Composition, form of production and packaging
The tablets covered with a film coating of white color, round, biconcave, with an engraving "KV" above the figure "2" on one side of the tablet and "ORGANON" with the image of a five-pointed star on the other side of the tablet; on the bend - white.
desogestrel 75 Ојg
Excipients: corn starch - 6.5 mg, povidone - 1.95 mg,? -tocopherol - 80 mcg, stearic acid - 650 mcg, silicon dioxide colloid - 650 mcg, lactose monohydrate - up to 65 mg.
The composition of the film shell: opadrai OY-S-28833 - 1.2 mg (hypromellose - 750 Ојg, macrogol 400 - 150 Ојg, titanium dioxide - 110 Ојg, talc - 190 Ојg).
28 pcs. - blisters (1) - sachets made of foil of aluminum laminated (1) - packs of cardboard.
28 pcs. - blisters (1) - sachets made of foil of aluminum laminated (3) - packs of cardboard.
28 pcs. - blisters (1) - sachets made of foil of aluminum laminated (6) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
Gestagen-containing oral contraceptive. Like other gestagen-containing oral contraceptives ("mini-drank"), Charozette В® is best suited for use during breastfeeding and for women who are contraindicated or who do not want to take estrogens. In contrast to the "mini-saws", the contraceptive effect of Charozette В® is achieved mainly by suppressing ovulation. Other effects include an increase in the viscosity of cervical mucus.
With the application of Charozette В® in the first 56 days, the frequency of ovulation does not exceed 1%, after stopping the 56-day treatment, ovulation occurs after 7-30 days (an average of 17 days).
In a comparative study of efficacy (in which it was allowed to take missed tablets for a maximum of 3 hours), the overall Perl index (an indicator reflecting the frequency of pregnancy in 100 women during the year of use of the contraceptive) of the Charosette В® drug was 0.4 in the group of all patients enrolled.
The Pearl Index of the Charozette В® drug is comparable to the Perl index of combined oral contraceptives in the general population taking oral contraceptives. The administration of Charozette В® leads to a decrease in the serum estradiol level, up to values вЂ‹вЂ‹characteristic of the early follicular phase. At the same time, there were no clinically significant changes in the carbohydrate, lipid metabolism and hemostasis parameters.
After taking Charozette В® inside, desogestrel is rapidly absorbed and converted to an active metabolite of etonogestrel. After achieving a steady state, Cmaxetonogestrel is achieved 1.8 hours after the administration of the next tablet. The absolute bioavailability of etonogestrel is approximately 70%.
C ss in blood plasma are reached after 4-5 days of admission.
Etonogestrel is 95.5-99% bound to serum proteins, predominantly albumin and to a lesser extent to globulin binding sex hormones.
Etonogestrel is excreted in breast milk in the ratio of milk / blood serum 0.37-0.55, therefore, with an approximate volume of milk consumed 150 ml / kg / day a newborn can get 0.00001-0.00005 mg etonogestrel.
Desogestrel is converted by hydroxylation and dehydrogenation into the active metabolite ethonogestrel. Etonogestrel is metabolized through the formation of sulfate and glucuronide conjugates.
Etonogestrel is eliminated with T 1/2 approximately 30 h as with 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 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).
The drug should be taken 1 tablet / day, daily, at the same time, for 28 days, in the order indicated on the package. Receipt of each subsequent package should be started immediately after the end of the previous one, without any interruption. The taken tablet can be washed down with a small amount of liquid.
How should I start taking Charozette В®
In the absence of a previous intake of hormonal contraceptives (for the last month)
Tablets should be taken on the 1st day of the menstrual cycle (1st day of menstrual bleeding). It is possible to start on the 2nd-5th day, but then during the first cycle during the first 7 days of taking the drug it is recommended to use an additional (barrier) method of contraception.
Transition from a combined hormonal contraceptive (combined oral contraceptive, vaginal ring or transdermal patch). The woman should start taking Charozette В®preferably on the day after the last active tablet of the combined oral contraceptive (last tablet containing the active substance) 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 Charosette В® the day after the usual interval in taking the tablets, plaster, ring, or the day after taking the placebo tablets of the previous combined oral contraceptive (ie, the day that you would start using new packaging of the combined oral contraceptive, insert a new ring or glue a new patch), but during the first 7 days of taking the tablets it is recommended to use an additional barrier method of contraception and.
Transition from other drugs containing only progestogen ("mini-drank", injections, implants or gestagen-releasing intrauterine system). A woman who takes "mini-drank" can go to Charozetta's reception any day. A woman using an implant or an intrauterine system is on the day of their removal. A woman who uses injectable contraceptive forms is the day the next injection is to be made. In all these cases, an additional contraceptive method is not required.
After abortion, made in the first trimester, it is recommended to start taking the drug immediately; an additional contraceptive method is not required.
After childbirth or abortion, made in the II trimester. The drug can be taken no earlier than 21-28 days after the abortion, made in the second trimester, and not earlier than 6 weeks after childbirth. At the beginning of taking the drug at a later date, the barrier method of contraception must be additionally applied during the first 7 days of taking the tablets. However, if a woman has had sexual intercourse after giving birth or having an abortion prior to taking the Charozette В® drug, pregnancy should be excluded before the beginning of the use of the drug or the woman should wait for the first menstruation.
Skipping the next dose of the drug
Contraceptive protection may decrease if the interval between taking two tablets is more than 36 hours. If the delay in taking the tablet is less than 12 hours , the missed tablet 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 tablet is more than 12 hours , the woman should follow the above recommendations, and also apply an additional contraceptive method within the next 7 days. If the pills were missed in the very first week of taking the drug and there was a sexual intercourse during the week preceding the missed intake of tablets, pregnancy should be excluded.
Recommendations in case of gastrointestinal disorders
In the case of severe gastrointestinal disorders (vomiting, diarrhea), absorption may be incomplete and in this case additional contraceptive methods should be used. If vomiting occurs within 3-4 hours after ingestion, the absorption may be incomplete. In this case, it is necessary to be guided by the recommendations regarding the intake of missed tablets.
In clinical studies of Charozette В® , side effects were most often noted (> 2.5%): irregular spotting, acne, mood changes, breast tenderness, nausea and weight gain.The undesirable effects presented in the table below were evaluated by the investigators as having an established, probable and possible association with the administration of the drug.
Often (? 1/100) Not infrequently (? 1/1000, <1/100) Rarely (<1/1000)
Infections and invasions
From the nervous system
mood changes, decreased libido, headache
From the side of the organ of vision
intolerance to contact lenses
From the digestive system
From the skin side
acne alopecia skin rash, hives, erythema nodosum
From the side of the reproductive system
tenderness of the mammary glands, irregular menstruation, amenorrhea dysmenorrhea, ovarian cyst, vaginitis discharge from the mammary glands, ectopic pregnancy
weight gain fatigue
In women who received (combined) oral contraceptives, there were various (serious) adverse effects. These include venous and arterial thromboses and thromboembolism, hormone-dependent tumors (eg, breast cancer), and chloasma.
There is no reliable connection with the use of progestogens: jaundice and / or skin itching associated with cholestasis; the formation of gallstones; porphyria; systemic lupus erythematosus; hemolytic-uremic syndrome; Sydenham's chorea; herpes pregnant; hearing loss associated with otosclerosis; (hereditary) angioedema.
- established or suspected pregnancy;
- the presence at the time or in an anamnesis of venous thromboembolism (including deep vein thrombosis of the lower leg, thromboembolism of the pulmonary artery);
- the presence at this time or in a history of severe liver disease (as long as the liver function is not normalized);
- hepatic insufficiency, incl. in the anamnesis;
- established or suspected malignant hormone-dependent tumors;
bleeding from the vagina of an unclear etiology;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- Hypersensitivity to the components of the drug.
Contraceptives containing only gestagens should not be taken if there is at least one of the above conditions. When it appears for the first time during the administration of the drug Charosette В® , you should immediately stop taking the drug.
If any of the following conditions / risk factors are present, the use of progestogen and the possible risk in each individual case should be weighed. This should be discussed with a woman even before she decides to start taking Charosette В® . In case of worsening, exacerbation of the disease or the onset of any of these conditions, the woman should first consult a doctor. The doctor should decide on the advisability of further use of the drug Charosette В® .
- stable hypertension, which develops against the background of taking Charozetta В® , or when ineffective antihypertensive therapy;
- thromboembolic disorders (including in the anamnesis); a woman should be warned about the possibility of relapse;
- prolonged immobilization associated with the operation or with the disease;
- Since it is impossible to exclude the biological effect of gestagens on the development of liver cancer, an individual assessment of the benefit-risk relationship in prescribing the drug to women with liver cancer should be conducted;
- Chloasma, especially in women with chloasma during pregnancy in history (women with a predisposition to chloasma should avoid exposure to sunlight or ultraviolet radiation during the application of Charosette В® ).
PREGNANCY AND LACTATION
In pregnancy, the use of the drug is contraindicated.
The results of preclinical studies have shown that very high doses of gestagens can cause masculinization of the female fetus.
Extensive epidemiological studies revealed no increased risk of birth defects in children whose mothers took oral contraceptives prior to pregnancy, or a teratogenic effect with unintentional intake of oral contraceptives at an early gestation period. Charozette В® does not affect the amount or quality (concentrations of proteins, lactose or fats) of breast milk. However, a small amount of etonogestrel is excreted in breast milk. As a result, 0.01-0.05 Ојg of etonogestrel per kg of body weight per day can be delivered to the baby's body (based on consumption of 150 ml / kg / day of breast milk).
There is limited data on long-term follow-up of children whose mothers started taking Charosette В® during the 4th-8th week after childbirth. The duration of breastfeeding was 7 months, and children were monitored until reaching the age of 1.5 (n = 32) or up to 2.5 years (n = 14). Assessment of growth, physical and psychomotor development did not reveal any differences with babies whose mothers used IUDs containing copper. The available data indicate that the preparation Charosette В® can be used during lactation. Nevertheless, it is necessary to carefully monitor the development and growth of an infant whose mother takes the drug Charosette В® .
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: the presence at this time or in an anamnesis of severe liver disease (as long as the liver function indices are not normalized). Contraindicated in hepatic insufficiency, incl. in the anamnesis.
APPLICATION IN ELDERLY PATIENTS
Before the appointment of the drug should carefully collect anamnesis in women and conduct a thorough gynecological examination to exclude pregnancy. Before the appointment of the drug should determine the cause of menstrual disorders, for example, oligomenorrhoea and amenorrhea. The interval between the control medical examinations is determined by the doctor in each individual case (the frequency of the examinations is at least 1 time per year). If the prescribed drug can affect the latent or existing disease, an appropriate schedule of control medical examinations should be made.
Despite the regular administration of Charozette В® , occasional spotting can sometimes occur. If bleeding is very frequent and irregular, consider using another method of contraception. If the above symptoms are stable, then in this case it is necessary to exclude organic pathology. The tactic for amenorrhea during the use of the drug depends on whether the tablets were taken according to the instructions, and may include a pregnancy test. In case of pregnancy, the drug should be stopped.
In case of acute or chronic violations of the liver, a woman should consult a specialist for examination and consultation.
Women should be informed that Charosette В® does not protect against HIV infection and other sexually transmitted diseases.
The effectiveness of gestagen-containing oral contraceptives can be reduced in case of missing tablets, gastrointestinal disorders or when taking other medications.
Changes in the nature of menstruation
During the use of gestagen-containing contraceptives in some women, vaginal bleeding may become more frequent or more prolonged, while in other women these bleeding may become more rare or even stop. These changes are often the reason that a woman refuses this method of contraception, or ceases to strictly follow the doctor's instructions. With detailed consultation with women who decide to start taking Charozette В® , the doctor should discuss the possibility of such changes in the nature of the menstrual cycle. Evaluation of vaginal bleeding should be based on a clinical picture and may include an examination to exclude malignant neoplasms or pregnancy.
Development of follicles
With the intake of all low-dose hormonal contraceptives, follicles develop, and occasionally the size of the follicle can reach sizes larger than 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.
Data on combined oral contraceptives have shown that the use of hormonal contraceptives can affect the results of some laboratory tests, including biochemical parameters of liver, thyroid, adrenal and kidney function, serum levels (transport) proteins, for example, globulin , binding corticosteroids, lipid / lipoprotein fractions, carbohydrate metabolism and blood coagulation and fibrinolysis. Usually these changes remain within the normal range. It is not known to what extent this also applies to contraceptives containing only gestagen.
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 is slightly increased. This increased risk disappears gradually within 10 years after discontinuation of oral contraceptives, it is not associated with the duration of application, and is dependent on the woman's age at the time of use of combined oral contraceptives. Expected number of diagnosed cases of breast cancer among 10,000 women using combined oral contraceptives (for 10 years after the termination of their use), with respect to women who never let them take over the same period, calculated for the respective age groups and is presented in the table below .
Age group Expected number of cases among women using combined oral contraceptives expected number of cases among women, do not apply oral contraceptives
16-19 4.5 4
20-24 17.5 16
25-29 48.7 44
30-34 110 100
35-39 180 160
40-44 260 230
The risk in women using oral contraceptives which contain only progestogen, e.g., Charozetta preparation В®Possibly similar to that when using a combined oral contraceptives. However, the data for oral contraceptives containing only progestin, is not so certain. Compared with the risk of breast cancer throughout their lives, increasing the risk associated with taking combined oral contraceptives is small. Breast cancer is diagnosed in women using combined oral contraceptives, it has a tendency to be less clinically advanced than cancers diagnosed in women who never used COCs. Increased risk in women using combined oral contraceptives, possibly due to earlier diagnosis, biological effects of the drug or a combination of these two factors.
Epidemiological studies have established a link between the use of combined oral contraceptives and an increased incidence of venous thromboembolism (VTE, deep venous thrombosis and pulmonary embolism). Although the clinical significance of these data for desogestrel as contraceptive, containing no estrogenic component is unknown, use of the drug Charozetta В® should be canceled in the case of thrombosis. It should consider removing the dosing Charozetta В® in case of prolonged immobilization associated with surgery or disease.
Although progestogens may influence the resistance of peripheral tissues to insulin and glucose tolerance, there is no evidence that there is a need to change the therapeutic scheme for patients with diabetes who use oral contraceptives gestagensoderzhaschie. However, women with diabetes should be monitored closely during the first month of the drug.
Bone mineral density
Application preparation Charozetta В® leads to a decrease in serum estradiol levels to a level corresponding to the early follicular phase. So far, it is unknown whether the decrease has any clinically relevant effect on bone mineral density.
Prevention of ectopic pregnancy
Prevention of ectopic pregnancy gestagensoderzhaschimi traditional oral contraceptives ( "mini-pill") is not as effective as when combined oral contraceptives, since the application of the "mini-pill" ovulation occurs frequently. Despite the fact that Charozetta В® effectively inhibits ovulation, in the case of amenorrhea or abdominal pain should be deleted ectopic pregnancy in the differential diagnosis.
Preparation Charozetta В® contains not more than 65 mg of lactose, however, women with rare inherited disorders associated with galactose intolerance, lapp lactase deficiency or glucose-galactose malabsorption, should refrain from taking the drug.
Impact on the ability to drive vehicles and manage mechanisms
Based on the pharmacodynamic profile, it is believed that the drug Charozetta В® does not influence the ability to drive and operate machinery.
No reports of serious side effects as a result of an overdose.
Symptoms: nausea, vomiting, and in young girls - a slight vaginal bleeding.
Treatment: there is no specific antidote. Conduct symptomatic therapy.
The interaction between oral contraceptives and other drugs may lead to breakthrough bleeding and / or to reduce contraceptive efficacy. The literature reports the following interactions (mainly with combined contraceptives but occasionally also been reported in relation gestagensoderzhaschih contraceptives).
May arise interaction 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 the drug Charozetta В®or choose another method of contraception. Barrier contraceptive method should be used during application of said preparations and for 28 days after cessation of administration. For women receiving prolonged treatment with hepatic enzyme inducers, should consider using a non-hormonal method of contraception.
In the application of the activated carbon absorption desogestrel present in the tablet can be reduced and, consequently, may decrease contraceptive efficacy. In this case, to proceed in accordance with recommendations for the missed for receiving pills.
Hormonal contraceptives may affect the metabolism of other drugs. Accordingly, the concentration of drug in plasma and tissues may either increase (e.g., cyclosporin) and decrease.
To identify possible interactions should read the instructions for use of these drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be kept out of the reach of children, dry, dark place at a temperature of from 2 В° to 30 В° C. Shelf life - 3 years.