Metapred

Methylprednisolone (METHAPRED) is a synthetic corticosteroid primarily used for its glucocorticoid activity and minimal mineralocorticoid properties. It is available in various strengths: 2 mg, 4 mg, 8 mg, 16 mg, and 32 mg tablets.

Mechanism of Action

METHAPRED works by diffusing across cell membranes and binding to specific cytoplasmic receptors. These complexes then enter the cell nucleus, bind to DNA, and stimulate the transcription of mRNA. This process leads to a variety of local and systemic effects, including the inhibition of leukocyte infiltration at the site of inflammation, interference with mediators of the inflammatory response, and suppression of humoral immune responses. The anti-inflammatory actions of corticosteroids involve phospholipase A2 inhibitory proteins, known as lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Pharmacokinetics

• Absorption: Readily absorbed from the gastrointestinal tract.
• Onset of Action: 1 to 2 hours.
• Duration of Action: 30 to 36 hours.
• Distribution: Distributed to all body tissues.
• Metabolism: Mainly in the liver but also in other tissues.
• Elimination Half-life: 3 to 3.5 hours.
• Excretion: Primarily through urine (as metabolites), with minimal excretion through feces.

Indications and Dosage

# Adult

• Anti-inflammatory: 4 mg to 48 mg daily.
• Immunosuppression: 4 mg to 48 mg daily.
• Asthma – Acute Asthma Exacerbations (Emergency Medical Care or Hospital Doses): 40 to 80 mg once a day or divided into two doses until peak expiratory flow is 70% of predicted or personal best.
• Short-course “Burst” (Acute Asthma): 40 to 60 mg once a day or divided into two doses for 3 to 10 days. Treatment should continue until symptoms resolve and peak expiratory flow is at least 80% of personal best, typically requiring 5 days of treatment, though longer treatment may be necessary.
• Asthma – Maintenance: 7.5 to 60 mg daily, given as a single dose in the morning or every other day as needed for asthma control.
• Allergic Conditions:
• Day 1: One tablet of 8 mg before breakfast, one tablet of 4 mg after lunch and dinner, and one tablet of 8 mg at bedtime.
• Day 2: One tablet of 4 mg before breakfast, after lunch and dinner, and one tablet of 8 mg at bedtime.
• Day 3: One tablet of 4 mg before breakfast, after lunch, dinner, and at bedtime.
• Day 4: One tablet of 4 mg before breakfast, after lunch, and at bedtime.
• Day 5: One tablet of 4 mg before breakfast and at bedtime.
• Day 6: One tablet of 4 mg before breakfast.
• May be tapered over 12 days to decrease the chance of dermatitis flare-up..
• Vestibular Neuritis: 100 mg for 3 days, then gradually taper as follows:
• Days 4 to 6: 80 mg.
• Days 7 to 9: 60 mg.
• Days 10 to 12: 40 mg.
• Days 13 to 15: 20 mg.
• Days 16 to 18: 10 mg.
• Days 20 and 22: 10 mg.
• Ulcerative Colitis: 40 to 60 mg per day.