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Гинепристон

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Гинепристон

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Method of action: Antigestagenic

Treatment option: Pregnancy

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Гинепристон

Property Description
Active ingredient Mifepristone (RU486)
Form Oral Tablet
Pharmacological class Antiprogestogen / Hormone Antagonist
General Origin Synthetic steroid compound
General Purpose To modify hormone-dependent physiological processes

Что Такое Гинепристон: Состав и Фармакологический Класс (What is Ginepriston: Composition and Pharmacological Class)

Гинепристон is a prescription-only medicinal product defined by its sole active ingredient, the potent synthetic steroid compound Mifepristone. This compound is formally classified as an Antiprogestogen and a powerful Hormone Antagonist. Presented for peroral administration, Гинепристон is an oral tablet preparation. The classification as a steroidal Antiprogestogen is central to its profile: the compound possesses a high affinity for the Progesterone receptor, establishing its specialized role in altering hormone-dependent stability.

Принадлежность к Группе Антагонистов Прогестерона (Belonging to the Progesterone Antagonist Group)

The drug's unique pharmacological profile is based on Mifepristone's function as a competitive blocker. By binding to the Progesterone receptor sites, it effectively disrupts the hormone's stabilizing signals, a mechanism associated with initiating decidual breakdown and cervical softening. This action is a differentiating factor, as it fundamentally alters an established physiological process rather than merely preventing a future one.

Furthermore, Mifepristone exhibits secondary Antiglucocorticoid activity, blocking the receptors for the stress hormone Cortisol. This simultaneous antagonism establishes its distinct pharmacological identity among Hormone Antagonists.

Общее Назначение: Роль в Изменении Гормонально-Зависимых Процессов (General Purpose: Role in Modifying Hormone-Dependent Processes)

The overall function of Гинепристон is to strategically influence or interrupt specific hormone-dependent physiological processes in women. By disrupting the critical effects of Progesterone, the drug enables the modification of a physiological outcome. This action is recognized for its utility: the Mifepristone combination regimen is categorized as an essential medicine, underscoring its role in healthcare systems.

Regulatory References

  1. Mifepristone: StatPearls
  2. WHO Essential Medicines List
  3. WHO Essential Medicines List Change 2019
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What side effects are possible with Гинепристон?

Official Adverse Reactions and Safety Profile

The safety profile of Mifepristone (the active ingredient in Ginepriston) is formally documented in government regulatory sources, with adverse reactions categorized by frequency and the body system affected. These classifications reflect the official understanding of the drug's risks.

Frequency-Classified Effects

Adverse reactions are classified according to regulatory standards:

  • Very Common (Affecting ge 1 in 10): These often include uterine contractions, vaginal bleeding or spotting, nausea, and weakness. These effects are generally recognized as anticipated physiological consequences related to the drug's primary action.
  • Common (Affecting ge 1 in 100 to < 1 in 10): Documented common effects include headache, diarrhea, vomiting, and fatigue. These reactions are grouped under various System-Organ Classes (SOCs), such as Gastrointestinal Disorders and Nervous System Disorders.

Serious Safety Considerations

The official labeling highlights the potential for serious adverse reactions that occur less frequently but are clinically significant. These include reports of serious and sometimes fatal infections and sepsis, which may present atypically without fever, requiring a high index of suspicion. Additionally, prolonged heavy bleeding (hemorrhage) requiring medical intervention is a documented risk, primarily classified under Vascular Disorders.

Population-Specific Constraints

Regulatory documents specify safety constraints for certain populations. The drug is generally not recommended for individuals with severe renal failure or severe hepatic failure due to limited safety data. Contraindications also apply to patients with chronic adrenal failure or pre-existing hemorrhagic disorders.

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Overdose and Emergency Response

Overdose and When to Seek Help

An overdose of Mifepristone (Гинепристон) is officially documented as potentially resulting from the amplification of its hormonal antagonist effects, particularly its potent antiglucocorticoid activity. A massive overdose requires close observation for the clinical presentation of adrenal insufficiency. This severe manifestation may present with hypotension (low blood pressure), weakness, increased fatigue, and hypoglycemia (low blood sugar). Regulatory authorities stipulate that the required procedural step for confirmed adrenal insufficiency is the immediate administration of glucocorticoids as a specific treatment measure. No specific antidote is formally listed.

When to Seek Immediate Medical Help

Patients must seek immediate medical attention and go to the nearest hospital emergency room for signs of life-threatening complications. These officially listed signs include prolonged heavy vaginal bleeding, syncope (fainting), or indications of serious infection such as persistent fever or severe abdominal pain. Furthermore, the official labeling notes that severe hepatic impairment increases the risk of toxicity due to slowed drug elimination, a key population-specific overdose consideration.

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Therapeutic Uses of Гинепристон

Approved Therapeutic Applications for Mifepristone

Mifepristone, the active substance in Гинепристон, is approved for several distinct therapeutic uses. The primary indication is for the medical termination of an intrauterine pregnancy up to 70 days of gestation, administered as part of a regimen with a prostaglandin analog such as misoprostol.

Another approved use of mifepristone involves the management of high blood glucose (hyperglycemia) that is secondary to hypercortisolism in adult patients with endogenous Cushing's syndrome who also have type 2 diabetes mellitus or glucose intolerance. This treatment is generally reserved for patients who are not surgical candidates or have had unsuccessful surgery to control their condition.

The therapeutic action of the substance derives from its ability to block the activity of the progesterone hormone, which is key for maintaining pregnancy, and to inhibit the effects of excessive cortisol at the cellular level. This provides two different mechanisms for clinical intervention.


Quick Facts: What Mifepristone Treats

  • Medical termination of intrauterine pregnancy up to 70 days gestation, when used in combination with misoprostol.
  • Control of high blood sugar in adults with endogenous Cushing's syndrome and coexisting type 2 diabetes or glucose intolerance, for those who have failed or cannot undergo surgery.
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Eligibility and Restrictions for Use

The eligibility profile for Гинепристон (Mifepristone) is defined by strict regulatory classification, primarily limiting use to adult patients (ge 18 years) for its approved indications.

Absolute Contraindications (Prohibited Use)

The medicine is formally contraindicated in patient groups facing severe risk. These prohibitions include patients with chronic adrenal failure, those receiving long-term systemic corticosteroid therapy, individuals with inherited porphyrias, or patients with hemorrhagic disorders or concurrent anticoagulant therapy. For its use in pregnancy termination, it is prohibited in cases of confirmed or suspected ectopic pregnancy or if an intrauterine device (IUD) is in place. Pregnancy itself is an absolute contraindication when the drug is used for Cushing's syndrome.

Restricted and Age-Based Eligibility

Use is highly restricted or not recommended for populations with significant organ impairment, specifically severe hepatic or renal impairment, where safety data are not established. Patients with pre-existing cardiovascular conditions or uncontrolled hypertension are directed to use with caution. Furthermore, safety and effectiveness have not been established for general pediatric or geriatric patients. For women who are breastfeeding, official labeling requires a decision to discontinue the drug or discontinue nursing.

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What should I know about interactions with other medicines?

Гинепристон Interactions with other medicines and products

The interaction profile of Гинепристон (Mifepristone) is defined by its role as a substrate and inhibitor of metabolic enzymes and its antagonistic effect on hormone receptors, as documented in official prescribing information.

Pharmacokinetic and Metabolic Interactions

Category Interacting Substances Official Interaction Outcome
Inhibitors of CYP3A4 Ketoconazole, Itraconazole, Erythromycin, Grapefruit juice Increase Mifepristone plasma concentration (exposure).
Inducers of CYP3A4 Rifampin, Phenytoin, Phenobarbital, St. John's Wort Decrease Mifepristone plasma concentration (exposure).
Substrates of CYP3A4/2C9 Simvastatin, Warfarin, Midazolam Mifepristone increases the exposure of these co-administered drugs.

Co-administration with strong CYP3A4 inhibitors is restricted due to the potential for Mifepristone accumulation. Conversely, strong CYP3A4 inducers are often restricted or prohibited due to the risk of reduced effectiveness. Mifepristone is also documented as an inhibitor of the P-glycoprotein (P-gp) transporter, which may alter the exposure of co-administered P-gp substrates.

Pharmacodynamic and Restricted Combinations

Due to the medicine's antagonistic effect on glucocorticoid receptors, co-administration with long-term systemic corticosteroids (e.g., for immunosuppression) is formally prohibited to prevent the counteraction of the corticosteroid's intended effects. The interaction profile also notes an increased risk of QTc prolongation when co-administered with other QT-prolonging drugs.

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Mechanism of Action

Competitive Antagonism of Progesterone Receptors

The primary mechanism involves the molecule binding with high affinity to the intracellular Progesterone Receptor (PR), preventing natural progesterone from activating gene transcription. This molecular interference disrupts the stability of the uterine lining and removes the hormone's natural inhibitory signal on the myometrial muscle, starting the subsequent mechanistic cascade.

Myometrial Contractility and Tissue Softening Cascade

The functional blockade of the PR causes the uterine muscle's intrinsic tone to increase, leading to increased sensitivity of the myometrium to contraction-inducing mediators like prostaglandins. Simultaneously, this mechanism promotes the breakdown of the specialized uterine lining (decidual necrosis) and structural changes that lead to cervical softening. These coordinated tissue-level changes lead to a significant shift in uterine physiological state.

Secondary Blockade of Glucocorticoid Receptors

Beyond its main action, Mifepristone functions as a competitive antagonist at the Glucocorticoid Receptor (GR), blocking the signaling effects of the stress hormone cortisol. This secondary mechanistic domain supports the overall pharmacological identity of the drug by demonstrating its influence on systemic steroid hormone regulation.

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Dosage and Administration Information

The administration of Mifepristone (Гинепристон) is governed by two distinct protocols, each specifying different dosage forms and schedules for its main labeled uses. The medication is formulated exclusively as an oral tablet for administration.


Official Administration Regimens

Indication Protocol Mifepristone Dosing & Schedule Specific Instructions
Termination Regimen A single oral dose of 200 mg is taken on Day 1. Administration requires the IUD to be removed prior to use. A follow-up assessment is required 7 to 14 days after the initial dose.
Cushing's Syndrome The starting dose is 300 mg once daily, titratable up to a maximum of 1200 mg once daily. Dose increases must occur no more frequently than once every 2 to 4 weeks.

Required Administration Conditions

  • Intake with Food: For Cushing's syndrome treatment, the medication must be taken with a meal.
  • Tablet Integrity: Tablets for daily use must be swallowed whole and should not be split, crushed, or chewed.
  • Dose Limits: The maximum daily dose is restricted to 600 mg for patients with mild to moderate hepatic or renal impairment.

These standard instructions establish strict timelines and conditions for the medicine's use, differentiating between the short-term, sequential course and the long-term, titrated maintenance regimen.

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Recent Clinical Evidence

Гинепристон (Mifepristone): Overview of Clinical Evidence

Гинепристон, which contains the active substance mifepristone, is a selective progesterone receptor modulator. Research on mifepristone focuses primarily on its use for medical termination of pregnancy and for the management of symptomatic uterine fibroids.


Clinical Trials for Uterine Fibroids

Studies examining mifepristone for the treatment of uterine fibroids typically evaluate its effect on symptom relief and fibroid size. Findings from various randomized controlled trials (RCTs) and observational studies suggest the following:

Outcome Evaluated Research Findings Clinical Evidence Summary
Heavy Menstrual Bleeding Low-dose regimens were associated with a significant reduction in heavy bleeding (amenorrhea was reported in many cases). Moderate to Strong Evidence of symptomatic relief.
Fibroid Volume Some studies were associated with a reduction in fibroid volume, while others found no significant effect. The optimal dose and duration of use for fibroid shrinkage are still under investigation. Mixed Evidence; further large-scale RCTs are needed to draw confident conclusions.
Quality of Life Improvements were reported in fibroid-specific quality of life scores, often linked to the relief of bleeding and associated anemia. Favorable Evidence of improving patient-reported outcomes.

️ Safety and Adverse Events

Clinical safety data for mifepristone in the context of its indicated uses show that serious adverse events, such as severe hemorrhage or infection, are generally rare, although some studies report different rates. Common, expected events during its use can include nausea, headache, and abdominal cramping. Studies have also noted an increased incidence of endometrial changes, such as cystic glandular dilation, which requires monitoring following treatment.

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Frequently Asked Questions (FAQ)

Common questions about Гинепристон (FAQ)


Q: Is Гинепристон the same drug as the one used for Cushing's Syndrome?

A: The active substance in Гинепристон, mifepristone, is utilized in different product preparations and protocols for both its approved indications. Official product information confirms that the medication is used under distinct regimens to achieve its specific therapeutic goals in each case.

Q: What is the purpose of the follow-up appointment mentioned in the official instructions?

A: Regulatory documents state that a follow-up assessment is required to confirm that the process has been completed and to assess the patient for any potential serious medical concerns, such as heavy bleeding or infection.

Q: How long after using Гинепристон can a person resume normal physical activities?

A: Official information does not specify an exact timeline for resuming normal physical activity. However, common side effects such as weakness and fatigue are documented in the product information, which is a factor to consider when planning physical activities.

Q: Are there any research papers or studies about the long-term effects of using this medicine?

A: Clinical research summaries for this medicine primarily focus on data collected during the clinical trial period and subsequent monitoring. Available regulatory evidence does not indicate an impact on the ability to become pregnant in the future.

Q: Is it possible for the tablet to fail to work completely?

A: Official clinical data reports that the regimen is effective in a high percentage of cases when used according to approved instructions. However, as with any medical procedure, a small percentage of cases may not be fully completed.

Q: Can the effectiveness of Гинепристон be reduced by consuming certain foods or drinks?

A: Regulatory sources document that the drug's metabolic process can be affected by certain substances. Specifically, strong CYP3A4 inducers (a type of enzyme that processes medicines) are known to decrease the concentration of the active ingredient in the bloodstream, which may potentially reduce its intended effect.

Q: Why is the drug required to be dispensed under a specific risk management program?

A: The drug is subject to a specific Risk Evaluation and Mitigation Strategy (REMS) program in some regions. This official program is designed to manage and ensure that the benefits of the medication outweigh the documented serious risks associated with its use, such as severe bleeding and infection.

Q: Can the tablet be affected if it is accidentally chewed or crushed?

A: Official instructions require that the tablets be swallowed whole and not split, crushed, or chewed. This requirement ensures that the medicine is delivered and absorbed into the body in the manner and at the time intended by the manufacturer.

Q: How does the medicine interact with common psychiatric medications?

A: Official information notes that the drug interacts with medications processed by the CYP3A4 enzyme in the body. Furthermore, co-administration is restricted with other drugs that can prolong the QT interval (a measurement of heart electrical activity) due to documented safety concerns.

Q: What is the risk of birth defects if the pregnancy continues after taking Гинепристон?

A: Official product information states that if the regimen fails and the pregnancy continues, there is an increased risk of congenital malformations (birth defects). Surgical completion of the process is generally discussed as an option in official guidelines.

Q: Are there any restrictions on driving or operating machinery after taking Гинепристон?

A: The official safety profile documents side effects such as weakness, fatigue, and headache. Patients are generally advised that these effects may temporarily affect their ability to safely drive or operate heavy machinery.

Q: How is the process of using Гинепристон described in official patient guides?

A: Official patient guides describe the process as a structured, multi-step regimen. This typically involves the administration of the mifepristone tablet followed by a second medication at a specific time interval, as defined by the approved protocol.

Q: Does alcohol consumption affect the safety profile of Гинепристон?

A: While alcohol is not listed as a specific contraindication in the interaction tables, the medicine may cause general side effects like weakness and fatigue. Official guidance often advises limiting or avoiding alcohol during treatment to prevent potentially compounding these effects.

Q: Is it possible to have severe abdominal pain without a serious complication?

A: Uterine contractions and cramping are a documented and expected effect of the drug's primary action and can be severe. However, severe, unrelenting abdominal pain is also listed as a symptom that may indicate a serious medical complication, which may warrant immediate medical attention.

Q: Why do some sources mention two different medications for this process?

A: Official regimens for the approved use of the medicine typically define a combined regimen. This involves the administration of mifepristone, followed by a prostaglandin medication (such as misoprostol), as part of the sequential regimen used to complete the process.

Q: How quickly does the effect of Гинепристон start after taking the tablet?

A: Pharmacokinetic data from official sources describe the medicine's absorption rate. Evidence indicates that the active substance reaches its peak concentration in the bloodstream approximately 1.5 to 2 hours after it is administered.

Q: Does Гинепристон affect the menstrual cycle immediately afterward?

A: Official information indicates that a person's normal reproductive cycle, including ovulation and menstruation, can return relatively quickly after using the drug. Official documents note that conception is possible before the return of the next expected period.

Q: What does 'ectopic pregnancy' mean in the context of using this medicine?

A: An ectopic pregnancy is a serious medical condition where the fertilized egg implants outside the uterus. The use of this medicine is prohibited in such cases because it is only effective for pregnancies located within the uterus.

Q: What is the difference in how Гинепристон is used for different medical indications?

A: The official use protocols differ significantly. For one indication, the regimen requires a single, high dose. For the other indication, the drug is used as a long-term, daily, titrated maintenance regimen.

Q: How long does the primary active ingredient stay in the body after use?

A: Official pharmacokinetic data reports that the active substance has a long elimination half-life (the time it takes for half the drug to leave the body) of approximately 18 hours. Furthermore, some metabolites may persist in the plasma for several days.

Q: What is the general expectation for the amount of bleeding after taking the tablets?

A: Expected bleeding is generally described in official patient guides as being heavier than a normal menstrual period and often includes the passage of clots. Prolonged or excessively heavy bleeding is specifically documented as a serious safety risk.

Q: Why do official documents mention 'adrenal failure' as a condition where the drug should not be used?

A: The medicine has a secondary Antiglucocorticoid effect which acts by blocking the receptors for the stress hormone cortisol. Use is officially prohibited in patients with chronic adrenal failure because this action may destabilize and worsen their underlying condition.

Q: Why is it important to know how far along a pregnancy is before using Гинепристон?

A: Official indications for one use of the drug specify a maximum gestational age (the length of the pregnancy) for which the medicine is approved. Knowing the timing is necessary to ensure the medicine is used within its regulatory constraints.

Q: Why do patients sometimes experience fever or chills after the process?

A: Fever and chills are documented symptoms that may be associated with the rare but serious risk of bacterial infection, including sepsis, following the procedure. Patients are advised to monitor for these symptoms, even if other typical signs of infection are absent.

Q: Why do official instructions specify a certain window (e.g., 24-48 hours) for taking the second medicine?

A: Official instructions specify a timing interval for the second medication that is based on clinical evidence. Studies have demonstrated that administering the medications sequentially within this particular window provides the optimal effectiveness for the regimen.

Q: What is the significance of the tablet strength (e.g., 200 mg) mentioned in the official data?

A: The specific dose of 200 mg is the established therapeutic dose for one particular indication, and this strength distinguishes it from the variable, higher-dose regimen used for the other approved indication.

Q: What are the general research themes regarding the psychological effects of the process?

A: Official post-marketing surveillance reports may, in rare cases, note psychiatric side effects. However, the primary research themes in clinical trials focus on the drug's physical effects and reproductive health outcomes.

Q: What is the average time it takes for bleeding to start after taking the first tablet?

A: Clinical trial data reports that bleeding typically begins after the administration of the second medication in the regimen. However, official information also indicates that bleeding may occasionally start shortly after taking the first tablet.

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How should Гинепристон be stored and disposed of?

How to Store and Dispose of Ginepriston

Official regulatory labeling dictates strict conditions for storing Ginepriston (Mifepristone 10 mg) to maintain its quality and potency.


Storage Requirements

The medication must be stored at a temperature not exceeding 30°C. It is mandatory to keep the tablets in the original package to ensure consistent protection from light and moisture. For safety, the product must be kept out of the reach of children at all times.

Disposal Instructions

Unused or expired Ginepriston must not be discarded in household waste or flushed down the toilet, as this can affect the environment. Disposal must be completed through a recognized pharmaceutical take-back program or according to all local regulations for unused medicinal products. These rules ensure proper environmental handling of the medication.

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

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