Ulipristal Acetate

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Ulipristal Acetate

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Overview of Ulipristal Acetate

Ulipristal Acetate: Quick Facts

Property Description
Active Ingredient Ulipristal Acetate (UPA)
Form Oral tablet
Pharmacological Class Selective Progesterone Receptor Modulator (SPRM)
Origin Synthetic organic molecule
Common Use (General) Emergency contraception; Uterine fibroid management

What is Ulipristal Acetate? Defining the Compound

Ulipristal Acetate (UPA) is the International Non-proprietary Name (INN) for a synthetic, steroidal compound that serves as an active pharmaceutical ingredient, most commonly taken orally as a tablet. As a derivative of 19-norprogesterone, UPA is classified as a fully synthetic organic molecule created through laboratory processes.

This INN is utilized in distinct commercial products based on its application. For time-sensitive contraception, it is known by brand names like ella (in the US) and ellaOne (in Europe). For the management of uterine fibroids, it is known by brands such as Esmya in certain markets, highlighting its versatility in women's health.

Pharmacological Class and Purpose

Ulipristal Acetate belongs to the distinct pharmacological class of Selective Progesterone Receptor Modulators (SPRMs). This classification means UPA selectively binds to and modifies the function of the body's progesterone receptors, which are vital components of the reproductive system.

The primary therapeutic applications of UPA are in emergency contraception and for the pre-operative management of moderate to severe symptoms of uterine fibroids (leiomyomas). This unique pharmacological profile is clinically recognized for providing effective options to address these hormone-dependent conditions. This section defines the purpose and identity of the drug without detailing the mechanisms of its action or usage instructions.

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What side effects are possible with Ulipristal Acetate?

Ulipristal Acetate: Possible side effects and safety information

Regulatory documents classify the potential adverse reactions of Ulipristal Acetate into frequency categories and by the physiological system affected. This structure allows for a clear communication of the expected safety profile based on clinical data.

Adverse Reaction Classifications

Category Examples (as listed in official labeling)
Very Common (ge 1/10) Headache (in emergency contraception use), Amenorrhea (expected effect during fibroid treatment)
Common (ge 1/100 to <1/10) Dizziness, Nausea, Abdominal pain, Breast tenderness, Fatigue, Mood changes
System-Organ Classes Nervous System, Gastrointestinal, Reproductive System and Breast Disorders, Hepatobiliary Disorders

Serious Adverse Reactions and Safety Constraints

The most significant safety consideration documented in regulatory labeling is the potential for serious liver injury, including rare cases of hepatic failure. This risk profile mandates specific risk mitigation protocols, including the requirement for routine monitoring of liver function tests prior to, during, and after stopping treatment for uterine fibroids.

Safety constraints define specific populations where the medicine should not be used. Ulipristal Acetate is officially contraindicated in individuals with pre-existing severe hepatic impairment. Furthermore, the concurrent use of the medication with strong or moderate inducers of the CYP3A4 enzyme is contraindicated, as this interaction can significantly reduce the drug's exposure, potentially compromising its effect. Use with other progestogen-containing medications is generally not recommended as they may interfere with Ulipristal Acetate's pharmacological action.

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Overdose and Emergency Response

Overdose and When to Seek Help

This section describes the officially documented manifestations of Ulipristal Acetate (UPA) overdose and the specific emergency actions required, as stated in government regulatory sources, such as the FDA and EMA.


Official Regulatory Profile

Overdose Component Regulatory Statement
Documented Manifestations Symptoms are generally mild to moderate and usually self-limiting. Reported symptoms include nausea, vomiting, dizziness, abdominal pain, and fatigue.
Severity and Outcome Severe adverse reactions or life-threatening events are not expected, even with acute single doses up to 200 mg (several times the usual dose).
Antidote Availability No specific antidote is known for Ulipristal Acetate overexposure.
Management Management of UPA overdose is strictly symptomatic and supportive.

Mandatory Emergency Actions

Seeking immediate medical attention is required for any known or suspected case of Ulipristal Acetate overdose, regardless of the apparent severity of symptoms. Regulatory guidance mandates contacting a Poison Control Center or local emergency services immediately for evaluation and professional guidance on management and monitoring. This ensures a standardized safety response is implemented, adhering to official health authority instructions.

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Therapeutic Uses of Ulipristal Acetate

Ulipristal Acetate: Main Uses and Therapeutic Areas

Ulipristal acetate is applied across domains where additional symptomatic support is needed, both related to domains of women’s health. This medication is commonly used to help with symptom clusters that may become intense or disruptive, applicable across domains where additional symptomatic support is needed: emergency contraception and uterine fibroids management.

Emergency Contraception

Ulipristal acetate is applied across domains where additional symptomatic support is needed, with a primary use as an emergency contraceptive (EC). This application is relevant for easing the need for short-term symptomatic assistance following unprotected sexual intercourse or suspected contraceptive failure. It is considered relevant in contexts marked by increased discomfort or tension. This use helps ease the overall symptom burden and may be part of symptomatic management in scenarios where symptoms escalate temporarily.


Uterine Fibroids Management

The second key therapeutic use is applied in addressing conditions presenting with systemic or localized discomfort from uterine fibroids. It is commonly used across conditions presenting with acute episodes, relevant for managing symptoms of uterine fibroids in adult women of reproductive age. It may assist with managing symptoms related to inflammatory or irritative states, which may create noticeable physiological strain. The second key therapeutic use is applied in addressing conditions characterized by periods of heightened symptoms associated with uterine fibroids. This assists with maintaining functional stability during symptomatic phases and is commonly used when short-term symptomatic assistance is needed.

“This medication is commonly used when short-term symptomatic assistance is needed.”


Quick Fact: Relevant for Symptoms that interfere with daily functioning

Regulatory References

  1. NIH MedlinePlus overview
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Eligibility and Restrictions for Use

Eligibility Profile for Ulipristal Acetate

The eligibility for Ulipristal Acetate (UPA) is defined by strict regulatory criteria, primarily distinguishing between the 5 mg (uterine fibroid) and 30 mg (emergency contraception) doses. The medication is generally intended for adult women of reproductive age.

Category Regulatory Status
Pregnancy Contraindicated (absolute prohibition for both doses).
Underlying Hepatic Disorder Contraindicated (5 mg dose). Not recommended for severe impairment (30 mg dose).
Specific Cancers Contraindicated (Uterine, cervical, ovarian, or breast cancer for 5 mg dose).
Age Restriction Not intended for use in postmenopausal or pre-pubertal women.

Use of the 5 mg dose for fibroids is further restricted to when surgical treatment options are unsuitable or have failed. Initiation of the 5 mg treatment is prohibited if baseline liver transaminases (ALT or AST) exceed 2 times the Upper Limit of Normal.

For breastfeeding women, the 5 mg dose is contraindicated, and the 30 mg dose is not recommended. Use is also not recommended in patients with severe renal impairment due to a lack of data.

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What should I know about interactions with other medicines?

Interactions with other medicines and products

Ulipristal acetate's effectiveness and concentration can be significantly altered by co-administered medications, primarily due to interactions involving the CYP3A4 enzyme and the drug's activity on hormone receptors.

Pharmacokinetic Interactions (Drug Levels)

Category Examples (per label) Effect on Ulipristal Acetate
Strong/Moderate CYP3A4 Inducers Rifampin, Phenytoin, St. John's Wort Significantly decreases plasma concentration; may lead to loss of effectiveness.
Strong CYP3A4 Inhibitors Ketoconazole, Itraconazole Significantly increases plasma concentration.

Pharmacodynamic Interactions (Mechanism of Action)

Co-administration with progestin-containing products (including hormonal contraceptives) is associated with a pharmacodynamic interaction. Ulipristal is a progesterone receptor modulator, and taking it with exogenous progestins may interfere with the intended effect of both medications. Therefore, regulatory information specifies a time separation requirement.

Interaction-Related Requirements

  • Enzyme Inducers: Strong and moderate CYP3A4 inducers must be avoided due to the documented risk of decreased drug exposure and treatment failure.
  • Hormonal Products: Progestin-containing hormonal contraceptives should not be initiated or resumed until five days after taking ulipristal acetate.
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Mechanism of Action

Selective Progesterone Receptor Modulation

Ulipristal Acetate (UPA) is defined by its selective, dual action on the Progesterone Receptor (PR), which serves as its sole primary molecular target. As a Selective Progesterone Receptor Modulator (SPRM), its interaction type varies based on the tissue, resulting in differential effects on hormone-responsive pathways across the body. This fundamental mechanism initiates the subsequent physiological consequences, including the modulation of hormonal feedback centrally and the regulation of cellular growth peripherally.


Inhibition of Central HPO Axis Signaling

UPA exerts a targeted, antagonist effect on the PR located in the pituitary gland, a key component of the Hypothalamic-Pituitary-Ovarian (HPO) Axis). This action suppresses the pituitary release of the Luteinizing Hormone (LH) surge, which is the physiological trigger for ovulation. The resulting physiological effect is the inhibition of follicular rupture, a functional consequence of disrupting the central hormonal cascade.


Direct Modulation of Uterine Tissue Viability

In parallel, UPA acts peripherally by directly modulating PR function on cells within the uterus. This local action activates signaling pathways that specifically inhibit cell proliferation and induce apoptosis (programmed cell death) in progesterone-responsive uterine tissue. The physiological result is a mechanism that contributes to limiting the proliferation of affected tissue and the creation of characteristic changes known as Progesterone Receptor Modulator-Associated Endometrial Changes (PAEC) within the endometrial lining.

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Dosage and Administration Information

Ulipristal acetate usage is defined by two distinct indications, each requiring specific dose and schedule adherence, and is administered exclusively via the oral route as a tablet. Administration may occur with or without food for both therapeutic uses.

For emergency contraception (EC), the official protocol requires a single 30 mg tablet to be taken as soon as possible, but no later than 120 hours (five days), following unprotected intercourse or contraceptive failure. This dose may be taken at any point in the menstrual cycle. If vomiting occurs within three hours of intake, consideration should be given to repeating the dose. Following the single EC dose, the initiation or resumption of any routine hormonal contraception must be deferred for at least 5 days. The 30 mg dose is considered suitable for use in postpubertal adolescents.

For the management of uterine fibroids, the prescribed regimen is one 5 mg tablet daily. This treatment is structured into intermittent courses of up to 3 months each, with the initial course required to begin during the first week of a menstrual period. If a daily dose is missed, it should be taken as soon as possible, but if the lapse exceeds 12 hours, the missed dose is skipped, and the regular schedule is resumed. For mild or moderate renal impairment, no dose adjustment is recommended.

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Recent Clinical Evidence

Research evidence / Overview of Studies for Ulipristal Acetate

Ulipristal Acetate was studied for conditions presenting with cycles of stability and flare-ups. The research examined how this agent was evaluated in studies that describe patterns observed in the studies in individuals. These studies were applied in studies examining patient-reported experiences in observational settings evaluating daily-life functioning. The focus was on patient-reported outcomes describing perceived discomfort and outcomes reflecting daily functioning or activity level, which are critical in conditions where symptoms may vary in intensity.

Findings from this research describe patterns observed in studies conducted during periods of increased symptom activity. Studies reported measurements of outcomes linked to physiological strain or stress, such as menstrual flow. However, the available evidence is limited regarding whether these patterns persist after the study period concludes, and long-term effects are not fully established regarding the continuation of measured symptom patterns. Follow-up durations were limited in many of these investigations, meaning the results apply only to the populations studied and the defined time intervals of observation.

Outcomes Related to Physical Discomfort

Research examined outcomes related to physical discomfort, particularly those linked to changes in bleeding patterns. Studies monitored how symptoms evolved in the observed populations during periods of use.

Research for Conditions Associated with Acute or Disruptive Episodes (Emergency Contraception)

Ulipristal Acetate was studied for conditions associated with acute or disruptive episodes, where research examined temporary physiological imbalance. These investigations were evaluated in trials assessing short-term or episodic symptom patterns. The primary focus was on the Observed Pregnancy Rate, which was evaluated in trials assessing short-term or episodic symptom patterns.

The studies monitored the outcome of interest over defined time intervals. Studies observed patterns related to the measured acute outcome. Because of the nature of this use, the research exploring short-term symptom changes inherently has follow-up durations were limited. Subgroup findings are uncertain within the existing evidence.

Key Studies & References

  1. Heavy menstrual bleeding: assessment and management (NICE guideline NG88)
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Frequently Asked Questions (FAQ)

Common questions about Ulipristal Acetate (FAQ)

Q: Is Ulipristal Acetate the same as other emergency contraception pills?

A: Ulipristal Acetate is not the same as emergency contraception pills containing only levonorgestrel. Official documents classify Ulipristal Acetate as a Selective Progesterone Receptor Modulator (SPRM), which gives it a distinct pharmacological mechanism of action. This difference is described as contributing to its effective use up to 120 hours after unprotected intercourse.


Q: Can Ulipristal Acetate affect my next menstrual period?

A: Official information indicates that Ulipristal Acetate may alter the timing of your next period, potentially causing it to be a few days earlier or later than expected. If the period is delayed by more than one week, official regulatory guidance indicates that pregnancy should be considered and ruled out.


Q: Is it normal to have spotting or bleeding after taking Ulipristal Acetate?

A: Yes, regulatory documents list intermenstrual bleeding, or spotting, as a common finding in clinical trials for the emergency contraception dose. These temporary changes in bleeding patterns are generally considered expected side effects of the medicine.


Q: How long can side effects from Ulipristal Acetate last?

A: Common side effects like headaches or nausea are typically described as transient, meaning they are temporary and usually resolve within a few days. Changes to the womb lining (endometrium) associated with the drug are also generally described in regulatory texts as being reversible after treatment is stopped.


Q: What if I vomit shortly after taking Ulipristal Acetate?

A: The official protocol for the emergency contraception dose advises that if vomiting occurs within three hours of taking the tablet, official guidance recommends consulting a healthcare provider immediately. Consideration for repeating the dose is outlined in the regulatory administration guidance.


Q: What kind of stomach issues are commonly reported after using Ulipristal Acetate?

A: Official regulatory documents list nausea and abdominal pain as common gastrointestinal side effects. Other stomach issues such as diarrhea or indigestion (dyspepsia) have also been reported, though less frequently, depending on the specific use of the drug.


Q: Can Ulipristal Acetate be used by someone who has asthma?

A: While regulatory documents generally do not list mild or moderate asthma as a specific contraindication, some sources advise that caution may be needed in cases of severe asthma that is insufficiently controlled by oral medication. Assessment of use is generally managed by a healthcare professional.


Q: How does Ulipristal Acetate compare to Levonorgestrel as an emergency option?

A: Regulatory-reviewed studies describe Ulipristal Acetate as maintaining a consistent effectiveness over the entire 120-hour (five-day) treatment window. This is often noted to be a difference from levonorgestrel, which official documents state is most effective within the first 72 hours.


Q: Is it safe to take Ulipristal Acetate more than once in the same menstrual cycle?

A: Official regulatory documents state that repeated use of the emergency contraception dose within the same menstrual cycle is not recommended. The safety and effectiveness of using the drug more than once within the same cycle have not been fully evaluated in studies.


Q: Is it possible for Ulipristal Acetate to cause changes in mood or headaches?

A: Yes, headaches are classified as a very common side effect in regulatory documents. Mood changes, which may include anxiety or emotional distress, are also listed as a common side effect of the medicine.


Q: Does body weight influence how effective Ulipristal Acetate is?

A: Regulatory-filed research has examined the use of Ulipristal Acetate in individuals with higher body weight. While some studies have suggested potential differences in effectiveness for emergency contraception at higher weights, official regulatory documents do not specify a weight limit or require a dose adjustment.


Q: Are there any food restrictions when taking Ulipristal Acetate?

A: The medicine is officially described as being administered with or without food. Although some beverages, such as grapefruit juice, may affect how the body processes the drug, this is generally considered less clinically significant for the single emergency dose.


Q: What kind of symptoms warrant immediate medical attention after taking Ulipristal Acetate?

A: Official documents specify that immediate medical attention is needed for symptoms of potential liver injury, such as yellowing of the skin (jaundice), dark urine, or severe fatigue. Immediate medical attention is also indicated for signs of a potential ectopic pregnancy, such as severe, unexplained pelvic pain.


Q: Is Ulipristal Acetate available in a generic version?

A: The FDA has approved a generic version of Ulipristal Acetate for emergency contraception. However, the commercial availability of a generic product in a specific location depends on market-specific patent status.


Q: Can Ulipristal Acetate be used by people with liver issues?

A: Ulipristal Acetate is explicitly contraindicated (prohibited) for individuals with severe hepatic (liver) impairment. For the chronic fibroid treatment dose, official guidance prohibits starting treatment if liver tests exceed a defined threshold.


Q: Has Ulipristal Acetate been studied in teenagers?

A: Yes, official documents state that the emergency contraception dose is considered suitable for use in postpubertal adolescents. Studies and safety monitoring have included this population to support its labeled use.


Q: Why is Ulipristal Acetate not considered a form of abortion?

A: Regulatory documents state that Ulipristal Acetate is not for use to terminate an existing pregnancy. Its primary action is to prevent or delay ovulation, thereby preventing fertilization. Official information explicitly states it does not interrupt an already implanted pregnancy.


Q: Does Ulipristal Acetate cause fatigue or tiredness?

A: Yes, fatigue, or a feeling of low energy, is listed as a common side effect in official regulatory labeling for the medicine.


Q: What if a person with known kidney problems takes Ulipristal Acetate?

A: For mild or moderate renal (kidney) impairment, official documents state that no dose adjustment is recommended for the fibroid treatment dose. However, use is not recommended in patients with severe renal impairment due to a lack of specific safety data.


Q: How does Ulipristal Acetate affect the womb lining (endometrium)?

A: Ulipristal Acetate causes specific, expected changes to the womb lining, known as the endometrium. These changes are called Progesterone Receptor Modulator-Associated Endometrial Changes (PAEC) and official documents confirm they are generally reversible once treatment is completed.


Q: How does Ulipristal Acetate affect ovarian function?

A: The main acute effect of the drug is to inhibit or delay ovulation. Regulatory documents advise that following the emergency contraception dose, a rapid return of fertility is expected.


Q: Are there differences in Ulipristal Acetate product names between countries?

A: Yes, while Ulipristal Acetate is the official name for the active ingredient, commercial brand names vary by country and indication. For example, the emergency contraception product is known by different names, such as ella in the US and ellaOne in Europe.


Q: Is Ulipristal Acetate safe to use while breastfeeding?

A: For the chronic fibroid dose, official documents state it is contraindicated (prohibited) during breastfeeding. For the single emergency dose, it is not recommended, and regulatory guidance suggests a period of expressing and discarding breast milk to reduce infant exposure.


Q: Can Ulipristal Acetate affect the results of a pregnancy test?

A: Regulatory guidance advises individuals to take a pregnancy test if menses is delayed. The drug itself does not interfere with the chemical accuracy of standard over-the-counter pregnancy tests, which detect the hormone hCG.


Q: Does Ulipristal Acetate affect the results of blood tests?

A: The drug is not generally listed as interfering with routine blood tests. However, official documents mandate regular monitoring of specific blood tests, such as liver function tests (LFTs), during the chronic fibroid treatment course.


Q: Why do some people experience abdominal pain after taking Ulipristal Acetate?

A: Abdominal pain is listed as a common side effect in regulatory documents. While the exact physiological reason for this temporary symptom is not detailed in patient-facing material, it is considered an expected adverse reaction linked to the drug's activity on the progesterone receptor.


Q: Are there any common misconceptions about how Ulipristal Acetate works?

A: A common misconception addressed in official patient information is the belief that the drug causes an abortion. Regulatory documents clarify that its primary function is to prevent or delay ovulation and that it is not used to terminate an existing pregnancy.


Q: What is the official patient leaflet say about missed doses (in the context of fibroid treatment)?

A: For the chronic treatment of uterine fibroids, official instructions advise that if a daily dose is missed, it should be taken as soon as possible. However, if the time lapse exceeds 12 hours, the missed dose is skipped, and the regular daily schedule is resumed.

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How should Ulipristal Acetate be stored and disposed of?

How to Store and Dispose of Ulipristal Acetate

Ulipristal acetate (UPA) tablets must be stored and disposed of according to the specific conditions detailed in official government labeling to maintain stability and ensure safety.


Official Storage Requirements

Condition Requirement
Temperature Store at controlled room temperature: 20°C to 25°C (68°F to 77°F).
Protection Keep the tablets in the original container and protect them from moisture.
Safety The medicine must be stored out of the sight and reach of children.
Stability Do not use the tablets after the expiry date printed on the carton.

Disposal Instructions

To discard unused or expired tablets, the product must not be thrown away via household waste or wastewater. Disposal must be completed in accordance with local regulatory requirements, such as taking the medicine to a designated pharmacy take-back program.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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