Composition, form of production and packaging
Tablets are white, round, flat, with beveled edges, engraved "TT" over "2" on one side and "ORGANON" on the other.
lynestrenol 500 mcg
Auxiliary substances: potato starch, amylopectin, lactose monohydrate, magnesium stearate.
28 pcs. - blisters (1) - packs of cardboard.
28 pcs. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
Eksluton is an oral contraceptive (OC), which does not contain estrogens and contains only the progestogen component of linestrenol (LIN). When ingested, the LIN is converted into a biologically active metabolite, norethisterone (NET), which binds to the receptors of progesterone in the target organs, incl. myometrium.
The contraceptive effect of Exluhuton is achieved, mainly, by increasing the viscosity of cervical mucus (thereby preventing the progress of spermatozoa), reducing the sensitivity of the endometrium to oocytes (thereby violating the nitration of a fertilized egg), disruption of the peristalsis of the fallopian tubes. Moreover, almost 70% of women do not undergo ovulation, which is confirmed by the absence of a peak increase in the luteinizing hormone (LH) in the middle of the cycle and an increase in the level of progesterone. At the same time, there was no clinically significant effect on carbohydrate, lipid and hemostasis metabolism.
After ingestion of the drug Eksluton, linestrinol, being a prodrug, is rapidly absorbed and converted into a pharmacologically active metabolite of norethisterone (NET). The maximum levels of NET in the blood plasma are reached 2-4 hours after taking the tablet inside, its absolute bioavailability is 64%.
NET is 96% associated with plasma beams, mainly with albumin (61%) and to a lesser extent with sex hormone binding globulin (35%).
I phase of LIN metabolism involves 3-hydroxylation and subsequent dehydrogenation. The active metabolite of NET is further restored; The decay products are in the form of conjugates with sulfates and glucuronides.
The average T 1/2 NET is about 15 hours. The rate of excretion from the plasma is approximately 0.6 l / h. LIN and its metabolites are secreted 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 intestine in a ratio of 1.5: 1.
How should I take the drug Elyuton
Tablets should be taken orally in the order given on the package, every day at approximately the same time, if necessary, with a small amount of water. Daily for 28 consecutive days should take one tablet. Each next package should be started immediately after the completion of the previous package.
How should I start taking Eksluton
In the absence of a previous application of hormonal contraceptives (within the last month)
Tablets should be taken on the first day of a woman's menstrual cycle (on the first day of menstrual bleeding). You can start taking and from 2-5 days of the cycle, but then during the first 7 days of the first cycle of taking the tablets it is recommended to additionally apply the barrier method of ontraception.
Transition from COC
The woman will begin to receive the drug Eksluton the next day after taking the last active pills KOC. In this case, there is no need for an additional method of contraception.
When switching from other drugs containing only progestogen ("mini-pili", injections, implants or progestogen-releasing intrauterine systems [IUDs]),
A woman using "mini-drank" can start receiving Ekslutona any day; using an implant or IUD - on the day of their removal; using injectable forms of contraceptives - the day the next injection is to be made. In all these cases, the woman should be advised to use the barrier method additionally during the first 7 days of taking the tablets.
After 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 breast-feeding women, see the section on "Application in pregnancy and lactation." A woman should be advised to start taking the drug on the 21-28 day field of labor or an abortion in the second trimester. At a later start of the drug, the barrier method should be recommended for the first 7 days of taking the tablets. However, if there have been sexual intercourse after childbirth or abortion, it is necessary to exclude pregnancy or wait for the first menstrual period before starting Eksluton.
What to do in case of missing tablets
Contraceptive protection can be reduced if more than 27 hours have passed between taking the tablets. 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 pill should be taken at the usual time. If the delay in taking the tablet is more than 3 hours, then in this case it is necessary to additionally apply the barrier method for the next 7 days of taking the tablets, according to the above recommendation. If the pills were missed during the very first week of use, and during the week before passing the pills there was a sexual act, in this case, the possibility of pregnancy should be considered.
Recommendations in case of gastrointestinal disorders
In the case of gastrointestinal disorders, the absorption of the drug may be incomplete and therefore additional contraceptive measures should be taken. If vomiting occurs within 3 hours after taking the pill, then in this case the recommendations for missed tablets listed above apply. If a woman does not want to change the usual mode of taking tablets, she must take the additional tablet (s) necessary (s) from the other package.
Esplueton's side effects include irregular menstruation, soreness in the mammary glands, mood swings, nausea and headache, which occur in almost half of the women in the first cycle of Eksluton's use and are reduced to approximately 30% by the 12th cycle. Among women breastfeeding up to 28% experience side effects, with a decrease of up to 5% to the 12th cycle.
Other side effects reported with respect to Eksluton or, in general, for hormonal contraceptives are listed below.
Mammary glands: hypersensitivity, soreness, enlargement, galactorrhea
From the side of the central nervous system: headache, migraine, changes in libido, depression, change of mood.
From the digestive tract: nausea, vomiting, abdominal pain, diarrhea or constipation.
From the skin: various skin disorders (rash, erythema nodosum, erythema multiforme)
On the part of the genitourinary system: irregular bleeding, changes in vaginal secretion.
From the side of the eyes: intolerance of contact lenses.
Other : fluid retention, change in body weight, sensitivity reactions.
Occasionally, chloasma may occur, especially in women with chloasma during pregnancy in the anamnesis. Women with a predisposition to chloasma should avoid exposure to sunlight or ultraviolet radiation during the use of Ekslutona.
When using oral (combined) contraceptives, a number of adverse effects have been observed, including venous and arterial thromboembolic disorders, chloasma, and hormone-dependent tumors (eg, 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 is not established: jaundice and / or skin pruritus associated with cholestasis; the formation of gallstones, porphyria, systemic lupus erythematosus, haemolytic-uremic syndrome, Sydenham's chorea, herpes of pregnant women, hearing loss associated with otosclerosis.
Contraceptives containing only prostagene should not be used in the presence of any of the conditions listed below. If any of these conditions occur during the period of Eksluton's administration, the drug should be stopped immediately.
- hypersensitivity to the active substance or to any other component of Eksluton;
- established or suspected pregnancy;
- venous thromboembolism at the present time;
- the present or in the history of severe liver disease - before the normalization of liver function;
- cholestatic jaundice;
- porphyria (diagnosed or in anamnesis);
otosclerosis (diagnosed or in anamnesis);
- a history of herpes pregnant women;
- Progestogen-dependent tumors;
bleeding from the vagina of an unclear etiology.
With caution: in the presence of any of the following conditions / diseases, the benefits of using progestogen and the possible risks for each individual woman should be weighed. This should be discussed with a woman before she starts taking Eksluton. In cases of worsening, exacerbation of the disease, or the onset of any of these conditions, a woman should first consult a doctor to decide the possibility of further use of Eksluton.
Risk of breast cancer. Increases with age. During the use of oral contraceptives (OC), the risk of breast cancer increases slightly, which may be due to earlier diagnosis, the effect of the drug or a combination of these two factors. However, such an increased risk gradually disappears within 10 years after discontinuation of the use of OC, it is not associated with the duration of use and depends on the age of the woman during the use of OC. Cases of breast cancer diagnosed in women using oral contraceptives are less clinically evident than cancer in women who have never used OC. 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 the 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 a link between the use of combined oral contraceptives (COCs) and an increased incidence of venous thromboembolism(deep vein thrombosis and pulmonary embolism). Although it has not been clinically confirmed for contraceptives that do not contain an estrogen component, Eplyuton should be withdrawn in the case of thrombosis. It should also provide for the elimination of Eksluton in case of possible surgery or other, requiring a long-term immobilization disease. Women with thromboembolic disorders in history should be warned about the possibility of their recurrence.
Although progestogens can affect the resistance of peripheral tissues to insulin and glucose tolerance, there is no evidence that there is a need to change hypoglycemic therapy in diabetic patients using progestogen-containing OK. However, women with diabetes should be closely monitored during the entire period of progestogen-containing OK.
PREGNANCY AND LACTATION
Eksluton is not prescribed during pregnancy. If pregnancy occurs, Exlujuton should be discontinued immediately. Epidemiologic studies have shown that there is no increased risk of developing birth defects in children born to women who have used OC prior to pregnancy, or an increased risk of a teratogenic effect, when the OC was unintentionally taken during an early pregnancy. Data on the use during pregnancy of OC containing only progestogen is not available.
Similar to other contraceptives containing only progestogen, Exluuter does not affect the amount and quality of breastmilk, but it is known that a small amount of progestogen is excreted with milk. The amount of linestrol and metabolites that are excreted in milk is about 0.15% of the daily dose, no adverse effects on the growth and development of newborns have been reported.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication - the presence at the present time or in an anamnesis of severe liver disease.
The daily dose of lactose in the preparation (<50 Ојg) is such that women with lactose intolerance are unlikely to experience problems. Prevention of ectopic (ectopic) pregnancy with traditional progestogen-containing OCs ("mini-pili") is not as effective as in the use of COCs, as some women experience ovulation when using mini-pills. Additional risk factors for ectopic pregnancy include the presence of an ectopic pregnancy in history and tubal disease as a result of infection or surgery. In the case of pregnancy, when using Ekslutona, it is necessary to exclude ectopic pregnancy. In addition, in the conduct of differential diagnosis in the case of amenorrhea and abdominal pain, ectopic pregnancy should also be excluded.
Medical examinations / consultations
Before prescribing the drug, you should carefully read the medical history of a woman and conduct a gynecological examination to exclude pregnancy. Before the appointment of the drug should determine the cause of menstrual disorders, for example, oligomenorrhoea and amenorrhea. The interval between the control medical examinations is determined in each individual case. If the prescribed drug can affect the latent or existing disease, an appropriate schedule of control medical examinations should be made.
Despite the regular reception of Ekslutona, sometimes irregular spotting may occur. If bleeding is very frequent and irregular, consider using another method of contraception. If the above symptoms are stable, then in this case it is necessary to exclude organic pathology. The tactic for amenorrhea during the use of the drug depends on whether the pill was taken according to the instructions and in some cases the study should include pregnancy tests. In case of pregnancy, the drug should be stopped. Women should be informed that Eksluton does not protect against HIV infections (AIDS) and other sexually transmitted diseases.
The effectiveness of progestogen-containing OK can be reduced in case of missing tablets, gastrointestinal disorders or other medications.
Changes in the nature of menstruation
During the use of progestogen-containing contraceptives in some women, bleeding from the vagina may become more frequent or longer, while in other women these bleeding may become more rare or even stop. 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 need to see a doctor for more information about the effect of the drug. It is also possible to examine for the purpose of excluding malignant neoplasms or pregnancy.
Development of follicles
When all low-dose hormonal contraceptives are taken, follicles develop, and occasionally the size of the follicle can reach a size exceeding normal ones. Usually the enlarged follicles disappear spontaneously and asymptomatically; in some cases, slight pain in the lower abdomen is noted, in rare cases, surgical intervention is possible.
The data obtained with regard to COCs showed 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 protein transport levels, for example globulin, corticosteroid binding, lipid / lipoprotein fractions, carbohydrate metabolism, blood coagulation and fibrinolysis. Usually these changes remain within the normal range. It is not known to what extent this applies to contraceptives containing only progestogen.
Influence on ability to drive and other mechanisms
Based on the pharmacodynamic profile, it is believed that Eksluton does not have or has a negligible effect on the ability to drive and work with machinery.
No serious side effects were reported as a result of an overdose. Since the toxicity of LIN is very low, in the case of simultaneous administration of several tablets of Eksluton, severe toxic symptoms are not expected. Symptoms that may occur in this case are: nausea, vomiting, minor bleeding from the vagina. Antidotes are absent, further treatment should be symptomatic.
The interaction between OC and other drugs can lead to breakthrough bleeding and / or contraceptive protection. Special studies of interactions Ekslyutona with other drugs have been conducted. The literature reports the following interactions (mostly with COCs, but sometimes with progestagensoderzhaschimi contraceptives).
Hepatic metabolism: mOguta arise interaction with drugs that induce hepatic microsomal enzymes which lead to an increase in clearance of sex hormones. Mounted interaction with hydantoins, barbiturates, primidone, carbamazepine and rifamiitsinom; also possible with okskarbazeiinom, topiramate, rifabutin, felbamate, ritonavir, griseofulvin and preparations containing St. John's wort (Hypericum perforatum). Women using any of these drugs should temporarily use a barrier method in addition to Ekslyutonu or select another method of contraception. The barrier method should be used both during the concomitant use of medicinal products and for 28 days after the termination of their use.
In the application of the activated carbon absorption LIN can be reduced, and therefore, contraceptive effectiveness may decrease. If reception of activated carbon occurs within 3 hours after administration of the tablet preparation, the absorption may be incomplete. In this case it is necessary to follow recommendations concerning reception missed pills.
OK may affect the metabolism of other drugs. Accordingly, it may change the drug concentration in plasma and in tissues (e.g., cyclosporin).
To identify possible interactions should read the instructions for use of these drugs.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
At a temperature of 2-30 В° C, protected from light. Do not freeze. Keep out of the reach of children.
Shelf life 5 years. Do not use after expiry date.