etiology. Migraine with focal neurological symptoms in an interview.

The use of combined oral contraceptives increases the risk of venous thromboembolism (VTE). The risk of VTE is highest during the first year of use. The risk of VTE occurring while using the drug is currently unknown. Epidemiological studies also indicate a relationship between the use of combined oral contraceptives and the increased risk of arterial thromboembolism (myocardial infarction, transient ischemic attack). Very rarely, thrombosis has been reported in other blood vessels, eg in the liver, mesentery, kidney, and cerebral vessels or veins and retinal arteries, in women using contraceptive pills. It has not been clearly established whether the occurrence of these events is associated with the use of hormonal contraception. Particularly cautiously use in patients with risk factors for venous or arterial thromboembolic disorders such as: advanced age, positive family history (venous thromboembolism in siblings or parents at a relatively young age), long-term immobilization, surgery, lower limb surgery or severe injuries (it is recommended to discontinue the preparation for at least 4 weeks).before the planned surgery and re-application only after 2 weeks from returning to full mobility; if the preparation is not interrupted, anticoagulation is recommended), obesity (body mass index over 30 kg / m2), smoking (women over 35 years of age should not smoke if they want to use COCs), dyslipoproteinaemia, hypertension, migraine, heart valve defects, atrial fibrillation. The presence of one serious or many risk factors for venous or arterial disease, respectively, may also be a contraindication to the use of the preparation. The possibility of using anticoagulant therapy should be considered. Women using combined oral contraceptives should be clearly advised to contact their doctor if symptoms appear that may indicate a thrombosis. If thrombosis is suspected or confirmed, the use of combined oral contraceptives should be discontinued. Because anticoagulant therapy (coumarin derivatives) causes teratogenic effects, the use of an appropriate alternative method of contraception should be started. The increased risk of thromboembolic events during the puerperium period should be considered. There are discrepancies in the role of varicose veins and thrombophlebitis of superficial veins in the initial stage or progression of venous thrombosis. Caution should also be exercised in the presence of other diseases that lead to circulatory disorders such as diabetes, systemic lupus erythematosus, haemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell disease. Due to the risk of pancreatitis, caution should be used in patients with hypertriglyceridemia or a positive family history of hypertriglyceridemia. Use with caution in patients with congenital angioedema, endogenous depression, epilepsy, Crohn's disease, ulcerative colitis, jaundice and / or pruritus associated with cholestasis, gallstones, porphyria, systemic lupus erythematosus, haemolytic-uremic syndrome , Sydbeck's chorea, herpes of pregnant women, hearing loss associated with otosclerosis, because the above diseases may become more severe when using hormonal contraceptives. In patients with renal insufficiency, using potassium sparing diuretics or those in whom the potassium level was above the upper limit of normal before starting treatment, it is recommended to check the concentration of potassium during the first cycle of treatment with the product. Patients with diabetes should be closely monitored, especially at the beginning of the treatment, due to the risk of drug effects on peripheral insulin resistance and Glucose tolerance. Women with a tendency to chloasma should avoid exposure to sunlight or UV radiation when using the product. The preparation should be discontinued if thrombosis is suspected or diagnosed, the incidence or severity of migraine pain, acute or chronic hepatic impairment (until hepatic parameters return to normal), recurrent cholestatic jaundice and / or pruritus associated with cholestasis. In case of clinically significant hypertension during the use of the preparation, the preparation should be discontinued and treatment of hypertension should be initiated; You can return to the use of the preparation when antihypertensive therapy will normalize the pressure. In women taking combined oral contraceptives, the occurrence of benign liver tumors, and even more rarely, liver malignancies has been reported rarely. These neoplasms in rare cases rarely lead to life-threatening abdominal bleeds. In case of severe pain in the epigastric region, enlargement of the liver or symptoms of abdominal bleeding, differential diagnosis should take into account the possibility of liver cancer. Acute or chronic hepatic impairment may necessitate the discontinuation of combined oral contraceptives until liver function values ​​return to normal.Recurrence of cholestatic jaundice and / or pruritus associated with bile stasis, which previously occurred during pregnancy or during the previous use of sex hormones require discontinuation of combined oral contraceptives. In some epidemiological studies, an increased risk of cervical cancer has been observed in women who have been on long-term (more than 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) infection . Women currently using combined oral contraceptives have a slightly increased relative risk of breast cancer. This increased risk gradually disappears within 10 years after the discontinuation of combined oral contraceptives. Because breast cancer is rare in women under 40 years of age, the increase in the number of diagnosed breast cancer cases in the group of women taking current and recent oral contraceptives is low, relative to the total risk of breast cancer. Due to the lactose content, do not use the preparation in patients with galactose intolerance, Lapp lactase deficiency, malabsorption of glucose-galactose. The placebo-coated tablets contain a sunset yellow pigment that can cause allergic reactions. In people allergic to soy, soybean lecithin induces slight allergic effects.

Do not use during pregnancy and until breastfeeding.

Common (≥1 / 100, <1/10): emotional instability; Headache; nausea; breast pain, uterine hemorrhage (irregularities in bleeding usually disappear during prolonged use), lack of menstruation. Uncommon (≥1 / 1,000, <1/100): depression, decreased libido, nervousness, drowsiness; central dizziness, paresthesia; migraine, varicose veins, hypertension; abdominal pain, vomiting, indigestion, bloating, gastritis, diarrhea; acne, pruritus, rash; back pain, limb pain, muscle cramps; vaginal candidiasis, pelvic pain, breast enlargement, fibrocystic cysts, uterine bleeding or vaginal bleeding (irregularities in bleeding usually disappear during prolonged use), vaginal discharge, hot flushes, vaginitis, menstrual disorders, dysmenorrhea, scanty menstrual periods, menorrhagia, vaginal dryness, suspected cytological picture of smear in Papanicolau classification; weakness, increased sweating, edema (general swelling, peripheral edema, facial edema); weight gain. Rare (≥1 / 10,000, <1/1000): candidosis; anemia, thrombocytopenia; Allergic reaction; endocrine disorders; increased appetite, anorexia, hyperkalemia, hyponatremia; lack of orgasm, insomnia; dizzy-type dizziness, tremor; conjunctivitis, dry eyes, eye disorders; tachycardia; phlebitis, vascular disorders, epistaxis, fainting; enlarged abdomen, intestinal and intestinal disorders, feeling of fullness in the abdomen, hernia of the esophagus, oral mycosis, constipation, dry mouth; gall bladder pain, cholecystitis; chloasma, eczema, alopecia, acne dermatitis, dry skin, erythema nodosum, hypertrichosis, skin disorders, bands on the skin, contact dermatitis, skin inflammation caused by photosensitivity, skin tumors; painful sexual intercourse, vulvovaginal inflammation, bleeding after intercourse, absence of menstrual bleeding, breast cysts, breast growth, breast cancer, cervical polyps, endometrial atrophy, ovarian cysts, enlargement of the uterus; bad mood; weight loss. 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). In women with an inheritable propensity to exogenous angioneurotic edema, estrogen may cause or worsen symptoms of angioedema.There are mixed data on the association of combined oral contraceptives with the following diseases: Crohn's disease, ulcerative colitis, epilepsy, migraine, uterine fibroids, porphyria, systemic lupus erythematosus, herpes simplex, Sydenham chorea, haemolytic-uremic syndrome, cholestatic jaundice. In women taking hormonal contraceptives, there is an increased risk of cervical cancer and breast cancer is also diagnosed more frequently (however, the causal relationship with the use of combined oral contraceptives is unknown).

Oral: 1 tablet once a day at the same time for 28 consecutive days. Do not interrupt your application. Each subsequent pack should be started the Next day after taking the last tablet from the previous pack. The withdrawal bleed usually starts in 2 -3. the day after you start taking placebo tablets (the last row) and may not finish before the next packet begins. Beginning of the preparation. If during the last month the patient did not use any hormonal contraceptive method, the preparation should be started on the first day of the cycle (ie on the first day of menstrual bleeding). If you have previously taken another combined oral contraceptive (a combined oral contraceptive, a therapeutic vaginal system or transdermal patch, patch), you should start taking the tablets the day after the last active tablet, but no later than the day after the usual break, at the latest which tablets containing hormones are not accepted. If a patient applies a vaginal or transdermal system, the preparation should be started preferably on the day of removal or, at the latest, when the next use of the previously used product is due. If the patient used only the progestagen method (tablets containing only progestin, injections, implants or intestinal release therapy), taking the preparation instead of a progestogen-only tablet can be started on any day of the cycle, in the case of the implant and system - on the date of removal of the implant or system in the case of injections - on the day on which the next injection should be administered; in all these cases an additional barrier method of contraception should be used for the first 7 days of the preparation. In the event of a miscarriage in the first trimester of pregnancy, the preparation can be immediately started; no other methods of contraception are necessary. In the event of delivery or miscarriage in the second trimester of pregnancy, the preparation may be started 21-28 days after delivery or after a miscarriage; if the patient starts using the product later, additional mechanical contraceptive methods should be used for the first 7 days. Patients who have had an intercourse before taking the preparation should exclude pregnancy or wait for the first menstrual bleeding. Proceeding if you miss a tablet. If you miss the tablet, if less than 12 hours have passed since the tablet was missed, the contraceptive effectiveness is maintained; omit the tablet should be taken as soon as possible, and the next - at the usual time. If more than 12 hours have elapsed since the tablet was missed, the effectiveness may be reduced, then proceed as follows. Never stop taking tablets for more than 4 days. It is necessary 7 days of uninterrupted taking of tablets to maintain the proper degree of inhibition of the hypothalamo-pituitary-ovary axis. If you miss a tablet on day 1-7, take the missed tablet as soon as possible, even if it means taking two tablets at the same time, take your next tablet at the usual time. For the next 7 days, an additional barrier method of contraception should be used. If there has been sexual intercourse during the 7 days preceding the missed tablet, there is a possibility of pregnancy. The more tablets are missed and the shorter the time between missed and the placebo-taking period, the greater the risk of getting pregnant.If you miss a tablet within 8-14 days, take the missed tablet as soon as possible, even if it means taking two tablets at the same time, take your next tablet at the usual time. If during the 7 days preceding skipping the first tablet the preparation was taken correctly, no additional contraceptive methods are necessary. If, however, more than one tablet has been omitted, barrier methods of contraception should be used for 7 days. If you miss a tablet on the 15th to 24th day, two options are possible.
There is a high risk of reducing the contraceptive effectiveness due to the upcoming period of taking placebo tablets. However, by adjusting the tablet intake regimen, it is possible to prevent the contraceptive effect from being reduced. If, for 7 days prior to skipping the first tablet, all the tablets were used correctly, you can choose one of the following recommendations without the need for any additional contraceptive methods. Otherwise, choose recommendation 1). and use barrier methods of contraception for 7 days. 1) Skip the tablet as soon as possible, even if it means taking two tablets at the same time, the next tablet should be taken at the usual time, until the active tablets are depleted. The four tablets from the last row of packaging (placebo tablets) should be discarded. You should start taking the tablets from the next blister pack immediately. If you stop taking the active tablets from the second pack, bleeding or intracycular bleeding may occur while taking the tablets. 2.) You can stop taking active tablets from the current packaging. In this case, take the placebo tablets from the last row of the pack for up to 4 days, including the days the tablet was left out, and then continue taking the tablets from the next blister pack. If the patient omitted the tablets and subsequently did not experience withdrawal bleeding during the first scheduled placebo treatment period, the possibility of pregnancy should be considered. Proceedings in the case of gastrointestinal disorders. If vomiting occurs within 3-4 hours after taking the tablet containing the active substance, take the additional tablet as soon as possible. If possible, take a new tablet within 12 hours of the usual time of taking the tablet. If more than 12 hours have elapsed, proceed as if you missed the tablet. If the patient does not want to change the set dosing schedule, she should take an additional tablet from the next pack. Procedure to delay bleeding. To delay the withdrawal bleed, start the next pack without taking the placebo tablets from the current pack. The use of tablets can continue for as long as needed until the active tablets from the second packet are finished. Meanwhile, intercyclic bleeding or spotting may occur. You should return to regular use after taking placebo tablets. If the patient wants to change the day of menstruation to a different day of the week than the current schedule, she can be advised to shorten the next period of use of placebo tablets for any number of days. The shorter this period, the greater the risk that there will be no withdrawal bleeding and there will be bleeding in the mid-cycles or spotting during the use of the tablets from the next pack (just as in the case of delaying menses).