Fibropress

• Approved Indication:
• Management of symptomatic uterine fibroids (leiomyomas) in adult women of reproductive age, particularly for preoperative treatment to reduce fibroid size and control heavy menstrual bleeding.
• Clinical Use Details:
• Used to control moderate to severe symptoms of uterine fibroids such as menorrhagia, pelvic pressure or pain, and anemia due to fibroid-related bleeding.
• Typically prescribed as a short-term treatment course prior to surgery or for intermittent long-term management to delay the need for surgical intervention.

• Adults (Reproductive-Age Women):
• Oral administration of 5 mg once daily for up to 3 months per treatment course.
• Treatment courses may be repeated with intermittent drug-free intervals (usually at least 2 menstrual cycles between courses) as per clinical judgment.
• Pediatrics:
• Safety and efficacy not established.
• Elderly:
• Not applicable (indication limited to premenopausal women).
• Special Populations:
• No specific dose adjustments established for hepatic or renal impairment; use with caution in severe hepatic impairment.
• Administration Route:
• Oral, with or without food.
• Duration:
• Typically 3 months per course; repeated courses based on clinical assessment.

Ulipristal Acetate is a selective progesterone receptor modulator (SPRM) that binds to progesterone receptors in uterine tissue, exhibiting both antagonist and partial agonist effects. By modulating progesterone activity, it inhibits cell proliferation and induces apoptosis in fibroid cells, reducing fibroid volume. It also decreases vascularization and alters the endometrium, leading to reduced menstrual bleeding. These combined effects result in symptom relief and fibroid shrinkage.

• Absorption:
• Well absorbed orally; peak plasma concentration (C_max) reached within 1 to 3 hours post-dose.
• Bioavailability:
• Approximately 98% oral bioavailability.
• Distribution:
• Highly protein bound (~98%).
• Metabolism:
• Extensively metabolized in the liver primarily via CYP3A4 to active metabolites.
• Elimination:
• Half-life approximately 32 hours.
• Excreted mainly through feces (~84%) and to a lesser extent urine (~6%).

• Pregnancy:
• Contraindicated during pregnancy. Ulipristal Acetate may harm the fetus; pregnancy must be excluded before treatment initiation.
• Lactation:
• It is unknown whether Ulipristal Acetate is excreted in human milk. Breastfeeding is not recommended during treatment and for at least one week after the last dose.
• Caution:
• Women of childbearing potential must use non-hormonal contraception during treatment.

• Selective Progesterone Receptor Modulator (SPRM)
• Antiproliferative agent for uterine fibroids

• Known hypersensitivity to Ulipristal Acetate or any excipients
• Pregnancy or suspected pregnancy
• Severe hepatic impairment (Child-Pugh Class C)
• Breastfeeding
• Unexplained vaginal bleeding prior to diagnosis

• Liver function monitoring recommended due to rare cases of severe liver injury; discontinue treatment if liver enzymes elevate significantly.
• Not recommended for long-term continuous use without monitoring.
• Women should have pregnancy excluded before starting treatment.
• Use contraception during and for at least one month after treatment.
• Caution in patients with mild to moderate hepatic impairment.
• Possible delay in return of menses after treatment cessation.
• Monitor for signs of allergic reactions.

• Common:
• Headache
• Fatigue
• Hot flushes
• Nausea
• Abdominal pain
• Menstrual irregularities (spotting, amenorrhea, delayed menstruation)
• Less Common:
• Breast tenderness
• Dizziness
• Back pain
• Serious/Rare:
• Severe hepatic injury (rare but serious)
• Allergic reactions including rash and urticaria
• Elevated liver enzymes
• Side effects are generally mild to moderate and reversible upon treatment discontinuation.

• CYP3A4 Inducers (e.g., rifampin, carbamazepine, St. John’s Wort):
• May decrease Ulipristal Acetate plasma concentration and reduce efficacy.
• CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole):
• May increase plasma levels; clinical significance unclear.
• No significant drug-food or drug-alcohol interactions reported.
• Use caution when co-administered with hormonal contraceptives; efficacy of contraceptives may be affected.

• Regulatory authorities have highlighted the importance of liver monitoring due to reports of rare but severe hepatic injury.
• Updated recommendations emphasize limited duration treatment courses (usually 3 months) with intervals between courses.
• Use is considered a valuable alternative to surgery in women seeking fertility preservation or delaying surgery.
• Not approved for postmenopausal women or for long-term continuous therapy without breaks.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep in original packaging until use.
• No refrigeration required.
• Keep out of reach of children.
• Avoid freezing.