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Ulipristal acetate is used for emergency contraception or treatment of uterine fibroids. The drug can have some potential side effects, so during the use of Ulipristal, patients need to strictly follow the instructions on the dose and time to take the drug as indicated.
1. What is Ulipristal acetate?
Ulipristal acetate is known as a selective progesterone receptor modulator, indicated for use in emergency contraception or treatment of uterine fibroids in women. Ulipristal serves as a derivative of 19-nor progesterone, with antagonistic agonist activity, commonly associated with glucocorticoids.Compared with Mifepristone (progesterone receptor antagonist), Ulipristal acetate is more easily tolerated, has better binding affinity and has lower glucocorticoid activity. Currently, Ulipristal acetate is recommended as first-line therapy for emergency contraception because its effectiveness is similar to that of the traditional Yuzpe regimen or the use of Levonorgestrel.
Ulipristal birth control pills are made in the form of tablets with a strength of 5mg or 30mg, containing the main active ingredient, Ulipristal and other excipients just enough.
2. Indications and uses of Ulipristal
2.1. Indications for use of the drug Ulipristal acetate Ulipristal acetate is usually indicated for use in the following cases:
Emergency contraception within 120 hours of unprotected sex or contraceptive failure (suspected) / known). However, Ulipristal is not intended for long-term contraception. Indicated for the preoperative treatment of moderate to severe symptoms of uterine fibroids in women of childbearing age. Indicated for the serial treatment of symptoms of moderate to severe uterine fibroids in women of childbearing age who have not responded to surgical treatment. 2.2. Uses of the drug Ulipristal acetate *Pharmacodynamics
The active ingredient Ulipristal has the ability to inhibit progesterone from binding to its receptors. Thanks to the mechanism of normal endometrial turnover, this active ingredient helps to delay ovulation by preventing rupture of the follicle and reducing the possibility of implantation. Besides, Ulipristal also has the ability to inhibit cell proliferation and apoptosis, thereby significantly reducing the size of uterine fibroids.
*Pharmacokinetics
Absorption: The active ingredient Ulipristal is rapidly absorbed from the gastrointestinal tract, taking approximately 1 hour after oral administration to reach peak plasma concentrations. Distribution: Over 98% of Ulipristal is bound to plasma proteins, to some extent to α1-acid glycoprotein, HDL cholesterol, LDL and albumin. Metabolism: Ulipristal is metabolised largely by the enzyme CYP3A4 and to a lesser extent by the enzyme CYP2D6, CYP1A2. In the body, the active ingredient Ulipristal will be converted to mono-demethylated and di-demethylated. Elimination: Ulipristal is eliminated mainly in the faeces and about 10% in the urine. Ulipristal has a terminal half-life of approximately 32–38 hours, with the metabolite taking approximately 27 hours. 2.3. Contraindications to the use of Ulipristal acetate The following are contraindications to the use of Ulipristal acetate, including:
Patients who are allergic to Ulipristal or hypersensitive to other active ingredients contained in the drug. Ulipristal is contraindicated for pregnant women, nursing mothers. Ulipristal should not be used in women with unexplained vaginal bleeding or causes other than uterine fibroids. The drug is contraindicated in women with cancer of the uterus, breast, ovaries or cervix. Ulipristal should not be used by women who have not had a period or have gone through menopause. People with underlying liver dysfunction should also avoid using Ulipristal.
3. Dosage, use and treatment of drug overdose Ulipristal acetate
3.1. Dosage and use of the drug Ulipristal acetate Ulipristal acetate is prepared in the form of tablets, so patients should take the drug orally with a sufficient amount of filtered water. Depending on the purpose of use of the drug, the dose of Ulipristal acetate will be determined in detail below:
Dose of emergency contraception: Take 30mg of Ulipristal as soon as possible after unprotected sex or contraception. failure (preferably within 120 hours). Dosage for treatment of uterine fibroids: Take 5mg Ulipristal / time / day for 3 consecutive months. Start the first fibroid treatment course within one week of the first menstrual period, with subsequent courses starting as early as the first week of the second menstrual period after the end of the previous course of treatment. The recommended treatment interval between cycles is usually 2 menstrual cycles. According to the study, repeated intermittent treatment with Ulipristal can be up to 4 courses. 3.2. How to handle an overdose of Ulipristal acetate The use of an overdose of Ulipristal acetate can lead to symptoms that are harmful to the patient's health. If you notice any unusual signs after taking an overdose of Ulipristal, you should immediately notify your doctor for proper treatment.
4. Some side effects of the drug Ulipristal acetate
Based on study data in patients with uterine fibroids treated with Ulipristal acetate for 3 months has shown some undesirable effects. Side effects can range from mild to severe, common and uncommon, and their effects on individual body systems. The following are the possible reactions after using Ulipristal acetate, including:
Very common side effects: Thickening of the endometrium or amenorrhea. Common side effects: Dizziness, headache, nausea, abdominal pain, acne, hot flashes, musculoskeletal pain, pelvic pain, breast tenderness/pain, ovarian cyst, weight gain or fatigue . Uncommon side effects: Hypersensitivity to the drug, anxiety, dizziness, emotional disturbances, constipation, dry mouth, dry skin, hair loss, back pain, enuresis, increased sweating, uterine bleeding, vaginal discharge, bleeding, breast discomfort, weakness, edema, hypercholesterolemia or hypertriglyceridemia. Rare side effects: Breast swelling, ruptured follicles, bloating, indigestion, nosebleeds. Side effects of unknown frequency: Angioedema or liver failure. When comparing repeated courses of Ulipristal, the overall incidence of adverse events in later courses tends to be lower than in the first course. In case of any side effects, you need to stop taking Ulipristal immediately and tell your doctor. With mild reactions, it is usually only necessary to reduce the dose or stop the drug temporarily for the symptoms to disappear. However, cases of severe hypersensitivity will require supportive measures such as oxygen, epinephrine, ventilation, corticosteroids or antihistamines.
5. Important notes when using Ulipristal acetate
5.1. What precautions should I take while using Ulipristal acetate? When using Ulipristal acetate for emergency contraception or treatment of uterine fibroids, the following precautions should be taken by patients:
People with severe uncontrolled asthma should use Ulipristal with caution. People with moderate to severe liver impairment or severe renal impairment should consult a doctor before taking the drug, if necessary adjust the dose accordingly. Do not take Ulipristal for the purpose of terminating an existing pregnancy. The drug can cause blurred vision, dizziness and attention disorders, so people with specific jobs such as operating machinery, driving or working at height should use caution when taking Ulipristal. During Ulipristal administration, patients should be monitored for endometrium and for persistent or unexpected bleeding symptoms. Assess the possibility of pregnancy or ectopic pregnancy in patients receiving 30 mg of Ulipristal who develop signs of a missed period > 7 days, lower abdominal pain, or persistent bleeding. 5.2. Does Ulipristal acetate interact with other drugs? When using Ulipristal acetate at the same time as the following drugs, an interaction reaction may occur:
Inducers of the CYP3A4 enzyme, such as Phenobarbital, Rifampicin, Carbamazepine, Felbamate, Phenytoin or Topiramate. Medications to increase gastric pH such as H2 blockers, antacids, proton pump inhibitors. Other hormonal contraceptives or reduce the contraceptive effect of progestogens. Reducing the plasma concentration of St. John's wort when taken with Ulipristal. In short, Ulipristal acetate is used for emergency contraception or treatment of uterine fibroids. To ensure safety and maximize the effectiveness of treatment, patients need to use the drug exactly as prescribed by the doctor.
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