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

Compound

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.

Negative effects of alcohol

Exceeding the ethanol dose of 20 mg per day leads to a negative effect on the body:

• increased functional load on the liver;
• negative effect on blood vessels with their expansion and subsequent narrowing;
• toxic effects on the structures of the central and peripheral nervous system;
• mood suppression;
• increased secretion of adrenal hormones, which include glucocorticosteroids;
• development of physical and psychological dependence.

Taking large amounts of alcohol has a pronounced effect on the processes of absorption, distribution in tissues, as well as subsequent metabolism and excretion of drugs.

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.

Contraindications

Taking Belara® is contraindicated for the following diseases/conditions:

hypersensitivity to the components of the drug;

the presence of thrombosis (venous and arterial) currently or in history (for example, deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke);

the presence of the first signs of thrombosis, thrombophlebitis or symptoms of embolism (for example, transient ischemic attacks, angina pectoris, see “Special Instructions”);

planned surgical intervention (at least 4 weeks before it) and a period of immobilization, for example after injury (including after applying plaster casts);

diabetes mellitus with vascular complications;

diabetes mellitus that is not adequately controlled;

uncontrolled hypertension or a significant increase in blood pressure (over 140/90 mm Hg, see “Special Instructions”);

hereditary or acquired predisposition to the development of venous or arterial thrombosis, such as increased body resistance to activated protein C (APC resistance); antithrombin III deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinemia and antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant);

acute or chronic severe liver diseases (until normalization of liver function indicators);

generalized itching, cholestasis, especially during a previous pregnancy or a history of taking sex hormones;

Dubin-Johnson syndrome, Rotor syndrome; violation of the outflow of bile;

the presence of liver tumors currently or in history;

severe epigastric pain, liver enlargement or symptoms of intra-abdominal bleeding;

newly diagnosed porphyria or its relapse (all three forms, especially acquired porphyria);

the presence of hormone-dependent malignant diseases, incl. history (for example, breast or uterus) or suspicion of them;

severe disorders of lipid metabolism;

pancreatitis currently or in history, in combination with severe forms of hypertriglyceridemia;

new attacks of migraine pain or frequent severe headaches;

migraine in combination with local neurological symptoms (associated migraine);

acute sensory impairment, such as visual or hearing impairment;

motor disorders (in particular paresis);

an increase in the number of epileptic attacks;

severe depression;

worsening otosclerosis during previous pregnancies;

amenorrhea of ​​unknown etiology;

endometrial hyperplasia;

bleeding from the vagina of unknown etiology;

smoking over the age of 35 (see “Special Instructions”);

lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

the presence of pronounced or multiple factors of arterial or venous thrombosis (increasing age, smoking, especially over the age of 35 years, obesity (<30 kg/m2); dyslipoproteinemia; a family history of venous or arterial insufficiency in 1st degree relatives; diseases heart valves; atrial fibrillation; bacterial endocarditis; any surgery on the lower extremities; major trauma).

pregnancy or suspicion of it;

breastfeeding period.

With caution: If you have the following conditions/diseases/risk factors, currently or in history, the use of Belara® requires careful medical supervision and assessment of the potential risk and expected benefit: epilepsy; multiple sclerosis; convulsive syndrome (tetany); migraine (without focal neurological symptoms); bronchial asthma; heart or kidney failure; chorea; uncomplicated diabetes mellitus; acute and chronic liver diseases of mild and moderate severity (with normal liver function tests); lipid metabolism disorders, dyslipoproteinemia (see also “Contraindications”); autoimmune diseases (including systemic lupus erythematosus); obesity (<30 kg/m2); controlled arterial hypertension; endometriosis; varicose veins, phlebitis of the superficial veins of the lower extremities (see also “Contraindications”); blood coagulation disorder; mastopathy; uterine fibroids; herpes during pregnancy; depression (see also “Contraindications”); chronic inflammatory bowel diseases (Crohn's disease, ulcerative colitis).

Why is alcohol prohibited?

Purely theoretically, the compatibility of alcohol and pills is beyond doubt. Both substances are absorbed, processed and excreted independently of each other, and the only organ on which they have the same effect is the liver.

The liver is required to perform a double load, driving blood through itself and simultaneously cleansing it of both drug components and alcohol processing products. And since one of the effects of oral contraceptives (OCs) is to increase and increase the duration of the effects of alcohol on the body, because of this, one can expect an increase in the need for maximum liver performance.

Drinking contraceptives (Belara or Jess) with alcohol is also not recommended because the effect of ethyl alcohol on the pills could potentially affect their effectiveness. And not only because of the toxicity of the ethanol components, but also because of the possibility of vomiting if the permissible dose of alcohol is exceeded, during which the body will also get rid of the medicine that has not had time to be absorbed.

Alcohol in combination with oral contraceptives (OCs) may increase the side effects of the medication, especially in the first month of taking contraceptives. While the work of internal organs is undergoing restructuring in a well-established process, alcohol entering the bloodstream can provoke increased headaches and nausea.

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.

Positive effects of drinking alcohol

Drinking a small amount of alcohol has several positive effects:

• feeling of euphoria;
• reducing feelings of tension;
• increasing a person’s sociability;
• improvement of metabolic processes in liver cells;
• positive effect on the condition of blood vessels.

The positive effects of alcohol are possible only if you consume a small amount, which does not exceed 20 mg per day.

Side effects

When taking Belara®, the most common adverse reactions (>20% of cases) are breakthrough bleeding, spotting from the vagina, headache and discomfort in the mammary glands. Intermenstrual bleeding usually decreases as the duration of taking Belara® increases.

The frequency of occurrence of adverse reactions is determined as follows: very often - ≥1/10; often - ≥1/100, <1/10; uncommon - ≥1/1000, <1/100; rarely - ≥1/10,000, <1/1000; very rarely - <1/10,000.

Adverse reactions from the following organs and systems may occur.

From the immune system: rarely - hypersensitivity to the components of the drug, including allergic reactions from the skin.

Metabolism and nutrition: rarely - increased appetite.

Mental disorders: often - depressed mood, nervousness, irritability.

From the nervous system: often - dizziness, migraine (and/or its intensification).

From the organs of vision: often - visual disturbances; rarely - conjunctivitis, intolerance to contact lenses.

From the organ of hearing and labyrinthine disorders: rarely - sudden hearing loss, tinnitus.

From the cardiovascular system: rarely - increased blood pressure, arterial hypotension, cardiovascular collapse, varicose veins, vein thrombosis.

From the gastrointestinal tract: very often - nausea; often - vomiting; infrequently - abdominal pain, flatulence, diarrhea.

From the skin and subcutaneous tissues: often - acne; uncommon - pigmentation disorders, chloasma, hair loss, dry skin; rarely - urticaria, eczema, erythema, skin itching, increased psoriasis, hypertrichosis; very rarely - erythema nodosum.

From the musculoskeletal and connective tissue side: often - a feeling of heaviness in the lower extremities; Uncommon: back pain, muscle disorders.

From the genital organs and mammary gland: very often - increased vaginal discharge, painful menstrual-like bleeding from the vagina, absence of menstrual-like bleeding; often - pain in the lower abdomen; uncommon - galactorrhea, breast fibroadenoma, vaginal candidiasis; rarely - breast enlargement, vulvovaginitis, menorrhagia, premenstrual-like syndrome.

General disorders and disorders at the injection site: often - fatigue, swelling, weight gain; uncommon - decreased libido, hyperhidrosis; rarely - increased appetite.

Impact on the results of laboratory and instrumental examinations: infrequently - changes in lipid levels in the blood plasma, including hypertriglyceridemia.

When using combined oral contraceptives (COCs), including those containing 0.03 mg EE and 2 mg CMA, 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 “Special Instructions”);

- increased risk of biliary tract diseases;

- in rare cases - an increased risk of developing benign liver tumors (and even less often - malignant liver tumors); 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, see also “Special Instructions”).

How do birth control pills work?

Oral contraceptives, or contraceptives, come in the form of tablets or capsules for oral use.
As active ingredients, they contain compounds that are similar to the hormones progesterone and estrogens. The mechanism of action is to suppress the ovulation process, which is the release of a mature egg from the follicle into the lumen of the fallopian tube. In this case, fertilization will be impossible. During the use of contraceptives, the development of negative reactions is possible:

• weight gain;
• swelling of soft tissues;
• thrombosis of the veins of the extremities;
• the appearance of bleeding not associated with the menstrual cycle;
• decreased sexual desire;
• development of acne and other skin changes.

The likelihood of negative reactions is less when using modern combined oral contraceptives. It increases in the case of simultaneous systematic consumption of alcohol.

Interaction

The interaction of EE, the estrogenic component of Belar®, with other drugs may cause an increase or decrease in the concentration of ethinyl estradiol in the blood serum. If long-term treatment with these medications is necessary, you should switch to non-hormonal contraception. A decrease in the concentration of EE in the blood serum can lead to more frequent episodes of breakthrough bleeding, cycle disruption and a decrease in the contraceptive effectiveness of Belara®. Increasing serum EE concentrations may increase the frequency and severity of side effects.

The following drugs/active substances can reduce the concentration of EE in the blood serum:

- all drugs that increase gastrointestinal motility (for example, metoclopramide) or impair absorption (for example, activated charcoal);

- substances that induce liver microsomal enzymes, such as rifampicin, rifabutin, barbiturates, anticonvulsants (for example, carbamazepine, phenytoin or topiramate), griseofulvin, barbexaclone, primidone, modafinil, some protease inhibitors (for example, ritonavir) and St. John's wort preparations;

- some antibiotics (eg ampicillin, tetracycline) in some women, possibly due to a decrease in enterohepatic recirculation of estrogens.

When using such drugs/active substances simultaneously with Belara®, it is necessary to use additional barrier methods of contraception, both during treatment and for 7 days after it. When taking active substances that reduce the concentration of EE in the blood plasma due to the induction of microsomal liver enzymes, additional barrier methods should be used within 28 days after the end of treatment.

If taking a concomitant drug needs to be continued after the end of the tablets in the Belara® package, then you should start taking the tablets from the next package without taking the usual 7-day break.

The following drugs/active substances can increase the concentration of EE in the blood serum:

- active substances that suppress sulfation of EE in the intestinal wall (for example, ascorbic acid or paracetamol);

— atorvastatin (increases the AUC of EE by 20%);

- active substances that inhibit the activity of microsomal liver enzymes, such as imidazole-derived antifungals (for example fluconazole), indinavir or troleandomycin.

EE may affect the metabolism of other substances:

- suppress the activity of hepatic microsomal enzymes and, accordingly, increase the concentration in the blood serum of such active substances as diazepam (and other benzodiazepines, the metabolism of which is carried out through hydroxylation), cyclosporine, theophylline and prednisolone;

- induce glucuronidation in the liver and, accordingly, reduce the concentration in the blood serum of substances such as clofibrate, paracetamol, morphine and lorazepam.

While taking Belara®, the need for insulin and oral hypoglycemic drugs may change, because the drug affects glucose tolerance.

This may also apply to medications that were taken shortly before taking Belara®.

Before prescribing any drug, you should study its summary characteristics to identify possible interactions with Belara®.

Directions for use and doses

Inside. The tablets marked with the corresponding day of the week should be removed from the blister pack and swallowed whole, with a small amount of water if necessary. One tablet should be taken every day at the same time (preferably in the evening) for 21 days in a row, then a 7-day break from taking the tablets should be taken; two to four days after taking the last tablet, withdrawal bleeding will occur, similar to menstrual bleeding.

After the end of the 7-day break, you should start taking Belara® from the next pack, regardless of whether the bleeding has stopped or not.

Starting to take pills

If hormonal contraceptives have not been used previously (during the last menstrual cycle). The first tablet should be taken on the first day of a woman’s natural cycle, i.e. on the first day of the next menstrual bleeding. If the first tablet is taken on the first day of menstrual bleeding, the contraceptive effect of the drug begins on the first day of administration and continues during the 7-day break in taking tablets.

The first tablet can also be taken on the 2nd to 5th day of menstrual bleeding, regardless of whether the bleeding has stopped or not. In this case, during the first seven days of admission it is necessary to use additional barrier methods of contraception.

If menstrual bleeding began more than five days ago, the woman should be advised to wait until the next menstrual bleeding begins before taking Belara®.

Switching from another hormonal contraceptive to taking Belara®

Switching from another combined oral contraceptive.

Switching from drugs containing 21 or 22 active tablets. You should stop taking all tablets in the old pack. The first tablet of Belar® should be taken the next day. There should be no break in taking the pills, and the patient should not wait for the next menstrual cycle. Additional contraceptive measures are not required.

When switching from another drug containing 28 tablets: the first tablet of Belara® should be taken the next day after taking the last active tablet from the package of the previous contraceptive drug containing 28 tablets. (i.e. after taking 21 active tablets). There should be no break in taking the pills, and the patient should not wait for the next menstrual cycle. Additional contraceptive measures are not required.

Transition from drugs containing only gestagen (mini-pills). The first tablet of Belara® must be taken the day after taking the last tablet containing only a progestogen. During the first seven days, additional barrier methods of contraception must be used.

Switching from hormonal injectable contraceptives or a contraceptive implant. You can start taking Belara® on the day of implant removal or on the day of the originally planned injection. During the first seven days, additional barrier methods of contraception must be used.

After spontaneous or medical abortion in the first trimester of pregnancy. You can start taking Belara® immediately after a spontaneous or medical abortion in the first trimester of pregnancy. In this case, there is no need to use additional contraceptive measures.

After childbirth, spontaneous or medical abortion in the second trimester of pregnancy. It is recommended to start taking Belara® on the 21st - 28th day after birth, if the woman is not breastfeeding, or after an abortion in the second trimester of pregnancy. In this case, there is no need to use additional barrier methods of contraception.

If the drug was started more than 28 days after childbirth or abortion, then additional barrier methods of contraception should be used during the first seven days.

If a woman has already had sexual intercourse, pregnancy should be excluded or wait until the start of the next menstrual cycle before starting to take the drug.

Breastfeeding period. During breastfeeding, it is contraindicated to take Belara®.

After stopping taking Belara®. After you stop taking Belara®, your current cycle may lengthen by approximately one week.

Irregular taking of pills. If the patient forgot to take the pill, but took it within the next 12 hours, no additional contraceptive measures are required. The patient should continue taking the drug as usual.

If the patient forgot to take the pill, but took it after 12 hours, contraceptive protection may be reduced. If you miss a pill, you should act according to the following two basic rules:

1. You should never stop taking pills for more than 7 days.

2. 7 days of continuous use of tablets is necessary to achieve adequate suppression of the regulation of the hypothalamic-pituitary-ovarian system.

The last missed tablet should be taken immediately, even if this means taking 2 tablets. simultaneously. The following tablets should be taken as usual. Over the next 7 days, you must additionally use barrier methods of contraception, such as condoms. If taking pills was missed during the 1st week of the cycle, and there was sexual intercourse within 7 days before the missed pills (including a 7-day break in taking pills), the possibility of pregnancy should be taken into account. The more pills were missed, and the closer they were to the usual break in taking pills, the higher the likelihood of pregnancy.

Skipping pills on the 2nd and 3rd weeks of taking the drug. You should take the missed tablet immediately, even if this means taking 2 tablets. simultaneously. Take the next tablet as usual. You should use additional methods of contraception, such as condoms, for the next seven days.

If there are less than 7 tablets left in the used pack, immediately after finishing taking the tablets from the used pack, you should start taking tablets from the new pack of Belara®, i.e. there should be no break between two packages. It is likely that normal withdrawal bleeding will not occur until the second pack of tablets is gone; however, while taking tablets from a new package, breakthrough bleeding or spotting from the vagina may occur. If withdrawal bleeding does not occur after finishing taking the tablets from the second package, you should take a pregnancy test.

Recommendations for gastrointestinal disorders

If vomiting or severe diarrhea occurs within 4 hours after taking the tablet, absorption of the drug may be incomplete and the reliability of contraception cannot be guaranteed. In this case, you should act in accordance with the recommendations given in the section “Irregular use of tablets” (see above). You should continue taking Belara®.

How to Delay Withdrawal Bleeding

To delay bleeding, a woman should continue taking tablets from the next package of Belara® without taking a break. You can continue taking tablets if you wish until the tablets from the second package run out. While taking tablets from the second package, minor spotting or breakthrough bleeding may occur. After the usual 7-day break from taking tablets, you should resume regular use of Belara®. To shift the onset of bleeding to another day of the week, different from the day the bleeding began according to the current regimen, a woman can be advised to shorten the next 7-day break by the desired number of days. The shorter the break from taking the pills, the higher the likelihood of no withdrawal bleeding and no breakthrough bleeding or minor spotting while taking the next pill pack (as well as with delayed bleeding).

And if you really want

With all that has been said above, we can still say that there is no strict and unconditional prohibition for the combination of oral contraceptives (OCs) and alcoholic beverages. You just need to follow a few simple conditions.

1. The tablets should be taken at least three hours before or three hours after drinking. This will allow the active ingredient of the medication to be absorbed into the blood before mixing with ethanol in the stomach.
2. You should drink in moderate doses - the daily portion cannot be more than 20 mg of pure ethanol (50 ml of vodka, 200 ml of red wine, 400 ml of beer), since a larger amount of alcohol will provoke intoxication of the body and overload the liver. Important: the figures given are average; for a particular woman it is important to take into account factors such as age, weight, and concomitant diseases.
3. You can drink intoxicating drinks, but not too often - no more than twice a week, so that the internal organs (mainly the liver, but if we are talking about drinks like beer, then the kidneys) do not have to work at the limit of endurance.