Angelique

The drug "Anzhelik" 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 antiandrogen 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, which is the main female sex hormone. It compensates for the lack of estrogen 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 drug helps to cope with hot flashes, night sweats, mood changes, vaginal dryness and other manifestations of menopause. In addition, "Angelique" can be used to prevent osteoporosis in postmenopausal women.

Indications Angelica

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

Release form

"Anzhelik" is available as tablets for oral (by mouth) administration. Each tablet contains a combination of two active ingredients: drospirenone (as drozepiron potassium) and estradiol (as estradiol hemihydrate). The 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 antagonist and antiandrogen properties. It binds to progesterone and estrogen receptors, which results in suppression of gonadotropin release and decreased pituitary hormone production. This results in decreased estrogen production by the testicles, as well as decreased androgen production. In addition, drospirenone has the ability to reduce fluid retention in the body, which can help in reducing edema and other symptoms associated with water retention in the body.
2. Estradiol: Estradiol is a natural estrogen and the primary female sex hormone. It penetrates target cells, binds to estrogen receptors, and is involved in regulating many processes in the body. The estrogens in Angelica help to compensate for the estrogen deficiency that women experience 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 is well absorbed from the gastrointestinal tract after oral administration.
   • Metabolism: It undergoes metabolic transformations in the liver to form active metabolites.
   • Excretion: Drospirenone metabolites are excreted mainly via the kidneys and partly via 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 primarily via the kidneys and intestines.

Dosing and administration

• Dosage: The standard dosage of "Anzhelika" is one tablet per day. It is usually taken for 28 days, followed by a 7-day break, during which menstruation usually appears. After the break, a new course of administration begins.
• Directions for use: Tablets should be taken orally with plenty 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 for taking "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. Impact on pregnancy:

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

2. Risks to the fetus:

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

3. Recommendations for use:

   • Angeliq is not intended for use in pregnant women. It 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 breast cancer or in women suspected of having this disease.
2. Cancers of estrogen-dependent organs: The drug is also contraindicated in cancers 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 in the presence of significant impairment of their 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 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 limitations in the use of Angelika.
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 disturbances: Insomnia or drowsiness may occur.
5. Breast pain: Some women may experience pain or discomfort in the breast area.
6. Abdominal pain: You may experience pain in the lower abdomen or discomfort in the abdomen.
7. Nausea and vomiting: Nausea or vomiting may occur in some patients.
8. Vaginal bleeding or discharge: Women going through menopause may experience irregular vaginal bleeding or discharge.
9. Edema: Edema 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 high blood pressure.
12. Weight changes: Weight changes, both increase and decrease, may occur.
13. Changes in laboratory tests: Changes in laboratory tests 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: Overdose of drospirenone may lead to hyperkalemia (increased potassium levels in the blood), which may cause muscle weakness, fatigue, arrhythmia (abnormal heart rhythms).

2. Other side effects:

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

Interactions with other drugs

1. Medicines containing cyclosporine: These medicines can increase the concentration of estrogens in the blood, which can lead to increased side effects of "Angelica".
2. Antiepileptic drugs (eg, phenytoin, carbamazepine): They may reduce the effectiveness of Angelika, so in some cases a dosage adjustment may be required.
3. Drugs containing topiramate: They may also reduce the effectiveness of Angelica.
4. Medicines containing rifampicin: This antibiotic can reduce the concentration of estrogens in the blood, which can reduce the effectiveness of Angelica.
5. Thyroxine-containing medications: These may increase hormone binding, thus increasing the risk of side effects.
6. Medicines containing cyclic antidepressants (eg, amitriptyline): These may increase the risk of hyponatremia when used in combination with Angelique.
7. Warfarin-containing drugs: May increase the risk of thromboembolic complications.