Exluton - description of the drug, instructions for use, reviews

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Manufacturers: Organon Inc.

Active ingredients

• Linestrenol

Disease class

• Not indicated. See instructions

Clinical and pharmacological group

• Not indicated. See instructions

Pharmacological action

• Contraceptive
• Progestogenic

Pharmacological group

• Estrogens, gestagens; their homologues and antagonists

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

An oral contraceptive (OC) containing LIN (the progestogenic component linestrenol). Entering the body, LIN is transformed into the metabolite NET ( norethisterone ), which tends to bind to progesterone in certain organs, including the myometrium .

The contraceptive effect of Exluton is carried out mainly due to an increase in the viscosity of the mucus of the cervical canal, thereby disrupting the advancement of sperm, peristalsis of the fallopian tubes, and also reducing the sensitivity of the endometrium to oocytes . As a result, almost 70% of women do not ovulate, and as confirmation there is an increase in progesterone levels and the absence of a growth peak in the middle of the luteinizing hormone (LH) cycle. Taking the drug does not have a clinically significant effect on metabolic processes and hemostasis.

Pharmacokinetics

Linestrinol, which is the main active ingredient of the drug, is quickly absorbed into the gastrointestinal tract and is transformed into the metabolite norethisterone. Bioavailability - 64%. After taking the drug, maximum levels of Linestrinol in the blood are reached within 2-4 hours. NET is highly bound to blood proteins (about 96%), mainly to albumin (61%) and less so to globulin (35%). Metabolites of the drug are excreted mainly in the form of sulfates and glucuronides through the kidneys and intestines. The half-life is about 15 hours.

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Exluton, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Exluton is provided for informational purposes and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!

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Contraindications

• Hypersensitivity to the drug;
• Established pregnancy or suspected pregnancy;
• A history of ectopic pregnancy ;
• Venous thromboembolism;
• Hormone-dependent malignant tumors;
• A history or current severe liver disease
• Bleeding from the vagina of unknown etiology;
• Jaundice;
• Porphyria;
• Otosclerosis;
• of herpes during pregnancy;
• Diabetes mellitus (type 1);
• Cholesterol metabolism disorders;
• Congenital conditions of hyperbilirubinemia ;
• Cholelithiasis;
• Lactase deficiency and galactose intolerance;

Exluton, instructions for use (Method and dosage)

Exluton tablets are taken orally daily for 28 days, one tablet with water. It is advisable to take the drug at the same time.

Taking Exluton, in cases where hormonal contraceptives have not been used during the last month, should be started at the beginning of the menstrual cycle (from the first day). If the first day of the cycle is missed, then the pills can be taken from days 2-5, but in this case it is necessary to use an additional barrier method of contraception during the first weeks of the cycle.

If contraception was previously carried out using a combined hormonal contraceptive, then taking the drug should be started the next day after the end of taking the active COC tablet. Additional contraception methods are not used in this case.

When switching from taking other progestogen-based drugs ( mini-pills , implants, IUDs), Exluton can be taken any day immediately after removal of the implant, on the day of the new injection. At the same time, additional methods of protection are not used.

If you have an abortion at the beginning of pregnancy (1st trimester), you should start taking the drug immediately. There is no need for an additional method of contraception.

After an abortion in a later period (2nd trimester) or childbirth, the drug should be taken on days 21-28 after the abortion or childbirth. If this period is missed, you should use an additional barrier method of contraception during the first week of taking the drug. But, if you have sexual intercourse after an abortion or childbirth, it is necessary to exclude pregnancy before starting to take Exluton. It's better to wait until your period starts.

If you miss taking the pills (less than 3 hours), the missed dose of the drug should be taken as soon as possible, and the next dose at the usual time. If the missed time is more than 3 hours, you should use the barrier method for the next 7 days. If a dose of the drug is missed during the first week of use, and there was sexual intercourse during the week before skipping the tablets, the possibility of pregnancy must be taken into account. In case of disorders of the gastrointestinal tract, the process of absorption of tablets in the gastrointestinal tract may be disrupted and it is necessary to use additional methods of contraception.

Oral tablets Exluton

Instructions for medical use of the drug

Description of pharmacological action

The drug Exluton is an oral contraceptive (OC) that does not contain estrogens and contains only the progestogenic component linestrenol (LIN). When entering the body, LIN is converted into the biologically active metabolite norethisterone (NET), which binds to progesterone receptors in target organs, incl. myometrium. The contraceptive effect of Exluton is achieved mainly by increasing the viscosity of cervical mucus (thus preventing the advancement of sperm), reducing the sensitivity of the endometrium to oocytes (thus disrupting the nidation of the fertilized egg), and disrupting the peristalsis of the fallopian tubes. Moreover, almost 70% of women do not ovulate, as evidenced by the absence of a mid-cycle peak in luteinizing hormone (LH) and an increase in progesterone levels. However, no clinically significant effect on the metabolism of carbohydrates, lipids and hemostasis was detected.

Indications for use

- contraception.

Release form

tablets 0.5 mg; blister 28, box (box) 1; tablets 0.5 mg; blister 28, box (box) 3; Composition Tablets 1 table. linestrenol 0.5 mg excipients: potato starch; amylopectin; lactose monohydrate; magnesium stearate in a blister of 28 pcs.; There are 1 or 3 blisters in a box.

Pharmacodynamics

The drug Exluton is an oral contraceptive (OC) that does not contain estrogens and contains only the progestogenic component linestrenol (LIN). When entering the body, LIN is converted into the biologically active metabolite norethisterone (NET), which binds to progesterone receptors in target organs, incl. myometrium. The contraceptive effect of Exluton is achieved mainly by increasing the viscosity of cervical mucus (thus preventing the advancement of sperm), reducing the sensitivity of the endometrium to oocytes (thus disrupting the nidation of the fertilized egg), and disrupting the peristalsis of the fallopian tubes. Moreover, almost 70% of women do not ovulate, as evidenced by the absence of a mid-cycle peak in luteinizing hormone (LH) and an increase in progesterone levels. However, no clinically significant effect on the metabolism of carbohydrates, lipids and hemostasis was detected.

Pharmacokinetics

Absorption After oral administration of the drug Exluton, linestrinol, which is a prodrug, is rapidly absorbed and converted into the pharmacologically active metabolite norethisterone (NET). Maximum levels of NET in blood plasma are reached 2-4 hours after taking the tablet orally, its absolute bioavailability is 64%. The distribution of NETs is 96% associated with plasma bulks, predominantly with albumin (61%) and to a lesser extent with sex hormone binding globulin (35%). Metabolism Phase I of LIN metabolism includes 3-hydroxylation and subsequent dehydrogenation. The active metabolite NET is further reduced; decomposition products are in the form of conjugates with sulfates and glucuronides. Elimination The average T1/2 NET is about 15 hours. The rate of elimination from plasma is approximately 0.6 l/hour. LIN and its metabolites are excreted by the kidneys (mainly in the form of glucuronides and sulfates and, to a lesser extent, in the form of unchanged LIN) and through the intestines in a ratio of 1.5:1.

Use during pregnancy

The drug Exluton is not prescribed during pregnancy. If pregnancy occurs, use of Exluton should be discontinued immediately. Epidemiological studies have shown that there is neither an increased risk of birth defects in children born to women who used OCs before pregnancy, nor an increased risk of teratogenicity when OCs were inadvertently taken during early pregnancy. There are no data regarding the use of progestogen-only OCs during pregnancy. Similar to other contraceptives containing only progestogen, Exluton does not affect the quantity and quality of breast milk, but it is known that a small amount of progestogen is excreted in milk. The amount of linesterol and metabolites that are excreted in milk is about 0.15% of the daily dose, and no adverse effects on the growth and development of newborns have been reported.

Other special occasions at reception

Contraindication: current or history of severe liver disease.

Contraindications for use

Prostagene-only contraceptives should not be used if any of the conditions listed below are present. If any of these conditions occur during use of Exluton, you should immediately stop taking the drug. - hypersensitivity to the active substance or to any other component of Exluton; - established or suspected pregnancy; - current venous thromboembolism; - current or history of severe liver disease - until liver function indicators normalize; - cholestatic jaundice; - porphyria (diagnosed or in history); - otosclerosis (diagnosed or in history); - history of pregnancy herpes; - progestogen-dependent tumors; - bleeding from the vagina of unknown etiology. With caution: if any of the conditions/diseases listed below are present, the benefits of using a progestogen should be weighed against the possible risks for each individual woman. This should be discussed with the woman before she starts taking Exluton. In cases of deterioration, exacerbation of the disease, or the occurrence of any of these conditions for the first time, a woman should consult a doctor to decide on the possibility of further use of Exluton. Breast cancer risk. Increases with age. The risk of breast cancer is modestly increased during oral contraceptive (OC) use, possibly due to earlier diagnosis, drug exposure, or a combination of the two. However, this increased risk gradually disappears within 10 years after discontinuation of OC use and is not associated with duration of use and depends on the woman's age at the time of OC use. Cases of breast cancer diagnosed in women using oral contraceptives are clinically less severe than those diagnosed in women who have never used OCs. An individual assessment of the benefit-risk ratio of contraceptive use in the presence of breast cancer should be carried out. Since it is impossible to exclude a negative effect of progestogens on the development of liver cancer, an individual assessment of the benefit-risk ratio should be carried out. Epidemiological studies have established an association between the use of combined oral contraceptives (COCs) and an increased incidence of venous thromboembolism (deep vein thrombosis and pulmonary embolism). Although this has not been clinically confirmed for contraceptives that do not contain an estrogen component, Exluton should be discontinued if thrombosis develops. It should also be considered to discontinue the drug Exluton in case of possible surgery or other disease requiring long-term immobilization. Women with a history of thromboembolic disorders should be warned about the possibility of recurrence. Although progestogens may affect peripheral insulin resistance and glucose tolerance, there is no evidence that there is a need to change hypoglycemic therapy in diabetic patients using progestogen-containing OCs. However, women with diabetes mellitus should be closely monitored during the entire period of use of progestogen-containing OCs.

Side effects

Side effects of Exluton include irregular menstruation, breast tenderness, mood swings, nausea and headache, which occur in almost half of women in the first cycle of using Exluton and decrease to approximately 30% by the 12th cycle. Among women breastfeeding, up to 28% experience side effects, with a decrease to 5% by the 12th cycle. Other side effects that have been reported with Exluton or with hormonal contraceptives in general are listed below. Mammary glands: hypersensitivity, soreness, enlargement, galactorrhea From the central nervous system: headache, migraine, changes in libido, depression, mood swings. From the gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea or constipation. From the skin: various skin disorders (rash, erythema nodosum, erythema multiforme) From the genitourinary system: irregular bleeding, changes in vaginal secretion. On the part of the visual organs: intolerance to contact lenses. Other: fluid retention, changes in body weight, hypersensitivity reactions. Chloasma can sometimes occur, especially in women with a history of chloasma during pregnancy. Women with a predisposition to chloasma should avoid exposure to sunlight or ultraviolet radiation while using Exluton. When using oral (combined) contraceptives, a number of undesirable effects have been observed, including venous and arterial thromboembolic disorders, chloasma and hormone-dependent tumors (for example, liver tumors, breast cancer). The following conditions have been described both during pregnancy and during the use of steroid drugs, but their relationship with the use of progestogens has not been established: jaundice and/or skin itching associated with cholestasis; gallstone formation, porphyria, systemic lupus erythematosus, hemolytic-uremic syndrome, Sydenham's chorea, herpes of pregnancy, hearing loss associated with otosclerosis.

Directions for use and doses

How to take Exluton Tablets should be taken orally in the order indicated on the package, every day at approximately the same time, if necessary, with a small amount of water. Take one tablet daily for 28 consecutive days. Each subsequent package should be started immediately after the completion of the previous package. How to start taking the drug Exluton In the absence of previous use of hormonal contraceptives (within the last month) Taking pills should start on the first day of a woman’s menstrual cycle (on the first day of menstrual bleeding). You can start taking it from day 2-5 of the cycle, but then during the first 7 days of the first cycle of taking pills, it is recommended to additionally use a barrier method of contraception. Switching from COCs A woman should start taking Exluton the next day after taking the last active COC tablet. In this case, there is no need to use an additional method of contraception. When switching from other progestogen-only medications (“mini-pills,” injections, implants, or progestogen-releasing intrauterine systems [IUDs]), a woman using the “mini-pill” can start taking Exluton on any day; using an implant or IUD - on the day of their removal; using injectable forms of contraceptives - on the day when the next injection is due. In all these cases, the woman should be advised to additionally use the barrier method during the first 7 days of taking the pills. After an abortion in the first trimester, a woman can start taking the drug immediately; in this case there is no need for an additional method of contraception. After childbirth or abortion in the second trimester For women who are breastfeeding, see the section “Use during pregnancy and lactation.” A woman should be advised to start taking the drug on days 21-28 after childbirth or abortion in the second trimester. If you start taking the drug later, it should be recommended to use the barrier method during the first 7 days of taking the tablets. However, if you have already had sexual intercourse after childbirth or abortion, you must rule out pregnancy or wait until your first menstruation before starting to take Exluton. What to do if you miss pills Contraceptive protection may be reduced if more than 27 hours pass between taking pills. If the delay in taking the tablet is less than 3 hours, then the missed tablet should be taken as soon as possible, and the next tablet should be taken at the usual time. If the delay in taking the pill is more than 3 hours, then in this case it is necessary to additionally use the barrier method for the next 7 days of taking the pills, according to the above recommendation. If tablets were missed during the very first week of use, and sexual intercourse took place during the week before the missed tablets, the possibility of pregnancy should be considered. Recommendations in case of gastrointestinal disorders In case of gastrointestinal disorders, absorption of the drug may be incomplete and therefore additional contraceptive measures should be resorted to. If vomiting occurs within 3 hours after taking the tablet, then the recommendations regarding missed tablets given above apply in this case. If a woman does not want to change her usual pill regimen, she should take the additional pill(s) needed from a different package.

Overdose

No serious side effects have been reported as a result of overdose. Since the toxicity of LIN is very low, severe toxic symptoms are not expected if several Exluton tablets are taken simultaneously. Symptoms that may occur in this case are the following: nausea, vomiting, slight bleeding from the vagina. There are no antidotes; further treatment should be symptomatic.

Interactions with other drugs

Interactions between OCs and other drugs may result in breakthrough bleeding and/or disruption of contraceptive protection. No special studies have been conducted to study the interactions of Exluton with other drugs. The following interactions have been reported in the literature (mainly with COCs, but sometimes with progestogen-containing contraceptives). Hepatic metabolism: Interactions may occur with drugs that induce liver microsomal enzymes, which lead to increased clearance of sex hormones. Interactions with hydantoins, barbiturates, primidone, carbamazepine and rifamycin have been established; also possible with oxcarbazein, topiramate, rifabutin, felbamate, ritonavir, griseofulvin and preparations containing St. John's wort (Hypericum perforatum). Women using any of these medications should temporarily use a barrier method in addition to Exluton or choose another method of contraception. The barrier method should be used both during the concomitant use of drugs and for 28 days after stopping their use. When using activated carbon, the absorption of LIN may be reduced and, therefore, contraceptive effectiveness may be reduced. If activated carbon is taken within 3 hours after taking a tablet of the drug, absorption may be incomplete. In this case, you must follow the recommendations regarding taking missed pills. OCs may affect the metabolism of other drugs. Accordingly, plasma and tissue concentrations of the drug (eg, cyclosporine) may change. To identify possible interactions, you should read the instructions for use of these medications.

Special instructions for use

Daily dose of lactose in the drug ( Medical examinations/consultations Before prescribing the drug, you should carefully review the woman’s medical history and conduct a gynecological examination to exclude pregnancy. Before prescribing the drug, the cause of menstrual irregularities, for example, oligomenorrhea and amenorrhea, should be determined. The interval between control medical examinations is determined in each individual case. If the prescribed drug may affect a latent or existing disease, an appropriate schedule of follow-up medical examinations should be made. Despite regular use of Exluton, irregular bleeding may sometimes occur. If bleeding is very frequent and irregular, another method should be considered contraception. If the above symptoms are persistent, then in this case it is necessary to exclude organic pathology. Tactics in relation to amenorrhea during use of the drug depend on whether the tablets were taken in accordance with the instructions and in some cases pregnancy tests should be included in the study . If pregnancy occurs, the drug should be discontinued. Women should be informed that Exluton does not protect against HIV infections (AIDS) and other sexually transmitted diseases. Reduced effectiveness The effectiveness of progestogen-containing OCs may be reduced if pills are missed, gastrointestinal disorders, or when taking other medications. Changes in menstrual patterns While using progestogen-containing contraceptives, some women may experience vaginal bleeding more frequently or for a longer period of time, while for other women the bleeding may become less frequent or stop altogether. These changes are often the reason that a woman refuses this method of contraception, or ceases to strictly follow the doctor's instructions. In this case, you should consult a doctor for further clarification about the effect of the drug. It is also possible to undergo an examination to exclude malignant neoplasms or pregnancy. Development of follicles When taking all low-dose hormonal contraceptives, follicle development occurs, and occasionally the size of the follicle can reach larger than normal sizes. Typically, enlarged follicles disappear spontaneously and asymptomatically; in some cases there is mild pain in the lower abdomen; in rare cases, surgical intervention is possible. Laboratory tests Data obtained with COCs have shown that the use of contraceptive steroids may affect the results of some laboratory tests, including biochemical parameters of liver, thyroid, adrenal and kidney function, plasma levels of transport proteins, such as globulin-binding globulin. corticosteroids, lipid/lipoprotein fractions, indicators of carbohydrate metabolism, blood clotting and fibrinolysis. Usually these changes remain within normal limits. It is not known to what extent this applies to progestogen-only contraceptives. Effect on the ability to drive a car and operate machinery Based on the pharmacodynamic profile, it is believed that Exluton does not have or has a negligible effect on the ability to drive a car and operate machinery.

Storage conditions

In a dry place, protected from light, at a temperature of 2–30 °C.

Best before date

60 months

ATX classification:

G Genitourinary system and sex hormones

G03 Sex hormones and modulators of the reproductive system

G03A Systemic hormonal contraceptives

G03AC Progestogens

G03AC02 Linestrenol

Interaction

Exluton, when interacting with other drugs, can cause disruption of contraceptive protection or lead to bleeding. It has been established that when the drug interacts with barbiturates , primidone , hydantoins , rifampicin , griseofulvin , oxcarbazepine , rifabutin , felbamate , topiramate , ritonavir and drugs containing St. John's wort, women need to use a temporary barrier method of contraception in addition to Exluton tablets or switch to another method of contraception . In this case, the barrier method must be used not only during the period of use of these medications, but also for 28 days after the end of their use.

Caution should be exercised when taking activated charcoal preparations, as absorption is reduced and contraceptive effectiveness may be reduced.

Side effects of the drug Exluton

The most common side effects observed in clinical trials of Exluton were irregular bleeding, breast tenderness, mood disturbances, nausea and headache. These symptoms were noted in approximately half of the women who used Exluton during the 1st cycle of administration and their severity decreased to 30% on the 12th cycle of administration. Among women who used Exluton during breastfeeding, 28% reported side effects during the 1st cycle of use, the rate decreased to 5% by the 12th cycle. Other side effects that have been reported with the use of Exluton or hormonal contraceptives in general are listed in the table.

The most serious side effects associated with taking Exluton are listed in the SPECIAL INSTRUCTIONS section.

Analogs

Level 4 ATX code matches:
Eskinor-F

Microlute

Postinor

Escapelle

Implanon NKST

Charosetta

Lactinet

Analogs by ATX code - Orgametril , Linestrenol , Exluton .