Norethisterone (Norethisteronum)

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

"Estrogens, gestagens, their homologues and antagonists"

Included in the formulation
  • Norkolut
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    G.03.D.C.02   Norethisterone

    Pharmacodynamics:

    Binding to Progesterone A and B Receptors: Detachment from Heat Shock Protein Receptors Hsp90, Hsp70 and FKBP4, phosphorylation of receptors with the formation of homo- and heterodimers, selectively reacting with progesterone-sensitive regulatory elements of target genes. Activating transcription by attracting co-activators (NCOA1 and NCOA2) and by direct interaction with common transcription factors (TFIIB). The receptor complex with coactivators attach additional proteins (CREB1 and EP300), acetylating histones. As a result of chromatin rearrangement, access to the proteins of the transcription apparatus (primarily RNA polymerase II) is facilitated, access to the promoter. Activation of A-receptor - blockade of transcription of target genes activated by receptors of other steroid hormones (estrogens, glucocorticosteroids, aldosterone and androgens) and B-receptors of progestogens. Activation of the B-receptor is the stimulatory effects of progestogens. Binding to membrane progesterone receptors in spermatozoa.

    Causes transformation of the mucous membrane of the uterus from the proliferation phase to the secretory phase,and after fertilization promotes its transition to a state favorable for the development of a fertilized egg. Has weakly expressed estrogenic and androgenic properties. Reduces the excitability and contractility of the musculature of the uterus, stimulates the development of the end elements of the breast.

    Pharmacokinetics:

    When ingestion is well absorbed from the digestive tract. The maximum concentration of active substance in the plasma is observed after 1-2 hours. The half-life period is 2.8-10 hours. 50-70% is excreted by the kidneys, 20-40% by the intestine.

    Indications:

    Premenstrual syndrome. Dysfunctional uterine bleeding, dysmenorrhea, algomenorrhea, amenorrhea, endometriosis, fibroids, endometrial cancer, mastodynia, mastopathy. Infertility, miscarriage. Contraception. Menopause. Diagnostic progesterone test. Cessation and prevention of lactation.

    ICD-10

    II.C51-C58.C54.1   Malignant neoplasm of endometrium

    II.D10-D36.D25   Leiomyoma of the uterus

    II.D10-D36.D26   Other benign neoplasms of the uterus

    XIV.N60-N64.N60   Benign breast dysplasia

    XIV.N60-N64.N64.4   Mammalgia

    XIV.N60-N64.N64.9   Disease of mammary gland, unspecified

    XIV.N80-N98.N80   Endometriosis

    XIV.N80-N98.N80.0   Endometriosis of the uterus

    XIV.N80-N98.N85.0   Glandular endometrial hyperplasia

    XIV.N80-N98.N91   Absence of menstruation, meager and rare menstruation

    XIV.N80-N98.N93   Other abnormal bleeding from the uterus and vagina

    XIV.N80-N98.N93.9   Abnormal uterine and vaginal bleeding, unspecified

    XIV.N80-N98.N94.3   Premenstrual tension syndrome

    XIV.N80-N98.N94.4   Primary dysmenorrhea

    XIV.N80-N98.N94.5   Secondary dysmenorrhea

    XIV.N80-N98.N94.6   Dysmenorrhea, unspecified

    XIV.N80-N98.N95.1   Menopause and menopause in women

    XIV.N80-N98.N95.3   Conditions associated with artificially induced menopause

    XIV.N80-N98.N95.9   Menopausal and premenopausal disorders, unspecified

    XIV.N80-N98.N97   Female infertility

    XV.O20-O29.O26.2   Medical care for a woman with a habitual miscarriage of pregnancy

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

    Contraindications:
    • Cirrhosis of the liver.
    • Cholestatic jaundice in pregnancy in anamnesis.
    • Tendency to thrombosis.
    • Benign hyperbilirubinemia.
    • Neoplasms of mammary glands and genitals.
    • Acute liver diseases (including benign and malignant neoplasms).
    • Impaired liver and kidney function.
    • Pregnancy (including the suspect).
    • The period of puberty.
    • Acute thrombophlebitis or thromboembolism.
    • Bleeding from the urinary tract is of unknown origin.
    • Bleeding from the genital tract is of unknown origin.
    • Hypersensitivity.
    • Obesity.
    • Herpes.
    Carefully:

    Bronchial asthma, chronic heart failure, epilepsy, hypertension, migraine, renal failure, seizures or other abnormalities of the central nervous system (including history), diabetes mellitus, liver disease (including history), hyperlipidemia, thrombophlebitis and thromboembolism ( including in the anamnesis).

    With caution combine the drug with oral anticoagulants, hypoglycemic agents, glucocorticosteroids.

    Pregnancy and lactation:

    Category FDA - X. Do not use during pregnancy, virilization of female fetuses is possible. Penetrates into breast milk. Depending on the type and dose, it can increase, decrease or not change the quality and quantity of milk. It is not recommended to use high doses during lactation.

    Dosing and Administration:

    The dosage regimen is set individually by the attending physician, the daily dose is 350 μg-30 mg.

    Inside. With premenstrual syndrome, mastalgia, dysmenorrhea: from the 16th to the 25th day of the menstrual cycle, 5-10 mg per day in combination with estrogens.

    With dysfunctional uterine bleeding, cystic glandular hyperplasia of the endometrium: to stop bleeding - 5-10 mg per day for 6-12 days; to prevent bleeding - 5-10 mg per day from the 16th to the 25th day of the cycle for 6 months.

    To stop lactation: the first 3 days - 20 mg per day, then 4 days - 15 mg, then 3 more - 10 mg.

    Contraception: 1,25-2,5 mg per day from the 1st-5th day of the menstrual cycle for 21 days (in combination with ethinylestradiol), then break for 7 days.

    Side effects:

    On the part of the endocrine system: engorgement of the mammary glands, uterine bleeding, weight gain.

    From the nervous system: increased fatigue, paresthesia.

    From the digestive system: vomiting, nausea.

    From the side of metabolism: peripheral edema.

    Others: itching, rash, melasma, chloasma.

    Overdose:

    Nausea, vomiting, vaginal bleeding. Treatment is symptomatic.

    Interaction:

    Barbiturates, hydantoins, rifampicin reduce the effect of the drug.

    Special instructions:

    Impact on the ability to drive vehicles and manage mechanisms.

    Does not affect the ability to drive and machinery.

    Instructions
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