GUPISONE 5/MG 20/TAB

Indications

Approved Uses

Systemic corticosteroid indicated for conditions responsive to glucocorticoids, including: allergic states; dermatologic diseases; endocrine disorders (including adrenocortical insufficiency as replacement therapy); gastrointestinal diseases (e.g., ulcerative colitis/Crohn’s); hematologic disorders; neoplastic diseases (palliative); ophthalmic inflammatory diseases; renal diseases (e.g., nephrotic syndrome); respiratory diseases (e.g., asthma exacerbations); and rheumatic/autoimmune disorders (e.g., RA, SLE).

Off-Label Uses

Common off-label uses include Bell’s palsy and adjunctive therapy in Pneumocystis jirovecii pneumonia; other uses depend on local protocols and evidence (e.g., certain severe inflammatory airway conditions).

Dosage & Administration

Dosing by Condition

Adults (general): initial 5-60 mg/day PO (single morning dose or divided), individualized by indication and response; then taper to the lowest effective dose. Condition-specific regimens vary widely and should follow the prescriber’s protocol for the diagnosed disease.

Initial Dose

5-60mg/day depending on condition severity

Maintenance Dose

2.5-15mg/day (lowest effective dose)

Maximum Dose

Up to 60 mg/day for most conditions; higher doses (e.g., 80 mg/day) may be used in specific pediatric cases or acute conditions.

Children's Dosage

0.1-2mg/kg/day orally in 1-4 divided doses depending on condition; nephrotic syndrome: 60mg/m²/day for 4 weeks then 40mg/m² on alternate days for 4 weeks

Dose Adjustment Notes

Use the lowest effective dose for the shortest duration; taper gradually after prolonged therapy or if adrenal suppression is possible; provide stress-dose steroids during major illness/surgery for patients on chronic therapy. No routine renal dose adjustment; use caution in hepatic impairment and in hypoalbuminemia (may increase free steroid exposure).

How to Take

Oral: take with food or milk to reduce GI irritation; swallow with water. Prefer a single morning dose (or the larger portion in the morning if divided) to better match circadian cortisol and reduce insomnia; follow prescriber directions (some regimens require divided dosing).

Side Effects

Common Side Effects

Weight gain, increased appetite, fluid retention, insomnia, mood changes (euphoria, irritability), acne, increased sweating, dyspepsia, nausea, headache, dizziness, hypertension, hyperglycemia, muscle weakness

Safety & Warnings

Contraindications

Systemic fungal infections; hypersensitivity to prednisolone/excipients; administration of live or live-attenuated vaccines in patients receiving immunosuppressive doses of corticosteroids.

Warnings & Precautions

Key precautions: increased infection risk (avoid exposure to varicella/measles if non-immune), avoid live vaccines at immunosuppressive doses, monitor glucose/BP/electrolytes, GI ulcer risk (esp. with NSAIDs), bone protection/monitoring for long-term use, psychiatric effects, ocular monitoring (cataract/glaucoma), growth monitoring in children, and taper after prolonged/high-dose therapy; consider a steroid card for long-term therapy.

Age Restriction

No absolute minimum age; prednisolone can be used in neonates/infants/children when clinically indicated under specialist supervision with weight-based dosing and monitoring.

Drug Interactions

Drug Interactions

Key interactions include: NSAIDs (↑GI ulcer/bleed risk), warfarin/anticoagulants (variable INR effect), antidiabetics (↑glucose/↓effect), diuretics/amphotericin B (↑hypokalemia), digoxin (↑toxicity via hypokalemia), CYP3A4 inducers e.g., rifampicin/phenytoin/carbamazepine (↓prednisolone), CYP3A4 inhibitors e.g., azoles/macrolides (↑prednisolone), cyclosporine (↑levels/toxicity both ways), and live vaccines (avoid/contraindicated at immunosuppressive doses).

Interaction Severity

MAJOR: live vaccines (avoid in immunosuppressive doses); strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin) can reduce effect; mifepristone can antagonize glucocorticoid effect. MODERATE: NSAIDs (GI ulcer/bleed risk), warfarin (INR changes), antidiabetics (hyperglycemia), azole antifungals/strong CYP3A inhibitors (increase exposure), cyclosporine (mutual level/toxicity increase), potassium-wasting diuretics (hypokalemia), digoxin (hypokalemia-related toxicity). MINOR: antacids may reduce absorption (separate dosing).

Food Interaction

Take with food

Special Populations

Children

0.1-2mg/kg/day orally in 1-4 divided doses depending on condition; nephrotic syndrome: 60mg/m²/day for 4 weeks then 40mg/m² on alternate days for 4 weeks

Kidney Impairment

No specific dose adjustment; use with caution in severe renal impairment due to fluid retention, hypertension, and electrolyte disturbances.

Storage & Patient Advice

Storage Conditions

Store below 30°C. Protect from light and moisture.

Missed Dose

Take the missed dose as soon as remembered the same day; if it is close to the next scheduled dose, skip the missed dose and resume the regular schedule-do not double doses.

Stopping the Medicine

Do not stop abruptly after prolonged or high-dose use; taper gradually as directed by a clinician (tapering is especially important after >2-3 weeks, repeated courses, or Cushingoid features).

Overdose

Acute overdose is usually managed supportively; clinically significant toxicity is more likely with chronic excessive dosing (Cushingoid features, hyperglycemia, hypertension, fluid retention, hypokalemia, psychiatric effects, adrenal suppression).

Patient Counseling

Take with food/milk; preferably take in the morning if once daily. Do not stop abruptly if used more than a few days-taper as directed. Seek advice urgently for fever/infection exposure (especially chickenpox/measles if non-immune). Avoid live vaccines while on immunosuppressive doses. Watch for mood changes, sleep disturbance, GI bleeding symptoms, swelling/weight gain, vision changes; diabetics should monitor glucose. For long-term therapy, ensure bone protection (calcium/vitamin D) and carry steroid identification if applicable.

Monitoring Requirements

Monitor: blood pressure, weight/edema, blood glucose (especially diabetics), electrolytes (esp. potassium), signs of infection; with prolonged therapy monitor bone health (calcium/vitamin D, consider BMD), ocular effects (cataract/glaucoma/intraocular pressure), and HPA-axis suppression/adrenal insufficiency risk; in children monitor growth.

Pharmacology

Mechanism of Action

Binds intracellular glucocorticoid receptors to alter gene transcription, decreasing pro-inflammatory cytokines/mediators and immune-cell trafficking, thereby producing anti-inflammatory and immunosuppressive effects.

Onset of Action

Oral onset is typically within a few hours; clinical improvement may be seen the same day, but timing depends on indication and severity.

Duration of Effect

Intermediate-acting glucocorticoid: biologic effect typically ~12-36 hours.

Half-Life

Plasma (elimination) half-life ~2-4 hours; biological (pharmacodynamic) half-life ~18-36 hours.

Bioavailability

High; approximately 70-90% oral bioavailability (well absorbed).

Metabolism

Primarily hepatic metabolism (largely via CYP3A4) with interconversion by 11β-hydroxysteroid dehydrogenase between prednisolone and prednisone; metabolites are inactive.

Excretion

Primarily renal excretion as inactive metabolites/conjugates (e.g., glucuronide and sulfate conjugates), with minor fecal excretion.

Protein Binding

Approximately 70-90% protein bound (mainly to corticosteroid-binding globulin/transcortin and albumin).

Product Information

Available Dosage Forms

For this SFDA-registered product: Tablet (oral) only.

Composition per Dose

Each tablet: 5mg prednisolone

Generic Availability

Yes

OTC Alternatives

No OTC alternative for systemic corticosteroid therapy; OTC antihistamines (cetirizine, loratadine) for mild allergic symptoms only

Symptom Target

Allergy, Inflammation

Sedating

No

Reviewed by Al Mujtama Pharmacy Medical Review Team. Last reviewed 27-05-2026