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Tuesday, July 29, 2025

Prednisolone tablets and liquid


Generic Name: Prednisolone
Brand Names: Prednisolone 5mg Tablets, Prednisolone Oral Solution, Orapred, Millipred, Pediapred, Prelone, Deltacortril
Drug Class: Glucocorticoid (Corticosteroid)
Pharmaceutical Category: Anti-inflammatory, Immunosuppressant, Endocrine therapy
Formulations: Oral tablets, dispersible tablets, soluble tablets, oral solution, oral suspension
Routes of Administration: Oral

1. Pharmacological Classification

Prednisolone is a synthetic glucocorticoid, closely related to the naturally occurring hormone cortisol. It exerts potent anti-inflammatory, immunosuppressive, and anti-allergic actions. It is approximately 4 times more potent than hydrocortisone and primarily acts on glucocorticoid receptors with minimal mineralocorticoid activity.

2. Mechanism of Action

Prednisolone diffuses across cell membranes and binds to intracellular glucocorticoid receptors. This complex translocates to the nucleus, where it modulates transcription of glucocorticoid-responsive genes. The pharmacological actions include:

  • Inhibition of inflammatory cytokines (IL-1, IL-6, TNF-α)

  • Suppression of immune cell migration and adhesion

  • Inhibition of phospholipase A2 and COX-2, reducing prostaglandin and leukotriene synthesis

  • Stabilization of lysosomal membranes and capillary permeability reduction

These actions result in suppression of both cell-mediated and humoral immunity, and a broad-spectrum anti-inflammatory response.

3. Therapeutic Uses

Prednisolone is used in a wide range of inflammatory, allergic, autoimmune, and endocrine disorders:

A. Allergic and Respiratory Conditions

  • Asthma exacerbations (acute or chronic management)

  • Chronic obstructive pulmonary disease (COPD)

  • Anaphylaxis (adjunct to epinephrine)

  • Allergic rhinitis and urticaria

  • Serum sickness

B. Autoimmune and Inflammatory Disorders

  • Rheumatoid arthritis

  • Systemic lupus erythematosus (SLE)

  • Psoriatic arthritis

  • Inflammatory bowel diseases (Crohn's disease, ulcerative colitis)

  • Vasculitis

C. Dermatologic Conditions

  • Severe eczema

  • Pemphigus vulgaris

  • Drug hypersensitivity reactions

D. Neurological and Musculoskeletal

  • Multiple sclerosis relapses

  • Bell’s palsy (inflammation-related)

  • Polymyalgia rheumatica

  • Myasthenia gravis (adjunctive)

E. Hematological and Neoplastic

  • Autoimmune hemolytic anemia

  • Idiopathic thrombocytopenic purpura (ITP)

  • Acute leukemia

  • Lymphoma (as part of chemotherapy protocols)

F. Gastrointestinal

  • Autoimmune hepatitis

  • Eosinophilic esophagitis

G. Ophthalmologic

  • Uveitis

  • Optic neuritis

H. Endocrine Replacement

  • Adrenal insufficiency (secondary or tertiary adrenal failure)

  • Congenital adrenal hyperplasia (as glucocorticoid replacement)

4. Dosage and Administration

General Principles

  • Dosage is highly individualized based on the disease, severity, duration, and patient response.

  • Tapering is necessary after prolonged use to prevent adrenal crisis.

  • Morning administration is preferred to mimic diurnal cortisol rhythm and reduce adrenal suppression.

Typical Adult Oral Doses

  • Mild conditions (e.g., allergy): 5–20 mg daily

  • Severe conditions (e.g., autoimmune diseases): 40–60 mg/day, taper based on clinical response

  • Acute exacerbations (e.g., asthma attack): 30–50 mg/day for 5–10 days

Children

  • Doses typically range from 0.5–2 mg/kg/day, depending on indication.

  • Oral solution/suspension (1 mg/mL, 5 mg/mL) is useful for accurate pediatric dosing.

Tapering Schedule

  • Taper gradually after prolonged use (>2–3 weeks) to allow hypothalamic-pituitary-adrenal (HPA) axis recovery.

  • Abrupt withdrawal risks adrenal insufficiency, fatigue, hypotension, and even death.

5. Pharmacokinetics

  • Absorption: Rapid and complete from GI tract; peak levels ~1–2 hours post-dose

  • Distribution: Wide distribution; crosses placenta and appears in breast milk

  • Metabolism: Primarily hepatic (CYP3A4); inactive metabolites

  • Elimination: Renal, as glucuronide/sulfate conjugates

  • Half-life: ~2–4 hours (biological effects last 12–36 hours)

6. Contraindications

  • Untreated systemic infections (especially fungal)

  • Hypersensitivity to prednisolone or excipients

  • Recent live virus vaccination in immunosuppressed individuals

  • Peptic ulcer disease (relative)

  • Uncontrolled diabetes or hypertension (caution)

  • Severe osteoporosis (long-term use contraindicated)

7. Warnings and Precautions

Infections

  • Masks signs of infection

  • Increases susceptibility to bacterial, viral, and fungal infections

  • Reactivation of latent TB, herpes, or hepatitis B possible

Endocrine

  • Risk of adrenal suppression and Cushingoid features

  • Glucose intolerance or frank diabetes

Bone and Muscle

  • Osteoporosis and fractures with long-term use

  • Muscle weakness (steroid myopathy)

Gastrointestinal

  • Gastric ulcers, GI bleeding, pancreatitis

Psychiatric

  • Mood changes: euphoria, depression, psychosis

  • Sleep disturbance, irritability

Ophthalmologic

  • Cataracts, glaucoma, increased intraocular pressure

Cardiovascular and Renal

  • Sodium retention and hypertension

  • Edema and hypokalemia

Growth Retardation

  • Suppresses linear growth in children

Vaccinations

  • Live vaccines contraindicated during high-dose or long-term therapy

8. Adverse Effects

Short-Term Use

  • Mood elevation, anxiety, restlessness

  • Hyperglycemia

  • Hypertension

  • Fluid retention

  • Increased appetite and weight gain

  • Insomnia

  • Gastric irritation

Long-Term Use

  • Cushingoid appearance (moon face, buffalo hump)

  • Osteoporosis

  • Adrenal suppression

  • Myopathy

  • Skin thinning and bruising

  • Impaired wound healing

  • Growth suppression in children

  • Increased infection risk

9. Drug Interactions

Enzyme Inducers

  • Rifampin, phenytoin, carbamazepine: Increase prednisolone metabolism → reduced efficacy

Enzyme Inhibitors

  • Ketoconazole, erythromycin, grapefruit juice: Increase blood levels → risk of toxicity

NSAIDs

  • Additive risk of GI bleeding and ulcers

Antidiabetic Drugs

  • Reduced effectiveness due to prednisolone-induced hyperglycemia

Live Vaccines

  • Reduced efficacy and increased risk of vaccine-derived disease

Diuretics

  • Risk of hypokalemia with loop or thiazide diuretics

Warfarin

  • Variable effect on INR; monitor coagulation profile closely

10. Pregnancy and Lactation

Pregnancy

  • Generally considered safe in low to moderate doses

  • High doses may increase risk of cleft palate, fetal growth restriction

  • Use lowest effective dose under specialist supervision

Lactation

  • Excreted into breast milk in small amounts

  • Generally considered safe, but monitor infant for signs of adrenal suppression or growth effects

11. Tapering and Withdrawal

Sudden withdrawal after long-term or high-dose therapy may lead to adrenal crisis:

  • Weakness

  • Hypotension

  • Nausea and vomiting

  • Hypoglycemia

  • Potential circulatory collapse

Tapering protocols vary based on duration and dosage. A common taper:

  • Reduce by 5–10 mg/week until 20 mg/day, then reduce by 2.5 mg/week

Alternate-day dosing may help reduce side effects and preserve adrenal function.

12. Formulations and Brand Availability

Tablets

  • 1 mg, 2.5 mg, 5 mg, 10 mg, 25 mg (depending on country)

  • Enteric-coated and soluble forms also available

Oral Solution / Suspension

  • 1 mg/mL, 5 mg/5 mL, and 15 mg/5 mL

  • Brands: Pediapred, Orapred, Redipred, Prednisolone Sodium Phosphate Solution

Dispersible Tablets (UK, EU)

  • Soluble in water for pediatric or swallowing difficulty

13. Monitoring Parameters

  • Blood pressure, weight, blood glucose

  • Growth in children

  • Bone density (DEXA scan for chronic use)

  • Electrolytes (Na⁺, K⁺)

  • Ophthalmologic exam (if used >6 weeks)

  • Signs of infection or adrenal suppression

  • Mood and psychiatric symptoms




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