Belara, 63 pcs., 2 mg+0.03 mg, film-coated tablets

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

A combined contraceptive drug taken orally.

Long-term use of the drug leads to a decrease in the secretion of follicle-stimulating hormone and luteinizing hormone , and, consequently, to suppression of the ovulation process. of the endometrium occurs , preventing the fixation of the fertilized egg. The viscosity of mucous secretions from the cervix increases, which causes difficulty in the passage of male germ cells through the cervical canal and inhibition of their mobility.

Chlormadinone acetate included in the drug is a gestagen with antiandrogenic properties. Its effect is based on the ability to compete with androgens at specific receptors, weakening the effect of androgens . The Pearl index (the probability of getting pregnant in 12 months) ranges from 0.291-0.698 and depends on how carefully the woman follows the medication regimen.

To completely block ovulation, approximately 1.7 mg of chlormadinone daily. The required dosage per cycle is 25 mg.

Pharmacokinetics

Chlormadinone acetate . Quickly and completely absorbed. The maximum concentration occurs in an hour and a half. 95% binds to human blood proteins, mainly albumin.

During the transformation process, many metabolites are formed, the main of which are 3-beta and 3-alpha-hydroxy-chlormadinone acetate.

The average half-life from the blood is 34 hours. Chlormadinone acetate and its metabolites are excreted in approximately equal quantities in the urine and through the intestines.

Ethinyl estradiol. It is quickly and almost completely absorbed from the intestine, reaching maximum concentration in plasma after an hour and a half. Absolute bioavailability is about 40%.

About 98% of the substance binds to blood proteins. Ethinyl estradiol is transformed through hydroxylation of the aromatic ring. The main derivative is 2-hydroxy-ethinyl estradiol.

The average half-life of ethinyl estradiol from the blood is 13 hours. Excreted by the kidneys and feces in a ratio of 2:3.

Compound

Contraindications

The use of the drug is contraindicated in the following diseases:

• the presence of initial signs of thrombophlebitis , thrombosis or symptoms of embolism (including temporary ischemic attacks );
• thrombosis and thromboembolism in progress or in history ( myocardial infarction , pulmonary embolism , venous thrombosis , cerebrovascular changes );
• planned surgical intervention (4 weeks before) and period of immobilization;
• uncontrolled arterial hypertension ;
• acute or chronic severe liver damage (until normalization of liver function);
• uncontrolled diabetes mellitus ;
• predisposition to the appearance of venous and arterial thrombosis : APC resistance , protein S , protein C deficiency, antithrombin 3 , antiphospholipid antibodies and hyperhomocysteinemia ;
• itching of the whole body , cholestasis , especially during a previous pregnancy or use of sex hormones in the past;
• liver tumors , including a history of;
• severe epigastric pain, hepatomegaly or signs of intra-abdominal bleeding ;
• Rotor syndrome, Dubin-Johnson syndrome, slowing of bile flow;
• porphyria in all forms and manifestations;
• hormone-dependent malignant tumors or suspicion of their presence;
• pancreatitis, in combination with severe hypertriglyceridemia ;
• pronounced changes in lipid metabolism;
• migraine attacks ;
• acute sensory disturbances;
• increased frequency of epileptic ;
• movement disorders;
• severe depression ;
• complication of otosclerosis during previous pregnancies;
• endometrial hyperplasia;
• cryptogenic amenorrhea;
• vaginal bleeding of unknown etiology;
• lactation period ;
• pregnancy and suspicion of it;
• addiction to smoking at the age of 35 years;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• the presence of multiple risk factors for arterial or venous thrombosis;
• sensitization to the components of the drug.

It is necessary to prescribe the drug with caution in the presence of the following diseases (including a history):

• multiple sclerosis, epilepsy;
• bronchial asthma;
• convulsive syndrome;
• migraine without neurological symptoms;
• renal or heart failure ;
• uncomplicated diabetes mellitus;
• chorea;
• mild liver diseases;
• dyslipoproteinemia , a disorder of lipid metabolism;
• autoimmune diseases;
• obesity;
• endometriosis;
• controlled arterial hypertension ;
• phlebitis of the superficial veins of the legs, varicose veins ;
• changes in blood clotting;
• uterine fibroids;
• mastopathy;
• herpes during pregnancy ;
• chronic inflammatory bowel diseases;
• depression.

Side effects

• Mental reactions: nervousness, depressed mood, irritability, weakened libido .
• Immune reactions: hypersensitivity to the components of the drug.
• Metabolic reactions: changes in blood fat composition, increased appetite.
• Reactions from the nervous system: migraine pain, dizziness .
• Reactions from the senses: intolerance to contact lenses, conjunctivitis , visual disturbances, hearing loss, tinnitus.
• Reactions from the circulatory system: increased pressure, arterial hypotension, arterial hypertension, varicose veins, collapse, vein thrombosis.
• Reactions from the digestive system: flatulence , nausea, vomiting, abdominal pain, diarrhea .
• Skin reactions: acne, chloasma , pigmentation disorders, hair loss, hyperhidrosis , dry skin, urticaria, erythema, eczema, itching , hypertrichosis , erythema nodosum .
• Reactions from the musculoskeletal system: feeling of heaviness, lumbodynia , muscle disorders.
• Reactions from the genitourinary system: dysmenorrhea , increased vaginal discharge, amenorrhea , lower abdominal pain , breast fibroadenoma , galactorrhea , vaginal candidiasis, menorrhagia, vulvovaginitis, premenstrual syndrome.
• General reactions: swelling , fatigue, weight gain.

The following side effects were also identified when using Belara:

• increased risk of biliary tract diseases;
• increased risk of arterial and venous thromboembolism ;
• increased risk of benign tumors in the liver; , intra-abdominal bleeding may develop ;
• exacerbation of chronic inflammatory bowel diseases.

Pharmacokinetics

KhMA

Suction. When the drug is taken orally, CMA is quickly and completely absorbed.

Tmax CMA - 1–2 hours.

Distribution. More than 95% of CMA binds to human plasma proteins, mainly albumin.

Metabolism. Various processes of reduction, oxidation and binding with glucuronides and sulfates lead to the formation of many metabolites. The main metabolites in blood plasma are 3-alpha and 3-beta-hydroxy-CMA with a half-life not significantly different from unmetabolized CMA. 3-hydroxy metabolites have antiandrogenic activity similar to that of CMA itself. In urine, metabolites are contained mainly in the form of conjugates. After enzymatic cleavage, 2-alpha-hydroxy-CMA becomes the main metabolite, and 3-hydroxy metabolites and dihydroxy metabolites are also formed.

Excretion. The average T1/2 of CMA from blood plasma is approximately 34 hours (after a single dose) and about 36–39 hours (with multiple doses). When taking the drug orally, CMA and its metabolites are excreted in approximately equal proportions by the kidneys and through the intestines.

Ethinyl estradiol (EE)

Suction. When taking the drug orally, EE is quickly and almost completely absorbed.

Tmax in blood plasma is 1.5 hours.

Due to presystemic binding and metabolism in the liver, absolute bioavailability is approximately 40% and is subject to strong individual variability (20–65%).

Distribution. The information available in the literature on the concentration of EE in blood plasma varies greatly. About 98% of EE is bound to plasma proteins, almost exclusively to albumin.

Metabolism. Like natural estrogens, EE is biotransformed through hydroxylation of the aromatic ring (the mediator is the cytochrome P450 system). The main metabolite is 2-hydroxy-EE, which is transformed into other metabolites and conjugates. EE undergoes presystemic binding both in the mucous membrane of the small intestine and in the liver. Mainly glucuronides are found in urine, and sulfates are found in bile and blood plasma.

Excretion. The average T1/2 of EE from blood plasma is approximately 12–14 hours. EE is excreted by the kidneys and through the intestines in a ratio of 2:3. EE sulfate, excreted in bile after hydrolysis by intestinal bacteria, undergoes enterohepatic recirculation.

Belara, instructions for use (Method and dosage)

Instructions for use of Belara prescribe taking birth control pills orally. They should be removed from the blister and swallowed whole, if necessary with a small amount of liquid. The tablets should be taken every day at the same time (preferably in the evening) for 21 days in a row, then you should stop taking them for 7 days; approximately 2-4 days after taking the last tablet, withdrawal bleeding similar to menstrual bleeding develops.

After completing the 7-day break, you must start using the drug from the next pack, regardless of whether the bleeding has stopped.

The first tablet must be taken on the first day of a woman’s physiological cycle (the first day of the next menstruation). In this case, the contraceptive effect begins on the first day of use and lasts during a week-long break in use.

The first tablet can be taken on days 1-5 of menstrual bleeding (whether the bleeding has stopped or not). In this case, during the first seven days of use, you must also use barrier methods of contraception.

If menstrual bleeding appeared more than 5 days ago, it is recommended to wait until the next menstruation begins and then begin the cycle of taking the drug.

Transition from another hormonal contraceptive (combined) to Belara

Switching from products containing 21-22 tablets. It is necessary to finish using all tablets from the previous package. Next, you need to take the first Belara tablet the next day. There should be no break in the use of the pills, and the woman is not advised to have her next menstruation. Additional methods of contraception are not required in this case.

Transition from products containing one gestagen (mini-pill)

In this case, the first Belara tablet should be taken the next day after using the last tablet, which includes only gestagen. During the first seven days, it is also recommended to use barrier methods of contraception.

Switching from hormonal contraceptives, injection or implant

You can start taking Belara on the first day of implant removal or on the first day of the planned injection. During the first seven days, it is recommended to use barrier contraceptive methods.

After an abortion (spontaneous or medical) in the first 3 months of pregnancy

You can start using Belara on the day of the abortion. In this case, you may not need to use additional methods to prevent pregnancy.

After childbirth or abortion (spontaneous or medical) at 3-6 months of pregnancy

It is recommended to start taking Belara in the fourth week after birth, if lactation is not occurring, or after an abortion in the second trimester of pregnancy. In this case, it is not necessary to use additional methods of contraception.

If the use of the drug is started later than the fourth week after childbirth or abortion, it is recommended to use additional methods of contraception during the first week.

If you have already had sexual intercourse, it is advisable to exclude pregnancy or wait until the next menstrual cycle before taking the drug.

If a woman forgot to take the pill, but took it 12 hours later, the contraceptive effect may be weakened.

If you miss a pill, you must follow the rules below:

• Do not stop taking the medication for more than a week;
• 7 days of continuous medication is necessary to achieve reliable suppression of the regulation of the hypothalamic-pituitary-ovarian system.

It is advisable to take a missed tablet immediately, even if this means that you need to take two tablets at a time. Then follow the standard scheme. Over the next week, it is necessary to use barrier methods of contraception.

If there are less than seven tablets left in a pack, immediately after finishing taking tablets from this pack, you must start taking tablets from a new pack - there should be no break between packs. Withdrawal bleeding will usually not occur until all the tablets in the second pack have been used, but exceptions may occur. If withdrawal bleeding does not appear after the end of the cycle of taking the second package, then you need to perform a pregnancy test .

Pharmacodynamics

Long-term use of the drug Belara® leads to a decrease in the secretion of FSH and LH and, consequently, suppression of ovulation. At the same time, proliferation of the endometrium and its secretory transformation occur, preventing the implantation of a fertilized egg, the viscosity of the mucous secretion of the cervix increases, which is accompanied by difficulty in the passage of sperm through the cervical canal and a violation of their motility.

To completely suppress ovulation, 1.7 mg of chlormadinone acetate (CMA) is required daily. The required dose per cycle is 25 mg.

The composition of the drug Belara® XMA is a gestagen with antiandrogenic properties. Its action is based on the ability to replace androgens on specific receptors, eliminating and weakening the effect of endogenous and exogenous androgens. The Pearl index is 0.291–0.698, depending on how carefully the woman follows the drug regimen.

Interaction

The following substances may lower the concentration of ethinyl estradiol in the blood and reduce contraceptive activity:

• all medications that increase intestinal motility or inhibit absorption;
• substances that activate microsomal liver enzymes , such as Rifabutin, Rifampicin, barbiturates, Griseofulvin, anticonvulsants, Barbexaclone, Modafinil, protease inhibitors, Primidone St. John's wort preparations ;
• a number of antibiotics (for example, Tetracycline , Ampicillin ).

When using such drugs simultaneously, it is necessary to use additional barrier methods of contraception during therapy and for a week after it. When taking substances that lower the concentration of ethinyl estradiol in the blood due to the activation of microsomal liver enzymes, additional barrier methods should be used within four weeks after the end of therapy.

The following substances may increase the concentration of ethinyl estradiol in the blood:

• substances that inhibit the sulfation of ethinyl estradiol in the intestine ( A scorbic acid , P -acetamol );
• substances that block the activity of microsomal liver enzymes ( antifungal imidazoles, indinavir, troleandomycin );
• atorvastatin.

Use during pregnancy and breastfeeding

The use of Belara® during pregnancy is contraindicated. Before you start using it, you must rule out pregnancy. If pregnancy occurs while taking Belara®, it should be stopped immediately. Existing epidemiological data do not contain information about the development of teratogenic or embryotoxic effects in women who accidentally took during pregnancy drugs containing estrogens and gestagens in the same combination as in Belara®.

It is contraindicated to use Belara® during breastfeeding, since the drug reduces the amount of milk produced and changes its composition. Small amounts of the hormones included in the contraceptive and/or their metabolites are excreted in breast milk and may affect the baby.

Analogs

Level 4 ATC code matches:
Ovidon

Rigevidon

Non-Ovlon

Mercilon

Yarina Plus

Yarina

Miniziston 20 fem

Novinet

Microgynon

Janine

Lindineth

Cyclo-Proginova

Regulon

Logest

Midiana

Femoden

Jess Plus

Jess

Zoely

Analogs of Belara: Vidora, Vidora Micro, Dayla, Darilia, Jess, Jess Plus, Difenda, Evra, Janine, Jastinda, Lindinet 20, Lindinet 30, Logest, Marvelon, Mercilon, Midiana, Milanda, Modell Anti, Modell Tin, Naadin, Novinet , Regulon, Rigevidon 21 +7, Silest, Simitsia, Femoden, Yarina, Yarina Plus.

Belara price, where to buy

The price of Belara in Russian pharmacies (21 tablets per package) is 491-536 rubles. The price of tablets No. 63 starts from 710 rubles.

Buying similar contraceptive pills No. 21 in Ukraine will cost 250-650 hryvnia, and the minimum cost of package No. 61 will be 910 hryvnia.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Belara tablets 21 pcs. Grunenthal GmbH/Gedeon Richter OJSC
  RUB 775 order
• Belara tablets 63 pcs. Grunenthal GmbH/Gedeon Richter OJSC

  RUB 1,979 order

Pharmacy Dialogue

• Belara (tab. No. 21)Gedeon-Richter

  810 rub. order

• Belara (tab.p/v. No. 21x3)Gedeon-Richter

  RUB 1,982 order

• Belara (table no. 21x3)Grunenthal GmbH

  RUB 2,302 order

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Pharmacy24

• Belara No. 21 tablets VAT "Gedeon Richter", Ugorshchina
  279 UAH. order

PaniPharmacy

• Belara tablets Belara tablets. No. 21 Hungary, Gedeon Richter

  290 UAH. order

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