Angelique

The drug "Angelique" is a combined hormonal drug containing two active ingredients: drospirenone and estradiol.

1. Drospirenone: This is a synthetic progestogen that is similar to natural progesterone, the female sex hormone. Drospirenone has androgen antagonist and antiandrogenic properties, making it useful in the treatment of hormonal disorders such as polycystic ovary syndrome and in reducing the symptoms of transient menopause.

2. Estradiol: This is a natural estrogen that is the main female sex hormone. It replenishes estrogen levels in the body and helps reduce menopausal symptoms such as hot flashes, sweating, sleep disturbances and mood changes.

Angelique is used to treat symptoms associated with estrogen deficiency in women before and during menopause. This medication helps relieve hot flashes, night sweats, mood changes, vaginal dryness, and other symptoms of menopause. In addition, Angelique can be used to prevent osteoporosis in postmenopausal women.

Indications Angelica

1. Symptoms of menopause: "Angelique" can help cope with hot flashes, night sweats, mood changes, insomnia, decreased sexual desire, dryness vaginal bleeding and other symptoms of menopause.
2. Preventing osteoporosis: In postmenopausal women, estrogen levels decrease, which can lead to thinning bones and an increased risk of osteoporosis. Angeliq may be prescribed to prevent osteoporosis and reduce the risk of fractures.
3. Treating polycystic ovary syndrome (PCOS): This condition can cause irregular menstrual cycles, hyperandrogenism (high levels of male sex hormones), and other symptoms. Angeliq with drospirenone may help manage PCOS symptoms.
4. Treatment of dysfunctional uterine bleeding: Angeliq may be used to treat dysfunctional uterine bleeding, which may occur in perimenopausal women due to changes in estrogen and progesterone levels.

Release form

Angelique is available in the form of tablets for oral (oral) administration. Each tablet contains a combination of two active ingredients: drospirenone (as drozepirone potassium) and estradiol (as estradiol hemihydrate). Tablets are usually packaged in blisters or bottles with instructions for use and dosage.

Pharmacodynamics

1. Drospirenone: Drospirenone is a synthetic progestogen that has androgen antagonistic and antiandrogenic properties. It binds to progesterone and estrogen receptors, which leads to suppression of the release of gonadotropins and a decrease in the production of hormones by the pituitary gland. This leads to a decrease in the production of estrogen by the testes, as well as a decrease in the production of androgens. In addition, drospirenone has the ability to reduce fluid retention in the body, which may help reduce swelling and other symptoms associated with water retention.
2. Estradiol: Estradiol is a natural estrogen and the main female sex hormone. It penetrates target cells, binds to estrogen receptors and is involved in the regulation of many processes in the body. The estrogens in Angelica help replenish the estrogen deficiency that occurs in women before and during menopause and help reduce menopausal symptoms such as hot flashes, sweating, mood changes and vaginal dryness.

Together, drospirenone and estradiol in Angelica provide a complex effect on the body aimed at reducing the symptoms of menopause and preventing complications associated with estrogen deficiency.

Pharmacokinetics

1. Drospirenone:

   • Absorption: Drospirenone after oral administration is well absorbed from the gastrointestinal tract.
   • Metabolism: It undergoes metabolic transformations in the liver with the formation of active metabolites.
   • Excretion: Drospirenone metabolites are excreted mainly through the kidneys and partly through the intestines.

2. Estradiol:

   • Absorption: Estradiol is also well absorbed after oral administration.
   • Metabolism: It is metabolized in the liver to form various metabolites, including estrone and estriol.
   • Excretion: Estradiol metabolites are excreted mainly through the kidneys and intestines.

Dosing and administration

• Dosage: The standard dosage of "Angelica" is one tablet per day. It is usually taken for 28 days, followed by a break of 7 days, during which periods usually appear. After a pause, a new course of treatment begins.
• Dosage: Tablets should be taken orally with a sufficient amount of water. It is best to take the tablets at the same time every day, this will help maintain a constant level of active components in the body.

When choosing the dosage and regimen of Angelica, it is necessary to take into account the patient’s age, the presence of concomitant diseases, the severity of menopausal symptoms and other individual characteristics.

Use Angelica during pregnancy

1. Effect on pregnancy:

   • Research has shown that the combination of drospirenone and estradiol is not intended for use during pregnancy. Drugs containing drospirenone and estradiol are used for hormone replacement therapy in postmenopausal women and should not be prescribed to pregnant women (Zhou et al., 2011).

2. Risks to the fetus:

   • Taking hormones during pregnancy can lead to teratogenic effects and fetal abnormalities. This is due to the fact that estradiol can affect hormonal balance and the development of the fetal reproductive system (Gaspard & van den Brûle, 2004).

3. Recommendations for use:

   • Angelique is not intended for use in pregnant women. The drug is indicated for the treatment of menopausal symptoms in postmenopausal women and is not indicated for use during pregnancy (Foidart, 2005).

Contraindications

1. Confirmed or suspected breast cancer: Angelica is contraindicated in women with or suspected of having breast cancer.
2. Cancer of estrogen-dependent organs: The drug is also contraindicated in cancer of estrogen-dependent organs, such as the endometrium or ovaries.
3. Severe liver disease: In patients with severe liver disease, the use of Angelica may be contraindicated due to the risk of deterioration of liver function.
4. Severe kidney disease: The drug may also be contraindicated in severe kidney disease, especially if there is significant impairment of kidney function.
5. Thrombosis and thromboembolism: Angeliq should not be used in patients with a high risk of thrombosis or thromboembolism, such as a history of thrombosis or the presence of hereditary bleeding disorders.
6. Severe atherosclerotic diseases: The drug is also contraindicated in severe atherosclerotic diseases, such as acute myocardial infarction or stroke.
7. Hypertension: Patients with severe uncontrolled hypertension may also have restrictions on the use of Angelica.
8. Manifestation of an allergic reaction to the components of the drug: If the patient has previously had an allergic reaction to drospirenone, estradiol or other components of Angelica, its use is also contraindicated.

Side effects Angelica

1. Headache: Headache or migraine may occur.
2. Hot flashes: Women may experience hot flashes or sweating.
3. Mood Changes: Some patients may notice mood changes, including depression or irritability.
4. Sleep disorders: Insomnia or drowsiness may occur.
5. Breast pain: Some women may experience pain or discomfort in the breast area.
6. Abdominal pain: Lower abdominal pain or abdominal discomfort may occur.
7. Nausea and vomiting: Nausea or vomiting may occur in some patients.
8. Vaginal bleeding or discharge: Menopausal women may experience irregular vaginal bleeding or discharge.
9. Swelling: Swelling may occur, especially in the lower extremities.
10. Joint or muscle pain: Some patients may experience joint or muscle pain.
11. Hypertension: Some patients may experience increased blood pressure.
12. Weight changes: Weight changes, both increase and decrease, may occur.
13. Changes in laboratory values: Changes in laboratory values, such as blood lipid levels or liver function, may occur.

Overdose

1. Hormonal side effects:

   • Estradiol: Overdosing on estradiol can cause nausea, vomiting, headaches, breast tenderness, fluid retention, and vaginal bleeding.
   • Drospirenone: An overdose of drospirenone can lead to hyperkalemia (increased potassium levels in the blood), which can cause muscle weakness, fatigue, arrhythmias (irregular heart rhythms).

2. Other side effects:

   • Dizziness
   • Stomach pain
   • Nausea and vomiting
   • Increased blood pressure

Interactions with other drugs

1. Medicines containing cyclosporine: These drugs may increase the concentration of estrogen in the blood, which may increase the side effects of Angelica.
2. Anti-epileptic drugs (for example, phenytoin, carbamazepine): These may reduce the effectiveness of Angelica, so dosage adjustment may be necessary in some cases.
3. Medicines containing topiramate: They may also reduce the effectiveness of Angelica.
4. Medicines containing rifampicin: This antibiotic may reduce the concentration of estrogen in the blood, which may reduce the effectiveness of Angelica.
5. Medicines containing thyroxine: These may increase the binding of hormones, thereby increasing the risk of side effects.
6. Drugs containing cyclic antidepressants (for example, amitriptyline): They may increase the risk of developing hyponatremia when used together with Angeliq.
7. Drugs containing warfarin: May increase the risk of thromboembolic complications.