ČAROZETTA

Active material: Desogestrel
When ATH: G03AC09
CCF: Gestagen for oral contraception
ICD-10 codes (testimony): Z30.0
When CSF: 15.11.03
Manufacturer: N.V. ORGAN (Netherlands)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Pills, coated white, round, diameter 5 mm, lenticular, labeled “KV” above the number “2” on one side and “an organ” – another.

Excipients: Colloidal anhydrous silica, a-токоферол, lactose monohydrate, corn starch, povidone, stearic acid, gipromelloza, macrogol 400, talc, Titanium dioxide.

28 PC. – blisters (1) – polyester-aluminum foil envelopes (1) – cardboard boxes.
28 PC. – blisters (1) – polyester-aluminum foil envelopes (3) – cardboard boxes.

Pharmacological action

Gestagen for oral contraception. Charozetta^® – contraceptive drug, containing only progestogen (desogestrel). Contraceptive effect of Charosetta^® reached, primarily, by inhibiting ovulation. This has been proven by serial echographic studies of the ovaries., the absence of a peak increase in the concentration of LH in the middle of the cycle and an increase in the level of progesterone. The contraceptive effect is also provided by the thickening of the cervical mucus.. In comparative studies of the drug Charozetta^® the pearl index was 0.14, while for drugs, containing 0.03 mg of levonorgestrel, this figure reached 1.6. Thus, pregnancy rate while taking Charosetta^® comparable to that in the appointment of combined estrogen-gestagenic drugs.

Charosetta reception^® leads to a decrease in the level of estradiol to values, characteristic of the early follicular phase. At the same time, no significant changes were found in carbohydrate, lipid metabolism and hemostasis.

Like other pills, containing only progestogen (“minipill”), Charozetta^® can be taken by breastfeeding mothers, as well as those women, for whom estrogen is contraindicated or undesirable.

Pharmacokinetics

Absorption

Then I took the preparation Charozetta^® inside, desogestrel is rapidly absorbed and converted into an active metabolite Etonogestrel. After reaching the steady state C_max etonogestrel is reached through 1.8 hours after taking the next pill. The absolute bioavailability of etonogestrel is approximately 70%.

Distribution

C_ss in plasma achieved through 4-5 days of admission.

Etonogestrel on 95.5-99% binds to serum proteins, predominantly with albumin and to a lesser extent with globulin, sex hormone binding.

Etonogestrel is excreted in breast milk in a milk/serum ratio. 0.37-0.55, so, with an approximate amount of milk consumed 150 ml/kg/day a newborn may receive 0.00001-0.00005 mg 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 T_1/2 about 30 h both single, and the course of taking the drug. Serum clearance after intravenous administration of etonogestrel is approximately 10 l /. Etonogestrel and its metabolites are excreted as free steroids., and in the form of conjugates with urine and feces (in relation to 1.5/1).

Testimony

- Contraception.

Dosage regimen

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

In the absence of previous use of hormonal contraceptives (for the last month)

Tablets should be started on the 1st day of the menstrual cycle (1-day of menstrual bleeding). May start on day 2-5, but then during the first cycle during the first 7 days of taking the drug, it is recommended to use an additional (barrier) contraceptive method.

Switching from a combined oral contraceptive

You should start taking Charosetta^® the day after taking the last pill of the combined oral contraceptive, containing hormones.

Switching from other drugs, containing only progestin (“minipill”, injection, implants)

Woman, host “minipill”, can switch to Charosetta any day. Woman, using an implant, may switch to Charosetta^® on the day of its removal. Woman, using the drug in the form of injections, – in a day, When should the next injection be given?. In all cases, during the first 7 days of taking Charosetta^® it is recommended to additionally use barrier contraception.

After abortion, made in the first trimester, the woman can start taking the drug immediately.

After childbirth or abortion, made in the second trimester

It is recommended to start taking the drug on the 21st or 28th day after childbirth or abortion. When you start taking the drug at a later date, it is recommended during the first 7 days of taking Charosetta^® use barrier methods of contraception. But, if a woman after childbirth or abortion before taking Charosetta^® already had sexual intercourse, should first exclude pregnancy before starting the drug or wait until the first menstruation.

Missing the next dose of the drug

Contraceptive effectiveness may decrease, if the interval between taking two tablets is more than 36 no. If the next pill is delayed by less than 12 no, should take a pill, as soon as the woman remembered it, and subsequent tablets to be taken at the usual time. If the next pill is delayed by more than 12 no, you should follow the above rules for taking pills. However, over the next 7 days, you should additionally use barrier methods of contraception. If the tablet was missed in the first week of their use, and had sexual intercourse a week, previous missed pills, pregnancy should be ruled.

Recommendations in case of vomiting

If vomiting occurs within 3-4 h after dosing, absorption may be incomplete. In this case, you should use the recommendations, concerning skipping the next dose of the drug. If a woman does not want to change her usual regimen, she needs to take more(s) tablet(and) from other packaging.

Side effect

Irregular spotting is the most common in clinical trials., acne, mood changes, breast tenderness, nausea and weight gain. Not all side effects, noted in studies and presented below, have an association with the intake of Charosetta^®.

Common (>1/100): headache, weight gain, breast tenderness, nausea, irregular bleeding, amenorrhea, acne, mood changes, decreased libido.

Less common (<1/100): vaginitis, dysmenorrhoea, ovarian cysts, vomiting, alopecia, fatiguability, discomfort when using contact lenses.

Few (<1/1000): rash, hives, uzlovataya эritema.

Contraindications

- Or suspected pregnancy;

- current or previous history of venous thromboembolism;

- current or history of severe liver disease (until, until liver function tests return to normal);

- progestogen-dependent tumors;

is vaginal bleeding unclear etiology;

- hypersensitivity to any of the components of Charosetta^®.

Pregnancy and lactation

Studies in pregnant animals have shown, that high doses of progestogen can cause masculinization in female fetuses.

Large-scale epidemiological studies have not revealed any increased risk of birth of children with developmental anomalies from mothers, taking oral contraceptives before pregnancy, no teratogenic effect in those cases, when oral contraceptives were taken in early pregnancy.

Monitoring data for side effects of various desogestrel-containing drugs also did not reveal an increase in risk.

Cautions

If you have any of the following conditions, the benefits and possible risks of taking Charosetta should be carefully weighed in each case individually.^®. This issue should be discussed with the patient before, How will she make her decision about taking the drug?. In case of aggravation, exacerbation of diseases, worsening of the course of the disease or the appearance of the first symptoms of the conditions mentioned below, the patient should immediately consult a doctor. The physician must decide, whether to stop the drug.

The risk of developing breast cancer increases with age. While taking oral contraceptives, the risk of, that a woman will be diagnosed with breast cancer, increases. These differences in risk disappear within 10 years after stopping oral contraceptives. The risk of breast cancer does not depend on the duration of the previous use of oral contraceptives, but it depends on her age. The expected number of breast cancer cases among 10 000 Women, who used combined oral contraceptives (during 10 years after they were canceled), in relation to those who never used them, is in the same age groups the following values: 4.5/4 (16-19 years), 17.5/16 (20-24), 48,7/44 (25-29), 110/100 (30-34), 180/160 (35-39) and 260/230 (40-44). Risk in users of oral contraceptives, containing only progestin, perhaps, similar to that for combined oral contraceptives. However, for oral contraceptives, containing only progestogens, the data is not so certain. Compared to lifetime risk of breast cancer, risk, associated with oral contraceptives, minor. Cases of breast cancer in women, taking oral contraceptives, tend to be diagnosed at an earlier stage, than those, who does not use these drugs. The increased incidence of breast cancer diagnosis in oral contraceptive users may be due to earlier diagnosis of the condition., biological effects of the drug or a combination of both. Since the biological effect of the drug cannot be excluded, an individualized risk-benefit analysis of Charosetta should be carried out^® female, previously treated for breast cancer.

Since the biological effect of progestogens on the development of liver cancer cannot be excluded, an individual risk-benefit analysis should be carried out before prescribing Charosetta^® female, previously treated for liver cancer.

As a result of epidemiological studies, an association has been established between the use of combined oral contraceptives and an increased risk of venous thrombotic and thromboembolic complications., such as deep vein thrombosis and pulmonary embolism. And although the clinical significance of the findings for contraceptives, containing a progestogen without an estrogen component, unknown, Charosetta reception^® should be discontinued if thrombosis develops. The drug should also be discontinued in case of prolonged immobilization, related to surgery or disease. A woman with a history of thromboembolic complications should be warned about the possibility of recurrence..

Although progestogens may affect peripheral tissue insulin resistance and glucose tolerance, there is no evidence, that diabetic patients, using pure progestogenic oral contraceptives (CHPOK), change in treatment regimen. However, women, patients with diabetes, should be under medical supervision during the entire period of taking POCs.

Charosetta reception^® leads to a decrease in the level of estradiol in the blood plasma to the level, characteristic of the early follicular phase. Still unknown, whether it has any clinically significant effect on bone mineral density.

Prevention of ectopic pregnancy with traditional POCs is not as effective as combined oral contraceptives, because ovulation often occurs when taking traditional PPOCs. Despite the fact, which is different from conventional drugs, containing progestogens, Charozetta^® effectively inhibits ovulation, in case of amenorrhea and abdominal pain, ectopic pregnancy should still be excluded in the differential diagnosis..

It is possible to develop chloasma with a history of the development of such during pregnancy. Women with a predisposition to chloasma should avoid prolonged sun exposure or UV exposure while taking Charosetta.^®.

The following conditions have been described as in pregnancy, and when taking steroids, however, their relationship with the appointment of progestogens has not been established: cholestatic jaundice and/or itchy skin, cholelithiasis, porphyria, systemic lupus erythematosus, hemolytic uremic syndrome, Huntington Sidenhema, Herpes pregnant, hearing loss, otosclerosis-related.

Medical examinations/consultations

Before prescribing the drug, you should carefully read the medical history of the woman. During a gynecological examination, pregnancy should be excluded. In violation of the menstrual cycle, incl. with amenorrhea or oligomenorrhea, reasons should be clarified. The interval between control medical examinations is decided in each case individually.. Despite regular intake of Charosetta^®, may have irregular bleeding. If bleeding is frequent and irregular, it is necessary to decide on the appointment of another contraceptive. If the above symptoms continue after discontinuation of Charosetta^®, organic pathology should be excluded. Tactics in relation to amenorrhea while taking the drug depends on whether, whether the tablets were used in accordance with the instructions or there were any violations in their intake. In some cases, pregnancy testing should be included in the study.. In the presence of pregnancy, the drug should be discontinued.

Women should be warned, that the reception of Charosetta^® does not protect against HIV infection (AIDS) and pathogens of other diseases, sexually transmitted.

Changes in menstruation

While taking POCs, some women may experience more frequent or longer-lasting or less frequent or no vaginal bleeding. These changes often result in, that the woman rejects this method of contraception or uses it in violation of the instructions. The acceptability of such menstrual changes can be improved by additional consultations.. Evaluation of existing vaginal bleeding should be done on a regular basis and may include testing to rule out malignancy and pregnancy.

Follicle development

When taking low-dose hormonal oral contraceptives, the growth and development of follicles occurs (including dimensions, exceeding normal). In general, these enlarged follicles disappear on their own without any manifestations.. Sometimes there is mild pain in the lower abdomen. Rarely requires surgery.

Decline in efficiency

Contraceptive effectiveness, containing only progestogen, may be reduced if tablets are missed, vomiting or taking certain medications.

Laboratory findings

Data, obtained when taking combined oral contraceptives, show, that the hormonal components they contain, may interfere with some lab results, including the biochemical indicators of liver function, Thyroid, adrenal glands and kidneys, level in the plasma transport proteins, eg, corticosteroid-binding globulin and lipid/lipoprotein fractions, parameters of carbohydrate metabolism and parameters of coagulation and fibrinolysis. Usually these changes occur within normal ranges.. Unknown, can this data be transferred to contraceptives, containing only progestogen.

Effects on ability to drive vehicles and management mechanisms

No influence of Charosetta has been identified^® on the ability to drive a car or other mechanisms.

Overdose

There are no reports of any serious complications from an overdose of Charosetta.^®.

Symptoms: nausea, vomiting, slight bleeding from the vagina.

Treatment: There is no specific antidote; further treatment should be symptomatic.

Drug Interactions

Interaction of drugs, leading to an increase in the clearance of sex hormones, may lead to breakthrough vaginal bleeding and reduced effectiveness of oral contraceptives. The mechanism of this interaction is based on the induction of liver enzymes. No specific drug-drug interaction studies have been performed to date.. Based on observations with other contraceptives, one would expect, that such cases can be while taking hydantoins, ʙarʙituratov, karʙamazepina, rifampicin, oxcarbazepine, rifaʙutina, troglitazone, felbamata and griseofulvin. The maximum level of enzyme induction is usually reached no earlier than after 2-3 of the week, but then it can persist until 4 weeks after discontinuation of the concomitant drug.

Women, who take any of the above drugs for a short period of time, you should temporarily use an additional barrier method of contraception throughout the course of treatment and during 7 days after discontinuation of the concomitant drug. When taking rifampin, a barrier method of contraception should be used throughout the course of the liver and during 28 days after stopping this drug.

Women, taking medications, inducing liver enzymes, over a long period of time, it is recommended to stop taking Charosetta^® and use non-hormonal methods of contraception.

Activated charcoal may reduce drug absorption and reduce contraceptive effectiveness.. In this case, you should proceed as if you missed a pill..

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dry, the dark place at a temperature from 2° to 30° c. Shelf life – 3 year.