Indications for use
Mechanism of action
Drospirenone is a gestagen-only drug. In a therapeutic dose, drospirenone also has antiandrogenic and weak antimineralocorticoid activity. Drospirenone is devoid of any estrogenic, glucocorticoid and antiglucocorticoid activity, which provides a pharmacological profile very close to the profile of the natural hormone progesterone. In clinical studies, data have been obtained indicating that weak antimineralocorticoid properties contribute to a slight antimineralocorticoid effect. Due to its small antimineralocorticoid activity, drospirenone increases the activity of renin and aldosterone in blood plasma.
Mode of application and dose
Take 1 pill of Drospirenone daily. The pack contains 24 active and 4 inactive pills. The pill should be taken at one and the same time. Take 1 pill of the this birth control drug washing it down with water. There is no break. When taking the latest 4 pills, menstruation will start.
Contraindications for the use of the combination of drospirenone are:
- the presence of risk factors for venous thromboembolism;
- the presence of risk factors for arterial thromboembolism development;
- severe liver disease (including history) to normalize liver function indices;
- a tumor of the liver (including a history);
- severe chronic renal failure or acute renal failure;
- diagnosed or suspected hormone-dependent malignant tumors (including genitals or mammary glands);
- vaginal bleeding of unknown etiology;
- Infectious and parasitic diseases: rarely – candidiasis.
- The hemopoietic system: rarely – anemia, thrombocytosis.
- The immune system: rarely – allergic reactions; frequency unknown – hypersensitivity reactions.
- The endocrine system: rarely – endocrine disorders.
- The side of metabolism: rarely – hyperkalemia, hyponatremia.
- Mental disorders: often – emotional lability; infrequently – depression, nervousness, decreased libido, drowsiness; rarely – anorgasmia, insomnia.
- The nervous system: often – headache; infrequently – dizziness, paresthesia, migraine; rarely – vertigo, tremor.
- The side of the organ of vision: rarely – conjunctivitis, dry eye syndrome, eye disease.
- The cardiovascular system: infrequently – varicose veins, arterial hypertension; rarely – tachycardia, venous thromboembolism (VTE), arterial thromboembolism (ATE), phlebitis, vascular disease, fainting, nosebleeds.
- The digestive system: often – nausea; infrequently – abdominal pain, vomiting, dyspepsia, bloating, gastritis, diarrhea; rarely – bloating, gastrointestinal upset, a feeling of fullness, abdominal hernia, candidiasis of the oral cavity, constipation, dry mouth.
- The liver and biliary tract: rarely – pain in the gallbladder, cholecystitis.
- The skin and subcutaneous tissue: infrequently – acne, itching, rash; rarely – chloasma, eczema, alopecia, acne dermatitis, dry skin, erythema nodosum, hypertrichosis, skin diseases, skin striae, contact dermatitis, photodermatitis, skin nodules; frequency unknown – erythema multiforme.
- The musculoskeletal system: infrequently – back pain, pain in the limbs, muscle cramps.
- The reproductive system and the mammary gland: often – pain in the mammary glands, metrorrhagia, amenorrhea; infrequently – vaginal candidiasis, pelvic pain, breast enlargement, fibrocystic mastopathy, uterine/vaginal bleeding, vaginal discharge, flushing, vaginitis, menstrual irregularities, dysmenorrhea, hypomenorrhea, menorrhagia, dryness of the vaginal mucosa; rarely – dyspareunia, vulvovaginitis, postcoital bleeding, withdrawal bleeding, breast cysts, breast hyperplasia, neoplasms in the mammary gland, cervical polyps, endometrial atrophy, ovarian cysts, uterus enlargement.
- General disorders: infrequently – asthenia, increased sweating, edema (generalized edema, peripheral edema, facial edema), weight gain; rarely – general malaise, weight loss.
The main metabolites of drospirenone in human blood plasma are formed without the involvement of enzymes of the cytochrome P450 system. Thus, inhibitors of this enzyme system do not affect the metabolism of drospirenone.
Based on the results of in vitro inhibition studies and in vivo interaction studies in female volunteers taking omeprazole, simvastatin and midazolam as substrate markers, the effect of 4 mg drospirenone on the metabolism of other active substances is unlikely.
In patients with normal renal function, the simultaneous use of drospirenone and an ACE inhibitor or NSAIDs does not significantly affect the serum potassium content.
What if I miss a dose?
Drospirenone and pregnancy
It is contraindicated for use during pregnancy but it is possible to use this drug during lactation.