prednisolone (systemic)
Delta-Cortef, Prelone

prednisolone acetate
Cotolone, Key-Pred 25, Predalone 50, Predcor-50

prednisolone sodium phosphate
Hydeltrasol, Key-Pred-SP, Orapred, Pediapred

prednisolone tebutate
Nor-Pred T.B.A., Predate TBA, Predcor-TBA, Prednisol TBA

Available forms
Available by prescription only
prednisolone
Syrup: 5 mg/ml, 15 mg/5 ml
Tablets: 5 mg
prednisolone acetate
Injection: 25 mg/ml, 50 mg/ml suspension
prednisolone sodium phosphate
Injection: 20 mg/ml solution
Oral liquid: 5 mg/5 ml, 15 mg/5 ml
prednisolone tebutate
Injection: 20 mg/ml suspension

Indications and dosages
 Severe inflammation, modification of body’s immune response to disease. prednisolone.
Adults: 2.5 to 15 mg P.O. b.i.d., t.i.d., or q.i.d.
Children: Initially 0.14 to 2 mg/kg/day P.O. or 4 to 60 mg/m²/day in 4 divided doses.
prednisolone acetate
Adults: 2 to 30 mg I.M. q 12 hours.
Children: 0.04 to 0.25 mg/kg or 1.5 to 7.5 mg/m² I.M. once or twice daily.
prednisolone sodium phosphate
Adults: 5 to 60 mg I.M., I.V., or P.O. daily.
Children: Initially 0.14 to 2 mg/kg/day or 4 to 60 mg/m²/day in three or four divided doses I.M., I.V., or P.O.
prednisolone tebutate
Adults: 4 to 40 mg into joints and lesions, p.r.n.
 Acute exacerbations of multiple sclerosis. prednisolone sodium phosphate. Children: 200 mg/day P.O. for a week followed by 80 mg every other day.
 Nephrotic syndrome. prednisolone sodium phosphate. Children: 60 mg/m²/day P.O. in three divided doses for 4 weeks, followed by 4 weeks of single dose alternate-day therapy at 40 mg/m²/day.
 Uncontrolled asthma in those taking by inhaled corticosteroids and long-acting bronchodilators. prednisolone sodium phosphate.
Children: 1-2 mg/kg/day P.O. in single or divided doses. It is further recommended that short course, or "burst" therapy, be continued until a child achieves a peak expiratory flow rate of 80% of his or her personal best or symptoms resolve. This usually requires 3 to 10 days of treatment, although it can take longer. There is no evidence that tapering the dose after improvement wil prevent a relapse.

Pharmacodynamics
Anti-inflammatory action: Prednisolone stimulates the synthesis of enzymes needed to decrease the inflammatory response. It suppresses the immune system by reducing activity and volume of the lymphatic system, thus producing lymphocytopenia (primarily of T-lymphocytes), decreasing immunoglobulin and complement levels, decreasing passage of immune complexes through basement membranes, and possibly by depressing reactivity of tissue to antigen-antibody interactions.
 The mineralocorticoids regulate electrolyte homeostasis by acting renally at the distal tubules to enhance the reabsorption of sodium ions (and thus water) from the tubular fluid into the plasma and enhance the excretion of both potassium and hydrogen ions.
 Prednisolone is an adrenocorticoid with both glucocorticoid and mineralocorticoid properties. It’s a weak mineralocorticoid with only half the potency of hydrocortisone but is a more potent glucocorticoid, having four times the potency of equal weight of hydrocortisone. It’s used primarily as an anti-inflammatory drug and an immunosuppressant. It’s not used for mineralocorticoid replacement therapy because of the availability of more specific and potent drugs.
 Prednisolone may be administered orally. Prednisolone sodium phosphate is highly soluble, has a rapid onset and a short duration of action, and may be given P.O., I.M., or I.V. Prednisolone acetate and tebutate are suspensions that may be administered by intra-articular, intrasynovial, intrabursal, intralesional, or soft-tissue injection. They have a slow onset but a long duration of action.

Pharmacokinetics
Absorption: Absorbed readily after oral administration. Acetate and tebutate suspensions for injection have a variable absorption rate over 24 to 48 hours, depending on whether injected into intra-articular space or muscle, and on blood supply to that muscle. Slow systemic absorption after intra-articular injection.
Distribution: Removed rapidly from blood and distributed to muscle, liver, skin, intestines, and kidneys. Extensively bound to plasma proteins (transcortin and albumin); only unbound portion is active. Adrenocorticoids distributed into breast milk and through the placenta.
Metabolism: Metabolized in liver to inactive glucuronide and sulfate metabolites.
Excretion: Inactive metabolites, and small amounts of unmetabolized drug, excreted in urine. Insignificant drug quantities excreted in feces. Biological half-life 18 to 36 hours.

Contraindications and precautions
Contraindicated in patients hypersensitive to drug or its components and in those with systemic fungal infections.
  Use cautiously in patients with a recent MI, GI ulcer, renal disease, hypertension, osteoporosis, diabetes mellitus, hypothyroidism, cirrhosis, diverticulitis, nonspecific ulcerative colitis, recent intestinal anastomoses, thromboembolic disorders, seizures, myasthenia gravis, heart failure, tuberculosis, ocular herpes simplex, emotional instability, or psychotic tendencies.

Interactions
Drug-drug. Amphotericin B, diuretics: Enhances hypokalemia. Monitor serum potassium level.
Antacids, cholestyramine, colestipol: Decreases prednisolone absorption. Separate administration times.
Barbiturates, phenytoin, rifampin: Decreases corticosteroid effects because of increased hepatic metabolism. Monitor patient.
Cardiac glycosides: May cause hypokalemia, increase risk of toxicity in patients receiving these drugs. Monitor serum potassium level.
Estrogens: Reduces metabolism of prednisolone via increased level of transcortin; half-life of corticosteroid prolonged because of increased protein-binding. Adjust dosage as needed.
Insulin, oral antidiabetics: Causes hyperglycemia. Adjust dosages of these drugs as needed.
Isoniazid, salicylates: Increases metabolism of these drugs. Monitor patient closely.
Oral anticoagulants: Decreases effects. Monitor PT and INR.
Ulcerogenic drugs (such as NSAIDs): Increases risk of GI ulceration. Use together cautiously.

Adverse reactions
CNS: euphoria, insomnia, psychotic behavior, pseudotumor cerebri, vertigo, headache, paresthesia, seizures.
CV: heart failure, thromboembolism, hypertension, edema, arrhythmias, thrombophlebitis.
EENT: cataracts, glaucoma.
GI: peptic ulceration, GI irritation, increased appetite, pancreatitis, nausea, vomiting.
GU: menstrual irregularities.
Metabolic: hypokalemia, hyperglycemia, carbohydrate intolerance.
Musculoskeletal: muscle weakness, osteoporosis, growth suppression in children.
Skin: delayed wound healing, acne, various skin eruptions, hirsutism.
Other: susceptibility to infections; acute adrenal insufficiency (with increased stress from infection, surgery, or trauma); cushingoid state (moonface, buffalo hump, central obesity).

Effects on lab test results
• May increase glucose and cholesterol levels. May decrease potassium and calcium levels.

Overdose and treatment
Acute ingestion, even in massive doses, is rarely a clinical problem. Toxic signs and symptoms rarely occur if drug is used for less than 3 weeks, even at large dosage ranges. However, chronic use causes adverse physiologic effects, including suppression of the hypothalamic-pituitary-adrenal axis, cushingoid appearance, muscle weakness, and osteoporosis.

Special considerations
• Determine if patient is sensitive to other corticosteroids.
• Use only prednisolone sodium phosphate for I.V. administration. When administering as direct injection, inject undiluted over at least 1 minute. When administering as intermittent or continuous infusion, dilute solution according to manufacturer’s instructions. Use D₅W or normal saline solution as diluent for I.V. infusion.
• Always adjust to lowest effective dose.
• Monitor patient’s weight, blood pressure, and serum electrolyte levels.
• Monitor patient for cushingoid effects, including moonface, buffalo hump, central obesity, thinning hair, hypertension, and increased susceptibility to infection.
• Prednisolone salts (sodium phosphate and tebutate) are used parenterally less often than other corticosteroids that have more potent anti-inflammatory action.
• Drug may be used for alternate-day therapy.
• Most adverse reactions to corticosteroids are dose- or duration-dependent.
• Give oral dose with food when possible to reduce GI irritation. Patient may need medication to prevent GI irritation.
• Give I.M. injection deeply into gluteal muscle. Rotate injection sites to prevent muscle atrophy. Avoid S.C. injection because atrophy and sterile abscesses may occur.
• Prednisolone acetate and tebutate aren’t for I.V. use.
• Unless contraindicated, give low-sodium diet that’s high in potassium and protein. Administer potassium supplements as needed.
• Drug may mask or worsen infections, including latent amebiasis.
• Gradually reduce dosage after long-term therapy.
 ALERT After abrupt withdrawal, patient may experience rebound inflammation, fatigue, weakness, arthralgia, fever, dizziness, lethargy, depression, fainting, orthostatic hypotension, dyspnea, anorexia, hypoglycemia. After prolonged use, sudden withdrawal may cause acute adrenal insufficiency and death.
 ALERT Don’t confuse prednisolone with prednisone.
• Prednisolone suppresses reactions to skin tests; causes false-negative results in the nitroblue tetrazolium test for systemic bacterial infections.
• Watch for depression or psychotic episodes, especially during high-dose therapy.
• Diabetic patient may need increased insulin. Monitor blood glucose levels.
Pediatric patients
• Prolonged use of adrenocorticoids or corticotropin may suppress growth and maturation in children and adolescents.
Geriatric patients
• Elderly patients may be more susceptible to osteoporosis with long-term use.

Patient education
• Tell patient not to stop drug abruptly or without medical approval.
• Instruct patient to take oral form of drug with food or milk.
• Tell patient symptoms of early adrenal insufficiency: fatigue, muscle weakness, joint pain, fever, anorexia, nausea, dyspnea, dizziness, and fainting.
• Instruct patient to carry or wear medical identification indicating his need for supplemental systemic glucocorticoids during stress. It should include prescriber’s name, name of drug, and dosage taken.
• Warn patient on long-term therapy about cushingoid effects (moonface, buffalo hump) and the need to report sudden weight gain or swelling.
• Tell patient to report slow healing.
• Advise patient receiving long-term therapy to consider exercise or physical therapy. Advise him about vitamin D or calcium supplement.
• Instruct patient to avoid exposure to infections and call if exposure occurs.
• Tell patient to avoid immunizations while taking drug.
• Advise patient to be aware of signs of infection; some of these signs may be masked during drug use.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use