Indications for use
Mechanism of action
Ella is a synthetic selective modulator of progesterone receptors, characterized by a tissue-specific partial antiprogesterone effect. Ulipristal has a direct effect on the endometrium. It change the endometrium. These changes are associated with an antagonistic effect on progesterone receptors. As a rule, histological changes are represented by an inactive and weakly proliferating epithelium, accompanied by asymmetry of stroma and epithelial growth, expressed by cystic expansion of the glands with mixed estrogenic (mitotic) and progestagenic (secretory) effects on the epithelium.
Mode of application and dose
Ulipristal can be used for as long as 5 days (120 hours) after unprotected intercourse, which significantly increases positive outcome. As early you take this emergency contraceptive, as effective it will be.
- Vaginal bleeding of unknown etiology or for reasons not related to uterine myoma;
- Uterine, cervix, ovary, or breast cancer;
- Bronchial asthma (severe, not amenable to correction by oral corticosteroids);
- Children and adolescents under 18 years of age;
- Hypersensitivity to ulipristal.
- Mental health: often – emotional disorders; infrequently – anxiety.
- Nervous system: often – headache; infrequently – dizziness.
- Side of metabolism: infrequently – weight gain.
- Side of the organ of hearing and balance: often – vertigo.
- The respiratory system: infrequently – nosebleeds.
- The digestive system: often – abdominal pain, nausea; infrequently – dyspepsia, dry mouth, flatulence, constipation.
- The skin and subcutaneous tissue: often – acne, excessive sweating; infrequently – skin lesions.
- The musculoskeletal system: often – pain in the bones and muscles; infrequently – back pain.
- The urinary system: infrequently – urinary incontinence.
- The reproductive system and mammary glands: very often – amenorrhea, thickening of the endometrium, hot flashes; often – metrorrhagia, ovarian cyst, tension/tenderness of the mammary glands, pelvic pain; infrequently – rupture of an ovarian cyst, vaginal discharge, discomfort in the area of the mammary glands.
- The body as a whole: often – edema, increased fatigue; infrequently – asthenia.
- Laboratory indicators: often – an increase in the concentration of cholesterol in the blood; infrequently – an increase in the concentration of triglycerides in the blood.
Ulipristal has a steroidal structure and acts as a selective modulator of progesterone receptors with a predominant inhibitory effect on progesterone receptors. Thus, hormonal contraceptives and progestogens can reduce the effectiveness of ulipristal acetate by competing on the progesterone receptor. Therefore, the simultaneous use of drugs containing gestagens is not recommended.
Ulipristal may inhibit the action of hormonal contraceptives (gestagen-containing tablets only, gestagen-releasing systems or combined oral contraceptives) and gestagen drugs used for other indications. Therefore, the concomitant use of drugs containing gestagen is not recommended. Gestagen-containing drugs should not be used within 12 days after withdrawing treatment with ulipristal acetate.
After the use of a moderate inhibitor of the isoenzyme CYP3A4 erythromycin propionate (500 mg 2 times / day for 9 days) in healthy female volunteers, the Cmax and AUC of ulipristal acetate increased by 1.2 and 2.9 times, respectively; the AUC of the active metabolite of ulipristal acetate increased by 1.5 times, while the Cmax of the active metabolite decreased (by 0.52 times). The combined use of potent inhibitors of the isoenzyme CYP3A4 (ketoconazole, ritonavir, nefazodone) can lead to a greater increase in the concentration of ulipristal acetate in the blood plasma. Dose adjustment when using ulipristal in patients taking weak inhibitors of the CYP3A4 isoenzyme is not required. The combined use of moderate or potent inhibitors of the CYP3A4 isoenzyme with ulipristal is not recommended.
In patients receiving inducers of the isoenzyme CYP3A4, a decrease in the concentration of ulipristal acetate in the blood plasma may be observed. The combined use of ulipristal acetate and powerful inducers of the CYP3A4 isoenzyme (rifampicin, carbamazepine, phenytoin, preparations of St. John’s wort perforated) is not recommended.
In vitro data show that in clinically significant concentrations of ulipristal during absorption in the gastrointestinal wall may be a P-gp inhibitor. Thus, the concomitant use of ulipristal can increase the concentration of other drugs – P-gp substrates in blood plasma. In the absence of clinical data, the simultaneous use of ulipristal and P-gp substrates (dabigatran etexilate, digoxin) is not recommended.
What if I miss a dose?
Ella and pregnancy
Use during pregnancy and lactation is contraindicated. Before treatment, pregnancy should be excluded.