Ulipristal


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Emergency contraception
Adult: 30 mg taken as soon as possible w/in 120 hr after unprotected intercourse or contraceptive failure. An additional dose should be taken if vomiting occurs w/in 3 hr.
Child: Postpubertal: Same as adult dose.

Oral
Uterine fibroids
Adult: 5 mg once daily for up to 3 mth, starting during the 1st wk of menstruation for moderate to severe symptoms. Re-treatment courses should start during the 1st wk of the 2nd menstruation following completion of previous course. Max: 4 courses.
Suy gan
Emergency contraception: Severe: Not recommended.
Cách dùng
May be taken with or without food.
Chống chỉ định
Genital bleeding of unknown aetiology other than uterine fibroids; breast, uterine, cervical, or ovarian cancer (5 mg tab). Pregnancy and lactation.
Thận trọng
Patient w/ severe uncontrolled asthma. Moderate to severe hepatic and severe renal impairment. Not indicated for termination of existing pregnancy.
Tác dụng không mong muốn
Significant: Reversible endometrial thickening, amenorrhea (5 mg tab).
Nervous: Headache, dizziness, mood disorders, fatigue, vertigo, tremor, anxiety.
GI: Abdominal pain, nausea, vomiting, dry mouth, flatulence.
Genitourinary: Functional ovarian cyst, uterine spasm or haemorrhage, urinary incontinence.
Endocrine: Increased cholesterol and triglycerides, breast tenderness, dysmenorrhoea, menorrhagia, spotting.
Musculoskeletal: Myalgia, back pain
Ophthalmologic: Blurred vision,
Dermatologic: Acne, rash, pruritus, urticaria, hot flushes.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, blurred vision, and attention disturbance, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor endometrium and unexpected/persistent irregular bleeding (5 mg tab). Evaluate for pregnancy or ectopic pregnancy if expected menses is delayed ≥1 wk, or if persistent irregular bleeding or lower abdominal pain develops (30 mg tab).
Tương tác
Decreased plasma concentration and reduced efficacy w/ CYP3A4 enzyme inducers (e.g. rifampicin, felbamate, carbamazepine, phenobarbital, phenytoin, topiramate). Reduced absorption w/ drugs that increase gastric pH (e.g. antacids, H2-blockers, proton pump inhibitors). Increased plasma concentration w/ CYP3A4 enzyme inhibitors (e.g. ketoconazole, itraconazole). May reduce contraceptive action of progestogen and other hormonal contraceptives.
Tương tác với thức ăn
Decreased plasma concentration w/ St. John’s wort.
Tác dụng
Description:
Mechanism of Action: Ulipristal is a synthetic 19-norprogesterone derivative that inhibits progesterone from binding to its receptors. It delays ovulation by inhibiting follicular rupture and impairs implantation by altering the normal endometrium. Additionally, it inhibits cellular proliferation and induces apoptosis, thereby reducing the size of uterine fibroids.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: 1 hr.
Distribution: Plasma protein binding: >98%, to albumin, α1-acid glycoprotein, HDL, and LDL.
Metabolism: Extensively metabolised mainly by CYP3A4 enzyme and to a lesser extent by CYP1A2 and CYP2D6 enzymes to mono-demethylated (active) and di-demethylated metabolites.
Excretion: Mainly via faeces; urine (<10%). Terminal elimination half-life: Approx 32-38 hr (ulipristal); approx 27 hr (mono-demethylated metabolite).
Đặc tính

Chemical Structure Image
Ulipristal

Source: National Center for Biotechnology Information. PubChem Database. Ulipristal, CID=13559281, https://pubchem.ncbi.nlm.nih.gov/compound/Ulipristal (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại MIMS
Thuốc uống ngừa thai
Phân loại ATC
G03AD02 - ulipristal ; Belongs to the class of emergency contraceptives. Used as systemic contraceptives.
G03XB02 - ulipristal ; Belongs to the class of antiprogestogens.
Tài liệu tham khảo
Anon. Ulipristal. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2017.

Buckingham R (ed). Ulipristal Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2017.

Ella Tablet (A-S Medication Solutions). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/06/2017.

Joint Formulary Committee. Ulipristal Acetate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Ulipristal Acetate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/06/2017.

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