Ulipristal


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Emergency contraception 30 mg as soon as possible w/in 120 hr after unprotected intercourse or contraceptive failure. Uterine fibroids 5 mg once daily for up to 3 mth, starting during the 1st wk of menstruation. Re-treatment courses should start during the 1st wk of the 2nd menstruation following completion of previous course. Max: 4 courses.
Dosage Details
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.
Hepatic Impairment
Emergency contraception: Severe: Not recommended.
Administration
May be taken with or without food.
Contraindications
Genital bleeding of unknown aetiology other than uterine fibroids; breast, uterine, cervical, or ovarian cancer (5 mg tab). Pregnancy and lactation.
Special Precautions
Patient w/ severe uncontrolled asthma. Moderate to severe hepatic and severe renal impairment. Not indicated for termination of existing pregnancy.
Adverse Reactions
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.
Patient Counseling Information
This drug may cause dizziness, blurred vision, and attention disturbance, if affected, do not drive or operate machinery.
MonitoringParameters
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).
Drug Interactions
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.
Food Interaction
Decreased plasma concentration w/ St. John’s wort.
Action
Description: 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).
Chemical Structure

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)

Storage
Store between 20-25°C. Protect from light.
MIMS Class
ATC Classification
G03AD02 - ulipristal ; Belongs to the class of emergency contraceptives. Used as systemic contraceptives.
G03XB02 - ulipristal ; Belongs to the class of antiprogestogens.
References
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.

Disclaimer: This information is independently developed by MIMS based on Ulipristal from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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