More info
Active ingredients
Gestoden + Ethinyl Estradiol
Release form
Pills
Composition
Active ingredient: Gestodene (Gestodene), Ethinylestradiol (Ethinylestradiol) Concentration of the active ingredient (mg): Gestodene - 0, 075 mg, ethinyl estradiol - 0, 020 mg
Pharmacological effect
Logest is a low-dose monophasic oral combined estrogen-gestagenic contraceptive drug. Logest's contraceptive effect is accomplished through complementary mechanisms, the most important of which include suppression of ovulation and changes in the state of cervical mucus. the intensity of menstrual bleeding, which reduces the risk of iron deficiency missions. In addition, there is evidence that the risk of developing endometrial cancer and ovarian cancer is reduced. When correctly used, the Pearl index (an indicator reflecting the pregnancy rate in 100 women during the year of using a contraceptive) is less than 1. If pills are used incorrectly, When skipping pills, the Pearl index may increase.
Pharmacokinetics
Gestodena Absorption. After ingestion, gestodene is quickly and completely absorbed, its maximum concentration in serum, equal to 3.5 ng / ml, is reached in approximately 1 hour. Bioavailability is approximately 99%. Distribution. Gestodene binds to serum albumin and sex hormone-binding globulin (SHBG). In free form is only about 1.3% of the total serum concentration; about 69% are specifically associated with SHBG. Induction of ethinyl estradiol synthesis of SHBG affects the binding of gestodene to plasma proteins. Metabolism. Gestodene is almost completely metabolized. Serum clearance is about 0.8 ml / min / kg. Excretion. The content of gestodene in serum undergoes a two-phase decrease. The elimination half-life in the terminal phase is about 12 hours. In unchanged form, gestodene is not excreted, but only in the form of metabolites, which are excreted by the kidneys and through the intestine in a ratio of about 6: 4 with a half-life of about 24 hours. Equilibrium concentration.Gestodene pharmacokinetics are influenced by serum SHBG concentration. As a result of the daily intake of the drug, the concentration of the substance in the serum increases by about 4 times during the second half of the contraceptive cycle. Ethynyl estradiol Absorption. After oral administration, ethinyl estradiol is rapidly and completely absorbed. The maximum serum concentration of about 65 pg / ml is reached in 1-2 hours. During suction and the first passage through the liver, ethinyl estradiol is metabolized, with the result that its bioavailability upon ingestion averages about 45%. Distribution. Ethinyl estradiol is almost completely (approximately 98%), although not specific, bound by albumin. Ethinyl estradiol induces the synthesis of SHBG. The apparent volume of distribution of ethinyl estradiol is 2.8-8.6 l / kg. Metabolism. Ethinyl estradiol undergoes presystemic conjugation, as in a thin mucosa. intestines and in the liver. The main metabolic pathway is aromatic hydroxylation. The rate of clearance from blood plasma is 2.3 -7 ml / min / kg. Excretion. The decrease in the concentration of ethinyl estradiol in the serum is biphasic; the first phase is characterized by a half-life of about 1 hour, the second - 10-20 hours. Unchanged from the body is not displayed. Ethinyl estradiol metabolites are excreted in urine and bile in a ratio of 4: 6 with a half-life of about 24 hours. Equilibrium concentration. Equilibrium concentration is reached in approximately one week.
Indications
Oral contraception.
Contraindications
Thrombosis and thromboembolism, cerebrovascular disorders identified acquired or inherited predisposition to venous or arterial thrombosis, including resistance to activated protein C, antithrombin III deficiency, protein C deficiency, protein deficit S, hyperhomocysteinemia, the presence of high risk of venous or arterial thrombosis, migraine with focal neurological symptoms, pancreatitis with severe hypertriglyceridemia, diabetes mellitus with vascular complications, liver failure and severity s liver disease, severe and / or acute renal failure, liver tumors (benign or malignant),identified or hormone-dependent malignant neoplasms (including genitals or mammary glands) or suspicion of them, vaginal bleeding of unknown origin, pregnancy or suspicion of it, breastfeeding, hypersensitivity or intolerance to any of the components of the drug, hereditary lactose intolerance.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Logest is contraindicated during pregnancy and lactation. If pregnancy is detected while taking the drug Logest, the drug should be immediately canceled. However, numerous epidemiological studies have not revealed any increased risk of developmental defects in children born to women who received sex hormones before pregnancy or teratogenic effects, when sex hormones were taken by negligence in the early stages of pregnancy. Reception of Logest, like other combined oral contraceptives, can reduce the number of breast milk and change its composition, therefore, their use is not recommended during lactation. A small amount of sex hormones and / or their metabolites can be excreted in breast milk.
Dosage and administration
Tablets should be taken orally one at a time for 21 days at about the same time, with a little water. Each pill must be taken on the appropriate day of the week indicated on the package, following the arrows.
Side effects
Nausea, abdominal pain, diarrhea, vomiting, hypersensitivity, weight gain, fluid retention, headache, migraine, decrease in mood, mood swings, decrease in libido, painful dairy gala, discharge from the genital tract, discharge from the dairy gland.
Overdose
If any of the conditions / diseases / risk factors listed below are present, then the potential risk and the expected benefits of using combined oral contraceptives, including Logest, in each individual case should be carefully weighed and discussed with the woman before how she decides to start taking the drug / In case of aggravation, amplification or the first manifestation of any of these conditions or risk factors,A woman should consult with an obstetrician / gynecologist who may decide to discontinue the drug. Cardiovascular diseases Epidemiological studies indicate a correlation between the use of combined oral contraceptives and an increased incidence of venous and arterial thrombosis and thromboembolism (such as thrombosis) , pulmonary embolism, myocardial infarction, cerebrovascular disorders) when taking a combined pen cial contraceptives. These diseases are rare. The risk of venous thromboembolism (VTE) is maximum in the first year of taking such drugs. Increased risk is present after the initial use of combined oral contraceptives or the resumption of the use of the same or different combined oral contraceptives (after a break between taking the drug in 4 weeks or more). Data from a large prospective study involving 3 groups of patients show that this increased risk is predominantly present during the first 3 months. The overall risk of VTE in patients taking low-dose combination oral contraceptives (<50 mcg ethinyl estradiol) is two to three times higher than in non-pregnant patients who do not take combined oral contraceptives, however, this risk remains lower compared to the risk of HTE during pregnancy and childbirth. VTE can be fatal (in 1-2% of cases). VTE, manifested as deep vein thrombosis, or pulmonary embolism, can occur when using any combined oral aceptives. Thrombosis of other blood vessels, such as the hepatic, mesenteric, renal, cerebral veins and retinal arteries or vessels, is extremely rare with combined oral contraceptives. There is no consensus regarding the relationship between the occurrence of these events and the use of combined oral contraceptives. Symptoms of deep vein thrombosis (DVT) include the following: unilateral edema of the lower limb or along the vein in the leg, pain or discomfort in the leg only in an upright position or when walking, local elevation temperature in the affected leg, redness or discoloration of the skin on the leg.Symptoms of pulmonary thromboembolism (pulmonary embolism) are as follows: difficulty breathing or rapid breathing; sudden cough, including hemoptysis; acute pain in the chest, which may increase with a deep breath; sense of anxiety; severe dizziness; rapid or irregular heartbeat. Some of these symptoms (eg, shortness of breath, cough) are nonspecific and can be interpreted incorrectly as signs of other more or less serious complications (eg, respiratory tract infection). Arterial thromboembolism can lead to stroke, vascular occlusion or myocardial infarction. The symptoms of a stroke include the following: a sudden weakness or loss of sensation of the face, arm, or leg, especially on one side of the body, sudden confusion, problems with speech and understanding; sudden one or two-sided vision loss; 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 epileptic seizures. Other signs of vascular occlusion are: sudden pain, swelling and weakness of the limbs, acute abdomen. Symptoms of myocardial infarction include: pain, discomfort, pressure, heaviness, a feeling of constriction or distension in the chest, arm, or behind the sternum; discomfort radiating to the back, cheekbone, larynx, arm, stomach; cold sweat, nausea, vomiting or dizziness, severe weakness, anxiety, or shortness of breath; rapid or irregular heartbeat. Arterial thromboembolism can be fatal. The risk of developing thrombosis (venous and / or arterial) and thromboembolism increases: with age; - in smokers (with increasing number of cigarettes or increasing age, the risk increases, especially in women 35 years;) if you have: - a family history (for example, venous or arterial thromboembolism, ever with close relatives or parents at a relatively young age). In case of hereditary or acquired predisposition, the woman should be examined by an appropriate specialist to decide whether it is possible to take combined oral contraceptives - obesity (body mass index more than 30 kg / m2); - dyslipoproteinemia; - hypertension; - migraine; - valve disease heart; - atrial fibrillation; - prolonged immobilization, serious surgery, any surgery on the legs, or extensive trauma.In these situations, it is desirable to stop the use of combined oral contraceptives (in the case of the planned operation, at least four weeks before it) and not to resume reception for two weeks after the end of immobilization. The question of the possible role of varicose veins and surface thrombophlebitis in the development of venous thromboembolism remains controversial. You should take into account the increased risk of developing thromboembolism in the postpartum period. Peripheral circulatory disorders can also be observed in diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. Increased frequency and severity migraine during the use of combined oral contraceptives (which may precede cerebrovascular disorders) may be grounds for To stop taking these drugs. Biochemical indicators indicating a hereditary or acquired susceptibility to venous or arterial thrombosis include the following: resistance to activated protein C, hyperhomocysteinemia, lack of antithrombin III, lack of protein C, lack of protein S, anti-phospholipid antibodies (anti-thrombin III, anti-phospholipid antibodies, anti-thrombin III, lack of anti-phosphine lipid). lupus anticoagulant). When assessing the risk / benefit ratio, it should be borne in mind that adequate treatment of the corresponding condition can reduce the associated risk of thrombosis. It should also be borne in mind that the risk of thrombosis and thromboembolism during pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg ethinyl estradiol). Tumors The most significant risk factor for developing cervical cancer, is persistent papillomavirus infection. There are reports of some increase in the risk of cervical cancer with prolonged use of combined oral contraceptives. Relationship with the reception of combined oral contraceptives is not proven. Controversy persists regarding the extent to which these findings are related to screening for cervical pathology or sexual behavior (more rare use of barrier methods of contraception). Meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of developing breast cancer. diagnosed in womencurrently taking combined oral contraceptives (relative risk 1.24). The increased risk gradually disappears within 10 years after discontinuation of these drugs. Due to the fact that breast cancer is rarely observed in women under 40 years old, an increase in the number of breast cancer diagnoses in women who are currently taking or taking a combined oral contraceptive pill is insignificant relative to the overall risk of the disease. His connection with the reception of combined oral contraceptives has not been proven. The observed increase in risk may also be due to an earlier diagnosis of breast cancer in women using combined oral contraceptives. In women who have ever used combined oral contraceptives, earlier stages of breast cancer are detected than in women who have never used them. In rare cases, the use of combined oral contraceptives has been observed to develop benign, and in extremely rare cases, malignant liver tumors, which in some cases led to life-threatening intra-abdominal bleeding. In case of severe abdominal pain, enlarged liver or signs of intra-abdominal bleeding, this should be considered when making a differential diagnosis. Other conditions In women with hypertriglyceridemia (or this condition in the family history), the risk of pancreatitis may increase - while taking combined oral contraceptives. Although a slight increase in blood pressure has been described in many women taking combined oral contraceptives, clinically significant enhancements were rare. However, if a persistent, clinically significant increase in blood pressure develops while taking combined oral contraceptives, this drug should be canceled and treatment of hypertension should be initiated. Reception of combined oral contraceptives can be continued if normal blood pressure values are achieved using antihypertensive therapy. The following conditions have been reported to develop or worsen as during pregnancy,and when taking combined oral contraceptives, but their relationship with the reception of combined oral contraceptives is not proven: jaundice and / or itching associated with cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic uremic syndrome; chorea; herpes pregnant; hearing loss associated with otosclerosis. Also described are cases of Crohn's disease and ulcerative colitis associated with the use of combined oral koshertseptivov. In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen the symptoms of angioedema. Acute or chronic liver dysfunction may require discontinuation of combined oral contraceptives until liver function returns to normal. Recurrent cholestatic jaundice, which develops for the first time during pregnancy or previous intake of sex hormones, requires discontinuation of combined oral contraceptives. Although combined oral contraceptives may have an effect on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in sugar patients diabetes using low-dose combination oral contraceptives (<0.05 mg ethinyl estradiol). However, women with diabetes should be carefully monitored while taking combined oral contraceptives. Chloasma can sometimes develop, especially in women with a history of pregnant chloasma. Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to the sun and exposure to ultraviolet radiation. Each tablet drug Logest contains 35 mg of lactose. Patients with rare hereditary diseases - galactose intolerance, lactase deficiency, glucose-galactose malabsorption, who are on a diet with no lactose, should take into account information on the lactose content in the preparation. Laboratory tests Admission of combined oral contraceptives can affect the results of some laboratory tests. liver, kidney, thyroid, adrenal gland functions, plasma transport proteins, carbohydrate metabolism, parameters coagulation and fibrinolysis.Changes usually do not go beyond the normal range. Reduced efficacyEffectiveness of combined oral contraceptive drugs can be reduced in the following cases: when skipping pills, vomiting and diarrhea, or as a result of drug interactions. (spotting or breakthrough bleeding), especially during the first months of use. Therefore, any irregular bleeding should be evaluated only after an adaptation period of approximately three cycles. If irregular bleeding recurs or develops after previous regular cycles, a thorough examination should be carried out to exclude malignant neoplasms or pregnancy. Some women may have do not develop withdrawal bleeding. If combined oral contraceptives were taken as directed, it is unlikely that the woman is pregnant. However, if previously combined oral contraceptives were taken irregularly or, if there are no two withdrawal bleeding in a row, pregnancy should be excluded before continuing the drug. Medical examinations Before starting or resuming use of the drug Logest, you should read the history of life, family history of the woman general medical (including measurement of blood pressure, determination of body mass index) and gynecological examination (including the study of the mammary glands and cyto nical study of cervical epithelium), to exclude pregnancy. The amount of additional research and the frequency of control examinations is determined individually. Usually, control tests should be carried out at least 1 time in 6 months. A woman should be warned that drugs like Logest do not protect against HIV infection (AIDS) and other sexually transmitted diseases! The effect on the ability to drive motor vehicles and control mechanisms is not detected.
Interaction with other drugs
The interaction of oral contraceptives with other drugs can lead to breakthrough bleeding and / or reduced contraceptive efficacy. Women taking these drugs should temporarily use barrier methods of contraception in addition to Logest, or choose another method of contraception.The following types of interactions have been reported in the literature. Effects on hepatic metabolism: the use of drugs that induce liver microsomal enzymes can lead to an increase in the clearance of sex hormones. Such drugs include: phenytoin, barbiturates, primidone, carbamazepine, rifampicin; there are also suggestions for oxcarbazepine, topiramate, felbamate, griseofulvin, and preparations containing St. John's wort. HYV proteases (eg, ritonavir) and non-nucleoside reverse transcriptase inhibitors (eg, nevirapine) and their combinations can also potentially affect hepatic metabolism. enteric-hepatic recycling: according to separate studies, some antibiotics (for example, penicillins and tetracyclines) can reduce the enterohepatic recirculation of estrogens, thereby reducing the ethinylestradiol concentration. While taking medications that affect liver microsomal enzymes, and within 28 days after they are canceled, you should additionally use a barrier method of contraception. While taking antibiotics (such as penicillins and tetracyclines) and within 7 days after they are canceled, you should additionally use barrier method of contraception. If the period of using the barrier method of contraception ends later than the pills in the package, you need to proceed to the next package of Logest without the usual interruption in taking the pills. Oral combination contraceptives can affect the metabolism of other drugs, which leads to an increase (eg, cyclosporine) or decrease ( for example, lamotrigine) their plasma and tissue concentrations.
special instructions
If any of the conditions / diseases / risk factors listed below are present, then the potential risk and the expected benefits of using combined oral contraceptives, including Logest, in each individual case should be carefully weighed and discussed with the woman before how she decides to start taking the drug / In case of aggravation, amplification or the first manifestation of any of these conditions or risk factors, the woman should consult with your obstetrician-gynecologist,which may decide to discontinue the drug. Cardiovascular diseases Epidemiological studies indicate a correlation between the use of combined oral contraceptives and an increase in the incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, and infarction, in case of an infantile heart disease). violations) when taking combined oral contraceptives. These diseases are rare. The risk of venous thromboembolism (VTE) is maximum in the first year of taking such drugs. Increased risk is present after the initial use of combined oral contraceptives or the resumption of the use of the same or different combined oral contraceptives (after a break between taking the drug in 4 weeks or more). Data from a large prospective study involving 3 groups of patients show that this increased risk is predominantly present during the first 3 months. The overall risk of VTE in patients taking low-dose combination oral contraceptives (<50 mcg ethinyl estradiol) is two to three times higher than in non-pregnant patients who do not take combined oral contraceptives, however, this risk remains lower compared to the risk of HTE during pregnancy and childbirth. VTE can be fatal (in 1-2% of cases). VTE, manifested as deep vein thrombosis, or pulmonary embolism, can occur when using any combined oral aceptives. Thrombosis of other blood vessels, such as the hepatic, mesenteric, renal, cerebral veins and retinal arteries or vessels, is extremely rare with combined oral contraceptives. There is no consensus regarding the relationship between the occurrence of these events and the use of combined oral contraceptives. Symptoms of deep vein thrombosis (DVT) include the following: unilateral edema of the lower limb or along the vein in the leg, pain or discomfort in the leg only in an upright position or when walking, local elevation temperature in the affected leg, redness or discoloration of the skin on the leg.Symptoms of pulmonary thromboembolism (pulmonary embolism) are as follows: difficulty breathing or rapid breathing; sudden cough, including hemoptysis; acute pain in the chest, which may increase with a deep breath; sense of anxiety; severe dizziness; rapid or irregular heartbeat. Some of these symptoms (eg, shortness of breath, cough) are nonspecific and can be interpreted incorrectly as signs of other more or less serious complications (eg, respiratory tract infection). Arterial thromboembolism can lead to stroke, vascular occlusion or myocardial infarction. The symptoms of a stroke include the following: a sudden weakness or loss of sensation of the face, arm, or leg, especially on one side of the body, sudden confusion, problems with speech and understanding; sudden one or two-sided vision loss; 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 epileptic seizures. Other signs of vascular occlusion are: sudden pain, swelling and weakness of the limbs, acute abdomen. Symptoms of myocardial infarction include: pain, discomfort, pressure, heaviness, a feeling of constriction or distension in the chest, arm, or behind the sternum; discomfort radiating to the back, cheekbone, larynx, arm, stomach; cold sweat, nausea, vomiting or dizziness, severe weakness, anxiety, or shortness of breath; rapid or irregular heartbeat. Arterial thromboembolism can be fatal. The risk of developing thrombosis (venous and / or arterial) and thromboembolism increases: with age; - in smokers (with increasing number of cigarettes or increasing age, the risk increases, especially in women 35 years;) if you have: - a family history (for example, venous or arterial thromboembolism, ever with close relatives or parents at a relatively young age). In case of hereditary or acquired predisposition, the woman should be examined by an appropriate specialist to decide whether it is possible to take combined oral contraceptives - obesity (body mass index more than 30 kg / m2); - dyslipoproteinemia; - hypertension; - migraine; - valve disease heart; - atrial fibrillation; - prolonged immobilization, serious surgery, any surgery on the legs, or extensive trauma.In these situations, it is desirable to stop the use of combined oral contraceptives (in the case of the planned operation, at least four weeks before it) and not to resume reception for two weeks after the end of immobilization. The question of the possible role of varicose veins and surface thrombophlebitis in the development of venous thromboembolism remains controversial. You should take into account the increased risk of developing thromboembolism in the postpartum period. Peripheral circulatory disorders can also be observed in diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. Increased frequency and severity migraine during the use of combined oral contraceptives (which may precede cerebrovascular disorders) may be grounds for To stop taking these drugs. Biochemical indicators indicating a hereditary or acquired susceptibility to venous or arterial thrombosis include the following: resistance to activated protein C, hyperhomocysteinemia, lack of antithrombin III, lack of protein C, lack of protein S, anti-phospholipid antibodies (anti-thrombin III, anti-phospholipid antibodies, anti-thrombin III, lack of anti-phosphine lipid). lupus anticoagulant). When assessing the risk / benefit ratio, it should be borne in mind that adequate treatment of the corresponding condition can reduce the associated risk of thrombosis. It should also be borne in mind that the risk of thrombosis and thromboembolism during pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg ethinyl estradiol). Tumors The most significant risk factor for developing cervical cancer, is persistent papillomavirus infection. There are reports of some increase in the risk of cervical cancer with prolonged use of combined oral contraceptives. Relationship with the reception of combined oral contraceptives is not proven. Controversy persists regarding the extent to which these findings are related to screening for cervical pathology or sexual behavior (more rare use of barrier methods of contraception). Meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of developing breast cancer. diagnosed in womencurrently taking combined oral contraceptives (relative risk 1.24). The increased risk gradually disappears within 10 years after discontinuation of these drugs. Due to the fact that breast cancer is rarely observed in women under 40 years old, an increase in the number of breast cancer diagnoses in women who are currently taking or taking a combined oral contraceptive pill is insignificant relative to the overall risk of the disease. His connection with the reception of combined oral contraceptives has not been proven. The observed increase in risk may also be due to an earlier diagnosis of breast cancer in women using combined oral contraceptives. Women who have ever used combined oral contraceptives have earlier stages of breast cancer than women.