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Active ingredients
Drospirenone + Ethinyl Estradiol
Release form
Pills
Composition
1 tablet (active) contains: Active substances: ethinyl estradiol (in the form of betadex clathrate) - 20 mcg, drospirenone - 3 mg. Adjuvants: lactose monohydrate - 48.18 mg, corn starch - 28 mg, magnesium stearate - 0.8 mg. Coat composition: hypromellose - 1.5168 mg, talc - 0.3036 mg, titanium dioxide - 1.1748 mg, iron dye red oxide - 0.0048 mg.1 tablet (placebo): Excipients: lactose monohydrate - 23.205 mg, microcrystalline cellulose - 54.21 mg, magnesium stearate - 0.585 mg The composition of the shell: hypromellose - 1.0112 mg, talc - 0.2024 mg, titanium dioxide - 0.7864 city
Pharmacological effect
Drug jess; - combined hormonal contraceptive with anti-mineralocorticoid and anti-androgenic effects. The contraceptive effect of combined oral contraceptives is based on the interaction of various factors, the most important of which include suppression of ovulation and changes in the properties of the cervix secretion, as a result of which it becomes less permeable to spermatozoa. Pearl (the number of pregnancies per 100 women per year) is less than 1. When you skip pills or misuse The pearl index can increase. In women taking combined oral contraceptives, the menstrual cycle becomes more regular, painful menstruation is less common, and the intensity of bleeding decreases, which reduces the risk of anemia. In addition, according to epidemiological studies, the use of combined oral contraceptives reduces the risk of developing endometrial cancer and ovarian cancer. Drospirenone contained in the drug Jess; has anti-mineralocorticoid action. Prevents weight gain and edema associated with estrogen-induced fluid retention, which ensures good tolerability of the drug. Drospirenone has a positive effect on premenstrual syndrome (PMS). The clinical efficacy of the drug Jess is shown; relieving severe PMS symptoms, such as severe psycho-emotional disorders, breast engorgement, headache, muscle and joint pain, weight gain, and other symptoms associated with the menstrual cycle. Drospirenone also has anti-androgenic activity and contributes to the reduction of acne and skin oilyness and hair.This action of drospirenone is similar to the action of natural progesterone produced by the body. Drospirenone does not possess androgenic, estrogenic, glucocorticoid, and antiglucocorticoid activity. All of this, in combination with the anti-mineralocorticoid and anti-androgenic effects, provides Drospirenone with a biochemical and pharmacological profile similar to natural progesterone. In combination with ethinyl estradiol, Drospirenone exhibits a favorable effect on the lipid profile characterized by elevated HDL cholesterol. can be used as in a normal mode (24 + 4 intake mode: taking 24 active pills for 24 days, then taking inactive pills for 4 days), and in a flexible mode. Adaptable elongated (flexible) mode of taking the drug Jess; based on the previously approved mode of taking the drug 24 + 4 and is that the active pills of the drug can be taken daily continuously for up to 120 days. Thus, the continuous period of taking active pills can be 24-120 days, and the duration of the break in taking pills should not exceed 4 days. A flexible regimen is only possible with a Click click dispenser (Clyk) and flex cartridges that allow you to follow the drug intake. The results of a multicenter comparative open randomized study in parallel groups showed that the flexible dose regimen of the drug Jess; aimed at achieving the maximum duration of intervals without bleeding up to 120 days, allowed to reduce the total number of menstruation days in a year from 66 (24 + 4 reception mode) to 41 days (flexible reception mode).
Pharmacokinetics
Drospirenone Absorption When ingested, drospirenone is rapidly and almost completely absorbed. After a single oral administration, serum Cmax of drospirenone is reached after about 1-2 hours and is about 38 ng / ml. Bioavailability - 76-85%. Compared with fasting, ingestion does not affect the bioavailability of drospirenone. DistributionAfter ingestion, a two-phase decrease in serum drospirenone is observed, with T1 / 2, respectively, 1.6 ± 0.7 h and 27 ± 7.5 h. Drospirenone is bound to serum albumin and is not binds to the sex hormone-binding globulin (SHBG) or corticosteroid-binding globulin (CAG).Only 3-5% of the total concentration of the substance in the serum is present as a free hormone. An ethinyl estradiol-induced increase in SHBG does not affect the binding of drospirenone to plasma proteins. The average apparent Vd is 3.7 ± 1.2 L / kg. The equilibrium concentration during the cycle intake (Cssmax) of serum drospirenone is reached between 7 and 14 days of treatment and is approximately 70 ng / ml. There was an increase in the concentration of drospirenone in serum by about 2-3 times (due to cumulation), which was caused by the T1 / 2 ratio in the terminal phase and the dosing interval. A further increase in the serum concentration of drospirenone is observed between 1 and 6 cycles of intake, after which there is no increase in concentration. Metabolism After ingestion, drospirenone is extensively metabolized. Most plasma metabolites are represented by the acidic forms of drospirenone. Drospirenone is also a substrate for oxidative metabolism catalyzed by the cytochrome P450 isoenzyme CYP3A4. Injection The serum metabolic clearance rate of drospirenone in the serum is 1.5 ± 0.2 ml / min / kg. In unchanged form, drospirenone is displayed only in trace amounts. Metabolites of drospirenone are excreted through the intestine and the kidneys in a ratio of approximately 1.2: 1.4. T1 / 2 is approximately 40 hours. The pharmacokinetics in special clinical situations Css Drospirenone in serum in women with mild renal insufficiency (CC 50-80 ml / min) were comparable to those in women with normal renal function (CC> 80 ml / min) In women with moderately severe renal failure (CK 30–50 ml / min), the serum level of drospirenone was, on average, 37% higher than in women with normal renal function. Drospirenone treatment was well tolerated in all groups. The intake of drospirenone did not have a clinically significant effect on serum potassium concentration. The pharmacokinetics of severe renal failure has not been studied. Drospirenone is well tolerated by patients with mild to moderate hepatic insufficiency (class B on the Child-Pugh scale). The pharmacokinetics for severe liver failure has not been studied. Ethinyl estradiol Absorption After ingestion, ethinyl estradiol is rapidly and completely absorbed.Cmax after a single ingestion is achieved in 1-2 hours and is about 88-100 pg / ml. Absolute bioavailability as a result of presystemic conjugation and metabolism during the first passage through the liver is approximately 60%. Concomitant food intake reduces the bioavailability of ethinyl estradiol in about 25% of those examined, while other participants in the study did not show similar changes. Distribution The concentration of ethinyl estradiol in serum decreases biphasic, T1 / 2 of the terminal phase - 24 hours. Ethinyl estradiol is largely but not specifically associated with serum albumin (about 98.5%) and causes an increase in serum SHBG concentrations. The apparent Vd is about 5 l / kg. Equilibrium concentration (Css) is reached during the second half of the treatment cycle, with the serum level of ethinyl estradiol increasing about 1.5-2.3 times. Metabolism Ethinyl estradiol undergoes significant primary metabolism in the intestine and liver. Ethinyl estradiol and its oxidative metabolites are primarily conjugated to glucuronides or sulfate. The rate of metabolic clearance of ethinyl estradiol is about 5 ml / min / kg. Injection of ethynyl estradiol is practically not excreted unchanged. Ethinyl estradiol metabolites are excreted by the kidneys and through the intestine in a ratio of 4: 6. T1 / 2 metabolites - 24 h.
Indications
- contraception; - contraception and treatment of moderate acne (acne vulgaris); - contraception and treatment of the severe form of premenstrual syndrome.
Contraindications
Drug jess; contraindicated in the presence of any of the conditions listed below; if any of these conditions / diseases develop for the first time while receiving, the drug should be immediately canceled: - thrombosis (venous and arterial) and thromboembolism at present or in history (including deep vein thrombosis, pulmonary thromboembolism, heart attack) myocardium), cerebrovascular disorders; conditions that precede thrombosis (including transient ischemic attacks, angina pectoris) currently or in history; revealed acquired or hereditary predisposition to venous or arterial thrombus zu, including resistance to activated protein C, antithrombin III deficiency, protein C deficiency, protein deficit S, hyperhomocysteinemiaantibodies to phospholipids (antibodies to cardiolipin, lupus anticoagulant); - high risk of venous or arterial thrombosis; - migraine with focal neurological symptoms now or in history; - diabetes mellitus with vascular complications; - liver failure and severe liver disease (before as long as the liver tests are not normalized); - liver tumors (benign or malignant) now or in history; - severe renal failure, acute renal failure ; - adrenal insufficiency; - identified hormone-dependent malignant diseases (including genital organs or mammary glands) or suspicion of them; - bleeding from the vagina of unclear genesis; - pregnancy or suspicion of it; - breastfeeding period; - lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the drug contains lactose monohydrate); - hypersensitivity to any of the components of the drug Jess;. Use with caution. If any of the conditions / factors are rice as listed below, are available now, you should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptives in each individual case: - risk factors for thrombosis and thromboembolism (smoking; thrombosis, myocardial infarction or cerebral circulation at a young age in one of the closest relatives; obesity; dyslipoproteinemia; arterial hypertension; migraine; valvular disease; heart rhythm disorder; prolonged immobilization; serious surgery; extensive trauma); - other diseases in which disorders of the peripheral circulation can be noted (diabetes mellitus; systemic lupus erythematosus; hemolytic uremic syndrome; Crohn's disease and ulcerative colitis; sickle cell anemia; phlebitis of superficial veins); hypertriglyceridemia; - liver disease; - diseases that first arose or worsened during pregnancy or against the background of previous intake of sex hormones (for example, jaundice, cholestasis, cholelithia h, otosclerosis with impairment of hearing, porphyria, herpes pregnant,Sydenhem's chorea); - postpartum period. Use during pregnancy and lactation. Use of the drug Jess; contraindicated during pregnancy and during breastfeeding. The possibility of pregnancy should not be excluded in any patient with preserved reproductive potential in the presence of symptoms characteristic of pregnancy, especially in those who did not comply with the regimen of the drug. only the absence of withdrawal bleeding during the 4-day free period of taking the pills (flexible mode) or against the background of the intake of white inactive pills (24 + 4 mode), but also the appearance of mornings weakness, vomiting, or swelling of the mammary glands, although not all women develop these symptoms and, in addition, they can be caused by other causes. The withdrawal bleeding does not occur, as usual, every 4 weeks, but usually develops every 4 weeks. 120 days, depending on when the patient chooses a 4-day break in taking the pills. Therefore, the absence of withdrawal bleeding cannot be used as a sign of an unforeseen pregnancy. In such cases, there are difficulties with the timely diagnosis of pregnancy. Although the onset of pregnancy with strict adherence to the mode of administration of the drug Jess; unlikely, if you suspect a pregnancy, you must immediately stop taking the drug Jess ;, consult a doctor and perform a pregnancy test. If the patient is planning a pregnancy, she may stop taking the drug Jess; Anytime. If the patient simultaneously takes potentially dangerous (teratogenic) drugs for the fetus and therefore needs to prevent pregnancy, the decision on the possibility of discontinuing the drug Jess; can be taken only after consulting a doctor. If pregnancy is detected while taking the drug Jess; the drug should be immediately canceled. However, extensive epidemiological studies have not revealed any increased risk of developmental defects in children born to women who received sex hormones (including combined oral contraceptives) before pregnancy, or teratogenic effects, when sex hormones were taken by negligence in the early stages of pregnancy. Existing results use of the drug Jess; during pregnancy are limited, which does not allow to draw any conclusions about the effect of the drug on the course of pregnancy, the health of the newborn and the fetus.Any significant epidemiological data on the drug Jess; currently not available. Reception of combined oral contraceptives may reduce the amount of breast milk and change its composition, therefore, their use is not recommended until breastfeeding is stopped. A small amount of sex hormones and / or their metabolites can penetrate into breast milk and affect the body of the newborn.
Use during pregnancy and lactation
Use of the drug Jess; contraindicated during pregnancy and during breastfeeding. The possibility of pregnancy should not be excluded in any patient with preserved reproductive potential in the presence of symptoms characteristic of pregnancy, especially in those who did not comply with the regimen of the drug. only the absence of withdrawal bleeding during the 4-day free period of taking the pills (flexible mode) or against the background of the intake of white inactive pills (24 + 4 mode), but also the appearance of mornings weakness, vomiting, or swelling of the mammary glands, although not all women develop these symptoms and, in addition, they can be caused by other causes. The withdrawal bleeding does not occur, as usual, every 4 weeks, but usually develops every 4 weeks. 120 days, depending on when the patient chooses a 4-day break in taking the pills. Therefore, the absence of withdrawal bleeding cannot be used as a sign of an unforeseen pregnancy. In such cases, there are difficulties with the timely diagnosis of pregnancy. Although the onset of pregnancy with strict adherence to the mode of administration of the drug Jess; unlikely, if you suspect a pregnancy, you must immediately stop taking the drug Jess ;, consult a doctor and perform a pregnancy test. If the patient is planning a pregnancy, she may stop taking the drug Jess; Anytime. If the patient simultaneously takes potentially dangerous (teratogenic) drugs for the fetus and therefore needs to prevent pregnancy, the decision on the possibility of discontinuing the drug Jess; can be taken only after consulting a doctor. If pregnancy is detected while taking the drug Jess; the drug should be immediately canceled.However, extensive epidemiological studies have not revealed any increased risk of developmental defects in children born to women who received sex hormones (including combined oral contraceptives) before pregnancy, or teratogenic effects, when sex hormones were taken by negligence in the early stages of pregnancy. Existing results use of the drug Jess; during pregnancy are limited, which does not allow to draw any conclusions about the effect of the drug on the course of pregnancy, the health of the newborn and the fetus. Any significant epidemiological data on the drug Jess; currently not available. Reception of combined oral contraceptives may reduce the amount of breast milk and change its composition, therefore, their use is not recommended until breastfeeding is stopped. A small amount of sex hormones and / or their metabolites can penetrate into breast milk and affect the body of the newborn.
Dosage and administration
Acceptance mode 24 + 4Tablets should be taken in the order indicated on the package, every day at about the same time, drinking a small amount of water. Tablets are taken without interruption in the reception. It should be taken on 1 tab. / Day consistently for 28 days. Each subsequent package should begin the day after taking the last tablet from the previous package. Withdrawal bleeding, as a rule, begins on the 2-3rd day after the start of inactive (white) pills and may not be completed until the next pack. Taking pills from a new package should always be started on the same day of the week, and withdrawal bleeding will occur approximately on the same days of each month. Flexible admission schedule Flexible administration of the drug Jess; it can be used only with a click dispenser (Clyk) and flex-cartridges. The drug should be taken 1 tablet daily at the same time with a small amount of liquid. Tablets should be taken continuously for at least 24 days. Between 25 and 120 days of use of the drug Jess; By decision of the patient, a 4-day break in the pill can be taken. A break in taking pills should not exceed 4 days.A 4-day break in taking pills should be made no later than 120 days of continuous taking pills. After each 4-day break in taking the pills, a new cycle begins with a minimum duration of 24 days and a maximum duration of 120 days. As a rule, withdrawal bleeding develops during the 4-day break in taking the pills, but may not end until the next pill is taken. If during the period from 25 to 120 days for 3 consecutive days, spotting / bleeding from the vagina appears, it is recommended to take a 4-day break in taking the pills. This will reduce the total number of bleeding days. Instructions for handling the packaging of the drug Jes; for the reception mode 24 + 4B package of the drug Jess; a blister is glued in, containing 24 active hormone-containing light pink pills and 4 inactive white, hormone-free pills (last row). The package also contains a reception calendar consisting of 7 self-adhesive strips with the names of the days of the week marked on them. You should choose the strip where the first day of the week is indicated, in which it is planned to start taking pills. For example, if a woman starts taking pills on Wednesday, you need to use a strip that starts with Wed .. The strip should be glued along the top of the package so that the first day symbol is above the tablet that the arrow with the inscription Start is pointing at. Thus, it will be seen which day of the week each pill should be taken. Click Meter Dispenser Operating Instructions (Clyk) Before starting and during operation, carefully read the detailed instructions for use of the dispenser. General description of the Click dispenser (Clyk): - side keys pressing area for receiving a tablet; - button for extracting a flex-cartridge — pressing this button removes the flex-cartridge; —the issue area of the tablet — part of the dispenser in which issued pills appear — indicator of the time of taking the tablet — shows time of taking the tablet; - display - displays the main screen and menu items; - OK button - pressing the button confirms the action, for example, the beginning of a 4-day break in taking the pills and changing the reminder sound. The most important functionsActivating the new dispenser: flex cartridge ( containing 30 pills) should be removed from the package and immediately inserted into the dispenser. Insert the narrow end of the flex cartridge into the dispenser so that the dispenser window (as well as the pills in the flex cartridge) is clearly visible.The flex-cartridge should be inserted to the end. The dispenser will automatically record the dispensing time of the first tablet, setting this time as Reception Time. Thus, a woman needs to: - be sure that she unpacks and inserts the flex cartridge on the day she plans to start taking the pills; - be sure that the time for issuing the first pill will be convenient for taking the pills daily. Each 24 h on the dispenser display, a signal will appear on the arrival of the next pill reception. Removing the pill With one hand, simultaneously press both side keys to remove the pill, which is received by the other hand. Replacing the flex cartridge When used normally The flex cartridge can be removed only if it is empty; in other cases, you must follow the instructions in the detailed instructions for using the Click dispenser (Clyk). An empty flex cartridge is removed by pressing the flex cartridge removal button. The dispenser saves all information about the current cycle, and the new filled flex cartridge should be inserted in accordance with the above instructions. Before starting and during the application, carefully read the detailed instructions for use of the Clyk dispenser (Clyk) enclosed in the package with the preparation. in the absence of taking any hormonal contraceptives in the previous month, taking the drug Jess; Begin on the 1st day of the menstrual cycle (i.e., on the 1st day of menstrual bleeding), in this case no additional contraceptive measures are required. It is allowed to start taking on the 2-5th day of the menstrual cycle, but in this case it is recommended to additionally use a barrier method of contraception during the first 7 days of taking the pills from the first package. Then the pills should be taken in the order indicated for the 24 + 4 intake mode or the flexible intake regimen. When switching from other combined oral contraceptives, a vaginal ring or a contraceptive patch, it is preferable to start taking the drug Jes; the next day after taking the last active pill from the previous package, but in no case later than the next day after the usual 7-day break (for preparations containing 21 pills) or after taking the last inactive tablet (for preparations containing 28 pills per pack ).Taking the drug Jess; should begin on the day of removal of the vaginal ring or patch, but not later than the day when a new ring needs to be inserted or a new patch is pasted. contraceptive A woman can switch from taking a mini-drink to the drug Jess; on any day (without a break), from the implant or intrauterine contraceptive with the progestogen - on the day of its removal, from the injection contraceptive - on the day when the next injection should be made. In all cases, you must use an additional barrier method of contraception during the first 7 days of taking the pills. After an abortion in the first trimester of pregnancy, a woman can start taking the drug immediately after a spontaneous or medical abortion in the first trimester of pregnancy. If this condition is observed, the woman does not need additional contraceptive measures. After childbirth or abortion in the second trimester of pregnancy. The drug can be started on days 21-28 after spontaneous or medical abortion or after childbirth, in the absence of breastfeeding. If reception is started later, you must use an additional barrier method of contraception during the first 7 days of taking the pills. However, if sexual contact has already taken place, prior to the initiation of taking the drug Jess it is necessary to exclude pregnancy or it is necessary to wait for the first menstruation. Termination of taking the drug Jess; You can stop taking the drug at any time. If a woman is not planning a pregnancy, or if a woman is contraindicated because she is taking drugs that are potentially dangerous for the fetus, you should discuss other methods of contraception with your doctor. If a woman is planning a pregnancy, it is recommended to stop taking the drug and wait for the natural menstrual bleeding, and then try to get pregnant. This will help to more accurately calculate the duration of pregnancy and the time of delivery. Acceptance of missed pillsA skip of inactive pills against the background of the 24 + 4 intake mode can be ignored. However, they should be thrown away in order not to accidentally extend the intake of inactive pills. The following recommendations apply only to skipping active (light pink) pills. If the delay in taking the drug was less than 24 hours, the contraceptive protection is not reduced.A woman should take the missed pill as soon as possible, and then take the next one at the usual time. If the delay in taking the pills is more than 24 hours, the contraceptive protection can be reduced. The more pills are missed and the closer the pass of pills to the intake phase of the inactive white pills when using the 24 + 4 mode or to the free period of taking the pills on the background of a flexible intake mode, the higher the probability of pregnancy. At the same time you can be guided by the following two basic rules: - reception the drug should never be interrupted for more than 7 days (you should pay attention to the fact that the recommended interval for inactive pills is 4 days for the 24 + 4 intake mode, and for the flexible intake mode the interval without EMA pills should not exceed 4 days) - to achieve adequate suppression of the hypothalamic-pituitary-ovarian system required 7 days of continuous reception tabletok.Dozator Click (Clyk) allows control pills and warns the woman about the need for additional contraceptive method. A warning exclamation mark appears on the display when you skip a pill or take an irregular pill for more than 7 consecutive days. The exclamation mark disappears after 7 days of continuous dispensing of pills. If more than one tablet is missed, it is recommended to consult a doctor. In the case of the 24 + 4 intake mode, as well as in the flexible mode, if the information from the Clyk dispenser is not available or there are doubts about its reliability, the following recommendations should be followed: during the 1st to the 7th day of taking the pills. A woman should take the last missed pill as soon as she remembers, even if it means taking two pills at the same time. She continues to take the following pills at the usual time. In addition, over the next 7 days, you must additionally use a barrier method of contraception (for example, a condom). If sexual intercourse took place within 7 days before the missed pill, consider the possibility of pregnancy. When skipping during the 8th to the 14th day of taking the pill when taking 24 + 4 mode or when skipping over the 8th to The 24th day of taking the pills with a flexible mode of admission A woman should take the last missed pill as soon as she remembers, even if it means taking two pills at the same time.She continues to take the following pills at the usual time. Provided that the woman took the pills correctly for 7 days preceding the first missed pill, there is no need to use additional contraceptive measures. Otherwise, as well as skipping two or more pills, you must additionally use barrier methods of contraception (for example, a condom) for 7 days, and with a flexible reception mode, barrier methods of contraception should be used until the continuous period of taking the pills reaches 7 When skipping during the 15th to the 24th day of taking pills with the 24 + 4 intake mode or when skipping during the 25th to the 120th day of taking the pills with a flexible reception mode, the risk of reduced reliability is inevitable due to the approaching phase of intake of white pills in the case of the use of 24 + 4 reception mode or a period free from pills with a flexible administration regimen. You must strictly adhere to one of the following two options. Moreover, if within the 7 days preceding the first missed pill, all pills were taken correctly, there is no need to use additional contraceptive methods. Otherwise, you must use the first of the following schemes and additionally use a barrier method of contraception (for example, a condom) within 7 days.1. A woman should take the last missed pill as soon as she remembers (even if it means taking two pills at the same time). For mode 24 + 4: the following pills are taken at the usual time, until the active light pink pills in the package run out, 4 inactive white pills should be discarded and immediately start taking the pills from the next package. Withdrawal bleeding is unlikely until the active light pink pills run out in the second pack, but there may be spotting and / or breakthrough bleeding while taking the pills. In the case of a flexible regimen, take at least 7 pills (one tablet daily) without interruption. 2. For 24 + 4 mode: a woman can also stop taking active light pink pills from the current package. Then you should take a break of no more than 4 days, including the days of skipping the pills, and then start taking the drug from the new package. If a woman missed taking active light pink pills, and while taking inactive white pills, no withdrawal bleeding occurred, it is necessary to exclude pregnancy.For a flexible regimen: a woman can also take a 4-day break in taking the pills, including the day of skipping the pills to cause withdrawal bleeding, and then start a new cycle of taking the drug. If a woman misses taking the pills, and the next period of interruption in taking the pills did not result in withdrawal bleeding, consider the possibility of pregnancy. Recommendations for gastrointestinal disorders In severe gastrointestinal disorders, absorption may be incomplete, so additional contraceptive measures should be taken. 3-4 hours after taking the active light pink pill was vomiting or diarrhea, you should be guided by the recommendations when skipping pills. If a woman does not want to change her usual regimen and postpone the onset of menstruation to another day of the week, an additional active light pink pill should be taken.