Implanon NKST 68 mg (etonohestrel)

Release form

Single-rod contraceptive implant placed in the needle of a sterile disposable applicator

Packaging

1 implant

Pharmacological action

The preparation Implanon NKST® is a radiopaque, disposable, sterile disposable applicator containing etonogestrel implant for s / c use that is not subject to biological degradation. Etonogestrel is a biologically active metabolite of desogestrel - a progestogen, which is widely used as an oral contraceptive hormonal agent (OC). Structurally, it is a derivative of 19-nortestosterone and in target organs with high affinity binds to progesterone receptors. The contraceptive effect of etonogestrel is mainly achieved by suppressing ovulation. Ovulation was not observed during the first 2 years of use, and only rarely did they occur during the 3rd year. In addition to suppressing ovulation, etonogestrel also causes an increase in the viscosity of the secretion of the cervix, which prevents the passage of sperm. Clinical studies have been conducted in women aged 18–40 years. Despite the lack of direct comparison, the contraceptive effect of the implant is at least comparable to the contraceptive effect of combined OK (more than 99%). A high degree of protection against pregnancy is achieved, among other reasons, by the fact that the contraceptive effect of the drug Implanon NKST® does not depend on the strict adherence of a woman to a daily, weekly or monthly regimen. The contraceptive effect of etonogestrel is reversible, which is reflected in the rapid restoration of the normal ovulatory menstrual cycle after removal of the implant. Although etonogestrel suppresses ovulation, ovarian activity is not completely suppressed. Average plasma concentrations of estradiol remain above the values ​​observed in the early phase of follicle formation. Etonogestrel does not affect changes in bone mineral density and lipid metabolism. The use of contraceptive hormones containing progestogens may have an effect on insulin resistance and glucose tolerance. It was shown that in patients using the drug Implanon NKST®, dysmenorrhea is less common.

Pharmacokinetics

Absorption. After implantation, etonogestrel is rapidly absorbed into the circulating blood. Concentrations that suppress ovulation are achieved after 1 day. Cmax in plasma (from 472 to 1270 pg / ml) is reached after 1–13 days. The rate of release of etonogestrel from the implant decreases over time, as a result of which its plasma concentration rapidly decreases during the first few months after administration. By the end of the 1st year of use, the average concentration is approximately 200 pg / ml (150–261 pg / ml) and slowly decreases to 156 pg / ml (111–202 pg / ml) by the end of the 3rd year. The observed variations in plasma concentrations may be partially associated with differences in body weight.

distribution. Etonogestrel binds to plasma proteins by 95.5–99%, mainly with albumin and to a lesser extent with sex hormone binding globulin. Vd in the central chamber and total Vd are 27 and 220 L, respectively, and it is unlikely that these indicators change while the Implanon NKST® preparation is in the body of a woman.

Metabolism. Etonogestrel undergoes hydroxylation and reduction. Metabolites are sulfates and glucuronides.

Withdrawal. With iv administration of etonogestrel, the average T1 / 2 is approximately 25 hours, and plasma clearance is approximately 7.5 l / h. The clearance and T1 / 2 remain constant during the use of the drug. Etonogestrel and its metabolites, both in the form of free steroids and in the form of conjugates, are excreted by the kidneys and through the intestines (ratio - 1.5: 1). After administration to women during breastfeeding, etonogestrel is excreted in breast milk in a milk / plasma ratio of 0.44–0.5 during the first 4 months. The average dose of etonogestrel received by a baby with breast milk is approximately 0.2% of the maternal daily dose of etonogestrel (about 2.2% when calculated per 1 kg of the baby’s body weight). It has been shown that concentrations gradually and statistically significantly decrease with time.

Indications

Contraception

Contraindications

Contraceptive hormones containing only a progestogen should not be used in the presence of any of the conditions / diseases listed below. If any of these conditions occurs during the period of use of the drug Implanon NKSTВ®, discontinue use of the drug immediately.

hypersensitivity to the active substance or any auxiliary substance of the drug Implanon NKSTВ®

thrombosis (arterial and venous) and thromboembolism at present or in the anamnesis (including thrombosis, deep vein thrombophlebitis, pulmonary artery thromboembolism, and infarction hemorrhagic cerebrovascular disorders)

the presence of antibodies to phospholipids

migraine with focal neurological symptoms

breast cancer, incl. a history of

identified or suspected malignant hormone-dependent tumors of

are benign or malignant liver tumors currently or in a history of

are severe forms of liver disease (before normalization of functional liver samples), including jaundice, congenital hyperbilirubinemia (including history)

uncontrolled arterial hypertension

vaginal bleeding of unknown etiology

pregnancy (including presumed)

childhood.

With caution (in the presence of any of the conditions or risk factors listed below, you should weigh the benefits of using an implant regarding the possible risks for each individual woman and discuss them with her before she decides to start using Implanon NKSTВ®. In case of deterioration , amplification, or at the first occurrence of any of these conditions, a woman should consult a doctor, after which the doctor must decide whether to continue using or discontinuing the drug Implanon NKSTВ®): prolonged immobilization caused by chir rgicheskim intervention or other causes state prior thrombosis (including transient ischemic attack, angina pectoris, complicated valvular heart disease, atrial fibrillation, extensive trauma) persistent arterial hypertension, diabetes mellitus, including diabetes mellitus with diabetic angiopathy is a hereditary or acquired predisposition to arterial thrombosis, including lack of protein C, protein S, antithrombin III liver disease of mild to moderate severity with normal liver function tests, anticoagulant therapy, severe depression.

Use during pregnancy and lactation

Use of the drug Implanon NKST® is not indicated during pregnancy. In case of pregnancy during the use of the drug Implanon NKST®, the implant should be removed. In preclinical studies, it was found that very high doses of progestogen compounds can cause masculinization of the female fetus. Information on the effect of the drug Implanon NKST® on the body of a pregnant woman and the fetus is insufficient.

The drug Implanon NKST® does not affect the formation or quality of breast milk (protein, lactose or fat concentrations). However it is known that a small amount of etonogestrel is excreted in milk. Based on the average daily milk intake of 150 ml / kg, the average daily dose of ethonogestrel for a child, calculated after one month of ethonogestrel release, is approximately 27 ng / kg / day. This corresponds to approximately 0.2% of the estimated absolute maternal daily dose (about 2.2% when converted to 1 kg of the child’s body weight). During the period of breastfeeding, the concentration of etonogestrel in milk gradually decreases.

Based on the available data, the use of the drug Implanon NKST® during breastfeeding is possible, but only under the supervision of a doctor over the development and growth of the baby. The drug Implanon NKST® should be administered 4 weeks after birth.

Special instructions

Typically, the risk of developing breast cancer increases with age. During the application of OK (including combined), the risk of developing breast cancer increases slightly. This increased risk gradually decreases within 10 years after the termination of the use of OK, and it is not associated with the duration of the use of OK, but is associated with the age of the woman during the use of OK. The ratio of the expected number of diagnosed cases of breast cancer in 10,000 women who used combined OK (including within 10 years after stopping their use) and women who never used them, for the same period calculated for the corresponding age groups , amounted to: 4.5 / 4 (16–19 years), 17.5 / 16 (20–24 years), 48.7 / 44 (25–29 years), 110/100 (30–34 years), 180 / 160 (35–39 years) and 260/230 (40–44 years). The risk in women using contraceptive methods containing only progestogens is probably similar to the risk when using combined OK. However, the data regarding these methods are not so specific. Compared to the lifetime risk of breast cancer, the increase in the risk associated with OK is small. Cases of the development of breast cancer diagnosed in women, those who use OK tend to be less clinically pronounced than cases of cancer diagnosed in women who have never used OK. The increased risk observed in women using OK is probably due to earlier diagnosis, the biological effects of OK, or a combination of these 2 factors.

In case of acute or exacerbation of chronic liver diseases, a woman should consult a specialist for examination and consultation.

In the course of epidemiological studies, it was found that there is a connection between the use of combined OK and an increase in the incidence of VTE (deep vein thrombosis and pulmonary embolism). Although the clinical relevance of these results is for etonogestrel (a biologically active metabolite of desogestrel), used as a contraceptive hormone, in the absence of an estrogen component is unknown, in case of thrombosis, the implant should be removed.

Consideration should also be given to removing the implant in the event of prolonged immobilization due to surgery or illness. Although Implanon NKSTВ® is a contraceptive hormone containing only progestogen, it is recommended to evaluate risk factors that are known to increase the risk of venous or arterial thromboembolism. Women with a history of thromboembolic disease should be warned about the possibility of a relapse.

In the post-registration period of the use of a non-radiopaque implant containing etonogestrel, severe arterial and venous thromboembolic complications were reported, including about pulmonary embolism (including with a fatal outcome), deep vein thrombosis, myocardial infarction, stroke. Implanon NKSTВ® should be removed in case of thrombosis.

If persistent hypertension develops during the period of use of the Implanon NKSTВ® preparation or significantly increased blood pressure does not decrease adequately in response to the antihypertensive therapy, the Implanon NKSTВ® implant should be removed.

Although progestogens can affect the peripheral tissue resistance to insulin and glucose tolerance, there is no evidence that there is a need to change the treatment regimen in patients with diabetes using contraceptive hormones containing progestogen only. Nonetheless, women with diabetes should be closely monitored during the entire period of use of contraceptive hormones containing only progestogen.

It is necessary to conduct periodic examinations of women who are undergoing therapy for hyperlipidemia. Some progestogens can increase LDL levels and impair hyperlipidemia control.

Chloasma can sometimes occur, especially in women with a history of pregnant chloasma. Women with a predisposition to chloasma should avoid exposure to sunlight or UV radiation while using Implanon NKSTВ®.

The contraceptive effect of the drug Implanon NKSTВ® is associated with the concentration of etonogestrel in blood plasma, which is inversely proportional to body weight and decreases over time after administration of the drug. Clinical experience in women with overweight in the third year of use of the drug is limited. It cannot be ruled out that the contraceptive effect in such women during the third year of using the drug may be lower than in women with normal body weight, so the doctor may need to consider an earlier implant replacement in women with overweight.

As a result of local inflammation or if the implant is not inserted in accordance with the instructions in the section “Dosage and administration”, in the section How to administer Implanon NKST®, the implant may be expelled.

In rare cases, mainly related to either too deep administration (see also the section “Dosage and administration”, subsection How to administer Implanon NKST®), and / or as a result of external forces (for example, manipulation with the implant or contact sports), the implant can migrate from the site of insertion. In such cases, determining the location of the implant may be difficult and removal may require a larger incision and time (see also the section “Method of application and dose”, subsection How to remove Implanon NKST®). If the implant is not removed, then contraception and the risk of undesirable effects associated with the progestogen may persist beyond the time desired by the woman.

When using all low-dose contraceptive hormonal agents, follicle growth can occur, and sometimes the follicle can reach a larger size than in the normal cycle. Typically, these follicles disappear spontaneously and are often asymptomatic in some cases, there is a slight pain in the lower abdomen. In rare cases, surgical intervention is necessary.

Prevention of ectopic pregnancy with traditional progestogen-containing contraceptive hormonal agents is not as effective as with combined OK, which is associated with the frequent occurrence of ovulation during the application of these methods. This statement does not apply to the use of progestin-based oral contraceptives with desogestrel and an implant with desogestrel. Despite the fact that the drug Implanon NKSTВ® suppresses ovulation, in the case of a woman with amenorrhea or abdominal pain, an ectopic pregnancy should be considered in the differential diagnosis.

There are reports of the following conditions that have occurred both during pregnancy and when using sex steroid hormones, but a connection with the use of progestogens has not been established: jaundice and / or itching, cholestasis-associated gallstones porphyria systemic lupus erythematosus hemolytic uremic chorea Sydenham herpes during pregnancy hearing loss associated with otosclerosis and (hereditary) angioedema.

The safety and efficacy of Implanon NKSTВ® have been evaluated for women of reproductive age. It is expected that efficacy and safety in adolescents in the post-puberty period will be similar. However, no clinical studies have been conducted in women under the age of 18 years. The use of this drug is not indicated until the onset of menarche (first menstruation).

Medical examinations / consultations

Before starting use or before replacing the drug Implanon NKST®, the woman’s medical history (including family history) should be carefully reviewed and pregnancy should be excluded. You should measure blood pressure, conduct a physical examination and be guided by contraindications (see "Contraindications") and warnings (see "Contraindications" section, with caution).

It is recommended that a woman 3 months after the administration of the drug Implanon NKSTВ® visit a doctor for a medical examination. During a medical examination, blood pressure should be measured and the patient ascertained if she had any undesirable effects, if there are any questions and complaints. The frequency and nature of further periodic medical examinations should be set individually for each woman (at least 1 time in 6 months).

A woman should be informed that the drug Implanon NKSTВ® does not protect against HIV infection (AIDS) and other sexually transmitted diseases.

Decreased effectiveness of

The effectiveness of the drug Implanon NKSTВ® can be reduced when using the drug in combination with other drugs (see "Interaction").

Changes in the nature of spotting

During the use of the drug Implanon NKSTВ® in women, a change in the nature of menstrual bleeding is likely. These may include changes in frequency (absence, less or more frequent), intensity (decrease or increase), or duration of bleeding. Amenorrhea was observed in 20% of women, while the other 20% had more frequent and / or prolonged bleeding. Dysmenorrhea tends to improve during the use of the drug Implanon NKSTВ®. The nature of the bleeding that occurs during the first 3 months allows us to predict the future nature of bleeding in most women. Informing, additional explanations and maintaining an individual diary will help a woman adequately perceive the bleeding that occurs. Evaluation of vaginal bleeding should be carried out individually. It may include examination to exclude gynecological pathology or pregnancy.

Laboratory parameters

Data obtained with combined OKs showed that the use of contraceptive hormones may affect some laboratory parameters, including biochemical parameters of liver, thyroid, adrenal and kidney function, plasma concentration of (transport) proteins, for example, corticosteroid-binding globulin and lipid / lipoprotein fractions, indicators of carbohydrate metabolism, blood coagulation and fibrinolysis. Typically, these changes remain within normal values. It is not known to what extent this applies to contraceptive hormones containing only a progestogen.

Influence on the ability to drive vehicles and work with mechanisms. Reactions when driving vehicles and using sophisticated equipment have not been studied. Implanon NKSTВ® may cause dizziness. Patients should be warned that if you experience dizziness, you should not drive or use sophisticated equipment.

Dosage and administration of

Pregnancy must be excluded before administration of Implanon NKST®. A gynecologist is strongly recommended to take part in a training session to become familiar with the use of the applicator of the Implanon NKST® preparation and the methods for introducing and removing the Implanon NKST® implant. Before the implant is inserted, you must carefully read the instructions for use and follow the instructions for the introduction and removal of the implant, presented in the sections How to enter Implanon NKST® and How to remove Implanon NKST®.

How to use Implanon NKST®

The drug Implanon NKST® is a long-acting hormonal contraceptive. SC implanted one implant, which can remain at the injection site for 3 years. The implant is removed no later than 3 years from the date of administration. A woman needs to be informed about the possibility of removing the implant at any time, at her request. A gynecologist may consider the possibility of earlier implant removal in overweight women. After removal of the implant, the immediate administration of another implant will lead to continued contraceptive protection. If a woman does not want to continue using Implanon NKST®, but she needs contraception, another method of contraception should be recommended.

The basis for the successful use and subsequent removal of the implant Implanon NKST® is the correct and carefully performed sc implant insertion in accordance with this instruction. Violation of the time and technique of implantation (see the subsections When to Implant Implant NKST®, How to administer Implanon NKST®) can lead to pregnancy.

Implant Implanon NKST® should be administered subcutaneously, directly beneath the skin on the inside of the shoulder, to prevent injury to large blood vessels and nerves that are located deeper in the connective tissue between the biceps and triceps.

Immediately after the implant is inserted, it is necessary to palpate its presence under the skin .. If the implant cannot be felt or its presence is in doubt, other diagnostic methods must be used to confirm its presence (see the section How to enter Implanon NKST®). Until the implant is confirmed, a woman should recommend the use of a non-hormonal (barrier) method of contraception.

The packaging of the Implanon NKST® preparation contains a User Card designed to record the implant's batch number. The gynecologist needs to write down the date of insertion, indicate the hand into which the implant was inserted, and the planned date of its removal in the User Card. The package of the preparation contains stickers for the records of the gynecologist, which indicate the series number of the implant.

When to administer Implanon NKST®

Important. Before the implant is introduced, pregnancy must be excluded.

The timing of administration depends on a woman's recent use of contraceptive hormones as follows.

If contraceptive hormones are not used in the previous month, the implant should be inserted between the 1st day (1st day of the menstrual bleeding) and the 5th day of the menstrual cycle, even if the menstrual bleeding is still ongoing.

If the implant is inserted correctly, an additional method of contraception is not required. If you deviate from the recommended implantation period, you should warn the woman about the need to use the barrier method of contraception for the next 7 days. If during this period there were sexual contacts, pregnancy should be excluded.

Switching from the hormonal method of contraception to Implanon NKST®

When switching from the combined method of hormonal contraception (combined oral contraceptive (COC), combined hormonal vaginal ring or combined hormonal transdermal patch). The implant should be administered preferably on the day following the day of the last active tablet (last tablet containing active ingredients) of the COC, but no later than the day following the usual interval in taking the tablets or the period during which the placebo tablets of the COC are taken. If previously used a vaginal ring or transdermal patch, the implant should be introduced preferably on the day of removal, but no later than the day of the next use of the previous drug.

If the implant is inserted correctly, an additional method of contraception is not required. If you deviate from the recommended implantation period, you should warn the woman about the need to use the barrier method of contraception for 7 days. If during this period there were sexual contacts, pregnancy should be excluded.

When switching from a progestogen contraceptive method (for example, tablets containing only progestogen, injections, an implant or hormonal intrauterine system (IUD). Since there are several types of progestogen methods, the implant should be administered as follows:

- injectable hormonal contraceptives: insert the implant into the day when you need to do the next

injection - tablets containing only progestogen: a woman can switch from tablets, containing only progestogen on Implanon NKST® any day. The implant must be inserted within 24 hours after the last

tablet - implant / IUD: the implant is inserted on the day the previous implant is removed or BMS.

If the implant is inserted correctly, an additional method of contraception is not required. If you deviate from the recommended implantation period, you should warn the woman about the need to use the barrier method of contraception for 7 days. If during this period there were sexual contacts, pregnancy should be excluded.

After an abortion or miscarriage

- I trimester: the implant must be inserted within 5 days after an abortion or miscarriage in the first trimester

- II trimester: the implant must be inserted between the 21st and 28th days after an abortion or miscarriage in the II trimester .

If the implant is inserted correctly, an additional method of contraception is not required. If you deviate from the recommended implantation period, you should warn the woman about the need to use the barrier method of contraception for 7 days. If during this period there were sexual contacts, pregnancy should be excluded.

After childbirth

- During breastfeeding: the implant should be inserted at the end of the 4th week after childbirth (see "Use during pregnancy and lactation"). A woman should use the barrier method of contraception within 7 days after implantation. If during this period there were sexual contacts, pregnancy should be excluded.

- In the absence of breastfeeding: the implant should be inserted between the 21st and 28th days after birth. With the correct introduction of the implant, an additional method of contraception is not required. If you deviate from the recommended implantation period, you should warn the woman about the need to use the barrier method of contraception for 7 days. If during this period there were sexual contacts, pregnancy should be excluded.

How to administer Implanon NKST®

The basis for the successful use and subsequent removal of the drug Implanon NKST® is the correct and carefully performed sc administration of the implant in the non-dominant hand, in accordance with the instructions. A gynecologist and a woman should palpation determine the presence of an implant after its introduction. The implant should be inserted directly under the skin. Too deep or improper implantation can be complicated by paresthesia (due to nerve damage), implant migration (due to IM or fascial injection) and, in rare cases, intravascular administration. In addition, when the implant is inserted too deeply, it may not palpate, and its location and / or removal may be difficult.

The introduction of the drug Implanon NKST® should be performed under aseptic conditions and only by a qualified gynecologist who is well acquainted with the method of administration. Insertion of the implant should only be performed using a special applicator.

It is recommended that the gynecologist be in a sitting position throughout the administration procedure so that he can clearly see the injection site and the movement of the needle under the skin.

Side effects of

Infectious and parasitic diseases: vaginal infection (vulvovaginitis) - pharyngitis, rhinitis urinary tract infection (urethritis, cystitis)

From the immune system: hypersensitivity to any component of

: metabolism and srd From the psyche: emotional lability, depression, nervousness, decreased libido, anxiety, insomnia

From the nervous system: headache, dizziness, migraine, drowsiness

From Ships:

tides From the digestive tract: abdominal pain, nausea, bloating, vomiting, constipation, diarrhea

Skin and subcutaneous tissue disorders: acne, alopecia, hypertrichosis, rash, itching

From the musculoskeletal and connective tissue: back pain, arthralgia, myalgia, musculoskeletal pain

from the kidneys and urinary tract: dysuria

From the genital and mammary glands: soreness in the mammary glands, chest pain, irregular menstruation, dysmenorrhea, ovarian cyst, vaginal discharge, discomfort in the vulva and vagina, galactorrhea, enlarged mammary glands, itching in the vulva and vagina

General disorders and disorders at the injection site: pain at the implant location a, reaction at the implant location, fatigue, flu-like state, pain, hyperthermia,

edema Laboratory and instrumental data: weight gain, weight loss

Drug interaction

Effect of other drugs on Implanon NKST®

The interaction between contraceptive hormones and other drugs can lead to menstrual bleeding and / or to reduce the contraceptive effect. Special studies, devoted to the study of interaction with the drug Implanon NKST®, has not been conducted. The following interactions have been reported in the literature (mainly SKOC, but sometimes also reported with respect to hormonal contraceptives containing only progestogen).

Hepatic metabolism: interaction is possible with drugs - inducers of microsomal liver enzymes, primarily isoenzymes of cytochrome P450 (e.g. phenytoin, phenobarbital, primidone, bosentan, carbamazepine, rifampicin and, possibly, oxcarbazepine, topiramate gum, rastiramate gum, rastiramate Hypericum perforatum-containing HIV protease inhibitors (e.g. ritonavir, nelfinavir) non-nucleoside reverse transcriptase inhibitors (e.g. nevirapine, e avirenz) and the latter combination, which can lead to increased clearance of sex hormones.

Women receiving treatment with one of the above drugs should additionally use the barrier method of contraception during their use and within 28 days after stopping their use.

Women receiving long-term treatment with drugs that induce microsomal liver enzymes are advised to remove the implant and prescribe a non-hormonal (barrier) method of contraception.

Increased plasma hormone concentrations associated with co-administration of drugs. Medications (such as ketoconazole) that inhibit microsomal liver enzymes (such as CYP3A4) can increase plasma hormone concentrations.

Impact of Implanon NKST® on other drugs

Contraceptive hormones may affect the metabolism of other drugs. Accordingly, plasma and tissue concentrations of drugs may increase (e.g. cyclosporine) or decrease (e.g. lamotrigine).

Note: to identify possible interactions, you should read the instructions for the use of simultaneously taken drugs.

Overdose

The implant should always be removed before inserting a new one. There are no data on an overdose of ethoestrel. There are no reports of serious side effects from the overdose of contraceptive hormones.

Storage Conditions

In a dry, dark place at 2–30 ° C.

Shelf life

5 years

Deystvuyushtee substance

Эtonogestrel

Terms and conditions

prescription

Formulation

implant

Possible product names

Implanon NKST implant 68 mg

N.V. Organon, the Netherlands



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