methylprednisolone

Action and Spectrum

Actions and spectrum: 

methylprednisolone is a synthetic glucocorticoid medication that exhibits anti-inflammatory, immunosuppressive, and anti-allergic actions. It is a potent corticosteroid with a broad spectrum of activities.

It acts by inhibiting inflammatory mediators’ production, suppressing immune responses, and reducing swelling, redness, and itching associated with various conditions.

methylprednisolone is used to treat a wide range of medical conditions, including allergic reactions, asthma, rheumatoid arthritis, skin disorders, and certain autoimmune diseases. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Adrenal suppression 

Delayed wound healing 

Diabetes mellitus 

Emotional instability 

Fluid retention 

Glucose intolerance 

Hallucinations 

Hepatomegaly 

Hypokalemic alkalosis 

Insomnia 

Menstrual irregularity 

Neuritis 

Peptic ulcer 

Pituitary adrenal axis suppression 

Pseudotumor cerebri 

Sodium and water retention 

Tachycardia 

Vertigo 

Acne 

Amenorrhea 

Delirium 

Edema 

Erythema 

GI perforation 

Growth suppression 

Headache 

Hepatitis 

Increased transaminases 

Leukocytosis 

Myopathy 

Osteoporosis 

Perianal pruritus 

Protein catabolism 

Psychosis 

Seizure 

Ulcerative esophagitis 

Vasculitis 

Weight gain 

Black Box Warning

Black Box Warning: 

methylprednisolone does not have a specific black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: methylprednisolone should not be used in individuals who have a known hypersensitivity or allergy to the drug or any of its components. 
• Systemic fungal infections: The use of methylprednisolone is contraindicated in the presence of systemic fungal infections, as corticosteroids can exacerbate these infections. 
• Live vaccines: Administration of live vaccines should be avoided in patients receiving high doses of methylprednisolone due to the risk of inadequate immune response to the vaccine. 
• Active viral or bacterial infections: methylprednisolone can suppress the immune system, and its use is avoided during active viral or bacterial infections, unless specifically indicated by a healthcare provider. 
• Untreated tuberculosis: methylprednisolone should not be used in individuals with untreated tuberculosis, as it can lead to the dissemination of the infection. 
• Varicella (chickenpox) infection: methylprednisolone should be avoided in individuals with varicella infection, as it can lead to severe complications. 
• Herpes simplex eye infections: methylprednisolone should not be used in individuals with herpes simplex eye infections, as it can worsen the condition. 
• Diverticulitis: methylprednisolone is contraindicated in patients with diverticulitis due to the risk of perforation. 

Caution: 

• Infections: Corticosteroids can suppress the immune system, making patients more susceptible to infections. Caution is needed when using methylprednisolone in individuals with a history of infections or in those who are at risk for acquiring infections. 
• Glaucoma and cataracts: Prolonged use of methylprednisolone can increase intraocular pressure, leading to the development or worsening of glaucoma. Caution is needed in patients with a history of glaucoma or cataracts. 
• Mental health disorders: methylprednisolone can cause mood changes and behavioral disturbances. Caution is advised in patients with a history of mental health disorders. 
• Vaccinations: Live vaccines should be avoided while on high doses of methylprednisolone, as the response to the vaccine may be diminished. 
• Pregnancy and lactation: methylprednisolone should be used with caution during pregnancy and breastfeeding.  
• Withdrawal: Abruptly stopping methylprednisolone after prolonged use can lead to adrenal insufficiency. Therefore, the medication should be tapered off gradually under medical supervision.

Comorbidities: 

• Diabetes: methylprednisolone can increase blood glucose levels, which may be problematic for individuals with diabetes or those at risk of developing diabetes. 
• Hypertension: Corticosteroids like methylprednisolone can cause sodium and fluid retention, potentially leading to elevated blood pressure. Caution is needed in patients with hypertension or a history of cardiovascular disease. 
• Osteoporosis: Long-term use of methylprednisolone can lead to bone loss and osteoporosis. Patients with a history of osteoporosis or those at risk for it require careful monitoring. 
• Peptic ulcer disease: Methylprednisolone can exacerbate peptic ulcers or increase the risk of developing ulcers. Caution is advised in patients with a history of gastric ulcers or other gastrointestinal issues. 
• Glaucoma and cataracts: Prolonged use of methylprednisolone can increase intraocular pressure, leading to the development or worsening of glaucoma. Caution is needed in patients with a history of glaucoma or cataracts. 
• Tuberculosis: Corticosteroids can exacerbate latent tuberculosis or increase the risk of reactivation. Patients with a history of tuberculosis or exposure to tuberculosis should be carefully evaluated before starting methylprednisolone. 
• Liver disease: methylprednisolone is primarily metabolized in the liver, so caution is needed in patients with liver impairment. 
• Renal impairment: methylprednisolone is excreted by the kidneys, and its dosage may need to be adjusted in patients with renal impairment. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: C 

Lactation: Excreted into human milk: Yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

methylprednisolone is a synthetic glucocorticoid with anti-inflammatory, immunosuppressive, and anti-allergic properties. It acts by binding to intracellular glucocorticoid receptors which leads to the modulation of gene transcription and protein synthesis.

It suppresses the production of pro-inflammatory cytokines and mediators, inhibits leukocyte migration and phagocytosis, and reduces capillary permeability. methylprednisolone is used to treat a variety of conditions, including inflammation, allergies, autoimmune diseases, and certain cancers. It is available in various formulations, including oral tablets, injectable solutions, and topical preparations.  

Pharmacodynamics: 

• Anti-inflammatory effects: methylprednisolone binds to glucocorticoid receptors in inflammatory cells and modulates the transcription of various genes involved in inflammation. This leads to the suppression of pro-inflammatory mediators, such as interleukins, tumor necrosis factor-alpha (TNF-α), and prostaglandins. As a result, the inflammatory response is attenuated, reducing redness, swelling, and pain associated with inflammation. 
• Immunosuppressive effects: By binding to glucocorticoid receptors in immune cells, methylprednisolone inhibits the production of various immune cells, including lymphocytes, monocytes, and eosinophils. This action reduces the body’s immune response and helps control autoimmune reactions, preventing the immune system from attacking its own tissues. 
• Antiallergic effects: methylprednisolone can suppress the activity of immune cells responsible for allergic reactions, including mast cells and eosinophils. By inhibiting the release of histamine and other inflammatory mediators from these cells, methylprednisolone helps alleviate allergy symptoms. 
• Anti-proliferative effects: methylprednisolone can slow down cell division and growth in certain tissues, including lymphoid and connective tissues. This property makes it useful in the treatment of some types of cancer and autoimmune disorders. 
• Metabolic effects: methylprednisolone influences carbohydrate, protein, and fat metabolism. It can increase blood glucose levels by promoting glucose production in the liver (gluconeogenesis) and reducing glucose uptake by peripheral tissues. Additionally, it enhances the storage of fat and reduces the utilization of proteins, leading to potential weight gain and muscle weakness. 
• Sodium and water retention: methylprednisolone can cause the kidneys to retain water and sodium, leading to fluid retention and edema. This effect is more prominent in high doses or prolonged therapy.

Pharmacokinetics: 

Absorption 

methylprednisolone can be administered through various routes, including oral, intravenous (IV), intramuscular (IM), and topical. When taken orally, it is absorbed in the gastrointestinal tract. The oral bioavailability of methylprednisolone is about 80-90%, meaning that a significant portion of the drug reaches the systemic circulation after oral administration. 

Distribution 

After absorption, methylprednisolone is transported throughout the body by the bloodstream. It has a moderate to high protein-binding capacity, primarily binding to plasma proteins, particularly albumin. The drug crosses blood-brain barrier and placental barrier, which may be relevant in certain clinical situations. 

Metabolism 

methylprednisolone undergoes hepatic metabolism, primarily in the liver, where it is converted into various metabolites. The main metabolic pathway involves the enzymatic action of cytochrome P450 (CYP) enzymes, particularly CYP3A4. These metabolites are mostly inactive and are eventually excreted from the body. 

Elimination and excretion 

The metabolites of methylprednisolone, along with a small fraction of unchanged drug, are primarily eliminated through the kidneys. The drug and its metabolites get excreted in the urine. A small amount of methylprednisolone is also excreted in the feces through biliary excretion. 

Adminstartion

Administration: 

• Oral (by mouth): methylprednisolone is available in tablet and liquid (syrup) forms for oral administration. The tablets are usually taken with a full glass of water. It is essential to follow the prescribed dose and dosing schedule given by the healthcare provider. 
• Intravenous (IV): methylprednisolone can be given intravenously as a solution directly into the bloodstream. IV administration is often used in emergency situations or when a rapid effect is required. 
• Intramuscular (IM): In some cases, methylprednisolone may be injected into the muscle. This route is less common and typically used when the oral or IV route is not feasible. 
• Topical: methylprednisolone is available as creams, ointments, and lotions for topical application to the skin. It is used to treat certain skin conditions, and the affected area should be clean and dry before applying the medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: methylprednisolone 

Pronounced: (meth-uhl-pred-NIS-oh-lohn)  

Why do we use Methylprednisolone? 

• Allergic Reactions: methylprednisolone can be used to manage severe allergic reactions, including anaphylaxis. 
• Asthma: It is used as a short-term treatment for acute exacerbations of asthma to reduce inflammation and bronchospasm. 
• Inflammatory Conditions: methylprednisolone is effective in treating various inflammatory conditions such as rheumatoid arthritis, osteoarthritis, tendonitis, bursitis, and synovitis. 
• Skin Disorders: It is used to treat skin conditions like eczema, psoriasis, and allergic dermatitis. 
• Autoimmune Diseases: methylprednisolone is employed in the management of autoimmune disorders like systemic lupus erythematosus (SLE) and multiple sclerosis (MS). 
• Respiratory Disorders: It is used to treat respiratory conditions such as chronic obstructive pulmonary disease. 
• Organ Transplantation: methylprednisolone is used to prevent organ rejection in transplant recipients. 
• Inflammatory Bowel Disease: It is used to manage flare-ups in patients with ulcerative colitis or Crohn’s disease. 
• Certain Cancers: In some cases, methylprednisolone is used as part of the treatment for certain cancers, such as lymphoma and leukemia. 
• Adrenal Insufficiency: In cases of adrenal insufficiency, methylprednisolone can be used as a replacement therapy for inadequate natural steroid production by the adrenal glands.