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-gestagenic drug. Compensates for the lack of female sex hormones in menopause. Eliminates somatic, mental...

Indications: Replacement therapy for lack of female sex hormones after a normal, premature or surgically caused onset ...

Levonova

International name: Levonorgestrel (Levonorgestrel)

Dosage form:

Pharmachologic effect:

Indications:

Microgynon

International name: Ethinylestradiol + Levonorgestrel (Ethinylestradiol + Levonorgestrel)

Dosage form: dragees, tablets, coated tablets

Pharmachologic effect: Contraceptive combined estrogen-gestagenic 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 (Levonorgestrel)

Dosage form: dragee

Pharmachologic effect: Synthetic gestagen with contraceptive action. Increases the viscosity of cervical mucus, which prevents the advancement of spermatozoa. Oppresses...

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-gestagenic drugs.

minisiston

International name: Ethinylestradiol + Levonorgestrel (Ethinylestradiol + Levonorgestrel)

Dosage form: dragees, tablets, coated tablets

Pharmachologic effect: Contraceptive combined estrogen-gestagenic 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: dragees, tablets, coated tablets

Pharmachologic effect: Contraceptive combined estrogen-gestagenic 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 (Levonorgestrel)

Dosage form: intrauterine therapy system

Pharmachologic effect: Contraceptive progestogen. Levonorgestrel as part of the IUD has a direct local effect on the endometrium, causes its temporary...

Indications: Contraception (long-term), menorrhagia, prevention of endometrial hyperplasia during estrogen replacement therapy.

Intrauterine contraception immediately became popular among women, because it gives a high result and is very convenient to use. One of these contraceptives is the Mirena spiral, which is effective for, but before using it, you need to familiarize yourself with the reviews and consequences. It also does not hurt to find out the features of the remedy and its effect on the body.

Use in menopause

Mirena with menopause, or rather in its initial stages, helps a woman prevent unwanted pregnancy and normalize the hormonal balance of the body. In the initial stages of the process of ovarian failure, the likelihood of conception remains. But it can be very difficult, because the symptoms are very similar to the manifestation of menopause. Yes, and the absence of menstruation may be associated with the approach of menopause.

In addition, you can not be one hundred percent sure of the result of a pregnancy test. The fact is that the level of hCG during menopause is increased, and its indicators correspond to those of the first weeks after conception. It turns out that the test may be negative, but in fact there is a pregnancy.

Therefore, women decide to use Mirena to continue an active sex life without the threat of conception. In this case, the spiral does not affect the quality sexual relations. It is installed for a long period of time with minimal control requirements.

It is worth noting that this spiral differs from the usual options, because its composition includes progesterone of synthetic origin. Due to this, the hormonal balance is stabilized, which leads to the elimination of unpleasant symptoms of menopause.

Spiral features

The hormonal contraceptive comes in the form of a T-shaped device with two special antennae. Thanks to this shape, the spiral can be securely fixed in the uterus. In addition, a loop of threads is provided, with the help of which the system is removed.

In the body of the device itself, a cavity is provided in which the hormonal component, represented by levonorgestrel (52 milligrams), is located. The tool itself is stored inside a special tube, protected vacuum packed made of plastic and paper. It must be stored at 15-30 degrees for no more than three years from the date of manufacture.

How it works

The active substance of the spiral belongs to the gestagens. Hormone:

• blocks the growth of the endometrium;
• does not give cancer cells multiply;
• normalizes the balance between estrogen and progesterone;
• does not affect the normal functioning of the ovaries;
• blocks the appearance of pathologies of the pelvic organs;
• reduces the symptoms of menopause;
• protects against unwanted conception;
• acts as an excellent means of preventing endometriosis.

After installing the system, the woman's body receives a certain dose of levonorgestrel (20 mcg) every day. By the end of the five-year period of use, this figure drops to 10 mcg per day. It is important to note that almost the entire dose of the hormone is concentrated in the endometrium, and the hormone content in the blood does not exceed the microdose.

The active substance does not begin to flow into the blood immediately. This happens after about an hour, and after 14 days the blood contains the highest concentration of levonorgestrel, but this figure depends on the weight of the woman. If a woman weighs no more than 54 kilograms, then this figure will be 1.5 times more.

According to reviews, after installing the system, unstable discharge of a smearing nature may be noted, but only during the first few months. This is due to the restructuring of the endometrium, after which the duration and volume of bleeding are significantly reduced. And sometimes they stop altogether.

Hormonal spiral against menopausal diseases

Symptoms of menopausal syndrome are caused by destabilization of the hormonal background. But not always this problem can be solved by taking hormonal drugs with estrogen. The fact is that many diseases in the female body provoke the predominance of estrogen over progesterone. Here, the use of estrogen-containing drugs only exacerbates the problem, increasing the speed and neglect of the disease.

Levonorgestrel, which is contained in the Mirena spiral, can help in the fight against the following problems:

endometrial hyperplasia

Estrogen provokes excessive division of tissue cells, which can cause cancer. In addition, hormone surges can increase the symptoms of hyperplasia. In this case, the spiral reduces the effect of estrogen on the endometrium, but at the same time does not prevent the hormone from having a positive effect on the work of the heart, blood vessels, urinary system, bone tissue, etc.

endometriosis

This disease is direct consequence lack of progesterone against the background of an excess of estrogen. Mirena blocks the development of endometriosis, and also contributes to the subsidence of the disease. Levonorgestrel has a beneficial effect on the uterine mucosa, blocking the further spread of endometriosis foci and the risk of developing cancer. It can be noted a huge number of positive reviews about the Mirena spiral for endometriosis in premenopause without negative consequences for women's health.

Myoma

We note right away that with such a disease it is not always possible to use a spiral. Everything will depend on the characteristics of the tumor (location and size). Here, the agent significantly reduces the supply of nutrition to the tumor.

Bleeding

Mirena contains an analogue of progesterone, which can reduce the activity of bleeding and their volume. But its use is allowed only if the bleeding is not associated with oncological diseases.

A change in the hormonal background always leads to a decrease in the body's defenses, which is why these diseases often occur precisely with the approach of menopause. Mirena and premenopause are connected in such a way that the spiral itself significantly reduces the risk of various pathologies due to the support of the vaginal microflora and the stabilization of hormonal balance.

The main indications and contraindications for use

Unfortunately, not every woman can use the tool. To begin with, it is worth noting that a prerequisite is the examination of the whole organism.

In this case, contraindications are:

• malignant tumors;
• breast oncology;
• bleeding associated with serious illness;
• individual intolerance to gestagens;
• vein thrombosis;
• inflammation of the pelvic organs;
• infection in the urinary system;
• endometritis;
• liver problems (hepatitis, cirrhosis);
• heart and kidney disease;
• recent abortion (three months ago).

Important! Any inflammatory pathology of the pelvic organs are indications for the removal of the spiral. In addition, intrauterine contraceptives are contraindicated at a high risk of infectious diseases (problems with immunity, lack of a permanent partner).

Despite the minimal effect of levonorgestrel on the functioning of the body, it is contraindicated in all cancers. Relatively contraindicated diseases include migraines, arterial hypertension, thrombophlebitis and diabetes mellitus. In these cases, the possibility of using an intrauterine hormonal contraceptive is determined by the doctor, but only after a comprehensive laboratory diagnosis.

Main indications for use:

1. Contraception. The main purpose of the installation of the IUD remains the prevention of unwanted conception.
2. Idiopathic menorrhagia. The IUD is used as an element of therapy only in the absence of hyperplastic processes in the uterine mucosa, as well as extragenital pathologies.
3. Prevention of endometrial hyperplasia. It is used when prescribing estrogen replacement therapy when it is necessary to balance estrogens and progestins in the body.
4. Profuse bleeding with no clear cause. After installing the spiral, or rather after 4 months, the amount of discharge should return to normal.

Side effects of the Mirena coil

It is worth noting that often side effects appear only in the first few months after the doctor has installed the system. Here you need to pay attention to the strength of their manifestation. If the side effects are minor, then the woman can continue to use the remedy, but this issue is resolved with the attending physician.

Among the side effects it is worth highlighting:

• migraine;
• headache;
• ectopic pregnancy;
• jumps in blood pressure;
• nausea;
• vomit;
• appearance excess weight;
• dizziness;
• allergic rashes;
• breast pain;
• unstable emotional state;
• irritability;
• insomnia.

These side effects most often appear only at the very beginning of using the remedy. Judging by the reviews, most women who have undergone a preliminary examination and installed a spiral with an experienced specialist do not suffer from side effects. , hot flashes and irritability disappear almost immediately.

Very rarely, the use of a spiral can cause:

• tumor development;
• stroke
• myocardial infarction;
• formation of cysts in the ovaries;
• jaundice.

Abundant discharge after the installation of the spiral

A certain number of women's reviews contain information about spotting after the installation of Mirena. During premenopause, the coil can cause spotting and spotting, but this is normal only in the first four months after the procedure.

Similarly, the female body adapts to changes and normalization of hormonal balance. In addition, in the first few months after the installation of the spiral, there is a significant risk of inflammatory processes. Therefore, with any complaints, you should consult a doctor to eliminate other causes of bleeding, even if there are no other painful symptoms.

As for the duration of bleeding, it is within five or seven days. But soon Mirena should reduce the abundance of secretions, gradually bringing them closer to normal.

For more information about , follow the link.

Possible side effects of Mirena

According to reviews and studies, the following consequences, although they appear very rarely, still take place:

• ectopic pregnancy. At risk are women who suffered from protracted infectious diseases and inflammatory processes. In this case, immediate surgical intervention is required. Symptoms of the complication include dizziness, nausea, pain in the lower abdomen, delayed menstruation, pallor of the skin and general weakness.
• Penetration. Ingrown means in the walls of the uterus occurs very rarely. This is possible against the background of lactation, the recent birth of a child, or a non-standard location of the uterus.
• The fall of the Navy. Spiral fallout is quite common. The likelihood of this undesirable process increases during menstruation, and it can go unnoticed. Women are advised to immediately consult a doctor to remove the product and install a new system.
• inflammatory processes and infectious diseases. High probability of development in the first month after the installation of the system. A woman needs to see a doctor who will prescribe treatment and decide whether the coil needs to be removed.
• Amenorrhea. Possible six months after using the IUD. The first thing to do here is to rule out pregnancy. Note that after removing the remedy, the cycle becomes normal if the cessation of menstruation is not caused by other reasons.
• . Occur in only 12% of patients (approximately). It is also worth noting that enlarged follicles independently acquire normal sizes after a few months.

Nothing more can be said about the consequences. This is due to the individuality of each case and the impossibility of collecting information about every woman who used Mirena. Note that this IUD with levonorgestrel is relatively safe, like all drugs containing hormones. In most cases, patients successfully endure all five years with this system, but subject to a responsible attitude to their health and passing the necessary examination.

Installation, removal and features of the spiral

It is worth noting that not all doctors have sufficient experience in installing the Mirena coil. A woman needs to find a specialist who has already worked with this type of IUD and knows the features of this procedure.

The product is available in sterile packaging that cannot be opened at home. This is done by a specialist immediately before installation. If the integrity of the package has been violated, then the installation of the spiral is not allowed. It is destroyed as medical waste. The same applies to the removal procedure, because the used spiral still contains hormones.

Examination before the installation of Mirena

Before buying a Mirena spiral, you should check your health in advance. First you need to visit the attending doctor, who will advise:

• examine the vagina;
• visit a mammologist;
• examine the microflora of the vagina;
• do an ultrasound of the genitals.

In addition, it is worth taking tests for hormones in order to accurately determine the state of the hormonal background of the body.

Features of using the tool for various purposes

There is a list of prescriptions for the date of installation of the IUD:

• For contraception. The procedure should be carried out in the first week of the cycle. But the replacement of the IUD is performed on any day of the menstrual cycle.
• After childbirth. Here you should wait for the complete involution of the uterus, but even with this factor, Mirena is contraindicated during the first six weeks after the birth of the child. In addition, if severe pain occurs, the pelvic organs should be examined to exclude perforations.
• To protect the endometrium. Can be used in conjunction with HRT. The procedure is carried out in the last days of the cycle. With amenorrhea, the coil can be installed at any time.

How often to visit the doctor after the installation of the spiral

V without fail a woman should appear at a gynecologist's appointment no later than 3 months after the installation of Mirena. Then you can visit the doctor once a year, and if you have complaints, you should immediately go to the hospital.

If the doctor allowed the installation of the spiral to a woman suffering from diabetes She needs to closely monitor her blood glucose levels. The fact is that levonorgestrel still negatively affects glucose tolerance. Any ailments should not be ignored.

Spiral Removal

The system is removed by gently pulling on specially designed threads using sterile forceps. Sometimes it is impossible to see the threads, then the doctor resorts to using a traction hook for safe extraction. In addition, in some cases, the specialist expands the cervical canal.

Important! The system is removed after five years of use when the patient feels normal. For any serious complaints, the IUD should be removed from the body immediately.

As for the re-installation of a new tool, the procedure can be carried out almost immediately. Here everything will depend on the monthly. When saving menstrual flow, the installation of a new system is carried out on the days of menstruation in order to eliminate the risk of fertilization of the egg.

The doctor should warn the patient that the insertion or removal of an intrauterine hormonal contraceptive may cause certain pain and bleeding. special care should be shown to women with epilepsy and cervical stenosis. Syncope, bradycardia or convulsive seizures are possible here.

After Mirena is removed, the system is checked for integrity in order to exclude slippage of the hormonal cavity of the spiral. Once the physician confirms the integrity of the remedy, no further action is required.

What the reviews say

Mirena solves several problems at once women's issues. Premenopause brings some discomfort, which is associated not only with unpleasant symptoms, but also with the need to select the optimal contraceptive. Most women note the practicality of this tool.

Often, patients wonder if they will be able to become pregnant after removing the system. So, 80% of women were able to conceive a child (planned) in the first year after the removal of the IUD. In other cases, diseases interfered or pregnancy occurred a little later.

Of course, with the approach of menopause, many women no longer plan to have a child. It is important to carry out the installation of the spiral at the right time.

In fact, the reviews are contradictory. The main group of women is not satisfied with the unstable emotional background in the first month of using the IUD. But here you need to take into account the restructuring of the body, which is trying to get used to the changes and the influence of the hormone.

In addition, women note that the Mirena spiral is much more convenient than oral ones, which require a strict regimen. If we take the price of the system, then it ranges from 9-13 thousand rubles. With the expectation of a five-year period, you can save a good amount in contrast to spending on contraceptives.

The Mirena intrauterine hormonal contraceptive is a real find during premenopause, when the likelihood of conception remains, and the hormonal balance needs to be normalized. In addition, Mirena shows itself well together with estrogen-based HRT. It remains only to follow the recommendations and monitor your health in order to avoid possible consequences.

Levonova; Levonorgestrel; Microlute; Mirena(spiral intrauterine); Norplant; Postinor; Escapelle.

Levonorgestrel- means for the prevention of pregnancy, contraception. It has a pronounced progestogenic and antiestrogenic activity, which contributes to the inhibition of conception at an early stage and the prevention of pregnancy. Levonorgestrel is the most studied progestogen, which has long been successfully used in many contraceptives.

Active active ingredient:
Levonorgestrel / Levonorgestrel.

Dosage forms:
Tablets.
Dragee.
Capsules.
Intrauterine system (intrauterine device).

Levonorgestrel

Properties / Action:
Levonorgestrel has a pronounced progestogenic and antiestrogenic activity, which contributes to the inhibition of conception at an early stage and the prevention of pregnancy. Levonorgestrel is an oral contraceptive (oral contraceptive) that works by ingestion. Distinctive feature levonorgestrel preparations in comparison with combined progestogen-estrogen oral contraceptives(microgynon, triquilar, femoden) is that they contain only progestogen (progestogen) as an active ingredient.
For emergency contraception Levonorgestrel is used at a dose of 0.75 mg. With prolonged daily intake at a dose of 0.03 mg, levonorgestrel has a contraceptive effect due to a number of mechanisms, among which the leading role is assigned to peripheral progestogen effects.
Under the influence of the drug, the viscosity of the mucus in the cervix (cervical or cervical mucus) increases, which makes it difficult for spermatozoa to enter the uterine cavity. Levonorgestrel inhibits the proliferation of the endometrium, which makes implantation of a fertilized egg impossible. Levonorgestrel is able to have an inhibitory effect on the release of releasing factors in the hypothalamus and reduce the production of luteinizing (LH) and follicle-stimulating (FSH) hormones by the pituitary gland, and lower the function of the corpus luteum. The severity of these effects of levonorgestrel at a low dosage is insignificant, but sufficient to provide a contraceptive effect. In low doses, it does not cause complete suppression of ovulation.
Intrauterine system:
The intrauterine contraceptive (mirena) is a T-shaped polyethylene system (device), the vertical rod of which consists of a levonorgestrel-containing container covered with a special membrane through which controlled diffusion of levonorgestrel 20 mcg / day continuously occurs.
Levonorgestrel, entering directly into the uterine cavity, has a direct local effect on the endometrium, preventing proliferative changes in it and thereby reducing its implantation function, and also increases the viscosity of the mucus of the cervical canal, which prevents the penetration of spermatozoa into the uterine cavity. Levonorgestrel also has a slight systemic effect, manifested by the inhibition of ovulation in a certain number of cycles. Reduces the amount of menstrual bleeding, reduces pre-and menstrual pain.

Pharmacokinetics:
Tablets, dragees:
Levonorgestrel, when taken orally, is rapidly and completely absorbed from the gastrointestinal tract. The bioavailability of levonorgestrel is about 100%. It has a high (more than 90%) connection with plasma proteins. The maximum concentration in the blood is observed after 0.5-2 hours. In the future, the concentration of the drug is characterized by a two-phase decrease with a half-life of 2 or 24 hours. It is metabolized in the liver. It is well distributed over organs and tissues. About 10% of the dose passed into breast milk. 60% of the drug is excreted in the urine, 40% - through the intestines. Daily repeated intake is not accompanied by cumulation of the active substance and its metabolites.
Intrauterine system:
Levonorgestrel enters directly into the uterine cavity. A small part of it is absorbed into the systemic circulation. The concentration of levonorgestrel in plasma is stable and is 100-200 pg / ml (0.3-0.6 nmol / l).

Indications:
Pregnancy warning.
Levonorgestrel 0.75 mg tablets are used for emergency contraception after intercourse if the male condom has broken or in case of unprotected intercourse.
Levonorgestrel dragee 0.03 mg is used for long-term contraception, as well as an additional method of contraception in women using non-hormonal methods of preventing pregnancy and in cases where there are objective or subjective reasons that do not allow the use of progestogen-estrogen contraceptives.
Idiopathic menorrhagia (for the intrauterine system).

Dosage and administration:
Tablets 0.75 mg:
0.75 mg (1 tablet) of levonorgestrel is taken within 72 hours (preferably immediately) after unprotected intercourse, another 1 tablet should be taken 12 hours after the first.
Dragee 0.03 mg:
0.03 mg (1 tablet) is taken orally 1 tablet per day, for a long time, without interruption. Reception begins on the 1st day of menstruation, using pills of the corresponding day of the week from the calendar package. Dragee is taken without chewing, and washed down with a small amount of liquid. The time of admission does not play a role, however, the subsequent administration of the drug should be made at the same selected hour, since the interval between taking the dragee should be close to 24 hours.
Capsules:
Implanted s / c in the inner region of the shoulder for a period of 5 years.

It is recommended to enter into the uterine cavity on the 4th-6th day of the menstrual cycle; after artificial abortion - immediately, or, preferably, after the next menstruation; after uncomplicated spontaneous childbirth - not earlier than after 6 weeks. The intrauterine system should be removed after 5 years. At the same time, it is possible to introduce a new intrauterine system at the same time.

Overdose:
In case of an overdose, the described side effects may increase.
There is no antidote, gastric lavage and symptomatic treatment are recommended.

With this method of application, an overdose is impossible.

Contraindications:
Pregnancy, breast-feeding (rejection of breast-feeding is obligatory);
Age of puberty;
Uterine bleeding of unknown etiology;
Infectious diseases of the genitourinary system, pelvic organs, the presence of a herpes infection during a former pregnancy;
Malignant neoplasms of the genital organs and mammary glands, hormone-dependent tumors;
Diseases of the liver and gallbladder, history of jaundice, liver tumors, Dubin-Johnson and Rotor syndromes (hereditary benign hyperbilirubinemia);
Tendency to thromboembolism, incl. with disorders of cerebral circulation and other cardiovascular diseases, thrombophlebitis;
sickle cell anemia;
Otosclerosis;
Severe diabetes with vascular complications;
Hypersensitivity;
Intrauterine system (mirena):
Congenital and acquired anomalies of the uterus that prevent the introduction of intrauterine contraceptives.

Use during pregnancy and lactation:
Levonorgestrel is contraindicated during pregnancy and lactation.

Side effect:
After the use of levonorgestrel, nausea, vomiting, headaches and abdominal pain, intermenstrual bleeding, shortening or lengthening of the cycle, oligo- and amenorrhea, dysmenorrhea, breast engorgement, mastalgia, rarely acne, depression, changes in body weight and libido.
Intrauterine system (mirena):
Side effects, as a rule, do not require additional therapy and disappear within a few months. Perhaps the development of expulsion of the intrauterine system, perforation of the uterus, ectopic pregnancy, described with the use of other intrauterine contraceptives.

Special instructions and precautions:
Tablets 0.75 mg:
The drug at a dose of 0.75 mg is intended only for emergency postcoital contraception!
Recommended for women with regular menstrual cycles.
It is not allowed to use the drug at a dose of 0.75 mg as a means of permanent and continuous contraception. With regular sexual activity, it is recommended to use permanent methods of contraception (0.03 mg pills).
In case of uterine bleeding, a gynecological examination is recommended.
Dragee 0.03 mg:
In most women, taking levonorgestrel pills at a dose of 0.03 mg does not affect the menstrual cycle: menstruation occurs at regular intervals, bleeding has a normal duration and intensity. In some cases, there may be changes in the interval between menstruation and the intensity of menstrual bleeding, which is a consequence of the development of a new model of the menstrual cycle. In the event that menstrual bleeding has not occurred 6 weeks after the last menstruation, it is necessary to conduct an examination for the presence of pregnancy and, only in its absence, continue taking levonorgestrel. After stopping the use of levonorgestrel, the functions of the gonads are quickly restored to their full extent, which ensures a normal ability to conceive.
To help your doctor evaluate your menstrual cycle when taking levonorgestrel 0.03 mg, complete the calendar and show it to your doctor.
During the period of taking the first 14 tablets, it is recommended to use additional non-hormonal methods of contraception (with the exception of the temperature method).
The contraceptive effect of the drug may be affected by: irregular intake of pills, vomiting and intestinal disorders accompanied by diarrhea, in rare cases, individual metabolic characteristics and the intake of certain groups of medications (see "Drug Interactions").
During the first months of admission, intermenstrual bleeding of varying intensity may occur, which does not prevent the continuation of the drug.
In cases of skipping a dose or when taking it more than 24 hours after the previous dragee, the contraceptive effect of the drug stops. In such cases, it is necessary to continue taking the dragee. It should be borne in mind that the contraceptive effect in full will come only on the 14th day of daily administration of the drug. During this period, it is necessary to use non-hormonal methods of contraception (with the exception of the temperature method).
The use of levonorgestrel after childbirth, abortion, when using other hormonal contraceptives, as well as in nursing mothers, is carried out on the recommendation of a doctor.
Before starting and every 6 months of using levonorgestrel at a dose of 0.03 mg, it is recommended to undergo a general medical and gynecological examination (including examination of the mammary glands). In cases of migraine-like headaches or unusually severe headaches, sudden visual and hearing impairments, signs of thrombophlebitis or thromboembolism, a significant increase in blood pressure, hepatitis, jaundice, generalized itching, increased epileptic seizures, severe pain in the epigastric region, you must immediately stop taking medication and consult a doctor.
Capsules:
3 months after the implantation of the capsules and once a year, medical supervision is necessary. Indications for immediate removal of capsules are acute visual impairment, planned surgery followed by immobilization for 6 months, the appearance of symptoms of thrombophlebitis or thromboembolism, acute liver disease, migraine.
Intrauterine system (mirena):
Before the introduction of the intrauterine system (mirena), a woman is recommended to undergo a thorough general medical and gynecological examination (including examination of the mammary glands), to exclude pregnancy. In addition, sexually transmitted diseases should be excluded. Preventive control examinations should be carried out at least once a year.
In some women, when using the intrauterine system (mirena), oligomenorrhea or amenorrhea develops, which has a therapeutic effect in menorrhagia. After removal of the intrauterine system, menstrual function is restored.
The design of the intrauterine system ensures the release of levonorgestrel at a rate of 20 mg / day. The intrauterine system is effective for 5 years. The ability to bear children is restored in 50% of women 6 months after the removal of the contraceptive, in 96% - after 12 months.

Drug interaction:
It is possible to reduce the contraceptive effect of levonorgestrel when used together with rifampicin, ampicillin and tetracycline, some antiepileptic drugs (for example, carbamazepine, fenition, etc.), barbiturates, benzodiazepines.
Due to the influence of steroid hormones on glucose tolerance, when taking progestin drugs, the dosage of antidiabetic drugs and insulin may be adjusted.

Gross formula

C 21 H 28 O 2

Pharmacological group of the substance Levonorgestrel

Nosological classification (ICD-10)

CAS code

797-63-7

Characteristics of the substance Levonorgestrel

Synthetic progestogen with a molecular weight of 315.45.

Pharmacology

pharmachologic effect- contraceptive, gestagenic.

Pharmacodynamics

Levonorgestrel is a synthetic gestagen with a contraceptive effect, pronounced gestagenic and antiestrogenic properties.

When taken orally at the recommended dosage regimen, levonorgestrel inhibits ovulation and fertilization if sexual intercourse occurs in the preovulatory phase, when the possibility of fertilization is greatest. It can also cause changes in the endometrium that prevent implantation of a fertilized egg. Increases the viscosity of the secret of the cervix, which prevents the advancement of spermatozoa. Levonorgestrel is ineffective if implantation has already occurred.

Efficiency: it is recommended to start taking levonorgestrel as soon as possible (but no later than 72 hours) after sexual intercourse, if no protective contraceptive measures were used. The more time elapsed between sexual intercourse and taking the drug, the lower its effectiveness (95% during the first 24 hours, 85% from 24 to 48 hours and 58% from 48 to 72 hours). At the recommended dose, levonorgestrel does not have a significant effect on blood coagulation factors, lipid and carbohydrate metabolism.

As part of the intrauterine therapeutic system (ITS), the released levonorgestrel has mainly a local progestogenic effect. The progestogen (levonorgestrel) is released directly into the uterine cavity, which allows it to be used at 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 exerting a strong antiproliferative effect. When using levonorgestrel as part of the VTS, morphological changes in the endometrium and a weak local reaction to the presence of a foreign body in the uterus are observed. Increasing the viscosity of the cervical secretion prevents the penetration of sperm into the uterus. Levonorgestrel as part of the VTS prevents fertilization due to inhibition of sperm motility and function in the uterus and fallopian tubes. Some women also experience suppression of ovulation. The previous use of levonorgestrel as part of the VTS does not affect the childbearing function. Approximately 80% of women who wish to have a child become pregnant within 12 months after the removal of the PTS.

In the first months of using levonorgestrel as part of the VTS, due to the process of inhibition of endometrial proliferation, there may be an initial increase in spotting bloody discharge from the vagina. Following this, a pronounced suppression of endometrial proliferation leads to a decrease in the duration and volume of menstrual bleeding in women using levonorgestrel as part of the VTS. Scanty bleeding often transforms into oligo- or amenorrhea. At the same time, ovarian function and the concentration of estradiol in the blood plasma remain normal.

Levonorgestrel as part of VTS can be used to treat idiopathic menorrhagia, i.e. menorrhagia in the absence of hyperplastic processes in the endometrium (endometrial cancer, metastatic lesions of the uterus, submucosal or large interstitial myomatous node, leading to deformation of the uterine cavity, adenomyosis), endometritis, extragenital diseases and conditions accompanied by severe hypocoagulation (for example, von Willebrand disease, severe thrombocytopenia), symptoms of which is menorrhagia. After 3 months of using levonorgestrel as part of the VTS, menstrual blood loss in women with menorrhagia is reduced by 62-94% and by 71-95% after 6 months of use. When using levonorgestrel as part of VTS for two years, its effectiveness (reducing menstrual blood loss) is comparable to surgical methods of treatment (ablation or resection of the endometrium). A less favorable response to treatment is possible with menorrhagia due to submucosal uterine myoma. Reducing menstrual blood loss reduces the risk of iron deficiency anemia. Levonorgestrel as part of the VTS reduces the severity of symptoms of dysmenorrhea.

The efficacy of levonorgestrel as part of the VTS in preventing endometrial hyperplasia during chronic estrogen therapy was equally high with both oral and transdermal estrogen.

Pharmacokinetics

Absorption

When taken orally, levonorgestrel is rapidly and almost completely absorbed. Absolute bioavailability is 100% of the dose taken.

After the introduction of VTS, levonorgestrel begins to be immediately released into the uterine cavity, as evidenced by the measurement data of its concentration in the blood plasma. The high local exposure of levonorgestrel in the uterine cavity, which is necessary for its local effect on the endometrium, provides a high concentration gradient in the direction from the endometrium to the myometrium (the concentration of levonorgestrel in the endometrium exceeds its concentration in the myometrium by more than 100 times) and low concentrations of levonorgestrel in blood plasma ( the concentration of levonorgestrel in the endometrium exceeds its concentration in blood plasma by more than 1000 times). Rate of release of levonorgestrel into the uterine cavity in vivo initially is approximately 20 mcg / day, and after 5 years it decreases to 10 mcg / day.

Distribution

After taking a dose of 0.75 mg or 1.5 mg Cmax of levonorgestrel in plasma is 14.1 or 18.5 ng / ml, respectively, and Tmax is 1.6 or 2 hours, respectively. After reaching Cmax, the concentration of levonorgestrel decreases.

Levonorgestrel binds nonspecifically to plasma albumin and specifically to SHBG. About 1-2% of circulating levonorgestrel is present as the free steroid, while 42-62% is specifically bound to SHBG.

During the use of levonorgestrel as part of the VTS, the concentration of SHBG decreases. Accordingly, the fraction associated with SHBG decreases during this period, while the free fraction increases. The average apparent V d of levonorgestrel is about 106 liters.

After the start of administration as part of the VTS, levonorgestrel is detected in the blood plasma an hour later, T max is 2 weeks. According to the decreasing release rate, the median plasma concentration of levonorgestrel in women reproductive age with a body weight above 55 kg decreases from 206 pg / ml (25-75th percentile: 151-264 pg / ml), determined after 6 months, to 194 pg / ml (146-266 pg / ml) after 12 months and up to 131 pg / ml (113-161 pg / ml) after 60 months.

It has been shown that body weight and plasma SHBG concentration affect the systemic concentration of levonorgestrel, i.e. with low body weight and / or high concentration of SHBG, the concentration of levonorgestrel is higher. In women of reproductive age with low body weight (37-55 kg), the median plasma concentration of levonorgestrel is approximately 1.5 times higher.

In postmenopausal women who use levonorgestrel as part of the VTS simultaneously with the use of intravaginal or transdermal estrogens, the median plasma concentration of levonorgestrel decreases from 257 pg / ml (25-75th percentile: 186-326 pg / ml), determined after 12 months , up to 149 pg / ml (122-180 pg / ml) after 60 months. When using levonorgestrel as part of the VTS simultaneously with oral estrogen, the concentration of levonorgestrel in blood plasma, determined after 12 months, increases to approximately 478 pg / ml (25-75th percentile: 341-655 pg / ml), which is due to the induction of SHBG synthesis .

Biotransformation

Levonorgestrel is largely metabolized. The main metabolites in plasma are unconjugated and conjugated forms of 3α-, 5β-tetrahydrolevonorgestrel. Pharmacologically active metabolites of levonorgestrel are unknown. Based on research results in vitro and in vivo, 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.

Elimination

The total clearance of levonorgestrel from blood plasma is approximately 1 ml / min / kg. In unchanged form, levonorgestrel is excreted only in trace amounts. Metabolites are excreted through the intestines and by the kidneys with an excretion coefficient equal to »1.77. T 1/2 after oral administration and when using levonogestrel as part of the VTS (in the terminal phase, represented mainly by metabolites), is about a day.

Linearity/Nonlinearity

VTS. The pharmacokinetics of levonorgestrel depends on the concentration of SHBG, which, in turn, is influenced by estrogens and androgens. When using levonorgestrel as part of the VTS, a decrease in the average concentration of SHBG by approximately 30% was observed, which was accompanied by a decrease in the concentration of levonorgestrel in the blood plasma. This indicates the non-linearity of the pharmacokinetics of levonorgestrel during the time of its use as part of the VTS. Given the predominantly local action of levonorgestrel as part of the VTS, the effect of changes in systemic concentrations of levonorgestrel on its effectiveness in this case is unlikely.

The use of the substance Levonorgestrel

inside. Emergency postcoital contraception in women (after unprotected intercourse or unreliability of the contraceptive method used).

For VTS. Contraception (long-term), idiopathic menorrhagia, prevention of endometrial hyperplasia during estrogen replacement therapy.

Contraindications

inside. Hypersensitivity to levonorgestrel; severe liver failure; pregnancy (including intended); breastfeeding period; age up to 16 years.

For VTS. Pregnancy or suspicion of it; existing or recurrent inflammatory diseases of the pelvic organs; infections of the lower urinary and genital tract; postpartum endometritis; septic abortion within the last 3 months; cervicitis; diseases accompanied by increased susceptibility to infections; cervical dysplasia; malignant neoplasms of the uterus or cervix; progestogen-dependent tumors, incl. mammary cancer; pathological uterine bleeding of unknown etiology; congenital or acquired anomalies of the uterus, incl. fibromyomas leading to deformation of the uterine cavity; acute diseases or tumors of the liver; hypersensitivity to levonorgestrel.

The use of levonorgestrel as part of VTS has not been studied in women over 65 years of age, therefore it is not recommended for this category of patients.

Application restrictions

inside. Diseases of the liver or biliary tract, jaundice (including history), Crohn's disease; a history of inflammatory diseases of the pelvic organs or ectopic pregnancy; the presence of a hereditary or acquired predisposition to thrombosis.

For VTS. 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; birth defects heart or valvular heart disease (because of the risk of developing septic endocarditis); diabetes.

Levonorgestrel should not be taken during pregnancy. If pregnancy developed while taking it, then, based on the available data, an adverse effect of levonorgestrel on the fetus is not expected.

PTS. The use of levonorgestrel as part of the VTS is contraindicated in pregnancy or suspected pregnancy. Pregnancy in women who have a VTS containing levonorgestrel is extremely rare. But if there is a prolapse of the PTS from the uterine cavity, the woman is no longer protected from pregnancy, and must use other methods of contraception before consulting a doctor.

During the use of levonorgestrel as part of the VTS, some women do not have menstrual bleeding. The absence of menstruation is not necessarily a sign of pregnancy. If a woman does not have periods and at the same time there are other signs of pregnancy (nausea, fatigue, soreness of the mammary glands), then it is necessary to consult a doctor for examination and a pregnancy test.

If pregnancy occurs in a woman during the use of levonorgestrel as part of the VTS, it is recommended to remove the VTS, because. any intrauterine contraceptive device left in situ increases the risk of spontaneous abortion, infection, or premature birth. Removing the PTS or probing the uterus can lead to spontaneous abortion. If careful removal of the intrauterine contraceptive is not possible, medical abortion should be discussed. If a woman wants to keep the pregnancy and VTS cannot be removed, the patient should be informed about the risks, in particular, about the possible risk of septic abortion in the second trimester of pregnancy, postpartum purulent-septic diseases, which can be complicated by sepsis, septic shock and death, as well as the possible consequences premature birth for a baby.

In such cases, the course of pregnancy should be carefully monitored. An ectopic pregnancy must be ruled out. A woman should be explained that she should inform the doctor about all symptoms suggesting complications of pregnancy, in particular, the appearance of spastic pain in the lower abdomen, bleeding or bloody discharge from the vagina, and fever. Levonorgestrel as part of the VTS is released into the uterine cavity. This means that the fetus is exposed to a relatively high local concentration of the hormone, although the hormone enters it in small quantities through the blood and placenta. Due to the intrauterine use and local action of the hormone, the possibility of a virilizing effect on the fetus must be taken into account. Due to the high contraceptive efficacy of levonorgestrel as part of the VTS, clinical experience related to pregnancy outcomes with its use is limited. However, the woman should be informed that at this point in time there is no evidence of birth defects caused by the use of levonorgestrel as part of the VTS in cases of continuation of pregnancy until delivery without removal of the VTS.

Levonorgestrel passes into breast milk. After taking it, breastfeeding should be stopped for 24 hours.

VTS. Breast-feeding child when using levonorgestrel as part of the VTS is not contraindicated. About 0.1% of a dose of levonorgestrel can enter the child's body during breastfeeding. However, it is unlikely to pose a risk to the child at doses released into the uterine cavity after insertion of the VTS.

It is believed that the use of levonorgestrel as part of the VTS 6 weeks after birth 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 levonorgestrel as part of VTS during lactation.

Fertility. After the removal of the PTS in women, fertility is restored.

Side effects of Levonorgestrel

The frequency of side effects (PD) after taking levonorgestrel: very often (≥1 / 10); often (≥1/100,

Often- nausea, fatigue, abdominal pain, acyclic bloody issues(bleeding).

Often- vomiting, diarrhea, dizziness, headache, soreness of the mammary glands, tension of the mammary glands, dysmenorrhea, heavy menstrual bleeding, delayed menstruation (no more than 5-7 days; if menstruation does not occur for a longer period, pregnancy must be excluded). Allergic reactions are possible: urticaria, rash, itching, swelling of the face.

VTS. In most women, after the installation of VTS containing levonorgestrel, there is a change in the nature of cyclic bleeding. During the first 90 days of use, an increase in the duration of bleeding is noted by 22% of women, and irregular bleeding occurs in 67% of women, the frequency of these phenomena decreases to 3 and 19%, respectively, by the end of the 1st year of VTS use. At the same time, amenorrhea develops in 0%, and rare bleeding in 11% of patients during the first 90 days of use. By the end of the first year of use, the frequency of these phenomena increases to 16 and 57%, respectively.

When using levonorgestrel as part of the VTS in combination with long-term estrogen replacement therapy in most women during the 1st year of use, cyclic bleeding gradually stops.

Below are data on the incidence of PD, which were reported with the use of levonorgestrel as part of the VTS. Frequency of occurrence of PD: very often (≥1/10); often (≥1 / 100, MedDRA. Frequency data reflect the approximate incidence of PD registered during clinical trials of levonorgestrel as part of VTS for the indications "contraception" and "idiopathic menorrhagia" involving 5091 women.

PD reported in clinical trials of levonorgestrel as part of VTS for the indication "prevention of endometrial hyperplasia during estrogen replacement therapy" (involving 514 women) were observed with the same frequency, except for cases indicated by asterisks (*, **) .

From the side immune system: frequency unknown - hypersensitivity to levonorgestrel, including rash, urticaria and angioedema.

From the side of the psyche: often - depressed mood, depression.

From the side of the nervous system: very often - headache; often migraine.

From the gastrointestinal tract: very often - abdominal pain, pain in the pelvic area; often - nausea.

From the skin and subcutaneous tissues: often - acne, hirsutism; infrequently - alopecia, itching, eczema.

From the musculoskeletal system and connective tissue: often - back pain**.

From the reproductive system and mammary glands: very often - a change in the volume of blood loss, including an increase and decrease in the intensity of bleeding, spotting, oligomenorrhea, vulvovaginitis *, discharge from the genital tract *; often - infections of the pelvic organs, ovarian cysts, dysmenorrhea, pain in the mammary glands **, engorgement of the mammary glands, expulsion of the VTS (complete or partial); rarely - perforation of the uterus (including penetration).

Survey results: frequency unknown - increased blood pressure.

* Often according to the indication "prevention of endometrial hyperplasia during estrogen replacement therapy."

** Very often, according to the indication "prevention of endometrial hyperplasia during estrogen replacement therapy."

To describe certain reactions, their synonyms and related states, in most cases, terminology is used corresponding to MedDRA.

Interaction

With the simultaneous use of drugs - inducers of microsomal liver enzymes, there is an acceleration of the metabolism of levonorgestrel.

The following drugs may reduce the effectiveness of levonorgestrel: amprenavir, lansoprazole, nevirapine, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates (including primidone), phenobarbital, phenytoin and carbamazepine, drugs containing St. John's wort (Hypericum perforatum), as well as rifampicin, ritonavir, ampicillin, tetracycline, rifabutin, griseofulvin, efavirenz. Reduces the effectiveness of hypoglycemic and anticoagulant (coumarin derivatives, phenindione) drugs. Increases plasma concentrations of corticosteroids. Drugs containing levonorgestrel may increase the risk of cyclosporine toxicity due to the suppression of its metabolism.

Levonorgestrel may reduce the effectiveness of ulipristal by competing with the progesterone receptor. Therefore, the simultaneous use of drugs containing levonorgestrel with ulipristal preparations is not recommended.

For military-technical cooperation(additionally). The effect of inducers of microsomal liver enzymes on the effectiveness of levonorgestrel in the composition of the VTS is unknown, but it is believed that it is not significant, since levonorgestrel in the composition of the VTS has a mainly local effect.

Overdose

Symptoms: nausea, vomiting, spotting/bleeding.

Treatment: symptomatic, there is no specific antidote.

For VTS. Not applicable.

Routes of administration

Inside, intrauterine.

Precautions for the substance Levonorgestrel

When taken orally

Levonorgestrel should only be taken for emergency contraception. Repeated use within one menstrual cycle is not recommended.

Levonorgestrel should be taken as soon as possible, but no later than 72 hours after unprotected intercourse. The effectiveness of emergency contraception with delayed use is significantly reduced.

Levonorgestrel does not replace the use of permanent methods of contraception. In most cases, it does not affect the nature of the menstrual cycle. However, there may be acyclic spotting and a delay in menstruation for several days. With a delay in menstruation for more than 5-7 days and a change in its nature (scanty or heavy discharge), pregnancy must be excluded. The appearance of pain in the lower abdomen, fainting may indicate an ectopic (ectopic) pregnancy.

In adolescents under 16 years of age, the use of levonorgestrel is possible only in exceptional cases (including rape) and only after consulting a gynecologist. After emergency contraception, a second consultation with a gynecologist is recommended.

In diseases of the gastrointestinal tract (eg Crohn's disease), as well as in overweight women, the effectiveness of levonorgestrel may decrease.

Levonorgestrel should be used with caution in women with liver or biliary tract disease, with a history of pelvic inflammatory disease or ectopic pregnancy, with a hereditary or acquired predisposition to thrombosis.

When using the military-technical cooperation

Before installing a VTS containing levonorgestrel, pathological processes in the endometrium should be excluded, since irregular bleeding / spotting is often noted in the first months of its use. Also, pathological processes in the endometrium should be excluded if bleeding occurs after the start of estrogen replacement therapy in a woman who continues to use levonorgestrel as part of the VTS, previously established for contraception. Appropriate diagnostic measures should also be taken when irregular bleeding develops during long-term treatment.

Levonorgestrel as part of VTS is not used for postcoital contraception.

Levonorgestrel as part of VTS 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 VTS, these patients should be given antibiotics for prophylaxis.

Levonorgestrel in low doses can affect glucose tolerance, and therefore its plasma concentration should be regularly monitored in women with diabetes who use levonorgestrel as part of VTS. 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.

Levonorgestrel as part of the VTS is not a first-choice drug for either young, previously unpregnant women, or for postmenopausal women with severe uterine atrophy.

Available data suggest that the use of levonorgestrel as part of VTS 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 this drug in the indication "prevention of endometrial hyperplasia during estrogen replacement therapy", the risk of breast cancer when it is used for this indication cannot be confirmed or refuted.

Oligo- and amenorrhea. Oligo- and amenorrhea in women of childbearing age develops gradually, in about 57 and 16% of cases by the end of the first year of using levonorgestrel as part of the VTS, respectively. If menstruation is absent within the 6th week after the start of the last menstruation, pregnancy should be excluded. Repeat pregnancy tests for amenorrhea are not necessary unless there are other signs of pregnancy.

When levonorgestrel in VTS is used in combination with continuous estrogen replacement therapy, most women gradually develop amenorrhea during the first year.

Pelvic inflammatory disease (PID). The guidewire helps protect the levonorgestrel-containing PTS from infection during insertion, and the PTS inserter is specifically designed to minimize the risk of infection. PID in patients using VTS is often classified as a sexually transmitted disease. It has been established that the presence of multiple sexual partners is a risk factor for PID. PID 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 group A streptococcal sepsis) can develop after PTS placement, although this is extremely rare.

For recurrent endometritis or PID, or for severe or acute infections that are resistant to treatment for several days, levonorgestrel-containing VTS should be removed. If a woman has persistent pain in the lower abdomen, chills, fever, pain associated with sexual intercourse (dyspareunia), prolonged or heavy spotting/bleeding from the vagina, a change in the nature of the discharge from the vagina, you should immediately consult a doctor. Severe pain or fever that occurs shortly after PTS placement may indicate a severe infection that needs to be treated promptly. Even in cases where only a few symptoms indicate the possibility of infection, bacteriological examination and monitoring are indicated.

Expulsion. Possible signs of partial or complete expulsion of any PTS are bleeding and pain. Contractions of the muscles of the uterus during menstruation sometimes lead to displacement of the PTS or even to push it out of the uterus, which leads to the termination of the contraceptive effect. Partial expulsion may reduce the effectiveness of VTS containing levonorgestrel. Since levonorgestrel in the composition of the VTS reduces menstrual blood loss, its increase may indicate the expulsion of the VTS. A woman is advised to check the threads with her fingers, for example, while taking a shower. If a woman finds signs of displacement or loss of the PTS or does not feel the threads, sexual intercourse or other methods of contraception should be avoided, and a doctor should be consulted as soon as possible.

If the position in the uterine cavity is incorrect, the PTS should be removed. At the same time, a new system can be installed.

Perforation and penetration. Perforation or penetration of the body or cervix of the PTS occurs rarely, mainly during insertion, and may reduce the effectiveness of levonorgestrel as part of the PTS. In these cases, the system should be removed. With a delay in diagnosing perforation and migration of VTS, complications such as adhesions, peritonitis, intestinal obstruction, intestinal perforation, abscesses or erosion of adjacent internal organs can be observed. The risk of uterine perforation is increased in breastfeeding women. There may be an increased risk of perforation when inserting a VTS after childbirth and in women with a fixed uterine tilt.

ectopic pregnancy. Women with a history of ectopic (ectopic) pregnancy, who have had fallopian tube 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 lower abdominal pain, 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 VTS containing levonorgestrel is approximately 0.1% per year. The absolute risk of ectopic pregnancy in women using this drug is low. However, if a woman with an established PTS containing levonorgestrel becomes pregnant, the relative likelihood of an ectopic pregnancy is higher.

Thread loss. If, during a gynecological examination, the threads for removing the PTS cannot be found in the cervical region, pregnancy must be excluded. The threads can be drawn into the uterine cavity or cervical canal and become visible again after the next menstruation. If pregnancy is excluded, the location of the threads can usually be determined using careful probing with an appropriate instrument. If the threads cannot be detected, it is possible that an expulsion of the PTS from the uterine cavity has occurred. Ultrasound can be used to determine the correct location of the system. If it is unavailable or unsuccessful, an X-ray examination is used to determine the location of the VTS.

Ovarian cysts. Since the contraceptive effect of levonorgestrel in the composition of the VTS is due mainly to its local action, women of childbearing age usually experience ovulatory cycles with rupture of the follicles. Sometimes the atresia of the follicles is delayed, and their development can continue. These enlarged follicles are clinically indistinguishable from ovarian cysts. Ovarian cysts have been reported as an adverse reaction in approximately 7% of women using VTS containing levonorgestrel. 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 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 carrying out therapeutic and diagnostic measures. In rare cases, it is necessary to resort to surgical intervention.

The use of levonorgestrel as part of VTS in combination with estrogen replacement therapy. When using levonorgestrel in the composition of VTS in combination with estrogen, it is necessary to additionally take into account the information specified in the instructions for use of the corresponding estrogen.

Influence on the ability to drive vehicles and work mechanisms. The effect of levonorgestrel on the ability to drive and use machines has not been studied. In case of dizziness, one should refrain from driving vehicles and working with mechanisms that require increased concentration of attention and speed of psychomotor reactions.

Formula: C21H28O2, chemical name: (17alpha)-13-ethyl-17-hydroxy-18,19-dinopregn-4-en-20-yn-3-one.
Pharmacological group: hormones and their antagonists / estrogens, gestagens; their homologues and antagonists.
Pharmachologic effect: gestagenic, contraceptive.

Pharmacological properties

Levonorgestrel is the pharmacologically active isomer of norgestrel. Levonorgestrel is twice as strong as norgestrel. Levonorgestrel changes the endometrium and slows down ovulation, prevents the implantation of a fertilized egg, reduces the sensitivity of the progesterone and estrogen receptors of the endometrium, making it immune to estradiol and exerting a strong antiproliferative effect. Levonorgestrel interferes with the advancement of spermatozoa as a result of an increase in the viscosity of cervical mucus. Levonorgestrel as part of an intrauterine therapeutic system has a local direct effect on the fallopian tubes, endometrium, and the viscosity of the mucus of the cervical canal. Levonorgestrel acts on the gonadotropic function of the pituitary gland, resulting in a slight decrease in the peak of luteinizing and follicle-stimulating hormones.
When taken orally, it is completely and rapidly absorbed in the gastrointestinal tract, bioavailability is approximately 100%. The maximum concentration in blood serum when taking 0.75 mg once is achieved after 0.9 - 2.3 hours and is 6.4 - 21.8 ng / ml. Levonorgestrel binds to plasma albumin by about 50% and sex hormone-binding globulin by 47.5%. The mean apparent volume of distribution of levonorgestrel is about 106 liters. Levonorgestrel is metabolized in the liver with the formation of pharmacologically inactive metabolites (conjugated and unconjugated forms of 3alpha-, 5beta-tetrahydrolevonorgestrel). The main isoenzyme involved in the metabolism of levonorgestrel is CYP3A4. CYP2E1, CYP2C19, and CYP2C9 isoenzymes may also be involved, but to a lesser extent. The half-life is 19.1 - 29.7 hours. The total clearance of levonorgestrel from blood plasma is about 1.0 ml / min / kg. Levonorgestrel is excreted mainly in the urine, a small amount is excreted in the faeces.
When using an intrauterine therapeutic system, the rate of release of levonorgestrel into the uterus at the beginning is about 20 micrograms per day, and after five years it decreases to about 11 micrograms per day. The average release rate of levonorgestrel is about 14 mcg per day for up to 5 years. Intrauterine therapeutic systems can be used in women who are receiving hormone replacement therapy, along with transdermal or oral estrogen preparations that do not contain progestogens. After administration, levonorgestrel is found in plasma after an hour, the maximum concentration is reached 2 weeks after the administration of the drug.

Indications

Intrauterine therapeutic system: idiopathic menorrhagia, contraception (long-term), prevention of endometrial hyperplasia during estrogen replacement treatment.
Inside: emergency postcoital contraception in women (including after unprotected intercourse, and if the method of contraception used is not reliable).

Dosing and Administration of Levonorgestrel

Levonorgestrel is taken orally, administered intrauterine. Inside, it is used in the first 96 hours after intercourse at a dose of 0.75 - 1.5 mg. The method of emergency contraception is not recommended to be used more than once every 4 to 6 months. Intrauterine, an intrauterine therapeutic system is inserted into the uterine cavity.
Due to the possibility of menstrual dysfunction, repeated use of levonorgestrel by mouth during the same menstrual cycle should be avoided. Do not use oral forms of levonorgestrel as a means of continuous and regular contraception, as this leads to an increase in side effects and a decrease in the effectiveness of the drug.
If uterine bleeding occurs after emergency postcoital contraception, a gynecological examination is recommended, and if menstruation is delayed by more than 5 to 7 days, pregnancy should be excluded.
Only after consulting a gynecologist and only in exceptional cases (including rape) is it possible to use levonorgestrel for emergency postcoital contraception in adolescents under 16 years of age.
Before installing an intrauterine therapeutic system, it is necessary to conduct a gynecological and general medical examination, including examination of the mammary glands, pelvic organs, examination of a smear from the cervix.
A re-examination is necessary 4-12 weeks after the installation of the intrauterine therapeutic system, then 1 time per year or more often, if indicated. The intrauterine therapeutic system remains effective for five years. An intrauterine therapy system should only be installed by a doctor who is well trained in this procedure or has experience with this form of the drug.
Women who take progestogen-containing contraceptives may increase the risk of venous thrombosis. When symptoms of venous thrombosis appear, appropriate diagnostic and therapeutic measures should be taken immediately.
After removal of the intrauterine therapeutic system, the ability to bear children is restored after six months in 50% of women, in a year - in 96.4%.
The contraceptive effect of levonorgestrel is less effective in overweight patients.

Contraindications for use

Hypersensitivity, thrombophlebitis, thromboembolic disorders, coronary artery disease, cerebrovascular disease, pregnancy (or suspicion of it); additionally for oral administration - jaundice (including history), severe pathology of the biliary tract or liver, breastfeeding, puberty; additionally for the intrauterine therapeutic system - lower urinary tract infections, recurrent or existing inflammatory diseases of the pelvic organs, postpartum endometritis, cervicitis, acute diseases or liver tumors, septic abortion within the last 3 months, cervical dysplasia, pathological uterine bleeding of unknown origin, malignant neoplasms of the cervix or uterus, acquired or congenital anomalies of the uterus, including fibromyomas that deform the uterine cavity; progestogen-dependent tumors, including breast cancer; pathology, which is accompanied by increased susceptibility to infections, age over 65 years (no safety data).

Application restrictions

For intrauterine therapeutic system. After consulting a doctor: unusually severe headache, migraine, focal migraine with asymmetric loss of vision or other symptoms that indicate transient cerebral ischemia; severe arterial hypertension, jaundice, severe circulatory disorders, including myocardial infarction and stroke; diabetes.
The feasibility of removing the intrauterine therapeutic system should be discussed at the first occurrence or presence of any of the above conditions.

Use during pregnancy and lactation

The use of levonorgestrel is contraindicated during pregnancy.
If pregnancy occurs while using an intrauterine therapeutic system, it is recommended that the system be removed because any intrauterine contraceptive that is left in situ increases the risk of preterm labor and miscarriage. Probing the uterus or removing the intrauterine therapy system can lead to spontaneous miscarriage. It is necessary to discuss the feasibility of artificial termination of pregnancy when it is impossible to carefully remove the intrauterine contraceptive. If the intrauterine therapeutic system cannot be removed and the woman wants to continue the pregnancy, the patient should be informed about the possible consequences and risks of preterm birth for the baby. In these cases, careful monitoring of the course of pregnancy is necessary. In a woman with an intrauterine therapeutic system installed, the risk of an ectopic pregnancy is increased, so it is necessary to exclude ectopic pregnancy. The woman must be explained that she must immediately report all symptoms that suggest a complication of pregnancy (for example, colicky abdominal pain that is accompanied by fever, and others).
Levonorgestrel is excreted in breast milk: when breastfeeding, approximately 0.1% of the drug enters the child's body with breast milk. Breastfeeding while taking oral levonorgestrel for emergency postcoital contraception should be stopped for 36 hours.
For the intrauterine therapeutic system, it is considered that the use of any pure progestogen method of contraception 6 weeks after birth does not adversely affect the development and growth of the child, therefore, the drug is unlikely to pose a risk to the child at doses that are released by the intrauterine therapeutic system located in the uterine cavity .

Side effects of levonorgestrel

Nervous system and sense organs: nervousness, low mood, headache, depression, migraine, mood lability, fatigue, dizziness, corneal curvature changes, contact lens intolerance.
Digestive system: abdominal pain, nausea, bloating, vomiting, diarrhea, flatulence, abdominal cramps.
Urogenital system: spotting, uterine/vaginal bleeding, benign ovarian cysts, oligo- and amenorrhea, heavy menstrual bleeding, pelvic pain, scanty menstrual bleeding, dysmenorrhea, vulvovaginitis, vaginal discharge, breast tightness, decreased libido, breast tenderness , endometritis, pelvic inflammatory disease, cervicitis, uterine perforation, chloasma, vaginal candidiasis, changes in cervical secretion, ectopic pregnancy, sensation of threads by a partner during intercourse, breast cancer,
Skin covers: acne, rash, alopecia, hirsutism, eczema, itching, rash, urticaria.
Others: back pain, weight gain, edema, weight loss, high blood pressure, hypersensitivity to the drug or a component of the drug, including urticaria, rash, angioedema, sepsis.
During the insertion/removal of the intrauterine therapy system: pain, bleeding, vasovagal reaction accompanied by dizziness or fainting, epileptic seizure in patients with epilepsy.

Interaction of levonorgestrel with other substances

With the combined use of levonorgestrel with inducers of cytochrome P450 isoenzymes, the effect of levonorgestrel may be reduced by increasing its metabolism. The following medicines may decrease the effectiveness of levonorgestrel: lansoprazole, amprenavir, nevirapine, tacrolimus, oxcarbazepine, topiramate, barbiturates (including primidone), tretinoin, carbamazepine, phenytoin, St. rifabutin, tetracycline, griseofulvin. Levonorgestrel reduces the effectiveness of anticoagulants (coumarin derivatives, phenindione), hypoglycemic, antihypertensive, anticonvulsant drugs. Levonorgestrel increases the content of glucocorticosteroids in the blood serum. Levonorgestrel may increase the toxicity of cyclosporine due to the suppression of its metabolism. Levonorgestrel can disrupt the metabolism of chlordiazepoxide and diazepam, which leads to cumulation in the blood plasma of the latter. Due to the inhibition of enterohepatic recirculation of sex steroids, which is associated with a change in the intestinal flora, an increase in intermenstrual bleeding may occur when levonorgestrel is used together with sulfamethoxypyridazine, ampicillin, chloramphenicol, phenoxymethipenicillin, nitrofurantoin, neomycin.

Overdose

With an overdose of levonorgestrel, side effects increase. Symptomatic treatment is necessary, there is no specific antidote.

Trade names of drugs with the active ingredient levonorgestrel

Combined drugs:
Levonorgestrel + Ethinylestradiol: Anteovin, Microgynon®, Minisiston, Minisiston® 20 fem, Ovidon, Oralcon, Trigestrel, Triquilar®;
Levonorgestrel + Estradiol: Klimonorm®;
Ethinylestradiol + Levonorgestrel: Rigevidon®, Rigevidon® 21+7, Tri-regol®, Tri-regol® 21+7, Triquilar®.

Levonorgestrel is a contraceptive drug.

Composition and form of release

The pharmaceutical industry produces a contraceptive in capsules and in the form of an intrauterine therapeutic system, where the active ingredient is levonorgestrel.

Pharmacological properties

Levonorgestrel is an isomer of norgestrel. The drug changes the endometrium, helps to slow down ovulation, in addition, prevents the introduction of a fertilized egg into the uterine tissue, reduces the sensitivity of endometrial receptors, and has an antiproliferative effect.

The contraceptive drug increases the viscosity of the so-called cervical mucus, which prevents sperm from moving into the uterus. Levonorgestrel, present in the intrauterine therapeutic system, affects the endometrium, fallopian tubes, and mucus viscosity.

When taking Levonorgestrel, its bioavailability is 100%. The maximum concentration in the blood occurs within two hours. In plasma, it binds to albumin by 50%. Metabolized in the liver. The half-life is from 19 to 29 hours. It is excreted in the urine, a small part - with the stool.

When using an intrauterine therapeutic system, the active compound levonorgestrel is released into the uterus at 20 micrograms per day, after a five-year period - up to 11 micrograms per day.

Indications for use

Levonorgestrel is indicated for use as an intrauterine therapeutic system for idiopathic menorrhagia, in addition, as long-term contraception, and also for the prevention of endometrial hyperplasia.

Inside the drug Levonorgestrel is prescribed for emergency so-called postcoital contraception for women.

Contraindications for use

I will list in which situations the drug Levonorgestrel is contraindicated:

Hypersensitivity to the components of the drug;
With thrombophlebitis;
Pregnancy;
thromboembolic disorders;
Pathology of the coronary arteries;
Lactation;
Jaundice;
Cerebrovascular diseases;
Pathology of the biliary tract;
Do not use the drug during puberty;
urinary tract infections;
cervicitis;
Inflammatory pathology of the pelvic organs;
Dysplasia of the cervix;
Postpartum endometritis;
Tumors of the liver;
Pathological uterine bleeding;
anomalies of the uterus;
Tumors of the uterus;
Progestogen-dependent tumors;
Mammary cancer;
Age over 65 years.

With caution, a contraceptive is used when a woman has such symptoms, when installing an intrauterine therapeutic system, migraine, arterial hypertension, stroke, circulatory disorders, diabetes, myocardial infarction. If these symptoms appear, it is necessary to discuss with the doctor the advisability of removing the intrauterine system.

Application and dosage

The contraceptive Levonorgestrel is taken orally, in addition, it is administered intrauterine. Inside the capsules are used in the first four days after unprotected intercourse, usually the drug is used at a dose of 0.75 - 1.5 milligrams. Emergency contraception is not recommended more than once every 4 or 6 months.

Do not use oral forms of the pharmaceutical preparation Levonorgestrel as regular contraception, as this will lead to an increase in side effects and decrease the effectiveness of the drug.

Before installing an intrauterine therapeutic system in a woman, a gynecological examination should be performed on the patient. It is necessary to re-examine one month or 12 weeks after the installation of this system, which remains effective for a period of five years.

Side effects

The use of the contraceptive Levonorgestrel can cause the following side effects: a woman becomes more nervous, her mood decreases, headache is possible, fatigue, depression, migraine are observed, in addition, mood lability, dizziness, and intolerance to contact lenses.

The use of a contraceptive can cause negative manifestations from the side of digestion, which will manifest as pain in the abdomen, nausea, bloating, vomiting may occur, diarrhea, flatulence, and the patient may complain of abdominal cramps.

Other negative reactions to the drug will be as follows: spotting of a smearing nature, uterine bleeding, ovarian cysts, vulvovaginitis joins, tension of the mammary glands, endometritis, decreased libido, pain on palpation of the mammary glands, cervicitis, uterine perforation, vaginal candidiasis, on the skin there is a rash, acne, in addition, alopecia, hirsutism, urticaria.

Among other side effects, it can be noted: back pain, an increase in body weight, edema, an increase in blood pressure are characteristic, in addition, hypersensitivity to a contraceptive, angioedema, sepsis.

drug overdose

In case of an overdose of the contraceptive pharmaceutical Levonorgestrel, symptomatic treatment is carried out.

Special conditions

The contraceptive effect of Levonorgestrel is less effective in overweight women.

Analogues

Pharmaceutical Microlute, Postinor, in addition, Mirena, Eskinor-F, Norplant, and Escapel.

Conclusion

Before using the Levonorgestrel contraceptive, a woman should consult with an experienced gynecologist.

Levonorgestrel is an active ingredient in a whole group of emergency and permanent contraceptives. Its effect on the female body is significant, has contraindications and frequent side effects. In order not to harm health, it is important to study these issues in advance - before using the substance.

What is levonorgestrel for?

The main scope of drugs with the specified active substance is the prevention of unwanted pregnancy and emergency contraception.

The funds are issued in three forms - each has its own purpose of use:

• Tablets. Most often, medications are intended for emergency contraception after unprotected or poorly protected intercourse;
• Intrauterine device (IUD). Means of long-term contraception, the validity period is 5 years. In addition, the IUD can be used as preventive measure hyperplasia of the inner uterine membrane during estrogen treatment, as well as with heavy and painful menstruation;
• Capsules for subcutaneous implantation. Just like the IUD, they are a means of contraception with a duration of effectiveness of 5 years.

How does levonorgestrel work

When taking a drug containing levonorgestrel, effect on the woman's body happens according to the following mechanism:

1. Ovulation slows down, the intrauterine membrane succumbs to changes, as a result of which the fertilized egg cannot catch on and remain in the uterine cavity;
2. Under the influence of the active substance, the mucus contained in the cervix becomes denser, which prevents spermatozoa from approaching the egg.

Levonorgestrel as part of intrauterine devices works in the same way:

1. Changes in the structure of the endometrium;
2. Mucus acquires greater viscosity, density;
3. The patency of the fallopian tubes is reduced.

After the drug stops being used, the possibility of becoming pregnant is restored.

For whom is levonorgestrel contraindicated?

Due to its significant effect, the substance has many contraindications.

Refuse to take drugs with levonorgestrel should be in such cases:

• when a woman has an allergy to a substance;
• these contraceptives are prohibited during pregnancy and breastfeeding;
• contraindications are liver diseases;
• should not be taken by girls under 18 years of age;
• The IUD is not used for cervical dysplasia, malignant tumors in the genitals or mammary glands, and also if the woman has had a complicated abortion in the last 4 months.

Side effects from the use

Based on which contraceptive contains levonorgestrel, the likelihood of side effects can vary from 5 to 15%.

Most often, they are slightly noticeable, do not cause complications and special inconvenience.

The most common side effects:

• nausea, dysfunction intestinal tract;
• aching pain in the abdomen;
• loss of strength, irritability;
• disruptions in the menstrual cycle, changes in blood intensity, spotting at 2-3 weeks of the cycle;
• frequent headaches;
• tension and enlargement of the mammary glands;
• skin rashes;
• swelling of the lower extremities.

Medicines containing levonorgestrel

There is a large selection of contraceptives with the specified active substance. The funds listed below are issued in different forms and differ in the nature of the effect on the female body.

When choosing a contraceptive, be sure to pay attention to its bioavailability, or ability to be absorbed.

Name (issue form)	Maximum concentration after application	Advantages	Flaws
Levonorgestrel (tablets)	1 to 2 hours	1. The most inexpensive among analogues; 2. Long half-life; 3. The dosage is divided into 2 tablets. Due to this, the effective concentration of the active substance is maintained longer.	1. Insignificant amount of assimilation; 2. Often there are side effects - in 15% of cases.
Postinor (tablets)		1. Low price; 2. The package contains 2 tablets; 3. Side effects are observed in 8% of cases; 4. High bioavailability; 5. Maximum half-life.	1. The time required to reach the maximum concentration is above average.
Escapelle (tablets)		1. Maximum bioavailability; 2. Maximum half-life; 3. Side effects were seen in only 5% of cases.	1. Expensive drug; 2. Produced in 1 tablet, because the high concentration in the body does not last long.
Eskinor-F (tablets)		1. Released in 2 different dosages, which allows you to maintain efficiency for a long time; 2. Inexpensive medicine; 3. Maximum digestibility.	1. Sufficiently high probability of side effects - about 11%.
Microlute (tablets, IUD)	1 to 1.5 weeks	1. Can be used for permanent contraception; 2. It has a therapeutic effect in some gynecological pathologies; 3. On average, only 6% of cases of using the drug showed side effects.	1. Poorly absorbed; 2. Short half-life.
Norplant (capsules for implantation under the skin)		1. A convenient form of release allows you to use the drug for contraception for 5 years, without uterine intervention; 0

Levonorgestrel

Latin name

Levonorgestrel

chemical name

(17alpha)-13-Ethyl-17-hydroxy-18,19-dinopregn-4-en-20-yn-3-one

Gross formula

C 21 H 28 O 2

Pharmacological group

Estrogens, gestagens; their homologues and antagonists

Nosological classification (ICD-10)

N92 Abundant, frequent and irregular menstruation
N95.1 Menopausal and climacteric conditions of women
Z30.0 General advice and advice on contraception
Z30.5 Supervision of (intrauterine) contraceptive use

CAS code

797-63-7

Characteristic

Contraceptive (gestagen).

Pharmacology

Pharmacological action - contraceptive, gestagenic.

Causes inhibition of ovulation and changes in the endometrium, prevents the implantation of a fertilized egg. Increases the viscosity of cervical mucus, which prevents the advancement of spermatozoa.

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. It binds to serum albumin (approximately 50%) and sex hormone-binding globulin (47.5%). Metabolized in the liver, metabolites are pharmacologically inactive. T 1/2 - (24.4 ± 5.3) hours. Excreted mainly with urine, a small amount - with feces.

When using the IUD, the rate of release of levonorgestrel into the uterine cavity at the beginning is approximately 20 μg / day and decreases after five years to approximately 11 μg / day. The average rate of release of levonorgestrel is approximately 14 mcg / day for up to 5 years. An 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 method of contraception used cannot be considered reliable).

For intrauterine therapeutic system. Contraception (long-term), idiopathic menorrhagia, prevention of endometrial hyperplasia during estrogen replacement therapy.

Contraindications

Hypersensitivity, pregnancy (or suspicion of it); for oral administration (optional) - severe liver or biliary tract disease, 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 increased susceptibility to infections; cervical dysplasia, malignant neoplasms of the uterus or cervix, progestogen-dependent tumors, incl. mammary cancer; pathological uterine bleeding of unknown etiology, congenital or acquired anomalies of the uterus, incl. fibromyomas leading to deformation of the uterine cavity; acute diseases or tumors of the liver.

Application restrictions

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 feasibility of removing the IUD should be discussed if any of the following conditions are present or first occur.

Use during pregnancy and lactation

Contraindicated in pregnancy.

If pregnancy occurs while using the IUD, it is recommended to remove the system, as any IUD left in situ increases the risk of miscarriage and preterm birth. Removing the IUD or probing the uterus can lead to spontaneous miscarriage. If careful removal of the intrauterine contraceptive is not possible, the feasibility of artificial termination of pregnancy should be discussed. If a woman wants to continue 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 carefully monitored. An ectopic pregnancy should be ruled out (if a woman with an IUD inserted becomes pregnant, the relative risk of an ectopic pregnancy is increased). The woman should be advised that she should report all symptoms suggestive of a pregnancy complication, in particular colicky abdominal pain accompanied by fever.

Penetrates into breast milk: when breastfeeding, about 0.1% of levonorgestrel, along with breast milk, enters the body of a newborn. Breastfeeding after taking the drug orally 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 progestogen method of contraception 6 weeks after birth does not harmful influence on the growth and development of the child, it is unlikely to pose a risk to the child at doses released by the IUD located in the uterine cavity.

Side effects

In clinical trials, most often in women taking oral levonorgestrel (0.75 mg), nausea (23.1%), abdominal pain (17.6%), fatigue (16.9%), headache (16, 8%), violation of the menstrual cycle, 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

From 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, 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 use of inducers of cytochrome P450 isoenzymes, the metabolism of levonorgestrel may increase and the effect may decrease. The following drugs may reduce the effectiveness of levonorgestrel: amprenavir, lansoprazole, nevirapine, oxcarbazepine, tacrolimus, topiramate, tretinoin, barbiturates (including primidone), phenytoin and carbamazepine, preparations containing St. , rifabutin, griseofulvin. Levonorgestrel reduces the effectiveness of hypoglycemic drugs and anticoagulants (coumarin derivatives, phenindione), increases plasma concentrations of HA. Preparations containing levonorgestrel may increase the risk of cyclosporine toxicity due to suppression of its metabolism.

Dosage and administration

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 method of emergency contraception more than once every 4-6 months.

Intrauterine, the 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 oral lekform as a means of regular and continuous contraception, because. this leads to a decrease in the effectiveness of the drug and an increase in adverse reactions. If menstruation is delayed by more than 5-7 days after emergency postcoital contraception, pregnancy should 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 an examination of the pelvic organs and mammary glands, as well as an examination of a smear from the cervix. A woman should be re-examined 4-12 weeks after the insertion of the IUD, and then once a year or more often, if clinically indicated. The IUD remains effective for five years. Only a physician experienced with this IUD or well trained in the procedure should install.

The results of some recent studies show that women taking progestogen-only contraceptives may have an increased risk of venous thrombosis; however, these results are not definitive. However, when symptoms of venous thrombosis appear, appropriate diagnostic and therapeutic measures should be taken immediately.

After removal of the IUD, the ability to bear children is restored in 50% of women after 6 months, in 96.4% - after 12 months.

Year of last adjustment

2011

Interactions with other active substances

Acarbose*
Glipizide*	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 (a dose increase may be required).
Carbamazepine*	Carbamazepine induces the activity of the CYP450 system in the liver, reduces plasma levels and reduces the reliability of the contraceptive effect of levonorgestrel.
Levothyroxine sodium*	Against the background of levonorgestrel, the level of thyroxin-binding globulin in plasma increases (a dose increase 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.

Levonorgestrel (the second name is "Ethinylestradiol") is widely used in modern gynecology in order to prevent unwanted pregnancy. The substance can also be used for other purposes, depending on the recommendations of the attending physician.

Levonorgestrel works by preventing ovulation, by changing the cervical mucus, and the lining of the uterus.

Modern pharmacology has more than 20 drugs with Ethinylestradiol. Let's consider some of them.

Classical oral contraceptives with levonorgestrel, such as Gravistat, Rigividon, Triquilar, Anteovin, help not only protect a woman from unwanted pregnancy, these drugs also regulate the menstrual cycle, alleviate premenstrual syndrome. Protection occurs due to an increase in the viscosity of cervical mucus and inhibition of the pituitary secretion of gonadotropic hormones. The release form of these drugs is tablets or dragees. The form of reception - orally.

Contraceptives with levonorgestrel have not only the form of the usual tablets or dragees. So Mirena and Levonov's preparations are an intrauterine therapeutic system or, more simply, an intrauterine device. The substance acts directly inside the woman's body, causing temporary atrophy of the endometrium and thereby preventing the fertilization of the egg. The spirals are designed for up to five years.

Another type of contraception is Norplant implantable subcutaneous capsules. Six capsules are surgically placed under the skin in the shoulder area, and their effect is up to five years.

In addition, levonorgestrel is also used in drugs that are designed to prevent ovulation and as a result of unwanted pregnancy after unprotected intercourse. The group of emergency postcoital contraception for women who have a regular menstrual cycle includes Escapel and Postinor. Their reception should take place no later than 48 hours after intercourse. No more than 4 doses per month are recommended, otherwise overdose symptoms described in the instructions may occur.

In addition to preventing pregnancy, levonorgestrel is used to improve the well-being of women during menopause. So the drug Klimonorm is used as a replacement therapy in case of insufficient amount of female sex hormones in the body, as well as in the postmenopausal period.

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