Methylprednisolone: Difference between revisions

Methylprednisolone
INN
Drug class
Routes of administration	By mouth, intramuscular, intra-articular, intravenous
Pregnancy category
Bioavailability
Metabolism	Liver (CYP3A4)
Elimination half-life	1.8–2.6 hours
Excretion	Urine
Legal status
CAS Number	83-43-2
PubChem	6741
DrugBank	DB00959
ChemSpider
KEGG

Latest revision as of 01:58, 20 March 2025

Corticosteroid medication

Methylprednisolone is a synthetic glucocorticoid primarily used for its anti-inflammatory and immunosuppressive properties.

Methylprednisolone is on the World Health Organization’s List of Essential Medicines.

Medical Uses[edit]

Methylprednisolone is prescribed for a variety of conditions, including:

Inflammatory and Autoimmune Disorders

Allergic and Respiratory Conditions

Severe allergies – including angioedema and anaphylaxis.
Asthma and COPD exacerbations – Used as an oral or IV corticosteroid in severe cases.

Endocrine and Oncological Uses

Adrenal insufficiency – As an alternative to hydrocortisone when mineralocorticoid activity is not required.
Cancer therapy – Used in the management of leukemia, lymphoma, and multiple myeloma.

Neurological Disorders

Multiple sclerosis (MS) relapses – Administered as high-dose IV methylprednisolone.
Spinal cord injury (off-label) – Used to reduce inflammation in acute cases.

Ophthalmic Conditions

Optic neuritis (often linked to MS)
Uveitis, iritis, and scleritis

Administration and Dosage[edit]

Methylprednisolone is available in oral tablets, intramuscular, intra-articular, and intravenous formulations. Dosage depends on the condition being treated:

Mild to moderate inflammation – 4–16 mg/day (oral)
Severe inflammation or autoimmune flares – IV pulse therapy (e.g., 500–1000 mg IV)
Acute asthma exacerbation – 40–80 mg/day PO or IV

Side Effects[edit]

Common Side Effects

Weight gain
Mood changes (insomnia, agitation)
Increased blood sugar levels (hyperglycemia)
Fluid retention

Serious Adverse Effects Long-term or high-dose use may lead to:

Osteoporosis and fractures
Adrenal suppression (requiring tapering)
Glaucoma and cataracts
Cushing’s syndrome (moon face, buffalo hump)
Infections due to immune suppression

Pharmacology[edit]

Mechanism of Action Methylprednisolone is a glucocorticoid receptor agonist that: 1. Suppresses inflammation by inhibiting pro-inflammatory cytokines (IL-1, IL-6, TNF-alpha). 2. Suppresses the immune response by reducing T-cell activation. 3. Regulates metabolism by increasing glucose levels and altering fat distribution.

Metabolism and Elimination

Metabolized in the liver (CYP3A4 pathway).
Eliminated via the kidneys.
Half-life: 1.8–2.6 hours.

Contraindications[edit]

Methylprednisolone should not be used in:

Systemic fungal infections
Uncontrolled infections
Hypersensitivity to corticosteroids
Live vaccine administration

Drug Interactions[edit]

NSAIDs – Increased risk of gastric ulcers.
Diabetes medications – May require higher insulin doses.
Live vaccines – Risk of severe infection.
Anticoagulants – May alter warfarin levels.

History[edit]

Methylprednisolone was first synthesized by The Upjohn Company (now Pfizer) and FDA-approved in 1957.

Availability[edit]

Methylprednisolone is available under multiple brand names:

Medrol (oral tablets)
Depo-Medrol (intramuscular injection)
Solu-Medrol (intravenous formulation)

@@ Line 1: / Line 1: @@
-{{intro}}
+{{Short description|Corticosteroid medication}}
-[[File:Methylprednisolone suleptanate.svg|thumb|Methylprednisolone suleptanate]] [[File:Sandoz.Methylprednisolone.4mg.jpg|thumb|Sandoz.Methylprednisolone.4mg]]
+{{Use dmy dates|date=March 2022}}
-[[File:Medrol, 32 mG methylprednisolone tablets by Pfizer which are made in Romania.jpg|thumb|Medrol, 32 mG methylprednisolone tablets by Pfizer which are made in Romania]]
+{{cs1 config |name-list-style=vanc |display-authors=6}}
-'''Methylprednisolone''' is a synthetic, intermediate-acting [[glucocorticoid]] that is widely used in the treatment of severe inflammation, autoimmune conditions, hypersensitivity reactions, and organ rejection. Its potent anti-inflammatory and immunosuppressive properties make it a valuable drug in the management of these conditions.
-== Pharmacology and Mechanism of Action ==
+{{Infobox drug
+| verifiedrevid = 4771699945
+| image = Methylprednisolone.svg
+| image_class = skin-invert-image
+| width = 250
+| tradename = Medrol, Depo-Medrol, Solu-Medrol
+| Drugs.com = {{drugs.com|monograph|methylprednisolone}}
+| MedlinePlus = a682795
+| DailyMedID = Methylprednisolone
+| pregnancy_AU = A
+| pregnancy_US = C
+| routes_of_administration = [[Oral administration|By mouth]], [[intramuscular]], [[intra-articular]], [[intravenous]]
+| ATC_prefix = D07
+| ATC_suffix = AA01
+| legal_CA = Rx-only
+| legal_UK = POM
+| legal_US = Rx-only
+| metabolism = [[Liver]] (CYP3A4)
+| elimination_half-life = 1.8–2.6 hours
+| excretion = [[Urine]]
+| CAS_number = 83-43-2
+| DrugBank = DB00959
+| PubChem = 6741
+| ChEBI = 6888
+| ChEMBL = 650
+}}
-Methylprednisolone, like other glucocorticoids, works by binding to glucocorticoid receptors in various types of cells, modulating gene expression and thus protein synthesis. It also interferes with various leukocyte inflammatory pathways, inhibiting leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, and suppression of humoral immune responses.
+'''Methylprednisolone''' is a synthetic glucocorticoid primarily used for its anti-inflammatory and immunosuppressive properties.
-== Dosage and Formulation ==
+Methylprednisolone is on the World Health Organization’s List of Essential Medicines.
-Methylprednisolone is available in multiple forms. The oral form is available in tablets of 2, 4, 8, 16, and 32 mg, both generically and under the brand name of Medrol, and in Medrol Dosepaks, which contain 21 tablets of 4 mg each. Injectable forms of methylprednisolone are also available generically and under the brand names of [[Solu-Medrol]] and [[Depo-Medrol]].
+== Medical Uses ==
+Methylprednisolone is prescribed for a variety of conditions, including:
-The potency of methylprednisolone is approximately five times greater than that of cortisol, a natural hormone produced by the adrenal glands. Because of this, the dosage used can vary significantly, with 4 mg daily being considered a physiological dose in adults. Notably, methylprednisolone has minimal mineralocorticoid activity, which refers to the effect on electrolyte and water balance.
+Inflammatory and Autoimmune Disorders
+* [[Rheumatoid arthritis]]
+* [[Systemic lupus erythematosus]] (SLE)
+* [[Psoriatic arthritis]]
+* [[Multiple sclerosis]] (MS)
+* [[Ulcerative colitis]]
+* [[Crohn’s disease]]
-== Indications and Usage ==
+Allergic and Respiratory Conditions
+* Severe allergies – including angioedema and anaphylaxis.
+* Asthma and COPD exacerbations – Used as an oral or IV corticosteroid in severe cases.
-Methylprednisolone is used for its anti-inflammatory and immunosuppressive effects in the treatment of various conditions, including:
+Endocrine and Oncological Uses
+* Adrenal insufficiency – As an alternative to hydrocortisone when mineralocorticoid activity is not required.
+* Cancer therapy – Used in the management of leukemia, lymphoma, and multiple myeloma.
-* Severe inflammatory conditions: These can include chronic inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease.
+Neurological Disorders
-* Autoimmune conditions: Conditions such as lupus and multiple sclerosis, where the body's immune system attacks its own tissues, can be managed with methylprednisolone.
+* Multiple sclerosis (MS) relapses – Administered as high-dose IV methylprednisolone.
-* Hypersensitivity reactions: Allergic reactions and other hypersensitivity responses can be treated with methylprednisolone.
+* Spinal cord injury (off-label) – Used to reduce inflammation in acute cases.
-* Organ rejection: Following organ transplantation, methylprednisolone can be used to suppress the immune response and prevent the body from rejecting the transplanted organ.
-== Side Effects and Warnings ==
-As with all medications, methylprednisolone use can be associated with adverse effects. These can include weight gain, fluid retention, high blood pressure, mood changes, increased blood sugar levels, and increased risk of infections due to its immunosuppressive effects. Long-term use can also lead to conditions such as osteoporosis.
+Ophthalmic Conditions
+* Optic neuritis (often linked to MS)
+* Uveitis, iritis, and scleritis
-== References ==
+== Administration and Dosage ==
+Methylprednisolone is available in oral tablets, intramuscular, intra-articular, and intravenous formulations. Dosage depends on the condition being treated:
+* Mild to moderate inflammation – 4–16 mg/day (oral)
+* Severe inflammation or autoimmune flares – IV pulse therapy (e.g., 500–1000 mg IV)
+* Acute asthma exacerbation – 40–80 mg/day PO or IV
-{{Reflist}}
+== Side Effects ==
+Common Side Effects
+* Weight gain
+* Mood changes (insomnia, agitation)
+* Increased blood sugar levels (hyperglycemia)
+* Fluid retention
+Serious Adverse Effects
+Long-term or high-dose use may lead to:
+* Osteoporosis and fractures
+* Adrenal suppression (requiring tapering)
+* Glaucoma and cataracts
+* Cushing’s syndrome (moon face, buffalo hump)
+* Infections due to immune suppression
+== Pharmacology ==
+Mechanism of Action
+Methylprednisolone is a glucocorticoid receptor agonist that:
+. Suppresses inflammation by inhibiting pro-inflammatory cytokines (IL-1, IL-6, TNF-alpha).
+. Suppresses the immune response by reducing T-cell activation.
+. Regulates metabolism by increasing glucose levels and altering fat distribution.
+Metabolism and Elimination
+* Metabolized in the liver (CYP3A4 pathway).
+* Eliminated via the kidneys.
+* Half-life: 1.8–2.6 hours.
+== Contraindications ==
+Methylprednisolone should not be used in:
+* Systemic fungal infections
+* Uncontrolled infections
+* Hypersensitivity to corticosteroids
+* Live vaccine administration
+== Drug Interactions ==
+* NSAIDs – Increased risk of gastric ulcers.
+* Diabetes medications – May require higher insulin doses.
+* Live vaccines – Risk of severe infection.
+* Anticoagulants – May alter warfarin levels.
+== History ==
+Methylprednisolone was first synthesized by The Upjohn Company (now Pfizer) and FDA-approved in 1957.
+== Availability ==
+Methylprednisolone is available under multiple brand names:
+* Medrol (oral tablets)
+* Depo-Medrol (intramuscular injection)
+* Solu-Medrol (intravenous formulation)
+== See Also ==
+* [[Glucocorticoid]]
+* [[Prednisolone]]
+* [[Cushing's syndrome]]
+* [[Adrenal insufficiency]]
+{{Glucocorticoids and antiglucocorticoids}}
+{{stub}}
-[[Category:Pharmacology]]
-[[Category:Medicine]]
-[[Category:Drugs]]
 [[Category:Glucocorticoids]]
-{{corticosteroids}}
+[[Category:Drugs developed by Pfizer]]
-{{coststubd}}
+[[Category:World Health Organization essential medicines]]