Usage
Prednisolone is prescribed for a wide range of medical conditions requiring anti-inflammatory or immunosuppressive effects. These include:
- Allergic reactions: Severe allergic reactions, drug reactions, serum sickness, allergic rhinitis, and urticaria.
- Autoimmune diseases: Rheumatoid arthritis, lupus, inflammatory bowel disease (Crohn’s disease and ulcerative colitis), multiple sclerosis, psoriasis, and autoimmune hepatitis.
- Breathing problems: Asthma, chronic obstructive pulmonary disease (COPD), and allergic bronchopulmonary aspergillosis.
- Cancers: Leukemia, lymphoma, and multiple myeloma.
- Endocrine disorders: Adrenal insufficiency and thyroiditis.
- Eye conditions: Allergic conjunctivitis, uveitis, and temporal arteritis.
- Gastrointestinal disorders: Ulcerative colitis and Crohn’s disease.
- Kidney diseases: Nephrotic syndrome and glomerulonephritis.
- Skin conditions: Eczema, pemphigus vulgaris, and contact dermatitis.
- Other conditions: Organ transplantation, prevention of organ rejection, and certain types of edema.
Pharmacological classification: Prednisolone is a corticosteroid, specifically a glucocorticoid.
Mechanism of action: Prednisolone works by binding to glucocorticoid receptors in the cytoplasm of cells. This complex then moves into the nucleus, where it affects gene transcription, leading to:
- Suppression of inflammation by inhibiting the production of inflammatory mediators (e.g., prostaglandins, leukotrienes, cytokines).
- Suppression of the immune system by inhibiting the proliferation and activity of lymphocytes.
Alternate Names
While “prednisolone” is the generic name most commonly used, it may also be referred to as:
- Prednisolone sodium phosphate (for injectable formulations)
- Prednisolone acetate (for ophthalmic formulations)
- Prednisolone tebutate
Brand names: Prednisolone is available under numerous brand names, which can vary regionally. Some examples include:
- Millipred
- Orapred
- Pediapred
- Prelone
How It Works
Pharmacodynamics: Prednisolone exerts its effects by binding to glucocorticoid receptors within cells. This binding initiates a series of intracellular events that alter the expression of various genes. Prednisolone mainly affects carbohydrate metabolism, protein metabolism, and fat metabolism. It exhibits potent anti-inflammatory and immunosuppressive actions by inhibiting inflammatory mediators, leukocyte infiltration, and antibody production.
Pharmacokinetics:
- Absorption: Prednisolone is well-absorbed orally. Peak plasma concentrations are achieved within 1-2 hours.
- Metabolism: Primarily metabolized in the liver to inactive metabolites. A small portion is converted to prednisone.
- Elimination: Excreted primarily in the urine, with a small amount eliminated in the feces.
Mode of action: Prednisolone inhibits inflammatory responses, modifies vascular permeability, and suppresses immune responses. It exerts these actions by interacting with intracellular glucocorticoid receptors and modifying gene transcription.
Receptor binding: Prednisolone binds to glucocorticoid receptors in the cytoplasm.
Enzyme inhibition: Prednisolone suppresses the synthesis of several enzymes involved in inflammatory processes.
Elimination pathways: Primarily renal excretion of metabolites, with minor hepatic involvement.
Dosage
Standard Dosage
Adults: The initial dose can vary depending on the condition and severity, ranging from 5 mg to 60 mg per day. The dose can be given once daily or in divided doses.
Children: The recommended dosage is 0.14 to 2 mg/kg per day, divided into 3 or 4 doses.
Special Cases:
- Elderly Patients: Lower initial doses and careful monitoring are advised due to increased susceptibility to side effects.
- Patients with Renal Impairment: Dose adjustment may be needed, although specific guidelines are not well-established. Close monitoring is recommended.
- Patients with Hepatic Dysfunction: Dose adjustment may be necessary due to decreased metabolism.
- Patients with Comorbid Conditions: Consider potential interactions with other medications and conditions like diabetes, hypertension, or infections.
Clinical Use Cases
Dosage in specific medical settings may vary and needs to be individualized based on patient response:
- Intubation: Doses can be adjusted from 5 mg to 60 mg per day, based on patient requirements.
- Surgical Procedures: Doses can range from 5 mg to 60 mg per day, adapted according to the nature of the surgery and patient condition.
- Mechanical Ventilation: Similar to surgical procedures, the dose is adjusted on a case-by-case basis, typically 5 mg to 60 mg per day.
- Intensive Care Unit (ICU) Use: The dose is titrated as needed, in the range of 5 mg to 60 mg daily.
- Emergency Situations: Higher doses may be used initially and then tapered down based on patient condition.
Dosage Adjustments
Dose modifications may be required based on factors like renal or hepatic dysfunction, concomitant medications, and individual response. The dose should be titrated to the lowest effective dose to minimize side effects.
Side Effects
Common Side Effects
- Increased appetite
- Weight gain
- Fluid retention
- Mood changes
- Insomnia
- Increased sweating
- Thinning of the skin
Rare but Serious Side Effects
- Infections
- Osteoporosis
- Peptic ulcers
- Hyperglycemia
- Hypertension
- Cataracts
- Glaucoma
Long-Term Effects
Long-term use may lead to adrenal suppression, growth retardation in children, osteoporosis, and increased risk of infections.
Adverse Drug Reactions (ADR)
Clinically significant ADRs requiring immediate attention can include severe allergic reactions, adrenal crisis, infections, and mental status changes.
Contraindications
- Systemic fungal infections
- Hypersensitivity to prednisolone
- Live virus vaccinations (when used at immunosuppressive doses)
Drug Interactions
Prednisolone can interact with several drugs, including:
- NSAIDs
- Anticoagulants (e.g., warfarin)
- Antidiabetics
- Antihypertensives
- Immunosuppressants
- CYP450 inducers and inhibitors
Lifestyle factors such as alcohol consumption and smoking should be considered.
Pregnancy and Breastfeeding
Prednisolone is generally considered safe during pregnancy, especially during the second and third trimesters. Low doses during breastfeeding are generally safe. However, monitoring infants for potential side effects like adrenal suppression may be necessary with prolonged higher maternal dosages.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, modulating gene transcription and suppressing inflammatory and immune responses.
- Side Effects: Common: Weight gain, fluid retention, mood changes, insomnia. Serious: Infections, osteoporosis, hyperglycemia, hypertension.
- Contraindications: Systemic fungal infections, hypersensitivity, live virus vaccines.
- Drug Interactions: NSAIDs, anticoagulants, antidiabetics, antihypertensives, immunosuppressants.
- Pregnancy & Breastfeeding: Generally safe in pregnancy and during breastfeeding (low doses); monitor infant.
- Dosage: Adults: 5–60 mg/day; Children: 0.14–2 mg/kg/day.
- Monitoring Parameters: Blood pressure, blood glucose, electrolytes, weight, bone density (long-term use), signs of infection.
Popular Combinations
Often combined with other medications to treat specific conditions, for example:
- DMARDs (Disease Modifying Antirheumatic Drugs) for rheumatoid arthritis
- Bronchodilators for asthma or COPD
Precautions
- General Precautions: Monitor for signs of infection, adrenal suppression, and other side effects. Gradual tapering is necessary after prolonged use.
- Specific Populations: Pregnant women (caution in the first trimester); breastfeeding mothers (monitor infant at higher doses).
- Lifestyle Considerations: Limit alcohol intake; consider smoking cessation.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Prednisolone?
A: Adults: 5–60 mg/day, Children: 0.14–2 mg/kg/day. Dosage is adjusted based on the condition and patient response.
Q2: How should Prednisolone be administered?
A: Prednisolone is available as oral tablets, oral solution, and injectable solutions. Oral formulations should be taken with food to minimize gastrointestinal upset.
Q3: What are the serious side effects of Prednisolone?
A: Serious side effects can include increased susceptibility to infections, osteoporosis, peptic ulcers, hyperglycemia, hypertension, cataracts, glaucoma, adrenal suppression, and psychiatric disturbances.
Q4: What are the contraindications to Prednisolone use?
A: Systemic fungal infections, hypersensitivity to prednisolone, and administration of live virus vaccines during immunosuppressive doses are contraindications to its use.
Q5: Can Prednisolone be used during pregnancy and breastfeeding?
A: It is generally considered safe during pregnancy, especially in the second and third trimesters. Low doses during breastfeeding are usually considered safe, but monitoring infants for potential side effects, especially with prolonged higher maternal dosages, is advised.
Q6: What are the common drug interactions with Prednisolone?
A: Prednisolone can interact with NSAIDs, anticoagulants like warfarin, antidiabetic drugs, antihypertensives, and other immunosuppressants.
Q7: How should Prednisolone be discontinued after long-term use?
A: Abrupt discontinuation should be avoided. The dose should be gradually tapered down under medical supervision to prevent adrenal insufficiency and withdrawal symptoms.
Q8: What monitoring parameters are essential for patients on long-term Prednisolone?
A: Blood pressure, blood glucose levels, electrolytes, weight, bone density (to assess for osteoporosis), and regular monitoring for signs of infection are important parameters to monitor.
Q9: What is the difference between prednisone and prednisolone?
A: Prednisone is a prodrug that is converted to prednisolone in the liver. Prednisolone is the active form of the drug. Patients with severe liver disease may not adequately metabolize prednisone.
