Silest - instructions for use, dose, side effects, contraindications

Active substanceNorgestimate + EthinylestradiolNorgestimate + Ethinylestradiol

Similar drugsTo uncover

The Silistus

pills inwards

Johnson & Johnson, LLC Russia

Dosage form: & nbsppills

Composition:

1 tablet contains:

active substances: norgestimate 0.250 mg, ethinylestradiol 0.035 mg;

auxiliary substances: lactose, gelatinized starch, magnesium stearate, FD & C Blue # 2 Lacquer 13%.

Description:

Tablets of blue color of round plano-cylindrical shape with bevelled edges and engraved "C250" on both sides.

Pharmacotherapeutic group:Contraceptive agent (estrogen + progestogen)

ATX: & nbsp

G.03.A.A.11 Norgestimate and Ethinylestradiol

Pharmacodynamics:

Silest is a combined oral contraceptive, the effect of which is determined by the central and peripheral mechanisms. Suppressing the secretion of gonadotropins, Sileste prevents the maturation of eggs in the ovaries and ovulation.

In addition, Sileste increases the viscosity of cervical mucus, which makes it difficult for sperm to penetrate the uterus, and acts on the epithelium of the endometrium, reducing the likelihood of implantation.

Pharmacokinetics:

When taken orally, norgestimate is well absorbed either alone or in combination with ethinylestradiol. The maximum concentration (C_mOh) in the blood plasma is achieved in 1-2 hours. Norgestimate is actively metabolized. The half-life is about 4 hours. Metabolites are excreted slowly from the body. After 2 weeks about 50 % the active substance is excreted in urine and about 40% - with feces.

Ethinyl estradiol is rapidly and almost completely absorbed when taken orally. FROMmah in the blood plasma is achieved after 1-2 hours. Ethinylestradiol only partially metabolized in the body. The half-life is 4.5 hours. Over 17% of the active substance is excreted unchanged in the urine and more than 10% is excreted with feces. Metabolites are estradiol, estriol and, mainly, 2-hydroxy and 16ß-hydroxyethynylestradiol.

Indications:

Contraception in women.

Contraindications:

- hypersensitivity to any of the components of the drug;

- venous thrombosis, including in the history (including deep vein thrombosis, pulmonary thromboembolism);

- arterial thrombosis, including in anamnesis (including acute disturbance of cerebral circulation, myocardial infarction, retinal artery thrombosis) or precursors of thrombosis (including angina pectoris or transient ischemic attack);

- presence of serious or multiple risk factors for arterial thrombosis:

- arterial hypertension (persistent increase in blood pressure above 160/100 mm Hg);

- diabetes mellitus with vascular lesions;

- hereditary dyslipoproteinemia;

- hereditary predisposition to venous or arterial thrombosis, eg, antithrombin III deficiency, protein C deficiency, protein deficiency S, hyperhomocysteinemia, the presence of antiphospholipid antibodies (antibodies against cardiolipin, a group of antibodies against negatively charged phospholipids);

- migraine with aura;

- confirmed or suspected breast cancer;

- endometrial cancer or other confirmed or suspected estrogen-dependent neoplasms;

- benign or malignant liver tumors;

- genital bleeding of unclear etiology;

- postmenopausal period;

- age to 18 years;

- postpartum period (4 weeks);

- lactation period.

- confirmed or suspected pregnancy

- Cholestatic jaundice during pregnancy, incl. and in the anamnesis;

- sickle-cell anemia

- liver failure

- hemolytic anemia

- otosclerosis.

Carefully:

- venous or arterial embolism in brothers, sisters or parents at a relatively young age;

- prolonged immobilization or extensive surgical operation;

- risk factors for coronary heart disease, such as smoking, hyperlipidemia, hypertension or obesity;

- arterial hypertension (persistent blood levels of 140-159 / 90-99 mm Hg);

- thrombophlebitis of superficial veins and varicose veins;

- damage to the valvular heart apparatus with complications (mitral stenosis with atrial fibrillation);

- diabetes;

- severe depression or history of the disease;

- systemic lupus erythematosus;

- Crohn's disease;

- ulcerative colitis;

- hypertriglyceridemia, including in family history;

- acute violation of liver function during previous pregnancy or previous use of sex hormones;

- menstrual cycle disorders;

- impaired renal function;

- diseases of the gallbladder;

- epilepsy;

- uterine myoma;

- mastopathy;

- tuberculosis.

Pregnancy and lactation:

The drug Silestus is contraindicated in pregnant women.

Epidemiological studies have not revealed an increase in the risk of birth defects in children whose mothers before the pregnancy have taken oral contraceptives. Most modern studies have also not revealed teratogenic effects,in particular, heart abnormalities and shortening of limbs, in offspring of women who mistakenly took oral contraceptives during pregnancy.

Combined oral contraceptives can affect lactation, i.e. reduce the amount and change the composition of breast milk. In addition, a small portion of contraceptive steroids and / or their metabolites can penetrate into breast milk. In connection with this, Silestus is contraindicated in the period of breastfeeding.

Dosing and Administration:

Inside. Use Silest should start with taking one tablet of the drug on the first day of menstrual bleeding. After that, within 20 days, one tablet should be taken daily. Then follows a seven-day break in taking the drug. Usually, a few days after the end of taking the tablets, menstrual bleeding occurs. The next cycle of reception of the Silestus should begin on the eighth day, i.e. seven days after the cessation of taking the tablets during the previous cycle. The first tablet of the new cycle should be taken regardless of whether the bleeding has stopped or is still bleeding.

The days of the week are marked on the blister pack of the drug. For the convenience of checking the regularity of taking tablets, it is recommended to start each new cycle with a tablet marked with a given day of the week, and continue without interruption the entire reception cycle.

Contraceptive tablets are most effective if taken at the same time of day, for example, in the morning.

If you miss the usual time of admission, the tablet should be taken immediately. Departure from the usual time of taking up to 12 hours provides a reliable contraceptive effect. The effectiveness of the drug decreases with a delay in taking the tablet for more than 12 hours. If more than 12 hours have passed since the usual time of taking the drug or if more than one pill is missed, the drug should be immediately resumed leaving a missing tablet in the package. However, before the end of this cycle, additional means of protection from pregnancy, such as a condom or vaginal contraceptive suppositories, should be used. In such situations, one can not rely on the method of "safe days" or "temperature" method of contraception.

After the birth of the child, the reception of Silest should be started no earlier than 4 weeks after the birth, provided that the woman does not breast-feed the baby.

After an abortion or miscarriage for a period of up to 20 weeks of pregnancy the taking of tablets can begin immediately, in these cases the use of additional methods of contraception is not required.After induced or spontaneous abortion at the term of pregnancy for more than 20 weeks, hormonal contraceptives can be started on the 21st day after the abortion or on the first day of the appearance of natural menstruation (whichever comes first). In these cases, during the first 7 days of the cycle, in addition to taking Silest, additional local contraceptives should be used. In exceptional cases, in the presence of medical indications to ensure immediate reliable contraception, the reception of Silest can be started 1 week after the abortion. It should be borne in mind that the risk of thromboembolic complications is increased with admission during the post-abortion period.

If there is vomiting or diarrhea, the silage may lose its effectiveness, because the body needs 4 hours to fully absorb the pill.In this case it is recommended to continue reception of the Silestas, supplementing its action with other contraceptive means before the onset of menstruation

Side effects:

The cardiovascular system: Arterial hypertension, myocardial infarction, cerebral circulation disorders, deep vein thrombosis, arterial thromboembolism, thromboembolism of pulmonary or other vessels, edema.

Tumors: benign and malignant liver tumors, cervical and breast cancer.

Hepatobiliary system: Cholestatic jaundice, Badda-Chiari syndrome, intrahepatic cholestasis, cholelithiasis.

Gastrointestinal tract: nausea, vomiting, abdominal pain, flatulence, colitis.

Genital organs: intermenstrual bleeding, spotting spotting, amenorrhea, changes in the menstrual cycle, increasing the size of uterine fibroids, vaginal candidiasis, increased secretion of the cervix, erosion of the cervix, decreased libido, premenstrual syndrome, temporary infertility after the end of the drug

Thoracic glands: soreness and sensation of tension, galactorrhea, engorgement, increase in size, reduction of lactation in admission immediately after childbirth.

Leather: nodosum erythema, skin rash, chloasma, exudative erythema, acne, seborrhea, alopecia, hirsutism, pigment spots on the face, hypertrichosis, pemphigoid (gestational herpes), melasma with a tendency to persist.

Organs of vision: cataract, damage to the eye nerve, changes in the curvature of the cornea, a feeling of discomfort when wearing contact lenses.

Central nervous system: headache, mood changes, irritability, depression, chorea.

Metabolism: fluid retention, changes in body weight (decrease or increase), decreased glucose tolerance, changes in appetite.

Kidney: decreased kidney function, hemolytic-uremic syndrome.

Others: dizziness, migraine.

When menstrual bleeding occurs, the reception of Silestus should be continued. If the bleeding does not stop, then a survey should be carried out to eliminate organic causes. Similar recommendations apply to spotting bloody discharge, which may appear irregularly during several cycles of receiving Silest or for the first time after prolonged use of the drug.If after the end of the cycle of taking the drug bleeding does not occur, it is necessary to exclude the presence of pregnancy before the start of a new cycle of reception of Silestus.

Overdose:

Serious cases of poisoning due to an overdose of Silestus were not noted. Overdose may cause nausea, vomiting, and vaginal bleeding.

There is no specific antidote. In case of an overdose, it is necessary to rinse the stomach (within the first hour after taking the drug) and perform symptomatic therapy.

Interaction:

Drugs that induce the induction of enzymes that metabolize estrogens (eg, estrogen-2-hydroxylase-coenzyme 3A4 of the cytochrome P-450 system), reduce the contraceptive effectiveness of hormonal drugs. It is also possible that induction of these same isozymes can lead to a decrease in the blood concentration of the progestogen component of the preparation Silest. Potentially clinically relevant in this regard are medicines and herbal remedies that affect the enzymes that participate in the biological transformation of contraceptive steroid hormones (for example, St. John's wort, barbiturates, carbamazepine, phenytoin, sulfonamides, pyrazolone derivatives, rifampicin).

It has been shown that some protease inhibitors and some antiretroviral drugs increase (for example, indinavir) or reduce (e.g., ritonavir) concentration in the blood of combined hormonal contraceptives.

Another type of interaction is the violation of intrahepatic circulation of estrogens, as a result of which the excretion is accelerated and the concentration of ethinyl estradiol is reduced. When co-administered with certain antibiotics (eg, ampicillin or tetracycline), insufficient cleavage of conjugates of estrogens and fatty acids by intestinal bacteria is observed.

Laboratory Tests

Oral contraceptives can cause changes in hormonal parameters and liver function parameters:

- The levels of prothrombin and factors II, VII, VIII, IX, X, XII and XIII increase; decreases the level of antithrombin 3; the platelet aggregation caused by norepinephrine is increased.

- Increases the concentration of thyroxine-binding globulin, which causes an increase in the concentration of the total thyroid hormone,

- The serum content of other binding proteins may be increased.

- Increase levels of globulins, binding sex hormones,as a result, the concentration of sex hormones increases; it should be noted, however, that levels of free or biologically active sex hormones decrease or do not change.

- Can increase the levels of cholesterol high-density lipoproteins (X- HDL) cholesterol and total cholesterol, cholesterol of low density lipoproteins (LDL-C) may be increased or decreased, while the ratio of LDL-C / HDL-X may be reduced, and the triglyceride levels remain unchanged .

- Glucose tolerance may decrease.

The use of oral contraceptives can cause a decrease in serum folate concentrations. This change can be important from a clinical point of view, if a woman becomes pregnant soon after stopping taking an oral contraceptive.

Special instructions:

Oral contraceptives are NOT PROTECTED from HIV infection (AIDS) and other sexually transmitted diseases.

Before appointing a patient to an oral contraceptive, it is recommended to collect a complete history and conduct a thorough physical examination. Surveys should be periodically repeated in accordance with the standards of quality gynecological care.

Before appointing a patient to an oral contraceptive, she needs to find out what herbal remedies she is taking, as well as read the information in the leaflets-inserts to the drugs that the woman will take simultaneously with the oral contraceptive.

In the presence of undiagnosed, permanent or repeated abnormal vaginal bleeding, a malignant tumor must be excluded.

After the hepatitis, the oral contraceptive can be given after 3 months (in severe cases after 6 months) after the normalization of the results of functional hepatic tests.

Thromboembolic and other vascular complications

It is established that the use of oral contraceptives increases the risk of thromboembolic complications and thromboses. Case-control studies have shown that the relative risk in women using oral contraceptives is 3: 1 for the first episode of superficial vein thrombosis, 11: 4 for deep vein thrombosis or thromboembolism compared to those who do not use these drugs pulmonary artery and 6: 1.5 in women with diseases predisposing to thromboembolic complications.Studies have shown that the relative risk is somewhat lower, about 3: 1 for new cases and about 4.5: 1 for new cases requiring hospitalization. The risk of thromboembolic complications associated with the use of oral contraceptives does not depend on the duration of administration of these drugs and disappears after discontinuation of their intake,

In women using oral contraceptives, the relative risk of postoperative thromboembolic complications is increased 2-4 times. The relative risk of venous thrombosis in women with diseases predisposing to this complication is 2 times higher than in women without such diseases. If possible, oral contraceptives should not be taken at least 4 weeks before and within 2 weeks after a scheduled operation that is associated with an increased risk of thromboembolism, and also during prolonged immobilization and during the recovery period. In the early postpartum period, the risk of thromboembolic complications is also increased, and therefore women who choose not to breast-feed can begin taking oral contraceptives no earlier than 3 weeks after delivery.After an artificial or spontaneous abortion that took place at the 20th week of pregnancy or later, the use of hormonal contraceptives can begin either on the 21st day after the abortion, or on the first day of the first spontaneous menstruation, whichever comes first.

The relative risk of arterial thrombosis (eg, stroke, myocardial infarction) increases with other predisposing factors, such as smoking, hypertension, hyperlipidemia, obesity, diabetes, preeclampsia in the anamnesis and middle-aged. These severe vascular complications were observed in women who took oral contraceptives with an estrogen content of 50 μg or more. The risk of vascular complications is probably less when using oral contraceptives,containing lower doses of estrogen and progestogen, but this assumption has not yet received solid evidence.

The risk of serious cardiovascular side effects increases with age, as well as in heavy smokers. This risk is very high among smokers over 35 years old. Women who use oral contraceptives should be strongly advised to stop smoking.

It was reported that the increase in blood pressure in women taking oral contraceptives. Studies have shown that with prolonged use of estrogen at a dose of 50 mcg or more, the likelihood of an increase in blood pressure increases with age. At many women after the termination of reception of oral contraceptives the arterial pressure is normalized. It was not possible to detect differences in the incidence of hypertension in women who had taken oral contraceptives in the past, and in women who had never taken such drugs.

In women with arterial hypertension (persistent blood pressure level of 140-159 / 90-99 mm Hg) before starting oral contraceptive it is necessary to normalize blood pressure. In the case of a strong increase in blood pressure, oral contraceptive should be stopped.

There are reports of the occurrence of retinal thrombosis associated with the use of oral contraceptives. The intake of oral contraceptives must be discontinued in case of unexplained transient, partial or complete loss of vision; the appearance of a veil before your eyes or diplopia; edema of the nipple of the optic nerve or the occurrence of changes in the vessels of the retina.In such situations, appropriate diagnostic and therapeutic actions must be carried out without delay.

Liver Neoplasms

Benign and malignant liver tumors (adenoma and hepatocellular carcinoma) are rare. Case-control studies have shown that the risk of these tumors can increase with the use of oral contraceptives and depends on the duration of their use. A rupture of benign adenomas of the liver can cause death due to internal bleeding.

Cancer of the genitals and mammary glands

The frequency of cancer of breast, endometrial, ovarian and cervical cancer in women who use oral contraceptives have been the subject of study of numerous epidemiological studies. There are conflicting results, but most studies have shown that the use of oral contraceptives is not associated with a general increase in the risk of breast cancer. Some authors reported an increase in the relative risk of breast cancer, especially in young women. It is shown that this increased relative risk depends on the duration of use of oral contraceptives.

A meta-analysis of the results of 54 epidemiological studies shows that women who use combined oral contraceptives now or have taken them in the previous 10 years have a slightly increased risk of detecting breast cancer. Based on these data, it is not possible to determine whether the increased risk is due to earlier diagnosis of breast cancer in women who have ever used oral contraceptives, the biological effects of hormonal contraceptives, or a combination of these two factors. This meta-analysis gives It is also reasonable to assume that the age at which women stop taking combined oral contraceptives is an important risk factor for breast cancer: the older the age, the more often breast cancer is diagnosed. The duration of oral contraceptive use is not so important.

Before the appointment of a woman with an oral contraceptive, it is necessary to discuss the possibility of increasing the risk of breast cancer and correlate this risk with the benefits of combined oral contraceptives.

Some epidemiological studies have shown that prolonged intake of oral contraceptives is accompanied by an increased risk of neoplasm of the cervix. The association of these data with the use of combined oral contraceptives has not been demonstrated. It should be noted, however, the uncertainty of the extent to which these data may be due to differences in sexual behavior and other factors.

Metabolic Effects

Oral contraceptives can reduce glucose tolerance. It is shown that this effect directly depends on the dose of estrogen. In addition, progestogen can increase insulin secretion and cause insulin resistance, and this effect is different for different progestogens. However, it should be noted that in women without diabetes, oral contraceptives, most likely, do not affect the fasting blood glucose level. Considering the above, it is necessary to closely monitor the condition of women with impaired glucose tolerance or diabetes mellitus taking oral contraceptives.

A small percentage of women with oral contraceptives receive persistent hypertriglyceridemia.In women using oral contraceptives, there were changes in serum triglyceride and lipoprotein levels.

Headache

AT the case the emergence or increase of migraine, and the appearance of a new type of headache that is recurrent, persistent or severe, it is necessary to stop taking the oral contraceptive and to find out the cause of the headache.

Menstrual disorders

Women who use oral contraceptives, especially in the first 3 months of their admission, may experience intermenstrual bleeding, spotting and / or amenorrhea. Non-hormonal causes of these disorders should be considered and, if necessary, appropriate diagnostic procedures should be conducted to exclude a malignant tumor or pregnancy.

In some women, amenorrhea or oligomenorrhoea may occur when taking an oral contraceptive, especially if these conditions were observed before the use of the contraceptive drug.

Chloasma

Against the background of taking oral contraceptives, sometimes there is chloasma, in particular in women who have a history of chloasma of pregnant women.Women who are prone to develop chloasma should avoid exposure to sun and ultraviolet radiation while using oral contraceptives. Chloasma often does not disappear completely.

Form release / dosage:

Tablets 250 mcg + 35 mcg.

Packaging:21 tablets per blister. 1 or 3 blisters with instructions for use in a cardboard bundle.

Storage conditions:

At a temperature of 15 to 30 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011462 / 01

Date of registration:16.02.2012

The owner of the registration certificate:Johnson & Johnson, LLC Johnson & Johnson, LLC Russia

Manufacturer: & nbsp

CILAG, AG Switzerland

Information update date: & nbsp06.08.2015

Illustrated instructions

Instructions

The Silistus (Cilest)