Qlaira, 28 pcs., film-coated tablets

Release form

Tablets with a thin film coating, round, biconvex. A total of five types of tablets are produced:

• Marked "DD". There are 2 tablets in the package. The shell is yellow, the core is white.
• Marked "DJ". There are 5 tablets in a package. The shell is pink, the core is white.
• Marked "DH". There are 17 tablets in a package. The shell is pale yellow, the core is white.
• Marked "DN". There are 2 tablets in the package. The shell is red, the core is white.
• Marked “DT”. There are 2 tablets in the package. The shell is white, the core is white.

Each package of Qlaira contains four types of active tablets, each type containing several different doses of hormones. Two dark yellow tablets contain 3 mg estradiol , five medium red tablets contain 2 mg estradiol and 2 mg dienogest , 17 light yellow tablets contain 2 mg estradiol and 3 mg dienogest , and two dark red tablets contain 1 mg estradiol . The package also contains two inactive white tablets.

pharmachologic effect

Qlaira is a low-dose combined contraceptive intended for oral use. The drug contains both estrogenic and gestagenic components, due to which the tablets are well tolerated by patients in 99% of cases. In addition to the active tablets, the package contains 2 more inactive tablets, which makes it possible to continuously take the drug. The contraceptive effect is achieved by suppressing ovulation , increasing the thickness of cervical mucus , and also reducing the level of sensitivity of the uterine endometrium to the blastocyst (the initial stage of embryo development).

In addition to the main effect, this drug stimulates a decrease in the intensity and duration of the menstrual cycle, relieves PMS symptoms and minimizes pain symptoms.

Pharmacodynamics and Pharmacokinetics

The estrogen in Qlaira is estradiol valerate , an ester of human 17β-estradiol (1 mg estradiol valerate corresponds to 0.76 mg 17β-estradiol ). This estrogen is different from ethinyl estradiol or its precursor mestranol , used in other COCs and containing an ethyl group 17a, which causes more stable metabolic activity , but at the same time has effects on the liver.

Dienogest (DNG) is a progestogen with previous clinical trials. It has a pronounced effect on the endometrium. Structurally derived from nortestosterone, it has the characteristics of nortestosterone and progestogen derivatives. DNG does not have androgenic activity , but does have antiandrogenic activity.

Pharmacokinetics

Estradiol valerate

Absorption: Following oral administration of estradiol valerate, it is completely absorbed by the intestinal mucosa. After initial absorption, E2V is hydrolyzed to produce E2 and valeric acid through a metabolic process in the gastrointestinal mucosa and liver.

Metabolism: metabolism occurs in the gastrointestinal mucosa and liver. Estradiol valerate undergoes extensive changes in first-pass metabolism, resulting in increased serum . Approximately 95% of an oral dose of estradiol valerate is metabolized before it enters the systemic circulation , so the bioavailability of E2V is approximately 3-5%. Metabolism of E2 in the intestinal mucosa and liver leads to the conversion to estrone (E1) and estriol (E3). Both E1 and E3 are metabolized into sulfate and glucuronide forms . These forms of limited cell penetration partly explain their low effectiveness. Estrone (E1) is converted to estrone sulfate (E1-S) by estrogen sulfotransefare and both can be converted back to E2. Since most of the orally absorbed E2 is converted to E1 and E1-S, E2 levels stabilize. Estrogens are further oxidized by liver cytochrome P450 , affecting the CYP3A4 and 1A2 pathways until completely eliminated.

Distribution: 5% of an oral dose of E2V reaches systemic circulation. E2 is bound to 38% of obligatory sex hormone globulin (SHBG), 60% to albumin , and 3% circulates in free form. The approximate volume of distribution is ~1.2 L/kg. Serum concentrations of E2 remain stable over the 28-day treatment period in the range of 0.0336-0.0647 ng/mL due to the steady state between E2-E1-E1-S. Recycling includes E1-S and estrone glucuronide . The half-life of estradiol is 1.5 hours, the terminal half-life of estradiol after oral administration is 13-20 hours and is dependent on the recirculation of estrogen sulfate .

Excretion: Estradiol and its metabolites are primarily excreted in the urine. 10% is excreted in feces.

Dienogest

Absorption: DNG is almost completely absorbed after oral administration and has high bioavailability (91%). There is no clinically established effect on the rate or extent of absorption of DNG by concomitant meals.

Distribution: DNG has a distribution volume of 46L. It circulates in serum with serum albumin (90%) and 9% in the form of free and bioavailable elements. Serum concentrations of DNG at steady state are: min 11.8ng/ml; max 82.9ng/ml.

Metabolism: The half-life from blood plasma is 12 hours. The substance is almost completely metabolized by cytochrome P450, the CYP3A4 isoform into pharmacologically inactive metabolites.

Excretion: DNG and its metabolites are excreted primarily by the kidneys. 86% of the hormone and its metabolites are eliminated after 6 days.

Klaira No. 28 tab.p.p.o.

Instructions for medical use of the drug Klayraâ Trade name Klayraâ International nonproprietary name No Dosage form Film-coated tablets Composition One dark yellow film-coated tablet contains the active substance - estradiol valerate, micro 20, calculated as 100% substance 3,000 mg, excipients: core: lactose monohydrate, corn starch, pregelatinized corn starch, povidone 25, magnesium stearate, shell: hypromellose type 2910, macrogol 6000, talc, titanium dioxide (E171), yellow iron oxide (E 172). One medium-red film-coated tablet contains the active substances: estradiol valerate, micro 20, calculated as 100% substance 2,000 mg, dienogest, micro, calculated as 100% substance 2,000 mg, excipients: core: lactose monohydrate, starch corn, pregelatinized corn starch, povidone 25, magnesium stearate, shell: hypromellose type 2910, macrogol 6000, talc, titanium dioxide (E171), yellow iron oxide (E 172). One light yellow film-coated tablet contains the active substances: estradiol valerate, micro 20, in terms of 100% substance 2,000 mg, dienogest, micro, in terms of 100% substance 3,000 mg, excipients: core: lactose monohydrate, starch corn, pregelatinized corn starch, povidone 25, magnesium stearate, shell: hypromellose type 2910, macrogol 6000, talc, titanium dioxide (E171), yellow iron oxide (E 172). One dark red film-coated tablet contains the active substance: estradiol valerate, micro 20, calculated as 100% substance 1,000 mg, excipients: core: lactose monohydrate, corn starch, pregelatinized corn starch, povidone 25, magnesium stearate, shell : hypromellose type 2910, macrogol 6000, talc, titanium dioxide (E171), yellow iron oxide (E 172). One white film-coated tablet (placebo) contains excipients: core: lactose monohydrate, corn starch, povidone 25, magnesium stearate shell: hypromellose type 2910, talc, titanium dioxide (E171). Description Dark yellow tablets "Estradiol valerate 3 mg" Film-coated tablets of dark yellow color, round in shape, biconvex, with an engraving "DD" in a regular hexagon on one side. Medium-red tablets “Estradiol valerate 2 mg + Dienogest 2 mg” Film-coated tablets of medium-red color, round, biconvex, with “DJ” engraved in a regular hexagon on one side. Light yellow tablets “Estradiol valerate 2 mg + Dienogest 3 mg” Film-coated tablets of light yellow color, round, biconvex, with “DN” engraved in a regular hexagon on one side. Dark red tablets "Estradiol valerate 1 mg" Film-coated tablets of dark red color, round, biconvex, with "DN" engraved in a regular hexagon on one side. White tablets “Placebo” Film-coated tablets are white, round, biconvex, with “DT” engraved in a regular hexagon on one side. Pharmacotherapeutic group Sex hormones and modulators of the reproductive system. Hormonal contraceptives for systemic use. Progestogens and estrogens (for “calendar” administration) ATX code G03AB Pharmacological properties Pharmacokinetics of Dienogest Absorption After oral administration, dienogest is quickly and almost completely absorbed. The maximum serum concentration of 90.5 ng/ml is achieved approximately 1 hour after oral administration of a Qlaira tablet containing 2 mg estradiol valerate + 3 mg dienogest. Bioavailability is about 91%. The pharmacokinetics of dienogest in the dose range from 1 to 8 mg is characterized by dose dependence. Simultaneous food intake does not have a clinically significant effect on the rate and degree of absorption of dienogest. Distribution A relatively large (10%) portion of circulating dienogest is found in unbound form, while about 90% is nonspecifically bound to albumin. Dienogest does not bind to SHBG or corticosteroid binding globulin (CBG). For this reason, there is no possibility of displacing testosterone from its connection with SHBG or cortisol from its connection with DRG. Any effect on the physiological processes of transport of endogenous steroids is therefore unlikely. The volume of distribution of dienogest at steady state concentration is 46 L after intravenous administration of 85 mcg of tritium-labeled dienogest. Metabolism Dienogest is almost completely metabolized, passing through the known pathways of steroid hormone metabolism (hydroxylation, conjugation), with the formation of predominantly endocrinologically inactive metabolites. Metabolites are eliminated very quickly, so that the predominant fraction in the blood plasma is unchanged dienogest. The total clearance after intravenous administration of tritium-labeled dienogest is 5.1 l/h. Elimination The half-life of dienogest from blood plasma is approximately 11 hours. After oral administration at a dose of 0.1 mg/kg, dienogest is excreted in the form of metabolites, which are excreted by the kidneys and through the intestines in a ratio of approximately 3:1. After oral administration, 42% of the dose is eliminated within the first 24 hours, and 63% is eliminated within 6 days by renal excretion. After 6 days, a total of 86% of the dose is excreted by the kidneys and intestines. Steady-state concentration The pharmacokinetics of dienogest do not depend on the concentration of SHBG. Steady-state concentrations are achieved after 3 days of taking the same dose of 3 mg dienogest in combination with 2 mg estradiol valerate. The minimum, maximum and average concentrations of dienogest in serum at steady state are 11.8 ng/ml, 82.9 ng/ml and 33.7 ng/m, respectively. The average accumulation coefficient for the area under the concentration-time curve (AUC0-24 h) is 1.24. Estradiol valerate Absorption After oral administration, estradiol valerate is rapidly and completely absorbed. The breakdown into estradiol and valeric acid occurs during absorption in the mucous membrane of the gastrointestinal tract (GIT) or during the first passage through the liver, resulting in the formation of estradiol and its metabolites - estrone and estriol. The maximum concentration of estradiol in the blood serum, equal to 70.6 pg/ml, is achieved between 1.5 and 12 hours after a single oral dose of a tablet containing 3 mg of estradiol valerate on the 1st day of the cycle. Concomitant food intake does not have a clinically significant effect on the rate and extent of absorption of estradiol valerate. Metabolism Valeric acid is metabolized very quickly. After oral administration, approximately 3% of the dose becomes directly bioavailable as estradiol. Estradiol undergoes an intense first-pass effect through the liver, and a significant part of the administered dose is metabolized in the gastrointestinal mucosa. Combined with first-pass metabolism in the liver, approximately 95% of an ingested dose is metabolized before entering the systemic circulation. The main metabolites are estrone, estrone sulfate and estrone glucuronide. Distribution In the blood serum, 38% of estradiol is associated with SHBG, 60% with albumin, and 2-3% circulates in an unbound form. Estradiol may slightly increase serum SHBG concentrations; this effect is dose dependent. On the 21st day of the dosing cycle, the SHBG concentration was approximately 148% of the initial level, and by the 28th day (completion of the phase of taking inactive tablets) it decreased to approximately 141% of the initial one. The apparent volume of distribution after intravenous administration is 1.2 l/kg. Elimination The half-life of estradiol from blood plasma is approximately 90 hours. However, the situation is different when taken orally. Due to the large circulating pool of estrogen sulfates and glucuronides, as well as enterohepatic recirculation, the terminal half-life of estradiol after oral administration is a complex parameter that depends on all these processes and is in the range of about 13-20 hours. Estradiol and its metabolites excreted mainly by the kidneys, with about 10% excreted through the intestines. Steady-state concentration The pharmacokinetics of estradiol is influenced by the concentration of SHBG. In women, the measured plasma estradiol concentration is the combination of endogenous estradiol and estradiol received while taking Qlaira. During the phase of taking tablets containing 2 mg estradiol valerate + 3 mg dienogest, the maximum and average concentrations of estradiol in the blood serum at steady state are 66.0 pg/ml and 51.6 pg/ml, respectively. Stable minimum estradiol concentrations were maintained throughout the entire 28-day cycle, ranging from 28.7 pg/ml to 64.7 pg/ml. Pharmacodynamics The contraceptive effect of Qlaira is based on the interaction of various factors, the most important of which are: inhibition of ovulation, changes in the viscosity of cervical mucus and changes in the endometrium. In addition to their contraceptive effects, combined oral contraceptives (COCs) have positive effects that should be considered when choosing a method of birth control. The cycle becomes more regular, painful menstruation is less frequent, the intensity 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. High-dose oral contraceptives (0.05 mg ethinyl estradiol) reduce the incidence of ovarian cysts, pelvic inflammatory disease, benign breast disease and ectopic pregnancy. The extent to which these data apply to low-dose contraceptives requires further study. The advantage of the drug Klayraâ is that it contains estradiol, which has a limited proliferative effect on the endometrium and progestogen with a pronounced effect on the endometrium, and also presents a dosage regimen in the form of reducing the dose of estrogen and increasing the dose of progestogen, which can be used for treatment heavy and/or prolonged menstrual bleeding in women without organic pathology who require the use of oral contraception. The estrogen in Qlaira is estradiol valerate, a precursor of natural human 17b-estradiol (1 mg estradiol valerate corresponds to 0.76 mg 17b-estradiol). The estrogen component used in this COC is therefore different from the estrogens commonly used in COCs, which are synthetic estrogens - ethinyl estradiol or its precursor mestranol, both containing an ethynyl group at position 17a. This group causes higher metabolic stability, but also a more pronounced effect on the liver. Taking Qlaira leads to a less pronounced effect on the liver compared to triphasic COCs containing ethinyl estradiol and levonorgestrel. The effect on sex hormone binding globulin (SHBG) concentrations and hemostatic parameters has been shown to be less pronounced. When combined with dienogest, estradiol valerate demonstrates an increase in high-density lipoprotein (HDL) cholesterol, while low-density lipoprotein (LDL) cholesterol concentrations are slightly reduced. Dienogest is an orally active progestogen that is characterized by additional partial antiandrogenic effects. Thanks to the special chemical structure, a spectrum of pharmacological action is provided that combines the most important advantages of 19-nor-progestogens and progesterone derivatives. Indications for use - oral contraception - treatment of heavy menstrual bleeding in women without organic pathology who require the use of oral contraception. The decision to prescribe Qlaira should be made on an individual basis, taking into account the woman’s risk factors, in particular the development of venous thromboembolism, and assessing the risk of developing venous thromboembolism while taking Qlaira in comparison with other oral contraceptives. Method of administration and dosage When combined oral contraceptives are taken correctly, the rate of “method failure” is no more than 1% per year. Contraceptive reliability may be reduced if pills are missed or taken incorrectly. Directions for use: For oral administration The tablets should be taken orally in the order indicated on the package, every day at approximately the same time with a small amount of water. You should take one tablet per day consecutively for 28 days. Each new pack is started after taking the last tablet from the previous calendar pack. Menstrual-like bleeding usually begins while taking the last tablets in a calendar pack and may not stop until the next calendar pack begins. In some women, menstrual-like bleeding begins after taking the first tablets from a new calendar package. How to start taking Qlairaâ - If you have not taken any hormonal contraceptives in the previous month, taking Qlairaâ starts on the first day of the menstrual cycle (i.e. on the first day of menstrual bleeding). — When switching from combined hormonal contraceptives (combined oral contraceptive, vaginal ring, transdermal patch), a woman should start taking Qlaira the next day after taking the last hormone-containing tablet from the previous package of combined oral contraceptive. When switching from a vaginal ring or transdermal patch, it is preferable to start taking Qlaira on the day the ring or patch is removed. If you previously used only a progestogen-only method of contraception (mini-pill, injection, implant) or a progestogen-releasing intrauterine system (IUD), a woman can switch to taking Qlairaâ with a mini-pill on any day (from an implant or IUD - on the day of their removal; from the injection method - on the day on which the next injection is scheduled), but in all cases, during the first 9 days of taking the pills, it is recommended to additionally use a barrier method of contraception. After an abortion in the first trimester of pregnancy, a woman can start taking the pills immediately. In this case, additional contraceptive measures are not necessary. After childbirth or abortion in the second trimester of pregnancy A woman should be advised to start taking the pills on days 21-28 after childbirth or abortion in the second trimester of pregnancy. If a woman started taking the pills later, she is recommended to additionally use a barrier method of contraception during the first 9 days of taking the pills. However, if sexual intercourse has already taken place, before actually starting to take the drug Qlaira, it is necessary to exclude pregnancy, or the woman should wait for the onset of her first menstruation. For breastfeeding women, see Pregnancy and Lactation. Taking missed tablets Missed (white) inactive tablets can be ignored. However, they should be thrown away to avoid inadvertently prolonging the interval between taking the active tablets. The following tips apply solely to skipping active tablets. If the delay in taking any of the active tablets is less than 12 hours, contraceptive protection is not reduced. A woman should take the missed pill as soon as she remembers, and take the remaining pills at the usual time. If the delay in taking any of the active tablets is more than 12 hours, contraceptive protection may be reduced. A woman should take the last missed tablet as soon as she remembers, even if this means taking 2 tablets at the same time. She will then continue to take her pills at the usual time. Depending on the day of the cycle on which the pill was missed (for details, see Table 1), it is necessary to use additional contraceptive measures (for example, a barrier method of protection, in particular condoms) in accordance with the following principles: Table 1. Principles for handling missed pills DAY Color Contents of estradiol valerate (EV) and diegnogest (DNG) Guidelines to follow if one tablet has been missed and more than 12 hours have passed: 1 - 2 Dark yellow tablets (3.0 mg EV) - Take the missed tablet immediately, and the next tablet at the usual time (even if this means taking 2 tablets in one day) - Continue taking the tablets as usual - Additional contraceptive measures for the next 9 days 3-7 Medium red tablets (2.0 mg EV + 2.0 mg DNG) 8-17 Light yellow tablets (2.0 mg EV + 3.0 mg DNG) 18-24 Light yellow tablets (2.0 mg EV + 3.0 mg DNG) Throw away current calendar pack and immediately start taking the first tablet from the new calendar pack Continue taking the tablets as usual Additional contraceptive measures for the next 9 days 25-26 Dark red tablets (1.0 mg EV) Immediately take the missed tablet, and the next tablet - at the usual time (even if this means taking 2 tablets in one day) No additional contraceptive measures necessary 27-28 White pills (Placebo) Throw away the missed pill and continue taking the tablets as usual No additional contraceptive measures necessary Can be taken no more than 2 tablets per day. If a woman forgets to start a new calendar pack or misses one or more tablets from days 3 to 9 of the calendar pack, she may already be pregnant (if she had sexual intercourse within 7 days before missing a pill). The more pills (especially those with a combination of two active ingredients on days 3 to 24) that are missed, and the closer they are to the inactive pill phase, the higher the chance of pregnancy. If a woman misses a pill and then does not have menstrual bleeding at the end of a calendar pack/at the start of a new calendar pack, the possibility of pregnancy should be considered. Recommendations for gastrointestinal disorders In severe gastrointestinal disorders, absorption may be incomplete, so additional contraceptive measures should be taken. If vomiting occurs within 3-4 hours after taking a hormone-containing tablet, then you should immediately take the next tablet, preferably no later than 12 hours after the last dose. If the period after vomiting is more than 12 hours, then in this case there are recommendations regarding missed tablets, which are given in the section “Reception of missed tablets”. If a woman does not want to change her usual scheme for taking tablets, she needs to drink an additional tablet (or tablet) from a new package. Additional information for certain categories of patients of the elderly is not applicable. The drug Klairaâ is not shown after the onset of menopause. Patients with impaired liver function of the Clyiraâ drug are contraindicated for women with severe liver diseases until the indicators of the liver function are normal. See also section "Contraindications". Patients with kidney function disorders, Klairaqi, was not specifically studied in patients with kidney function disorders. Available data do not suggest adjustment of the dosage regimen in such patients. The use in pediatrics Available data on the use of the drug Klairaâ in patients under 18 years of age are absent. Side effects data on adverse reactions presented below are classified in accordance with the medical dictionary for the regulatory activity of Meddra, SOSC. The frequency is based on clinical research data. The most suitable term Meddra was used to describe a certain reaction, its synonyms and related diseases. Often (³1/100, <1/10) - headache (including sinus headache and headache of stress) - abdominal pain, nausea - acne (including pustular) - amenorrhea, discomfort in the mammary glands (including pain, tension in mammary glands, violations and pain in the nipple), dysmenorrhea, interciucial bleeding, metroRegia (including irregular menstruation)-body weight loss is rare (³1/1,000, <1/100)-fungal infections, vulvo-vaginal fungal infections (including vulvo-vaginal Candidiasis and detection of a specific cervical fungal infection), vaginal infections - increased appetite - depression, mood decrease, emotional lability (including tearfulness and affective lability), insomnia, decrease in libido (including loss of libido), psyche disorders, changes in mood - dizziness, migraine (including migraine with an aura and without aura)-rides of heat, arterial hypertension-diarrhea, vomiting-an increase in the activity of the liver enzymes (including ALT, AST and Gamma-glutoletransferraz)-alopecia, increased sweating, itching (including generalized), rash (including Moscow )-muscle cramps-an increase in the mammary glands (including swelling), densification in the mammary gland, cervix dysplasia, dysfunctional uterine bleeding, dyspareunia, fibrous-acid disease of the mammary glands, menorrhagia, impaired menstrual cycle, ovarian cyst, premenstrual syndrome, uterine leiomioma, uterine cyst, uterine. Pain in the pelvic area - spastic reduction of the uterus, uterine/vaginal bleeding, including ointing discharge, vaginal discharge, dry vaginal - fatigue, irritability, swelling (including generalized edema) - reduction of body weight, changes in blood pressure (including increase and decrease) Rarely (³1/10,000, <1/1000) - candidiasis, herpes of the oral cavity, inflammatory diseases of the pelvic organs, the syndrome of the estimated histoplasmosis of the eyes, governing lichen, infection of the urinary system, bacterial vaginitis - gear retention, hyperthyglyceridemia - aggression, dysphoria, dysphoria, dysphoria, dysphoria Increase in libido, nervousness, nightmares in a dream, anxiety, sleeping, stress - impaired attention, paresthesia, vertigo - intolerance to contact lenses, dry eyes, edema of the eyes - myocardial infarction, varicose veins, venous thromboembolism, arterial thromboembolism, arterial hypotensionia surface phlebitis - pain in the veins - dryness in the mouth, constipation, dyspepsia, gastroesophageal reflux - focal nodular liver hyperplasia, chronic cholecystitis - allergic skin reactions (including allergic dermatitis and urticaria), chlorias, dermatitis, hiresism, hypertrichosis, neurodermatitis, pigmentation disorders , seborrhea, skin disorders, including compaction - back pain, jaw pain, a feeling of severity - pain in the urinary system - pathological bleeding of the cancellation, benign non -plate of the mammary gland, the neoplasm of the mammary gland in Situ, the breast cyst, and discharge from the mammary glands, uterine polyp, cervical erythema, postcoiteal bleeding, galactorrhea, vaginal discharge, hypomenorrhea, menstruation delay, ovary rupture, smell from the vaginal region-a feeling of burning and discomfort in the vulvo-vaginal region-lymphoadenopathy-asthma, shortness of breath, nasal bleeding. - chest pain, malaise, hyperthermia - disturbances from the cervical canal, description of individual adverse reactions reported an increased risk of developing arterial and venous thrombotic and thromboembolic disorders, including myocardial infarction, stroke, transient ischemic attacks, venous thrombomboosis and pulmonary thromboembolism in women Using combined hormonal contraceptives, which are written in more detail in the "Special Instructions" section. The following adverse reactions were observed in women using oral combined contraceptives, which are also described in the “Special Instructions” section: - venous thromboembolic disorders - arterial thromboembolic disorders - arterial hypertension - the liver tumors - the appearance or deterioration of conditions for which the interconnection with the reception of combined oral contraceptives Not proven: Crohn's disease, ulcerative colitis, epilepsy, uterine fiberids, porphyria, systemic lupus, gestational herpes, sodengam chorea, hemolytic-uremic syndrome, cholestatic jaundice-chronic or chronic impaired liver function may require the ceasefire of a combined oral counter-contraceptive, So far, functional liver tests will not return to normal - in women with hereditary angioedema, exogenous estrogen can provoke or exacerbate the symptoms of this disease - the frequency of diagnosis of breast cancer is slightly increased among women taking oral contraceptives. Since breast cancer is rare in women under 40 years of age, an increase in the number of diagnoses is insignificant in relation to the total risk of developing this disease. His connection with the reception of combined oral contraceptives has not been proven. For more information, see the sections of “contraindications” and “special instructions” with an unknown frequency (despite the fact that these adverse reactions were not detected in the process of clinical studies by Clair®, the possibility of their occurrence cannot be excluded): - multiforme erythema, erythema, discharge, discharge Combined oral contraceptives should not be used from the mammary glands and the reactions of gypensitivity of contraindications in the presence of any of the conditions listed below. If any of these conditions develop for the first time against the background of administration, the drug should be immediately canceled. - the presence or risk of venous thromboembolism Including the V Leiden factor), the deficiency of antitrombin III, protein C or protein S · Large surgical interventions with prolonged immobilization · High risk of venous thromboembolism due to multiple risk factors - the presence or risk of arterial thromboembolism · Arterial thromboembome at present or in an anamnesis (for example, in an anamnesis (for example, anamnesis (for example, in an anamnesis myocardial infarction) or conditions preceding arterial thromboembolism (for example, angina pectoris) · cerebrovascular disorders - a stroke at present or in an anamnesis or conditions preceding cerebrovascular disorders (for example, transient ischemic attacks) · hereditary or acquired predisposition to arterial thromb emboly (for example,, for example,, for example,, for example,, for example,, for example,, for example. Hypergomocysteinemia and antiphospholipid antibodies (antibodies to cardiolipin and lupus anticoagulant) · Migraine with focal neurological symptoms high risk of arterial thromboembohylia due to the presence of multiple risk factors, such as: - diabetes with vascular complications - pronounced arterial arterial hypertic hypertic hypertic Zia - pronounced dyslipoproteinemia - pancreatitis with pronounced hyperthyglyceridemia at present or in a history of severe liver diseases at present or in a history of liver (to normalize liver tests) - the liver tumors (benign or malignant) at present or in an anamnesis - detected hormone -dependent malignant diseases (for example, genital orphan the gland) or suspicion of them is vaginal bleeding of unclear genesis - hypersensitivity to any of the components of the drug Medicine interaction the effects of other drugs on Clair â is possible interaction with drugs that induce microsomal enzymes of the liver, which can contribute to an increase in clearance of sex hormones and lead to breakthrough bleeding And/or a decrease in the contraceptive effectiveness of the drug. During the use of such drugs, a woman should additionally use a barrier or other method of contraception in addition to Klairaâ. In this case, the barrier method of contraception should be used during the period of concomitant administration of drugs and within 28 days after their cancellation. Substances that increase the clearance of sex hormones (reducing the effectiveness of combined hormonal contraceptives due to the induction of liver enzymes), for example: phenytoine, barbiturates, primidon, carbamazepine and rifampicin; There are also assumptions regarding Okskarbazepine, topiramate, felbamat, griseofulvin and drugs containing St. John's wort. Substances with various effects on the clearance of combined oral contraceptives, with combined use with combined oral contraceptives, many HIV/HCV prosthesis inhibitors and non-coaloside inhibitors of reverse transcription can increase or reduce the concentration of estrogens or bloody blood plasma. The indicated changes in some cases may have a relevant value. Substances that reduce the clearance of combined oral contraceptives (enzymes inhibitors) Dyenogest is a substrate of the cytochrome P450 (SYR) 3A4. The well -known CYP3A4 inhibitors, such as antifungal drugs (for example, Itraconazole, Voriconazole, Fluconazole), Verapamil, Macrolides (for example, clarithromycin, erythromycin), diltiazem and grapefruit juice can increase the level of blood dyenogest.

Contraindications

The contraceptive drug Qlaira should not be taken:

• Women who are breastfeeding (combined birth control pills should not be taken until the baby is weaned or for six months after birth);
• women with venous thromboembolism , such as deep vein thrombosis or blood clots in the lungs ( pulmonary embolism );
• women with blood diseases, since the substances included in the drug, as well as their effect on the body, increase the risk of blood clots in the veins;
• women undergoing sclerosing treatment for varicose veins ;
• women with two or more risk factors for a blood clot in a vein, such as a family history of deep vein thrombosis or pulmonary embolism under the age of 45 (parent, sibling);
• women with obesity, smoking, long-term immobility;
• women who have ever had a heart attack, stroke or mini-stroke caused by a blood clot in an artery;
• women with sore throat, heart valve disease or irregular heartbeat - atrial fibrillation ;
• women with unstable blood pressure;
• women who smoke more than 40 cigarettes a day;
• women over 50 years old;
• women with severe diabetes;
• women with diabetes , high blood pressure, high cholesterol, migraines ;
• women with breast cancer ;
• women with abnormal vaginal bleeding , the cause of which is unknown;
• women with excess urea in the blood, resulting in damaged blood cells ( hemolytic uremic syndrome );
• women with active liver disease , such as liver cancer, hepatitis ;
• women with impaired bile secretion, which causes jaundice ;
• women with gallstones ;
• hereditary blood diseases known as porphyrias.

Interaction

The influence of other drugs on the active components of the drug Qlaira®

The interaction of COCs with other drugs may lead to breakthrough uterine bleeding and/or lack of contraceptive effect. The following types of interactions have been described in the literature on COCs in general or studied during clinical trials of Qlaira®:

Isoenzyme inducers (CYP3A4 isoenzyme). There may be an interaction with drugs that induce microsomal enzymes (for example, cytochrome P450 systems), as a result of which the clearance of sex hormones can increase (such drugs include phenytoin, barbiturates, primidone, carbamazepine, rifampicin and possibly also oxcarbazepine, topiramate, felbamate, ritonavir, griseofulvin, as well as preparations containing St. John's wort). It has been reported that HIV protease inhibitors (eg ritonavir), non-nucleoside reverse transcriptase inhibitors (eg nevirapine) and combinations thereof may also have an effect on hepatic metabolism.

Effect on enterohepatic recirculation. When taking certain groups of antibiotics (for example, penicillin and tetracycline groups), the enterohepatic circulation of estrogen may decrease, which can lead to a decrease in the concentration of estradiol.

Women who are treated with microsomal enzyme-inducing drugs or antibiotics are advised to temporarily use a barrier method of contraception or choose another method of contraception in addition to Qlaira®. The barrier method of contraception should be used during the entire period of taking concomitant medications and for another 28 days after their discontinuation.

Isoenzyme inhibitors (CYP3A4 isoenzyme). Co-administration of rifampicin with tablets containing estradiol valerate and dienogest resulted in a significant reduction in Css and systemic exposure of dienogest and estradiol. Systemic exposure of dienogest and estradiol at Css, measured based on AUC0–24, decreased by 83 and 44%, respectively.

Known inhibitors of CYP3A4, such as azole antifungals, cimetidine, verapamil, macrolides, diltiazem, antidepressants and grapefruit juice, may increase plasma concentrations of dienogest. When administered concomitantly with the potent inhibitor ketoconazole, the AUC0–24 value at steady state increased for dienogest by 186%, and for estradiol by 57%. When administered concomitantly with the moderate inhibitor erythromycin, the AUC0–24 value of dienogest and estradiol at steady state increased by 62 and 33%, respectively.

Effects of Qlaira® in relation to other drugs: COCs can affect the metabolism of a number of other drugs (for example, lamotrigine), which can lead to either an increase or decrease in the concentration of these substances in the blood plasma and tissues. However, based on data from in vitro studies, inhibition of CYP enzymes when using Qlaira® at a therapeutic dose is unlikely.

Note: To identify possible interactions, you should read the instructions for accompanying drugs.

Incompatibility. Absent.

Side effects of Qlaira

• nausea and vomiting;
• abdominal pain;
• migraines or attacks of severe headaches;
• enlargement of the mammary glands and pain in this area;
• weight changes;
• retention of water in body tissues (fluid retention);
• vaginal thrush (candidiasis);
• change in menstrual bleeding;
• spotting or breakthrough bleeding;
• depression;
• lack of sexual desire;
• unstable blood pressure;
• skin reactions;
• irregular brown patches on the skin, usually on the face ( chloasma );
• liver dysfunction;
• gallstones.

Side effects

By frequency, undesirable effects are divided into frequent (≥1/100 and <1/10), infrequent (≥1/1000 and <1/100) and rare (≥1/10000 and <1/1000) see table. 2.

table 2

Undesirable effects when using the drug Qlaira®

The following serious adverse events have been reported in women using COCs (which include Qlaira®): arterial and venous thrombosis and thromboembolic complications; worsening or provoking symptoms of angioedema; liver tumors; acute pancreatitis

For more information, see the "Special Instructions" section.

Qlaira tablets, instructions for use (Method and dosage)

In accordance with the instructions for use of Qlaira, the tablets are taken daily at approximately the same time, one piece at a time. You should take the drug every day, no matter how often you have sex. The tablets should be swallowed without chewing and washed down with plenty of liquid. Eating does not affect the action of the active substances.

Each package contains 26 active tablets and 2 inactive white tablets.

Typically, the period of use begins with taking the second dark red or white and does not end until the next package is opened. Some women experience bleeding after taking the first tablet of a new package, which is considered completely natural and in most cases does not require specialist intervention.

The tablets should be taken continuously, even if the bleeding has not stopped. This means you must start a new pack of tablets on the same day of the week as your current one.

Using the drug for the first time

Provided that no contraceptives have been taken previously, you should start taking Qlaira tablets on the first day of the menstrual cycle. Taking the first pill is guaranteed to protect against pregnancy. After the birth of a child or abortion, you should consult your doctor before taking the drug.

Taking Qlaira after using other oral contraceptives is carried out the next day after taking the last active tablet of the previous package.

If you miss a dose

Inactive tablets:

If the white tablets (the last ones in the package) were not taken on time, they can be taken at any convenient time, since they do not contain active ingredients. The only rule is that you need to take them in any case, so as not to get confused about the number of days you take active pills, as this increases the risk of developing an unwanted pregnancy.

Active tablets:

Depending on the day of your cycle when one dose of the active pill is missed, you may need to take additional contraceptive precautions. If the time that has passed since the usual use of Qlaira is less than 12 hours, then protection against pregnancy is not reduced and you can take the pill without using additional contraceptives. If the time is more than 12 hours, then protection against pregnancy may be reduced. Depending on the day of the cycle when one pill was missed, it is necessary to use an additional method of contraception.

In normal cases, the tablets should be taken orally in the order indicated on the package, at the same time every day. Do not chew the tablets and take them with a moderate amount of water.

You should take one tablet per day for 28 days. A new package of tablets is opened after the last inactive tablet from the previous calendar package has been taken.

You should stop taking Qlaira and consult a doctor immediately if at least one of the possible signs of a blood clot occurs. They include:

• unusual cough;
• severe pain or heaviness in the chest;
• shortness of breath;
• unusual, severe or prolonged headache or migraine attack ;
• partial or complete loss of vision ;
• slurred speech;
• sudden changes in hearing, smell, or taste;
• dizziness or fainting;
• weakness or numbness in any part of the body;
• severe abdominal pain;
• severe pain, swelling, or discoloration of the legs.

Pharmacokinetics of the drug

Absorption of the drug is assessed as high. An hour after taking the tablet, the maximum possible concentration in the blood is already reached. Food intake does not have any effect on the bioavailability of components, so it is not taken into account and is not mentioned in the recommendations.

About 90% of the substances received with the dose are bound to albumin, while the remaining 10% circulate in an unbound form. Qlaira has no effect on the transport of endogenous steroids.

The plasma half-life of dienogest is 11 hours. Some of it is released in the form of metabolites through the kidneys and intestines. Slightly less than half of the dose is excreted per day, and the larger remainder requires at least 6 days to exit through the kidneys.

The main indication for buying Qlaira is a woman’s desire to protect herself from unwanted pregnancy. It is important to remember that oral contraceptives cannot prevent sexually transmitted infections. Therefore, obstetricians strongly recommend using Qlaira and other tablet forms of contraception only if you have a regular sexual partner.

To protect against pregnancy, in the case of constantly changing partners, it is wiser to use barrier precautions.

In addition, Qlaira is prescribed for long or uneven menstrual cycles, as well as in combination with drugs prescribed by psychotherapists, the action of which is aimed at normalizing the neuropsychic state of a woman during premenstrual syndrome.

Interaction with other drugs

The following drugs may speed up the breakdown of the hormones contained in Qlaira in the liver, making the tablets less effective at preventing pregnancy:

• aprepitants;
• Bosentan;
• barbiturates;
• Carbamazepine;
• Modafinil;
• Nevirapine;
• Oxcarbazepine;
• Phenobarbital;
• Phenytoin;
• Primidone;
• Rifampicin;
• Rifabutin;
• Ritonavir;
• Telaprevir;
• Topiramate;
• herbal remedies containing St. John's wort.

If you regularly take one of the listed drugs, Qlaira is not suitable as a method of contraception, since the contraceptive effect of these pills will be minimal and will not provide the proper level of protection against unplanned pregnancy.

If a patient is prescribed Rifampicin or Rifabutin , it is always recommended to use an alternative method of contraception, since these two antibiotics make birth control pills ineffective. It is also recommended to use an alternative method of contraception when treating with other antibiotics (for example, Amoxicillin, Erythromycin, Doxycycline ).

Antifungals such as Griseofulvin may make the tablets less effective. When taking such drugs, you must use an additional method of contraception throughout the course of treatment and for one month after its completion.

Weight loss drugs ( Xenical, Turboslim and others) when taken simultaneously with Qlaira cause severe diarrhea .

diabetes medications . If you have diabetes, the use of any oral contraceptives should be accompanied by regular measurement of blood sugar levels.

Taking Qlaira and medications to reduce high blood pressure provokes a decrease in the effect of the latter.

Qlaira prevents the excretion of fluid with loss of the effects of diuretics.

The tablets may increase the blood levels of the following drugs, which may increase the risk of side effects:

• Cyclosporine
• Melatonin
• Ropinirole
• Selegilin
• Tacrolimus
• Theophylline
• Tizanidine
• Voriconazole

special instructions

The transition from Qlaira to the ring should take place after consultation with a gynecologist, since the amount of hormone in the ring is significantly less than what is contained in the tablets. In contrast, the body may not notice a small dose, as a result of which ovulation will occur unhindered.

After changing the type of contraceptive, even from one form of tablet to another, in the first 9 days of using the new product, it is strongly recommended to additionally protect yourself using a barrier method.

Storage conditions

It is necessary to store Qlaira tablets in an airtight container until it is time to open it. If you have already started taking the tablets, they should not be stored longer than the scheduled dosage plan.

Store the drug in a cool, dry place where the temperature does not exceed 30° C.

It is not recommended to store pills or other medications in the bathroom or near the sink. Do not leave it on a windowsill or in a car. Heat and dampness destroy some components of the drug.

The drug should be kept in a place inaccessible to children.

Use during pregnancy and breastfeeding

Taking Qlaira® is contraindicated during pregnancy. If pregnancy occurs while using the drug Qlaira®, further use must be discontinued. However, large-scale epidemiological studies have not shown an increased risk of birth defects in children born to women who used COCs before pregnancy, nor have there been any teratogenic effects of COCs from accidental use early in pregnancy.

COCs can affect lactation because they can reduce the volume of breast milk produced and also change its composition. Therefore, COCs are generally not recommended for use until after lactation. Small amounts of contraceptive hormones and/or their metabolites may be excreted in breast milk.

Analogues of Qlaira

Level 4 ATX code matches:
Trisequence

Silhouette

Angelique

Divina

Klaira birth control pills have analogues, including:

• Pharmatex;
• Escapelle;
• Nonoxylol;
• Tri-Regol;
• Noretin;
• Diana-35;
• Gynepristone (used as emergency contraception);
• Nuvaring hormonal ring ;
• Benatex (prescribed as a contraceptive after abortion, childbirth, in the presence of contraindications to the use of other contraceptives, as well as during breastfeeding);
• Erotex (used for local contraception in women of reproductive age);
• Jess;
• Microgynon;
• Lindinet 20;
• Decasol;
• Mirena;
• Logest;
• Yarina;
• Novinet;
• Marvelon;
• Regulon;
• Jeannine;
• Lactinet;
• Charosetta;
• Femoden.

Contraindications to the use of the drug Qlaira

Combined oral contraceptives should not be used if you have one of the following conditions or diseases:

• deep vein thrombosis of the lower extremities, pulmonary embolism or thrombosis of another location, currently or in the past;
• acute coronary syndrome (ACS) and acute cerebrovascular accident (ACVA) - ischemic or hemorrhagic in nature - currently or in the past;
• prodromal manifestations of ACS (angina) or stroke (transient ischemic attack - TIA) currently or in the past;
• migraine accompanied by focal neurological symptoms (impaired vision, speech, paresthesia or paresis of various localizations);
• diabetes mellitus with vascular complications;
• pancreatitis associated with hyperlipidemia, currently or in history;
• liver disease currently or in history until liver function tests return to normal;
• hormone-dependent malignant tumors of the genital organs or breast, currently or in history;
• benign or malignant liver tumor currently or in history;
• vaginal bleeding of unknown origin;
• established or probable pregnancy;
• hypersensitivity to estradiol valerate or dienogest, or other components of the drug.

You should immediately stop using the drug if one of the above conditions occurs and switch to taking non-hormonal contraceptives (see also section Special instructions ).

Reviews about Klaira

Reviews from doctors about Qlaira indicate the high contraceptive effect that the drug has on women. Experts agree that this drug perfectly protects against unplanned pregnancy and at the same time has a positive effect on the health of the female body as a whole.

Reviews about Qlaira birth control pills are generally varied. Some women claim that taking the drug had an effective effect without the side effects of Qlaira; others experienced side effects, but they were short-lived.

Those who took hormonal pills left reviews about Claira on the forums and most of the reviews were positive or neutral. Women who have used a contraceptive for endometriosis speak especially well of the drug. They claim that specific symptoms disappeared after regularly taking birth control pills. However, the duration of taking the drug is different in all cases.

Interactions of the drug Qlaira

reduce the effectiveness of Qlaira or may cause bleeding: primidone, phenytoin, barbiturates, carbamazepine, oxcarbazepine, topiramate, felbamate, rifampicin, ritonavir, nevirapine, penicillin, tetracycline, griseofulvin, drugs based on St. John's wort. Increase the concentration of the active substances of Qlaira in the blood plasma : antifungal drugs containing ketoconazole, erythromycin antibiotics. Qlaira may affect the effectiveness of lamotrigine. Laboratory research . Oral contraceptives may interfere with the results of some laboratory tests.

Qlaira price

The price of Qlaira birth control pills is considered affordable for all segments of the population. You can buy this product in pharmacies. The price of Klayra ranges from 800 to 860 rubles per package, which includes 28 tablets.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Klaira tab.
  p.p.o. n28 Bayer Weimar/Bayer Pharma RUB 1,171 order
• Klaira tab. p.p.o. n28x3 Bayer Weimar GmbH and Co. KG

  RUB 3,089 order

Pharmacy Dialogue

• Klaira (tab. p/o No. 28) Bayer

  RUB 1,164 order

• Klaira (tab. p/o capt. No. 28 x 3)Shering AG

  RUB 3,019 order

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Pharmacy24

• Qlaira N28 tablets Bayer Weimar GmbH & Co.
  KG, Nimechchina 269 UAH. order

PaniPharmacy

• Qlaira tablets Qlaira tablets No. 28 Germany, Bayer Weimar

  267 UAH order

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