prednisone
Apo-Prednisone ◆, Deltasone, Meticorten, Orasone, Prednicen-M, Sterapred, Winpred ◆

Pharmacologic classification: adrenocorticoid
Therapeutic classification: anti-inflammatory, immunosuppressant
Pregnancy risk category C


Available forms
Available by prescription only
Oral solution: 5 mg/ml, 5 mg/5 ml
Syrup: 5 mg/5 ml
Tablets: 1 mg, 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg

Indications and dosages
 Severe inflammation, modification of body’s immune response to disease. Adults: 5 to 60 mg P.O. daily in single dose or divided doses. Maximum daily dose is 250 mg. Maintenance dose given once daily or every other day. Dosage must be individualized.
Children: 0.14 to 2 mg/kg or 4 to 60 mg/m2 P.O. daily in divided doses.
 Adjunct to anti-infective therapy in treatment of moderate to severe Pneumocystis carinii pneumonia ◇. Adults or children older than age 13 with AIDS: 40 mg P.O. b.i.d. for 5 days; then 40 mg P.O. once daily for 5 days; then 20 mg P.O. once daily for 11 days (or until completion of the concurrent anti-infective regimen).

Pharmacodynamics
Immunosuppressant action: Stimulates the synthesis of enzymes needed to decrease the inflammatory response. 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.
Anti-inflammatory action: One of the intermediate-acting glucocorticoids, with greater glucocorticoid activity than cortisone and hydrocortisone but less anti-inflammatory activity than betamethasone, dexamethasone, and paramethasone. About four to five times more potent as an anti-inflammatory than hydrocortisone, but has only half the mineralocorticoid activity of an equal weight of hydrocortisone. The oral glucocorticoid of choice for anti-inflammatory or immunosuppressive effects.

Pharmacokinetics
Absorption: Absorbed readily after oral administration.
Distribution: Distributed rapidly to muscle, liver, skin, intestines, and kidneys. Extensively bound to plasma proteins (transcortin and albumin); only unbound portion is active. Distributed into breast milk and through the placenta.
Metabolism: Metabolized in liver to active metabolite prednisolone, which is then metabolized to inactive glucuronide and sulfate metabolites.
Excretion: Inactive metabolites and small amounts of unmetabolized drug excreted by kidneys. Insignificant drug quantities also excreted in feces. Biological half-life of prednisone is 18 to 36 hours.

Route Onset Peak Duration
P.O. Variable 1-2 hr Variable


Contraindications and precautions
Contraindicated in patients hypersensitive to drug and in those with systemic fungal infections.
  Use cautiously in patients with 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, and psychotic tendencies.

Interactions
Drug-drug. Amphotericin B, diuretics: Enhances hypokalemia. Monitor serum potassium level.
Antacids, cholestyramine, colestipol: Decreases prednisone absorption. Separate administration times.
Barbiturates, phenytoin, rifampin: Decreases corticosteroid effects because of increased hepatic metabolism. Monitor patient.
Cardiac glycosides: May cause hypokalemia, increasing risk of toxicity in patients receiving these drugs. Monitor serum potassium level.
Estrogens: Reduces metabolism of prednisone 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.
Drug-herb. Alfalfa sprouts, astragalus, echinacea, licorice: May interfere with immunosuppressive effect of drug. Discourage use together.

Adverse reactions
CNS: euphoria, insomnia, psychotic behavior, pseudotumor cerebri, vertigo, headache, paresthesia, seizures.
CV: hypertension, edema, arrhythmias, thrombophlebitis, thromboembolism, heart failure.
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.
• Drug may be used for alternate-day therapy.
• Always adjust to lowest effective dose.
• Most adverse reactions to corticosteroids are dose- or duration-dependent.
• 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.
• For better results and less toxicity, give a once-daily dose in the morning.
• Unless contraindicated, give oral dose with food when possible to reduce GI irritation. Patient may need medication to prevent GI irritation.
• The oral solution may be diluted in juice or other flavored diluent or semi-solid food (such as applesauce) before administration.
• Drug may mask or worsen infections, including latent amebiasis.
• Unless contraindicated, give low-sodium diet that’s high in potassium and protein. Administer potassium supplements as needed.
 ALERT Gradually reduce dosage after long-term therapy. After abrupt withdrawal: 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 prednisone with prednisolone.
• For patients who can’t swallow tablets, liquid forms are available. The oral concentrate (5 mg/ml) may be diluted in juice or another flavored diluent or mixed in semisolid food (such as applesauce) before administration.
• Prednisone 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.
Breast-feeding patients
• Drug appears in breast milk. Women shouldn’t breast-feed while taking this drug.
Pediatric patients
• Prolonged use of prednisone in children or adolescents may delay growth and maturation.
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 drug with food or milk.
• Teach patient evidence 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.
• Advise patient receiving long-term therapy to consider exercise or physical therapy. Also, advise patient about vitamin D or calcium supplement.
• Tell patient to report slow healing.
• Advise patient receiving long-term therapy to have periodic ophthalmic examinations.
• Instruct patient to avoid exposure to infections and to call if exposure occurs.
• Tell patient to report fluid retention if it occurs.
• Instruct patient to not become immunized during drug therapy.
• 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