Active substanceDrospirenone + EthinylestradiolDrospirenone + Ethinylestradiol
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  • Dosage form: & nbsppills
    Composition:

    Each tablet contains:

    Active substances: drospirenone 3,000 mg; ethinylestradiol 0.030 mg;

    Excipients:

    lactose monohydrate 72.010 mg, corn starch 2,000 mg, crospovidone 1,400 mg, povidone K-25 0.800 mg, magnesium stearate 0.600 mg, iron oxide yellow 0.160 mg.

    Description:

    Yellow round biconvex tablets with engraving "143" on one side and even on the other side.

    Pharmacotherapeutic group:Contraceptive agent combined (estrogen + progestogen)
    ATX: & nbsp

    G.03.A.A.12   Drospirenone and ethinylestradiol

    Pharmacodynamics:

    Preparation Yamera - monophasic low-dose combined oral contraceptive estrogen-progestin medication.

    Yamera contraceptive effect of the drug is carried out primarily by suppressing ovulation and increase the viscosity of cervical secretions.

    When used properly, Pearl Index (an indicator of the number of pregnancies in 100 women using contraceptive within one year) is less than 1. When skipping tablets or incorrect application Pearl index may increase.

    The incidence of venous thromboembolism (VTE) in women with risk factors for venous thromboembolism or without applying the drospirenone + etinilestradiolsoderzhaschie oral contraceptives 3 mg + 0.03 mg, the same as in women using levonorgestrel-containing combined oral contraceptives (COCs ) or other COCs. This was confirmed in a prospective controlled study database, in which the comparing women using oral contraceptives 3 mg drospirenone + 0.03 mg ethinylestradiol with women using other COCs.Analysis of the data revealed the same risk of occurrence of VTE among the sample.

    In women taking COC, the cycle becomes more regular, less painful menstrual-like bleeding is observed, the intensity and duration of bleeding decreases, resulting in a reduced risk of iron deficiency anemia. There is also evidence of a reduced risk of endometrial and ovarian cancer. Drospirenone, which is a part of the drug Jamera, has antimineralocorticoid action and is able to prevent weight gain and other symptoms (eg edema) associated with estrogen-dependent fluid retention. Drospirenone also has anti-androgenic activity and helps reduce acne (acne), oiliness of the skin and hair (seborrhea). This effect of drospirenone is similar to the action of natural progesterone, produced by the female body. This should be considered when choosing a contraceptive, especially for women with hormone-dependent fluid retention, as well as women with acne and seborrhea.

    Pharmacokinetics:

    Drospyrenone

    Absorption

    When administered orally, drospirenone quickly and almost completely absorbed.After a single oral intake, the maximum concentration (Cmah) drospirenone in serum, equal to 38 ng / ml, is achieved after 1-2 hours. Bioavailability ranges from 76% to 85%. Eating does not affect the bioavailability of drospirenone.

    Distribution

    Drospirenone binds to plasma albumin (95-97%) and does not bind to sex hormone binding globulin (SHBG), or corticosteroid-binding globulin (CSG). In the free form is only 3-5% of the total concentration in the blood plasma. The increase in SHBG induced by ethinyl estradiol does not affect the binding of drospirenone with plasma proteins.

    After oral administration, drospirenone is completely metabolized.

    Most metabolites in the blood plasma are acidic forms of drospirenone, which are formed without the involvement of cytochrome P450.

    Excretion

    The concentration of drospirenone in the blood plasma is reduced in 2 phases. In unmodified form, drospirenone is excreted in trace amounts. Metabolites of drospirenone are excreted by the kidneys and through the intestine in a ratio of approximately 1.2: 1.4. The half-life (T1 / 2) for excretion of metabolites by the kidneys and through the intestine is approximately 40 h.

    The equilibrium concentration

    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 2-3 times, the equilibrium concentration is reached after 8 days of taking the drug.

    Pharmacokinetics in special clinical cases

    When a violation of liver function

    In women with moderate impaired liver function (class B on the Child-Pugh scale), the area under the concentration-time curve (AUC) is comparable with the corresponding index in healthy women with close values ​​of Cmin the absorption and distribution phases. T1 / 2 drospirenone in women with moderate impaired liver function was 1.8 times higher than in healthy volunteers with preserved liver function.

    In women with moderate impairment of liver function, a decrease in clearance of drospirenone by 50% was observed compared to women with preserved liver function, and there was no difference in the potassium concentration in the blood plasma in the studied groups. In the detection of diabetes mellitus and concomitant use of spironolactone (both conditions are regarded as factors predisposing to the development of hyperkalemia), an increase in the concentration of potassium in the blood plasma is not established.It should be concluded that tolerability of drospirenone in women with mild and moderate impairment of liver function is good (class B on the Child-Pugh scale).

    In case of impaired renal function

    The concentration of drospirenone in blood plasma upon reaching the equilibrium state was comparable in women with mild renal impairment (creatinine clearance (KC) - 50-80 ml / min) and in women with a preserved kidney function (KC - more than 80 ml / min). However, less, in women with moderate renal dysfunction (CK - 30-50 ml / min), the average concentration of drospirenone in the blood plasma was 37% higher than in patients with preserved kidney function. Drospirenone was well tolerated by all groups of women. There was no change in the concentration of potassium in blood plasma with drospirenone.

    Ethnicity

    There is no evidence of the influence of ethnicity (the study was conducted on cohorts of women of the Caucasian and Japanese women) on the parameters of the pharmacokinetics of drospirenone and ethinylestradiol.

    Ethinylestradiol

    Absorption

    After oral administration ethinyl estradiol quickly and completely absorbed. FROM max in blood plasma, equal to 100 pg / ml, is achieved within 1-2 hours.During suction and "first pass" through the liver ethinyl estradiol is metabolized, as a result of which its bioavailability when ingested is an average of about 45%.

    Distribution

    Ethinyl estradiol, non-specifically, but firmly binds to blood plasma albumin (about 98%) and induces an increase in the concentration in the plasma of SHBG. The estimated volume of distribution is 5 l / kg.

    Metabolism

    Ethinyl estradiol undergoes presystemic conjugation, both in the mucosa of the small intestine and in the liver. The main pathway of metabolism is aromatic hydroxylation.

    Excretion

    Reduction in the concentration of ethinyl estradiol in blood plasma is biphasic; the first phase is characterized by Tt about 1 hour, the second - 20 hours. Ethinylestradiol almost not output in unmodified form. Metabolites of ethinyl estradiol are excreted by the kidneys and through the intestine in a ratio of 4: 6. T1 / 2 metabolites is approximately 24 hours.

    The equilibrium concentration

    The equilibrium state is reached in the second half of the cycle, when the concentration of ethinyl estradiol in the blood plasma increases by 40-110% compared with the use of a single dose.

    Indications:

    Contraception.

    Contraindications:

    The drug is contraindicated in the presence of Yamera any of the conditions / diseases / risk factors listed below. If any of these diseases / conditions or risk factors are detected or developed for the first time against the background of the drug, the taking of the drug should be stopped immediately.

    - Thrombosis (venous and arterial) and thromboembolism now or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke), cerebrovascular disorders.

    - Conditions preceding thrombosis (including, transient ischemic attacks, angina pectoris) are currently or in history.

    - Revealed acquired or hereditary predisposition to venous or arterial thrombosis, including resistance to activated protein C, deficiency of antithrombin III, protein deficiency S, hyperhomocysteinemia, antibodies to phospholipids (cardiolipin, lupus anticoagulant).

    - Migraine with focal neurologic symptoms at present or in the anamnesis.

    - Diabetes mellitus with vascular complications.

    - Multiple or expressed risk factors for venous or arterial thrombosis, including complicated heart valve disease, atrial fibrillation, cerebrovascular or coronary artery disease; uncontrolled arterial hypertension, serious surgical intervention; prolonged immobilization, extensive trauma; smoking over the age of 35; Obesity (BMI ≥ 30 kg / m2); severe dyslipoproteinemia; air flight lasting more than 4 hours.

    - Pancreatitis with severe hypertriglyceridemia at present or in the anamnesis.

    - Hepatic insufficiency and severe liver disease (before the normalization of liver tests).

    - Liver tumors (benign or malignant) are currently or in the anamnesis.

    - Severe and / or acute renal failure.

    - Revealed hormone-dependent malignant diseases (including genital organs or mammary glands) or suspected of them.

    - Bleeding from the vagina of unknown origin.

    - Pregnancy or suspicion of it.

    - Breastfeeding period.

    - Hypersensitivity to any of the components of the drug YAmer.

    - Hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

    Carefully:

    The potential risk and the expected benefit of using COCs in each individual case should be carefully weighed in the presence of the following diseases / conditions and risk factors:

    - Risk factors for thrombosis and thromboembolism: smoking; overweight (BMI more than 25 kg / m2 and less than 30 kg / m2); dyslipoproteinemia, controlled arterial hypertension; migraine without focal symptoms; heart valve flaws; hereditary predisposition to thrombosis (thrombosis, myocardial infarction, or cerebrovascular accident at the age of 50 years from any of the next of kin).

    - Other diseases not related to contraindications, in which there may be violations of peripheral circulation: diabetes mellitus; systemic lupus erythematosus; hemolytic-uremic syndrome; Crohn's disease and ulcerative colitis; sickle-cell anemia; phlebitis of superficial veins.

    - Hereditary angioedema.

    - Hypertriglyceridemia.

    - Diseases of the liver.

    - Diseases that first appeared or worsened during pregnancy or against the background of previous administration of sex hormones (eg jaundice and / or itching associated with cholestasis, cholelithiasis, otosclerosis with hearing impairment, porphyria, herpes during pregnancy, Sydenham's chorea).

    - Postpartum period.

    Pregnancy and lactation:

    The drug is contraindicated during pregnancy and during breastfeeding. There are data on the adverse effects of the drug in pregnancy and lactation in studies on animals, which does not allow to exclude such effects on the fetus or the newborn in humans.

    If pregnancy is detected during the administration of the drug, the drug should be discontinued immediately.

    Conducted epidemiological studies did not reveal an increased risk of defects in children born to women who received sex hormones before pregnancy or teratogenicity in cases of taking sex hormones by negligence in the early stages of pregnancy. The available data on the results of taking Yama's drug during pregnancy are limited, which does not allow us to draw any conclusions about the negative effect of the drug on pregnancy, the health of the newborn and the fetus.Currently, there are no significant epidemiological data.

    Admission COC can reduce the amount of breast milk and change its composition, so the use of the drug is contraindicated until the termination of breastfeeding. A small amount of sex hormones and / or their metabolites can penetrate into breast milk and influence the health of the child.

    Dosing and Administration:

    Tablets should be taken orally in the order given on the package, every day at about the same time, with a small amount of water. Take one tablet a day continuously for 21 days. Receiving tablets from the next package begins after a 7-day break, during which menstrual-like bleeding usually develops (bleeding "cancellation"). As a rule, it begins on the 2-3 day after the last pill and may not end before taking the tablets from the new package.

    How to start taking the drug YaMera

    - In the absence of taking any hormonal contraceptives in the previous month.

    Reception of the drug begins on the first day of the menstrual cycle (i.e.on the first day of menstrual bleeding). It is acceptable to start taking the menstrual cycle for 2-5 days, but in this case it is recommended to use the barrier method of contraception (for example, a condom) during the first 7 days of taking the tablets from the first package.

    - When switching from other combined hormonal contraceptive drugs (COC, vaginal ring or transdermal patch)

    It is preferable to start taking the drug on the next day after taking the last active tablet from the previous package, but in no case later than the day after the usual 7-day break (for preparations containing 21 tablets) or after taking the last inactive tablet (for drugs, containing 28 tablets in a package). Reception of the drug Yamera should be started on the day of removal vaginal ring or patch, but no later than the day when a new ring is to be inserted or a new patch is stuck.

    - In the transition from contraceptives containing only gestagens ("mini-pili", injectable forms, implant), or from the intrauterine therapeutic system with the release of the progestogen

    Go to the "mini-drink" on the drug Yamera can be any day (without interruption), with the implant or intrauterine contraceptive with gestagen - the day it is removed, with the injection form - from the day the next injection is to be made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets.

    - After abortion, including spontaneous, in the first trimester of pregnancy

    You can start taking the drug immediately - on the day of abortion. If this condition is met, the woman does not need additional contraception.

    - After childbirth or abortion in the second trimester

    You should start taking the drug no earlier than 21-28 days after giving birth (if there is no breastfeeding) or termination of pregnancy in the second trimester. If the reception is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets. However, if sexual intercourse took place before the start of the drug, the pregnancy should be ruled out.

    Acceptance of missed tablets

    If the delay in taking the drug was less than 12 hours, the contraceptive protection is not reduced. A woman should take the pill as soon as possible, the next - is taken at the usual time.

    If the delay in taking the tablets was more than 12 hours, the contraceptive protection is reduced. The more pills are missed, and the closer the pass to a 7-day break in taking pills, the greater the likelihood of pregnancy.

    It should be remembered:

    - The drug should never be interrupted for more than 7 days.

    - 7 days of continuous intake of tablets are required to achieve adequate suppression of hypothalamic-pituitary-ovarian regulation.

    Accordingly, if the delay in taking the tablets exceeds 12 hours (the interval from the time of taking the last tablet is more than 36 hours), depending on the week when the tablet is missed, it is necessary:

    - The first week of taking the drug

    It is necessary to take the last missed tablet as soon as possible, as soon as a woman remembers this (even if it is necessary take two tablets simultaneously). The next tablet is taken at the usual time. In addition, a barrier method of contraception (for example, a condom) should be used for the next 7 days. If sexual intercourse took place within a week before passing the pill, it is necessary to consider the likelihood of pregnancy.

    - The second week of taking the drug

    It is necessary to take the last missed pill as soon as possible, as soon as a woman remembers it (even if you need to take two tablets at the same time). The next tablet is taken at the usual time. Provided that the woman took the pill correctly for 7 days preceding the first missed pill, there is no need to use additional contraceptive measures. Otherwise, as well as when two or more tablets are missed, barrier methods of contraception (for example, a condom) should be used additionally within 7 days.

    - The third week of taking the drug

    The risk of reducing contraceptive reliability is inevitable due to the upcoming interruption in the intake of tablets. In this case, you must adhere to the following algorithms:

    - if within 7 days preceding the first missed tablet, all tablets were taken correctly, there is no need to use additional methods of contraception. When accepting the missed tablets, follow steps 1 or 2.

    - if within 7 days preceding the first missed tablet, the tablets were taken incorrectly,then for the next 7 days, the barrier method of contraception (for example, a condom) needs to be additionally used, and in this case, paragraph 1 should be followed to receive missed tablets.

    1. It is necessary to take the missed tablet as soon as possible, as soon as the woman remembers it (even if it means taking two tablets at the same time). The following tablets are taken at the usual time, until the tablets from the current package run out. Receiving tablets from the next package should start immediately without the usual 7-day break. Bleeding "cancellation" is unlikely until the tablets from the second package run out, but there may be "smearing" discharge and / or "breakthrough" bleeding on the days of taking the drug.

    2. You can also interrupt the taking of tablets from the current package, take a break for 7 or less days (including the days of skipping the tablets), and then start taking the tablets from the new package.

    If the woman missed taking the pills, and during the break in the reception she does not bleed "withdrawal", you must exclude pregnancy.

    It is allowed to take no more than two tablets in one day.

    Recommendations for gastrointestinal disorders

    In severe gastrointestinal disorders, absorption of the drug may be incomplete, so additional methods of contraception should be used.

    If vomiting or diarrhea occurs within 3-4 hours after taking the tablets, depending on the week of taking the drug, you should be guided by the recommendations when skipping the tablets mentioned above. If a woman does not want to change her usual schedule of taking and transfer the onset of menstruation on another day of the week, an additional pill should be taken from another package.

    Termination of the drug YaMera

    You can stop taking the drug at any time. If a woman does not plan pregnancy, care should be taken for other methods of contraception. If pregnancy is planned, you should just stop taking the drug and wait for natural menstrual bleeding.

    Postponement of menstrual bleeding

    In order to delay the onset of menstrual bleeding, it is necessary to continue taking the tablets from a new package of YaMER preparation without a 7-day break.Tablets from a new package can be taken for as long as necessary, including until the tablets from the package are exhausted. Against the background of taking the drug from the second package, there may be "smearing" spotting from the vagina and / or "breakthrough" uterine bleeding. To resume the reception of the drug YAmer from the next package follows the usual 7-day break.

    Change in the day of menstrual bleeding

    In order to postpone the start of menstrual bleeding the next day of the week, a woman should shorten (but not extend) the next 7-day break in taking pills for as many days as the woman wants. For example, if the cycle usually starts on Friday, and in the future the woman wants it to start on Tuesday (3 days earlier), taking the tablets from the next package should start 3 days earlier than usual. The shorter the break in taking the tablets, the higher the likelihood that menstrual bleeding will not occur, and during the reception of tablets from the second package, there will be "smearing" discharge and / or "breakthrough" bleeding.

    Application in separate groups of patients

    Children and teens

    The drug of Yamera is shown only after the onset of menarche. The available data are not suggest dose adjustments in this group of patients.

    Elderly age

    Not applicable. The drug is not shown after the onset of menopause.

    Impaired liver function

    The drug Yamera is contraindicated in women with severe liver disease until the liver function is normal (see also the section "Contraindications" and "Pharmacological properties").

    Impaired renal function

    The drug is contraindicated in women with severe renal failure or with acute renal failure (see also the sections "Contraindications" and "Pharmacological properties").

    Side effects:

    Data on incidence of adverse reactions reported during clinical trials of drospirenone + ethinyl estradiol (N = 4897) are shown in the table below.

    Within the limits of each group, allocated depending on the incidence, adverse reactions are presented in order of decreasing severity. In frequency, they are divided into frequent (≥1 / 100 and <1/10), infrequent (≥1 / 1000 and <1/100) and rare (≥1 / 10000 and <1/1000). For additional side reactions, revealed only in the process of post-marketing research,and for which it was not possible to estimate the incidence, "frequency is unknown" is indicated.

    System-Organ Classes (MedDRA version)

    Often

    Infrequently

    Rarely

    Frequency

    unknown

    Disorders of the psyche

    Mood swings, depression / depressed mood

    Increased libido

    Reduction or loss of libido



    Disturbances from the nervous system

    Migraine

    Headache




    Immune system disorders



    Bronchial asthma


    Hearing disorders and labyrinthine disorders



    Hearing loss


    Vascular disorders


    Reduction of blood pressure

    Venous and arterial thromboembolic complications *


    Disorders from the gastrointestinal tract

    Nausea

    Vomiting

    Diarrhea



    Disturbances from the skin and subcutaneous tissues


    Acne

    Eczema

    Itching

    Alopecia


    Erythema multiforme

    Violations of the genitals and mammary gland

    Menstrual irregularities

    Pain in the mammary glands

    Acyclic bleeding / bleeding from the genital tract

    Bleeding from the genital tract, unspecified genesis

    Candidiasis vulvovaginitis

    Sensitivity of mammary glands

    Mammary gland enlargement

    Vaginitis

    Discharge from the mammary glands


    General disorders


    Fluid retention

    Weight gain

    Weight reduction



    Adverse events in clinical trials have been codified using the MedDRA dictionary (Medical Dictionary of Regulatory Activity, version 12.1). The various MedDRA terms reflecting the same symptom were grouped together and presented as the only side reaction, in order to avoid weakening or blurring the true effect.

    * Estimated frequency according to epidemiological studies covering the COC group.

    Venous and arterial thromboembolic complications combine the following nosological forms: peripheral deep vein occlusion, thrombosis and thromboembolism / pulmonary vascular occlusion, thrombosis, embolism and myocardial infarction / cerebral infarction and stroke not classified as hemorrhagic.

    For venous and arterial thromboembolism, migraine, see also "Contraindications" and "Special instructions". The following are adverse reactions with a very low incidence or with delayed development of symptoms that are considered to be associated with the COC group.also the sections "Contraindications", "Special instructions"):

    Tumors

    - Women who use COC have a very slight increase in the incidence of breast cancer. Because breast cancer is rare in women younger than 40 years, an increase in the incidence of cancer in women using COC is insignificant in relation to the overall risk of breast cancer. The causal relationship with the use of COC is unknown.

    - Liver tumors (benign and malignant).

    Other states

    - Nodular erythema.

    - Women with hypertriglyceridemia (increased risk of pancreatitis when using COCs).

    - Increased blood pressure.

    - The onset or deterioration of conditions in which communication with the use of COCs

    is not undeniable: jaundice and / or itching associated with cholestasis; formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; chorea; herpes during pregnancy; hearing loss associated with otosclerosis.

    - In women with hereditary angioedema, exogenous estrogens can cause or exacerbate symptoms of angioedema.

    - Dysfunction of the liver.

    - Impairment of glucose tolerance or influence on peripheral insulin resistance.

    - Crohn's disease, ulcerative colitis.

    - Hloazm.

    - Hypersensitivity (including symptoms such as rash, hives).

    Interaction

    Due to the interaction of other drugs (inducers of enzymes) with oral contraceptives, "breakthrough" bleeding and / or a decrease in the contraceptive effect may occur (see section "Interaction with other drugs").

    Overdose:

    No serious violations were reported in case of an overdose. Based on the combined experience of the use of COC, symptoms that may occur during an overdose: nausea, vomiting, "spotting" spotting from the vagina or metrorrhagia.

    There is no specific antidote, symptomatic treatment should be performed.
    Interaction:

    It is possible to interact with drugs that induce microsomal enzymes of the liver, as a result of which the clearance of sex hormones can increase, which in turn can lead to "breakthrough" uterine bleeding and / or a reduction in the contraceptive effect.

    Women who are treated with such drugs in addition to the drug YaMera, it is recommended to use barrier method of contraception or choose a different non-hormonal method of contraception. The barrier method of contraception should be used during the entire period of taking concomitant medications, and also within 28 days after their withdrawal. If the period of application of the barrier method of contraception ends later than the tablets in the packaging of the drug, Yamera, you should start taking the tablets of the drug Jamera from the new package without interruption in taking the tablets.

    - Substances that increase the clearance of drospirenone + ethinylestradiol (weakening the efficiency by inducing enzymes): phenytoin, barbiturates, primidon, carbamazepine, rifampicin and, possibly, also oxcarbazepine, topiramate, felbamate, griseofulvin, as well as preparations containing St. John's wort pitted.

    - Substances with different effects on the clearance of drospirenone + ethinyl estradiol In combination with the preparation of Yama, many HIV protease inhibitors or hepatitis C virus and non-nucleicidal reverse transcriptase inhibitors may both increase,and to reduce the concentration of estrogens or progestogens in blood plasma. In some cases, such an effect may be clinically significant.

    - Substances that reduce the clearance of COCs (enzyme inhibitors)

    Strong and moderate inhibitors CYP3A4, such as azole antimycotics (eg, itraconazole, voriconazole, fluconazole), verapamil, macrolides (for example, clarithromycin, erythromycin), diltiazem and grapefruit juice can increase plasma concentrations of estrogen or progestogen, or both.

    It was shown that etorikoksib in doses of 60 and 120 mg / day, when taken together with COC containing 0.035 mg of ethinylestradiol, increases the concentration of ethinyl estradiol in blood plasma by 1.4 and 1.6 times, respectively.

    Effect of drospirenone + ethinylestradiol on other drugs COCs can affect the metabolism of other drugs, leading to an increase (for example, ciclosporin) or decrease (for example, lamotrigine) of their concentration in blood plasma and tissues.

    In vitro Drospirenone is able to weakly or moderately inhibit cytochrome P450 enzymes CYP1A1, CYP2C9, CYP2C19 and CYP3A4.

    Based on interaction studies in vivo women volunteers who took omeprazole, simvastatin and midazolam as marker substrates, it can be concluded that the clinically significant effect of 3 mg of drospirenone on the metabolism of medications mediated by cytochrome P450 enzymes is unlikely.

    In vitro ethinyl estradiol is a reversible inhibitor CYP2C19, CYP1A1 and CYP1A2, as well as an irreversible inhibitor CYP3A4/5, CYP2C8 and CYP2J2. In clinical trials, the appointment of a hormonal contraceptive containing ethinyl estradiol, did not lead to any increase or led only to a slight increase in concentrations cybctpathe CYP3A4 in plasma of blood (for example, midazolam), while plasma concentrations of substrates CYP1A2 may grow weakly (for example, theophylline) or moderately (for example, melatonin and tizanidine).

    Other forms of interaction

    In patients with intact renal function, the combined use of drospirenone and angiotensin-converting enzyme inhibitors or non-steroidal anti-inflammatory drugs does not have a significant effect on the potassium concentration in the blood plasma. However, the combined use drospirenone + ethinyl estradiol with aldosterone antagonists or potassium-sparing diuretics has not been studied. When co-administered with these drugs, the concentration of potassium in the blood plasma should be monitored during the first intake cycle (see section "Special instructions").

    Special instructions:

    If any of the conditions, diseases and risk factors identified below are present, careful consideration should be given to the potential risk and the expected benefit of using the YaMER drug in each individual case and to discuss it with a woman before she decides to start taking the drug. In the case of weighting, strengthening or the first manifestation of any of these conditions, diseases or factors risk, a woman should consult with her doctor who can decide whether to cancel the drug.

    Diseases of the cardiovascular system

    The results of epidemiological studies indicate the existence of a relationship between the use of COCs and an increase in the incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disorders) with COCs. These diseases are rare.

    The risk of developing VTE is maximal in the first year of taking COC. An increased risk is present after the initial use of COC or the resumption of the use of the same or another COC (after a break between doses of 4 weeks or more). Data from a large-scale prospective study with 3 groups of patients show that this increased risk is present mainly during the first 3 months.

    The overall risk of VTE in women taking low-dose COCs (<0.05 mg ethinyl estradiol) is 2-3 times higher than in non-pregnant patients who do not take COC, however, this risk remains lower compared to the risk of VTE during pregnancy and childbirth.

    VTE can be life threatening or lead to death (in 1-2% of cases).

    VTE, manifested as deep vein thrombosis or pulmonary embolism, can occur with any COCs.

    It rarely occurs when using COCs thrombosis other blood vessels, for example, hepatic, mesenteric, renal, and cerebral arteries veins or the retinal vascular eye.

    Symptoms of deep vein thrombosis: unilateral swelling of the lower extremity or swelling along the veins on the lower limb,pain or discomfort in the lower extremity only in the vertical position or walking, local temperature increase in the affected lower limb, redness or discoloration of the skin on the lower limb.

    Symptoms of thromboembolism of the pulmonary artery: difficulty or rapid breathing; sudden cough, including hemoptysis; acute pain in the chest, which can intensify with deep inspiration; sense of anxiety; severe dizziness; rapid or irregular heartbeat. Some of them symptoms (eg, dyspnea, cough) are nonspecific and may be misinterpreted as signs of other less severe conditions / diseases (eg, respiratory tract infections).

    Arterial thromboembolism can lead to stroke, vascular occlusion or myocardial infarction.

    Symptoms of a stroke: sudden weakness or loss of sensitivity of the face, limbs, especially on one side of the body, sudden confusion, problems with speech and understanding; sudden one- or two-sided loss of vision; sudden gait disturbance, dizziness, loss of balance or coordination of movements; sudden,severe or prolonged headache for no apparent reason; loss of consciousness or fainting with or without an epileptic seizure. Other signs of vascular occlusion: sudden pain, puffiness and weak blueing of the extremities, "sharp" abdomen.

    Symptoms of myocardial infarction: pain, discomfort, pressure, heaviness, a feeling of contraction or raspiraniya in the chest or behind the breastbone, with irradiation in the back, jaw, left upper extremity, epigastric region; cold sweats, nausea, vomiting or dizziness, severe weakness, anxiety, or shortness of breath; rapid or irregular heartbeat. Arterial thromboembolism can be life threatening or fatal.

    Women with a combination of several risk factors or high severity of one of them should consider the possibility of their mutual reinforcement. In such cases, the total value of the available risk factors is increased. In this case, the administration of the drug is contraindicated (see the section "Contraindications").

    The risk of developing thrombosis (venous and / or arterial) and thromboembolism or cerebrovascular disorders is increased:

    - with age;

    - for smokers (with an increase in the number of cigarettes smoked or an increase in the age, the risk increases, especially in women over 35);

    in the presence of:

    - obesity (BMI ≥ 30 kg / m2);

    - family history (for example, venous or arterial thromboembolism ever at close relatives or parents under the age of 50 years). In the case of a hereditary or acquired predisposition, a woman should be examined by an appropriate specialist to decide on the possibility reception of a preparation of YAmer.

    - prolonged immobilization, extensive surgical intervention, any operation on the lower extremities or extensive trauma. In these cases, the taking of the drug should be stopped (in the case of a planned operation, at least four weeks before) and do not resume taking two weeks after the end of immobilization. Temporary immobilization (for example, air travel lasting more than 4 hours) may also be a risk factor for venous thromboembolism, especially if there are other risk factors;

    - severe dyslipoproteinemia;

    - arterial hypertension;

    - migraine;

    - heart valve diseases;

    - atrial fibrillation.

    The question of the possible role of varicose veins and superficial thrombophlebitis in the development of VTE remains controversial.

    You should consider the increased risk of thromboembolism in the postpartum period. Violations of peripheral circulation can also occur in diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia.

    An increase in the frequency and severity of migraine during the use of COCs (which may precede cerebrovascular disorders) is the basis for the immediate withdrawal of these drugs.

    Biochemical indicators indicating a hereditary or acquired predisposition to venous or arterial thrombosis include the following: resistance to activated protein C, hyperhomocysteinemia, deficiency of antithrombin III, deficiency of protein C, protein deficiency S, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).

    When assessing the relationship between risk and benefit, it should be borne in mind that adequate treatment of the relevant condition can reduce the risk of thrombosis associated with it.It should also be taken into account that the risk of thrombosis and thromboembolism in pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg of ethinyl estradiol).

    Tumors

    The most significant risk factor for cervical cancer is persistent papillomavirus infection. There are reports of a slight increase in the risk of developing cervical cancer with prolonged use of COCs. but communication with the reception of the COC has not been proved. The possibility of interrelation of these data with screening of cervical disease or with features of sexual behavior (more a rare application of barrier methods of contraception).

    A meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of developing breast cancer diagnosed in women currently taking COC (relative risk 1.24). The increased risk gradually disappears within 10 years after discontinuation of these medications. Due to the fact that breast cancer is rarely seen in women under 40 years of age, an increase in the number of diagnoses of breast cancer in women who are currently taking COCs or who have recently taken COC is insignificant in relation to the overall risk of this disease. His connection with the use of COC has not been proven.The observed increase in risk may also be due to careful follow-up and earlier diagnosis of breast cancer in women using COCs. Women who have ever used COC have earlier stages of breast cancer than women who have never used them.

    In rare cases, the development of benign, and extremely rare, malignant liver tumors, which in some cases led to life-threatening intraabdominal hemorrhage, was observed with the use of COCs. In the event of severe pain in the abdomen, liver enlargement, or signs of intra-abdominal bleeding, this should be taken into account when making a differential diagnosis. Malignant tumors can be life threatening or lethal.

    Other states

    The progestin component in the preparation of Yama is an aldosterone antagonist with potassium-sparing properties. In most cases there should be no increase in the concentration of potassium in the blood plasma. In clinical studies in some patients with mild or moderate renal failure and concomitant intake of potassium-sparingthe concentration of potassium in the blood plasma increased slightly during the administration of drospirenone. Therefore, the concentration of potassium in the blood plasma should be monitored during the first cycle of taking the drug in patients with renal insufficiency and at the initial concentration potassium at the upper limit of the norm, especially with concomitant reception of potassium-sparing preparations (see the section "Interaction with other drugs").

    In women with hypertriglyceridemia (or the presence of this condition in a family history), an increased risk of developing pancreatitis during COC administration is possible.

    Despite the fact that a small increase in blood pressure was described in many women taking COC, clinically significant increases were rarely noted. Nevertheless, if a persistent, clinically significant increase in blood pressure develops during the administration of the drug, these drugs should be discontinued and the treatment of hypertension should begin. Reception of the drug can be continued if normal blood pressure values ​​are achieved with the help of antihypertensive therapy.The following conditions have been reported to develop or worsen, both during pregnancy and when taking COC, but their relationship with COCs has not been proven: jaundice and / or pruritus associated with cholestasis; formation of stones in the gallbladder; porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; chorea; herpes during pregnancy; hearing loss associated with otosclerosis. Also, cases of worsening of the course of endogenous depression, epilepsy, Crohn's disease and ulcerative colitis are described along with the use of COCs.

    In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen symptoms of angioedema.

    Acute or chronic liver dysfunction may require discontinuation of the drug until the liver function test results return to normal. Recurrence of cholestatic jaundice, which developed for the first time during previous pregnancy or previous reception of sex hormones, requires discontinuation of the drug.

    Although COCs may have an effect on insulin resistance and glucose tolerance, the need for correcting the dose of hypoglycemic drugs in patients with sugardiabetes, using low-dose COCs (<0.05 mg of ethinylestradiol), as a rule, does not occur. Nevertheless, women with diabetes should be carefully monitored while taking COC.

    Sometimes chloasma can develop, especially in women with a history of pregnancy chloasma. Women with a tendency to chloasma during the intake of the drug Yama should avoid prolonged exposure to the sun and exposure to ultraviolet radiation.

    Preclinical safety data

    Pre-clinical data obtained from standardized studies for detection of toxicity with multiple doses of the drug, as well as genotoxicity, carcinogenic potential and toxicity for the reproductive system, do not indicate the existence of a special risk to humans. Nevertheless, it should be remembered that sex hormones can promote the growth of certain hormone-dependent tissues and tumors.

    Laboratory Tests

    The intake of Yama's drug can affect the results of some laboratory tests, including liver, kidney, thyroid, adrenal, plasma protein transport, carbohydrate metabolism, blood coagulation and fibrinolysis parameters. Changes usually do not go beyond the limits of normal values.Drospirenone increases plasma renin activity and aldosterone concentration, which is associated with its antimineralocorticoid effect.

    Decreased efficiency

    The effectiveness of the drug YaMera can be reduced in the following cases: when missing tablets, gastrointestinal disorders or as a result of drug interactions.

    Frequency and severity of menstrual bleeding

    Against the background of taking the drug, Yamera may experience irregular (acyclic) bleeding from the vagina ("spotting" bloody discharge and / or "breakthrough" uterine bleeding), especially during the first months of use. Therefore, any irregular menstrual bleeding should be evaluated after an adaptation period of approximately 3 cycles. If irregular menstrual bleeding repeats or develops after previous regular cycles, a thorough examination should be performed to exclude malignant neoplasms or pregnancy.

    Some women during the break in taking pills may not develop bleeding "withdrawal".If the drug Jamera was taken according to recommendations, it is unlikely that a woman is pregnant. However, with irregular use of the drug and the absence of two consecutive menstrual bleeding, the drug can not be continued until exclusion of pregnancy.

    Medical examinations

    Before starting or resuming the use of the drug, you need to familiarize yourself with the history of life, a family history of a woman, conduct a thorough general medical and gynecological examination, and exclude pregnancy. The scope of studies and the frequency of follow-up visits should be based on existing norms of medical practice with the necessary consideration of the individual characteristics of each patient. As a rule, blood pressure, heart rate, body mass index are measured, the condition of mammary glands, abdominal cavity and pelvic organs is checked, including cytological examination of the cervical epithelium (Pap test). Usually, follow-up examinations should be conducted at least once every 6 months.

    It must be borne in mind that the preparation of YAmer does not protect against HIV infection (AIDS) and other sexually transmitted diseases!

    States, requiring medical advice

    - Any changes in the state of health, especially the emergence of conditions, diseases and risk factors listed in the sections "Contraindications" and "With caution."

    - Local compaction in the mammary gland.

    - Simultaneous reception of other medications (see also the section "Interaction with other drugs").

    - If prolonged immobility is expected (for example, gypsum is applied to the lower limb), hospitalization or surgery is planned (at least 4 weeks before the proposed operation).

    - Unusually violent bleeding from the vagina.

    - Missed the pill in the first week of taking the drug and had sex for 7 or less days before.

    - The absence of another menstrual bleeding 2 times in a row or a suspicion of pregnancy (do not start taking pills from the next package before consulting a doctor).

    You should stop taking the pills and immediately consult a doctor if there are possible signs of thrombosis, myocardial infarction or stroke: an unusual cough; unusually severe pain behind the sternum, giving to the left arm; unexpected shortness of breath; unusual,severe and prolonged headache or migraine attack; partial or complete loss of vision or double vision; inarticulate speech; sudden changes in hearing, smell, or taste; dizziness or fainting; weakness or loss of sensitivity in any part of the body; severe pain in the abdomen; severe pain in the lower limb or a sudden onset of swelling in either of the lower extremities.

    Effect on the ability to drive transp. cf. and fur:

    Not found.

    Form release / dosage:

    Tablets, 3 mg + 0.03 mg.

    Packaging:

    For 21 tablets in a blister of PVC-PVDC / aluminum foil.

    The blister is packed in a package of laminated aluminum foil.

    For 1 or 3 bags of laminated aluminum foil with instructions for use in a pack of cardboard.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    2 years.

    Do not use after the expiration date!

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004401
    Date of registration:02.08.2017
    Expiration Date:02.08.2022
    The owner of the registration certificate:Fami Ker LimitedFami Ker Limited India
    Manufacturer: & nbsp
    Representation: & nbspFami Ker LimitedFami Ker LimitedIndia
    Information update date: & nbsp04.09.2017
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