Cerazette pills 75mcg, 28pcs

Composition

1 film-coated tablet contains:

Desogestrel 0.075 mg.

Auxiliary substances:

Corn starch; Povidone; alpha-tocopherol; Stearic acid;Colloidal silicon dioxide;Lactose monohydrate.

Shell composition:

Hypromellose; Macrogol 400; Talc;Titanium dioxide.

Pharmacological action

Charozetta is a progestogen-containing oral contraceptive. Similar to other progestogen-containing oral contraceptives (“mini-pili”) Charosetta is best suited for use during breastfeeding and for women who are contraindicated or who do not want to take estrogens. Unlike mini-pili, the contraceptive effect of Charosetta is achieved mainly by suppressing ovulation. Other effects include an increase in the viscosity of cervical mucus.

When using the drug Charosetta in the first 56 days, the frequency of ovulation does not exceed 1%, after stopping the 56-day intake of the drug, ovulation occurs in 7-30 days (on average, after 17 days).

In a comparative efficacy study (in which missed pills were allowed to be taken for a maximum of 3 hours), the overall Pearl index (an indicator that reflects the frequency of pregnancy in 100 women during the year of contraceptive use) of Charosetta was 0.4 in the group of all patients included in the study.

The Pearl index of Charosetta is comparable to the Pearl index of combined oral contraceptives in the general population taking oral contraceptives. Taking the drug Charosetta leads to a decrease in serum estradiol levels, to values characteristic of the early follicular phase. There were no clinically significant changes in carbohydrate, lipid metabolism, or hemostasis parameters.

Pharmacokinetics

Suction

After oral use of Charosetta, desogestrel is rapidly absorbed and converted to the active metabolite etonogestrel. After reaching a stationary state, the_cmax of etonogestrel is reached in 1.8 hours after taking the next tablet. The absolute bioavailability of etonogestrel is approximately 70%.

Distribution

of_csss in blood plasma is achieved after 4-5 days of use.

Etonogestrel binds 95.5-99% to serum proteins, mainly albumin and to a lesser extent to globulin, which binds sex hormones.

Etonogestrel is excreted in breast milk at a milk/serum ratio of 0.37-0.55, therefore, with an approximate volume of milk consumed of 150 ml/kg/day, a newborn can receive 0.00001-0.00005 mg of etonogestrel.

Metabolism

Desogestrel is converted by hydroxylation and dehydrogenation to the active metabolite etonogestrel. Etonogestrel is metabolized through the formation of sulfate and glucuronide conjugates.

Deduction

Etonogestrel is eliminated with a T_1/2 of approximately 30 hours both with a single and course use of the drug. The serum clearance after intravenous use of etonogestrel is approximately 10 l/h. The excretion of etonogestrel and its metabolites is carried out both in the form of free steroids and in the form of conjugates with urine and feces (in a ratio of 1.5 / 1).

Indications

Contraception. If Charosetta is used correctly, according to the instructions (without skipping pills), the probability of pregnancy is very low. Charosetta can be taken by women who do not tolerate estrogens, as well as nursing mothers.

Use during pregnancy and lactation

During pregnancy, the use of the drug is contraindicated.

The results of preclinical studies have shown that very high doses of progestogens can cause masculinization of the female fetus.

Extensive epidemiological studies have found neither an increased risk of birth defects in children whose mothers took oral contraceptives before pregnancy, nor a teratogenic effect when unintentionally taking oral contraceptives in early pregnancy. Charosetta does not affect the quantity or quality (protein, lactose, or fat concentrations) of breast milk. However, a small amount of etonogestrel is excreted in breast milk. As a result, the child’s body can receive 0.01-0.05 mcg of etonogestrel per kg of body weight per day (based on the consumption of 150 ml/kg/day of breast milk).

There are limited data on long-term follow-up of children whose mothers started taking Charosetta within 4 to 8 weeks after delivery. The duration of breast-feeding was 7 months, and children were monitored until the age of 1.5 (n=32) or 2.5 years (n=14). The assessment of growth, physical and psychomotor development did not show any differences with children whose mothers used IUDs containing copper. Available data suggest that Charosetta can be used during lactation. However, it is necessary to carefully monitor the development and growth of an children whose mother takes Charosetta.

Contraindications

• Hypersensitivity to the Active ingredient or any excipient of the drug.
• Established or suspected pregnancy.
• The presence or history of venous thromboembolism (including deep vein thrombosis of the lower leg, pulmonary embolism).
• The presence of severe liver disease at the moment or in the anamnesis (until liver function indicators return to normal).
• Hepatic insufficiency, including in the anamnesis.
• Established or suspected malignant hormone-dependent tumors.
• Vaginal bleeding of unclear etiology.
• Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution, in the presence of any of the following conditions/risk factors, the benefits of using progestogen should be weighed against the possible risks for each individual woman. This should be discussed with the woman before she decides to start taking the drug. If the disease worsens, worsens, or any of these conditions occur for the first time, a woman should consult a doctor. The doctor should decide whether to continue using Charosetta):

• Persistent hypertension that develops while taking Charosetta, or when antihypertensive therapy is ineffective.
• Thromboembolic disorders, including in the anamnesis: the woman should be warned about the possibility of relapse.
• Prolonged immobilization associated with surgery or a medical condition.
• Since it is impossible to exclude the biological effect of progestogens on the development of liver cancer, an individual assessment of the benefit-risk ratio should be carried out when prescribing the drug to women with liver cancer.
• Chloasma, especially in women with a history of chloasma during pregnancy: women with a predisposition to chloasma should avoid exposure to sunlight or ultraviolet radiation while using Charosetta.

Side effects

The most common adverse effect reported in clinical trials was irregular menstruation. Up to 50% of women who used desogestrel reported acyclic spotting: in 20-30% of women, menstruation becomes more frequent, while in the other 20%, it is more rare or may even stop completely. Menstruation may also become more prolonged.

After several months of taking the drug, menstruation tends to become less frequent. Informing your doctor, following up with your doctor, and using a menstrual diary can increase compliance with medication.

The following are undesirable effects that have an established, probable or possible association with the use of the drug.

In the event that any of the following conditions/risk factors are present, the expected benefits and risks of using a contraceptive should be carefully weighed when consulting your doctor throughout the entire period of contraception. If any of the following conditions/risk factors appear, increase, or change, the patient should immediately consult a doctor to decide whether to continue using the drug.

Often — acne, nausea, mood changes, decreased libido, breast tenderness, menstrual disorders, headache, weight gain.

Infrequently — alopecia, fatigue, vomiting, discomfort when wearing contact lenses, vaginitis, dysmenorrhea, ovarian cysts.

Rarely — redness of the skin, rash, urticaria, erythema nodosum.

Although a reliable association with the use of progestogens has not been established, cholestatic jaundice, pruritus, cholelithiasis, chorea, herpes of pregnant women, otosclerosis, deafness, and the development of hemolytic-uremic syndrome are possible when taking them.

Interaction

Interactions between oral contraceptives and other medications may lead to breakthrough bleeding and / or reduced contraceptive effectiveness. The following interactions are reported in the literature (mainly with combined contraceptives, but sometimes also reported for progestogen-containing contraceptives).

Interaction with drugs that induce microsomal enzymes may occur, which leads to an increase in the clearance of sex hormones (hydantoins /for example, phenytoin/, barbiturates /for example, phenobarbital/, primidone, carbamazepine, rifampicin, oxcarbazepine, rifabutin, topiramate, felbamate, ritonavir, nelfinavir, griseofulvin, preparations containing St. John’s wort). Women using any of these medications should temporarily use a barrier method in addition to Charosetta or choose a different method of contraception. The barrier method of contraception should be used during the use of these drugs and within 28 days after discontinuation of their use. For women receiving long-term treatment with inducers of liver enzymes, the possibility of using a non-hormonal method of contraception should be considered. When using activated charcoal, the absorption of desogestrel in the tablet may decrease and, therefore, the contraceptive effectiveness may decrease. In this case, you should act in accordance with the recommendations regarding missed pills. Hormonal contraceptives can affect the metabolism of other medications. Accordingly, the concentrations of the drug in plasma and in tissues can both increase (for example, cyclosporine) and decrease. To identify possible interactions, you should read the instructions for use of these drugs.

How to take, course of use and dosage

The drug should be taken 1 tablet/day, daily, at the same time, for 28 days, in the order indicated on the package. Reception of each subsequent package should begin immediately after the end of the previous one, without any interruption. The taken tablet can be washed down with a small amount of liquid.

In the absence of previous use of hormonal contraceptives (during the last month), tablets should be taken on the 1st day of the menstrual cycle (on the 1st day of menstrual bleeding). It is allowed to start taking for 2-5 days, but then during the first cycle during the first 7 days of taking tablets, it is recommended to additionally use a barrier method of contraception. Switching from a combined hormonal contraceptive (combined oral contraceptive, vaginal ring, or transdermal patch): a woman should start taking Charosetta, preferably on the day after taking the last active tablet of the combined oral contraceptive (the last tablet containing the Active ingredient) or on the day of removal of the vaginal ring or patch. In these cases, there is no need for additional contraception. At the latest, a woman can also start taking Charosetta the day after the end of the usual interval in taking tablets, patches, rings or the day after taking placebo tablets of the previous combined oral contraceptive (i. e., on the day when it would be necessary to start using a new package of combined oral contraceptive, insert a new ring or stick a new patch), but during the first 7 days of taking tablets, it is recommended to use an additional barrier method of contraception. Switching from other progestogen-only medications (mini-pills, injections, implants, or a progestogen-releasing intrauterine system): a woman taking mini-pills. can switch to taking the drug Charosetta any day. A woman using an implant or intrauterine device – on the day of their removal. A woman who uses injectable forms of contraceptives – on the day when the next injection should be made. In all these cases, an additional method of contraception is not required. After an abortion performed in the first trimester, it is recommended to start taking the drug immediately: an additional method of contraception is not required. Taking the drug is possible no earlier than 21-28 days after an abortion made in the second trimester, and no earlier than 6 weeks after delivery. When starting taking the drug at a later date, it is necessary to additionally apply a barrier method of contraception during the first 7 days of taking the tablets. However, if a woman has already had sex after giving birth or having an abortion before taking Charosetta, pregnancy should be excluded before using the drug, or the woman should wait for the first menstruation. What should I do if I miss my next pill intake?: contraceptive protection may decrease if the interval between taking two tablets is more than 36 hours. If the delay in taking the pill is less than 12 hours, then the missed pill should be taken as soon as the woman remembers it, and the next pill should be taken at the usual time. If the delay in taking the pill is more than 12 hours, then the woman should follow the above recommendations, as well as use an additional method of contraception for the next 7 days. If the pills were missed in the very first week of taking the drug and sexual intercourse took place during the week preceding the omission of taking the pills, pregnancy should be excluded. In case of severe gastrointestinal disorders (vomiting, diarrhea), absorption may be incomplete and in this case additional methods of contraception should be used. If vomiting occurs within 3-4 hours after ingestion, the absorption may be incomplete. In this case, you should follow the recommendations regarding the use of missed pills.

Overdose

No serious side effects have been reported as a result of overdose.

Symptoms: nausea, vomiting and, in young girls, minor vaginal bleeding.

Treatment: there is no specific antidote. Conduct symptomatic therapy.

Special instructions

Medical examinations/consultations: before prescribing the drug, a woman’s medical history should be carefully collected and a thorough gynecological examination should be performed to exclude pregnancy. Before prescribing the drug, you should determine the cause of menstrual disorders, for example, oligomenorrhea and amenorrhea. The interval between control medical examinations is determined by the doctor in each individual case (the frequency of examinations is at least once a year). If the prescribed drug may affect a latent or existing disease, an appropriate schedule of follow-up medical examinations should be drawn up.

Despite regular use of the drug Charosetta, sometimes irregular spotting may occur. If the bleeding is very frequent and irregular, you should consider using another method of contraception. If the above symptoms are persistent, then in this case it is necessary to exclude organic pathology. Treatment of amenorrhea during the use of the drug depends on whether the tablets were taken in accordance with the instructions, and may include a pregnancy test. In case of pregnancy, the drug should be discontinued. In case of acute or chronic liver function disorders, a woman should consult a specialist for examination and consultation. Women should be informed that Charosetta does not protect against HIV infection (AIDS) and other sexually transmitted diseases.

Reduced efficiency: the effectiveness of progestogen-containing oral contraceptives may be reduced if you skip taking pills, have gastrointestinal disorders, or take other medications.

Changes in the nature of menstruation: during the use of progestogen-containing contraceptives, some women may experience more frequent or prolonged vaginal bleeding, while other women may experience less frequent or stop bleeding altogether. These changes are often the reason that a woman refuses this method of contraception, or stops strictly following the doctor’s instructions. In a detailed consultation with women who have decided to start taking Charosetta, the doctor should discuss the possibility of such changes in the nature of the menstrual cycle. Evaluation of vaginal bleeding should be based on the clinical picture and may include examination to exclude malignancies or pregnancy.

Follicle development: when taking all low-dose hormonal contraceptives, follicles develop, and occasionally the size of the follicle can reach sizes that exceed those in the normal cycle. In general, these enlarged follicles disappear spontaneously. Often, this occurs without symptoms; in some cases, there is a slight pain in the lower abdomen. Surgical intervention is rarely required.

Laboratory tests: the data obtained in respect of combined oral contraceptives showed that the use of hormonal contraceptives can affect the results of certain laboratory tests, including biochemical parameters of liver, thyroid, adrenal and kidney failure, the levels (transport) proteins in serum, for example, globulin, corticosteroid binding, the fraction of lipids/lipoproteins, carbohydrate metabolism and parameters of coagulation and fibrinolysis. These changes usually remain within the normal range. It is not known to what extent this also applies to progestogen-only contraceptives.

Breast cancer: the risk of breast cancer increases with age. During the use of combined oral contraceptives, the risk that a woman will be diagnosed with breast cancer slightly increases.This increased risk gradually disappears within 10 years after stopping the use of oral contraceptives, it is not related to the duration of use, but depends on the age of the woman during the use of combined oral contraceptives.

The risk in women using oral contraceptives containing only progestogen, for example, Charosetta, may be similar to that when using combined oral contraceptives. However, the data for oral contraceptives containing only progestogen are not so clear. Compared to the lifetime risk of breast cancer, the increased risk associated with taking combined oral contraceptives is small. Breast cancer diagnosed in women who use combined oral contraceptives tends to be less clinically advanced than cancer diagnosed in women who have never used combined oral contraceptives. The increased risk in women using combined oral contraceptives may be due to earlier diagnosis, biological effects of the drug, or a combination of these two factors.

Venous thromboembolism: Epidemiological studies have established a link between the use of combined oral contraceptives and an increased incidence of venous thromboembolism (VTE, deep vein thrombosis, and pulmonary embolism ). Although the clinical significance of these data for desogestrel, as a contraceptive that does not contain an estrogenic component, is unknown, the use of Charosetta should be discontinued in case of thrombosis. Discontinuation of Charosetta should be considered in the event of prolonged immobilization associated with surgery or disease.

Diabetes mellitus: Although progestogens can affect peripheral tissue insulin resistance and glucose tolerance, there is no evidence that there is a need to change the therapeutic regimen in diabetic patients using progestogen-containing oral contraceptives. However, women with diabetes should be closely monitored during the first months of using the drug.

Bone mineral density: the use of Charosetta leads to a decrease in serum estradiol levels to the level corresponding to the early follicular phase. To date, it is not known whether this reduction has any clinically significant effect on bone mineral density.

Prevention of ectopic pregnancy with traditional progestogen-containing oral contraceptives (“mini-pili”) is not as effective as with combined oral contraceptives, since ovulation often occurs with the use of “mini-pili”. Despite the fact that Charosetta effectively suppresses ovulation, in the case of amenorrhea or abdominal pain, ectopic pregnancy should be excluded during differential diagnosis.

Charosetta contains no more than 65 mg of lactose, so women who have rare hereditary problems associated with galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption should refrain from taking the drug.

Influence on the ability to drive motor vehicles and manage mechanisms:

based on the pharmacodynamic profile, it is considered that the drug does not affect the ability to drive vehicles and work with mechanisms.

Form of production

Film-coated tablets.

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light at a temperature of 2° to 30°C.

Shelf

life is 3 years.

Active ingredient

Desogestrel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

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

Indications

Contraception