Gynepristone

Gynepristone, also known as mifepristone, is a medicine used for medical abortion. It is an antiprogestagen, which means it blocks the action of progesterone, a hormone necessary to maintain pregnancy.

Mifepristone is usually used in combination with a prostaglandin (usually misoprostol), which helps cause the uterus to contract and cause the contents of the uterus to be expelled, leading to termination of pregnancy.

This medication can be used in a medical setting under strict supervision and guidance of a physician. It is often offered as an alternative to surgical abortion, especially in early pregnancy. In some countries, mifepristone can also be prescribed for medical abortion at home, but this requires strict adherence to instructions and supervision of a physician.

It is important to note that the use of mifepristone can have side effects and risks, so its use should only be carried out under the supervision of a qualified healthcare professional.

Indications Gynepristone

1. Medical termination of pregnancy: Mifepristone can be used for medical termination of pregnancy during the first 7-9 weeks of pregnancy. It is used in combination with a prostaglandin (usually misoprostol) to induce abortion.
2. Abortion due to miscarriage or embryonic death: In some cases, the pregnancy may stop on its own, but remains of the fetus may still remain in the uterus. In such cases, mifepristone may be used to help remove fetal debris.
3. Termination of a dangerous pregnancy: In rare cases, pregnancy can pose a risk to the mother's health. In such situations, mifepristone can be used to terminate a pregnancy.
4. Research Studies: Mifepristone may also be used in research studies related to abortion or its consequences.

Release form

Gynepristone, also known as mifepristone, is usually available in tablet form for oral use. This drug is used in medicine to terminate early pregnancy.

Usually, the method of use and dosage of Ginepristone (mifepristone) are determined by the doctor and may depend on the individual characteristics of the patient and the specific situation. However, in general terms, the use of the drug may look like this:

1. First dose: The patient usually takes one tablet of Gynepristone (mifepristone) under the supervision of a physician in a medical facility.
2. Second dose: Usually 24-48 hours after taking mifepristone, the patient takes a second dose of the drug - progesterone (usually misoprostol) - also under the supervision of a doctor.

It is important to remember that the establishment of dosage and regimen should only occur under the supervision of a qualified medical specialist. Patients should strictly follow the doctor's instructions and not change the dosage or regimen without his consent.

Pharmacodynamics

1. Mechanism of action:

   • Gynepristone is an antiprogesterone. It binds to progesterone receptors, blocking their activity.
   • Progesterone is necessary to maintain pregnancy, so blocking its receptors leads to the destruction of the endometrium (the inner layer of the uterus), which leads to rejection of the fetus or embryo.
   • Gynepristone also stimulates contraction of the uterine muscle, which helps expel the contents of the uterus.

2. Medical use:

   • For medical abortion: Gynepristone is often used in combination with prostaglandins (such as misoprostol) to induce abortion.
   • To treat hyperprolactinemia: Gynepristone can be used to reduce prolactin levels in the blood by blocking prolactin receptors in the pituitary gland.

3. Efficiency and safety:

   • Gynepristone is generally considered effective and safe for medical abortion, especially in the early stages of pregnancy. However, it is important to use it under the supervision of qualified medical personnel due to potential complications.
   • As with any medicine, side effects may occur, such as bleeding, abdominal pain, nausea and vomiting.

Pharmacokinetics

1. Absorption: Mifepristone is usually well absorbed from the gastrointestinal tract after oral administration. The time to reach maximum concentration in the blood is usually several hours.
2. Metabolism: Mifepristone is metabolized in the liver to form active and inactive metabolites. This mainly occurs through the processes of oxidation and hydroxylation.
3. Excretion: Mifepristone and its metabolites are usually excreted through bile and urine. The half-life from the body can be long, which is associated with a long half-life in the blood.
4. Interactions with food and other drugs: Food may affect the rate and extent of absorption of mifepristone. Some drugs may affect its metabolism and elimination, which may require dosage adjustments or monitoring.
5. Kinetics in different populations: The kinetics of mifepristone may vary in different populations, including pregnant women, the elderly, and patients with impaired liver or kidney function. This may require individualizing dosage or monitoring for side effects.

Dosing and administration

Gynepristone, also known as mifepristone, is commonly used to terminate early pregnancy. Here is a typical method of application and dosage:

1. First dose: Typically, the patient takes one tablet of Gynepristone (mifepristone) orally under the supervision of a physician in a medical facility. This usually occurs within the first days after pregnancy is confirmed.

2. Second dose: After a certain period of time (usually 24-48 hours) after taking mifepristone, the patient takes a second dose of progesterone medication, most often misoprostol, which helps complete the process of ending the pregnancy. This is also done under the supervision of a doctor.

Dosage and regimen may vary depending on the individual characteristics of the patient and the doctor’s recommendations. It is important for patients to strictly follow the doctor's instructions and not change the dosage or regimen without his consent. Before starting treatment with Gynepristone (mifepristone), it is recommended to discuss the possible risks and side effects with a healthcare professional.

Use Gynepristone during pregnancy

Mifepristone (also known as RU-486) is used for medical termination of early pregnancy. It is an antiprogesterone drug that blocks the action of progesterone, which is necessary to maintain pregnancy. In clinical studies, Mifepristone was used in combination with misoprostol to terminate pregnancies up to 9 weeks with high efficacy and good tolerability.

Uses of Mifepristone include:

1. Induction of cervical ripening before early surgical abortion.
2. Interruption of pregnancy in the first trimester by combination with prostaglandin for an effective medical abortion.

Studies show that mifepristone is effective for ending pregnancies up to 9 weeks. The success rate of abortion is about 92% up to 49 days and decreases to 77% at 57 to 63 days (Spitz et al., 1998). It is important to note that the use of Mifepristone is not recommended if the pregnancy is desired and it is planned to continue it, since this substance is intended to terminate it.

Contraindications

1. Confirmed or suspected pregnancy beyond the stated period: Mifepristone should not be used if pregnancy is already confirmed or suspected to be beyond the specified period for safe use of the drug.
2. Acute or chronic adrenal disease: Patients with acute or chronic adrenal disease may be at increased risk of complications when using mifepristone.
3. Corticosteroid use: Mifepristone should not be used in patients taking high doses of corticosteroids as this may increase the risk of adverse effects.
4. Taking anticoagulants: The use of mifepristone may increase the effect of anticoagulants, which increases the risk of bleeding.
5. Drug Hypersensitivity: People with a known hypersensitivity to mifepristone or any other component of the drug should avoid its use.
6. Presence of rare hereditary diseases such as porphyria: In these cases, the use of mifepristone may be contraindicated due to the potential for increased disease symptoms.

Side effects Gynepristone

1. Bleeding and Bleeding: Bleeding may occur after use of mifepristone and prostaglandins and may be severe or heavy.
2. Lower Abdominal Pain: Some women may experience pain or cramping in the lower abdomen, which may be accompanied by contractions.
3. Headache and dizziness: Some patients may experience headache or dizziness during or after the procedure.
4. Nausea and vomiting: These symptoms may also occur as a result of the use of mifepristone and prostaglandins.
5. Fatigue and weakness: Some women may feel tired or weak after the procedure.
6. Emotional changes: Some patients may experience emotional changes such as anxiety, sadness, or irritability.

Overdose

An overdose of Gynepristone (mifepristone) can have serious consequences and require immediate medical attention. Since gynepristone is used for medical purposes, its dosage and use should be strictly controlled by a doctor.

Overdose symptoms can be varied and may include uterine bleeding, abdominal pain, nausea, vomiting, dizziness, fainting and other unpleasant conditions.

Interactions with other drugs

1. Drugs affecting cytochrome P450: Mifepristone is metabolized in the liver through enzymes of the cytochrome P450 system. Drugs that are inhibitors or inducers of these enzymes can affect the metabolism of mifepristone and change its concentration in the blood. For example, cytochrome P450 inhibitors such as ketoconazole or rifampicin may increase or decrease mifepristone blood concentrations, which may require dosage adjustments.
2. Antihistamines: The use of mifepristone may enhance the sedative effects of antihistamines, which may lead to increased drowsiness.
3. Hormonal drugs: Mifepristone affects the hormonal balance in the body, so its use with other hormonal drugs, such as contraceptives or hormone replacement therapy, may lead to changes in the effectiveness of their actions.
4. Anticoagulants: Mifepristone may affect the metabolism of vitamin K, which may increase or decrease the effect of anticoagulants. Patients taking anticoagulants should consult a physician for dosage adjustments and monitoring.
5. Anti-cancer drugs: Interactions of mifepristone with anti-cancer drugs may result in changes in their effectiveness or toxicity. Patients with cancer should tell their doctor about all medications they are taking.

Storage conditions

1. Temperature: It is generally recommended to store Gynepristone at room temperature, between 20°C and 25°C. Slight deviation from these limits is sometimes acceptable, but it is important to avoid extreme temperatures.
2. Humidity: The drug should be stored in a dry place, protected from moisture. High humidity may affect the stability of the drug.
3. Light: Store Ginepristone in a dark place, away from direct sunlight. Light can degrade the active ingredients of the drug.
4. Packaging: Follow the instructions on the package to ensure proper storage of the drug.