prednisolone
Corticosteroids· Brands: Deltacortril, Solupred, Predsol, Orapred, PreloneIVPOPRTOP
Mechanism of action
Prednisolone is a corticosteroid that binds to cytoplasmic glucocorticoid receptors, modulating gene transcription to produce anti-inflammatory and immunosuppressive effects. It inhibits phospholipase A2, reducing the release of arachidonic acid, thus decreasing prostaglandins and leukotrienes. It also suppresses cytokine production and reduces the activity of immune cells.
Pharmacokinetics
Prednisolone is well absorbed orally, with peak concentrations within 1 to 2 hours. It is metabolised in the liver, primarily by CYP3A4, and is excreted in urine largely as inactive metabolites. The plasma half-life is approximately 2 to 3 hours, but the biological half-life is longer, lasting up to 24 hours, due to intracellular effects.
Indications & dosing
Acute asthma exacerbation
Short course, usually 5-7 days. No taper needed if used for less than 2 weeks.
- adult · PO: 30–50 mg once daily · Short course, usually 5-7 days. No taper needed if used for less than 2 weeks.
COPD exacerbation
Use for 5-7 days. Taper if more than 2 weeks of therapy.
- adult · PO: 30–50 mg once daily · Use for 5-7 days. Taper if more than 2 weeks of therapy.
Allergic reactions
Short-term use for acute allergic conditions.
- adult · PO: 10–20 mg once daily · Short-term use for acute allergic conditions.
Inflammatory bowel disease
Taper required if used for more than 2 weeks.
- adult · PO: 20–40 mg once daily · Taper required if used for more than 2 weeks.
Rheumatoid arthritis
Low-dose maintenance. Taper to lowest effective dose.
- adult · PO: 5–10 mg once daily · Low-dose maintenance. Taper to lowest effective dose.
Acute asthma exacerbation (paediatric)
Short course for 3-5 days. Maximum 60 mg per day.
- pediatric · PO: 1–2 mg/kg/day once daily · Short course for 3-5 days. Maximum 60 mg per day.
Contraindications & precautions
- Systemic fungal infections · Corticosteroids may worsen fungal infections; antifungal treatment should be established first.
- Live vaccines (concurrent use) · Immunosuppression may increase risk of vaccine-associated infection.
- Hypersensitivity to prednisolone or any component · Avoid in patients with known allergy.
- Peptic ulcer disease (active) · Use with caution; consider gastroprotection.
- Diabetes mellitus · May cause hyperglycaemia; monitor blood glucose.
- Osteoporosis · Risk of bone loss; consider bone protection if long-term use.
- Use the lowest effective dose for the shortest possible duration, and taper gradually after prolonged therapy to avoid adrenal crisis.
- Monitor for signs of infection, hyperglycaemia, and fluid retention, especially in patients with diabetes, cardiovascular disease, or hypertension.
- Consider bone protection (e.g., calcium and vitamin D, bisphosphonates) for patients on long-term systemic corticosteroids.
- Avoid live vaccines during immunosuppressive doses; inactivated vaccines may be given but response may be reduced.
- During intercurrent illness, surgery, or trauma, the dose may need to be increased; co-management with a specialist is advised.
- For patients with peptic ulcer disease, consider co-prescription of a proton pump inhibitor or H2 antagonist.
Adverse effects
- Increased appetite and weight gain
- Insomnia and mood changes (e.g., euphoria, depression)
- Hyperglycaemia (glucose intolerance)
- Increased susceptibility to infectionsserious
- Osteoporosis with long-term useserious
- Adrenal suppression with prolonged useserious
- Peptic ulcerationserious
- Myopathyserious
- Growth retardation in childrenserious
Interactions
- metforminmoderateMonitor blood glucose regularly when prednisolone is started, stopped, or the dose is changed. Consider adjusting the metformin dose, adding other antihyperglycaemic agents, or using a non-steroidal alternative if appropriate for the underlying condition.
- ibuprofenmajorAvoid co-prescription where alternative analgesic or anti-inflammatory options exist. If unavoidable, prescribe a proton pump inhibitor or misoprostol, use the lowest effective doses for the shortest duration, and monitor for dyspepsia, melaena, or anaemia. Exercise extreme caution in high-risk groups.
- digoxinmajorMonitor serum potassium, digoxin levels, and ECG at baseline and periodically during concurrent therapy. Correct any hypokalemia promptly. Consider potassium-sparing diuretics or potassium supplementation if needed. Adjust digoxin dose based on clinical response and levels. In patients with hypokalemia, digoxin toxicity may occur even at therapeutic digoxin levels.
- warfarinmajorMonitor the INR frequently, particularly within the first 2-3 days after initiating or stopping prednisolone, and adjust the warfarin dose accordingly. Consider adding a gastroprotective agent (e.g., a proton pump inhibitor) in patients at increased risk of gastrointestinal bleeding. Advise patients to report any signs of bleeding, such as easy bruising, dark stools, or haematuria.
Renal & hepatic adjustment
- Hepatic impairment (mild): No dose adjustment required; monitor for adverse effects.
- Hepatic impairment (moderate): No dose adjustment required; monitor for adverse effects and increased systemic exposure.
- Hepatic impairment (severe): Consider reducing the dose by 50% or using an alternative; monitor closely for adverse effects.
Monitoring, pregnancy & toxicity
- Blood pressure · Baseline and periodically during therapy
- Blood glucose · In patients with diabetes or at risk; at baseline and periodically
- Serum potassium · In patients on high doses or long-term therapy
- Weight · To detect fluid retention
- Bone mineral density · For long-term use
- Eye examination · For long-term use (cataracts/glaucoma)
- Pregnancy: Prednisolone is generally considered safe in pregnancy, but use at the lowest effective dose for the shortest duration. It crosses the placenta but is inactivated by placental 11β-HSD2, reducing fetal exposure. Prolonged use may cause fetal adrenal suppression and growth restriction, so monitor accordingly.
- Toxicity: Acute overdose: hyperglycaemia, hypertension, mood disturbances · Supportive care; monitor blood glucose, electrolytes, and vital signs; administer insulin if needed.
- Toxicity: Chronic high-dose effects: Cushing's syndrome, osteoporosis, myopathy · Use lowest effective dose; taper gradually; monitor for bone loss, consider bisphosphonates and calcium/vitamin D supplementation.
- Toxicity: Adrenal insufficiency during treatment or on withdrawal · Taper the dose slowly; in stress or illness, may need mineralocorticoid supplementation; consider stress-dose steroids if necessary.
- Toxicity: Increased risk of infections and masking of signs · Monitor for infection; avoid live vaccines; consider prophylactic antibiotics in neutropenic patients.
Clinical notes
Prednisolone is used for inflammatory and autoimmune conditions, including asthma, COPD exacerbations, allergic reactions, and rheumatoid arthritis. It is also used for adrenal insufficiency and as part of certain cancer regimens. Long-term use requires gradual dose tapering to avoid adrenal suppression. Monitor for hyperglycaemia, hypertension, osteoporosis, and signs of infection. Consider prophylactic bone protection if used chronically.
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