Spiral intrauterine Mirena 20mcg day
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Levonorgestrel
Composition
1 intrauterine device contains: levonorgestrel 52 mg. Auxiliary substance: polydimethylsiloxane elastomer 52 mg.
Pharmacological effect
Mirena is an intrauterine contraceptive. It is a T-shaped elastomer system (device), the vertical rod of which consists of a levonorgestrel containing container covered with a special membrane through which controlled diffusion of levonorgestrel at 20 mcg / day (during the initial period) occurs continuously. The levonorgestrel, which enters directly into the uterine cavity, has direct local effect on the endometrium, preventing proliferative changes in it and thereby reducing its implant function, and also increases the viscosity of the cervical mucus cial channel that prevents penetration of sperm into the cavity matki.Levonorgestrel also has negligible systemic exposure, which manifests itself in the inhibition of ovulation including a tsiklov.Mirena reduces the amount of menstrual bleeding, pre- and reduces menstrual pain. In women with menorrhagia, after 2-3 months of using Mirena, the volume of menstrual bleeding decreases by 88%. Reducing menstrual blood loss reduces the risk of developing iron deficiency anemia. Efficacy Mirena in preventing endometrial hyperplasia during ongoing estrogen therapy was equally high in oral and transdermal estrogen use.
Pharmacokinetics
Absorption: After the administration of the drug Mirena, the levonorgestrel begins to be immediately released into the uterus, as evidenced by the measurement data of its concentration in the blood plasma. High local exposure of the drug in the uterus, necessary for local exposure of the drug Mirena to the endometrium, provides a high concentration gradient from endometrium to myometrium (concentration of levonorgestrel in the endometrium exceeds its concentration in myometrium more than 100 times) and low concentrations of levonorgestrel in the blood plasma (concentration of levonorgestrel in the endometrium exceeds its concentration in the blood plasma by more than 1000 times). The rate of release of levonorgestrel into the uterus in vivo initially is about 20 mcg / day, and after 5 years it drops to 10 mcg / day. After the administration of Mirena, levonorgestrel is detected in blood plasma after 1 hour. Cmax is reached 2 weeks after the administration of Mirena.In accordance with the decreasing rate of release, the median concentration of levonorgestrel in the blood plasma of women of reproductive age with a body weight above 55 kg decreases from 206 pg / ml (the 25th-75th percentile: 151 pg / ml-264 pg / ml) determined after 6 months, up to 194 pg / ml (146 pg / ml-266 pg / ml) after 12 months and up to 131 pg / ml (113 pg / ml-161 pg / ml) after 60 months. Distribution: Levonorgestrel binds non-specifically serum albumin and specifically with sex hormone-binding globulin (SHBG). About 1-2% of circulating levonorgestrel is present as a free steroid, while 42-62% is specifically associated with SHBG. During the use of the drug Mirena concentration of SHBG decreases. Accordingly, the fraction associated with SHBG during the use of the drug Mirena decreases, and the free fraction increases. The average apparent Vd of levonorgestrel is about 106 liters. The pharmacokinetics of levonorgestrel depends on the concentration of HBHG, which, in turn, is influenced by estrogens and androgens. With the use of the drug Mirena, a decrease in the average concentration of SHBG by approximately 30% was observed, which was accompanied by a decrease in the plasma concentration of levonorgestrel. This indicates the nonlinearity of levonorgestrel pharmacokinetics over time. Given the predominantly local action of the drug Mirena, the effect of changes in systemic concentrations of levonorgestrel on the efficacy of the drug Mirena is unlikely. It was shown that body weight and the concentration of SHBG in blood plasma affect the systemic concentration of levonorgestrel. those. with low body mass and / or high SHBG concentration, the concentration of levonorgestrel is higher. In women of reproductive age with low body weight (37-55 kg), the median concentration of levonorgestrel in blood plasma is about 1.5 times higher. In postmenopausal women who use Mirena simultaneously with estrogen intravaginally or transdermally, the median concentration of levonorgestrel in blood plasma decreases with 257 pg / ml (25th-75th percentile: 186 pg / ml-326 pg / ml) determined after 12 months, to 149 pg / ml (122 pg / ml-180 pg / ml) after 60 months. With the use of the drug Mirena simultaneously with oral estrogen therapy, the concentration of levonorgestrel in the blood plasma, determined after 12 months, increases to about 478 pg / ml (25th-75th percentile: 341 pg / ml-655 pg / ml), due to induction HSPG synthesis. Metabolism: Levonorgestrel is largely metabolized.The main metabolites in the blood plasma are unconjugated and conjugated forms of 3α, 5β-tetrahydrolevonorgestrel. Based on the results of in vitro and in vivo studies, the main isoenzyme involved in the metabolism of levonorgestrel is CYP3A4. The isoenzymes CYP2E1, CYP2C19 and CYP2C9 may also be involved in the metabolism of levonorgestrel, but to a lesser extent. Excretion: The total clearance of levonorgestrel from blood plasma is about 1 ml / min / kg. Unchanged levonorgestrel is displayed only in trace amounts. Metabolites are excreted through the intestines and by the kidneys with an excretion rate of approximately 1.77. T1 / 2 in the terminal phase, represented mainly by metabolites, is about a day.
Indications
Contraception; idiopathic menorrhagia; prevention of endometrial hyperplasia during estrogen replacement therapy.
Contraindications
Pregnancy or suspicion of it; inflammatory diseases of the pelvic organs (including recurrent); infections of the lower urinary tract; postpartum endometritis; septic abortion for the last 3 months; cervicitis; diseases accompanied by increased susceptibility to infections, cervical dysplasia ; malignant neoplasms of the uterus or cervix; progestogen-dependent tumors, including breast cancer; pathological uterine bleeding of unknown etiology; congenital and acquired uterine anomalies, including fibroids leading to deformation of the uterus, acute liver disease, liver tumors, over 65 years of age (studies in this category of patients have not been conducted), hypersensitivity to the drug.
Precautionary measures
With caution and only after consulting a specialist should use the drug in the following conditions. It is necessary to discuss the feasibility of removing the system in the presence or first occurrence of any of the following conditions: migraine, focal migraine with asymmetric loss of vision or other symptoms indicating transient cerebral ischemia, an unusually severe headache; jaundice; severe hypertension; severe circulatory disorders, incl.stroke and myocardial infarction; congenital heart defects or valvular heart disease (due to the risk of developing septic endocarditis); diabetes.
Use during pregnancy and lactation
Miren cannot be used during pregnancy or suspected her. If pregnancy occurs in a woman while using Mirena, it is recommended to remove the IUD, since any contraceptive left in situ increases the risk of miscarriage and premature birth. Removing Mirena or probing the uterus can also cause miscarriage. If it is impossible to remove the intrauterine contraceptive carefully, you need to think about the feasibility of abortion. If a woman wants to preserve a pregnancy, she should be informed about the risk and possible consequences of premature birth for the child. In such cases, the course of pregnancy should be carefully monitored. It is necessary to exclude an ectopic pregnancy. A woman should be explained that she should report all the symptoms suggesting pregnancy complications, in particular, pain such as colic in the lower abdomen, accompanied by fever. Despite the intrauterine use and local effect of the hormone, its teratogenic effect (especially virilization) cannot be completely excluded. Due to Mirena's high contraceptive effectiveness, clinical experience related to pregnancy outcomes in her application is limited. However, the woman should be informed that there is no evidence of birth defects caused by Mirena's use in cases of continuing pregnancy before giving birth without removing the IUD. Levonorgestrel was found in breast milk, but it is unlikely that it would increase the risk for the baby at doses released by Miren, located in the uterus. It is assumed that the use of any progestin-only method of contraception 6 weeks after birth does not have a serious impact on the growth and development of the child. Only progestin methods do not affect the quantity and quality of breast milk. Rare cases of uterine bleeding have been reported in women using Mirena during lactation.
Dosage and administration
Mirena is inserted into the uterine cavity and remains effective for five years.The rate of lsvonorgsgrel release in vivo at the beginning is about 20 μg per day and decreases after five years to about 11 μg per day. The average release rate of levonorgestrel is about 14 micrograms per day for up to five years. Mirena can be used in women receiving hormone replacement therapy in combination with oral or trandermal estrogen preparations that do not contain gestagens. When properly installed, Mirena, carried out in accordance with the instructions for use, Pearl index (an indicator reflecting the number of pregnancies in 100 women who use contraceptive during the year) is approximately 0.1% per year. 11In expulsion or perforation, the Pearl Index may increase.
Side effects
Side effects more often develop in the first months after Mirena is introduced into the uterus; with prolonged use, they gradually disappear. The following undesirable effects were described in women using Mirena, but their relationship with the use of the drug was not confirmed in all cases. Changes in the nature of uterine bleeding and benign ovarian cysts are common side effects (noted by more than 10% of women using Mirena). Various types of changes in the nature of bleeding (frequent, prolonged or severe bleeding, spotting, oligo- and amenorrhea) are observed in all women using Mirena. The average number of days and months when spotting is noted in women of childbearing age gradually decreases from 9 to 4 days during the first 6 months after the installation of the IUD. The proportion of women with prolonged (more than 8 days) bleeding decreases from 20 to 3% in the first 3 months of using Mirena. In clinical studies, it was found that in the first year of Mirena use, 17% of women had amenorrhea for at least 3 months. When Mirena is used in combination with estrogen replacement therapy, in the first months of treatment in most women in the perimenopausal and postmenopausal period spotting and irregular bleeding are observed. In the future, their frequency decreases, and approximately 40% of women receiving this therapy in the last 3 months of the first year of treatment completely disappear.Bleeding disorders are more common in the perimenopausal period than in the postmenopausal period. The frequency of detecting benign ovarian cysts depends on the diagnostic method used. According to clinical trials, enlarged follicles were diagnosed in 12% of women using Mirena. In most cases, an increase in follicles was asymptomatic and disappeared within 3 months.
Interaction with other drugs
The effectiveness of hormonal contraceptives may decrease when taking drugs that alter the work of liver enzymes, in particular primidone, barbiturates, difenina, carbamazepine, rifampicin, oxcarbazepine; suggest that griseofulvin also acts. The effect of these drugs on contraceptive activity of Mirenin has not been studied, it is probably not essential, since Mirena has mainly local effects.
special instructions
Before installing the drug Mirena, pathological processes in the endometrium should be excluded, since in the first months of its use irregular bleeding / spotting is often noted. Pathological processes in the endometrium should also be excluded if bleeding occurs after the start of estrogen replacement therapy in a woman who continues to use Mirena, previously prescribed for contraception. Appropriate diagnostic measures should also be taken when irregular bleeding develops during long-term treatment. Mirena's preparation is not used for post-coital contraception. Mirena's preparation should be used with caution in women with congenital or acquired valvular heart disease, bearing in mind the risk of septic endocarditis. When installing or removing an IUD, these patients should be given antibiotics for prophylaxis. Low-dose levonorgestrel can affect glucose tolerance, and therefore its plasma concentration should be regularly monitored in women with diabetes who use Mirena. As a rule, dose adjustment of hypoglycemic drugs is not required. Some manifestations of polyposis or endometrial cancer may be masked by irregular bleeding.In such cases, additional examination is necessary to clarify the diagnosis. Mirena's preparation does not apply to first-choice drugs for young, never-pregnant women, or for postmenopausal women with severe uterine atrophy. Available data indicate that the use of Mirena does not increase the risk of developing breast cancer in postmenopausal women under the age of 50 years. Due to the limited data obtained during the study of the drug Mirena according to the indications Prevention of endometrial hyperplasia during estrogen replacement therapy, the risk of breast cancer with the use of the drug Mirena according to this indication cannot be confirmed or disproved. Oligo- and amenorrhea: Oligo- and Amenorrhea in women of fertile age develops gradually, in about 57% and 16% of cases by the end of the first year of using Mirena, respectively. If menstruation is absent within 6 weeks after the start of the last menstruation, pregnancy should be excluded. Repeated pregnancy tests for amenorrhea are not necessary unless other signs of pregnancy are present. When Mirena is used in combination with permanent estrogen replacement therapy, most women gradually develop amenorrhea during the first year. Inflammatory diseases of the pelvic organs: A conductor tube helps to protect the drug Mirena from infection during installation, and the device for administering the drug Mirena is specially designed to minimize the risk of infection. Inflammatory diseases of the pelvic organs in patients using IUDs are often referred to as sexually transmitted diseases. It has been established that the presence of multiple sexual partners is a risk factor for infections of the organs of the small pelvis. Inflammatory diseases of the pelvic organs can have serious consequences: they can impair fertility and increase the risk of ectopic pregnancy. As with other gynecological or surgical procedures, severe infection or sepsis (including streptococcal sepsis group A) can develop after the IUD is installed, although this happens extremely rare. In recurrent endometritis or inflammatory diseases of the pelvic organs, as well as in severe or acute infections resistant to treatment for several their days, the drug Mirena should be removed.If a woman has constant pain in the lower abdomen, chills, fever, pain associated with sexual intercourse (dyspareunia), prolonged or heavy bleeding / vaginal bleeding, changes in the nature of vaginal discharge, you should immediately consult with your doctor. Severe pain or fever, which appears shortly after the installation of the IUD, may indicate the presence of a serious infection that must be treated immediately. Even in cases where only individual symptoms indicate the possibility of infection, bacteriological examination and monitoring are indicated. Expulsion: Possible signs of partial or complete expulsion of any IUD are bleeding and pain. Contractions of the uterus muscles during menstruation sometimes lead to a shift of the IUD or even to pushing it out of the uterus, which leads to the cessation of contraceptive action. Partial expulsion may reduce the effectiveness of Mirena. Since Mirena reduces menstrual blood loss, its increase may indicate an expulsion of the IUD. A woman is recommended to check the threads with her fingers, for example, while taking a shower. If a woman shows signs of an IUD moving or falling out or doesn’t feel the threads, you should avoid sexual intercourse or use other methods of contraception, and also see a doctor as soon as possible. If the position is wrong in the uterine cavity, the IUD should be removed. At the same time, a new system can be installed. It is necessary to explain to a woman how to check the threads of the drug Mirena. Perforation and penetration: Perforation or penetration of the body or cervix of the IUD rarely occurs, mainly during installation, and may decrease the effectiveness of Mirena. In these cases, the system should be removed. When delayed diagnosis of perforation and migration of the IUD, complications can occur, such as adhesions, peritonitis, intestinal obstruction, intestinal perforation, abscesses or erosion of adjacent internal organs. The risk of perforation of the uterus is increased in women with breastfeeding. There may be an increased risk of perforation when installing IUDs after childbirth and in women with a fixed uterus bend.The possibility of ectopic pregnancy should be considered in case of pain in the lower abdomen, especially if it is combined with the cessation of menstruation, or when a woman with amenorrhea begins to bleed. The frequency of ectopic pregnancy with the use of the drug Mirena is approximately 0.1% per year. The absolute risk of ectopic pregnancy in women using Mirena is low. However, if a woman with an established drug Mirena becomes pregnant, the relative probability of ectopic pregnancy is higher. Loss of filaments: If, during a gynecological examination of a thread to remove an IUD, it cannot be detected in the cervix, it is necessary to exclude pregnancy. The filaments can be drawn into the uterine cavity or the cervical canal and become visible again after the next menstruation. If pregnancy is excluded, the location of the filaments can usually be determined by careful probing with an appropriate tool. If it is not possible to detect the filament, it is possible that an expulsion of the IUD from the uterus has occurred. To determine the correct location of the system, an ultrasound scan can be performed. If it is unavailable or unsuccessful to determine the localization of the drug, Mirena performs an x-ray examination. Ovarian cysts: Since the contraceptive effect of Mirena is mainly due to its local effect, ovulatory cycles with follicle rupture are usually observed in women of fertile age. Sometimes atresia of the follicles is delayed, and their development may continue. Such enlarged follicles are clinically impossible to distinguish from ovarian cysts. Ovarian cysts were reported as an adverse reaction in approximately 7% of women using Mirena. In most cases, these follicles do not cause any symptoms, although sometimes they are accompanied by pain in the lower abdomen or pain during intercourse. As a rule, ovarian cysts disappear independently during two to three months of observation. If this does not happen, it is recommended to continue observation using ultrasound, as well as therapeutic and diagnostic measures. In rare cases, it is necessary to resort to surgery. Auxiliary substancescontained in the drug MirenaT-shaped basis of the drug Mirena contains barium sulfate, which becomes visible during X-ray examination. It is necessary to bear in mind that the drug Mirena does not protect against HIV infection and other sexually transmitted diseases. The effect on the ability to drive and control MechanismsNot observed.