Desogestrel + Ethinylestradiol (Desogoestrelum + 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
  • Benidette
    pills inwards 
    Actavis PTS ehf Group     Iceland
  • Daisy-30
    pills inwards 
    Fami Ker Limited     India
  • Marvelon®
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    Organon, N.V.     Netherlands
  • Mersilon®
    pills inwards 
    Organon, N.V.     Netherlands
  • MODELL® OBULE
    pills inwards 
    Actavis PTS ehf Group     Iceland
  • Novinet®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Regulon
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Tri-Mercy®
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    Aspen Pharma Trading Limited    
    • АТХ:

    G.03.A.A   Progestogens and estrogens (fixed combinations)

    G.03.A.A.09   Desogestrel and ethinyl estradiol

    Pharmacodynamics:

    It leads to a decrease in serum concentrations of follicle-stimulating and luteinizing hormone, suppresses ovulation, increases the viscosity of the secretion of the cervix, disrupts the progression of sperm through the fallopian tube, causes the restructuring of the endometrium, which complicates the implantation of a fertilized egg.

    Pharmacokinetics:

    Desogestrel

    Fast and complete absorption, bioavailability - 70%, almost completely binds to plasma proteins. Rapidly metabolized in the intestinal wall and in the liver with the formation of an active metabolite (ethonogestrel). Half-life is 30 hours.Eliminated by the kidneys and through the gastrointestinal tract.

    Ethinylestradiol

    Quickly and completely absorbed from the gastrointestinal tract. The maximum concentration in the blood serum is achieved in 1-2 hours, bioavailability is 60%. It binds to plasma proteins by 97.5%. Metabolised in the liver and intestine to etonogestrel. The elimination half-life is 24 hours. Eliminated by the kidneys by 45% and the gastrointestinal tract by 30%. The half-life of metabolites is approximately 1 day.

    Indications:

    Contraception.

    ICD-10

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

    Contraindications:

    - Venous or arterial thrombosis;

    - Precursors of thrombosis (including a transient attack of coronary heart disease, angina pectoris);

    - The presence of severe or multiple risk factors for venous or arterial thrombosis (including arterial hypertension with arterial pressure 160/100 mm Hg and above);

    - Thromboembolism;

    - Embolism of the pulmonary artery;

    - Pancreatitis;

    - Hormone-dependent malignant neoplasms of genital organs or mammary glands (including suspected);

    - Vaginal bleeding of unclear etiology;

    - Pregnancy, breast-feeding;

    - Migraine;

    - Smoking over the age of 35 (more than 15 cigarettes a day);

    - Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

    - Hypersensitivity;

    - Diabetes;

    - Severe liver disease (before the normalization of liver function), including in history;

    - Tumors of the liver.

    Carefully:

    Diseases of the gallbladder and liver; depression; epilepsy; ulcerative colitis; tuberculosis; adolescence; uterine myoma; age over 35 years; presence of thromboembolic diseases in a family history (venous or arterial thrombosis / thromboembolism in brothers, sisters or parents at a relatively early age); obesity; dyslipoproteinemia; arterial hypertension; valvular heart disease; atrial fibrillation; long-term immobilization; extensive surgical intervention; surgical intervention on the lower limbs; severe trauma; phlebeurysm; superficial thrombophlebitis; the postpartum period; changes in biochemical parameters that may be markers of a congenital or acquired predisposition to venous or arterial thrombosis; systemlupus erythematosus; hemolytic-uremic syndrome; sickle-cell anemia.

    Pregnancy and lactation:

    Category FDA - X. In case of pregnancy, stop taking the drug. The drug can affect lactation, as combined oral contraceptives reduce the amount and change the composition of breast milk. Therefore, the drug is not recommended until the breast feeding mother completely stops breastfeeding. A small number of contraceptive steroids and / or their metabolic products can be excreted in breast milk.

    Dosing and Administration:

    Tablets should be taken orally in the order given on the package, every day at approximately the same time, with a small amount of water, if necessary.

    Orally 1 tablet (20 mcg ethinyl estradiol and 150 μg desogestrel) per day from the first day of the cycle. Admission for 21 days, then a break for 7 days, after which the drug is repeated.

    Side effects:

    From the immune system: hypersensitivity.

    From the side of metabolism and nutrition: weight gain, fluid retention, and rarely weight loss.

    From the nervous system: headache, migraine, decreased libido, depression, mood swings, minor chorea, sometimes increased libido.

    From the side of the organ of vision: intolerance to contact lenses.

    From the digestive system: nausea, vomiting, abdominal pain, diarrhea, ulcerative colitis, cholelithiasis, Crohn's disease.

    From the skin and subcutaneous tissues: skin rash, hives, herpes, erythema nodosum, erythema multiforme, chloasma.

    On the part of the reproductive system: pain in the chest, tenderness of the mammary glands, enlargement of the mammary glands, discharge from the vagina, discharge from the mammary glands, intermenstrual bloody discharge.

    Other: thrombosis / thromboembolism, increased blood pressure, porphyria, hearing loss.

    Overdose:

    Vomiting, nausea, in young girls - spotting from the vagina. Treatment is symptomatic.

    There were no serious complications with drug overdose.

    Interaction:

    The interaction between oral contraceptives and other drugs can lead to acyclic bleeding and / or a decrease in the effectiveness of contraceptives.

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

    Amoxicillin, benzylpenicillin, doxycycline, tetracycline, ampicillin - reduce the effectiveness of the drug.

    Anticoagulants - a change in their activity.

    Atorvastatin - an increase in the concentration of estrogens.

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

    Sugar reduction drugs (insulin, drugs taken orally) increase glucose tolerance, especially in patients with diabetes mellitus.

    Benzodiazepines, caffeine - inhibition of their metabolism.

    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.

    Clofibrate - a decrease in its effectiveness.

    Smoking is a possible reduction in the concentration of estrogens (induction of microsomal liver enzymes), an increased risk of developing cardiovascular diseases.

    Ritonavir - decrease in the concentration of estrogens.

    Tamoxifen - a decrease in its anti-estrogenic activity.

    Tricyclic antidepressants, neuroleptics - increased risk of motor disorders, chorea (rarely), increased risk of increasing the concentration of antidepressants.

    Cyclosporine - an increase in its plasma concentration.

    Special instructions:

    Before starting the drug, and every six months, a gynecologist's consultation and a general medical examination are necessary. In the case of acute liver disease, the drug can be administered only after the liver has been completely normalized.

    Impact on the ability to drive vehicles and manage mechanisms

    Effects of the drug on the ability to drive vehicles and work with mechanisms are not noted.

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