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Active ingredients
Linestrenol
Release form
Pills
Composition
Linestrenol 500 mcg; Excipients: potato starch, amylopectin, lactose monohydrate, magnesium stearate.
Pharmacological effect
Exluton is an oral contraceptive (OC) that does not contain estrogen and contains only the progestogen component linestrenol (LIN). When it enters the body, the PIN is converted into the biologically active metabolite norethisterone (NET), which binds to the progesterone receptors in target organs, including myometria .; The Contraceptive Effect of Exlyuton is achieved mainly by increasing the viscosity of the cervical mucus (thereby preventing sperm from moving), reducing the endometrial sensitivity to oocytes (thus disturbing the fertilized egg's nidation), and impaired peristalsis of the fallopian tubes. Moreover, almost 70% of women do not ovulate, as evidenced by the absence of a peak increase in luteinizing hormone (LH) in the middle of the cycle and an increase in progesterone level. At the same time, no clinically significant effect on the metabolism of carbohydrates, lipids and hemostasis was detected.
Pharmacokinetics
After ingestion of the drug Exluton, linestrinol, which is a prodrug, is rapidly absorbed and converted into a pharmacologically active metabolite norethisterone (NET). The maximum levels of NET in the blood plasma are reached 2-4 hours after ingestion of the pill, its absolute bioavailability is 64%; Distribution; 96% of NET is associated with plasma beams, mainly with albumin (61%) and to a lesser extent with globulin that binds sex hormones (35%) .; Metabolism; IH metabolism phase I includes 3-hydroxylation and subsequent dehydrogenation. The active metabolite NET is then restored; degradation products are in the form of conjugates with sulfates and glucuronides .; Withdrawal; The average T1 / 2 NET is about 15 hours. The rate of removal 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 PIN) and through the intestine in a 1.5: 1 ratio.
Indications
- contraception.
Contraindications
Contraceptives containing only prostagens should not be used in the presence of any of the conditions listed below. If any of these conditions occur while Exluton is in use, the drug should be stopped immediately; - hypersensitivity to the active substance or to any other component of Exluton; - established or suspected pregnancy; - venous thromboembolism at present; - the presence at present or in the history of severe liver disease - to normalize the indicators of liver function; - cholestatic jaundice; - porphyria (diagnosed or in history); - otosclerosis (diagnosed or in the anamnesis); - Herpes of pregnant women in history; - progestogen-dependent tumors; - bleeding from the vagina of unknown etiology .; With care: if you have any of the conditions / diseases listed below, you should weigh the benefits of using progestogen and 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 whether it is possible to continue using Exluton .; The risk of breast cancer. Increases with age. During the use of oral contraceptives (OC), the risk of breast cancer slightly increases, possibly 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 stopping the application of OC, it is not related to the duration of application and depends on the age of the woman during the use of OA. Cases of breast cancer diagnosed in women, using oral contraceptives are clinically less pronounced than the identified cancer in women who have never used OK. An individual assessment should be made of the relationship between the benefits and the risk of using contraceptives in the presence of breast cancer .; Since it is impossible to exclude the negative effect of progestogens on the development of liver cancer, an individual assessment of the balance between benefits and risks should be carried out .; In epidemiological studies, a link has been established between the use of combined oral contraceptives (OCCs) and the increased incidence of venous thromboembolism (deep vein thrombosis and pulmonary embolism).And although this is not clinically confirmed for contraceptives that do not contain an estrogen component, Exluton should be discontinued in the event of thrombosis. It should also provide for the withdrawal of the drug Exluton in the event of a possible operation or another, requiring prolonged immobilization of the disease. Women with a history of thromboembolic disorders should be warned about the possibility of their recurrence .; Although progestogens may affect peripheral tissue insulin resistance and glucose tolerance, there is no evidence that there is a need to change hypoglygemic therapy in diabetics who use progestogen-containing OK. However, women suffering from diabetes should be carefully monitored during the entire period of use of progestogenic OK.
Use during pregnancy and lactation
Exluton is not prescribed during pregnancy. In case of pregnancy, Exlyuton should be discontinued immediately. Epidemiologic studies have shown that there is neither an increased risk of birth defects in children born to women who used OC before pregnancy, nor an increased risk of a teratogenic effect, when OK was inadvertently taken in early pregnancy. There are no data on the use of progestogen-only OC during pregnancy. Like other contraceptives containing only progestogen, Exluton does not affect the quantity and quality of the breast molog, 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; undesirable effects on the growth and development of the newborn have not been reported.
Dosage and administration
How to take the drug Exlyuton; Tablets should be taken orally in the order indicated on the packaging, every day at about the same time, if necessary, with a small amount of water. Daily for 28 consecutive days should be taken one tablet. Each subsequent package should be started immediately after the previous package has been completed .; In the absence of previous use of hormonal contraceptives (during the last month); Taking pills should be started on the first day of the woman's menstrual cycle (on the first day of menstruation).You can start taking and 2-5 days of the cycle, but then during the first 7 days of the first cycle of taking the pills, it is recommended to additionally apply a barrier method of ontraception .; Transition from COC; A woman should start taking Exluton on the 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 drugs that contain progestogen only ("mini-pili", injections, implants or progestogen-containing intrauterine systems [IUD]); A woman using the "mini-pili" can start taking Exluton on any given day; using an implant or IUD - on the day of their removal; using injection forms of contraceptives - on the day when the next injection should be given. In all these cases, the woman should be advised to additionally use a 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 breastfeeding women, see the section "Use during pregnancy and lactation". A woman should be recommended to start taking the drug on the 21-28 day field of childbirth or abortion in the second trimester. At a later start of taking the drug, it should be recommended to apply the barrier method during the first 7 days of taking the pills. However, if you have already had sexual intercourse after childbirth or abortion, you must exclude pregnancy or wait for the first menstrual period before you start taking Exluton. What to do if you miss the pills; Contraceptive protection can be reduced if it has been more than 27 hours between taking the pill. If the delay in taking the pill is less than 3 hours, in this case, the missed pill should be taken as soon as possible, and the next pill 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 apply a barrier method within the next 7 days of taking the pills, according to the above recommendation. If the pills were missed during the very first week of use, and during the week before the pills were missed, sexual intercourse took place,in this case, the possibility of pregnancy should be considered .; Recommendations in case of gastrointestinal disorders; In case of gastrointestinal disorders, the absorption of the drug may be incomplete and therefore additional contraceptive measures should be used. If vomiting occurs within 3 hours after taking the pill, then the recommendations regarding the missed pills given above apply in this case. If a woman does not want to change the usual mode of taking the pills, she must take the additional pill (s) needed from the other package.
Side effects
The side effects of Escluton include irregular menstruation, breast tenderness, change of mood, nausea and headache, which occur in almost half of women in the first cycle of Exluton use 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 hormonal contraceptives in general are listed below .; Mammary glands: hypersensitivity, soreness, increase, galactorrhea; From the side of the central nervous system: headache, migraine, changes in libido, depression, changing moods .; On the part of the digestive tract: nausea, vomiting, abdominal pain, diarrhea or constipation .; On the part of the skin: various skin disorders (rash, erythema nodosum, erythema multiforme); On the part of the urogenital system: irregular bleeding, changes in vaginal secretion .; On the part of the organs of vision: intolerance to contact lenses .; Other: fluid retention, change in body weight, hypersensitivity reactions .; Chloasma can sometimes occur, especially in women with a chloasma during pregnancy in history. 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 were observed, including venous and arterial thromboembolic disorders, chloasma and hormone-dependent tumors (for example, liver tumors, breast cancer) .; The following conditions have been described as during pregnancy,and during the use of steroid drugs, but their relationship with the use of progestogens has not been established: jaundice and / or itchy skin associated with cholestasis; gallstones, porphyria, systemic lupus erythematosus, hemolytic-uremic syndrome, Sydenhem's chorea, herpes of pregnant women, hearing loss associated with otosclerosis.
Overdose
No serious adverse effects have been reported as a result of overdose. Since the toxicity of PIN is very low, in case of simultaneous administration of several pills of Exluton, severe toxic symptoms are not expected. Symptoms that may arise in this case are the following: nausea, vomiting, slight bloody discharge from the vagina. There are no antidotes, further treatment should be symptomatic.
Interaction with other drugs
The interaction between OC and other drugs can lead to breakthrough bleeding and / or a violation of contraceptive protection. Special studies on the interaction Exluton with other drugs have not been conducted. The following interactions have been reported in the literature (mainly with COCs, but sometimes with progestogen-containing contraceptives) .; Hepatic metabolism: there may be interactions with drugs that induce microsomal liver enzymes, which lead to an increase in the clearance of sex hormones. Interactions with hydantoins, barbiturates, primidone, carbamazepine and rifamycin have been established; It is also possible with oxcarbazein, topiramate, rifabutin, felbamate, ritonavir, griseofulvin and preparations containing St. John's wort (Hypericum perforatum). Women using any of these medicines should temporarily use a barrier method in addition to Exluton or choose another method of contraception. Barrier method should be used during concomitant use of drugs, and within 28 days after the cessation of their use .; With the use of activated carbon, the absorption of PIN may decrease and, therefore, contraceptive efficacy may decrease. If the intake of activated carbon occurs within 3 hours after taking the pill of the drug, the absorption may be incomplete.In this case, you should be guided by the recommendations regarding the administration of the missed pills .; OK can affect the metabolism of other drugs. Accordingly, drug concentrations in plasma and in tissues may change (for example, cyclosporin) .; To identify possible interactions, you should read the instructions for use of these medicines.
special instructions
The daily dose of lactose in the preparation (<50 µg) is such that women with lactose intolerance are unlikely to have problems. Prevention of ectopic (ectopic) pregnancy with traditional progestogen-containing OK ("mini-drank") is not as effective as with the use of COC, because when using the "mini-drank" in some women ovulation occurs. Additional risk factors for ectopic pregnancy include a history of ectopic pregnancy and tubal disease as a result of infection or surgery. In case of pregnancy, when using Exluton, it is necessary to exclude an ectopic pregnancy. In addition, when conducting a differential diagnosis in the case of amenorrhea and abdominal pain, ectopic pregnancy should also be excluded .; Medical examinations / consultations; Before prescribing the drug, carefully review the woman’s medical history and conduct a gynecological examination to rule out pregnancy. Before the appointment of the drug should establish the cause of violations of the menstrual cycle, for example, oligomenorrhea and amenorrhea. The interval between the control medical examinations is determined in each individual case. If the prescribed drug can affect a latent or existing disease, an appropriate schedule of follow-up medical examinations should be drawn up .; Despite regular use of Exlyuton, occasional bleeding may sometimes occur. If the bleeding is very frequent and irregular, you should consider using another method of contraception. If the above symptoms are persistent, then in this case it is necessary to exclude organic pathology. Tactics in relation to amenorrhea during the use of the drug depends on whether the pills were taken in accordance with the instructions and, in some cases, pregnancy tests should be included in the study. In the event of pregnancy, the drug should be discontinued.Women should be informed that Exluton does not protect against HIV infections (AIDS) and other sexually transmitted diseases .; Reduced efficacy; The efficacy of progestagen-containing OC may be reduced if a patient misses pills, gastrointestinal disorders, or other medications. Changes in the nature of menstruation; During use of progestogen-containing contraceptives in some women, bleeding from the vagina may become more frequent or more prolonged, while in other women these bleeding may become more rare or stop altogether. These changes are often the reason that the woman refuses this method of contraception, or ceases to strictly follow the instructions of the doctor. In this case, you need to contact your doctor for further clarification about the effect of the drug. It is also possible to examine for the purpose of excluding malignant neoplasms or pregnancy .; Follicle development; When all low-dose hormonal contraceptives are taken, follicles develop, and occasionally the size of the follicle may reach sizes that are larger than normal. Usually enlarged follicles disappear spontaneously and asymptomatically; in some cases there is a slight pain in the lower abdomen, in rare cases surgical intervention is possible .; Laboratory analyzes; The data obtained for COCs have shown that the use of contraceptive steroids may influence the results of some laboratory tests, including biochemical indicators of liver, thyroid, adrenal and kidney function, plasma transport protein levels, for example, globulin, corticosteroids binding, lipid / lipoprotein fractions, carbohydrate metabolism, blood clotting and fibrinolysis. Usually these changes remain within the normal range. It is not known to what extent this also applies to contraceptives containing only progestogen .; Influence on the ability to drive a car and other mechanisms; Based on the pharmacodynamic profile, Exluton is considered to have no or negligible impact on the ability to drive a car and work with mechanisms.