Belara tabs #63

Instruction for Belara

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Belara is a combined oral contraceptive drug.

Release form and composition

Belara is available in the form of light pink round film-coated tablets (21 pcs. In a contour package).
Contents in 1 tablet:
    Active substances: ethinylestradiol - 0.03 mg, chlormadinone acetate - 2 mg;
    Excipients: titanium dioxide (E171), talc, magnesium stearate, macrogol 6000, corn starch, propylene glycol, povidone K30, lactose monohydrate, hypromellose 6 mPa × s, iron III dye red oxide (E172).

Pharmacodynamics

Long-term use of Belara helps to reduce the production of luteinizing hormone (LH) and follicle-stimulating hormone (FH), which results in suppression of ovulation. At the same time, proliferative processes occur in the endometrium, and its secretory transformation occurs. This causes an increase in the viscosity of the cervical mucus, which leads to difficulties in the passage of spermatozoa through the cervical canal and a decrease in their mobility, as well as the impossibility of implantation of a fertilized egg.
To completely suppress ovulation, a daily intake of 1.7 mg of chlormadinone acetate, the active component of Belara, is required. The recommended dose to be taken during a cycle is 25 mg.
Chlormadinone acetate is a gestagen characterized by antiandrogenic properties. It is able to replace androgens at specific receptors, suppressing and weakening the action of exogenous and endogenous androgens. Pearl's index is 0.291-0.698 and depends on the thoroughness of adherence to the regimen of the drug.

Pharmacokinetics of Chlormadinone Acetate

Chlormadinone acetate (CMA) is rapidly and completely absorbed after oral administration. Its maximum content in the blood is noted after 1–2 hours. More than 95% of the compound binds to plasma proteins, mainly albumin.
CMA is involved in redox reactions, and also binds to sulfates and glucuronides. This contributes to the formation of a large number of metabolites. The main metabolites in blood plasma are 3-alpha- and 3-beta-hydroxy-CMA, the half-life of which does not differ significantly from that of CMA. 3-hydroxy-metabolites have antiandrogenic activity similar to that of CMA. The metabolites enter the urine mainly in the form of conjugates. After cleavage by enzymes, 2-alpha-hydroxy-CMA is the main metabolite; 3-hydroxy metabolites and dihydroxy metabolites are also detected.
The half-life of CMA from blood plasma averages about 34 hours (after taking a single dose) and about 36-39 hours with repeated use. When taken orally, CMA and its metabolites are excreted in approximately equal amounts through the intestines and kidneys.

Pharmacokinetics of ethinyl estradiol

Ethinylestradiol (EE) is almost completely and rapidly absorbed after oral administration. The maximum level of the substance in the blood plasma is detected 1.5 hours after ingestion. Due to metabolism in the liver and presystemic binding, its absolute bioavailability is approximately 40%, but can vary over a wide range from 20 to 65%, depending on the individual response of the body.
Approximately 98% of EE binds to blood plasma proteins, a significant part exclusively with albumin.
Biotransformation of EE occurs by hydroxylation of the aromatic ring, and the cytochrome P450 system is the mediator. The main metabolite is 2-hydroxy-EE, which is converted to other metabolites and conjugates. EE is available for presystemic binding both in the liver and in the lining of the small intestine. Mainly glucuronides are found in urine, and sulfates are found in blood plasma and bile.
The half-life of EE from blood plasma averages about 12-14 hours. The compound is excreted from the body in urine and feces in a ratio of approximately 2: 3. EE sulfate, which is excreted in the bile after hydrolysis by intestinal microorganisms, is involved in the process of intestinal hepatic recirculation.

Indications for use

Belara is used for oral contraception.

Contraindications

    Uncontrolled diabetes mellitus and diabetes with vascular complications;
    The presence of thrombosis, multiple or severe risk factors for venous or arterial thrombosis, as well as the presence of symptoms of embolism and thrombophlebitis;
    Acute renal failure, hepatitis, the presence of liver tumors, jaundice, liver dysfunction;
    Uncontrolled arterial hypertension or a significant increase in blood pressure;
    Dubin-Johnson and Rotor syndromes;
    Diseases accompanied by a violation of the outflow of bile;
    The presence of hormone-dependent malignant diseases;
    Pancreatitis
    Severe depression.
The following diseases / conditions are also contraindications to taking the drug:
    Vaginal bleeding or amenorrhea of ​​unknown etiology;
    Inflammatory diseases of the female genital organs;
    Migraine or frequent headache attacks;
    Epilepsy;
    Severe lipid metabolism disorders;
    Porphyria;
    Visual and hearing impairments, as well as movement disorders;
    Hypersensitivity to the components that make up the tablets.
If pregnancy is confirmed, the drug should be discontinued.
It is not recommended to take the drug during breastfeeding, as it reduces the amount of milk produced and changes its composition. It is also contraindicated to take Belara when smoking over the age of 35.
The drug is taken with caution:
    Convulsive syndrome;
    Diabetes mellitus with uncomplicated course;
    Autoimmune diseases;
    Obesity;
    Renal failure;
    Endometriosis;
    Chronic heart failure;
    Multiple sclerosis;
    Arterial hypertension;
    Violation of fat metabolism.
Irregular vaginal bleeding may occur during the first months of using the contraceptive. In this case, it is recommended to undergo additional examination.

Instructions for the use of Belara: method and dosage

Belara tablets are recommended to be taken at the same time. The first pill is taken on the first day of the menstrual cycle. After 21 days of admission, you should take a break of 7 days, during which menstrual bleeding should begin. After a break, you must resume taking the drug. The tablets are taken from the pack marked with the corresponding day.
When switching from another hormonal contraceptive containing 28 tablets, the 7-day break is not taken, taking the first Belara tablet from the new package immediately after the old one is completed. In this case, additional contraceptive measures are not required. When switching from contraceptives containing only gestagen, the drug can be taken without interruption, on any day of the menstrual cycle.
In case of vomiting or diarrhea while taking the drug, it is recommended to use additional methods of contraception, since the contraceptive effect of the drug decreases.

Side effects

Most often, taking Belara causes mastodynia, headache and bloody discharge from the vagina. In addition, the following are noted:
    Decreased hearing, visual disturbances, tinnitus, discomfort when wearing contact lenses and conjunctivitis;
    Irritability, depression, dizziness, migraine;
    Collapse, arterial hypertension or hypotension, varicose veins;
    Muscle aches and back pain;
    Nausea, vomiting, flatulence and diarrhea;
    Acne, pigmentation disorders, allergic skin reactions, chloasma, hair loss, dry skin, urticaria, eczema, erythema, itching, increased psoriasis;
    Transient swelling, fatigue, weight gain, heaviness in the legs, increased appetite and increased sweating;
    Strengthening of mucous discharge from the vagina, genital candidiasis, premenstrual syndrome, amenorrhea, dysmenorrhea, pain in the pelvic area, enlargement of the mammary glands, ovarian cyst.
When taking the drug, the risk of developing the following diseases may increase:
    Diseases of the biliary tract;
    Neoplasms of the liver and mammary gland;
    Venous and arterial thromboembolism;
    Inflammatory bowel disease.

Overdose

In case of an overdose, there are no serious toxic reactions. In case of accidental oral administration of too large a dose of the drug, bleeding from the vagina, nausea, and vomiting are possible.
There is no specific antidote. If necessary, symptomatic therapy is prescribed and monitoring of liver function and indicators of water-electrolyte metabolism is carried out.

Special instructions

With the simultaneous use of certain drugs, it should be borne in mind that they can reduce the contraceptive effect:
    All drugs that increase gastrointestinal motility or interfere with absorption, including activated charcoal;
    Rifabutin, modafinil, rifampicin, carbamazepine, phenytoin, oxcarbazepine, topiramate, phenylbutazone, St. John's wort, felbamate, griseofulvin, barbiturates, barbexaclon, primidone and ritonavir;
    Antibiotics - tetracycline, ampicillin, rifampicin and some others.
With the simultaneous use of such drugs, it is recommended to use additional barrier methods of contraception throughout the entire course of treatment with these drugs and within a week after it.
Before you start taking Belara, it is recommended to conduct a full medical examination in order to exclude possible conditions or diseases included in the list of contraindications.
It should be borne in mind that the drug does not protect against sexually transmitted infections, including HIV infection (AIDS).
If you have a tendency to develop chloasma while using a contraceptive, you should avoid direct sunlight and UV radiation.

Influence on the ability to drive vehicles and complex mechanisms

According to the instructions, Belara does not affect the patient's ability to drive a car or work with complex or moving mechanisms.

Application during pregnancy and lactation

Belara is contraindicated in pregnancy. Before starting therapy, it is imperative to exclude the onset of pregnancy. If conception occurs during the period of taking the drug, it must be immediately canceled. The data of epidemiological studies do not contain information confirming the development of embryotoxic or teratogenic effects in patients who took oral contraceptives during pregnancy containing estrogens and gestagens in the same ratio as in Belara.
The use of a contraceptive during lactation is contraindicated, since it reduces the production of breast milk and changes its composition. Small concentrations of hormones and / or their metabolites are detected in breast milk and can affect the baby's body.

With impaired renal function

In renal failure, Belara is used with caution.

For violations of liver function

The use of a contraceptive is contraindicated in acute or chronic liver diseases of a severe degree (until the normalization of hepatic function), as well as in cases of diagnosed liver cancer at present or in history.
The drug should be used with caution in acute or chronic liver diseases of mild or moderate severity (after normalization of liver function tests).

Drug interactions

The interaction of ethinyl estradiol with other drugs can cause an increase or decrease in its concentration in the blood serum. If long-term therapy with such drugs is necessary, it is recommended to switch to non-hormonal contraceptives. A decrease in the level of EE in the blood serum can provoke a higher frequency of episodes of breakthrough bleeding, a violation of the cycle and a decrease in the contraceptive effectiveness of Belara. An increase in the content of EE in the blood serum often leads to an increase in the manifestation of side effects and an increase in their severity.
The following drugs / active ingredients can lower serum estradiol levels:
    some antibiotics (in particular, tetracycline and ampicillin) due to suppression of enterohepatic circulation of estrogens;
    active substances - inducers of microsomal liver enzymes: preparations of St. John's wort, rifampicin, some protease inhibitors (for example, ritonavir), rifabutin, modafinil, barbiturates, primidone, anticonvulsants (in particular, topiramate, phenytoin, carbamazepine), barbexofaclone;
    all drugs that enhance gastrointestinal motility (for example, metoclopramide) or alter absorption (for example, activated carbon).
With the simultaneous use of such drugs with Belara, it is recommended to use additional barrier methods of contraception both during therapy and for 7 days after it. When taking active substances that reduce the content of EE in the blood serum due to the induction of microsomal liver enzymes, additional barrier contraceptives should be used for 28 days after completion of the course of treatment.
The following drugs / active drug ingredients can increase serum estradiol levels:
    substances that inhibit the activity of liver microsomal enzymes, in particular, troleandomycin, indinavir, antifungal imidazoles (for example, fluconazole);
    atorvastatin (increases EE AUC by 20%);
    active substances that inhibit the sulfation of EE in the intestinal wall, for example, paracetamol or ascorbic acid.
Ethinylestradiol can inhibit the activity of liver microsomal enzymes and increase the serum content of such active components of drugs as prednisolone, diazepam and other benzodiazepines metabolized by hydroxylation, theophylline and cyclosporine. EE also induces hepatic glucuronidation, which leads to a decrease in serum concentrations of lorazepam, clofibrate, morphine and paracetamol.
Since Belara affects glucose tolerance, while taking a contraceptive, a dose adjustment of insulin and oral hypoglycemic drugs may be required.
Before prescribing any drug in conjunction with Belara, its characteristics should be carefully studied to determine possible interactions with the active components of the contraceptive.

Terms and conditions of storage

The drug is dispensed with a doctor's prescription.
Store at temperatures up to 25 ° C.
Shelf life is 2 years.

Reviews about Belara

According to doctors, the contraceptive drug is a reliable method of contraception, although it is relatively expensive. Reviews of the majority of patients about Belara are also positive, however, some women note frequent side effects: weight gain and the appearance of acne, for the treatment of which a course of appropriate therapy is required.

Terms of sell

You don't need a prescription to buy Belara.