Belara, pills, 21pcs

Composition

One film-coated tablet contains

active ingredients:

chlormadinone acetate 2 mg and ethinyl estradiol 0.03 mg;

excipients:

povidone K 30-4.5 mg,

corn starch-9.0 mg,

lactose monohydrate-68.97 mg,

magnesium stearate-0.5 mg

film coating:

hypromellose 6 MPa. c-1.115 mg,

lactose monohydrate-0.575 mg,

macrogol 6000-0.279 mg,

propylene glycol-0.093 mg,

talc-0.371 mg,

titanium dioxide dye,

E 171-0

.557 mg, iron oxide red (III) dye, E 172-0.01 mg

Pharmacological action

Pharmacodynamics :

Prolonged (more than 21 days) use of BELARA leads to a decrease in the secretion of follicle-stimulating hormone and luteinizing hormone, and, consequently, suppression of ovulation, endometrial proliferation and its secretory transformation. At the same time, the properties of the mucus of the cervical canal change, which is accompanied by difficulty in passing spermatozoa through the cervical canal and a violation of their mobility.

Chlormadinone acetate, which is part of BELARA, is a progestogen with antiandrogenic properties. Its action is based on the ability to replace androgens at specific receptors, eliminating and weakening the effect of endogenous and exogenous androgens. Complete ovulation suppression requires 1.7 mg of chlormadinone acetate daily. The required dose per cycle is 25 mg.

Another active component of BELARA — ethinyl estradiol-inhibits the secretion of skin sweat glands. It also significantly increases the production of sex hormone-binding globulin, thereby reducing the amount of free testosterone in the blood plasma.

It interacts with specialized estrogen receptors in target organs (in the fallopian tubes, cervix, vagina, external genitalia, excretory ducts of the mammary glands), causes endometrial proliferation.

In addition to a reliable contraceptive effect, the positive effect of BELARA is manifested in the normalization of the menstrual cycle, reducing the severity of premenstrual syndrome, the frequency of iron deficiency anemia, dysmenorrhea, functional ovarian cysts, ectopic pregnancy, endometrial and ovarian malignancies, some forms of benign breast diseases and pelvic inflammatory diseases.

Pharmacokinetics

When taken orally, chlormadinone acetate and ethinyl estradiol are rapidly and completely absorbed. The maximum concentration of ethinyl estradiol is reached in 1.5 hours. The maximum concentration of chlormadinone acetate is reached in 1-2 hours.

The half-life of chlormadinone acetate is approximately 34-39 hours, ethinyl estradiol-12-14 hours. Metabolites of chlormadinone acetate are excreted by the kidneys and through the intestines in a ratio of 2: 3.

The elimination half-life of ethinyl estradiol is approximately 12-14 hours.

Ethinyl estradiol metabolites are water-soluble derivatives of sulfate or glucuronic conjugation.

Metabolites of ethinyl estradiol are excreted by the kidneys and through the intestines in a ratio of 4: 6.

Indications

Oral contraception.

Use during pregnancy and lactation

Pregnancy: the use of Belara during pregnancy is contraindicated. Before starting the use of the drug Belara, it is necessary to exclude the presence of pregnancy.

If pregnancy occurs while taking Belara, the drug should be stopped immediately. Currently available data do not contain information on the development of teratogenic or embryotoxic effects in women who accidentally took drugs containing estrogens and progesterones in the same combination as in the preparation Belara during pregnancy.

Lactation period: it is not recommended to use Belara during breastfeeding, as the drug reduces the amount of milk produced and changes its composition. Small amounts of the hormones and/or their metabolites that make up the contraceptive are excreted in breast milk and may affect the baby being fed.

Contraindications

Combined oral contraception (CPC) is contraindicated in the following cases. Belara should be discontinued immediately if at least one of the following symptoms occurs: :

• the presence of thrombosis (venous and arterial) in the present or in history (e. g., deep venous thrombosis, pulmonary embolism, myocardial infarction, stroke);
• also, the first signs of thrombosis, thrombophlebitis or symptoms of embolism (e. g., transient ischemic attack, angina);
• planned surgery (at least 4 weeks ahead of time) and the period of immobilization, for example, after trauma (i. e. after the application of the plaster bandages);
• diabetes mellitus with vascular complications;
• diabetes mellitus that can not be adequately controlled;
• uncontrolled hypertension or significant increase in blood pressure (over 140/90 mm. St., see section “Special instructions”);
• hereditary or acquired predisposition for venous or arterial thrombosis, such as increased resistance of the body to an activated C-protein (APC-resistance);
• deficiency of antithrombin III deficiency With protein S deficiency protein, hyperhomocysteinemia and antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant);
• hepatitis, jaundice, abnormal liver function (up to normalization of liver tests);
• generalized pruritus, cholestasis, especially during a previous pregnancy or estrogen therapy;
• syndrome Dubin-Johnson syndrome Rotor, conditions/ diseases associated with disruption of bile flow;
• the presence or history of liver tumors;
• expressed epigastric pain, liver enlargement or. symptoms of intra-abdominal bleeding (see section “Side effect”);
• the first manifestation or recurrence of porphyria (all three forms, especially the acquired porphyria);
• the presence of hormone-dependent malignancies, including history (e. g. of the breast or uterus) or suspicion of them;
• marked disorders of lipid metabolism;
• pancreatitis currently or in history, in combination with severe hypertriglyceridemia;
• the first attacks of migraine pain, frequent or severe headaches;
• migraine combined with local neurological symptoms (associated migraine);
• acute sensory impairment, for example, disturbances of vision or hearing;
• movement disorders (in particular, paralysis);
• worsening of the course of epilepsy;
• severe depression;
• otosclerosis during previous pregnancies;
• amenorrhea of unknown etiology;
• endometrial hyperplasia;
• vaginal bleeding of unknown etiology;
• hypersensitivity to the drug;
• pregnancy or suspicion of it;
• the breast-feeding period;
• Smoking at the age of 35 years (see “Special instructions”).

With caution, the use of the estrogen/progestogen combination may have a negative effect on the course of certain diseases/states. Special medical supervision is required in the following cases: epilepsy, multiple sclerosis; convulsive syndrome (tetany); migraine; bronchial asthma; heart or kidney failure; chorea minor; diabetes mellitus with an uncomplicated course; diabetes mellitus (see also the section “Contraindications”); liver diseases (see also the section “Contraindications”); lipid metabolism disorders, dyslipoproteinemia (see also the section “Contraindications”); autoimmune diseases diseases (including systemic lupus erythematosus); obesity; arterial hypertension (see also the section “Contraindications”); endometriosis; varicose veins; phlebitis (see also the section “Contraindications”); blood coagulation disorders; mastopathy; uterine fibroids; herpes of pregnancy; depression (see also the section “Contraindications”); chronic inflammatory bowel diseases (Crohn’s disease, ulcerative colitis).

Side effects

There may be adverse reactions from the following organs and systems: :

The immune system. Infrequently: hypersensitivity to the components of the drug, including allergic reactions from the skin.

Metabolism. Infrequently: changes in blood lipid composition including hypertriglyceridemia. Rare: increased appetite.

The psycho-emotional sphere. Often: depressive state, nervousness, irritability. Infrequently: decreased libido.

The nervous system. Common: dizziness, migraines (and/or worse).

Organs of vision. Common: visual disturbances. Rare: conjunctivitis, contact lens intolerance.

Hearing organs and vestibular apparatus. Rare: sudden hearing loss, tinnitus.

The cardiovascular system. Often: increased blood pressure. Rare: hypertension, hypotension, cardiovascular collapse, varicose veins, venous thrombosis.

The digestive system. Very Common: nausea. Common: vomiting. Infrequently: abdominal pain, flatulence, diarrhea.

Skin and subcutaneous tissue. Common: acne. Infrequently: pigmentation disorders, chloasma, hair loss, dry skin, hyperhidrosis. Rare: urticaria, eczema, erythema, itchy skin, increased psoriasis, hypertrichosis. Very rare: erythema nodosum.

Musculoskeletal system. Often: feeling heavy. Infrequently: back pain, muscle disorders.

Reproductive system and mammary glands. Very Common: increased mucosal discharge from the vagina, dysmenorrhea, amenorrhea. Common: pain in the lower abdomen. Infrequently: galactorrhea, breast fibroadenoma, vaginal candidiasis.Rare: breast enlargement, vulvovaginitis, menoragia, premenstrual syndrome.

General disorders. Common: fatigue, swelling, weight gain.

When using combined oral contraceptives (COCs), including containing 0.03 mg of ethinyl estradiol and 2 mg of chlormadinone acetate, the following undesirable effects were also observed::

– increased risk of venous and arterial thromboembolism (for example, venous thrombosis, pulmonary embolism, stroke, myocardial infarction). The risk may be increased by additional factors, see the section “Special instructions”. — increased risk of biliary tract disease— – in rare cases, an increased risk of developing benign liver neoplasms (and even less often-malignant liver neoplasms) and isolated cases can lead to life-threatening intra-abdominal bleeding (see also “Special instructions”), – exacerbation of chronic inflammatory bowel diseases (Crohn’s disease, ulcerative colitis).

Interaction

Interaction of ethinyl estradiol, an estrogenic component of BELARA®, with other drugs may cause an increase or decrease in the concentration of ethinyl estradiol in the blood serum. If you need long-term treatment with these medications, you should switch to non-hormonal contraceptives.

A decrease in the concentration of ethinyl estradiol in the blood serum can lead to an increase in episodes of breakthrough bleeding, disruption of the cycle and a decrease in the contraceptive effectiveness of BELARA®. Increasing the concentration of ethinyl estradiol in the blood serum can increase the frequency and severity of side effects.

The following medications /active substances can reduce the concentration of ethinyl estradiol in the blood serum:— all drugs that increase the motility of the gastrointestinal tract (e. g., metoclopramide) or interferes with the adsorption (e. g., activated carbon);

— active substances, inducing microsomal liver enzymes, such as rifampicin, rifabutin, barbiturates, antiepileptic agents (eg, carbamazepine, oxcarbazepine, phenytoin, topiramate) anticonvulsant felbamate, phenylbutazone, griseofulvin, barbexaclone, primidon, modafinil, some protease inhibitors (eg, ritonavir) and St. John’s wort preparations;

some antibiotics (eg, ampicillin, tetracycline, rifampicin) — due to the reduction antropogennoi circulation of estrogens. When such drugs /active substances are used simultaneously with BELARA® tablets, additional barrier methods of contraception should be used, both during treatment and for 7 days after it. When taking active substances that reduce the concentration of ethinyl estradiol in the blood serum due to the induction of hepatic microsomal enzymes, additional barrier methods (condom, spermicides) should be used within 28 days after the end of treatment.

The following medications /active substances may increase the concentration of ethinyl estradiol in the blood serum:

– active substances that inhibit the sulfation of ethinyl estradiol in the intestinal wall, for example, ascorbic acid or paracetamol;— atorvastatin;- substances that inhibit the activity of hepatic microsomal enzymes, such as antifungal imidazoles (for example, fluconazole), indinavir or troleandomycin.

Ethinyl Estradiol can affect the metabolism of other substances:

— suppress the activity of hepatic microsomal enzymes and, consequently, to increase the concentration in the blood serum of such active substances as diazepam (and other benzodiazepines, the metabolism of which is via hydroxylation), cyclosporine, theophylline and prednisolone; to induce glucuronidation in the liver and, consequently, to reduce the concentration in the blood serum, for example, clofibrate, paracetamol, morphine and lorazepam.

The need for insulin and oral antidiabetic agents may change due to the drug’s effect on glucose tolerance.

How to take, course of use and dosage

Belara tablets begin to be taken on the 1st day of the menstrual cycle and continue to be taken daily (preferably at the same time) for 21 days. Then you should take a 7-day break, during which menstrual-like bleeding should begin. After a 7-day break, you should resume taking the drug from the next blister, regardless of whether the menstrual-like bleeding has stopped or not.

If hormonal contraceptives have not been used during the previous menstrual cycle, the pill should be taken on the first day of the normal menstrual cycle (the first day of menstruation). The contraceptive effect begins on the first day of admission. If menstruation lasts more than one day, the first pill should be taken on the 5th day of menstruation, regardless of whether the bleeding has stopped or not. In this case, you should use additional, non-hormonal methods of contraception during the first 7 days. If more than 5 days have passed since the beginning of menstruation, then a woman is recommended to start taking the drug from the next menstrual cycle.

When switching from another hormonal contraceptive containing 21 active tablets, you should stop taking all the tablets of the old package. The first tablet of Belara should be taken the next day. There should be no break in taking pills; the patient should not wait for the next menstrual cycle to occur.

When switching from another hormonal contraceptive containing 28 tablets, the first tablet of Belara should be taken the day after taking the last active tablet from the package of the previous contraceptive (i. e., after taking 21 active tablets). There should be no break in taking pills; the patient should not wait for the next menstrual cycle to occur.

When switching from progestogen-only contraceptives (mini-pili), a woman can start taking Belara on any day (without interruption); when switching from using an implant containing a progestogen – on the day of its removal; when switching from injectable progestogens – from the day when the next injection should have been made. In all cases, it is necessary to use additional barrier methods of contraception during the first 7 days of taking Belara.

After an abortion in the first trimester of pregnancy, you should start taking the drug immediately after the abortion. Additional methods of contraception are not required.

After giving birth, women who are not breast-feeding can start taking Belara on the 21st-28th day of the postpartum period. In this case, no additional contraceptive measures should be taken. If the use of the drug in the postpartum period is started 28 days after delivery, then additional contraceptive measures should be taken within 7 days. If a woman has had sexual contact, then before using the drug, it is necessary to exclude pregnancy and wait for the next menstrual cycle.

If the patient did not take the drug at the usual time and less than 12 hours have passed since the set time of admission, the contraceptive effect of the drug remains, and the missed tablet should be taken as soon as possible. The next tablet must be taken at the set time.

If more than 12 hours have passed since the set time of use, the contraceptive effect of the drug may decrease. You should immediately take the missed pill and then continue taking the drug at the usual time. At the same time, it is necessary to use additional barrier methods of contraception for the next 7 days. If within these 7 days the tablets in the package have run out, then taking tablets from the next package should start immediately after the tablets in the previous package are completed, i. e. there is no break between taking tablets from different packages. If there was no menstrual-like bleeding after taking the second package, pregnancy should be excluded.

If vomiting or diarrhea occurs while taking Belara tablets, it is recommended to use additional methods of contraception, since the contraceptive effect of the drug may decrease due to incomplete absorption of the active substances of the drug in the intestine. Tablets should be swallowed whole, choosing the tablet that is marked with the corresponding day of the week. The choice of tablets is determined by the direction of the arrow on the package.

Overdose

In case of overdose with the drug, no severe toxic reactions are observed.

If you accidentally take a large number of tablets, you may develop nausea, vomiting, spotting/ bleeding from the vagina.

There is no specific antidote.

Treatment is symptomatic.

In rare cases, monitoring of water-electrolyte metabolism and liver function is necessary.

Special instructions

Smoking increases the risk of developing severe cardiovascular side effects of COCs, the risk increases with age and depending on the number of cigarettes smoked and is more pronounced in women over the age of 35, smoking women over the age of 35 should use other methods of contraception.

When using COCs, the risk of developing serious diseases increases: myocardial infarction, thrombosis/thromboembolism, stroke, and liver neoplasms.

Other risk factors such as hypertension, hyperlipidemia, obesity, and diabetes clearly increase the risk of morbidity and mortality.

If you have one of the above diseases/risk factors, you should weigh the possible benefits of using Belara® against the risks, and this should be discussed with the woman before starting taking the drug. If these diseases or risk factors begin to manifest or progress while taking the drug, you should consult a doctor.

The doctor must decide whether to stop taking this medication.

Thromboembolism and other vascular diseases

It is noted that there is a correlation between the use of COCs and an increased risk of diseases caused by venous or arterial thromboembolism, for example, myocardial infarction, brain stroke, deep vein thrombosis or pulmonary embolism. These complications are rare.

Taking COCs increases the risk of venous thromboembolism (VTE). The risk of VTE is greatest during the first year of treatment. The degree of such risk is lower than in pregnancy, when the VTE rate is 60 cases per 100,000 pregnancies. VTE is fatal in 1-2% of cases. There are no data on the assessment of the development of VTE risk when taking Belara® in comparison with other COCs. The risk of venous thromboembolic complications increases when taking COCs:

• with age
• in the presence of thromboembolism in relatives (venous thromboembolism in one of the siblings or parents at a relatively young age). If a hereditary predisposition is suspected, it is recommended to refer the woman for consultation with a specialist before making a decision on the appointment of COCs
• for long-term reduced mobility
• with obesity (body mass index > 30 kg / m2). The risk of developing arterial thromboembolic complications increases when taking COCs:
• with age
• in smokers
• with dyslipoproteinemia
• with obesity (body mass index > 30 kg/m2)>
• with hypertension
• with heart defects
• with atrial fibrillation in the presence of thromboembolism in relatives (arterial thromboembolism in one of the siblings or parents at a relatively young age). If you have chronic intestinal inflammation (Crohn’s disease and ulcerative colitis), sickle anemia. When assessing the risk / benefit, keep in mind that adequate treatment of the above diseases can reduce the risk of thrombosis. It is necessary to take into account the increased risk of developing thromboembolic complications in the postpartum period. There is no consensus on whether there is a relationship between superficial venous thrombophlebitis and / or varicose veins and the etiology of venous thromboembolism. When venous or arterial thrombosis develops, the following symptoms may occur::
• leg pain and/or swelling
• , sudden severe chest pain, radiating or without irradiation in the left arm
• , sudden breathlessness and cough without an obvious cause
• unexpected strong long-lasting headache
• partial or complete loss of vision, double vision/speech disorders or aphasia
• dizziness, collapse, in some cases accompanied by focal epileptic attack is a
• sudden weakness or disesthesias (the distortion sensitivity) on one side or in one part of the body
• , movement disorders
• acute abdominal pain.

Women taking COCs should be informed that if they experience symptoms that resemble those of thrombosis, they should consult their healthcare provider. Belara® should be discontinued if a diagnosis of thrombosis is suspected or confirmed. The increased frequency or severity of migraine attacks while taking COCs (which may be a harbinger or symptom of cerebrovascular disease) may be a reason to discontinue them.

Tumors It is noted that the use of COCs is: a risk factor for cervical cancer in women infected with the human papillomavirus (HPV). However, the extent to which other concomitant factors (such as the number of sexual partners or the use of mechanical contraceptives) influence the results of this observation remains controversial (see also “Medical examination”).

There is evidence that the relative risk (RR=1.24) of developing breast cancer in women who take COCs is slightly higher. Within 10 years after stopping taking COCs, the risk level gradually decreases and returns to the age-related level. Since breast cancer is rare in women under the age of 40, there is little difference between the risk of breast cancer among women who are currently and recently taking COCs and the overall risk of developing the disease.

There are reports of rare cases of benign and even rarer cases of malignant liver tumors developing while taking COCs. In some cases, these tumors cause life-threatening intra-abdominal bleeding. In case of severe abdominal pain that does not go away on its own, hepatomegaly, or signs of intra-abdominal bleeding, the possibility of a liver tumor should be taken into account and Belara®should be discontinued.

Other diseases

Many women taking oral contraceptives experience a slight increase in blood pressure; however, clinically significant increases are rare. The relationship between the use of oral contraceptives and the clinical manifestation of hypertension has not yet been confirmed. If a clinically significant increase in blood pressure occurs while taking Belara®, the drug should be discontinued and hypertension should be treated. As soon as the blood pressure values return to normal on the background of antihypertensive therapy, Belara® can be continued.

Women with a history of herpes during pregnancy may have a relapse of the disease while taking COCs. Women with a history of hypertriglyceridemia or a family history of hypertriglyceridemia have an increased risk of developing pancreatitis while taking COCs. Acute or chronic liver function disorders may require discontinuation of COCs until liver function is normalized. Relapse of cholestatic jaundice, which first occurred during pregnancy or previous use of sex hormones, requires the withdrawal of COCs.

COCs may have an effect on peripheral tissue insulin resistance or glucose tolerance. Therefore, diabetic patients should be constantly monitored while taking oral contraceptives. In rare cases, chloasma can develop, especially in women who have had chloasma during pregnancy. Women at risk of developing chloasma should avoid exposure to the sun and ultraviolet radiation while taking oral contraceptives.

Patients with a rare congenital condition such as galactose intolerance, Lapp lactase deficiency, or glucose — galactose malabsorption syndrome should not take this medication.

Medical examination

Before prescribing oral contraceptives, it is necessary to collect complete data on the health of the woman and her relatives in order to identify contraindications (see the section “Contraindications”) and risk factors (see the section “With caution”). The woman must undergo a medical examination.

A medical examination should be performed annually while taking Belara®. Regular medical examination is also necessary due to the fact that diseases that are contraindications (for example, transient ischemic attacks), or risk factors (for example, venous or arterial thrombosis in relatives) may first occur while taking oral contraceptives. A medical examination should include measuring blood pressure, examining the mammary glands, abdomen, internal and external genitalia, taking a swab from the cervix, and performing appropriate laboratory tests.

A woman should be warned that the use of oral contraceptives, including Belara®, does not protect her from infection with HIV (AIDS) or other sexually transmitted diseases.

Insufficient efficiency

Skipping a pill (see section “Dosage and use”, “Skipping the drug”), nausea or symptoms of digestive disorders, including diarrhea, prolonged simultaneous use of certain medications (see section “Use in case of diarrhea, vomiting”, “Interaction with other medications”) or, in very rare cases, metabolic disorders can reduce the effectiveness of contraception.

Effects on the menstrual cycle

Bleeding or “breakthrough” spotting (intermenstrual)

All oral contraceptives can cause irregular vaginal bleeding (breakout bleeding/spotting), especially during the first few cycles of taking the drug. Therefore, a medical examination for irregular cycles should be performed only after the adjustment period, which usually lasts for 3 cycles. If during the use of Belara® the occurrence of extraordinary bleeding continues or appears for the first time in a woman with a regular cycle, it is necessary to conduct an examination to exclude pregnancy or organic pathology; After the exclusion of pregnancy and organic pathology, Belara® can be continued or switched to another drug.

Bleeding that occurs between cycles may be a sign of insufficient contraceptive effectiveness.

No menstrual-like bleeding (withdrawal bleeding)

Withdrawal bleeding usually occurs 21 days after taking the drug. Sometimes, especially in the first few months of taking the drug, withdrawal bleeding may be absent.

However, this is not evidence of an insufficient contraceptive effect. If bleeding does not occur after taking the drug for one cycle, provided that no film-coated tablets were missed, the period after the drug was completed did not exceed 7 days, no other medications were taken at the same time, there was no nausea or diarrhea, fertilization was unlikely to occur, and taking Belara® pregnancy or organic pathology.After excluding pregnancy and organic pathology, Belara® may be continued. If the instructions for taking Belara® were not followed 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 in order to decide whether to continue taking the drug.

At the same time as taking Belara, you should not take herbal medicines containing St. John’s wort (Hypericum perforatum).

Laboratory parameters

Changes in some laboratory parameters may occur while taking COCs, including functional activity of the liver, adrenal glands, and thyroid gland, the level of bound plasma proteins (for example, SHBG (SHBG), lipoproteins), carbohydrate metabolism, coagulation, and fibrinolysis.

The nature and extent of changes are partly determined by the nature and dose of hormones taken.

THE ABILITY TO DRIVE A CAR OR WORK ON PRECISION INSTRUMENTS IS not affected.

Form of production

Film-coated tablets

Storage conditions

store in the original packaging out of the reach of children at a temperature not exceeding 30°C.

Shelf

life is 3 years.

Active ingredient

Ethinyl Estradiol, Chlormadinone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, For women of childbearing age

Indications

Contraception