Comprehensive Guide to Ulipristal Acetate: Uses, Dosage, Side Effects, and More

1. What is Ulipristal Acetate?

2. Overview of Ulipristal Acetate

Generic Name

Ulipristal acetate

Brand Name

Ella, Esmya, Fibristal (varies by region), generics

Drug Group

Selective progesterone receptor modulator (SPRM)

Commonly Used For

This medication is used to:

• Prevent pregnancy after unprotected intercourse.
• Manage uterine fibroids.
• Control heavy menstrual bleeding.

Key Characteristics

• Form: Oral tablets (30 mg for emergency contraception, 5 mg for fibroids) (detailed in Dosage section).
• Mechanism: Modulates progesterone receptors, delaying ovulation and reducing fibroid growth.
• Approval: FDA-approved (2010 for Ella as emergency contraception) and EMA-approved for both indications.

3. Indications and Uses of Ulipristal Acetate

Ulipristal acetate is indicated for reproductive and gynecologic conditions, leveraging its hormonal modulation effects:

• Emergency Contraception: Prevents pregnancy within 120 hours (5 days) after unprotected intercourse or contraceptive failure, offering a high efficacy rate (up to 98% if taken early), per WHO and CDC guidelines.
• Uterine Fibroids (Pre-Operative): Treats moderate to severe symptoms of uterine fibroids (e.g., heavy bleeding, pelvic pain) for up to 3 months before surgery, reducing fibroid size, supported by gynecologic trials.
• Uterine Fibroids (Long-Term Management): Used off-label for extended management of fibroids in patients unsuitable for surgery, improving quality of life, with data from longitudinal studies.
• Endometriosis-Associated Pain: Investigated off-label to alleviate pelvic pain and dysmenorrhea in endometriosis, modulating progesterone activity, supported by emerging gynecologic research.
• Polycystic Ovary Syndrome (PCOS): Explored off-label to regulate menstrual cycles and reduce androgen levels in PCOS, with promising results from endocrinology studies.
• Abnormal Uterine Bleeding: Employed off-label to control heavy or irregular bleeding not due to fibroids, stabilizing the endometrium, with evidence from reproductive health trials.
• Pre-Menopausal Hormone Regulation: Used off-label to manage pre-menopausal symptoms (e.g., irregular cycles) in women nearing menopause, with cautious application under specialist care.
• Fertility Preservation Support: Investigated off-label to delay ovulation in fertility preservation protocols (e.g., before chemotherapy), preserving ovarian function, noted in oncology-gynecology research.
• Postpartum Contraception: Explored off-label as a short-term contraceptive option postpartum, adjusting for breastfeeding status, with data from maternal health studies.

Note: This drug requires medical supervision, especially for repeated use or long-term therapy; consult a healthcare provider for appropriate indications.

4. Dosage of Ulipristal Acetate

Important Note: The dosage of this selective progesterone receptor modulator must be prescribed by a healthcare provider. Dosing varies by indication and patient profile, with adjustments based on clinical evaluation.

Dosage for Adults

• Emergency Contraception:
  • 30 mg single dose, taken within 120 hours of unprotected intercourse, with or without food.
• Uterine Fibroids (Pre-Operative):
  • 5 mg once daily for up to 3 months (84 days), taken with or without food, followed by a break.
• Uterine Fibroids (Long-Term, Off-Label):
  • 5 mg once daily for extended periods (e.g., 6–12 months), under gynecologic supervision, with monitoring.

Dosage for Adolescents

• Emergency Contraception (16+ years):
  • 30 mg single dose, as for adults, under medical guidance.
  • Not recommended under 16 years unless critical.

Dosage for Pregnant Women

• Pregnancy Category X: Contraindicated if pregnancy is confirmed; use only as emergency contraception before pregnancy is established. Consult an obstetrician for post-use monitoring.

Dosage Adjustments

• Renal Impairment: No adjustment needed; monitor in severe cases (CrCl <30 mL/min).
• Hepatic Impairment:
  • Mild (Child-Pugh A): No adjustment; moderate (Child-Pugh B): Use caution; severe (Child-Pugh C): Avoid.
• Elderly: Limited data; start with 5 mg once daily for fibroids, if indicated, with monitoring.
• Concomitant Medications: Avoid with strong CYP3A4 inducers (e.g., rifampin) or inhibitors (e.g., ketoconazole), altering efficacy.

Additional Considerations

• Take this active ingredient with or without food, using a glass of water.
• Avoid repeated emergency use within the same menstrual cycle.

5. How to Use Ulipristal Acetate

• Administration:
  • Swallow tablets whole with water, with or without food; avoid grapefruit juice.
  • Take the 30 mg dose as soon as possible after unprotected intercourse for emergency contraception.
• Timing: Use once daily for fibroid treatment or as a single dose for emergency contraception, as directed.
• Monitoring: Watch for abdominal pain, irregular bleeding, or signs of liver issues (e.g., yellowing skin).
• Additional Tips:
  • Store at 20–25°C (68–77°F), protecting from moisture and heat.
  • Keep out of reach of children due to hormonal effects.
  • Report severe headache, dizziness, or signs of allergic reaction immediately.

6. Contraindications for Ulipristal Acetate

This drug is contraindicated in:

• Hypersensitivity: Patients with a known allergy to Ulipristal acetate or its components.
• Confirmed or Suspected Pregnancy: Contraindicated due to potential fetal harm.
• Severe Hepatic Impairment: Contraindicated in Child-Pugh Class C due to toxicity risk.
• Undiagnosed Abnormal Genital Bleeding: Avoid until etiology is determined.

7. Warnings & Precautions for Ulipristal Acetate

General Warnings

• Hepatotoxicity: Risk of liver injury, including rare cases of liver failure; monitor liver function during long-term use.
• Hormonal Imbalance: May cause irregular bleeding or amenorrhea; assess endometrial health.
• Ectopic Pregnancy: Risk if pregnancy occurs; rule out ectopic pregnancy post-use.
• Ovarian Cysts: Potential for cyst formation; monitor with ultrasound if symptoms arise.
• Drug Resistance: Repeated emergency use may reduce efficacy; limit to one dose per cycle.

Additional Warnings

• Breast Cancer Risk: Theoretical risk with long-term use; screen patients with breast cancer history.
• Depression: Rare mood changes; monitor mental health.
• Cardiovascular Effects: Rare hypertension or thromboembolism; assess in at-risk patients.
• Bone Mineral Density: Potential loss with prolonged use; monitor in pre-menopausal women.
• Hypersensitivity Reactions: Rare anaphylaxis; discontinue if swelling occurs.

Use in Specific Populations

• Pregnancy: Category X; avoid unless for emergency contraception before pregnancy.
• Breastfeeding: Excreted in breast milk; avoid or monitor infant for effects.
• Elderly: Limited data; use only if indicated with caution.
• Adolescents: Limited to 16+ years for emergency contraception.
• Renal/Hepatic Impairment: Adjust dose; avoid in severe cases.

Additional Precautions

• Inform your doctor about liver disease, pregnancy plans, or medication history before starting this medication.
• Avoid concurrent use with hormonal contraceptives; use backup methods.

8. Overdose and Management of Ulipristal Acetate

Overdose Symptoms

Overdose may cause:

• Nausea, abdominal pain, or fatigue.
• Severe cases: Liver dysfunction, hormonal disruption, or uterine bleeding.
• Dizziness, headache, or irregular menstruation as early signs.
• Seizures with extremely high doses (rare).

Immediate Actions

• Contact the Medical Team: Seek immediate medical help.
• Supportive Care: Administer activated charcoal if ingested recently, monitor vital signs, and provide IV fluids.
• Specific Treatment: Manage liver function and hormonal symptoms; no specific antidote.
• Monitor: Check liver enzymes, hormone levels, and uterine health for 24–48 hours.

Additional Notes

• Overdose risk is low; store securely.
• Report persistent symptoms (e.g., jaundice, severe pelvic pain) promptly.

9. Side Effects of Ulipristal Acetate

Common Side Effects

• Headache (15–25%, relieved with rest)
• Nausea (10–20%, manageable with food)
• Abdominal Pain (8–18%, transient)
• Irregular Bleeding (5–15%, stabilizes post-treatment)
• Fatigue (4–12%, decreases with tolerance)
  These effects may subside with dose adjustment or cycle completion.

Serious Side Effects

Seek immediate medical attention for:

• Hepatic: Jaundice, hepatitis, or liver failure.
• Gynecologic: Severe uterine bleeding, ovarian cysts, or endometrial changes.
• Hormonal: Amenorrhea, mood swings, or adrenal insufficiency.
• Allergic: Rash, angioedema, or anaphylaxis.
• Cardiovascular: Hypertension or thromboembolism.

Additional Notes

• Regular monitoring for liver function, endometrial health, and hormonal status is advised.
• Report any unusual symptoms (e.g., yellow skin, severe abdominal cramps) immediately to a healthcare provider.

10. Drug Interactions with Ulipristal Acetate

This active ingredient may interact with:

• CYP3A4 Inhibitors: Increases levels (e.g., ketoconazole); reduce dose or avoid.
• CYP3A4 Inducers: Decreases efficacy (e.g., rifampin); avoid concurrent use.
• Hormonal Contraceptives: Reduces efficacy of both; use non-hormonal backup.
• Anticonvulsants: Alters metabolism (e.g., phenytoin); monitor levels.
• Statins: Potential for increased myopathy risk; use cautiously.

Action: Provide your healthcare provider with a complete list of medications.

11. Patient Education or Lifestyle

• Medication Adherence: Take this selective progesterone receptor modulator as prescribed for emergency contraception or fibroid management, following the exact schedule.
• Monitoring: Report irregular bleeding, abdominal pain, or fatigue immediately.
• Lifestyle: Avoid alcohol; maintain a balanced diet to support liver health.
• Diet: Take with or without food; avoid grapefruit during fibroid treatment.
• Emergency Awareness: Know signs of liver failure or ectopic pregnancy; seek care if present.
• Follow-Up: Schedule regular check-ups every 1–3 months during fibroid treatment or post-emergency use to monitor liver, uterine, and hormonal health.

12. Pharmacokinetics of Ulipristal Acetate

• Absorption: Well-absorbed orally (peak at 0.5–2 hours); enhanced with food.
• Distribution: Volume of distribution ~77 L; 98–99% protein-bound.
• Metabolism: Hepatic via CYP3A4 to active metabolites (e.g., monodemethyl-ulipristal acetate).
• Excretion: Primarily fecal (90%) as metabolites; renal (<10%); half-life 32–38 hours.
• Half-Life: 32–38 hours, with sustained endometrial and ovulatory effects.

13. Pharmacodynamics of Ulipristal Acetate

This drug exerts its effects by:

• Binding selectively to progesterone receptors, delaying ovulation and altering endometrial growth.
• Reducing fibroid size by inhibiting progesterone-driven proliferation.
• Demonstrating dose-dependent suppression of endometrial proliferation and potential liver impact.
• Exhibiting variable efficacy based on menstrual cycle phase and fibroid characteristics.

14. Storage of Ulipristal Acetate

• Temperature: Store at 20–25°C (68–77°F); protect from moisture.
• Protection: Keep in original container, away from light.
• Safety: Store in a locked container out of reach of children due to hormonal effects.
• Disposal: Dispose of unused tablets per local regulations or consult a pharmacist.

15. Frequently Asked Questions (FAQs)

Q: What does Ulipristal acetate treat?
A: This medication treats emergency contraception and uterine fibroids.

Q: Can this active ingredient cause irregular bleeding?
A: Yes, irregular bleeding may occur; report if persistent.

Q: Is Ulipristal acetate safe for adolescents?
A: Yes, for 16+ years for emergency use with a doctor’s guidance.

Q: How is this drug taken?
A: Orally as a single 30 mg dose or 5 mg daily, as directed.

Q: How long is Ulipristal acetate treatment?
A: Single dose for emergency use or up to 3 months for fibroids.

Q: Can I use Ulipristal acetate if pregnant?
A: No, avoid if pregnant; consult a doctor.

16. Regulatory Information

This medication is approved by:

• U.S. Food and Drug Administration (FDA): Approved in 2010 (Ella) for emergency contraception, with fibroid use under review.
• European Medicines Agency (EMA): Approved for emergency contraception and uterine fibroids (Esmya).
• Other Agencies: Approved globally for reproductive health; consult local guidelines.

17. References

1. U.S. Food and Drug Administration (FDA). (2023). Ella (Ulipristal Acetate) Prescribing Information.
   • Official FDA documentation detailing the drug’s approved uses, dosage, and safety.
2. European Medicines Agency (EMA). (2023). Ulipristal Acetate Summary of Product Characteristics.
   • EMA’s comprehensive information on the medication’s indications and precautions in Europe.
3. National Institutes of Health (NIH). (2023). Ulipristal Acetate: MedlinePlus Drug Information.
   • NIH resource providing detailed information on the drug’s uses, side effects, and precautions.
4. World Health Organization (WHO). (2023). WHO Guidelines on Emergency Contraception: Ulipristal Acetate.
   • WHO’s recommendations for Ulipristal acetate in emergency contraception.
5. Fertility and Sterility. (2022). Ulipristal Acetate in Fibroid Management.
   • Peer-reviewed article on Ulipristal acetate efficacy (note: access may require a subscription).