Etonogestrel + Ethinylestradiol (Aetonogestrelum + Aethinyloestradiolum)

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
  • NovaRing®
    implant the vagina. 
    Organon, N.V.     Netherlands
    • АТХ:

    G.02.B.B.01   Intravaginal ring with progestogen and estrogen

    Pharmacodynamics:

    Hormonal combination (estrogen-progestin) means low-dose sustained release contraceptive for vaginal use.

    Reduced serum levels of LH and FSH (a sharp decrease in the pulse frequency of GnRH secretion, reduced sensitivity to GnRH pituitary, direct inhibition of pituitary FSH secretion of estrogen), disappears lift LH at mid-cycle, reduced synthesis of endogenous estrogen and progesterone inhibited ovulation.

    It prevents the release of an egg from the ovary (ovulation) and thus prevents the occurrence of pregnancy violates the promotion of sperm into the fallopian tube, causing the formation of thick sticky mucus glands of the cervix, which hinders the passage of sperm on the female sexual ways.

    Along with contraceptive action normalizes the menstrual cycle, which becomes more regular menses occur less painful, less bleeding intensity; reduces the risk of developing endometrial cancer and ovarian cancer.

    Pharmacokinetics:

    Etonogestrel

    Absorption of etonogestrel is 100% (with intravaginal application). Relationship with plasma proteins 98%. Biotransformation occurs in the liver (CYP3A4). Half-life 29.3 hours. Creatinine clearance 0.81 ml / min. Elimination by the kidneys and with feces.

    Ethinylestradiol

    Ethinyl estradiol, released from the vaginal ring, is rapidly absorbed through the mucous membrane of the vagina. Absolute bioavailability is approximately 56% and is comparable to that for oral administration of ethinylestradiol. It binds to serum albumin. Apparent volume of distribution is about 15 l / kg. Metabolized by aromatic hydroxylation. During its biotransformation, a large number of hydroxylated and methylated metabolites are formed which circulate both in the free state and in the form of glucuronide and sulfate conjugates. The apparent clearance is approximately 3.5 l / h.

    The concentration of ethinylestradiol in blood plasma is reduced in two phases. Half-life in the terminal phase varies widely; median is about 34 hours. Ethinylestradiol not output in unmodified form; its metabolites are excreted by the kidneys and through the intestine in a ratio of 1.3: 1. Half-life metabolites is about 1.5 days.

    Indications:

    Contraception in women.

    ICD-10

    XXI.Z30-Z39.Z30   Monitoring the use of contraceptives

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

    Contraindications:

    Hypersensitivity, thrombosis (including deep vein thrombosis, pulmonary thromboembolism, myocardial infarction, stroke), angina pectoris, transient circulatory disorders, diabetic angiopathy, liver disease, pancreatitis, migraine with focal neurological symptoms, hormone-dependent malignant tumors, liver tumors (including number in the anamnesis), vaginal bleeding of unclear etiology, pregnancy (including presumed etiology), lactation period.

    Carefully:

    Diabetes mellitus, obesity, arterial hypertension, arrhythmia, valvular heart disease, Crohn's disease, ulcerative colitis, sickle cell disease, systemic lupus erythematosus, hemolytic-uremic syndrome, epilepsy, smoking in combination with the age of more than 35 years, prolonged immobilization,extensive surgical interventions, fibrocystic mastopathy, uterine fibroids, congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson syndrome and Rotor syndrome), conditions complicating the use of the vaginal ring (prolapse of the cervix, bladder hernia, rectal hernia, severe chronic constipation).

    Pregnancy and lactation:

    Action category for the fetus by FDA - X.

    In the absence of two consecutive menstrual cycles, you should cancel the appointment and exclude pregnancy. If the scheme of taking the drug is violated, pregnancy should be excluded after the first absent cycle. After the withdrawal of funds in order to attempt to become pregnant, you should take a break for 1-2 months or wait for regular menstruation.

    Penetrates into breast milk. Contraindicated in the period of breastfeeding (to begin therapy after the establishment of lactation).

    Dosing and Administration:

    Intravaginal. To achieve a contraceptive effect, the ring is inserted into the vagina and left for 3 weeks. Then the ring is removed from the vagina and take a break for 1 week. The ring may fall out of the vagina if improperly inserted or when the tampon is removed (in this case, rinse the ring with warm water and re-insert it).If in the previous cycle a combined oral contraceptive was used, calculated for 21 days of administration, then the drug should be administered the day after the last pill; if the contraceptive is designed for 28 days of admission, there should not be a break between its use and the use of this drug. The transition from contraceptives containing only gestagens in the form of mini-saws, can be carried out any day. Transition from the implant or progestagen-releasing intrauterine contraceptives is carried out from the day they are removed, and from the injection drug - the day the next injection is needed.

    In all cases it is necessary to use an additional barrier method of contraception during the first 7 days of using the ring. If the ring was temporarily removed from the vagina for a period of up to 3 hours, the contraceptive effect does not subside, if more than 3 hours, the effect can be reduced, so an additional barrier method of contraception must be used for the next 7 days. If the ring was removed more than 3 hours during the last third week of use, its use should be extended beyond 3 weeks (within 7 days of its reintroduction into the vagina).When the ring is in the vagina for more than 3 weeks, but less than 4 weeks, you should take a week break, and then put a new ring in the vagina. If the ring is in the vagina for more than 4 weeks, the contraceptive effect may be weakened and pregnancy should be excluded before applying the new ring. To change the time of onset of menstruation shorten the break in using the ring for the required number of days. If the interval in application of the ring is too short, bleeding "cancellation" may not occur, but "smearing" discharge or bleeding from the vagina appears during the use of the next ring. To skip one menstruation, you must start using a new ring without a one-week break. The next ring should be used for 3 weeks. In this case, there may be "smearing" discharge or bleeding from the vagina. After a week's break, the woman returns to a regular schedule of using the drug.

    Side effects:

    From the side nervous system: headache, migraine, emotional lability.

    From the side genitourinary system: a feeling of discomfort in the vagina, vaginitis, cervicitis, cystitis, urinary tract infections, painful menstruation; tenderness, tension, enlargement of the mammary glands; a decrease in sexual desire, the sensation of a foreign body in the vagina, and coital discomfort.

    Other: allergic reactions, acne, weight change, nausea, abdominal pain.

    Overdose:

    Nausea, vomiting. Treatment is symptomatic.

    Interaction:

    Amoxicillin, ampicillin, benzylpenicillin, doxycycline, tetracycline - a decrease in the effectiveness of oral contraceptives.

    Anticoagulants, derivatives of coumarin and indanedione - there may be a multidirectional change in the activity of anticoagulants.

    Ascorbic acid, paracetamol - an increase in the concentration of estrogens, possibly due to inhibition of conjugation.

    Atorvastatin - an increase in the concentration of estrogens.

    Hepatotoxic drugs - increased toxicity due to activation of hepatic blood flow by estrogens.

    Glucocorticoids - a decrease in their metabolism, an increase in the synthesis of transcortin.

    Benzodiazepines, caffeine - inhibition of the metabolism of benzodiazepines, caffeine.

    Clofibrate - a decrease in the effectiveness of clofibrate.

    Tobacco smoking is a possible reduction in the concentration of estrogens (induction of microsomal liver enzymes), an increased risk of cardiovascular disease.

    Ritonavir - decrease in the concentration of estrogens.

    Sugar-reducing drugs taken inwards, insulin - a decrease in hypoglycemic action, an increase in glucose tolerance, especially in individuals with diabetes mellitus.

    Means that induce microsomal enzymes of the liver (especially barbiturates, carbamazepine, griseofulvin, phenytoin, primidon, rifabutin, rifampicin) - decreased activity of oral contraceptives.

    Tamoxifen - a decrease in its anti-estrogenic activity.

    Tricyclic antidepressants, neuroleptics - increased risk of motor disorders, sometimes chorea, increased risk of increasing the concentration of antidepressants.

    Cyclosporine - an increase in its plasma concentration.

    Special instructions:

    The drug does not protect against infection, including from HIV infection and other sexually transmitted diseases.

    Sometimes, during the period of the ring in the vagina, irregular vaginal bleeding may occur.In this case, you should continue to use the ring in normal mode. If the bleeding increases, continues or recurs, you should consult your doctor.

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