Mepred

Approved Indications:

A. Endocrine Disorders

• Primary or secondary adrenocortical insufficiency (as replacement therapy)
• Congenital adrenal hyperplasia
• Nonsuppurative thyroiditis
• Hypercalcemia associated with cancer

B. Rheumatic Disorders

• Rheumatoid arthritis
• Ankylosing spondylitis
• Psoriatic arthritis
• Acute or subacute bursitis
• Synovitis of osteoarthritis
• Acute gouty arthritis
• Epicondylitis

C. Collagen Diseases

• Systemic lupus erythematosus
• Systemic dermatomyositis (polymyositis)
• Acute rheumatic carditis

D. Dermatologic Diseases

• Pemphigus
• Bullous dermatitis herpetiformis
• Severe erythema multiforme (Stevens-Johnson syndrome)
• Exfoliative dermatitis
• Severe psoriasis
• Severe seborrheic dermatitis

E. Allergic States

• Severe bronchial asthma
• Contact dermatitis
• Drug hypersensitivity reactions
• Serum sickness
• Allergic rhinitis
• Urticaria

F. Ophthalmic Diseases

• Severe acute and chronic allergic and inflammatory eye conditions:
• Iritis, iridocyclitis, optic neuritis
• Chorioretinitis, anterior segment inflammation
• Allergic conjunctivitis

G. Respiratory Disorders

• Symptomatic sarcoidosis
• Loeffler's syndrome
• Aspiration pneumonitis
• Exacerbation of COPD

H. Hematologic Disorders

• Idiopathic thrombocytopenic purpura (in adults)
• Secondary thrombocytopenia
• Autoimmune hemolytic anemia
• Erythroblastopenia
• Congenital (erythroid) hypoplastic anemia

I. Neoplastic Diseases

• Palliative management of:
• Leukemias and lymphomas in adults and children

J. Gastrointestinal Diseases

• Ulcerative colitis
• Regional enteritis (Crohn’s disease)

K. Nervous System Disorders

• Acute exacerbations of multiple sclerosis
• Cerebral edema due to brain tumors

Off-Label / Clinically Accepted Uses:

• Prevention and treatment of chemotherapy-induced nausea and vomiting
• Acute spinal cord injury (high-dose protocol)
• Post-transplant immunosuppression
• Severe COVID-19-related inflammation (in select cases)

Routes: Oral, Intravenous (IV), Intramuscular (IM), Intra-articular, Intralesional

Adults

• Oral: 4 to 48 mg/day in divided doses or single dose depending on condition severity
• IV/IM (Solu-Medrol): 10 to 500 mg per dose; higher doses (e.g., 1–2 g/day) used for severe conditions like cerebral edema or acute MS
• IV pulse therapy (MS exacerbation): 1 g/day for 3–5 days
• Intra-articular (arthritis):
• Small joints: 4–10 mg
• Medium joints: 10–40 mg
• Large joints: 20–80 mg
• Intralesional (e.g., keloids): 20–60 mg/mL (diluted), volume varies

Pediatrics

• Oral/IV: 0.5–1.7 mg/kg/day (up to 60 mg/day) in divided doses
• High-dose IV (e.g., nephrotic syndrome or leukemia): Up to 30 mg/kg/dose IV once daily for 3 days under specialist supervision

Elderly

• Use lowest effective dose; increased sensitivity to adverse effects

Renal Impairment

• No initial dose adjustment required, but monitor fluid retention and blood pressure closely

Hepatic Impairment

• Use with caution due to reduced metabolism; monitor for prolonged systemic exposure

Administration Notes:

• IV: Administer over several minutes (doses ≥250 mg over at least 30 minutes)
• Oral: Take with food to minimize GI irritation
• Taper gradually after prolonged use to prevent adrenal insufficiency

Methylprednisolone is a synthetic glucocorticoid that exerts its effects by binding to cytosolic glucocorticoid receptors. The drug-receptor complex then translocates into the nucleus, where it modulates gene expression, leading to suppression of pro-inflammatory cytokines (e.g., IL-1, IL-6, TNF-α) and increased expression of anti-inflammatory proteins like lipocortin-1. These actions result in reduced leukocyte migration, decreased capillary permeability, and diminished immune activity, contributing to its broad anti-inflammatory and immunosuppressive properties across multiple organ systems.

• Absorption: Rapid and nearly complete after oral administration
• Bioavailability: ~89–98%
• Distribution: Widely distributed; crosses placenta and into breast milk; ~77% plasma protein bound
• Onset of Action:
• IV: 1–2 hours
• Oral: 2–6 hours
• Metabolism: Extensively metabolized in the liver by CYP3A4
• Active Metabolites: No active metabolites; methylprednisolone is the active moiety
• Half-life:
• Plasma: ~2.5–3.5 hours
• Biological: 18–36 hours
• Excretion: Renally as inactive metabolites

• Pregnancy: Category C (FDA). Use only if potential benefit justifies risk. High doses in pregnancy may cause fetal growth restriction or adrenal suppression.
• Lactation: Excreted in breast milk in small amounts. Considered generally safe for short-term use; monitor infants for growth or adrenal suppression with long-term maternal use.

• Primary Class: Glucocorticoid (Systemic Corticosteroid)
• Subclass: Intermediate-acting corticosteroid
• Formulations: Oral tablets, IV/IM injection (Solu-Medrol), depot injections (Methylprednisolone acetate)

• Known hypersensitivity to methylprednisolone or other corticosteroids
• Systemic fungal infections
• Intrathecal or epidural administration (not approved)
• Untreated active infections
• Administration of live vaccines during high-dose therapy
• Idiopathic thrombocytopenic purpura (for IM route)

• Immunosuppression: Increased susceptibility to infections; may mask infection symptoms
• HPA Axis Suppression: Risk with long-term use; taper gradually
• Metabolic Effects: Can cause hyperglycemia, weight gain, and dyslipidemia
• Psychiatric Reactions: Insomnia, mood swings, psychosis
• Musculoskeletal: Osteoporosis, myopathy, tendon rupture with chronic use
• GI: Risk of peptic ulcers and GI bleeding
• Vaccination: Avoid live vaccines during treatment
• CNS: Seizures, pseudotumor cerebri reported, especially in pediatric patients

Common:

• Endocrine/Metabolic: Weight gain, moon face, hyperglycemia
• Gastrointestinal: Nausea, abdominal discomfort, increased appetite
• Neurological: Insomnia, mood changes
• Musculoskeletal: Muscle weakness, osteoporosis
• Dermatologic: Acne, skin thinning, delayed wound healing

Serious/Rare:

• Psychiatric: Psychosis, depression, euphoria
• Cardiovascular: Hypertension, arrhythmias
• Immune: Increased risk of severe infections
• Ophthalmic: Glaucoma, cataracts
• Hematologic: Leukocytosis
• Adrenal: Suppression of endogenous cortisol production

Timing: Systemic effects may occur within days; long-term use increases risk of serious complications

• CYP3A4 Inhibitors (e.g., Ketoconazole, Ritonavir): May increase methylprednisolone levels, risk of toxicity
• CYP3A4 Inducers (e.g., Rifampin, Phenytoin): May reduce effectiveness
• NSAIDs: Increased risk of GI ulceration and bleeding
• Diuretics (especially thiazides): Potentiation of hypokalemia
• Antidiabetic Agents: Reduced efficacy due to hyperglycemic effects
• Vaccines (Live): Risk of vaccine failure or disseminated infection

Enzyme System: Primarily metabolized by CYP3A4

• Updated Corticosteroid Use Guidelines (e.g., NICE, FDA): Emphasize using lowest effective dose and shortest duration possible to minimize systemic risks
• COVID-19 Usage (Short-Term): Included in guidelines for managing severe COVID-19-associated inflammation; typically IV dosing of 40–125 mg/day for limited duration
• EMA/FDA: No recent new indications; labeling updated to reinforce infection and adrenal suppression warnings

• Oral Tablets:
• Store at 20°C to 25°C (68°F to 77°F)
• Protect from light and moisture
• Injectable Forms (Solu-Medrol):
• Store vials at 20°C to 25°C
• Do not freeze
• Use reconstituted solution within the manufacturer-recommended time
• Depot Injections (e.g., acetate suspensions):
• Shake well before use
• Store between 15°C to 30°C
• Protect from freezing