Methylprednisolone

Methylprednisolone is a drug from the group of glucocorticoids. Methylprednisolone is a derivative of the substance prednisolone. Methylprednisolone is administered orally and intramuscularly and is indicated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, gastrointestinal, nervous, and other conditions.

These include:

• neurodermatitis, contact eczema, hives, psoriasis
• acute and chronic lung diseases such as bronchial asthma and COPD
• rheumatic diseases such as lupus erythematosus, vasculitis, arthritis
• Crohn's disease and ulcerative colitis

The efficacy of methylprednisolone in coronavirus-related pneumonia is currently being evaluated in clinical trials.

Methylprednisolone was first synthesized and manufactured by the Upjohn Company (now Pfizer) and approved by the FDA in the United States in October 1957. Methylprednisolone is also on the World Health Organization's list of essential medicines.

Pharmacodynamics

Corticosteroids are structurally related to endogenous cortisol and therefore can bind to glucocorticoid receptors. The short-term effects of corticosteroids are decreased vasodilation and permeability of capillaries and decreased migration of leukocytes to the site of inflammation. Binding of corticosteroids to the glucocorticoid receptor causes changes in gene expression that take time to exert their effects. Glucocorticoids also inhibit the enzyme phospholipase A2, which reduces the formation of arachidonic acid derivatives. These are responsible for various inflammatory reactions. They also inhibit the enzyme NF-Kappa B and other inflammatory transcription factors and promote the expression of anti-inflammatory genes such as interleukin- 10. Higher doses of corticosteroids have an immunosuppressive effect.

Pharmacokinetics

Oral methylprednisolone has a bioavailability of 90%. The average volume of distribution of methylprednisolone is approximately1.38 l/kg. Methylprednisolone is approximately 76% bound to human serum albumin in plasma. The substance is degraded in the liver and has a half-life of 2.3 hours.

Drug interactions

Interactions may occur with the following substances:

• Enzyme inducers such as phenobarbital and phenytoin.
• Cytochrome CYP 3A4 inhibitors such as troleandomycin, ketoconazole, and clarithromycin.
• Oral contraceptives may decrease methylprednisolone clearance
• Methylprednisolone may increase the rate of excretion with Cox1 inhibitors such as aspirin

Side effects

• Growth retardation in children
• Diabetes mellitus
• Disorders of lipid metabolism
• Cardiac arrhythmias
• Hypertension
• Steroid acne
• Nervousness
• Psychoses
• Depression

Contraindications

• Hepatitis
• Osteoporosis
• Infectious diseases of the skin caused by viruses, bacteria or fungi
• Untreated or refractory hypertension
• Untreated or poorly controlled diabetes mellitus
• Psychoses
• Pregnancy and lactation