Methylprednisolone

Methylprednisolone is a synthetic glucocorticosteroid that is widely used in medical practice to treat various inflammatory and allergic conditions. Here is a brief characterization of this drug:

1. Anti-inflammatory action: Methylprednisolone has a strong anti-inflammatory effect. It inhibits inflammatory reactions in the body by blocking the synthesis and release of inflammatory mediators.
2. Immunosuppressive action: The drug can suppress the immune system, which is especially important in the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus.
3. Allergic reactions: Methylprednisolone is effective in treating allergic reactions such as allergic dermatitis, asthma, and allergic rhinitis.
4. Other indications: The drug can also be used in the treatment of diseases of the organs of vision, skin diseases, cancer and other pathologies.
5. Dosageforms: Methylprednisolone is available in a variety of forms including tablets, injections, eye drops, ointments and skin creams.
6. Undesirable effects: The drug may cause various side effects such as hypertension, hyperglycemia, osteoporosis, decreased immunity and others. Therefore, it should be used under the supervision of a doctor.
7. Contraindications: Methylprednisolone is not recommended in pregnancy, infectious diseases, fungal infections, gastric and duodenal ulcers, and high blood pressure.

It is important to consult your doctor before starting methylprednisolone to evaluate the indications for its use, dosage, and possible side effects.

Indications Methylprednisolone

1. Inflammatory joint diseases: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis and other inflammatory joint diseases.
2. Allergicdiseases: Allergic rhinitis, allergic dermatitis, allergic asthma and allergic reactions to medicines.
3. Collagenoses: Systemic lupus erythematosus, dermatomyositis, systemic sclerosis and other collagenoses.
4. Skin diseases: Dermatitis, psoriasis, eczema and other skin inflammatory processes.
5. Respiratory diseases: Bronchial asthma, obstructive bronchitis and other respiratory diseases with an allergic or inflammatory basis.
6. Oncological diseases: Treatment of tumors, especially leukemia, lymphoma, myeloma and other malignant tumors.
7. Organ transplants: Prevention and treatment of graft rejection.
8. Autoimmune diseases: Treatment of diseases such as Crohn's disease, sarcoidosis and other autoimmune diseases.

Release form

1. Oral tablets: This is the most commonly used form of methylprednisolone, convenient for long-term treatment at home. Tablets may have different dosage of the active ingredient.
2. Solution for injection: Used for rapid action in acute conditions, including emergencies. The solution can be intended for both intramuscular (v/m) and intravenous (v/v) administration.
3. Lyophilizate for preparation of solution for injection: Powder from which a solution is prepared for intramuscular or intravenous administration. It is used in hospital settings for accurate dosing and for individual dose adjustment if necessary.
4. Suspension for injection: Injection of the suspension provides a longer duration of action of the drug, which may be preferable for some treatment conditions.

Pharmacodynamics

1. Anti-inflammatory action:

   • Methylprednisolone suppresses inflammation by inhibiting the production of prostaglandins and other inflammatory mediators such as leukotrienes and cytokines. It also inhibits the migration of leukocytes to areas of inflammation, reducing phagocytosis and the release of inflammatory mediators.

2. Immunosuppressive action:

   • Methylprednisolone suppresses the body's immune system by reducing the activity of lymphocytes, monocytes, macrophages and other cells responsible for the immune response. This property makes it useful in the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus, as well as in transplantology to prevent transplant rejection.

3. Anti-allergic action:

   • Methylprednisolone reduces the production of allergic mediators such as histamine and suppresses the body's response to allergens. This makes it an effective treatment for allergic reactions as well as asthma and allergic rhinitis.

4. Metabolic effects:

   • Methylprednisolone can cause a number of metabolic effects such as increased gluconeogenesis and glycogenolysis, which can lead to hyperglycemia. It can also cause sodium and water retention in the body, decreased collagen synthesis and increased membrane calcium permeability.

5. Other effects:

   • Methylprednisolone can also affect many other body systems, including the endocrine, cardiovascular, gastrointestinal, and nervous systems.

Pharmacokinetics

1. Absorption: Methylprednisolone is usually well absorbed from the gastrointestinal tract after oral administration. Absorption may be delayed when taken with food.
2. Distribution: It is well distributed in the body and can penetrate many barriers, including the plasma-brain barrier. It binds to plasma proteins to varying degrees, which may vary depending on the concentration of the drug.
3. Metabolism: Methylprednisolone is metabolized in the liver to form active and inactive metabolites, which can then be excreted by the kidneys or through the bile.
4. Excretion: It is excreted mainly through the kidneys as metabolites. A small proportion is excreted through the bile.
5. Half-life: The half-life of methylprednisolone is about 2-3 hours, which means that its effects disappear quickly after discontinuation.
6. Metabolism of substances: Methylprednisolone may affect the metabolism of other drugs, especially those metabolized in the liver via cytochrome P450.

Dosing and administration

Oral tablets

• Dosage: The starting dose for adults is usually 4 mg to 48 mg per day depending on the specific disease. The dosage may be adjusted by the doctor depending on the response to treatment.
• Use: Tablets should be taken with food or milk to minimize stomach irritation. The dosage may be divided into several meals throughout the day, depending on the doctor's recommendations.

Solution for injection and lyophilizate for preparation of solution

• Intravenous (IV) and intramuscular (IM) administration: The dosage and frequency of administration will be determined by a physician depending on the condition. Acute conditions may require a single high dose; chronic conditions may require regular lower doses.
• Use: Intravenous administration should be done slowly. V/m injections are administered into deep muscle tissues.

Suspension for injection

• Intramuscular use: Suspension provides a longer duration of action. The dosage is determined individually.

Special Instructions

• To avoid a "withdrawal syndrome", long-term treatment with methylprednisolone should be completed with a gradual reduction in dose.
• With long-term use, monitoring of bone health, blood sugar levels, blood pressure and adrenal function is necessary.
• The use of glucocorticoids may increase the risk of infections, especially with high doses or prolonged therapy.

Use Methylprednisolone during pregnancy

When using methylprednisolone during pregnancy, the physician should evaluate the benefits of its use compared to the potential risks to the fetus and mother. The decision to use methylprednisolone during pregnancy should be individualized and based on a careful analysis of all factors, including the condition of the mother and fetus, as well as possible alternative therapies.

It is usually preferable to minimize the use of glucocorticosteroids to the necessary minimum during pregnancy, especially in the early stages of pregnancy when fetal organogenesis is most active. However, in some cases, methylprednisolone may be prescribed by a physician for the treatment of serious conditions in the mother that may pose a threat to her health or life.

Contraindications

1. Fungal infections: The use of methylprednisolone may provoke the growth of fungal infections. Therefore, it should not be used in the presence of fungal infections without a doctor's prescription.
2. Viral infections: Methylprednisolone can depress the immune system, making the body more vulnerable to viral infections. Use of methylprednisolone can make viral infections such as herpes or chickenpox worse or spread.
3. Tuberculosis: Glucocorticosteroids, including methylprednisolone, may mask the symptoms of tuberculosis and exacerbate its course. Therefore, the use of methylprednisolone may be contraindicated in patients with active tuberculosis or a positive tuberculin test.
4. Systemic fungal infections: Methylprednisolone is contraindicated in patients with systemic fungal infections such as coccidiomycosis and histoplasmosis because it may promote their spread and worsen the course of infection.
5. Uncontrolled arterial hypertension: The use of methylprednisolone may lead to an increase in blood pressure, therefore its use may be contraindicated in patients with uncontrolled arterial hypertension.
6. Mental Disorders: Methylprednisolone may exacerbate or cause psychiatric disorders such as depression, aggression, or anxiety, so it should be used with caution in patients with a predisposition to these conditions.
7. Pregnancy and breastfeeding: The use of methylprednisolone during pregnancy may be contraindicated due to potential adverse effects on the fetus. If use during breastfeeding is necessary, the woman should consult a physician.

Side effects Methylprednisolone

1. Increased blood pressure: Methylprednisolone may increase blood pressure, which is especially important for patients with hypertension.
2. Hyperglycemia: This drug can increase blood glucose levels, which can be problematic for people with diabetes.
3. Osteoporosis: Long-term use of glucocorticosteroids can lead to osteoporosis, increasing the risk of bone fractures.
4. Immunosuppression: Methylprednisolone suppresses the immune system, which may increase the risk of infections and delay wound healing.
5. Weight changes: Methylprednisolone may cause weight changes, including weight gain or loss, in some people.
6. Mood changes: Glucocorticosteroids can cause mental side effects such as irritability, insomnia, depression, or euphoria.
7. Gastrointestinal problems: Long-term use of methylprednisolone may cause stomach ulcers, bleeding from the gastrointestinal tract, or other problems.
8. Increased risk of cataracts: Prolonged use of glucocorticosteroids may increase the risk of cataracts.

Overdose

1. Increasedside effects: Existing side effects of methylprednisolone such as hyperglycemia (high blood sugar), increased blood pressure, sodium and water retention in the body, osteoporosis, glucocorticoid induced hypertension, decreased immunity and others may be increased.
2. Hyperglycemia: An overdose of methylprednisolone can cause a significant increase in blood glucose levels (hyperglycemia), which is especially dangerous for people with or predisposed to diabetes.
3. Hypertension: Increased blood pressure may occur, which may lead tohypertensive crisis or other cardiovascular complications.
4. Electrolyte disturbances: Overdose may cause electrolyte imbalances, including retention of sodium and water in the body and increased excretion of potassium and calcium.
5. Other side effects: Other side effects such as decreased immunity, weight gain, gastrointestinal problems, hypothyroidism, myopathies, etc. Are possible.

Interactions with other drugs

1. Drugs that increase hyperglycemia: Methylprednisolone may increase blood glucose levels. Use with other medicines such as glucocorticosteroids, diuretics, thyroid hormones or sugar preparations may increase this effect.
2. Drugs that increase the risk of peptic ulcer disease: Methylprednisolone may increase the risk of peptic ulcer disease. Use with certain NSAIDs (e.g. Aspirin, ibuprofen), anticoagulants (e.g. Warfarin) or corticosteroids may increase this risk.
3. Drugs that increase the risk of infections: Methylprednisolone may increase the risk of infections. Use with other immunosuppressive drugs or drugs that suppress the immune system (e.g. Cyclosporine) may increase this effect.
4. Drugs that increase the risk of osteoporosis: Long-term use of methylprednisolone may lead to osteoporosis. Use with other medicines such as anticonvulsants or calcium-containing medicines may increase this risk.
5. Drugs affecting electrolyte balance: Methylprednisolone may cause retention of sodium and water in the body. Use with other medicines such as diuretics or potassium-containing medicines may alter electrolyte balance.
6. Drugs affecting hormonal status: Methylprednisolone may affect the function of hypothalamus and pituitary gland. Use with other medicines, such as antiepileptic drugs or hormonal preparations, may lead to disturbances in hormonal balance.