Composition, form of production and packaging
The tablets covered with a cover of white color, the round form.
1 tab.
ethinylestradiol 20 Ојg
gestodene 75 mcg
Auxiliary substances: lactose monohydrate 37.155 mg, corn starch 15.5 mg, polyvidone 25,000 1.7 mg, magnesium stearate 550 Ојg, sucrose 19.66 mg, polyvidone 700,000 171 Ојg, macrogol 6000 2.18 mg, calcium carbonate 8.697 mg mg, talc - 4.242 mg, wax mountain glycolic - 50 mcg.
21 pcs. - blisters (1) - packs of cardboard.
21 pcs. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Logest В® is a low-dose monophasic oral combined estrogen-progestative contraceptive.
The contraceptive effect of Logest is carried out by means of complementary mechanisms, the most important of which are suppression of ovulation and changes in the state of cervical mucus.
In women taking combined oral contraceptives, the cycle becomes more regular, the pain and intensity of menstrual bleeding decreases, which reduces the risk of iron deficiency anemia. In addition, there is evidence that the risk of developing endometrial cancer and ovarian cancer is reduced.
When properly applied, the Perl index (an indicator that reflects the frequency of pregnancy in 100 women during the year of use of the contraceptive) is less than 1. If the tablets are misused, including pills, the Pearl index may increase.
PHARMACOKINETICS
Gestoden
Absorption. After oral administration, Gestodene is rapidly and completely absorbed, its maximum serum concentration, equal to 3.5 ng / ml, is reached after about 1 hour. Bioavailability is approximately 99%. Distribution. Gestodene binds to blood serum albumin and globulin, which binds sex hormones (SHBG). In a free form there is only about 1.3% of the total concentration in the blood serum; about 69% - are specifically related to SHGS. Induction with ethinylestradiol synthesis of SHBG affects the binding of Gestodene to plasma proteins.
Metabolism. Gestodene is almost completely metabolized. The serum clearance is approximately 0.8 ml / min / kg.
Excretion. The content of Gestodene in the serum undergoes a two-phase reduction. The half-life in the terminal phase is about 12 hours. In unmodified form, Gestodene is not excreted, but only in the form of metabolites that are excreted by the kidneys and through the intestine in a ratio of approximately 6: 4 with a half-life of about 24 hours.
Equilibrium concentration. The pharmacokinetics of Gestodene is influenced by the concentration of SHBG in serum. As a result of the daily intake of the drug, the concentration of the substance in the serum increases approximately 4-fold during the second half of the contraceptive cycle.
Ethinylestradiol
Absorption. After ingestion, ethinylestradiol is rapidly and completely absorbed. The maximum serum concentration in the blood serum is about 65 pg / ml, reached within 1-2 hours. During absorption and "first passage" through the liver, ethinylestradiol is rendered unstable, resulting in an average bioavailability of about 45%.
Distribution. Ethinyl estradiol is almost completely (approximately 98%), although non-specific, bound by albumin. Ethinyl estradiol induces synthesis of SHBG. The apparent volume of distribution of ethinylestradiol is 2.8-8.6 l / kg. Metabolism. Ethinyl estradiol undergoes presystemic conjugation, as in the mucosa thin. guts, and in the liver. The main pathway of metabolism is aromatic hydroxylation. The clearance rate from plasma is 2.3-7 ml / min / kg.
Excretion. The decrease in the concentration of ethinyl estradiol in 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 excreted. Metabolites of ethinyl estradiol are excreted in the urine and bile in a ratio of 4: 6 with a half-life of about 24 hours.
Equilibrium concentration. The equilibrium concentration is reached after about one week.
INDICATIONS
- oral contraception.
DOSING MODE
Tablets should be taken orally in the order given on the package, every day at about the same time, with a small amount of water. Take one tablet a day continuously for 21 days. Acceptance of the next package begins after a 7-day break in taking the tablets, during which bleeding "cancellation" usually develops. Bleeding, as a rule, begins on day 2-3 after the last pill and may not end before the start of the new package.
How to start receiving Logist
• In the absence of taking any hormonal contraceptives in the previous month.
The admission of Logest begins on the first day of the menstrual cycle (ie on the first day of menstrual bleeding). It is permissible to start taking the 2-5 menstrual cycle, but in this case it is recommended to additionally use the barrier method of contraception during the first 7 days of taking the tablets from the first package .
• When switching from other combined oral contraceptives, vaginal rings or contraceptive patches.
It is preferable to start Logesta the next day after taking the last hormone-containing tablet from the previous package, but in no case later than the day after the usual 7-day break (for preparations containing 21 tablets) or after taking the last inactive tablet (for preparations containing 28 tablets in a package). Logest should be taken on the day of removal of the vaginal ring or patch, but no later than the day when a new ring is to be inserted or a new patch is stuck.
• When switching from contraceptives containing only gestagens (mini-pili, injection, implant), or with the progestogen-releasing progestogen (Mirena®).
A woman can switch from a mini-drink to Logest any day (without interruption), from an implant or intrauterine contraceptive with gestagen - on the day of its removal, from the injection form - from the day the next injection is to be made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets.
• After abortion in the first trimester of pregnancy.
A woman can start taking the drug immediately. If this condition is met, the woman does not need additional contraceptive protection.
• After childbirth or abortion in the second trimester of pregnancy.
It is recommended to start taking the drug on the 21-28th day after the birth, if the woman does not breast-feed, or after the abortion in the second trimester of pregnancy. If the reception is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking the tablets. However, if a woman has already lived a sexual life, pregnancy should be excluded before the beginning of the admission, or it is necessary to wait for the first menstruation.
Acceptance of missed tablets
If the delay in taking the drug was less than 12 hours, the contraceptive protection is not reduced. A woman should take the pill as soon as possible, the next one is taken at the usual time.
If the delay in taking the tablets is more than 12 hours, the contraceptive protection can be reduced. The more pills are missed, and the closer the pass to the 7-day break in taking pills, the greater the probability of pregnancy. In this case, you can follow the following two basic rules:
• The drug should never be discontinued for more than 7 days.
• 7 days of continuous taking of tablets are required to achieve adequate suppression of hypothamapo-pituitary-ovarian regulation.
Accordingly, the following recommendations can be given if the delay in taking the tablets was more than 12 hours (the interval from the time of taking the last tablet is more than 36 hours).
• The first week of taking the drug
A woman should take the last missed pill as soon as possible, as soon as she remembers (even if it means taking two tablets at the same time). The next pill is taken at the usual time. In addition, a barrier method of contraception (for example, a condom) should be used for the next 7 days. If the sexual intercourse took place during the week before passing the pill, it is necessary to take into account the probability of pregnancy.
• The second week of taking the drug
A woman should take the last missed pill as soon as possible, as soon as she remembers (even if it means taking two tablets at the same time). The next tablet is taken at the usual time.
Provided that the woman took the pill correctly for 7 days preceding the first missed pill, there is no need to use additional contraceptive measures. Otherwise, as well as when two or more tablets are missed, barrier methods of contraception (for example, a condom) should be used additionally within 7 days.
• The third week of taking the drug
The risk of a decrease in reliability is inevitable due to the upcoming interruption in the intake of tablets. A woman should strictly adhere to one of the following two options. However, if in 7 days preceding the first missed tablet, all tablets were taken correctly, there is no need to use additional contraceptive methods.
1. A woman should take the last missed pill as soon as possible, as soon as she remembers (even if it means taking two tablets at the same time). The following tablets are taken at the usual time, until the tablets from the current package run out. The next package should be started immediately. Bleeding "cancellation" is unlikely until the second package is finished, but there may be spotting and "breakthrough" bleeding during the taking of tablets.
2. A woman can also interrupt the taking of tablets from the current package. Then she should take a break for 7 days, including the day of skipping the tablets and then start taking a new package.
If the woman missed taking the pills, and then during a break in admission she does not have a withdrawal bleeding, it is necessary to exclude pregnancy.
Recommendations in case of vomiting and diarrhea
If a woman has vomiting or diarrhea within 4 hours after taking the pill, absorption may be incomplete and additional contraceptive measures should be taken. In these cases, recommendations should be followed when skipping tablets.
Change in menstrual bleeding days
In order to delay - the beginning of menstrual bleeding, a woman should continue taking the tablets from the new Logest package just after taking all the pills from the previous one, without taking a break. Tablets from this new package can be taken for as long as the woman wishes (until the package is finished). Against the background of taking the drug from the second package, a woman may have spotting or "breakthrough" uterine bleeding. To resume the reception of Logesta from a new pack follows after an ordinary 7-day break.
In order to transfer the day of the onset of menstrual bleeding to another day of the week, the woman should shorten the nearest break in taking the pills for as many days as she wants. The shorter the interval, the greater the risk that it will not have withdrawal bleeding, and thereafter there will be spotting and "breakthrough" bleeding during the second package (as well as in the case when it would like to delay the onset of menstrual bleeding).
Additional information for individual groups of patients
Older patients
Not applicable. The drug Logest is not indicated after the onset of menopause.
Patients with hepatic impairment
The drug Logest is contraindicated in women with severe liver diseases until the liver function test results are normal. See also the section "Contraindications".
Patients with impaired renal function
The drug Logest has not been specifically studied in patients with impaired renal function. The available data do not suggest correction of the dosing regimen in such patients.
SIDE EFFECT
When taking Logest, as well as other combined oral contraceptives, irregular bleeding (spotting spotting or "breakthrough" bleeding) can occur, especially during the first months of use. Against the background of taking combined oral contraceptives, other undesirable effects were observed in women, the relationship of which with taking drugs was not confirmed, but not disproved.
Body System Often (> 1/100) Infrequent (> 1/1000 and <1/100) Rarely (<1/1000)
Body of sight intolerance to contact lenses (discomfort when wearing them)
Gastrointestinal pain, nausea, abdominal pain, vomiting, diarrhea
Immune system hypersensitivity
General symptoms of weight gain, weight loss
Metabolism of fluid retention
Nervous system headache migraine
Mental disorders decreased mood, mood swings decreased libido increased libido
Reproductive system and mammary glands soreness of the mammary glands, breast engorgement mammary gland hypertrophy vaginal discharge, mammary gland secretion
Skin and subcutaneous tissue rash, erythema nodosum urticaria, erythema multiforme
The following serious adverse events have been reported in women using combined oral contraceptives. Additional information on the possible side effects of oral combined contraceptives, including Logest, is presented in the section "Special instructions":
• Venous thromboembolic disorders
• Arterial thromboembolic disorders
• Cerebrovascular disorders
• Increased blood pressure
• Hypertriglyceridemia
• Changes in glucose tolerance or effects on peripheral insulin resistance
• Liver tumors (benign and malignant)
• Impaired liver function
• Chloasma
• Onset or worsening of conditions for which communication with combined oral contraceptives has not been proven: jaundice and / or pruritus associated with cholestasis; formation of gallstones; porphyrin disease; systemic lupus erythematosus; hemolytic-uremic syndrome; chorea; herpes pregnant; hearing loss associated with otosclerosis; Crohn's disease; ulcerative colitis; cervical cancer.
The frequency of diagnosing breast cancer in women using oral contraceptives is increased very slightly. Breast cancer is rarely seen in women under 40 years of age, exceeding the frequency is insignificant in relation to the overall risk of breast cancer. Causality of the occurrence of breast cancer using combined oral contraceptives is not established. For more information, see "Contraindications" and "Special instructions".
CONTRAINDICATIONS
The drug Logest should not be used in the presence of any of the conditions / diseases listed below. If any of these conditions / diseases develop for the first time against the background of admission, the drug should be immediately withdrawn;
- Thrombosis (venous and arterial) and thromboembolism now or in the anamnesis (including, deep vein thrombosis, pulmonary embolism, myocardial infarction), cerebrovascular disorders;
- conditions preceding thrombosis (including, transient ischemic attacks, angina pectoris) at present or in the anamnesis;
- presence of expressed or multiple risk factors of venous or arterial thrombosis may also be a contraindication (see section "Special instructions");
- migraine with focal neurologic symptoms at present or in anamnesis;
- diabetes mellitus with vascular complications;
- pancreatitis with severe hypertriglyceridemia at present or in the anamnesis;
- liver failure and severe liver disease (until liver tests are normal);
- Liver tumors (benign or malignant) at present or in the anamnesis;
- identified hormone-dependent malignant neoplasms (including genital organs or mammary glands) or suspicion of them;
bleeding from the vagina of unknown origin;
- Pregnancy or suspicion of it;
- breast-feeding;
- Hypersensitivity to any of the components of the drug Logest.
Carefully:
If any of the conditions / diseases / risk factors listed below are currently available, the potential risk and the expected benefit of using combined oral contraceptives in each individual case should be carefully weighed:
- risk factors for thrombosis and thromboembolism: smoking; thrombosis, myocardial infarction or cerebrovascular accident at a young age in someone of the next of kin; obesity; dyslipoproteinemia, arterial hypertension; migraine without focal neurological symptoms; heart valve diseases; heart rhythm disturbances, prolonged immobilization, serious surgical interventions, extensive trauma;
- other diseases in which the may occur peripheral circulation disorders: diabetes without vascular complications; systemic lupus erythematosus; gsmolitiko-uremic syndrome; Crohn's disease and nespstsifichssky '. ulcerative colitis; sickle cell anemia; and phlebitis of superficial veins;
- hypertriglyceridemia;
- liver disease;
- diseases caused or aggravated by the first time during pregnancy, or on the background of the previous use of sex hormones (eg, jaundice, cholestasis, gallbladder disease, otosclerosis with hearing impairment, porphyria, herpes gestationis, Sydenham's chorea);
- in women with hereditary angioedema exogenous estrogens may induce or exacerbate symptoms of angioedema.
PREGNANCY AND LACTATION
Logest В® is contraindicated during pregnancy and lactation. If a pregnancy is detected during treatment Logest В® , the drug should be immediately canceled. However, numerous epidemiological studies have revealed no increased risk of defects in children born to women treated with hormones prior to pregnancy or teratogenic effect when sex hormones were taken inadvertently in early pregnancy.
Receiving Logest as other combined oral contraceptives, can reduce the amount of breast milk and change its composition, however, their use is not recommended during lactation. A small amount of hormones and / or their metabolites may be excreted in breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug Logest not been specifically studied in patients with disorders of the kidneys. Available data do not suggest correction dosing regimen in these patients.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Logest drug is contraindicated in women with severe liver disease as long as liver function tests have not come back to normal. See. Also Contraindications section.
APPLICATION FOR CHILDREN
Preparation Logest В® shown only after menarche.
APPLICATION IN ELDERLY PATIENTS
Not applicable. Preparation Logest В® not shown after menopause.
SPECIAL INSTRUCTIONS
If any of the conditions / diseases / risk factors mentioned below are currently available, you should carefully weigh the potential risks and expected benefits of the use of combined oral contraceptives, including Logest, in each individual case and discuss it with the woman before she decides to start taking the drug / In case of aggravation, the gain or the first manifestation of any of these conditions or risk factors, the woman should consult with your obstetrician-gynecologist, who can take dec ix of the need to discontinuation of the drug.
Diseases of the cardiovascular system
Epidemiological studies indicate a relationship between the use of combined oral contraceptives and increased incidence of venous and arterial thrombosis and thromboembolism (such as deep vein thrombosis, pulmonary embolism, myocardial infarction, cerebrovascular disturbances) when receiving combined oral contraceptives. These diseases are rare.
The risk of developing venous thromboembolism (VTE) is greatest in the first year of taking these drugs. The increased risk is present after initial use of combined oral contraceptives or resume use of the same or different combined oral contraceptives (after the interval between doses of the drug in 4 weeks or more). Data from a large prospective study involving 3 groups of patients suggest that this increased risk is present mainly in the first 3 months. The overall risk of VTE in patients receiving low-dose combined oral contraceptives (<50 micrograms ethinyl estradiol) are two to three times higher than that neberemenngh patients who are not taking combined oral contraceptives, however,this risk remains lower than the risk of VTE in pregnancy and childbirth.
VTE may be fatal (in 1-2% of cases).
VTE, manifested as deep vein thrombosis or pulmonary embolism may occur when using any combined oral contraceptives. Very rarely using COCs thrombosis occurs in other blood vessels, for example, hepatic, mesenteric, renal, and cerebral arteries veins or the retinal vessels. Consensus about the connection between the occurrence of these events and the use of combined oral contraceptives available.
Symptoms of deep vein thrombosis (DVT) include lower extremity edema unilateral or along veins in the leg, pain or discomfort in the foot only in a vertical position or during walking, the local temperature rise in the affected leg, redness or discoloration of the skin on the foot. Symptoms of pulmonary embolism (PE) are the following: difficulty or shortness of breath; sudden cough, including hemoptysis; sharp chest pain, which may be aggravated by deep inspiration; sense of anxiety; severe dizziness; fast or irregular heartbeat. Some of these symptoms (eg, dyspnea, coughing) are nonspecific and may be incorrectly interpreted as signs of other more or less severe complications (e.g., respiratory infection).
Arterial thrombosis may lead to stroke, vascular occlusion or myocardial infarction. The symptoms of stroke are: sudden weakness or loss of sensitivity of the face, arm or leg, especially on one side of the body, sudden confusion, trouble speaking and understanding; single- or double-sided sudden vision loss; sudden gait disturbance, dizziness, loss of balance or coordination; sudden, severe or prolonged headache with no apparent cause; loss of consciousness or fainting with or without epileptic seizure him. Other signs of vascular occlusion: sudden pain, swelling and slight bluish limbs, "acute" abdomen.
Symptoms of heart attack include: pain, discomfort, pressure, heaviness, or constriction of fullness in the chest, arm or behind the breastbone; discomfort radiating to the back, cheeks, throat, arm, stomach; cold sweat, nausea, vomiting or dizziness, severe weakness, anxiety or shortness of breath; fast or irregular heartbeat.
Arterial thromboembolism can be fatal.
The risk of thrombosis (venous -and / or arterial) and thromboembolism is increased:
-c age;
y smoking (with the number of cigarettes or increasing age the risk increases, especially in women over 35 years old);
in the presence of:
- family history (eg venous or arterial thromboembolism ever in close relatives or parents at a relatively young age). In the case of hereditary or acquired predisposition, the woman should be assessed and the appropriate specialist to address the issue of the possibility of using combined oral contraceptives;
- obesity (BMI over 30 kg / m2);
- dislipoproteinemia;
- hypertension;
- migraine;
- diseases of the heart valves;
- atrial fibrillation;
- prolonged immobilization, major surgery, any surgery to the legs, or major trauma. In these situations, it is desirable to discontinue the use of combined oral contraceptives (in case the intended operation of at least four weeks prior to it) and not to resume reception within two weeks after the immobilization.
The possible role of varicose veins and superficial thrombophlebitis in venous thromboembolism is controversial. It should take into account the increased risk of thromboembolism during the postpartum period.
Peripheral circulatory disorders as may occur in diabetes mellitus, systemic lupus erythematosus, hemolytic-uremic syndrome, chronic inflammatory bowel diseases (Crohn's disease or ulcerative colitis) and sickle cell anemia.
The increase in frequency and severity of migraine during use of combined oral contraceptives (which may be preceded by cerebrovascular disorders) can be grounds for immediate discontinuation of these drugs.
By biochemical parameters indicating the inherited or acquired predisposition to venous or arterial thrombosis include: resistance to activated protein C, hyperhomocysteinemia, lack of antithrombin III, protein C deficiency, protein deficiency S, antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant). In assessing the risks and benefits should be taken into account that adequate treatment of the relevant condition may reduce the associated risk of thrombosis. It should also be borne in mind that the risk of thrombosis and thromboembolism in pregnancy is higher than when taking low-dose oral contraceptives (<0.05 mg ethinylestradiol).
Tumors
The most significant risk factor for cervical cancer is persistent HPV infection. There are reports of some increase in the risk of cervical cancer in long-term use of combined oral contraceptives. Communication with the reception of combined oral contraceptives has not been proved. Reserved controversy as to what extent these findings associated with screening for cervical abnormalities or features with sexual behavior (less frequent use of barrier methods of contraception).
A meta-analysis of 54 epidemiological studies showed that there is a slightly increased relative risk of breast cancer diagnosed in women taking combined oral contraceptives currently (relative risk 1.24). The increased risk disappears gradually within 10 years after discontinuation of these drugs. Due to the fact that breast cancer is rare in women under 40 years, an increase in the number of breast cancer diagnoses in women taking combined oral contraceptives are currently taking or have recently, it is insignificant in relation to the total risk of the disease. His connection with the reception of combined oral contraceptives has not been proved. The observed increase in risk may be due to an earlier diagnosis of breast cancer in women,applying the combined oral contraceptives. In women, ever use a combined oral contraceptives, revealed earlier stages of breast cancer than women who never let them apply.
In rare cases on the background of the use of combined oral contraceptives observed the development of benign and in extremely rare - malignant tumors of the liver, which in some cases lead to life-threatening intraabdominal bleeding. In case of severe pain in the abdomen, liver enlargement or signs of intra-abdominal bleeding it should be considered in the differential diagnosis.
Other conditions
Women with hypertriglyceridemia (or the presence of this condition have a family history) may increase the risk of pancreatitis - while taking combined oral contraceptives.
Although small increases in blood pressure have been reported in many women taking COCs, clinically relevant increases were rare. However, if while taking combined oral contraceptives develops persistent, clinically significant increase in blood pressure, you should cancel this medication and treat hypertension. Receiving COCs can be continued, if using antihypertensive therapy achieved normal blood pressure values.
The following conditions have been reported to develop or worsen both during pregnancy and when taking combined oral contraceptives, but their connection with the reception of combined oral contraceptives has not been proven: jaundice and / or pruritus related to cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; chorea; herpes gestationis; hearing loss associated with otosclerosis. cases of Crohn's disease and ulcerative colitis against application of combined oral koshratseptivov also described.
In women with hereditary forms of angioedema exogenous estrogens may induce or worsen symptoms of angioedema. Acute or chronic disturbances of liver function may require the cancellation of combined oral contraceptives as long as liver function tests have not returned to normal. Recurrent cholestatic jaundice that develops for the first time during pregnancy or previous use of sex hormones, requires discontinuation of COCs.
Although combined oral contraceptives, may exert influence on insulin resistance and glucose tolerance, there is no need to change the therapeutic regimen in diabetics using low-dose combined oral contraceptives (<0.05 mg ethinylestradiol). However, women with diabetes should be carefully observed while taking combined oral contraceptives. Sometimes it can develop chloasma, especially in women with a history of chloasma during pregnancy. Women with a tendency to chloasma while taking combined oral contraceptives should avoid prolonged exposure to sunlight and ultraviolet radiation. Each tablet Logest preparation comprises 35 mg of lactose.Patients with rare hereditary diseases - galactose intolerance, lactase deficiency, glucose-galactose malabsorption who are on a diet with the exception of lactose, should take into account information about lactose content in the product.
Laboratory tests
using combined oral contraceptives can affect the results of certain lab tests, including liver function, kidney, thyroid, adrenal glands, contain transport proteins in the plasma, carbohydrate metabolism, coagulation and fibrinolysis parameters. Changes do not usually go beyond the normal range.
Reduced efficacy
The efficacy of combined oral contraceptives, drugs can be reduced in the following cases: when skipping tablets, vomiting and diarrhea, or resulting from drug interactions.
Effect on bleeding patterns
In patients receiving combined oral contraceptives may experience irregular bleeding (spotting or "breakthrough" bleeding), especially during the first few months of use. Therefore, evaluation of any irregular bleeding should be performed only after an adaptation period of approximately three cycles.
If irregular bleeding recur or develop after previous regular cycles, you should conduct a thorough examination to exclude malignancy or pregnancy.
Some women during the tablet-free interval may not develop bleeding "cancel". If combined oral contraceptives are taken according to the directions, it is unlikely that the woman is pregnant. However, if before taking combined oral contraceptives
