Yarin plus film coated pills N28x3
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Active ingredients
Drospirenone + Ethinyl Estradiol + [Calcium levomepholinate]
Release form
Pills
Composition
In 1 active combination tablet: ethinyl estradiol (micronized, in the form of betadex clathrate) 30 mcg; drospirenone (micronized) 3 mg; calcium levofefolat (micronized) 451 mcg. Adjuvants: lactose monohydrate - 45.319 mg, microcrystalline cellulose - 24.8 mg, croscarmellose sodium - 3.2 mg, hyprolosis (5 cP) - 1.6 mg, magnesium stearate - 1.6 mg. In 1 auxiliary vitamin tablet: calcium levofefolat (micronized) 451 mcg. Adjuvants: lactose monohydrate - 48.349 mg, microcrystalline cellulose - 24.8 mg, croscarmellose sodium - 3.2 mg, hyprolosis (5 cP) - 1.6 mg, magnesium stearate - 1.6 mg.
Pharmacological effect
Yarin; Plus - a low-dose monophasic combined estrogen-progestin contraceptive drug, including active pills and auxiliary pills containing calcium levomefolat. The contraceptive effect of Yarin; Plus, mainly due to the suppression of ovulation and increasing the viscosity of the cervical secretions. In women taking combined oral contraceptives, the cycle becomes more regular, pain, intensity and duration of menstrual bleeding decrease, resulting in a reduced risk of iron deficiency anemia. There is also evidence of a reduction in the risk of endometrial cancer and ovarian cancer. To assess the risk of VTE when using the drug Yarin; (ethinyl estradiol / drospirenone at doses of 0.03 mg / 3 mg) two post-registration studies were conducted. The first prospective observational study showed that the incidence of VTE in women using Yarin; in the presence or in the absence of other risk factors for VTE was in the same range as for women using levonorgestrel-containing and other combined oral contraceptives. The second, prospective, controlled database study, in which a comparative evaluation of women using the Yarin drug; with women using other combined oral contraceptives, was also confirmed a similar frequency of VTE among all women’s cohorts. Drospirenone contained in Yarin; Plus, it has anti-mineralocorticoid activity and helps prevent hormone-dependent fluid retention, which can manifest itself in weight loss and a reduced likelihood of peripheral edema.Drospirenone also has antiandrogenic activity and helps reduce acne (acne), oily skin and hair (seborrhea). These features of drospirenone should be considered when choosing a contraceptive for women with hormone-dependent fluid retention, as well as women with acne and seborrhea. According to its characteristics, drospirenone is similar to the natural progesterone produced by the female body. When properly used, the Pearl index (an indicator reflecting the number of pregnancies in 100 women using a contraceptive during the year) is less than 1. If you skip the pills or misuse, the Pearl index may increase. methyltetrahydrofolate (L-5-methyl-THF), the main folate form found in food. The average concentration of L-5-methyltetrahydrofolate in the blood plasma of people who do not eat food enriched with folic acid is about 15 nmol / l. Levomefolat, unlike folic acid, is a biologically active form of folate. Because of this, it is absorbed better than folic acid. Levomefolat is indicated to meet the increased need and provide the necessary folate content in the woman’s body during pregnancy and lactation. Introduction of calcium levomefolata to the oral contraceptive reduces the risk of developing a fetal neural tube defect if a woman becomes pregnant immediately after discontinuation of the use of contraception (or, in very rare cases, when using oral contraception).
Pharmacokinetics
Drospirenone. Absorption: After oral administration, drospirenone is rapidly and almost completely absorbed. After a single oral administration, Cmax of drospirenone in plasma of 38 ng / ml is achieved in 1-2 hours. Eating does not affect bioavailability, which ranges from 76% to 85%. Distribution: Drospirenone is bound to serum albumin and is not binds to 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, 95-97% binds non-specifically to albumin. An ethinyl estradiol-induced increase in SHBG does not affect the binding of drospirenone to plasma proteins.The average apparent Vd is 3.7–4.2 l / kg. The concentration of SHBG does not affect the pharmacokinetics of drospirenone. With daily use of the drug inside the concentration of drospirenone in the blood plasma increases by 2-3 times, Css is achieved after 8 days of taking the drug. Metabolism: After oral administration, 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 CYP3A4 isoenzyme. The rate of clearance of drospirenone from plasma is 1.2-1.5 ml / min / kg. Excretion: The concentration of drospirenone in the blood plasma decreases two-phase. T1 / 2 of drospirenone in the second phase is about 31 hours. In unchanged form, drospirenone is excreted in trace amounts. Its metabolites are excreted through the gastrointestinal tract and kidneys in a ratio of approximately 1.2: 1.4. T1 / 2 metabolites is approximately 40 hours. Pharmacokinetics in special groups of patients: Studies have shown that the concentration of drospirenone in the blood plasma of women with mild renal impairment (CC 50-80 ml / min) when reaching equilibrium and in women with intact kidney function (QC more than 80 ml / min) are comparable. However, in women with moderate renal dysfunction (CC 30-50 ml / min), the average concentration of drospirenone in the blood plasma was 37% higher than in patients with preserved renal function. There was no change in the concentration of potassium in the blood plasma when using drospirenone. In women with moderate liver dysfunction (class B on the Child-Pugh scale), AUC is comparable to the corresponding indicator in healthy women with similar Cmax values in the phase of absorption and distribution. T1 / 2 of drospirenone in patients with moderately impaired liver function was 1.8 times higher than in healthy volunteers with intact liver function. In patients with moderately impaired liver function, clearance of drospirenone was reduced by approximately 50% compared with women with preserved liver function, there were no differences in the concentration of potassium in the blood plasma in the studied groups. When diabetes mellitus is detected and the concomitant use of spironolactone (both states are regarded as factors predisposing to the development of hyperkalemia), an increase in the concentration of potassium in the blood plasma has not been established. The tolerability of drospirenone in women with mild and moderate liver dysfunction is good (class B on the Child-Pugh scale). Ethinyl estradiol. Absorption: After oral administration, ethinyl estradiol is quickly and completely absorbed.Cmax is achieved within 1-2 hours and is 100 pg / ml. During suction and first passage through the liver, ethinyl estradiol is metabolized, with the result that its bioavailability when taken orally averages about 45% with a high interindividual variability - from 20% to 65%. Simultaneous food intake in some cases is accompanied by a 25% decrease in the bioavailability of ethinyl estradiol. Distribution: Ethinyl estradiol is nonspecific but firmly bound to plasma albumin (about 98%) and induces an increase in plasma concentration of SHBG. Estimated Vd is 5 l / kg. Equilibrium concentration (Css) is reached in the second half of the intake cycle, when the concentration of ethinyl estradiol in the blood plasma increases by 40-110% compared with a single dose. 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. Output: The decrease in the concentration of ethinyl estradiol in the blood plasma is biphasic; The first phase is characterized by T1 / 2 about 1 hour, the second - 20 hours. Ethinyl estradiol is excreted only in the form of metabolites by the kidneys and through the intestine in a 4: 6 ratio with T1 / 2 about 24 hours. Pharmacokinetics in special groups of patients: The influence of ethnicity has not been established (( The study was conducted on cohorts of women of the Caucasian race and Japanese women on the pharmacokinetic parameters of Drospirenone and Ethinyl Estradiol. Levomefolat calcium. Absorption: After ingestion of calcium, levomefolat is rapidly absorbed and included in the body folate pool. After a single oral administration of calcium, levomefolata at a dose of 451 μg in 0.5–1.5 h Cmax becomes 50 nmol / l higher than the initial concentration. Distribution: The pharmacokinetics of folate has a two-phase character: the folate pool is determined with a fast and slow metabolism. A pool with a fast metabolism is likely to represent folates in the body, which is consistent with T1 / 2 of calcium levomefolat, which is about 4-5 hours after it is taken orally at a dose of 451 μg. The slow metabolism pool reflects the conversion of polyglutamate folate, T1 / 2 of which is about 100 days.Inward-entering folates and folates going through the hepato-hepatic cycle maintain the constant concentration of L-5-methyl-THF in the body. L-5-methyl-THF represents the main form of folate in the body in which they are delivered to peripheral tissues to participate in the cellular folate metabolism. Equilibrium concentration (Css) of L-5-methyl-THF in the blood plasma after ingestion of calcium levomefolata at a dose of 451 μg is reached after 8-16 weeks and depends on its initial concentration. In erythrocytes, Css is achieved at a later date due to the erythrocyte life span, which is about 120 days. Metabolism: L-5-methyl-THF represents the main folate transported form in plasma. When comparing 451 μg of calcium levomefolata and 400 μg of folic acid, similar mechanisms of metabolism were established for other significant folates. Folate coenzymes are involved in 3 major conjugated metabolic cycles in the cytoplasm of cells. These cycles are necessary for the synthesis of thymidine and purines, precursors of DNA and RNA, as well as for the synthesis of methionine from homocysteine and the conversion of serine to glycine. Excretion: L-5-methyl-THF is excreted by the kidneys unchanged and in the form of metabolites, as well as through the intestines .
Indications
Contraception, intended primarily for women with symptoms of hormone-dependent fluid retention in the body; - contraception and treatment of moderate acne (acne vulgaris); - contraception in women with folate deficiency.
Contraindications
Drug Yarin; Plus is contraindicated in the presence of any of the conditions / diseases 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 venous thrombosis, pulmonary thromboembolism, heart attack) myocardium, cerebrovascular disorders); - conditions preceding thrombosis (including transient ischemic attacks, angina pectoris) currently or in history; - revealed acquired or hereditary predisposition to venous or arterial thrombosis y, including resistance to activated protein C, antithrombin III deficiency, protein deficit S, protein C deficiency, hyperhomocysteinemia,antibodies to phospholipids (antibodies to cardiolipin, lupus anticoagulant); - high risk of venous or arterial thrombosis; - migraine with focal neurological symptoms now or in history; - pancreatitis with severe hypertriglyceridemia, currently or anamnesis, or anamnesis; vascular complications - liver failure and severe liver disease (before normalization of liver tests); - severe and / or acute renal failure; - liver tumors (benign or malignant) natural) now or in history; identified hormone-dependent malignant neoplasms (including genital organs or mammary glands) or suspicion of them; bleeding from vaginal obscure genesis; pregnancy or suspicion of it; breastfeeding period; - rare hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption (due to the lactose content); - hypersensitivity or intolerance to any of the components of the Yarin preparation; A plus.
Precautionary measures
The potential risk and expected benefit of using Yarin should be assessed; Plus in each individual case with the following diseases / conditions and risk factors: - risk factors for thrombosis and thromboembolism: smoking, obesity, dyslipoproteinemia, controlled arterial hypertension, migraine without focal neurological symptoms, uncomplicated valvular heart disease, hereditary predisposition to thrombus. , myocardial infarction or impaired cerebral circulation at a young age in any of the closest relatives); - other diseases in which they may be noted Peripheral circulatory disorders: diabetes mellitus without vascular complications, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease and ulcerative colitis, sickle cell anemia, phlebitis of superficial veins; - hereditary angioedema; - hemorrhagglyceridemia; contraindications; - diseases that first arose or worsened during pregnancy or against the background of previous intake of sex hormones (for example, jaundice and / or itching associated with cholestasis, cholelitis az, otosclerosis with hearing impairment, porphyria, herpes, pregnancy,Chorea Sydenhem); - The postpartum period (not earlier than 21-28 days after giving birth in the absence of breastfeeding).
Use during pregnancy and lactation
The drug is contraindicated in pregnancy. If pregnancy is detected while taking the drug Yarin; Plus, the drug should be immediately lifted. Data on the results of the use of the drug Yarin; Plus, pregnancy is limited, and do not allow to draw any conclusions about the negative impact of the drug on pregnancy, the health of the fetus and the newborn child. At the same time, extensive epidemiological studies have not revealed an increased risk of developmental defects in children born to women who took combined oral contraceptives before pregnancy or a teratogenic effect in cases of taking combined oral contraceptives during early pregnancy. Specific epidemiological studies on the drug Yarin; Plus was not carried out. The drug is contraindicated in the period of breastfeeding. The drug can reduce the amount of breast milk and change its composition, therefore, the use of the drug is contraindicated until the termination of breastfeeding. A small amount of sex hormones and / or their metabolites may be excreted in breast milk and affect the health of the child.
Dosage and administration
Tablets should be taken orally in the order indicated on the package, every day at the same time, without chewing, with a small amount of water. Take 1 tab. / Day continuously for 28 days. Taking the pills from the next package should be started immediately after the completion of the previous package. Blood flow withdrawal usually starts 2-3 days after the start of taking the inactive pills and may not finish before taking the pills from the next package. In the package of Yarin; Plus includes 1 or 3 blisters, which contain 21 active pills and 7 auxiliary 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. It is necessary to choose a strip where the day of the week is indicated first, on which the pill begins.For example, if the start of taking pills falls on the medium, you should 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 on which day of the week each pill should be taken. The beginning of the drug Yarin; Plus: In the absence of taking any hormonal contraceptives in the previous month, taking the drug Yarin; Plus, you should start on the 1st day of the menstrual cycle (ie, on the 1st day of menstrual bleeding). The drug Yarin; Plus begins to act immediately, so there is no need to use additional barrier methods of contraception. It is allowed to start taking the drug 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. When switching from other combined contraceptive drugs, vaginal ring or transdermal patch, it is preferable to start taking Yarin; Plus the next day after taking the last active tablet from the previous package, but in no case no later than the next day after the usual 7-day break (for drugs containing 21 pills) or after taking the last inactive tablet (for drugs containing 28 pills packaged). Taking the drug Yarin; Plus, you should start on the day of removal of the vaginal ring or patch, but not later than the day when a new patch should be introduced or a new patch is pasted. When switching from contraceptives containing only gestagens (mini-pili, injection forms, implant), or with an intrauterine device systems with the release of progestogen can go with a mini-drank drug Yarin; Plus on any day (without a break), from an implant or IUD with a progestogen - on the day of its removal, from an injection contraceptive - on the day when the next injection should be given. In all cases, you must use an additional barrier method of contraception during the first 7 days of taking the pills. After an abortion (including spontaneous) in the first trimester of pregnancy, you can start taking the drug immediately.If this condition is observed, the woman does not need additional contraception. After childbirth (in the absence of breastfeeding) or abortion (including spontaneous), it is recommended to start the drug in the second trimester of pregnancy no earlier than 21-28 days after delivery (in the absence of breastfeeding ) or abortion in the II trimester of pregnancy. If reception is started later, you must use an additional barrier method of contraception during the first 7 days of taking the pills. If sexual intercourse took place before the start of the drug Yarin; Plus, you must exclude pregnancy or wait for the first menstruation. Acceptance of missed pills: Skipping inactive pills 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 pills: If the delay in taking any active pill is less than 12 hours, the contraceptive protection of Yarin; Plus persists. You must take the missed pill as soon as possible, and take the next pill at the usual time. If the delay in taking any active pill is more than 12 hours, contraceptive protection may be reduced. The more pills in a row are missed and the closer the pass to the beginning of the reception or the end of the reception, the greater the likelihood of pregnancy. At the same time, you can be guided by the following two basic rules: 1. The drug should never be interrupted for more than 7 days. To achieve adequate suppression of the hypothalamic-pituitary-ovarian regulation, it takes 7 days to continuously take active pills. Accordingly, if the delay in taking active pills was more than 12 hours (the interval since the last tablet was taken more than 36 hours), we can recommend the following: : You must take the missed pill as soon as possible, as soon as the woman remembers it (even if it means taking two pills at the same time). The following pills should be taken 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 pill is missed, the likelihood of pregnancy must be considered. Second week of taking the drug: You must take the missed pill as soon as possible when the woman remembers (even if it means taking two pills at the same time).The following pills should be taken at the usual time. Subject to the admission pills for 7 days preceding the first missed pill, there is no need to use additional measures of contraception. Otherwise, as well as skipping two or more pills, you must additionally use barrier methods of contraception for 7 days. The third week of taking the drug: The risk of pregnancy increases due to the approaching phase of taking inactive pills. It is necessary to strictly adhere to one of the following two options: - if within the 7 days preceding the first missed pill, all pills were taken correctly, additional contraceptive methods are not necessary. When taking missed pills, you should be guided by points 1 or 2. - if during the 7 days preceding the first missed pill, the pills were taken incorrectly, then over the next 7 days you must additionally use a barrier method of contraception (for example, a condom) and in this case you should be guided clause 1 for taking missed pills.1. You must take the missed pill as soon as possible as soon as the woman remembers this (even if it means taking two pills at the same time). The following pills are taken at the usual time until the orange (active) pills in the package run out. Seven light orange (auxiliary) pills should be discarded and the orange (active) pills should be taken from the new package immediately. Until the orange (active) pills from the second package run out, withdrawal bleeding is unlikely, but there may be spotting and / or breakthrough bleeding. Stop taking the orange (active) pills from the current package, then take a break for 7 days or less (including the days of missing the pills), after which you should start taking the drug from the new package. If the woman missed taking the orange (active) pills and while taking the light -orange (auxiliary) pills, no withdrawal bleeding has occurred, it is necessary to make sure that there is no pregnancy. Recommendations for gastrointestinal disorders: In severe gastrointestinal disorders, absorption may be incomplete, This should additionally use a barrier method kontratseptsii.Esli vomiting or diarrhea develops within 3-4 h after administration of active pills to be guided to the recommendations when skipping pills.If a woman does not want to change her usual regimen and transfer the onset of menstruation to another day of the week, an additional active pill should be taken from another package. Delaying the onset of menstrual bleeding: To delay the onset of menstrual bleeding, you should skip taking 7 inactive (light orange) pills from the current package and start taking active (orange) pills from the next package of Yarin; A plus. If a woman has taken all the active pills from the second package, you should also take 7 inactive (light orange) pills and start taking the pills from the new package right away. Thus, the cycle can be extended at will for any period, up to 3 weeks, incl. until all active pills from the second package are taken. If it is necessary that menstrual bleeding starts earlier, you should stop taking active (orange) pills from the second package, discard it and take a break in taking the drug for no more than 7 days, and then start taking pills from new packaging. In this case, menstrual bleeding will begin approximately 2-3 days after taking the last active (orange) tablet from the second package. While taking the drug Yarin; Plus from the second package may be spotting and / or breakthrough bleeding. Changing the day of the start of menstrual bleeding If a woman takes the pill as recommended, menstrual-like bleeding will occur about the same day every 4 weeks. If the woman wants to change the day the menstrual-like bleeding begins , you should stop taking inactive (light orange) pills for as many days as necessary to change the beginning of the menstrual blood. For example, if the cycle usually begins on Friday, and in the future a woman wants it to start on Tuesday (3 days earlier), the pills from the next package should be started 3 days earlier than usual, i.e. Do not take the last 3 inactive (light orange) pills from the current package and start taking the pills from the next package. The fewer inactive (light orange) pills a woman takes, the higher the likelihood that menstrual bleeding will not occur. While taking the drug Yarin; Plus from the next package may be spotting and / or breakthrough bleeding. Termination of taking Yarin; Plus: You can stop taking Yarin; Plus anytime.If pregnancy is not planned, you should take care of other methods of contraception. If pregnancy is planned, you should simply stop taking the drug. Special categories of patients: The efficacy and safety of Yarin; Plus studied in women of reproductive age. It is assumed that the efficacy and safety of the drug in post-pubertal age up to 18 years of age are similar to those in women over 18 years of age. Use of the drug is contraindicated before the menstrual cycle is established. The drug is not indicated after menopause. The drug is contraindicated for use in women with severely impaired liver function. The drug is contraindicated for use in women with severely impaired renal function and with acute renal failure.
Side effects
Data on the incidence of adverse reactions, which were reported during clinical trials of the drug Yarin; involving 2614 patients, are shown below. Adverse reactions described for the drug Yarin ;, can also be attributed to the drug Yarin; Plus (the difference is only in the presence of calcium levomefolata, which is a stabilized salt of the natural folates contained in food). Within each group, selected depending on the frequency of occurrence, adverse reactions are presented in order of decreasing severity. In terms of frequency, they are separated as follows: often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100) and rarely (≥1 / 10 000 and <1/1000). For additional adverse reactions identified only in the process of post-marketing research, and for which it was not possible to estimate the frequency of occurrence, the frequency is unknown. From the immune system: frequency is unknown - hypersensitivity reactions. From the metabolic and nutritional side: infrequently - weight change , fluid retention. Mental disorders: often - depressed mood; infrequently - a change in libido; frequency is unknown - mood swings. From the nervous system: often - headache, migraine. From the organ of vision: frequency is unknown - intolerance of contact lenses. From the organ of hearing: rarely - hypoacusia. From the cardiovascular system: infrequently - increase in blood pressure , lowering blood pressure; rarely - thromboembolism. On the part of the respiratory system: rarely - bronchial asthma. On the side of the gastrointestinal tract: often - nausea; infrequently - vomiting; frequency is unknown - abdominal pain, diarrhea. On the side of the skin and subcutaneous tissues: rarely - acne, eczema, itching, alopecia; frequency is unknown - rash, urticaria, erythema nodosum,erythema multiforme. From the genitals and mammary gland: often - pain in the mammary glands (including breast engorgement), breast tenderness, leucorrhea (including vaginal secretions), vulvovaginal candidiasis, absence of menstrual bleeding, painful menstrual bleeding, abundant menstrual bleeding scanty menstrual-like discharge, absence of menstrual-like bleeding, acyclic bleeding (usually reduced with prolonged use of prepar ata); infrequently - vaginitis; rarely - discharge from the mammary glands; frequency unknown - increase in mammary glands. Adverse events were classified using the MedDRA dictionary. Synonyms or conditions related to adverse reactions are not listed, but they should also be taken into account. The following serious adverse reactions have been reported in women using combined oral contraceptives: - venous thromboembolic disorders; - arterial thromboembolic disorders; - cerebrovascular disorders; - increased blood pressure; - hyperkalemia (in patients with impaired renal function and serum potassium concentration in excess of the reference values before starting the use of the drug); - hypertriglyceridemia; - changes in glucose tolerance or effects on peripheral insulin resistance; - liver tumors (benign and malignant); - functional impairment of the liver; - chloasma; - in women with hereditary angioedema, exogenous estrogens can cause or exacerbate the symptoms of angiography; the onset or deterioration of conditions for which the association with the use of combined oral contraceptives is not indisputable: jaundice and / or itching associated with x lestazom; the formation of gallbladder stones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; Chorea Sydenham; herpes pregnant; hearing loss associated with otosclerosis; Crohn's disease; ulcerative colitis; cervical cancer. The frequency of diagnosing breast cancer in women using oral contraceptives is very slightly elevated.Breast cancer is rarely observed in women under the age of 40 years, the excess frequency is negligible relative to the overall risk of developing breast cancer. The causal relationship of breast cancer with the use of combined oral contraceptives has not been established.
Overdose
About cases of drug overdose Yarin; Plus not reported. Symptoms that may occur during an overdose: nausea, vomiting, spotting from the vagina or metrorrhagia (often in young women). Treatment: there is no specific antidote, should be carried out