Composition, form of production and packaging
The tablets covered with a film shell of white or almost white color, round, biconcave, with engraving "D" on one side and "75" on the other.
1 tab.
desogestrel 75 Ојg
Auxiliary substances: lactose monohydrate - 55.095 mg, potato starch - 6.5 mg, povidone K30 - 1.95 mg, silicon dioxide colloid - 0.65 mg, stearic acid 50 - 0.65 mg, all-rac -? - tocopherol - 0.08 mg.
The composition of the shell: opedrai II white (talc - 0.148 mg (14.8%), macrogol 3000 - 0.202 mg (20.2%), titanium dioxide (E171) 0.25 mg (25%), polyvinyl alcohol 0.4 mg (40%)) 1 mg.
28 pcs. - blisters (1) - packages of laminated aluminum foil (1) - packs of cardboard.
28 pcs. - blisters (1) - packages of laminated aluminum foil (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
PHARMACHOLOGIC EFFECT
Gestagen-containing contraceptive for oral administration, the active ingredient of which is desogestrel.
Like other gestagen-containing oral contraceptives (mini-pili), Lactineth В® -Richter is best suited for use during breastfeeding and for women who are contraindicated or who do not want to take estrogens. In contrast to mini-pills, the contraceptive effect of LactitetВ®-Richter is achieved mainly by suppressing ovulation. Other effects include an increase in the viscosity of cervical mucus.
When using Lactaneth В® -Richter in the first 56 days, the frequency of ovulation does not exceed 1%, after stopping the 56-day administration of the drug, 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 incidence of pregnancy in 100 women during the year of use of the contraceptive) desogestrel was 0.4 in the group of all the patients included in the study.
The Pearl Index of the drug Lactiton ®- Richter is comparable to the Perl index of combined oral contraceptives (POC) in the general population of women taking oral contraceptives. Administration of the drug Lactiton ® -Richter leads to a decrease in the concentration of estradiol in the blood plasma to values ​​that are characteristic of the early follicular phase. At the same time, there were no clinically significant changes in the carbohydrate, lipid metabolism and hemostasis parameters.
PHARMACOKINETICS
Suction
When ingestion, desogestrel is absorbed rapidly. The mean C max in the blood serum is reached after 1.8 h (T max ) after taking the tablet. Bioavailability of etonogestrel is about 70%.
Distribution
Etonogestrel in 95.5-99% binds to blood plasma proteins, mainly with albumin and to a lesser extent with sex hormone binding globulin (GSHG).
C ss in the blood plasma are established after 4-5 days.
Metabolism
Desogestrel by hydroxylation and dehydrogenation is metabolized into the active metabolite ethonogestrel. Ethonogestrel is metabolized by the formation of sulfate and glucuronide conjugates.
Excretion
The mean T 1/2 of etonogestrel is about 30 hours, both with single and repeated administration. Etonogestrel and its metabolites are excreted by the kidneys and through the intestine (in a ratio of 1.5: 1) in the form of free steroids and conjugates.
In lactating mothers, etonogestrel is excreted in breast milk in a ratio of milk / serum 0.37-0.55. Thus, with an approximate milk consumption of the mother in the amount of 150 mg / kg body weight / day, the newborn can receive 0.01-0.05 Ојg etonogestrel / kg / day.
INDICATIONS
- Contraception.
DOSING MODE
In the absence of previous application of hormonal contraceptives (during the last month), the taking of tablets starts from the 1st day of the menstrual cycle to 1 tablet / day, if possible at the same time of the day, following in the direction indicated on the package, so that the interval between admission two tablets was 24 hours, if necessary with a small amount of liquid. This drug does not require a break in admission. Each next package should be started immediately after the end of the previous one.
The first drug intake
Women who did not take oral contraceptives in the previous month
The first tablet should be taken from the first day of the menstrual cycle (menstruation). In this case, no additional methods of contraception are required.
You can start taking tablets from the 2nd-5th day of menstruation, but in this case, additional contraceptive methods should be used in the first cycle in the first 7 days of taking the tablets.
Transition from a combined hormonal contraceptive (PDA, vaginal ring or transdermal patch)
The preparation of LactanethВ®-Richter should be started the day after the last active PDK tablet (the 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.
The drug LactitetВ®-Richter can also be started the day after the end of the usual interval in taking the tablets, plaster, ring or the day after receiving the placebo tablets of the previous PDA (that is, the day when you would start using a new PDA package , insert a new ring or glue a new patch), but during the first 7 days of taking the tablets, an additional barrier method of contraception is recommended.
Transition from other drugs containing only gestagen (minipili, injection, implant or gestagen-releasing intrauterine system)
A woman who takes a mini-drip can switch to taking Lactaneth В®- Richter on any given day. A woman who uses an implant or an intrauterine system - the day they are removed. A woman who uses injectable contraceptive forms - the day the next injection is to be given. In all these cases, an additional contraceptive method is not required.
Admission after abortion in the first trimester of pregnancy
After abortion in the first trimester of pregnancy, it is recommended to start taking the drug immediately after the abortion, in this case there is no need for additional methods of contraception.
Admission of the drug after childbirth or after termination of pregnancy in the second trimester
Admission of the drug begins no earlier than 21-28 days after the termination of pregnancy in the second trimester or after childbirth. If the drug is supposed to start later, then it is necessary to use the barrier method of contraception during the first 7 days. In addition, if there was unprotected sexual contact before starting the use of the drug, pregnancy should be excluded or the beginning of the drug on the first day of the next menstruation (during the restoration of the menstrual cycle) should be postponed.
Missed (forgotten) tablets
The effectiveness of the contraceptive is reduced if more than 36 hours have passed between two tablets. If the break does not exceed 12 hours , the contraceptive effect does not decrease, and the use of an additional contraceptive method is not required. The intake of the remaining tablets is continued according to the usual schedule.
In the case of a more than 12-hour break, the contraceptive effect may decrease. To achieve effective blocking of the hypothalamic-pituitary-ovarian system, it is necessary to take the drug daily for 7 days. Thus, with a break of more than 12 hours, the drug is continued in normal mode, however, additional (barrier) methods of contraception must be used in the next 7 days. If the intake of the pill was missed during the first week of the drug and in the previous 7 days there was an unprotected sexual intercourse, it is impossible to exclude the possibility of pregnancy.
Measures taken in case of vomiting
If vomiting develops within 3-4 hours after taking the pill, then the tablet is not fully absorbed. In this case, you should do the same as in the case of missed tablets.The necessary tablet (the necessary pills) should be replenished from another package.
SIDE EFFECT
In clinical studies, desogestrel at a dose of 75 mcg, side effects were most often noted (> 2.5%): irregular spotting, acne, mood changes, breast tenderness, nausea and weight gain. Undesirable adverse reactions are presented according to the class of organ systems according to the MedDRA classification and frequency of occurrence: often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10 000, <1/1000).
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.
Frequency of adverse reactions
Often (? 1/100, <1/10) Not infrequently (? 1/1000, <1/100) Rarely (? 1/10 000, <1/1000)
Disorders of the psyche
Change in mood, decreased libido, depressive disorder
From the nervous system
Headache
From the side of the organ of vision
Intolerance to contact lenses
From the digestive system
Nausea, vomiting
From the skin and subcutaneous tissues
Acne Alopecia Skin rashes, hives, erythema nodosum
From the genitals and breast
Soreness of the mammary glands, irregular menstrual bleeding, amenorrhea Dysmenorrhea, ovarian cyst, vaginitis Discharge from the mammary glands, ectopic pregnancy
General reactions
Increased body fatigue
In women who received (combined) oral contraceptives, various serious adverse effects were rarely observed: venous and arterial thrombosis 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
CONTRAINDICATIONS
The use of the drug Lactiton В® -Richter is contraindicated in the presence of at least one of the following conditions; if any of these conditions occur for the first time during the use of Lactaneth В® -Richter, stop taking it immediately:
- Presence at present or in an anamnesis of venous thromboembolism (including deep vein thrombosis of the lower limbs, pulmonary thromboembolism);
- severe liver disease at present or in anamnesis (before the normalization of liver function);
- hepatic insufficiency at present or in the anamnesis;
- established or suspected malignant hormone-dependent tumors (including breast cancer);
bleeding from the vagina of an unclear etiology;
- established or suspected pregnancy;
- Children and adolescents under 18 years of age - due to the lack of information confirming the efficacy and safety of the drug in girls and girls under the age of 18.
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- Hypersensitivity to desogestrel or any other component of the drug.
Carefully
If any of the following conditions / risk factors are present, the benefits of using gestagens and the possible risk for each woman should be weighed. This should be discussed with the woman even before she decides to start taking the drug. 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 whether to continue using Lactaneth В® -Richter.
- Persistent arterial hypertension (with a significant increase in blood pressure or inefficiency of antihypertensive therapy, the drug should be discontinued).
- Long-term immobilization associated with surgical intervention, disease or trauma.
- Since it is impossible to exclude the biological influence of gestagens on the development of liver cancer, an individual assessment of the benefit-risk ratio for the administration of the drug to women with liver cancer should be carried out.
- Chloasma, especially in women with chloasma during pregnancy in the anamnesis.
- Diabetes mellitus (because of the possible effect of progestogens on peripheral insulin resistance and glucose tolerance).
"Porphyria."
- Systemic lupus erythematosus.
- Herpes (during pregnancy in anamnesis).
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy. In pre-clinical studies with the administration of progestogen very high doses observed masculinization of the female fetus.
In epidemiological studies, there was no increased risk of a teratogenic effect and congenital developmental defects among children whose mothers took oral hormonal contraceptives prior to pregnancy or unintentionally - in the early stages of pregnancy.
Like other preparations containing only progestogen, LactitetВ®-Richter does not affect the quality and quantity of maternal milk, but a small amount of the metabolite of desogestrel (etonogestrel) is excreted in the mother's milk and is approximately 0.01-0.05 Ојg / kg / day (with the amount of breast milk 150 ml / kg / day). The results of a 7-month follow-up showed no increased risks for breastfed infants when assessing their growth, psychomotor and physical development.
Nevertheless, careful monitoring of the development and growth of the infant during breastfeeding is necessary if the woman uses Lactaneth В® -Richter for the purpose of contraception.
APPLICATION FOR FUNCTIONS OF THE LIVER
There is no data on the use of the drug in patients with impaired renal function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in the use of severe liver disease, incl. in the anamnesis (before normalization of indicators of liver function), as well as with hepatic insufficiency, incl. in the anamnesis.
SPECIAL INSTRUCTIONS
Medical examination / counseling
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, such as 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 use of the drug Lactiton В®- Richter, 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 Lactiton В®- Richter does not protect against HIV infection (AIDS) and other sexually transmitted diseases.
Decreased efficiency
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 a woman who decided to start taking Laktionet В® -Richter, 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. Usually these enlarged follicles disappear spontaneously. Often this is asymptomatic, but in some cases there is a slight pain in the lower abdomen. Surgical intervention is rarely required.
Laboratory research
Data from the CCP showed that the use of hormonal contraceptives may affect the results of some laboratory tests, including biochemical parameters of liver, thyroid, adrenal and kidney function, the content of transport proteins of blood plasma (eg, globulin, corticosteroids, lipid fractions /липопротеинов), показатели углеводного обмена и показатели свертываемости крови и фибринолиза. Usually, these changes are within the normal range. It is unknown to what extent this also applies to contraceptives containing only progestin.
Mammary cancer
The risk of breast cancer increases with age. During the application of the CPC is a risk that women will be diagnosed with breast cancer increases slightly. This increased risk gradually declines for 10 years after cessation of use of oral contraceptives, it is not associated with the duration of application, and is dependent on the woman's age at the time of application of the CPC. Expected number of diagnosed cases of breast cancer among 10,000 women using the CPC (for 10 years after the termination of their use), with respect to women who had not used them during the same period, calculated for the respective age groups and is presented in the table below.
Age group Expected number of cases among women who had used PDAs Expected number of cases among women do not apply the CCP
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 of women who use oral contraceptives which contain only progestogen, e.g., a drug Laktinet В®-Rihter possibly similar to that when using CPC. 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 the reception of the CPC, it is small. Women using PDA, diagnosed earlier clinical stages of breast cancer than women never let them apply. The increased risk in women who use PDAs possibly due to earlier diagnosis, biological effects of the drug or a combination of these two factors.
venous thromboembolism
Epidemiologic studies have established a link between the application of the CPC and the increased incidence of venous thromboembolism (VTE, deep venous thrombosis and pulmonary embolism). Although the clinical significance of these data for desogestrel as a contraceptive, containing no estrogenic component is unknown, the drug Laktinet В® -Rihter should be canceled in the case of thrombosis. Consideration should be given drug withdrawal Laktinet В® -Rihter in case of prolonged immobilization associated with surgery or disease.
Diabetes
Although progestogens may affect on peripheral insulin resistance and glucose tolerance usually correct dose and dosing regimen hypoglycemic agents in patients with diabetes mellitus is needed. However, such patients should be monitored closely during the first month of the drug.
Bone mineral density
Application preparation Laktinet В® -Rihter leads to a decrease in plasma oestradiol concentrations to values 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 the application of the CPC, as the application of mini-pill ovulation occurs frequently. Despite the fact that Laktinet В® -Rihter effectively inhibits ovulation, in the case of amenorrhea or abdominal pain should be deleted ectopic pregnancy in the differential diagnosis.
Chloasma
chloasma may occur from time to time, especially in women who have been pregnant noted chloasma history. Women with susceptibility to chloasma should avoid exposure to sunlight or UV radiation during the drug Laktinet В® -Rihter.
Excipients
Patients with lactose intolerance should be borne in mind that one tablet Laktinet В® -Rihter contains 55,095 mg lactose monohydrate. Patients with rare hereditary conditions such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this drug.
Impact on the ability to drive vehicles and manage mechanisms
Based on the pharmacodynamic profile, it is believed that the drug Laktinet В® -Rihter not affect the ability to drive vehicles and mechanisms.
OVERDOSE
Symptoms: nausea, vomiting, spotting / vaginal bleeding.
Treatment: there is no specific antidote. Symptomatic therapy.
DRUG INTERACTION
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 (mostly with the CCP, but sometimes reported and gestagensoderzhaschih contraceptives).
Hepatic metabolism
possible drug interactions with drugs that induce microsomal enzymes, resulting in increased clearance of sex hormones, e.g., hydantoins (phenytoin), barbiturates (phenobarbital), primidone, carbamazepine, rifampicin; and possibly also oxcarbazepine, rifabutin, topiramate, felbamate, ritonavir, nelfinavir, griseofulvin and products containing St. John's wort .Women using any of these drugs should temporarily use a barrier method in addition to the drug Laktinet В® -Rihter or select another method of contraception. Barrier contraceptive method should be used during application of these preparations and for 28 days after cessation of administration. For women receiving prolonged treatment with hepatic enzyme inducers, should consider the possibility of using non-hormonal method of contraception.
In the application of the activated carbon desogestrel absorption can be reduced and, consequently, may decrease contraceptive efficacy. In this case it is necessary to follow recommendations regarding missed pills. Hormonal contraceptives may affect the metabolism of other drugs. Accordingly, the plasma concentration of the drug in tissues and may either increase (e.g., cyclosporin) and decrease.
To evaluate possible drug interactions should obtain information from instructions simultaneously used drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The preparation should be stored in their original packaging in reach of children at a temperature not higher than 25 В° C. Shelf life - 3 years. Do not use the drug after the expiration date.
