Belara, 2 mg+0.03 mg 21 pcs

Pharmacodynamics:

Prolonged (more than 21 days) use of BELARA leads to decreased 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 cervical mucus change, which is accompanied by difficulty in the passage of sperm through the cervical canal and impaired sperm motility.

The component of BELARA, chlormadinone acetate, is a progestagen with anti-androgenic properties. Its action is based on the ability to replace androgens at specific receptors, eliminating and weakening the effect of endogenous and exogenous androgens. It takes 1.7 mg of chlormadinone acetate daily to completely suppress ovulation. The required dose per cycle is 25 mg.

The other active ingredient in BELARA, ethinylestradiol, inhibits the secretion of skin sweat glands. It also significantly increases the production of globulin binding sex hormones, thereby reducing the amount of free testosterone in the blood plasma.

Interacts with specialized estrogen receptors in the target organs (in the fallopian tubes, cervix, vagina, external genitalia, mammary ducts) and causes endometrial proliferation.

In addition to its reliable contraceptive properties, the positive effects of BELARA may be observed in menstrual cycle normalization, reduction of premenstrual syndrome, incidence of iron deficiency anemia, dysmenorrhea, functional ovarian cysts, ectopic pregnancy, endometrial and ovarian malignancies, certain forms of benign breast diseases and pelvic inflammatory diseases.

Pharmacokinetics

Chlormadinone acetate and ethinylestradiol are quickly and completely absorbed when the drug is taken orally. The maximum concentration of ethinylestradiol is reached after 1.5 hours. The maximum concentration of chlormadinone acetate is reached in 1-2 hours.

The elimination half-life of chloradinone acetate is approximately 34-39 h, of ethinylestradiol 12-14 h. Chlormadinone acetate metabolites are excreted by the kidneys and through the intestine in the ratio of 2:3.

The elimination half-life of ethinylestradiol is approximately 12-14 h.

The metabolites of ethinylestradiol are water-soluble sulfate or glucuron conjugation derivatives.

Ethinylestradiol metabolites are excreted by the kidneys and through the intestine at a ratio of 4:6.

Indications

Contraception

Oral contraception.

Composition

One film-coated tablet contains

active ingredients:

chlormadinone acetate 2 mg and ethinylestradiol 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 jacket:

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,

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

How to take, the dosage

Belara pills are started on day 1 of your menstrual cycle and continued daily (preferably at the same time) for 21 days. Then take a 7-day break, during which time menstrual bleeding should start. After the 7-day break, you should resume taking the drug from the next blister, whether or not the menstrual-like bleeding has stopped.

If hormonal contraceptives were not used during the preceding menstrual cycle, the pills should be started on the first day of the normal menstrual cycle (the first day of menstruation). The contraceptive effect begins on the first day of taking the pill. If your period lasts more than one day, you should take the first pill on the 5th day of your period, regardless of whether bleeding has stopped or not. In this case, you should use additional, non-hormonal methods of contraception for the first 7 days. If more than 5 days have passed since the beginning of menstruation, it is recommended that the woman start taking the drug from the next menstrual cycle.

If you switch from another hormonal contraceptive with 21 active pills, you should finish taking all pills of the old package. The first pill of Belara should be taken the next day. There should be no interruption in taking the pills; the patient should not wait for the next menstrual cycle.

If you are switching from another hormonal contraceptive with 28 pills, the first Belara pill should be taken the day after taking the last active pill from the previous contraceptive package (that is, after taking 21 active pills). There should be no interruption in taking the pills; the patient should not wait for the next menstrual cycle.

When switching from contraceptives containing only gestagen (mini-pills), a woman may start taking Belara any day (without a break); when switching from the use of an implant containing gestagen, on the day it is removed; when switching from gestagens in injectable form, from the day when the next injection should have been made. In all cases, additional barrier methods of contraception should be used 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 necessary.

After childbirth, women who are not breastfeeding can start Belara on day 21-28 of the postpartum period. No additional contraceptive measures should be taken in this case. If the use of the drug in the postpartum period is started 28 days after delivery, additional contraceptive measures should be taken for 7 days. If a woman has had sexual intercourse, it is necessary to rule out pregnancy and wait for the next menstrual cycle before starting the use of the drug.

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

If more than 12 hours have elapsed since the prescribed time, the contraceptive effect of the drug may decrease. It is necessary to take the missed pill immediately and continue taking the drug at the usual time. It is necessary to use additional barrier methods of contraception for the next 7 days. If during these 7 days the pills in the package ran out, you should start taking pills from the next package immediately after completing the pills in the previous package, i.e. there is no break between the intake of pills from different packages. If there was no menstrual bleeding after taking the second package, pregnancy should be ruled out.

If vomiting or diarrhea occurs while taking Belara tablets, additional contraceptive methods are recommended because the contraceptive effect of the drug may be reduced due to incomplete absorption of its active ingredients in the intestine.
Tablets should be swallowed whole, selecting the tablet that is marked with the corresponding day of the week. The direction of the arrow on the package determines the choice of tablets.

Interaction

The interaction of ethinylestradiol, the estrogenic component of BELARA®, with other medicinal products may increase or decrease serum concentrations of ethinylestradiol. If long-term treatment with these drugs is necessary, you should switch to non-hormonal contraception.

Decreased serum ethinylestradiol concentrations may increase the frequency of breakthrough bleeding episodes, disrupt the cycle, and decrease the contraceptive efficacy of BELARA®. Increased serum ethinylestradiol concentrations may increase the frequency and severity of side effects.

The following drugs/active ingredients may decrease serum ethinylestradiol concentrations:
– all drugs that increase gastrointestinal motility (e.g., metoclopramide) or impair adsorption (e.g., activated charcoal);

– Active agents that induce microsomal liver enzymes, such as rifampicin, rifabutin, barbiturates, antiepileptics (e.g., carbamazepine, oxcarbazepine, phenytoin and topiramate) anticonvulsant felbamate, phenylbutazone, griseofulvin, barbecsalone, primidone, modafinil, some protease inhibitors (e.g., ritonavir) and St John’s wort preparations;

– some antibiotics (e.g., ampicillin, tetracycline, rifampicin) – due to decreased enterohepatic circulation of estrogen.
When concomitant use of such drugs/active substances with BELARA® tablets, additional barrier methods of contraception should be used both during treatment and within 7 days after it. If active agents that reduce the concentration of ethinylestradiol in blood serum by induction of hepatic microsomal enzymes are taken, additional barrier methods (condom, spermicides) should be used for 28 days after the end of treatment.

The following drugs/active substances may increase the serum concentration of ethinylestradiol:

– active agents that inhibit ethinylestradiol sulfation in the intestinal wall, such as ascorbic acid or paracetamol;
– atorvastatin;
– agents that inhibit hepatic microsomal enzyme activity, such as antifungal imidazoles (such as fluconazole), indinavir or troleandomycin.

Ethinylestradiol can affect the metabolism of other substances:

-inhibit the activity of hepatic microsomal enzymes and therefore increase the serum concentrations of active substances such as diazepam (and other benzodiazepines metabolized through hydroxylation), cyclosporine, theophylline and prednisolone;
– induce glucuronidation in the liver and, accordingly, reduce serum concentrations of, for example, clofibrate, paracetamol, morphine and lorazepam.

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

Special Instructions

Smoking increases the risk of serious cardiovascular side effects of PDA, the risk increases with age and according to the number of cigarettes smoked and is more pronounced in women over the age of 35, women who smoke over 35 should use other methods of contraception.

The risk of serious conditions such as myocardial infarction, thrombosis/thromboembolism, stroke, and liver neoplasms increases with use of PDA.

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

If any of the above diseases/risk factors are present, the possible benefits of prescribing Belara® versus risks should be weighed, and this should be discussed with the woman before she starts taking the drug. If these diseases or risk factors start to appear or progress while taking this drug, you should contact your doctor.

The doctor must decide if the drug should be stopped.

Thromboemboli and other vascular disease

It has been noted that there is an association between taking PDA and an increased risk of diseases caused by venous or arterial thromboembolism, such as myocardial infarction, cerebral stroke, deep vein thrombosis, or pulmonary embolism. These complications are rare.

PDA administration leads to an increased risk of venous thromboembolism (VTE). The risk of VTE is greatest during the first year of use. This risk is less than in pregnancy, where the rate of VTE is 60 per 100,000 pregnancies. VTE is fatal in 1-2% of cases. There are no data to assess the risk of VTE when taking Belara® compared to other PDAs.
The risk of venous thromboembolic complications increases when taking PDAs:

• with age
• when a relative has thromboembolism (venous thromboembolism in a sibling or parent at a relatively young age). If a hereditary predisposition is suspected, it is advisable to refer the woman to a specialist for consultation before deciding to prescribe CPC
• with prolonged reduced mobility
• with obesity (body mass index > 30 kg/m2).
  The risk of arterial thromboembolic complications increases with PDA administration:
• with age
• in smokers
• in dyslipoproteinemia
• in hypertension
• in heart disease
• in heart defects
• in atrial fibrillation
  in the presence of thromboemboli in relatives (arterial thromboembolism in one sibling or parent at a relatively young age). If chronic intestinal inflammation (Crohn’s disease and ulcerative colitis), sickle cell anemia. In the risk/benefit assessment, it should be remembered that adequate treatment of the above diseases may reduce the risk of thrombosis. The increased risk of thromboembolic complications in the postpartum period should be taken into account.
  There is no consensus on whether there is a relationship between superficial venous thrombophlebitis and/or varicose veins and the etiology of venous thromboembolisms.
  If venous or arterial thrombosis develops, the following symptoms may occur:
• pain in the legs and/or edema
• sudden severe chest pain, with or without irrigation to the left arm
• sudden shortness of breath, cough for no apparent reason sudden severe prolonged headache
• partial or total loss of vision, diplopia/speech impairment or aphasia
• dizziness, collapse, in some cases accompanied by a focal epileptic seizure
• motion disorders
• acute abdominal pain.

Women taking PDA should be informed that if symptoms resemble those of thrombosis occur, they should see their doctor. Belara® should be stopped if thrombosis is suspected or confirmed.
An increase in the frequency or severity of migraine attacks while taking CRPs (which may be a precursor or symptom of cerebrovascular disease) may be a reason to stop them.

Tumors
It has been noted that PDA use is: a risk factor for cervical cancer in women infected with human papillomavirus (HPV). However, the extent to which other concomitant factors (e.g., number of sexual partners or use of mechanical contraceptives) influence the results of this observation remains debatable (see also Health Check).

There is evidence that the relative risk (RR=1.24) of developing breast cancer is slightly higher in women who take the PDA. Within 10 years of stopping taking PDAs, the risk level gradually decreases and returns to age-related risk. Because breast cancer is rare in women under age 40, there is little difference between the risk of breast cancer in women currently taking and recently taking CRP 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 CRP. In some cases, these tumors have caused life-threatening intra-abdominal bleeding. If severe abdominal pain does not resolve on its own, hepatomegaly, or signs of intra-abdominal bleeding occur, the possibility of a liver tumor should be considered, and Belarus® should be stopped.

Other conditions

Many women taking oral contraceptives experience mild increases in blood pressure; however, clinically significant increases are rare. The relationship between oral contraceptive use 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 the hypertension should be treated. As soon as blood pressure values return to normal on hypotensive therapy, Belara® can be continued.

In women with a history of herpes in pregnancy, there may be a relapse of the disease while taking CRPS. In women with a history of hypertriglyceridemia or such a family history increases the risk of pancreatitis while taking CRP. Acute or chronic liver dysfunction may require withdrawal of CRP until liver function normalizes. Relapse of cholestatic jaundice that first occurred during, pregnancy, or previous use of sex hormones requires discontinuation of CRP.

CTCs may have an effect on peripheral tissue insulin resistance or glucose tolerance.
Therefore, diabetic patients should be kept under constant observation while taking oral contraceptives.
In rare cases, chloasma may develop, especially in women who have had pregnancy chloasma. Women at risk of developing chloasma should avoid sun exposure and ultraviolet radiation while taking oral contraceptives.

Patients with the rare congenital pathology of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption syndrome should not take this medication.

Medical screening

Preferral for oral contraceptives requires complete health information for the woman and her family to identify contraindications (see Contraindications) and risk factors (see Caution). The woman should undergo a medical exam.

Medical check-ups should be performed annually while taking Belara®. Regular medical check-ups are also necessary because conditions that are contraindications (such as transient ischemic attacks) or risk factors (such as venous or arterial thrombosis in relatives) may first occur while taking oral contraceptives. The physical examination should include blood pressure, breast, abdominal, internal and external genital exams, cervical smears, and appropriate laboratory tests.

Women should be warned that the prescription of oral contraceptives, including Belara®, does not protect them from HIV infection (AIDS) or other sexually transmitted diseases.

Lack of efficacy

Missing the pill (see “Dosage and administration,” “Skipping the pill”), nausea or digestive symptoms, including diarrhea, prolonged concomitant use of certain medications (see “Use for diarrhea,” “Skip the medicine” section).

In the case of diarrhea, vomiting, and interactions with other medications

In very rare cases, metabolic disturbances may decrease the effectiveness of contraception.

The effect on the menstrual cycle

Bleeding or bleeding “breakthrough” (intermenstrual)

All oral contraceptives can cause irregular vaginal bleeding (bleeding/burst bleeding), especially during the first few cycles of the pill. Therefore, medical examinations for irregular cycles should be performed only after a period of adjustment, which usually lasts for 3 cycles. If unscheduled bleeding continues or occurs for the first time while taking Belar® in a woman with a regular cycle, an examination to rule out pregnancy or organic pathology should be performed; Once pregnancy and organic pathology are ruled out, Belar® may be continued or switched to another medication.

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

Lack of menstrual-like bleeding (bleeding withdrawal)

At 21 days after taking the drug, bleeding withdrawal usually occurs. Sometimes, especially in the first few months of taking the drug, there may be no bleeding of withdrawal.

This, however, is not an indication of insufficient contraceptive effect. If bleeding does not occur after taking the medication for one cycle, provided no bleeding has been missed, the period after completion of taking the film-coated pill has not exceeded 7 days, no other medications have been taken simultaneously, no nausea or diarrhea has occurred, fertilization is unlikely, and taking Belara® is not pregnant or organic pathology. Once pregnancy and organic pathology have been ruled out, taking Belara® may be continued. If instructions were not followed while taking Belara® before the first absence of bleeding withdrawal, or if bleeding withdrawal was absent for two consecutive cycles, pregnancy must be ruled out to decide whether to continue taking the drug.

A herbal medicines containing St. John’s wort (Hypericum perforatum) should not be taken at the same time as Belara.

Laboratory measures

There may be changes in some laboratory parameters while taking CRP, including liver, adrenal, and thyroid function, plasma levels of bound proteins (e.g., SHBG (hBG), lipoproteins), carbohydrate metabolism, coagulation, and fibrinolysis.

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

Impact on the ability to drive a car or operate precision instruments
Not affected.

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Contraindications

Combined oral contraception (COC) is contraindicated in the following cases. You should stop taking Belara immediately if any of the following symptoms occur:

• present or history of thrombosis (venous and arterial) (e.g., deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke);
• Planning surgery (at least 4 weeks prior) and period of immobilization, such as after trauma (including plaster casts).
• diabetes mellitus with vascular complications
• diabetes mellitus not adequately controlled
• uncontrolled hypertension or significant elevation of blood pressure (greater than 140/90 mmHg),
• Uncontrolled hypertension or significant elevation of blood pressure (>140/90 mmHg, see
• Special considerations

. Hereditary or acquired predisposition to venous or arterial thrombosis, such as increased resistance to activated protein C (APC resistance);

• antithrombin III deficiency, C-protein deficiency, S-protein deficiency, hyperhomocysteinemia and antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant);
• generalized pruritus, cholestasis, especially during previous pregnancy or estrogen therapy;
• Dubin-Johnson syndrome, Rotor syndrome; conditions/diseases accompanied by impaired bile flow;
• current or history of liver tumors;
• explicit epigastric pain, liver enlargement, or symptoms of intra-abdominal bleeding (see
• existence or recurrence of porphyria (all three forms, especially acquired porphyria);
• hormone-dependent malignancies, including a history (e.g., breast or uterus) or suspected malignancies;
• pancreatitis present or in the history, in combination with severe forms of hypertriglyceridemia;
• first attacks of migraine pain or frequent severe headaches;
• migraine in combination with local neurological symptoms (associated migraine);
• acute sensory disturbances, such as visual or hearing impairment;
• motor disturbances (especially paresis);
• aggravation of the course of epilepsy;
• severe depression;
• autosclerosis during previous pregnancies;
• amenorrhea of unclear etiology;
• endometrial hyperplasia;
• blooding from the vagina of unknown etiology;
• high sensitivity to the components of the drug;
• pregnancy or suspected pregnancy;
• breast-feeding period;
• smoking over 35 years of age (see
• Specific directions.

WARNING
The use of estrogen/progestagen combination may have adverse effects on the course of some diseases/conditions.
Special medical monitoring is required for the following conditions: epilepsy, multiple sclerosis; seizures (tetany); migraine; bronchial asthma; cardiac or renal insufficiency; minor chorea; uncomplicated diabetes mellitus (see also Contraindications); liver disease (see also Contraindications). also section “Contraindications”); lipid metabolism disorders, dyslipoproteinemia (see also section “Contraindications”); autoimmune diseases (including systemic lupus erythematosus); obesity; arterial hypertension (see also section “Contraindications”); endometriosis; varicose veins; phlebitis (see also section “Contraindications”). also section “Contraindications”); clotting disorders; mastopathy; uterine myoma; herpes pregnancy; depression (see also section “Contraindications”); chronic inflammatory bowel disease (Crohn’s disease, nonspecific ulcerative colitis).

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Side effects

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

Immune system.
Infrequent: hypersensitivity to the components of the drug including allergic skin reactions.

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

Psycho-emotional sphere.
Often: depression, nervousness, irritability.
Infrequent: decreased libido.

Nervous system.
Often: dizziness, migraine (and/or its aggravation).

Visual organs.
Often: visual disorders.
Rarely: conjunctivitis, intolerance of contact lenses.

Hearing organs and vestibular system.
Rarely: sudden hearing loss, tinnitus.

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

The digestive system.
Very common: nausea.
Frequent: vomiting.
Infrequent: abdominal pain, flatulence, diarrhea.

Skin and subcutaneous tissue.
Often: acne.
Infrequent: pigmentation disorders, chloasma, hair loss, dry skin, hyperhidrosis.
Rare: urticaria, eczema, erythema, skin itching, psoriasis aggravation, hypertrichosis.
Very rare: erythema nodosum.

Musculoskeletal system.
Often: feeling of heaviness.
Infrequent: back pain, muscle disorders.

Reproductive system and mammary glands.
Very Frequent: increased mucous vaginal discharge, dysmenorrhea, amenorrhea.
Frequent: lower abdominal pain.
Infrequent: galactorrhea, breast fibroadenoma, vaginal candidiasis.
Rare: breast enlargement, vulvovaginitis, menorrhea, premenstrual syndrome.

General disorders.
Often: fatigue, edema, weight gain.

The following adverse effects have also been reported with combined oral contraceptives (OCPs), including those containing 0.03 mg of ethinylestradiol and 2 mg of chlormadinone acetate:

– Increased risk of venous and arterial thromboembolism (e.g., venous thrombosis, pulmonary embolism, stroke, myocardial infarction). The risk may be increased by additional factors, see section “Cautions”.
– increased risk of biliary tract disease,
– in rare cases an increased risk of benign liver neoplasms (and even more rarely – malignant liver neoplasms) and single cases may lead to life-threatening intra-abdominal bleeding (see also “Special Indications”).
– exacerbation of chronic inflammatory bowel diseases (Crohn’s disease, ulcerative colitis).

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Overdose

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

If a large number of pills are taken accidentally, nausea, vomiting, bloody discharge/vaginal bleeding may occur.

There is no specific antidote.

The treatment is symptomatic.

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

Pregnancy use

Pregnancy: Use of Belara is contraindicated during pregnancy. Before you start using Belara, you should rule out the presence of pregnancy.

If you become pregnant while taking Belara, stop taking it immediately. The data available to date contain no information on the development of teratogenic or embryotoxic effects in women who have accidentally taken preparations containing estrogens and progesterones in the same combination as Belara during pregnancy.

Lactation: Belara is not recommended during breastfeeding because it 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 with breast milk and may affect a breast-fed baby.