Norgestimate + Ethinylestradiol (Noraelgestrominum + Aethinyloestradiolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

"Estrogens, gestagens, their homologues and antagonists"

Included in the formulation
  • The Silistus
    pills inwards 
    Johnson & Johnson, LLC     Russia
    • АТХ:

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

    Pharmacodynamics:

    The central mechanism:

    By the mechanism of negative feedback, the drug causes a sharp decrease in the frequency of impulse secretion of gonadoliberin. As a result, in the proliferative phase of the menstrual cycle oppresses the production of FSH by the pituitary (action due to exogenous estrogen), which slows the growth and maturation of follicles in the ovaries. Exogenous gestagens suppress the release of LH by the pituitary gland, which leads to suppression of ovulation. There is a decrease in the synthesis of endogenous estrogens and progesterone.

    Peripheral mechanism:

    The drug increases the viscosity of cervical mucus, complicating the penetration of spermatozoa into the uterine cavity.

    Decrease in peristalsis of fallopian tubes, caused by gestagens, leads to the untimely entry of a fertilized egg into the uterine cavity. Under the influence of combined estrogen-progestogen drugs there are changes in the structure of the endometrium, which complicates the normal implantation of a fertilized egg.

    Pharmacokinetics:

    Norgestimate: when taken orally absorbed for 2 hours, is metabolized to 17-deactyl norgestimate and levonorgestrel.

    The half-life is about 4 hours. Metabolites are excreted slowly from the body. After 2 weeks, about 50% of the active substance is excreted in the urine and about 40% - with feces.

    Ethinyl estradiol: quickly and almost completely absorbed when taken orally. The maximum concentration in the blood plasma is achieved in 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 16β-hydroxyethyne estradiol.

    Indications:

    Contraception.

    ICD-10

    XXI.Z30-Z39.Z30.0   General advice and advice on contraception

    Contraindications:

    Venous thrombosis, including in the anamnesis (including deep vein thrombosis, pulmonary thromboembolism).

    Arterial thrombosis, including in the history (including acute disorders of cerebral circulation, myocardial infarction, retinal arterial 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).

    Diabeteswith the defeat of blood vessels.

    Hereditary dyslipoproteinemia.

    Hereditary predisposition to venous or arterial thrombosis, for example, deficiency of antithrombin-lll, deficiency of protein C, deficiency of protein S, hyperhomocysteinemia, presence of antiphospholipid antibodies (antibodies against cardiolipin, group of antibodies against negatively charged phospholipids).

    Hypersensitivity.

    Migraine with aura.

    Thromboembolism.

    Cerebrovascular disorders.

    Breast carcinoma and endometrium, other estrogen-dependent formations.

    Liver failure.

    Hemolytic anemia.

    Benign or malignant liver tumors.

    Otosclerosis.

    Cholestatic jaundice during pregnancy, including in the anamnesis.

    Sickle-cell anemia.

    Cardiac ischemia.

    Bleeding from the genitals of unclear etiology.

    The postmenopausal period.

    Age to 18 years.

    Postpartum period (4 weeks).

    Pregnancy and lactation.

    Carefully:

    Ulcerative colitis.

    Venous or arterial embolism in brothers, sisters or parents at a relatively young age.

    Long-term immobilization or extensive surgical operation.

    Risk factors for coronary heart disease, such as smoking, hyperlipidemia, arterial hypertension or obesity.

    Arterial hypertension (persistent blood levels of 140-159 / 90-99 mm Hg).

    Mastopathy.

    Thrombophlebitis superficial veins and varicose veins.

    Myoma of the uterus.

    Depression.

    Diseases of the liver and gallbladder.

    Epilepsy.

    Disorders of valvular heart apparatus with complications (mitral stenosis with atrial fibrillation).

    Adolescence.

    Tuberculosis.

    Crohn's disease.

    Hypertriglyceridemia, including in family history.

    Systemic lupus erythematosus.

    Kidney diseases.

    Acute disruption of liver function during previous pregnancy or previous use of sex hormones.

    Violations of the menstrual cycle.

    Pregnancy and lactation:

    Category FDA - X. The drug 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 limb shortening, in offspring of women who mistakenly took oral contraceptives during pregnancy.

    Combined oral contraceptives can affect lactation, that is, 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, take 1 tablet every day for 20 days, then make a seven-day break. The interval between doses of the drug should not exceed 36 hours.

    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. The deviation from the usual intake time up to 12 h provides a reliable contraceptive effect. The effectiveness of the drug decreases with a delay in taking the tablet for more than 12 hours.If the usual time of taking the drug has been more than 12 hours or missed taking more than one pill, taking the drug should be immediately renewed, leaving the package missed the pill. 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.

    Side effects:

    Kidney disease, depression, decreased libido, decreased glucose tolerance, weight change.

    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.

    GIT: nausea, vomiting, abdominal pain, flatulence, colitis, a violation of appetite.

    Genitals: intermenstrual bleeding, spotting bleeding, amenorrhea, changes in the menstrual cycle, increased uterine fibroids, vaginal candidiasis, increased cervical secretion, cervical erosion, decreased libido, premenstrual syndrome, temporary infertility after the end of the drug intake

    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.

    CNS: headache, mood changes, irritability, depression, chorea, dizziness, migraine,

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

    Kidney: decreased kidney function, hemolytic-uremic syndrome.

    Others: kidney disease, decreased libido.

    When menstrual bleeding occurs, the drug 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 taking the drug 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 taking the drug.

    Overdose:

    Vomiting, nausea 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:

    Enhancing the metabolism of steroid hormones with simultaneous admission Hypericum perforatum, barbiturates, carbamazepine, phenytoin, sulfonamides, pyrazolone derivatives, rifampicin.

    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.

    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.

    When taking hypoglycemic medicines at the same time, you may need to adjust the dose of the latter.

    Special instructions:

    It is necessary to observe the gynecologist at the time of taking the drug.

    Oral contraceptives do not protect against 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.

    Efficiency decreases with the regular use of ethanol.

    Impact on the ability to drive vehicles and manage mechanisms

    Not found.

    Instructions
    Up