Lindynette 20 coated pills 20mg N63
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Active ingredients
Gestoden + Ethinyl Estradiol
Release form
Pills
Composition
In 1 tablet: ethinyl estradiol 20 mcg; Gestodene 75 mcg. Auxiliary substances: sodium calcium edetate - 0.065 mg, magnesium stearate - 0.2 mg, colloidal silicon dioxide - 0.275 mg, povidone - 1.7 mg, corn starch - 15.5 mg, lactose monohydrate - 37.165 mg.
Pharmacological effect
Monophasic oral contraceptive. Inhibits the secretion of pituitary gonadotropic hormones. The contraceptive effect of the drug is associated with several mechanisms. The estrogen component of the drug is ethinyl estradiol - a synthetic analogue of the follicular hormone estradiol, which is involved with the hormone of the corpus luteum in the regulation of the menstrual cycle. The progestin component is gestodene, a derivative of 19-nortestosterone, which is superior in strength and selectivity to not only the natural hormone of the corpus luteum progesterone, but also other synthetic gestagens (for example, levonorgestrel). Due to its high activity, gestodene is used in low dosages, in which it does not exhibit androgenic properties and has virtually no effect on lipid and carbohydrate metabolism. Along with these central and peripheral mechanisms that prevent the maturation of an oocyte capable of fertilization, it is caused by a decrease in the susceptibility of endometrium to the blastocyst , as well as an increase in viscosity of mucus in the cervix, which makes it relatively impassable for sperm. In addition to the contraceptive effect, the drug with a regular intake also has a therapeutic effect, normalizing the menstrual cycle and helping to prevent the development of a number of gynecological diseases, including neoplastic nature.
Pharmacokinetics
GestodenaVsasyvaniyuAfter ingestion is quickly and completely absorbed from the gastrointestinal tract. After a single dose, Cmax is noted after 1 h and is 2-4 ng / ml. Bioavailability is about 99%. Distribution Gestoden is associated with albumin and sex hormone-binding globulin (SHBG). 1-2% is in plasma in free form, 50-75% specifically binds to SHBG. An increase in the level of GSPG in blood caused by ethinyl estradiol affects the gestodene level: the fraction associated with GSPG increases, and the fraction associated with albumin decreases.The average Vd is 0.7-1.4 l / kg. The pharmacokinetics of gestodene depends on the level of SHBG. The concentration of SHBG in plasma under the action of estradiol is increased by 3 times. With daily intake, the concentration of gestodene in plasma increases by 3-4 times and in the second half of the cycle reaches a state of saturation. Metabolism and elimination of Gestoden biotransformed in the liver. The average plasma clearance is 0.8-1 ml / min / kg. The level of gestodene in serum decreases two-phase. T1 / 2 in the β-phase - 12-20 hours. Gestodene is displayed only in the form of metabolites, 60% - with urine, 40% - with feces. T1 / 2 metabolites - about 1 day. Ethinyl estradiol Absorption After ingestion, ethinyl estradiol is absorbed quickly and almost completely. The average Cmax in serum is achieved within 1-2 hours after administration and is 30-80 pg / ml. Absolute bioavailability due to presystemic conjugation and primary metabolism is about 60%. DistributionCompletely (about 98.5%), but nonspecifically binds to albumin and induces an increase in the level of HSPG in the blood serum. The average Vd is 5–18 l / kg. Css is established by the 3-4 day of taking the drug, and it is 20% higher than after a single dose. Metabolism Subject to aromatic hydroxylation with the formation of hydroxylated and methylated metabolites, which are present in the form of free metabolites or form of conjugates (glucuronides and sulfates). Metabolic clearance of blood plasma is about 5-13 ml. Excretion Concentration in serum decreases in two phases. T1 / 2 in the β-phase - about 16-24 hours. Ethinyl estradiol is secreted only in the form of metabolites, in a 2: 3 ratio with urine and bile. T1 / 2 metabolites - about 1 day.
Indications
Contraception.
Contraindications
presence of severe and / or multiple risk factors for venous or arterial thrombosis (including complicated lesions of the cardiac valve apparatus, atrial fibrillation, vascular diseases of the brain or coronary arteries, severe or moderate arterial hypertension with BP ≥ 160/100 mm Hg Art.); - Presence or indication in the history of thrombosis precursors (including transient ischemic attack, angina); - migraine with focal neurological symptoms, incl. in history - venous or arterial thrombosis / thromboembolism (including myocardial infarction, stroke,deep vein thrombosis of the leg, pulmonary embolism) currently or in history; - presence of venous thromboembolism in the history of relatives; - surgical intervention with prolonged immobilization; - diabetes mellitus (with angiopathy); - pancreatitis (including in history ), accompanied by severe hypertriglyceridemia; - dyslipidemia; - severe liver disease, cholestatic jaundice (including during pregnancy), hepatitis, including in history (before normalization of functional and laboratory parameters and within 3 months after their normalization); jaundice when taking GCS; cholelithiasis now or in history; Gilbert syndrome, Dubin-Johnson syndrome, Rotor syndrome; liver cancer (including in history); - severe itching, otosclerosis or its progression during a previous pregnancy or taking GCS; - hormone-dependent malignant neoplasms of the genital organs and mammary glands (including those suspected of them); - vaginal bleeding unclear etiologist AI; - Smoking over the age of 35 years (more than 15 cigarettes per day); - Pregnancy or suspicion of it; Contraindicated in disorders of liver function. The drug is not recommended to be prescribed in case of kidney diseases. - lactation period; - hypersensitivity to the drug components.
Precautionary measures
The drug should be prescribed with caution in conditions that increase the risk of developing venous or arterial thrombosis / thromboembolism: age over 35, smoking, hereditary predisposition to thrombosis (thrombosis, myocardial infarction or impaired cerebral circulation at a young age in any of the closest relatives), hemolytic-uremic syndrome, hereditary angioedema, liver disease, diseases that first arose or worsened during pregnancy or against the background of previous sexual intercourse hormones (including porphyria, herpes in pregnant women, minor chorea / Sydenhem disease /, Sydenhem chorea, chloasma), obesity (BMI over 30 kg / m2), dyslipoproteinemia, hypertension, migraine, epilepsy, valvular heart disease, predates fibrillation , prolonged immobilization, extensive surgery, surgery on the lower limbs, severe trauma, varicose veins and superficial thrombophlebitis, the postpartum period (non-lactating women / 21 days after delivery /; lactating women after the end of the lactation period), the presence of severe depression (includingin history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, deficiency of antithrombin III, deficiency of protein C or S, antiphospholipid antibodies, including antibodies to cardiolipin, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, diabetes mellitus, not complicated by vascular disorders, lupus anticoagulant), diabetes mellitus not complicated by vascular disorders, swelling , Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including in the family history), acute and chronic liver diseases.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation. In small quantities, the components of the drug are excreted in breast milk. When used during lactation, milk production may decrease.
Dosage and administration
Assign 1 tab. / Day for 21 days, if possible at the same time of day. After taking the last tablet out of the package, a 7-day break is taken, during which withdrawal bleeding occurs. The next day after the 7-day break (ie, 4 weeks after taking the first pill, on the same day of the week), the drug is resumed. Reception of the first tablet of Lindynette 20 should be started from the 1st to the 5th day of the menstrual cycle . When switching to Lindynette 20 from another combined oral contraceptive, Lindynette 20 should be taken after taking the last pill from a package of another oral hormonal contraceptive, on the first day of withdrawal bleeding. When switching to Lindy em 20 with drugs containing only gestagen (mini-pili, injections, implant), while taking the mini-pill, you can start taking Lindynette 20 on any day of the cycle, switch from using an implant to taking Lindynette 20 on the next day after removing the implant , when using injections, on the eve of the last injection. In these cases, in the first 7 days, additional methods of contraception should be used. After an abortion in the first trimester of pregnancy, you can begin taking Lindynette 20 immediately after surgery. In this case, there is no need to use additional methods of contraception. After childbirth or after an abortion in the second trimester of pregnancy, the drug can be started on days 21-28.In these cases, in the first 7 days it is necessary to apply additional methods of contraception. At a later start of the drug in the first 7 days, an additional, barrier method of contraception should be used. In the case when sexual intercourse took place before the start of contraception, pregnancy should be excluded before the start of the drug or the start of the first period should be postponed. If you skip the pill, you should take the missed pill as soon as possible. If the interval in taking pills was less than 12 hours, the contraceptive effect of the drug is not reduced, and in this case there is no need to use an additional method of contraception. The remaining pills should be taken at the usual time. If the interval is more than 12 hours, the contraceptive effect of the drug may decrease. In such cases, you should not replenish the missed dose, taking the drug continues as usual, but in the next 7 days, you need to use an additional method of contraception. If at the same time there is less than 7 tabs in the package, taking the drug from the next package should be started without interruption. In this case, the withdrawal bleeding does not occur before the completion of taking the drug from the second package, but there may be spotting or breakthrough bleeding. If the bleeding does not occur after the completion of taking the drug from the second package, pregnancy should be excluded before continuing. 4 hours after taking the drug begins vomiting and / or diarrhea, possibly a decrease in contraceptive effect. In such cases, you should proceed in accordance with the instructions for skipping pills. If the patient does not want to deviate from the usual contraceptive regimen, the missed pills should be taken from another package. To speed up the onset of menstruation, reduce the break in taking the drug. The shorter the break, the more likely the occurrence of breakthrough or spot bleeding while taking the pills from the next package (like cases with delayed menstruation). To delay the onset of menstruation, the drug should be continued from the new package without a 7-day break. Menstruation can be delayed as long as necessary until the end of the last pill from the second pack.With delayed menstruation, breakthrough or spot bleeding may occur. Regular intake of the drug Lindynette 20 can be restored after the usual 7-day break.
Side effects
Side effects requiring discontinuation of the drug. From the side of the cardiovascular system: arterial hypertension; rarely, arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary thromboembolism); very rarely, arterial or venous thromboembolism of the liver, mesenteric, renal, retinal arteries and veins. On the part of the sense organs: hearing loss caused by otosclerosis. Others: hemolytic-uremic syndrome, porphyria; rarely, exacerbation of reactive systemic lupus erythematosus; very rarely - Sydenham chorea (passing after discontinuation of the drug). Other side effects are more common, but less severe. The feasibility of continuing to use the drug is decided individually after consultation with the doctor, based on the benefit / risk ratio. On the part of the reproductive system: acyclic bleeding / bleeding from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, development of vaginal inflammation, candidiasis, stress, pain, breast enlargement, galactorrhea. From the digestive system: epigastric pain, nausea, vomiting, Crohn's disease, ulcerative colitis, or aggravation e jaundice and / or pruritus associated with cholestasis, cholelithiasis, hepatitis, liver adenoma. Dermatological reactions: erythema nodosum, exudative erythema, rash, chloasma, increased hair loss. From the side of the central nervous system: headache, migraine, mood lability, depression. the senses: hearing loss, increased sensitivity of the cornea (when wearing contact lenses). On the side of metabolism: fluid retention in the body, change (increase) in body weight, decrease in carbohydrate tolerance, hyperglycemia, increase in TG level. e: allergic reactions.
Overdose
Symptoms: nausea, vomiting, in girls - bleeding from the vagina. Treatment: prescribed symptomatic therapy, there is no specific antidote.
Interaction with other drugs
The contraceptive activity of Lindynette 20 is reduced when taken simultaneously with ampicillin, tetracycline, rifampicin, barbiturates, primidone, carbamazepine, phenylbutazone, phenytoin, griseofulvin, topiramate, felbamate, oxcarbazepine. The contraceptive effect of oral contraceptives is reduced with the use of these combinations, breakthrough bleeding and menstrual disorders are increasing. During the reception of Lindynette 20 with the above drugs, as well as within 7 days after completion of the course of their reception, you must use additional non-hormonal (condom, spermicidal gels) methods of contraception. When using rifampicin, additional contraceptive methods should be used within 4 weeks after completing the course of its administration. When used simultaneously with Lindynette 20, any drug that improves gastrointestinal motility decreases the absorption of active substances and their plasma levels. Ethinyl estradiol sulfation occurs in the intestinal wall. Drugs that also undergo sulfation in the intestinal wall (including ascorbic acid) competitively inhibit sulphation of ethinyl estradiol and thereby enhance the bioavailability etinilestradiola.Induktory liver microsomal enzymes reduce the level of ethinyl estradiol in blood plasma (rifampicin, barbiturates, phenylbutazone, phenytoin, griseofulvin, topiramate, hydantoin, felbamate, rifabutin, Oscarbazepine). Liver enzyme inhibitors (itraconazole, fluconazole) increase the level of ethinyl estradiol in the blood plasma. Some antibiotics (ampicillin, tetracycline), preventing intrahepatic circulating estrogen levels decrease ethinyl estradiol plazme.Etinilestradiol by inhibiting liver enzymes or acceleration conjugation (primarily glyukuronirovaniya) may affect the metabolism of other drugs (including cyclosporin, theophylline); The concentration of these drugs in the blood plasma may increase or decrease. With simultaneous use of Lindynette 20 with St. John's wort preparations (including infusion), the concentration of active substances in the blood decreases, which can lead to breakthrough bleeding and pregnancy.The reason for this is the inducing effect of Hypericum on liver enzymes, which continues for another 2 weeks after completing the course of Hypericum. It is not recommended to prescribe this combination of drugs. Ritonavir reduces ethinyl estradiol AUC by 41%. In this regard, during the use of ritonavir, hormonal contraceptives with a higher content of ethinyl estradiol should be used or additional non-hormonal methods of contraception should be used. May require correction of the dosage regimen when using hypoglycemic agents, since oral contraceptives can reduce carbohydrate tolerance, increase insulin or oral antidiabetic requirements.
special instructions
Before using the drug, it is necessary to conduct general medical (detailed family and personal history, blood pressure measurement, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of cervical smear). A similar examination in the period of taking the drug is carried out regularly, every 6 months. The drug is a reliable contraceptive: Pearl index (an indicator of the number of pregnancies occurring during the use of the contraceptive method in 100 women within 1 year) with proper use is about 0.05. Due to the fact that the contraceptive effect of the drug from the start of the intake is fully manifested by day 14, then in the first 2 weeks of taking the drug, it is recommended to additionally use non-hormonal methods of contraception. . This issue should be discussed with the patient, who after receiving the necessary information will make the final decision on the preference for hormonal or any other method of contraception. The health status of the woman should be carefully monitored. If any of the following conditions / diseases appear or worsen while taking the drug, it is necessary to stop taking the drug and switch to another non-hormonal method of contraception: - diseases of the hemostasis system, - conditions / diseases predisposing to the development of cardiovascular,renal failure; - epilepsy; - migraine; - risk of developing an estrogen-dependent tumor or estrogen-dependent gynecological diseases; - diabetes mellitus not complicated by vascular disorders; - severe depression (if depression is associated with a tryptophan metabolic disorder, vitamin B6 can be used for correction) - sickle cell anemia, because in some cases (for example, infections, hypoxia), estrogen-containing drugs with this pathology can provoke thromboembolism phenomena; - appearance of abnormalities in laboratory tests assessing liver function. venous thromboembolic diseases (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, thromboembolus pulmonary artery). Proved an increased risk of venous thromboembolic diseases, but it is significantly less than during pregnancy (60 cases per 100 thousand pregnancies). With the use of oral contraceptive drugs, arterial or venous thromboembolism of the hepatic, mesenteric, renal or retinal vessels is very rarely observed. The risk of arterial or venous thromboembolic diseases increases: with age; when smoking (intensive smoking and age over 35 years are considered to be risk factors); If you have a family history of thromboembolic disease (for example, a parent, brother, or sister). If you suspect a genetic predisposition, you must consult with a specialist before using the drug; with obesity (BMI over 30 kg / m2); with dyslipoproteinemia; with hypertension; with valvular diseases complicated by hemodynamic disorders; with atrial fibrillation; in diabetes mellitus complicated by vascular lesions; during prolonged immobilization, after a large surgery, after surgery on the lower extremities, after a severe injury. In these cases, it is assumed a temporary cessation of the use of the drug (not later than 4 weeks before the surgery, and to resume - not earlier,than 2 weeks after remobilization). Women after childbirth increase the risk of venous thromboembolic diseases. It should be noted that diabetes, systemic lupus erythematosus, hemolytic-uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia, increase the risk of developing venous thromboembolic diseases. It should be noted that resistance to activated protein C, hyperhomocysteinemia, deficiency of proteins C and S, deficiency of antithrombin III, the presence of antiphospholipid an titel, increase the risk of arterial or venous thromboembolic diseases. When assessing the benefit / risk of taking the drug, it should be borne in mind that targeted treatment of this condition reduces the risk of thromboembolism. Symptoms of thromboembolism are: - sudden pain in the chest, which radiates to the left hand; sudden shortness of breath; any unusually severe headache, lasting for a long time or appearing for the first time, especially when combined with sudden complete or partial loss of vision or diplopia, aphasia, dizziness, collapse, focal epilepsy, weakness or severe numbness of half of the body, movement disorders, severe unilateral pain in gastrocnemius muscle, a symptom of an acute abdomen. Tumor diseases. Some studies have reported an increase in the incidence of cervical cancer in those women who have long been There are hormonal contraceptives, but the results are inconsistent. Sexual behavior, infection with human papillomavirus and other factors play a significant role in the development of cervical cancer. A meta-analysis of 54 epidemiological studies has shown that there is a relative increase in the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection of breast cancer glands could be associated with more regular medical examinations. Breast cancer is rare among women younger than 40 years old, regardless of whether they take hormonal contraceptives or not, and increases with age. Taking pills can be considered as one of many risk factors.However, a woman should be made aware of the possibility of developing breast cancer risk, based on an evaluation of the benefit-risk ratio (protection against ovarian cancer and endometrial cancer). There are few reports about the development of a benign or malignant liver tumor in women who take hormone for a long time. contraceptives. This should be borne in mind when the differential diagnostic assessment of abdominal pain, which may be associated with an increase in liver size or intraperitoneal bleeding. Chloasma: Chloasma may develop in women with a history of pregnancy. Those women who are at risk of chloasma should avoid contact with sunlight or ultraviolet radiation while taking Lindynette 20. Efficacy: The effectiveness of the drug may decrease in the following cases: missed pills, vomiting and diarrhea, the simultaneous use of other drugs that reduce the effectiveness of contraceptives pills. If the patient simultaneously takes another drug that can reduce the effectiveness of birth control pills, additional methods of contraction should be used. eprtsii.Effektivnosti drug may decrease if after several months of their use there are irregular, spotting or breakthrough bleeding, in such cases it is advisable to continue taking the pills until their end in the next package. If the menstrual-like bleeding does not start at the end of the second cycle, or the acyclic bleeding does not stop, stop taking the pills and resume it only after pregnancy is excluded. Changes in laboratory parameters Under the action of oral contraceptive pills - due to the estrogen component - some laboratory parameters may change liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, levels of lipoproteins and transport einov) For additional informatsiya.Posle suffering acute viral hepatitis drug should be taken after the normalization of liver function (not earlier than 6 months) .If diarrhea or intestinal disorders, vomiting contraceptive effect may decrease.Without stopping the drug, it is necessary to use additional non-hormonal methods of contraception. Smoking women have an increased risk of developing vascular diseases with serious consequences (myocardial infarction, stroke). The risk depends on age (especially in women over 35) and on the number of cigarettes smoked. It is necessary to warn a woman that the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases. The effect on the ability to drive motor vehicles and control mechanisms to study the effect of the drug Lindynette 20 on the ability to drive a car and production mechanisms, was not carried out.