A synthetic progestogen that transforms the endometrium minimizes ovulation by preventing the prepared egg from fertilizing. In addition, with its help, the receptors of the mucous membranes receive reduced sensitivity. In this article, we will consider a drug containing the named hormone.
Pharmacology
The drug "Levonorgestrel" is an estrogen that prevents the activation of sperm due to an increase in the viscous properties of mucus. The drug inside the uterus locally affects the fallopian tubes, endometrium, mucus consistency, as a result of which it reduces its activity.
When taken orally, the named drug is actively absorbed in the gastrointestinal tract, the bioindicators are up to 100%. In the blood, its components are maximally concentrated when 75 ml is taken once in 60 - 130 minutes. The hormone in question interacts with plasma and binding globulin components by about 50%.
Metabolism is focused on the liver, with the formation of pharmacologically passive metabolism. The main isoenzyme of this hormone is CYP3A4. The half-life can last up to 30 hours.
Properties
In response to the question "Levonorgestrel - what is this hormone?" you should be guided by the instructions for the drug of the same name and the recommendations of the attending doctor. The total difference is of the order of 1.0 ml / min / kg (from plasma). The hormone is eliminated mainly through the ureter, a small part is removed with feces.
With systemic therapy, the rate of entry into the uterus is no more than 20 μg daily, and after five years they drop to 11. On average, the rate of hormone release varies around 14 μg / 24 hours for 50-60 months.
Intrauterine therapy is allowed for women with hormone replacement therapy in conjunction with estrogens that do not include a progestogenic composition. Levonorgestrel is a hormone that is released into the plasma 60 minutes after ingestion. The maximum concentration in it is fixed after 14 days of use.
Indications
The use of this drug is possible with intrauterine therapy, as well as in the following cases:
- Menorrhagia of idiopathic orientation.
- Long-term contraceptive protection.
- Preventive measures for estrogen replacement recovery.
- Emergency postcoital contraception.
The hormone levonorgestrel, which has a wide range of effects, should be used only after a doctor's recommendation.
Application and dosage
The drug in question is activated by intrauterine injection - injected into the uterine cavity. It is used within 4 days after intercourse in a volume of 0.75 to 1.5 mg. Experts strongly advise against practicing emergency contraception more than once every six months.
To exclude a violation of the menstrual cycle, you must follow the recommended dosage without repeated use. You can not use the drug in question orally as a method of permanent contraception, as this provokes the appearance of side effects and reduces the effectiveness of the drug. In the case of uterine hemopoiesis after emergency contraception, an examination by a gynecologist is strongly recommended, and if menopause is disturbed for more than one week, conception should be delayed.
Only after the consultation and informed decision of the gynecologist in extraordinary cases is it possible to use the drug for contraception in minors in case of emergency.
How is levonorgestrel hormone used?
How does the use of the described hormone affect the body, and what to do to avoid side effects? Many people ask this question. Strict adherence to the recommendations of a specialist, adherence to dosage and adherence to instructions are guarantees of the safe use of the drug.
Before using the IUD, it is necessary to undergo an examination by a gynecologist, including checking the mammary glands, pelvic organs, and making a smear of the cervix.
Re-examination is carried out after 30-40 days after the installation of the spiral, then annually, and if there are appropriate prerequisites, more often. This intrauterine therapy is effective for 4 to 5 years. Its installation should be carried out exclusively by a doctor specializing in this area or having experience with the drug sorting in question.
Risks
In women taking drugs with gestagen, an increase in venous thrombosis at a critical moment is possible. With such symptoms, it is necessary to urgently take urgent measures for diagnosis and treatment.
After the removal of the IUD, fertility is resuscitated in six months in half of the women who applied, after 12 months - in more than 96 percent. Contraceptive focus is less effective for obese patients.
Contraindications
Asking the question "Levonorgestrel - what is this hormone?" all contraindications should be studied. Among them:
- Over (hyper) sensitivity, thrombophlebitis formations.
- Thromboembolism, changes in arteries.
- focus, pregnancy.
- With regard to ingestion: jaundice (including a history), pathological complications of the withdrawal of bile or liver, lactation period.
- Sexual maturity.
- In addition, for the IUD - infections of the urogenital node, relapses or active inflammation in the small pelvis, excesses of postpartum liver disease.
- Septic abortive intervention in the last trimester, dysplasia transformation of the uterine cervix, pathology with similar bleeding of unexplained origin, malignant formations.
- Coming or congenital anomalies that deform fibroids.
- Progestogenosis (tumor, including breast cancer).
Restrictions
The limiting factor is often relevant for therapeutic intervention inside the uterus if the following symptoms or chronic diseases occur:
- severe headaches, common and local migraine with visual impairment, other symptoms focused on the possibility of ischemic disease;
- obvious hypertension of the arterial direction, jaundice, complex destructive processes in the circulatory system, including heart attacks and strokes;
- diabetes mellitus.
It is necessary to immediately consult about the elimination of the IUD during the formation or the presence of any of these conditions.
Pregnancy and lactation period
Although levonorgestrel is a female hormone, it should not be used during pregnancy. If it occurs, the elimination of the system is recommended due to the fact that any increases the risk of premature birth and miscarriage. Uterine intubation or elimination of the system sometimes results in a miscarriage that occurs spontaneously. You will need to consult a specialist on the advisability of artificial termination of pregnancy if it is impossible to correctly remove the contraceptive.
If it is impossible to remove the intrauterine system and a persistent desire to maintain pregnancy, the patient should be aware of the possible consequences and risks for the child due to premature birth. In such cases, careful monitoring of the course of pregnancy is imperative. The patient should be informed that she should immediately report all symptoms that will help suggest a complication of the process.
Lactation
When breastfeeding and using Levonorgestrel, approximately one tenth of the drug enters the baby's body. Oral breastfeeding for emergency contraception should be discontinued for 1.5 days.
For a therapeutic system installed intrauterinely, as for any purely gestagenic method of contraception, it is characteristic that the use one and a half months after childbirth does not have a detrimental effect on the development and growth of the child, therefore, the drug most likely does not pose a risk to the fetus at the recommended dosage ...
Side Symptoms
And returning to the question "Levonorgestrel" - what is it? ", Let's consider the possible side effects and contraindications of the drug. They can occur in different body systems and represent the following symptoms:
- From the nervous system: fatigue, depression, headache, mood swings.
- Gastrointestinal tract. Vomiting, upset, cramping, bloating.
- Genitourinary organs. Bleeding, discharge, pain, candidiasis, the likelihood of the formation of malignant and benign tumors.
- Skin rashes, manifestation of eczema, itching, urticaria, acne.
- Others: edema, joint pain, pressure surges, sepsis.
In rare cases, epileptic seizures, seizures and fainting are possible.
Combination with other drugs
Studying "Levonorgestrel" (what kind of hormone), it is necessary to mention the possibility of its combination with other medicinal and organic preparations. In the case of using the substance under consideration with inducers of cytochrome P450 isoenzymes, a decrease in efficiency is possible due to an increase in its metabolic processes.
The following medicines can reduce the effect of Levonorgestrel:
- The group of barbiturates, "Tretinoin", "Carbamazepine", St. John's wort compounds and their composition.
- The effectiveness of anticoagulants, hypoglycemic, anticonvulsants decreases.
- "Levonorgestrel" increases the capacity of glucocorticosteroids in the blood, and is also capable of disorganizing metabolism.
- Due to the inhibition of the recirculation of sex steroids, which is due to the reorganization of the intestinal flora, an increase in menstrual bleeding may occur with the complex use of certain drugs.
One cannot but add, speaking about how "Levonorgestrel" is used, that this agent causes an increase in the side effects of other medications, there is no antidote to it. In case of overdose, it is required
LevonorgestrelLatin name
LevonorgestrelChemical name
(17alpha) -13-Ethyl-17-hydroxy-18,19-dinopregn-4-en-20-in-3-one
Gross formula
C 21 H 28 O 2Pharmacological group
Estrogens, gestagens; their homologues and antagonistsNosological classification (ICD-10)
N92 Heavy, frequent and irregular mensesN95.1 Menopause and climacteric state in women
Z30.0 General advice and advice on contraception
Z30.5 Supervision of contraceptive (intrauterine) use
CAS code
797-63-7Characteristic
Contraceptive (gestagen).
Pharmacology
Pharmacological action - contraceptive, gestagenic.It slows down ovulation and changes the endometrium, prevents the implantation of a fertilized egg. Increases the viscosity of cervical mucus, which interferes with the movement of sperm.
As part of the intrauterine therapeutic system (IUD), levonorgestrel has a direct local effect on the endometrium, fallopian tubes and the viscosity of the mucus of the cervical canal.
After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract, bioavailability is about 100%. C max in plasma after taking a single dose of 0.75 mg is noted after (1.6 ± 0.7) hours and is (14.1 ± 7.7) ng / ml. Binds to serum albumin (approximately 50%) and sex hormone binding globulin (47.5%). It is metabolized in the liver, the metabolites are pharmacologically inactive. T 1/2 - (24.4 ± 5.3) hours. It is excreted mainly in the urine, a small amount in the feces.
When using the IUD, the release rate of levonorgestrel into the uterine cavity is initially approximately 20 μg / day and decreases after five years to approximately 11 μg / day. The average release rate of levonorgestrel is approximately 14 mcg / day for up to 5 years. The IUD can be used in women receiving hormone replacement therapy in combination with progestogen-free oral or transdermal estrogen preparations.
Application
Inside. Emergency postcoital contraception in women (including after unprotected intercourse and if the contraceptive method used cannot be considered reliable).
For intrauterine therapy system. Contraception (long-term), idiopathic menorrhagia, prevention of endometrial hyperplasia during estrogen replacement therapy.
Contraindications
Hypersensitivity, pregnancy (or suspicion of it); for oral administration (additionally) - severe liver or biliary tract diseases, jaundice (including history), puberty, breastfeeding; for the IUD (optional) - existing or recurrent inflammatory diseases of the pelvic organs, infections of the lower urinary tract, postpartum endometritis, septic abortion within the last 3 months, cervicitis, diseases accompanied by an increased susceptibility to infections; dysplasia of the cervix, malignant neoplasms of the uterus or cervix, progestogen-dependent tumors, incl. mammary cancer; pathological uterine bleeding of unknown etiology, congenital or acquired uterine anomalies, incl. fibroids leading to deformation of the uterine cavity; acute diseases or tumors of the liver.
Restrictions on use
For the Navy. After consultation with a specialist: migraine, focal migraine with asymmetric loss of vision or other symptoms indicating transient cerebral ischemia; unusually severe headache; jaundice, severe arterial hypertension; severe circulatory disorders, incl. stroke and myocardial infarction.
The advisability of removing the IUD should be discussed in the presence or first occurrence of any of the conditions listed below.
Application during pregnancy and lactation
Contraindicated in pregnancy.
If pregnancy occurs while using the IUD, it is recommended that the system be removed. any intrauterine device left in situ increases the risk of miscarriage and premature birth. Removing the IUD or probing the uterus can lead to miscarriage. If it is not possible to carefully remove the intrauterine contraceptive, the advisability of artificial termination of pregnancy should be discussed. If a woman wants to preserve the pregnancy and the IUD cannot be removed, the patient should be informed about the risks and possible consequences of preterm birth for the baby. In such cases, the course of pregnancy should be closely monitored. It is necessary to exclude ectopic pregnancy (if a woman with an installed IUD becomes pregnant, the relative risk of ectopic pregnancy increases). The woman should be told that she should report all symptoms suggestive of a pregnancy complication, in particular colicky abdominal pain with fever.
Penetrates into breast milk: during breastfeeding, about 0.1% of levonorgestrel enters the newborn's body along with breast milk. Breastfeeding after taking the drug inside for the purpose of emergency postcoital contraception should be discontinued for 36 hours.
For the Navy. It is believed that the use of any purely gestagenic method of contraception 6 weeks after birth does not adversely affect the growth and development of the child, it is unlikely that it poses a risk to the child at doses released by the IUD located in the uterine cavity.
Side effects
In clinical trials, the most common cases in women taking oral levonorgestrel (0.75 mg) were nausea (23.1%), abdominal pain (17.6%), fatigue (16.9%), headache (16, 8%), menstrual irregularities, incl. heavy menstrual bleeding (13.8%), scanty menstrual bleeding (12.5%), dizziness (11.2%), breast tension (10.7%), vomiting (5.6%), diarrhea (5, 0%).
When using the IUD
On the part of the nervous system and sensory organs: ≥1%,<10% — пониженное настроение, нервозность, головная боль; ≥0,1%, <1% — лабильность настроения, мигрень.
From the digestive tract: ≥1%,<10% — боль в животе, тошнота; ≥0,1%, <1% — вздутие живота.
From the genitourinary system: ≥1% - uterine / vaginal bleeding, spotting spotting, oligo- and amenorrhea, benign ovarian cysts; ≥1%,<10% — боль в области органов малого таза, дисменорея, вагинальные выделения, вульвовагинит, напряженность молочных желез, болезненность молочных желез, снижение либидо; ≥0,1%, <1% — воспалительные заболевания органов малого таза, эндометрит, цервицит; ≥0,01%, <0,1% — перфорация матки.
On the part of the skin: ≥1%,<10% — угри; ≥0,1%, <1% — алопеция, сыпь, гирсутизм, зуд, экзема; ≥0,01%, <0,1% — сыпь, крапивница.
Others: ≥1%,<10% — боль в спине, повышение массы тела; ≥0,1%, <1% — отеки.
Interaction
With the simultaneous administration of inducers of cytochrome P450 isoenzymes, the metabolism of levonorgestrel may increase and the effect may decrease. The following drugs may decrease the effectiveness of levonorgestrel: amprenavir, lansoprazole, nevirapine, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates (including primidone), phenytoin and carbamazepine, drugs containing St. , rifabutin, griseofulvin. Levonorgestrel reduces the effectiveness of hypoglycemic drugs and anticoagulants (coumarin derivatives, phenindione), increases plasma concentrations of HA. Medicines containing levonorgestrel may increase the risk of cyclosporine toxicity by inhibiting its metabolism.
Method of administration and dosage
Inside, intrauterine. Inside, it is used in the first 96 hours after intercourse at a dose of 0.75-1.5 mg. It is not recommended to use the emergency contraception method more often than once every 4-6 months.Intrauterine, an IUD is inserted into the uterine cavity.
Precautionary measures
Repeated use of the drug inside during the same menstrual cycle should be avoided due to the possibility of menstrual dysfunction. It is not allowed to use the oral dosage form as a means of regular and continuous contraception, because this leads to a decrease in the effectiveness of the drug and an increase in the frequency of adverse reactions. If menstruation is delayed by more than 5-7 days after emergency postcoital contraception, pregnancy must be excluded, and in case of uterine bleeding, a gynecological examination is recommended.
In adolescents under 16 years of age, the use of emergency postcoital contraception is possible only in exceptional cases (including rape) and only after consulting a gynecologist.
Before installing the IUD, it is necessary to conduct a general medical and gynecological examination, including examination of the pelvic organs and mammary glands, as well as examination of a smear from the cervix. The woman must be re-examined 4-12 weeks after the installation of the IUD, and then once a year or more often, if clinically indicated. The IUD remains effective for five years. This should only be installed by a physician who has experience with the IUD or is well trained in this procedure.
The results of some recent studies show that women taking contraceptives containing only progestogen may have an increased risk of venous thrombosis; however, these results are not well defined. However, if symptoms of venous thrombosis appear, appropriate diagnostic and treatment measures should be taken immediately.
After removal of the IUD, fertility is restored in 50% of women after 6 months, in 96.4% - after 12 months.
Year of last adjustment
2011Interaction with other active ingredients
| Acarbose * | |
| Glipizid * | Against the background of levonorgestrel, the hypoglycemic effect is weakened; with a combined appointment, constant monitoring of the concentration of glucose in the blood is necessary. |
| Soluble insulin [porcine monocomponent] * | Against the background of levonorgestrel, the hypoglycemic effect is weakened (an increase in the dose may be required). |
| Carbamazepine * | Carbamazepine induces the activity of the CYP450 system in the liver, decreases plasma levels and reduces the reliability of the contraceptive effect of levonorgestrel. |
| Levothyroxine sodium * | Against the background of levonorgestrel, the plasma level of thyroxine-binding globulin increases (an increase in the dose may be required). |
| Retinol * | Against the background of levonorgestrel, a significant increase in plasma levels is possible. |
| Rifampicin * | Rifampicin, as an inducer of liver enzymes, accelerates biotransformation, can weaken the effect of levonorgestrel and reduce the reliability of contraception. |
| Phenytoin * | Phenytoin induces the activity of cytochrome P450, accelerates biotransformation, and can weaken the contraceptive effect of levonorgestrel. |
International name:
Dosage form: dragee
Pharmachologic effect:
Indications:
Gravistat 125
International name:
Dosage form:
Pharmachologic effect:
Indications:
Klimonorm
International name: Estradiol + Levonorgestrel (Estradiol + Levonorgestrel)
Dosage form: dragee
Pharmachologic effect: Combined estrogen-progestogen drug. Replenishes the lack of female sex hormones in menopause. Eliminates somatic, mental ...
Indications: Replacement therapy for a lack of female sex hormones after a normal, premature or surgical onset ...
Levonova
International name: Levonorgestrel
Dosage form:
Pharmachologic effect:
Indications:
Microginon
International name: Ethinylestradiol + Levonorgestrel (Ethinylestradiol + Levonorgestrel)
Dosage form: pills, tablets, film-coated tablets
Pharmachologic effect: A contraceptive combined estrogen-progestogen drug. When taken orally, it inhibits the pituitary secretion of gonadotropic hormones. Contraceptive ...
Indications: Contraception, functional disorders of the menstrual cycle (including dysmenorrhea without an organic cause, dysfunctional metrorrhagia, premenstrual syndrome).
Microlute
International name: Levonorgestrel
Dosage form: dragee
Pharmachologic effect: Synthetic gestagen with contraceptive action. Increases the viscosity of cervical mucus, which interferes with the movement of sperm. Depressing ...
Indications: Contraception as an additional drug in women using non-hormonal methods, as well as in the presence of contraindications to the use of estrogen-progestogen drugs.
Minisiston
International name: Ethinylestradiol + Levonorgestrel (Ethinylestradiol + Levonorgestrel)
Dosage form: pills, tablets, film-coated tablets
Pharmachologic effect: A contraceptive combined estrogen-progestogen drug. When taken orally, it inhibits the pituitary secretion of gonadotropic hormones. Contraceptive ...
Indications: Contraception, functional disorders of the menstrual cycle (including dysmenorrhea without an organic cause, dysfunctional metrorrhagia, premenstrual syndrome).
Miranova
International name: Ethinylestradiol + Levonorgestrel (Ethinylestradiol + Levonorgestrel)
Dosage form: pills, tablets, film-coated tablets
Pharmachologic effect: A contraceptive combined estrogen-progestogen drug. When taken orally, it inhibits the pituitary secretion of gonadotropic hormones. Contraceptive ...
Indications: Contraception, functional disorders of the menstrual cycle (including dysmenorrhea without an organic cause, dysfunctional metrorrhagia, premenstrual syndrome).
Mirena
International name: Levonorgestrel
Dosage form: intrauterine therapy system
Pharmachologic effect: Contraceptive gestagenic agent. Levonorgestrel as part of the IUD has a direct local effect on the endometrium, causing its temporary ...
Indications: Contraception (long-term), menorrhagia, prevention of endometrial hyperplasia against the background of estrogen replacement therapy.
Indications for use
Description of the effect on the body
The levonorgestrel-releasing intrauterine therapeutic system has a primarily local progestogenic effect.
The gestagen is released directly into the uterine cavity, which allows it to be used in an extremely low daily dose.
High concentrations of levonorgestrel in the endometrium contribute to a decrease in the sensitivity of its estrogen and progesterone receptors, making the endometrium immune to estradiol and having a strong antiproliferative effect.
When using Mirena, morphological changes in the endometrium and a weak local reaction to the presence of a foreign body in the uterus are observed.
Thickening of the mucous membrane of the cervical canal prevents the penetration of sperm into the uterus.
Mirena ® prevents fertilization due to inhibition of the motility and function of sperm in the uterus and fallopian tubes.
In some women, ovulation is suppressed. Previous use of Mirena does not affect fertility.
Approximately 80% of women who wish to have a baby will become pregnant within 12 months after the IUD is removed. In the first months of using Mirena, due to the process of inhibition of endometrial proliferation, an initial increase in spotting bleeding may be observed.
Following this, pronounced suppression of the endometrium leads to a decrease in the duration and volume of menstrual bleeding in women using Mirena.
Lean bleeding often transforms into oligo- or amenorrhea.
At the same time, the function of the ovaries and the concentration of estradiol in the blood remain normal. Mirena ® can be successfully used for the treatment of idiopathic menorrhagia, i.e.
menorrhagia in the absence of genital diseases, extragenital diseases and conditions accompanied by severe hypocoagulation, the symptoms of which are menorrhagia. By the end of the third month since the installation of Mirena in women with menorrhagia, the volume of menstrual bleeding decreased by 88%.
Reduction of menstrual blood loss reduces the risk of iron deficiency anemia Mirena ® also reduces the severity of dysmenorrhea. The effectiveness of Mirena in the prevention of endometrial hyperplasia during continuous estrogen therapy was equally high with both oral and percutaneous estrogen use.
Contraindications to the drug
Side effects on the body
Side effects usually do not require additional therapy and disappear within a few months.
It is possible to develop expulsion of the intrauterine system, perforation of the uterus, ectopic pregnancy, described with the use of other intrauterine contraceptives.
Side effects often develop in the first months after the introduction of Mirena into the uterus; with prolonged use of the IUD, they gradually disappear.
Very often: uterine / vaginal bleeding, spotting spotting, oligo- and amenorrhea, benign ovarian cysts. The average number of days when spotting is noted in women of childbearing age gradually decreases from 9 to 4 days per month during the first 6 months after IUD insertion. The number of women with prolonged 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's use, 17% of women had amenorrhea lasting at least 3 months. When Mirena is used in combination with estrogen replacement therapy, in the first months of treatment, most women in the peri- and postmenopausal period experience spotting and irregular bleeding. In the future, their frequency decreases, and in about 40% of women receiving this therapy in the last 3 months of the first year of treatment, bleeding generally disappears. Changes in the nature of bleeding are more common in the perimenopausal period than in the postmenopausal period. The frequency of detection of benign ovarian cysts depends on the diagnostic method used. According to clinical trials, enlarged follicles were diagnosed in 12% of women who used Mirena. In most cases, the increase in follicles was asymptomatic and disappeared within 3 months.
The table shows side effects, the frequency of which is consistent with clinical studies.
If a woman with installed Mirena becomes pregnant, the relative risk of ectopic pregnancy increases.
Cases of breast cancer have been reported.
Cautions for use
During pregnancy:
Mirena should not be used if pregnant or suspected of being pregnant. If a woman becomes pregnant while using Mirena, it is recommended to remove the IUD, because Any IUD left in situ increases the risk of spontaneous abortion and premature birth. Removal of Mirena or probing of the uterus can lead to spontaneous abortion. If it is not possible to carefully remove the intrauterine contraceptive, the advisability of artificial termination of pregnancy should be discussed. If a woman wants to preserve the pregnancy and the IUD cannot be removed, the patient should be informed about the risks and possible consequences of preterm birth for the baby. In such cases, the course of pregnancy should be closely monitored. Ectopic pregnancy must be ruled out.
The woman should be told that she should report all symptoms suggestive of pregnancy complications, in particular colicky abdominal pain with fever.
Due to the intrauterine use and the local action of the hormone, it is necessary to take into account the possibility of a virilizing effect on the fetus. Due to the high contraceptive efficacy of Mirena, clinical experience related to pregnancy outcomes with its use is limited. However, the woman should be informed that today there is no evidence of congenital defects caused by the use of Mirena in cases of continued pregnancy before childbirth without removing the IUD.
About 0.1% of a dose of levonorgestrel can be absorbed by a newborn during breastfeeding. However, it is unlikely to pose a risk to the baby at the doses released by Mirena in the uterine cavity.
It is believed that the use of Mirena 6 weeks after childbirth does not have a harmful effect on the growth and development of the child. Monotherapy with gestagens does not affect the quantity and quality of breast milk. Rare cases of uterine bleeding have been reported in women using Mirena during lactation.
Some recent studies have shown that women taking progestin-only contraceptives may have a slight increase in the risk of venous thrombosis; however, these results are not statistically significant. However, if symptoms of venous thrombosis appear, appropriate diagnostic and therapeutic measures should be taken immediately.
To date, it has not been established whether there is a connection between varicose veins or superficial thrombophlebitis with the phenomenon of venous thromboembolism. Mirena 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 prescribed antibiotics for prophylaxis.
Levonorgestrel in low doses can affect glucose tolerance, and therefore should regularly monitor blood glucose levels in women with diabetes using Mirena. However, as a rule, there is no need to change the therapeutic prescriptions for women with diabetes who use Mirena.
Some manifestations of polyposis or endometrial cancer can be masked by irregular bleeding. In such cases, an additional examination is required to clarify the diagnosis.
Mirena ® does not belong to the first choice methods either for young women who have never had a pregnancy, or for women in the postmenopausal period with severe uterine atrophy.
With estrogen monotherapy, the incidence of endometrial hyperplasia can reach 20%. In a clinical study of Mirena's use during a 5-year observation period in a group of postmenopausal women, no cases of endometrial hyperplasia were observed.
Oligo- and amenorrhea:
Oligo- and amenorrhea in women of childbearing age develops gradually, in about 20% of cases of Mirena use. If menstruation is absent within 6 weeks after the start of the last menstrual period, pregnancy should be excluded. Repeated pregnancy tests for amenorrhea are not necessary unless there are other signs of pregnancy.
When Mirena is used in combination with continuous estrogen replacement therapy, most women gradually develop amenorrhea during the first year.
Pelvic infections:
The guide tube helps protect Mirena from contamination by microorganisms during installation, and the Mirena insertion device is specially designed to minimize the risk of infection. It has been established that the presence of multiple sexual partners is a risk factor for infections of the pelvic organs. Pelvic infections can have serious consequences: they can disrupt fertility and increase the risk of ectopic pregnancy.
In case of recurrent endometritis or infection of the pelvic organs, as well as in severe or acute infections that are resistant to treatment for several days, Mirena® should be removed.
Even in cases where only isolated 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. However, the system can be expelled from the uterine cavity unnoticed by the woman, which leads to the termination of contraceptive action. Partial expulsion can reduce the effectiveness of Mirena. Since Mirena ® reduces menstrual blood loss, its increase may indicate expulsion of the IUD.
If the position is incorrect, Mirena ® must be removed. At the same time, a new system can be installed.
It is necessary to explain to a woman how to check Mirena's threads.
Perforation and penetration:
Perforation or penetration of the body or cervix with an intrauterine contraceptive is rare, mainly during installation, and can reduce the effectiveness of Mirena. In these cases, the system should be removed. There may be an increased risk of perforation with IUD insertion after childbirth, during lactation, and in women with a fixed bend of the uterus.
Ectopic pregnancy:
Women with a history of ectopic pregnancy who have had tubal surgery or a pelvic infection are at a higher risk of ectopic pregnancy. The possibility of ectopic pregnancy should be considered in the 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 when using Mirena is approximately 0.1% per year. The absolute risk of ectopic pregnancy in women using Mirena is low. However, if a woman with installed Mirena becomes pregnant, the relative likelihood of an ectopic pregnancy is higher.
Loss of threads:
If, during a gynecological examination, the thread for removing the IUD cannot be found in the cervical region, pregnancy must be excluded. The threads can be pulled into the uterine cavity or cervical canal and become visible again after the next menstruation. If pregnancy is ruled out, the location of the sutures can usually be determined by careful probing with an appropriate instrument. If it is not possible to find the threads, it is possible that the IUD expulsion from the uterine cavity has occurred. An ultrasound scan can be used to determine if the system is correctly positioned. If it is unavailable or unsuccessful, X-ray examination is used to determine the localization of Mirena.
Delayed follicular atresia:
Since the contraceptive effect of Mirena is mainly due to its local action, ovulatory cycles with rupture of follicles are usually observed in women of childbearing age. Sometimes follicular atresia is delayed, and their development can continue. Such enlarged follicles are clinically indistinguishable from ovarian cysts. Enlarged follicles were found in 12% of women who used 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.
In most cases, enlarged follicles disappear on their own within two to three months of observation. If this does not happen, it is recommended to continue monitoring with ultrasound, as well as conducting therapeutic and diagnostic measures. In rare cases, it is necessary to resort to surgical intervention.
Influence on the ability to drive vehicles and use mechanisms:
Not observed.
How to apply
Mirena ® is injected into the uterine cavity. The effectiveness lasts for 5 years. The release rate of levonorgestrel in vivo at the beginning is approximately 20 μg / day and decreases after 5 years to approximately 10 μg / day. The average release rate of levonorgestrel is approximately 14 mcg / day for up to 5 years. Mirena can be used in women receiving hormone replacement therapy in combination with oral or transdermal estrogen preparations that do not contain progestogen.
With the correct installation of Mirena, carried out in accordance with the instructions for medical use, the Pearl index is approximately 0.2% for 1 year. The cumulative indicator reflecting the number of pregnancies in 100 women using contraceptives for 5 years is 0.7%.
For the purpose of contraception women of childbearing age Mirena should be placed in the uterine cavity within 7 days from the onset of menstruation. Mirena ® can be replaced with a new IUD on any day of the menstrual cycle. The IUD can also be installed immediately after an abortion in the first trimester of pregnancy .:
After delivery, the IUD should be inserted when the uterus involution occurs, but not earlier than 6 weeks after delivery. With prolonged subinvolution, it is necessary to exclude postpartum endometritis and postpone the decision to administer Mirena until the end of involution. In case of difficulties with IUD insertion and / or very severe pain or bleeding during or after the procedure, physical and ultrasound should be performed immediately to exclude perforation .
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To protect the endometrium during estrogen replacement therapy in women with amenorrhea, Mirena ® can be installed at any time; in women with preserved menstruation, the installation is performed in menstrual bleeding or withdrawal bleeding .:
Mirena should not be used for postcoital contraception.
Rules for using the IUD
Mirena ® is supplied in sterile packaging, which is opened only immediately before the installation of the IUD. It is necessary to observe the rules of asepsis when handling the opened system. If the sterility of the packaging appears to have been compromised, the IUD should be disposed of as medical waste. You should also handle the IUD removed from the uterus, since it contains the remains of the hormone.
Installation, removal and replacement of the IUD
Before installation Mirena woman should be informed about the effectiveness, risks and side effects of this IUD. It is necessary to conduct a general and gynecological examination, including examination of the pelvic organs and mammary glands, as well as examination of a smear from the cervix. Pregnancy and sexually transmitted diseases must be ruled out, and genital infections must be completely healed. Determine the position of the uterus and the size of its cavity. It is especially important to correctly position Mirena in the fundus of the uterus, which ensures a uniform effect of gestagen on the endometrium, prevents IUD expulsion and creates conditions for its maximum effectiveness. Therefore, you should carefully follow the instructions for installing Mirena. Since the technique of installation in the uterus of different IUDs is different, special attention should be paid to working out the correct technique for installing a particular system.
The woman needs to be re-examined 4-12 weeks after installation, and then once a year or more often if clinically indicated.
Before installation Mirena should exclude pathological processes in the endometrium, since in the first months of its use, irregular bleeding / spotting spotting is often noted. You should also exclude pathological processes in the endometrium when bleeding occurs after the start of estrogen replacement therapy in a woman who continues to use Mirena, previously established for contraception. Appropriate diagnostic measures must also be taken when irregular bleeding develops during long-term treatment.
Mirena remove by gently pulling on the threads captured by forceps. If the threads are not visible and the system is in the uterine cavity, it can be removed with a traction hook to remove the IUD. In this case, the expansion of the cervical canal may be required.
The system should be removed 5 years after installation. If a woman wants to continue using the same method, a new system can be installed immediately after removing the previous one.
If further contraception is necessary, in women of childbearing age, the removal of the IUD should be performed during menstruation, provided that the menstrual cycle is preserved. If the system is removed mid-cycle and the woman has had intercourse in the previous week, she is at risk of becoming pregnant unless the new system was installed immediately after the old one was removed.
Insertion and removal of the IUD can be accompanied by certain painful sensations and bleeding. The procedure may cause fainting due to a vasovagal reaction or seizure in people with epilepsy.
After removing Mirena, you should check the system for integrity. With difficulties with the removal of the IUD, there were isolated cases of slipping of the hormonal-elastomeric core onto the horizontal arms of the T-shaped body, as a result of which they were hidden inside the core. Once the integrity of the IUD is confirmed, this situation does not require additional intervention. The restraints on the horizontal arms usually prevent the core from separating completely from the T-body.
Instructions for the introduction of the IUD
Installed only by a doctor using sterile instruments.
Mirena ® is supplied together with the guidewire in sterile packaging, which must not be opened prior to installation.
Do not re-sterilize. For single use only. Do not use Mirena if inner packaging is damaged or opened. Do not install Mirena after the month and year indicated on the package.
Before installation, you should read the information on the use of Mirena ®.
Preparation for the introduction:
1. Conduct a gynecological examination to establish the size and position of the uterus and to exclude any signs of acute genital infections, pregnancy or other gynecological contraindications for the Mirena installation.
2. Visualize the cervix with speculum and completely clean the cervix and vagina with a suitable antiseptic solution.
3. If necessary, use the help of an assistant.
4. Grasp the upper lip of the cervix with forceps. Straighten the cervical canal with sharp traction with forceps. Forceps should be in this position during the entire time of Mirena insertion to ensure careful traction of the cervix towards the inserted instrument.
5. Carefully advancing the uterine probe through the cavity to the bottom of the uterus, determine the direction of the cervical canal and the depth of the uterine cavity, exclude septa in the uterine cavity, synechiae and submucosal fibroids. If the cervical canal is too narrow, dilation of the canal is recommended and pain relievers / paracervical block may be used.
Introduction:
1. Open the sterile packaging. After that, all manipulations should be carried out using sterile instruments and sterile gloves.
2. Move the slider forward to the farthest position to pull the IUD into the guide tube.
Do not move the slider downward, as this could lead to the premature release of Mirena. If this happens, the system will not be able to be reinserted into the conductor.
3. While holding the slider in the farthest position, adjust the top edge of the index ring to match the probe's distance from the outer os to the fundus.
4. Continuing to hold the slider in the farthest position, advance the guide wire carefully through the cervical canal into the uterus until the index ring is about 1.5-2 cm from the cervix.
Do not push the guidewire forcibly. If necessary, the cervical canal should be widened.
5. Keeping the guide stationary, move the slider up to the mark to reveal the horizontal shoulders of Mirena. Wait 5-10 seconds until the horizontal shoulders open completely.
6. Carefully slide the guide wire inward until the index ring contacts the cervix. Mirena ® should now be in a fundic position.
7. Keeping the conductor in the same position, release Mirena by moving the slider down as far as possible. While holding the slider in the same position, carefully remove the wire by pulling on it. Cut the threads so that their length is 2-3 cm from the outer os of the uterus.
If you have any doubts that the system is installed correctly, check the position of the Mirena, for example, using an ultrasound scan or, if necessary, remove the system and insert a new, sterile system. Remove the system if it is not completely in the uterine cavity. The remote system must not be reused.
Removal / replacement of Mirena:
Before removing / replacing Mirena, you should read the instructions for use of Mirena.
Mirena is removed by gently pulling on the threads captured by forceps.
The doctor can install a new Mirena ® system immediately after removing the old one.
Consequences of incorrect dosage
With this method of application, an overdose is impossible.
Combination with other medicines
It is possible to increase the metabolism of gestagens with the simultaneous use of substances that are inducers of enzymes, especially isoenzymes of the cytochrome P450 system, involved in the metabolism of drugs, such as anticonvulsants and drugs for the treatment of infections. The effect of these drugs on the effectiveness of Mirena is unknown, but it is assumed that it is insignificant, since Mirena® has a mainly local effect.
Levonorgestrel, also referred to as ethyl estradiol, is a synthetic progestogen with a contraceptive effect, which consists in the implementation of antiestrogenic and progestogenic activity:- It helps to slow down the ovulation process, thereby preventing the occurrence of an unplanned pregnancy - it is an emergency contraceptive.
- Levonorgestrel-based drugs also change the consistency of cervical mucus, making it thicker and more viscous, which greatly complicates the process of sperm penetration into the uterine cavity.
- Levonorgestrel has a slowing effect on the activity of endometrial growth. Therefore, even in the event of an accidental fertilization of the egg, pregnancy will not occur. This is due to the fact that the fertilized egg simply cannot attach to the wall of the uterine cavity due to the too thin inner layer of the mucous membranes of this organ.
- Regular use of drugs based on levonorgestrel slows down the production of luteinizing and follicle-stimulating hormones, which are responsible for the reproductive functionality of the female body. And also a decrease in the activity of the temporary gland (corpus luteum) of the endocrine system in a woman, the action of which is to prepare the uterine organ for possible fertilization.
How does the hormone levonorgestrel affect a woman's body?
Getting into the body:- Levonorgestrel, as a form of progesterone, acts on the hypothalamus through a negative feedback mechanism, which causes a decrease in the secretion of luteinizing and follicle-stimulating hormones, which stimulate ovulation. Thus, by decreasing their excretion, levonorgestrel serves to suppress ovulation.
- prevents thickening of the uterus (endometrium) every month in preparation for fertilization of the egg. This stops the attachment of an already fertilized egg to the wall of the uterus, and thus prevents pregnancy in a different way.
- prevents the release of an egg from the ovary (ovulation), but this does not necessarily happen in all women who use an IUD.
How does emergency contraception with levonorgestrel affect a woman's body
The hormone works mainly by stopping the secretion of an egg from the ovary, as well as preventing fertilization of the egg or preventing attachment (implantation) to the uterus. Each body will react to this pill differently, but there are several facts you need to know about the effects of levonorgestrel on a woman's body:- Delayed ovulation
After taking a pill with Levonorgestrel, ovulation is delayed and sperm that may be present after unprotected intercourse will not be able to fertilize an egg, thereby preventing pregnancy. - Possible endometrial lining change
Progestin (the full analogue of which is levonorgestrel) is a synthetic hormone that acts in a similar way to the natural hormone that regulates the uterine lining.
And the side effect after taking it is that in the process of preventing pregnancy, it can somehow affect the endometrium. - Delay of menstruation
There is no cause for alarm if your period is late after emergency contraception. Since this hormone delays ovulation, it can lead to changes in the menstrual cycle, and it starts earlier or later than usual. - Other changes in the cycle
A slight delay is not the only thing that can happen after taking the pill. Sometimes a light discharge may appear before the actual menstrual cycle. But don't worry about that. Menstrual fluctuations in this case are natural and over time the cycle should return to normal. If you do not have your menstrual period within 3 weeks after emergency contraception, have a pregnancy test. The pill might not work, it's rare, but it happens. - Nausea
If you are afraid of getting pregnant, you need to know that the most common side effects after emergency contraception are nausea, vomiting, and irregular bleeding.
About 20 percent of women experience nausea, and half of them also vomit, which disappears within a few hours. Important: you must be careful, and if a pill comes out during vomiting, you need to see a doctor, since the prevention of pregnancy did not happen. - Levonorgestrel does not terminate a pregnancy
This is important to know: emergency contraception is not an abortion that terminates a pregnancy by separating the fertilized egg from the uterine lining. The main purpose of such contraception is to prevent fertilization. - Doesn't harm when breastfeeding
Emergency contraception will not harm the baby. Women who are breastfeeding can take levonorgestrel. This can lead to a short-term decrease in milk production, but it will not harm the baby. - Drug interactions
This type of hormone is available without a prescription, but that doesn't mean you need to take it without first consulting a healthcare professional. Also, it may not be as effective if you have been taking certain medications (including barbiturates, St. John's wort, and some HIV / AIDS medications), so it's best to always talk to a specialist. - Has no long-term effect on the body
Levonorgestrel is metabolized relatively quickly and does not have any long-term health effects, even when taken multiple times. The only thing that will be frustrating in the long run is the immediate side effects, such as nausea and the likelihood of pregnancy. Levonorgestrel pills are not as effective as condoms or birth control pills.
If any side effects occur that are particularly troubling or unusual, always see your doctor. But in most cases, such a pill is a well-regulated, safe option if emergency contraception is needed.
The effect of the IUD with levonorgestrel on the female body
Mirena is an intrauterine device with the highest dose of this hormone. Others, in comparison with it, contain it several times less. Therefore, being the most effective contraceptive, it ultimately has its drawbacks:Often, women with the Mirena coil complain about the absence of menstruation, in some cases they are much lighter and shorter compared to the flow and duration before it is established (Mirena has a coverage of 52 mg. Of the hormone levonorgestrel). Premenstrual pain is also much easier.
At first glance, there are solid benefits, but most of the side effects with the levonorgestrel-releasing IUD include changes in the uterus and vaginal bleeding, which occur in about 52% of cases, and the cessation of menstruation in 24% of cases.
But...
Menstruation, increased estrogen, ovulation, and increased progesterone are all necessary for a woman's overall health. Estrogen, for example, promotes bone growth and progesterone promotes bone maintenance. If these hormones do not reach their optimal levels every month, over time, the lack of estrogen and progesterone can lead to osteoporosis in postmenopausal women.
When to take levonorgestrel medications and why
Medicines with levonorgestrel are available in capsule and tablet form, as well as in the form of intrauterine devices. Each form of the drug is used for a specific purpose:- It is recommended to take pills for emergency contraception, after unprotected sex with a sexual partner, as well as with a low level of reliability of the contraceptive method used;
- The intrauterine device is usually used for long-term protection of the female body from unwanted pregnancy for up to 5 years;
- When carrying out replacement therapy with the use of estrogens to prevent hyperplasia of the endometrial layer in the uterine cavity, it is also recommended to use an intrauterine device with levonorgestrel;
- Capsules for subcutaneous administration are prescribed for long-term contraception - from 2 to 5 years.
- If a woman has heavy and painful periods, accompanied by an increased level of blood loss, which reduces the level and quality of life, doctors also recommend setting an intrauterine device containing the hormone levonorgestrel.
When not to take levonorgestrel medications and why
Any hormone-containing medication requires the utmost level of care in prescribing, selecting a dosage and using it. Before using drugs with levonorgestrel, you should read the following list of absolute contraindications to their use.The following contraindications are characteristic of the tablet form:
- increased sensitivity of the body to the active ingredient;
- the presence of blood clots or the body's predisposition to their appearance, since taking levonorgestrel promotes the appearance with all that it implies;
- an increase in the likelihood of the appearance and complications of such pathologies;
- with diseases of the liver and biliary tract;
- the period of pregnancy, since the intake of a synthetic hormone can cause premature birth, miscarriage, and other equally serious consequences;
- the period of breastfeeding, since the active components of the drug, with long-term administration, penetrate into the composition of breast milk;
- in the postpartum period with the development of endometritis;
- with pathology of the coronary arteries;
- not recommended for girls under the age of 16.
- pathology of the pelvic organs with an inflammatory nature of the course;
- infectious diseases of the lower genital and urinary tract;
- carrying out a septic abortion, it is not recommended to insert an IUD during the first 3-4 months after such an intervention;
- the development of cervicitis, dysplasia of the cervix of the uterine organ and the occurrence of pathological changes of a malignant nature in the uterine cavity;
- breast cancer;
- uterine hemorrhages of unknown etiology;
- fibroids;
- an increased level of sensitivity of the body to levonorgestrel.
- severe headaches and migraines;
- loss of consciousness;
- the appearance of suspicions of the development of ischemia;
- pathological disorders in the blood flow system (thick blood), up to the occurrence of a stroke or myocardial infarction;
- the occurrence of diabetes mellitus.
Excess dosage
When taking the tablet form of the drug with levonorgestrel and exceeding the dosages prescribed by the doctor, the following side effects may occur:- headache;
- psychoemotional disorders with an increased level of nervousness;
- pathological changes in the performance of the digestive system of organs may appear in the form of nausea, increased gas production or diarrhea;
- the nature of menstrual flow may change;
- allergic skin rashes.
- in some women, the IUD can lead to fainting, bleeding, and dizziness.
What drugs contain levonorgestrel
Oral contraceptives, which contribute not only to the prevention of unplanned pregnancy, but also to restore and normalize the course of the menstrual cycle, and also reduce the intensity of the symptoms of premenstrual syndrome:- Gravistat,
- Triquilar,
- Rigevidon,
- Anteovin.
- Levonov,
- Mirena.
One package of Norplant contains 6 capsules, which are sewn into the subcutaneous layer in the area of the scapula. The contraceptive effect of the capsules lasts for 5 years.