Long-term (over 21 days) use of the drug Belarus ® reduces the secretion of follicle stimulating hormone and luteinizing hormone, and therefore, suppression of ovulation, endometrial proliferation and secretory transformation. At the same time change the properties of cervical mucus, which is accompanied by difficulty passing of sperm through the cervical canal and the violation of their mobility. Part of the Belarus ®andriol bodybuilding acetate – progestogen having antiandrogenic properties. Its action is based on the ability to displace androgens on specific receptors, excluding and weakening the effect of endogenous and exogenous androgens. For a complete suppression of ovulation is required andriol bodybuilding acetate 1.7 mg daily. The required dose per cycle -. 25 mg The other active component of Belarus ® – ethinyl estradiol – inhibits the secretion of sweat glands of skin. It also significantly increases the production of binding globulin sex hormones, thereby reducing the amount of free testosterone in the blood plasma. Interaction with specialized estrogen receptors in target organs (in the fallopian tubes, cervix, vagina, vulva, excretory ducts of the mammary glands), causes proliferation of the endometrium. In addition to a reliable contraceptive action, positive action Belarus drug ® appears in the normalization of the menstrual cycle, reducing the severity of symptoms of premenstrual syndrome, the incidence of iron deficiency anemia, dysmenorrhea, functional ovarian cysts, ectopic pregnancy, malignancy of the endometrium and ovaries, some forms of benign breast diseases and inflammatory diseases of the pelvic organs. Pharmacokinetics: The ingestion of the drug andriol bodybuilding acetate and ethinyl estradiol quickly and completely absorbed. The maximum concentration of ethinyl estradiol is achieved after 1.5 h Maximum andriol bodybuilding acetate concentration is achieved in 1-2 hours.. The half-life andriol bodybuilding acetate is about 34-39 hours, ethinyl estradiol -. 12-14 hours andriol bodybuilding acetate metabolites excreted by the kidneys and the bowel in a ratio of 2 . 3 The half-life of ethinyl estradiol is about 12-14 hours. The metabolites of ethinyl estradiol – the water-soluble derivatives of sulfate or glucuronic conjugation. Ethinyl estradiol metabolites are excreted via the kidneys and intestines in a ratio of 4: 6.
Combined oral contraception (CCP) is contraindicated in the following cases. Admission Belarus ® should be discontinued immediately in the event of at least one of the following symptoms:
– the presence of thrombosis (venous and arterial) present or in history (eg deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke);
– the availability of First signs of thrombosis, thrombosis or embolism symptoms (eg, transient ischemic attack, angina, see “Special instructions.”);
– planned surgery (at least 4 weeks before) and the period of immobilization, for example, after injury (in Vol. hours after application of plaster casts).
– diabetes mellitus with vascular complications;
– diabetes that can not be adequately controlled;
– uncontrolled hypertension or a significant increase in blood pressure (over 140/90 mmHg; see section “Special instructions. ‘);
– hereditary or acquired predisposition for venous or arterial thrombosis, such as increased resistance of the organism to activated C protein (APC-resistance);
– lack of antithrombin III of, the lack of C-protein insufficiency S-protein, hyperhomocysteinemia, and antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant)
– hepatitis, jaundice, abnormal liver function (up to normalization of liver function tests);
– generalized pruritus, cholestasis, especially during a previous pregnancy or estrogen therapy;
– Dubin-Johnson syndrome, Rotor syndrome; condition / disease, accompanied by violation of the outflow of bile,
– the presence of current or a history of liver tumors;
– expressed epigastric pain, enlargement of the liver or. symptoms of intra-abdominal bleeding (see “Side effects” section.);
– display for the first time or recurrence of porphyria (all three forms, in particular acquired porphyria);
– the presence of hormone-dependent malignancies, including history, (for example, breast or uterus) or suspicion on them;
– The expressed disturbances of lipid metabolism,
– pancreatitis, now or in history, in combination with severe hypertriglyceridemia,
– the first attacks of migraine pain or frequent severe headaches
– migraines in conjunction with a local neurological symptoms (associated migraine) ;
– acute sensory disturbances, such as blurred vision or hearing;
– motor disorders (particularly paresis);
– exacerbation of epilepsy;
– severe depression
– otosclerosis during the preceding, pregnancies;
– amenorrhoea of unknown etiology;
– endometrial hyperplasia;
– bleeding from the vagina of unknown etiology;
– hypersensitivity to the drug;
– pregnancy or suspected it;
– the period of breast-feeding;
– smoking over the age of 35 years (see. See “Special Instructions”).
Use of the combination of estrogen / progestogen may have a negative impact on the course of certain diseases / conditions.
Special medical supervision is required in the following cases: epilepsy, multiple sclerosis; convulsions (tetany); migraine; bronchial asthma; cardiac or renal failure; chorea; diabetes with uncomplicated;diabetes mellitus (see also “Contraindications” section.) liver disease (see also “Contraindications” section.) abnormal lipid metabolism, dislipoproteinemia (see also “Contraindications” section.) autoimmune diseases (including systemic lupus erythematosus); obesity; arterial hypertension (see also “Contraindications” section.) endometriosis; varicose disease; phlebitis (see also “Contraindications” section.)violation of blood coagulation; breast; uterine fibroids; herpes gestationis; Depression (see also “Contraindications” section.) chronic inflammatory bowel disease (Crohn’s disease, ulcerative colitis).
Pregnancy and lactation Pregnancy: the use of the drug Belara ® during pregnancy is contraindicated. Before you begin to use the drug Belara ® , is necessary to exclude the presence of pregnancy. If pregnancy occurs while taking Belarus ® , the drug should be discontinued immediately. The presently available data do not contain information about the development of a teratogenic or embryotoxic effect in women who have accidentally taken during pregnancy drugs containing estrogen and progesterone in the same combination as in the preparation Belara ® . Lactation: not recommended Belara drug in during breastfeeding, because the drug reduces the amount of milk produced and changes its composition. Small amounts of a part of contraceptive hormones and / or their metabolites are excreted in breast milk and may influence breast-fed baby.
DOSAGE AND ADMINISTRATION
Tablets Belarus ® should be taken orally (preferably at the same time).
It is necessary to take the first pill on the 1st day of the menstrual cycle, and continue taking them every day for the 1st tablet per day for 21 days. Then take a 7-day break, during which menstrualnopodobnoe bleeding should begin.
After a 7-day break should resume taking pills Belarus ® from the next blister, whether stopped menstrualnopodobnoe bleeding or not.
Tablets must be squeezed out of the blister and swallowed whole , choosing the tablet, which is appropriately labeled the day of the week. Selection of the tablets is determined by the direction of the arrow on the package. Start taking the pills before used hormonal contraception (during the preceding menstrual cycle). The first tablet should be taken on the first day of menstruation. In this case the contraceptive action begins with the first day of dosing Belarus ® and maintained during a 7-day interval when the tablets are not taken. Furthermore, the first pill of Belarus ® can be taken at the 2nd-5th day of menstruation, irrespective of , stopped the bleeding or not. However, in this case, in the first 7 days of taking the pills need to use additional barrier contraception. If menstruation began early (more than 5 days), should be encouraged women to delay initiation of Belarus drug ® before the next bleeding. Switching from another hormonal contraceptive to Belarus drug ® . Go with preparations containing 21 or 22 active tablets: to be complete acceptance of all the tablets of the old package. The first tablet of the drug Belarus ® must be taken on the next day. There should be no break in the pill, and the patient does not wait until the next menstrual cycle. Additional contraceptive measures are not required. 28 tablets: the first tablet formulation Belarus ® should be taken the next day after the last active tablet from the packaging prior contraceptive preparation containing 28 tablets (i.e., after administration 21 active tablets ). There should be no break in the pill, and the patient does not wait until the next menstrual cycle.Additional contraceptive measures are not required. Go with contraceptives containing only progestogen (mini drank, injectable form, the implant). A woman can go with a mini drank the drug Belarus ® on any day (without a break), with the implant – the day of his removal with injectable forms – from the day when the next injection should have to be made. In all cases, you must use an additional barrier method of contraception during the first 7 days of taking the drug Belarus ® . After an abortion in the first trimester of pregnancy. It is necessary to start taking the drug Belarus ® immediately after abortion in the first trimester of pregnancy. Additional methods of contraception are not required. After delivery or abortion in the second trimester of pregnancy. After birth, the use of the drug in women not breastfeeding can be started at 21-28 days post-partum period. In this case, should not take additional contraceptive measures. If the use of the drug in the postpartum period started 28 days after birth, it is necessary to take additional measures of contraception for 7 days. If a woman has had sexual contact, before the use of the drug is necessary to exclude pregnancy or wait until the next menstrual cycle. Skipping taking the pill. If it has been less than 12 hours after it has been forgotten a pill, the contraceptive effect of the drug Belarus ® is preserved. Missed tablet should be taken immediately, as soon as she remembers about her, and the next tablet should be taken at the usual time. If more than 12 hours after the missed pills, may reduce the contraceptive action of the drug. It is necessary to take the missed pill immediately.Subsequent tablets should be taken at the usual time, but it should be for the next 7 days to apply additional barrier methods of contraception (condoms). If within 7 days of pills in a package does not run out, the pills of the next pack should be started immediately after the completion of the tablets in the previous package, ie do not pause between taking tablets from a variety of packages. If there was no menstrualnopodobnoe bleeding after taking the second pack, you must exclude pregnancy. The use in case of diarrhea, vomiting. If you experience vomiting or diarrhea while taking pills Belarus ® is recommended to use additional barrier methods of contraception, because contraceptive effect of the drug may be reduced due to incomplete absorption of the drug in the intestine.
When receiving the drug Belara ® the most common adverse reactions (more than 20% of cases) are breakthrough bleeding, bloody vaginal discharge, headache and discomfort in the breast. Intermenstrual bleeding usually decrease with increasing duration of admission of Belarus ® .
The frequency of adverse reactions is defined as follows: Very often: ≥ 1/10 Frequently: ≥ 1/100, <1/10 Uncommon: ≥ 1/1000; <1/100 Rare: ≥ 1/10 000, <1/1000 Very rare: <1/10 000 adverse reactions from the following organs and systems can be observed: The immune system . Uncommon: Hypersensitivity to the components of the preparation including an allergic reaction on the part of skin. Metabolism .Uncommon: changes in blood lipids including hypertriglyceridemia. rare: Increased appetite. Psycho-emotional sphere . Common: depression, nervousness, irritability. Uncommon: decreased libido. Nervous system . Often: dizziness, migraine (and / or its gain). The bodies of view . Common: visual disturbances. rare: conjunctivitis, contact lens intolerance. Organs of hearing and vestibular apparatus . rare:sudden hearing loss, tinnitus. Cardiovascular system . Common: increase in blood pressure. rare: hypertension, hypotension, cardiovascular collapse, varicose vein disease, venous thrombosis. The digestive system . Very common: nausea. Common: vomiting. Uncommon: abdominal pain, flatulence, diarrhea. Skin and subcutaneous tissue . Often: acne. Uncommon: pigmentation disorders, chloasma, hair loss, dry skin, rash. rare: urticaria, eczema, erythema, itching, increased psoriasis, hypertrichosis. Very rarely . erythema nodosum Musculoskeletal . Common: feeling of heaviness. Uncommon: back pain ., muscle disorders reproductive system and mammary glands . Very common: strengthening the mucous vaginal discharge, dysmenorrhea, amenorrhea. Common: pain in the lower abdomen.Uncommon: galactorrhoea, fibroadenoma of the breast, vaginal candidiasis. rare: breast enlargement, vulvovaginitis, . menorrhagia, premenstrual syndrome general disorders . Often: . fatigue, edema, weight gain When using combined oral contraceptives (CCP), including containing 0.03 mg ethinylestradiol and 2 mg andriol bodybuilding acetate, also note the following undesirable effects: – increase the risk of venous and arterial thromboembolism (such as venous thrombosis, pulmonary embolism, stroke, myocardial infarction). The risk may be exacerbated by additional factors sm. section “Special Instructions”. – Increase the risk of biliary tract disease, – in rare cases, increase the risk of benign tumors of the liver (and even more rarely – malignant tumors of the liver) and single cases can lead to life-threatening intra-abdominal bleeding (see also “Special instructions”.) – exacerbation of chronic inflammatory bowel disease (Crohn’s disease, ulcerative colitis, so zhe see “Special instructions”.).
If overdose is not observed any severe toxic reactions. If you accidentally taking a large number of tablets may develop nausea, vomiting, bleeding / vaginal bleeding.
No specific antidote. Treatment is symptomatic. In rare cases, requires monitoring indicators of water and electrolyte metabolism and liver function.
Interactions with other drugs
Interactions of ethinylestradiol, the estrogen component of the drug Belarus ® , with other medicines may increase or decrease in the ethinyl estradiol concentration in blood serum. If you need long-term treatment with these drugs, you should go to a non-hormonal contraceptive.
The decrease in the serum concentration of ethinyl estradiol may lead to more frequent episodes of breakthrough bleeding, disruption of the cycle and reducing the contraceptive effectiveness of the drug Belarus ® . Increasing the concentration of ethinyl estradiol in serum may increase the frequency and severity of side effects.
The following drugs / active substance can reduce the concentration of ethinyl estradiol in the blood serum:
– all drugs that enhance the motility of the gastrointestinal tract (eg, metoclopramide) or violate adsorption (e.g. activated carbon),
– active substances that induce microsomal liver enzymes, such as rifampin, rifabutin, barbiturates, antiepileptics (e.g., carbamazepine, oxcarbazepine, phenytoin, and topiramate), an anticonvulsant felbamate, phenylbutazone, griseofulvin, barbeksaklon, primidone, modafinil, some inhibitors proteases (eg, ritonavir) and drugs St. John’s wort;
-. some antibiotics (eg, ampicillin, tetracycline, rifampin) – due to lower enteropechenochnoy circulating estrogens
with simultaneous use of such drugs / active agents with pills Belarus ® necessary to use additional barrier methods of contraception both during treatment and for 7 days after. When receiving the active substances that reduce the concentration of ethinyl estradiol in the serum due to the induction of hepatic microsomal enzymes, additional barrier methods (condoms, spermicides) should be used within 28 days after treatment.
The following drugs / active ingredients may increase ethinyl estradiol concentration in the blood serum:
– active substances that inhibit sulfation of ethinyl estradiol in the intestinal wall, for example, ascorbic acid or paracetamol;
-. substances that suppress the activity of hepatic microsomal enzymes such as antifungal imidazoles (e.g., fluconazole), indinavir or troleandomycin
ethinylestradiol may affect the metabolism of other substances:
– suppress the activity of hepatic microsomal enzymes and thus increase the serum concentration of such active substances, such as diazepam (and other benzodiazepines metabolism which through hydroxylation), cyclosporin, theophylline and prednisolone;
– induce glucuronidation in the liver and correspondingly to reduce the concentration in serum, for example, clofibrate, paracetamol, morphine and lorazepam.
The need for insulin and oral antidiabetic agent may vary due to the influence of the drug on the glucose tolerance.
Smoking increases the risk of serious cardiovascular side PDAs effects, the risk increases with age and, depending on the number of cigarettes smoked and the more pronounced in women aged older than 35 years, smoking women aged over 35 years should use other methods of contraception.
If applying CCP increases the risk of serious diseases:. myocardial infarction, thrombosis / thromboembolism, stroke, and liver tumors
Other risk factors such as hypertension, hyperlipidemia, obesity and diabetes distinctly increase the risk of morbidity and mortality.
If you have one of these diseases / risk factors you must weigh the possible benefits of the drug from the destination Belara ® against the risks, and this should be discussed with the woman before taking her medication. If these diseases or risk factors will begin to appear or progress during treatment, consult your doctor.
The doctor must decide whether to stop taking the drug. Thromboembolism and other vascular diseases has been noted that there is a relationship between the intake of the CCP and an increased risk of of diseases caused by arterial or venous thromboembolism, such as myocardial infarction, cerebral stroke, deep vein thrombosis or pulmonary embolism. These complications are rare. CCP reception leads to an increased risk of venous thromboembolism (VTE). The risk of VTE is highest during the first year of admission. This risk is less than during pregnancy, when the VTE incidence is 60 cases per 100,000 pregnancies. VTE is fatal in 1-2% of cases. No assessment of the risk of VTE when receiving data Belarus ® compared to other PDAs. The risk of developing venous thromboembolic events increases when receiving CCP:
- with age
- in the presence of venous thromboembolism in relatives (venous thromboembolism in one of the brothers, sisters or parents at a relatively young age). If you intend to availability, hereditary predisposition, it is recommended to send a woman to consult a specialist before taking a decision on the appointment of the CCP
- decreased mobility at long
- obesity (body mass index> 30 kg / m 2 ).
The risk of arterial thromboembolic complications increases when receiving CCP:
- with age
- when dislipoproteinemia
- obesity (body mass index> 30 kg / m 2 )
- with heart disease
- in atrial fibrillation
in the presence of venous thromboembolism in relatives (arterial thromboembolism in one of the brothers, sisters or parents at a relatively young age). If a chronic inflammatory bowel disease (Crohn’s disease and ulcerative colitis), sickle-cell anemia. In assessing the risk / benefit ratio should be remembered that adequate treatment of the above diseases may reduce the risk of thrombosis. . It is necessary to take into account the increased risk of thromboembolic complications in the postpartum period
is no consensus about whether a relationship exists between thrombophlebitis of superficial veins and / or varicose veins and the aetiology of venous thromboembolism.
The following symptoms may occur when the development of venous or arterial thrombosis:
- leg pain and / or swelling
- sudden severe pain in the chest, radiating or without irradiation to the left arm
- sudden shortness of breath, coughing for no apparent reason
- sudden severe prolonged headache
- partial or complete loss of vision, diplopia / speech disorders or aphasia
- dizziness, collapse, in some cases accompanied by focal epileptic seizures
- sudden weakness or dysesthesia (sensitivity distortion) on one side or in one part of the body
- movement disorders
- acute abdominal pain.
Women taking the CPC shall be informed of the fact that the appearance of symptoms that resemble the symptoms of thrombosis, you should consult your doctor. Belara ® should be canceled in cases of suspected or confirmed thrombosis diagnosis.
Increased or increase in severity of migraine attacks during the reception of the CCP (which may be a precursor to the development of or a symptom of cerebrovascular disease) may be the reason for their withdrawal. Tumors noted that the use of the PDA is: a risk factor the development of cervical cancer in women infected with human papillomavirus (HPV). However, it is still controversial question of the degree of influence on the results of the observations of other confounding factors (eg, number of sexual partners or the use of mechanical contraceptives) (see. Also “Medical examination” ). There is evidence that the relative risk (RR = 1.24) of breast cancer in women taking CCP slightly above. During the 10 years after stopping the CCP’s risk level gradually decreases and returns to age. Because breast cancer is rare in women under the age of 40 years, the difference between the degree of risk of breast cancer in those taking currently and recently took PDAs women and the degree of the overall disease risk is low. There are reports of the development, in rare cases, benign, even more rare cases of malignant tumors of the liver at the time of reception of the CCP. In some cases, these tumors are the causes of life-threatening bleeding vnutibryushnyh. In case of severe abdominal pain that does not go by yourself, hepatomegaly or signs of intra-abdominal bleeding, you need to take into account the possibility of a liver tumor, and to cancel Belarus ® . Other Diseases Many women taking oral contraceptives, there is a slight increase in blood pressure; however, clinically significant increase is rare. The relationship between administration of oral contraceptives and clinical manifestation of hypertension has not been confirmed to date. If, during the reception of Belarus ® appears clinically significant increase in blood pressure, the drug should be discontinued and treat hypertension. As soon as the blood pressure will return to normal on the background of antihypertensive therapy, reception Belarus ® can be extended. In women with herpes pregnancy in history, on the background of the PDA can be a relapse of the disease. Women with a history of hypertriglyceridemia or a family history of such an increased risk of developing pancreatitis while taking handheld. Acute or chronic disturbances of liver function may require the cancellation of the CCP to the normalization of liver function. Relapse holestatacheskoy jaundice, which first appeared during the time of pregnancy or previous use of sex hormones, requires the abolition of the CCP. CCP may have effects on the resistance of peripheral tissues to insulin or glucose tolerance. Therefore, people with diabetes while taking oral contraceptives should be under constant supervision. In rare cases it can develop chloasma, especially in women who have had chloasma pregnant. Women are at risk of developing chloasma should avoid exposure to sunlight and ultraviolet radiation while taking oral contraceptives. Patients with a rare congenital defect – galactose intolerance, deficiency Lapp lactase or malabsorption syndrome glucose-galactose – should not take this medication. Medical examination Before prescribing oral contraceptives you need to collect comprehensive data on the health of the woman and her relatives to identify contraindications (see. section “Contraindications”) and risk factors (see “Precautions”). A woman should undergo a medical examination. The medical examination must be carried out each year while taking the drug Belara ® . Regular medical examination is also necessary due to the fact that diseases are contraindications (eg transient ischemic attack) or risk factors (eg, venous or arterial thrombosis in relatives) may first occur in patients receiving oral contraceptives. The medical examination should include measurement of blood pressure, examination of the breasts, abdomen, inner and outer genital swabbing the cervix and conduct appropriate laboratory tests. Women should be advised that the purpose of oral contraceptives, including drug Belara ® , does not protect it from HIV infection (AIDS) or other diseases, sexually transmitted diseases. Lack of efficiency skip taking the pill (see. section “Dosing and administration”, “missed doses” ), nausea, or symptoms of digestive disorders including diarrhea, prolonged concomitant use of certain drugs (see. section “Use in case of diarrhea, vomiting,” “Interaction with other medicinal products”) or, in very rare cases metabolic disorders may decrease the effectiveness of birth control. The effect on the menstrual cycle bleeding or spotting “breakthrough” (intermenstrual) All oral contraceptives may cause irregular vaginal bleeding (bleeding / spotting “breakthrough”), especially during the first few cycles in patients receiving the drug. Therefore, medical examination about irregular cycles should only be done after the adaptation period, which usually lasts for 3 cycles. If during the reception Belara ® appearance early bleeding continues or appeared for the first time a woman has a regular cycle, it is necessary to conduct a survey to exclude organic pathology or pregnancy; After excluding pregnancy and organic pathology reception Belarus ® can continue or switch to other medications. Bleeding appearing between cycles may be a sign of lack of contraceptive efficacy (see. “Missed doses”, “The application in the case of diarrhea, vomiting” ) Absence menstrualnopodobnoe bleeding (withdrawal bleeding) 21 days after dosing withdrawal bleeding usually occurs. Sometimes, especially in the first few months of drug administration, withdrawal bleeding may be omitted. However, this does not indicate a lack of contraceptive effect. If the bleeding does not occur after drug administration for one cycle, provided that has not been passed, no reception film-coated tablets, the period after completion of dosing did not exceed 7 days were not taken at the same time other drugs absent nausea or diarrhea, fertilization unlikely Is there, and welcome Belarus ® pregnancy or organic pathology. After excluding pregnancy and organic pathology reception Belarus ® can be continued. If the reception of Belarus ® instructions are not carried out before the first absence of withdrawal bleeding or withdrawal bleeding was absent for two consecutive cycles, it is necessary to exclude the presence of pregnancy for a decision on the continuation of treatment. At the same time taking Belara drug should not take herbal remedies containing St. John’s wort ( Hypericum perforatum ). laboratory parameters during the reception of the CPC may change some laboratory parameters, including the functional activity of the liver, adrenal and thyroid level associated proteins in plasma (e.g., SHBG (SHBG), cholesterol), carbohydrate metabolism, coagulation and fibrinolysis. The nature and extent of changes in part determined by the nature and dose of hormones taken.Effects on ability to drive a car or work on a precision instrument
is not affected.