AHFS Class:

• Adrenals 68:04

Generic Name(s):

• prednisoLONE

• prednisoLONE Sodium Phosphate

Prednisolone is a synthetic glucocorticoid.

Prednisolone is used principally as an anti-inflammatory or immunosuppressant agent. Because prednisolone has only minimal mineralocorticoid properties, the drug is inadequate alone for the management of adrenocortical insufficiency. If prednisolone is used in the treatment of this condition, concomitant therapy with a mineralocorticoid is also required.

Dosage

The dosage of prednisolone and its derivatives depends on the condition being treated and the response of the patient. Dosage for infants and children should be based on the severity of the disease and the response of the patient rather than on strict adherence to dosage indicated by age, body weight, or body surface area. After a satisfactory response is obtained, dosage should be decreased in small decrements to the lowest level that maintains an adequate clinical response. Patients should be continually monitored for signs that indicate dosage adjustment is necessary, such as remissions or exacerbations of the disease and stress (surgery, infection, trauma). When long-term oral prednisolone therapy is necessary, an alternate-day dosage regimen should be considered. Following long-term therapy, prednisolone should be withdrawn gradually.

Prednisolone

Prednisolone is administered orally. The initial adult dosage of prednisolone may range from 5-60 mg daily, depending on the disease being treated, and is usually administered in 2-4 divided doses. Some clinicians state that children may be given a prednisolone dosage of 0.14-2 mg/kg daily or 4-60 mg/m² daily, administered in 4 divided doses.

Prednisolone Sodium Phosphate

Prednisolone sodium phosphate is administered orally as a solution or orally disintegrating tablets; the drug also has been given by IM, IV, intra-articular, intralesional, or soft tissue injection or by IV infusion (a parenteral preparation of prednisolone sodium phosphate no longer is commercially available in the US). Patients should be instructed not to remove the orally disintegrating tablet from the blister card until just prior to dosing. Prednisolone sodium phosphate orally disintegrating tablets should be allowed to dissolve on the tongue or should be swallowed whole with or without water ; the tablets should not be broken. If the dosage of prednisolone required does not correspond to the strength of the commercially available prednisolone sodium phosphate orally disintegrating tablets, another formulation of prednisolone should be used.

Dosage of prednisolone sodium phosphate is expressed in terms of prednisolone. The amount of drug each patient receives should be individualized according to diagnosis, severity, and patient response. The initial dosage of prednisolone ranges from 5-60 mg daily depending on the disease being treated. In less severe diseases, a lower dosage may be sufficient, while in selected patients with severe disease, dosages greater than the initial dosage may be required. In pediatric patients, the initial dosage of prednisolone may range from 0.14-2 mg/kg daily in 3 or 4 divided doses or 4-60 mg/m² daily. The initial dosage should be maintained or adjusted until a satisfactory response is obtained. Patients should be continually monitored for signs that indicate dosage adjustment is necessary, such as remission or exacerbations of disease and stress. Patients may require higher dosages of prednisolone when they are subjected to stress. Following long-term therapy, prednisolone should be withdrawn gradually.

Multiple Sclerosis

For the treatment of acute exacerbations of multiple sclerosis, the usual oral dosage of prednisolone is 200 mg daily for one week, followed by 80 mg every other day for a month.

Nephrotic Syndrome

In the treatment of nephrotic syndrome in children, the usual oral dosage of prednisolone solution is 60 mg/m² daily given in 3 divided doses for 4 weeks, followed by 4 weeks of alternate-day therapy at single doses of 40 mg/m².

Asthma

To gain prompt control of asthma in infants and children 4 years of age or younger with very poorly controlled, moderate-to-severe asthma (i.e., more than 3 exacerbations per year requiring oral corticosteroids) and in children 5-11 years of age with asthma of comparable control and severity (i.e., at least 2 exacerbations per year requiring oral corticosteroids), prednisolone 1-2 mg/kg daily (maximum 60 mg daily) may be added to existing asthma therapy.

In adults and adolescents with very poorly controlled, moderate-to-severe asthma (i.e. at least 2 exacerbations per year requiring oral corticosteroids), prednisolone 40-60 mg daily as a single dose or in 2 divided doses may be added to low-to-high maintenance dosages of the inhaled corticosteroid and a long-acting inhaled β₂-agonist bronchodilator.

A short course of oral corticosteroid therapy (usually 3-10 days) should be continued until the patient achieves a peak expiratory flow (PEF) of at least 80% of his or her personal best and until symptoms resolve. However, a longer duration of treatment may be needed in some patients. There is no evidence that tapering the dosage after improvement will prevent a relapse.

For the treatment of moderate-to-severe exacerbations of asthma associated with a viral respiratory infection in infants and children 4 years of age or younger with intermittent asthma, prednisolone 1 mg/kg daily for 3-10 days or equivalent daily dosage should be considered. For those with a history of viral-associated severe asthma exacerbations, initiation of oral corticosteroids should be considered at the first sign of infection.

For the treatment of acute asthma exacerbations in the community setting, 0.5-1 mg/kg of prednisolone or equivalent during a 24-hour period is recommended to quickly resolve all but the mildest exacerbations of asthma, especially in patients whose response to a short-acting inhaled β₂-agonist is not prompt or sustained. For emergency department treatment of moderate-to-severe acute asthma exacerbations not controlled with an inhaled β₂-adrenergic agonist in children 11 years of age or younger, prednisolone 1-2 mg/kg daily in 2 divided doses (maximum 60 mg daily) can be added. For treatment of such exacerbations in adults and adolescents, prednisolone 40-80 mg daily as a single dose or in 2 divided doses can be added to an inhaled β₂-agonist. Treatment should be continued until the patient achieves a PEF of 70% of predicted or personal best. .

Chemistry and Stability

Chemistry

Prednisolone is a synthetic glucocorticoid. Prednisolone occurs as white to practically white, odorless, crystalline powder. Prednisolone, which may be anhydrous or contain 1.5 molecules of water of hydration, is very slightly soluble in water and sparingly soluble in alcohol. The sodium phosphate ester of prednisolone occurs as white or slightly yellow, friable granules or powder which is odorless or has a slight odor and is freely soluble in water, soluble in methanol, slightly soluble in alcohol and chloroform, and very slightly soluble in acetone and dioxane. The sodium phosphate ester of prednisolone is hygroscopic. Each 6.7 mg of prednisolone sodium phosphate is equivalent to 5 mg of prednisolone.

Stability

Commercially available preparations of prednisolone should be stored at a temperature less than 40°C, preferably between 15-30°C; freezing of the oral solutions should be avoided. Prednisolone oral solution should be stored at 15-30°C; such solutions should not be refrigerated. Prednisolone sodium phosphate oral solution (Pediapred^®) should be stored at 4-25°C and may be refrigerated. Prednisolone sodium phosphate oral solutions (Orapred^® and some generic preparations) should be stored at 2-8°C. Prednisolone sodium phosphate orally disintegrating tablets (Orapred ODT^®) should be stored at 20-25°C and protected from moisture. Prednisolone and prednisolone sodium phosphate oral solutions should be protected from light. Solutions of prednisolone and its derivatives are heat labile and must not be autoclaved.

Additional Information

For further information on chemistry, pharmacology, pharmacokinetics, uses, cautions, drug interactions, laboratory test interferences, and dosage and administration of prednisolone, see the Corticosteroids General Statement 68:04. For EENT uses, see 52:08.08. The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.