Emergency contraceptive. Synthetic, selective Progesterone receptor modulator with high affinity for this receptor. When used as emergency contraception, the mechanism of action is to inhibit or delay ovulation by stopping the ejection of the lutidizing hormone (LH). Pharmacodynamic data show that even immediately before expected ovulation (when the LH level starts to increase), ulipristal acetate is able to delay follicular cracking for at least 5 days in 78.6% of cases. The drug has minimal affinity for the androgen receptor and has no affinity for the estrogen and mineralocorticoid receptor. The drug is quickly absorbed from the digestive tract, reaching Cmax about 1 hour after administration. Adopting a preparation with a high-fat food leads to a 45% reduction in Cmax, T elongationmax and up to a 25% increase in AUC compared to administration on an empty stomach. Ulipristal acetate binds to a high degree (> 98%) to plasma proteins such as albumin, alpha-1 acid glycoproteins and high density lipoproteins. It is subject to intense metabolism to metabolites: mono-demethylated (pharmacologically active) and di-methylated and hydroxylated. Metabolism occurs mainly via CYP3A4 and to a small extent CYP1A2 and CYP2D6. T0,5 in the blood is 32.4 ± 6.3 h.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients.
Precautions:
The preparation is intended for use in sporadic cases. Under no circumstances should it replace the constant method of contraception. The tablet is not intended for use during pregnancy and should not be taken by women who suspect that they are pregnant or aware of being pregnant. The preparation does not, however, break the existing pregnancy. The preparation does not always prevent pregnancy. In the case of delay in the onset of menstruation by more than 7 days, abnormal menstrual cycle or the occurrence of pregnancy symptoms, or in case of doubt, a pregnancy test should be performed. As with any pregnancy, the possibility of an ectopic pregnancy should be considered. It is important to know that uterine bleeding does not rule out an ectopic pregnancy. Women who become pregnant after taking the tablet should contact their doctor. The tablets inhibit or delay ovulation. If ovulation has already occurred, the preparation is not effective. It is not possible to predict the time of ovulation and therefore the tablet should be taken immediately after sexual intercourse without protection. There are no data on the efficacy of the preparation taken later than 120 h (5 days) after unprotected intercourse. Limited and inconclusive data suggest that the efficacy of the tablet may be reduced in the event of weight gain or body mass index (BMI). In all women, if an unprotected sexual intercourse occurs, urgent contraception should be used immediately in emergencies, regardless of the woman's weight or BMI. After taking the tablet, menstrual bleeding may occur a few days earlier or later than expected. Co-administration of ulipristal acetate and immediate contraceptives containing levonorgestrel is not recommended. The use of the preparation is a method of emergency contraception, which reduces the risk of pregnancy after sexual intercourse without protection, but does not ensure contraception in the event of subsequent sexual intercourse. Therefore, after using contraception in emergency cases, it is recommended to secure using a reliable mechanical method until the beginning of the Next menstrual cycle.Although the use of a tablet does not constitute a contraindication to continuation of permanent hormonal contraception, the preparation may reduce its contraceptive effect. Therefore, if a woman wants to start or continue hormonal contraception, she can do it immediately after applying the preparation, but she should use a reliable mechanical method for the next menstrual cycle. It is not recommended for use in women suffering from severe asthma treated with oral glucocorticosteroid. Due to the lack of appropriate tests, it is not recommended for patients with severe hepatic impairment. The preparation is not used in children before puberty. The tablets are suitable for women of childbearing age, including adolescents. There were no differences in safety or efficacy compared to adult women aged 18 or over. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation is not indicated for use during pregnancy and should not be taken by women if pregnancy or pregnancy is suspected. The preparation does not break the existing pregnancy. After taking the preparation, you may occasionally get pregnant. Although no teratogenic effects have been observed, the results of animal studies are insufficient to assess reproductive toxicity. The limited amount of data on the risk of exposure of a pregnant woman to the use of the preparation does not suggest a safety risk. Ulipristal acetate is excreted in human milk. Influence / infants have not been studied. A danger to a breastfed child can not be excluded. After taking the product, breast-feeding is not recommended for 1 week. During this time, it is recommended to suck and discard milk to stimulate lactation. Rapid return of fertility is likely after the preparation for immediate contraception. Women should be advised of the need to use a reliable mechanical method of contraception for all subsequent sexual intercourses until the next menstrual cycle occurs.
Side effects:
Common: mood disorders, headache, dizziness, nausea, abdominal pain, discomfort in the abdomen, vomiting, muscular pains, back pain, dysmenorrhea, pelvic pain, breast sensitivity, fatigue. Uncommon: influenza, appetite disorders, emotional disturbances, anxiety, insomnia, excessive mobility, changes in libido, drowsiness, migraine, visual disturbances, diarrhea, dry mouth, indigestion, bloating, acne, skin changes, pruritus, excessive menstrual bleeding, vaginal discharge, menstrual disorders, intermenstrual bleeding, vaginitis, hot flushes, premenstrual syndrome, chills, malaise, fever. Rare: confusion, tremor, attention deficit, taste disturbance, unusual feeling in the eye, eye congestion, photophobia, labyrinth-like dizziness, dry throat, urticaria, pruritus, dyspareunia, ovarian cyst rupture, vaginal and vulvar pain, miserly and short-lasting menstruation, thirst. After taking the tablet, menstrual bleeding may occur a few days earlier or later than expected. About 7% of women had menstrual bleeding more than 7 days earlier than expected. About 18.5% of women had a delay in menstrual bleeding by more than 7 days, and in 4% of women the delay was above 20 days. In women under the age of 18, the safety profile of the preparation was similar to that of adult women.
Dosage:
Orally. One table should be accepted as soon as possible. not later than 120 hours (5 days) after unprotected sexual intercourse or if the method of contraception has failed. The tablet can be taken on any day of the menstrual cycle. If vomiting occurs within 3 hours after taking the tablet, take another tablet. In the event of a delay in the menstrual cycle or in case of pregnancy symptoms, pregnancy should be ruled out before taking the tablet. No need to change the dosage in patients with impaired renal function. Due to the lack of appropriate studies, alternative doses of the preparation can not be established in patients with impaired hepatic function.Use in patients with severe hepatic impairment is not recommended. The tablet can be taken with or without food.
(C)
