Charosette, 75 mcg 28 pcs

Charosetta is a gestagen-containing oral contraceptive. Like other gestagen-containing oral contraceptives (“mini-pills”) Charosette is best suited for use during breastfeeding and for women who are contraindicated or who do not want to take estrogens. Unlike the “mini-pill,” Charosette’s contraceptive effects are achieved mainly by suppressing ovulation. Other effects include an increase in cervical mucus viscosity.

When using Charosette for the first 56 days, the rate of ovulation is less than 1%; after discontinuing the 56-day drug, ovulation occurs in 7 to 30 days (averaging 17 days).

In a comparative efficacy study (in which missed pills were allowed for a maximum of 3 hours), Charosette’s overall Perl index (a measure of the frequency of pregnancy in 100 women during one year of contraceptive use) was 0.4 in the group of all patients enrolled in the study.

The Charosette Perl Index is comparable to the Perl Index of combined oral contraceptives in the general population of oral contraceptive users. Administration of Charosette leads to a decrease in serum estradiol levels to values characteristic of the early follicular phase. No clinically significant changes in carbohydrate, lipid metabolism and hemostasis parameters were found.

Pharmacokinetics

Inabsorption

. After oral administration of Charosette, desogestrel is rapidly absorbed and converted to the active metabolite etonogestrel. After reaching steady state C_max etonogestrel is reached 1.8 h after taking the next tablet. The absolute bioavailability of etonogestrel is approximately 70%.

Distribution

C_ss in plasma are reached after 4-5 days of administration.

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

Etonogestrel is excreted with breast milk at a milk/serum ratio of 0.37-0.55, so for an approximate milk intake 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.

Elimation

Atonogestrel is eliminated with a T_1/2 of approximately 30 h by both single and course administration of the drug. Serum clearance after intravenous administration of etonogestrel is approximately 10 L/h. Excretion of etonogestrel and its metabolites occurs both as free steroids and as conjugates in the urine and feces (1.5/1 ratio).

Indications

If Charosette is used correctly, according to the instructions (without skipping the pills), the chance of pregnancy is very low.
Charosette can be taken by women who cannot tolerate estrogens, as well as by nursing mothers.

Active ingredient

Composition

1 film-coated tablet contains:

Desogestrel 0.075 mg.

Auxiliary substances:

Corn starch;
Povidon;
α-tocopherol;
Stearic acid;
Colloidal silicon dioxide;
Lactose monohydrate.

Composition of the shell:

Hypromellose;
Macrogol 400;
Talc;
Titanium dioxide.

How to take, the dosage

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

Interaction

Interactions between oral contraceptives and other medications may result in breakthrough bleeding and/or decreased contraceptive efficacy. The following interactions have been reported in the literature (mostly with combination contraceptives, but sometimes also reported with gestagen-containing contraceptives).

. Interactions may occur with drugs that induce microsomal enzymes, resulting in increased clearance of sex hormones (hydantoins /e.g., phenytoin/, barbiturates /e.g. phenobarbital/, primidone, carbamazepine, rifampicin, oxcarbazepine, rifabutin, topiramate, felbamate, ritonavir, nelfinavir, griseofulvin, preparations containing St. John’s wort). Women using any of these drugs should temporarily use a barrier method in addition to Charosette or choose another contraceptive method. A barrier method of contraception should be used during the use of these drugs and for 28 days after stopping their use. For women receiving long-term treatment with liver enzyme inducers, a non-hormonal contraceptive method should be considered.

If activated charcoal is used, absorption of the desogestrel in the tablet may be reduced and therefore contraceptive efficacy may decrease. In such a case, act according to the recommendations for missed pills.
Hormonal contraceptives can affect the metabolism of other drugs. Accordingly, plasma and tissue concentrations of the drug may both increase (e.g., cyclosporine) and decrease.
To identify possible interactions, you should read the instructions for use of these drugs.

Special Instructions

Medical examinations/consultations:Before prescribing the drug, the woman’s medical history should be carefully collected and a thorough gynecological examination should be performed to rule out pregnancy. The cause of menstrual irregularities, such as oligomenorrhea and amenorrhea, should be determined before prescribing the drug. The interval between control medical examinations is determined by the doctor in each individual case (frequency of examinations – at least once a year). If the prescribed drug may affect the latent or existing disease, an appropriate schedule of control medical examinations should be made.

Despite regular use of Charosette, occasional irregular bleeding may occur. If bleeding is very frequent and irregular, another contraceptive method should be considered. If the above symptoms are persistent, then organic pathology should be ruled out. The tactic for amenorrhea during the use of the drug depends on whether the pills were taken as directed and may include a pregnancy test. If pregnant, the drug should be discontinued. In case of acute or chronic liver dysfunction, the woman should consult a specialist for examination and consultation. Women should be informed that Charosette does not protect against HIV infection (AIDS) and other sexually transmitted diseases.

Decreased efficacy:The effectiveness of gestagen-containing oral contraceptives may be reduced if pills are missed, gastrointestinal distress or other medications are taken.

Changes in menstrual bleeding patterns:While using gestagen-containing contraceptives, some women may experience more frequent or prolonged vaginal bleeding, while other women may experience less frequent or no bleeding at all. These changes are often the reason why women refuse this method of contraception or stop strictly following the doctor’s instructions. In a detailed consultation with women who decide to start Charosette, your doctor should discuss the possibility of these changes in menstrual bleeding patterns. Evaluation of vaginal bleeding should be based on the clinical picture and may include evaluation to rule out malignancy or pregnancy.

Follicle development:All low-dose hormonal contraceptives cause follicle development, occasionally follicle size may reach a size larger than that of a normal cycle. In general, these enlarged follicles disappear spontaneously. Often, it runs symptom-free; in some cases, mild lower abdominal pain is noted. Surgical intervention is rarely required.

Laboratory tests:. Data from combined oral contraceptives have shown that hormonal contraceptive use can affect several laboratory tests, including biochemical measures of liver, thyroid, adrenal and renal function, serum (transport) protein levels such as corticosteroid-binding globulin, lipid/lipoprotein fractions, carbohydrate metabolism and blood clotting and fibrinolysis measures. Usually these changes remain within the normal range. It is not known to what extent this also applies to gestagen-only contraceptives.

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

The risk in women using gestagen-only oral contraceptives, such as Charosette, may be similar to that of combined oral contraceptives. However, the data for gestagen-only oral contraceptives are less certain. Compared with the lifetime risk of breast cancer, the increase in risk associated with taking the combined oral contraceptive pill 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 who use combined oral contraceptives may be due to earlier diagnosis, biological effects of the drug, or a combination of the two.

Venous thromboembolism:Epidemiologic studies have linked combined oral contraceptive use to an increased incidence of venous thromboembolism (VTE, deep vein thrombosis, and pulmonary embolism). Although the clinical significance of these data for desogestrel as an estrogen-free contraceptive is unknown, Charosette should be discontinued if thrombosis develops. Consideration should be given to discontinuing Charosette if there is prolonged immobilization associated with surgery or disease.

Diabetes mellitus:While gestagens may 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 gestagen-containing oral contraceptives. However, women with diabetes should be closely monitored during the first months of use.

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

The prevention of ectopic pregnancy with traditional gestagen-containing oral contraceptives (“mini-pills”) is not as effective as with combined oral contraceptives because ovulation is common with “mini-pills.” Despite the fact that Charosette is effective in suppressing ovulation, in case of amenorrhea or abdominal pain, ectopic pregnancy should be excluded in differential diagnosis.

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

Influence on driving and operating machinery:

Based on the pharmacodynamic profile, the drug is not considered to affect the ability to drive and operate machinery.

Contraindications

Side effects

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

Menstrual periods tend to become less frequent after a few months of taking the drug. Informing your doctor, monitoring your doctor, and using a menstrual diary may improve compliance with treatment with the drug.

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

If any of the following conditions/risk factors are observed, the expected benefits and risks of contraceptive use should be carefully weighed in consultation with your doctor for the duration of contraception. If any of the following conditions/risk factors appear, worsen, or change, the patient should see her doctor immediately to decide whether to continue using the medication.

Often – acne, nausea, mood changes, decreased libido, breast soreness, menstrual irregularities, headache, weight gain.

Infrequent – alopecia, fatigue, vomiting, discomfort when wearing contact lenses, vaginitis, dysmenorrhea, ovarian cysts.

Rarely – redness of skin, rash, urticaria, erythema nodosum.

While no reliable association with gestagen intake has been established, cholestatic jaundice, skin itching, cholelithiasis, chorea, pregnancy herpes, otosclerosis, deafness, development of hemolytic-uremic syndrome are possible with their intake.

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. Symptomatic therapy is carried out.

Pregnancy use

The use of the drug is contraindicated in pregnancy.

Preclinical studies have shown that very high doses of gestagens can cause masculinization of the female fetus.

Widespread epidemiological studies have found no increased risk of birth defects in children whose mothers took oral contraceptives before pregnancy, nor a teratogenic effect from unintentional oral contraceptive use early in pregnancy. Charosette has no effect on the quantity or quality (protein, lactose, or fat concentrations) of breast milk. However, a small amount of etonogestrel is excreted with breast milk. As a result, an infant may receive 0.01-0.05 mcg of etonogestrel per kg body weight per day (based on an intake of 150 ml/kg/day of breast milk).

Limited long-term follow-up data are available for children whose mothers were started on Charosette within 4-8 weeks after delivery. The duration of breastfeeding was 7 months, and children were monitored until age 1.5 (n=32) or 2.5 years (n=14). Assessment of growth, physical and psychomotor development showed no differences with infants whose mothers used IUDs containing copper. The available data suggest that Charosette may be used during lactation. However, the development and growth of an infant whose mother is taking Charosette should be monitored closely.

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