Dosing & Uses
tablet, delayed release
5-60 mg/day PO in single daily dose or divided q6-12hr
- When converting from immediate-release to delayed-release formulation, note that delayed-release formulation takes about 4 hours to release active substances
- Note that exogenous steroids suppress adrenal cortex activity least during maximal natural adrenal cortex activity (between 4:00 and 8:00 AM)
40-60 mg/day PO in single daily dose or divided q12hr for 3-10 days
Giant Cell Arteritis
40-60 mg PO qDay (1-2 years usual duration of treatment)
Idiopathic Thrombocytopenic Purpura
Day 1: 10 mg PO before breakfast, 5 mg after lunch and after dinner, and 10 mg at bedtime
Day 2: 5 mg PO before breakfast, after lunch, and after dinner and 10 mg at bedtime
Day 3: 5 mg PO before breakfast, after lunch, after dinner, and at bedtime
Day 4: 5 mg PO before breakfast, after lunch, and at bedtime
Day 5: 5 mg PO before breakfast and at bedtime
Day 6: 5 mg PO before breakfast
Immediate-release: ≤10 mg/day PO added to disease-modifying antirheumatic drugs (DMARDs)
Delayed-release: 5 mg/day PO initially; maintenance: lowest dosage that maintains clinical response; may be taken at bedtime to decrease morning stiffness with rheumatoid arthritis
Advanced Pulmonary/Extrapulmonary Tuberculosis
40-60 mg/day PO, tapered over 4-8 weeks
Pneumocystis (carinii) jiroveci Pneumonia in Patients With AIDS (Off-label)
40 mg PO q12hr for 5 days, then 40 mg PO q24hr for 5 days, then 20 mg q24hr for 11 days
Crohn’s Disease (Off-label)
40-60 mg PO qDay until resolution and resumption of weight gain (7-28 days usual duration)
60 mg PO qDay for 1 week; THEN 40 mg qDay for 1 week; THEN 30 mg qDay for 2 weeks; follow by 20 mg qDay; give half this dose if giving in combinaiton with azathioprine
Take with meal or snack
High-dose glucocorticoids may cause insomnia; immediate-release formulation is typically administered in morning to coincide with circadian rhythm
Delayed-release formulation takes about 4 hours to release active substances; thus, with this formulation, timing of dose should take into account delayed-release pharmacokinetics and disease or condition being treated (eg, may be taken at bedtime to decrease morning stiffness with rheumatoid arthritis)
Dosage Forms & Strengths
tablet, delayed release
0.5-2 mg/kg/day PO in single daily dose or divided q12hr; not to exceed 80 mg/day
<12 years: 1-2 mg/kg/day PO in single daily dose or divided q12hr for 3-10 days; not to exceed 80 mg/day
≥12 years: 40-60 mg/day PO in single daily dose or divided q12hr for 3-10 days
2 mg/kg/day PO; not to exceed 80 mg/day
Pneumocystis (carinii) jiroveci Pneumonia in Patients With AIDS (Off-label)
<12 years: 1 mg/kg PO q12hr for 5 days, then 0.5-1 mg/kg q12hr for 5 days, then 0.5 mg/kg q24hr for 11-21 days
>12 years: 40 mg PO q12hr for 5 days, then 40 mg PO q24hr for 5 days, then 20 mg q24hr for 11 days
Serious – Use Alternative
Significant – Monitor Closely
Frequency Not Defined
Allergic: Anaphylaxis, angioedema
Cardiovascular: Bradycardia, cardiac arrest, cardiac arrhythmias, cardiac enlargement, circulatory collapse, congestive heart failure, fat embolism, hypertension, hypertrophic cardiomyopathy in premature infants, myocardial rupture after recent myocardial infarction, pulmonary edema, syncope, tachycardia, thromboembolism, thrombophlebitis, vasculitis
Dermatologic: Acne, allergic dermatitis, cutaneous and subcutaneous atrophy, dry scalp, edema, facial erythema, hyper- or hypopigmentation, impaired wound healing, increased sweating, petechiae and ecchymoses, rash, sterile abscess, striae, suppressed reactions to skin tests, thin fragile skin, thinning scalp hair, urticaria
Endocrine: Abnormal fat deposits, decreased carbohydrate tolerance, development of cushingoid state, hirsutism, manifestations of latent diabetes mellitus and increased requirements for insulin or oral hypoglycemic agents in diabetics, menstrual irregularities, moon facies, secondary adrenocortical and pituitary unresponsiveness (particularly in times of stress, as in trauma, surgery, or illness), suppression of growth in children
Fluid and electrolyte disturbances: Fluid retention, potassium loss, hypertension, hypokalemic alkalosis, sodium retention
Gastrointestinal: Abdominal distention, elevation of serum liver enzymes levels (usually reversible upon discontinuance), hepatomegaly, hiccups, malaise, nausea, pancreatitis, peptic ulcer with possible perforation and hemorrhage, ulcerative esophagitis
General: Increased appetite and weight gain
Metabolic: Negative nitrogen balance due to protein catabolism
Musculoskeletal: Osteonecrosis of femoral and humeral heads, Charcot-like arthropathy, loss of muscle mass, muscle weakness, osteoporosis, pathologic fracture of long bones, steroid myopathy, tendon rupture, vertebral compression fractures
Neurologic: Arachnoiditis, convulsions, depression, emotional instability, euphoria, headache, increased intracranial pressure with papilledema (pseudotumor cerebri; usually following discontinuance of treatment), insomnia, meningitis, mood swings, neuritis, neuropathy, paraparesis/paraplegia, paresthesia, personality changes, sensory disturbances, vertigo
Ophthalmic: Exophthalmos, glaucoma, increased intraocular pressure, posterior subcapsular cataracts, central serous chorioretinopathy
Reproductive: Alteration in motility and number of spermatozoa
Untreated serious infections
Administration of live or attenuated live vaccine (Advisory Committee on Immunization Practices (ACIP) and American Academy of Family Physicians (AAFP) state that administration of live virus vaccines usually is not contraindicated in patients receiving corticosteroid therapy as short-term (<2 weeks) treatment, in low-to-moderate dosages, as long-term alternate-day treatment with short-acting preparations, or in maintenance of physiologic dosages, such as, replacement therapy)
Monitor for hypothalamic-pituitary-adrenal (HPA) axis suppression, Cushing syndrome, and hyperglycemia
Prolonged use associated with increased risk of infection; monitor
Use with caution in cirrhosis, ocular herpes simplex, hypertension, diverticulitis, hypothyroidism, myasthenia gravis, peptic ulcer disease, osteoporosis, ulcerative colitis, psychotic tendencies, renal insufficiency, pregnancy, diabetes mellitus, congestive heart failure, thromboembolic disorders, GI disorders
Long-term treatment associated with increased risk of osteoporosis, myopathy, delayed wound healing
Patients receiving corticosteroids should avoid chickenpox or measles-infected persons if unvaccinated
Latent tuberculosis may be reactivated (patients with positive tuberculin test should be monitored)
Some suggestion (not fully substantiated) of slightly increased cleft palate risk if corticosteroids are used in pregnancy
Methylprednisolone is preferred in hepatic impairment because prednisone must be converted to prednisolone in liver
Prolonged corticosteroid use may result in elevated intraocular pressure, glaucoma, or cataracts
May cause impairment of mineralocorticoid secretion; administer mineralocorticoid concomitantly
May cause psychiatric disturbances; monitor for behavioral and mood changes; may exacerbate pre-existing psychiatric conditions
Monitor for Kaposi sarcoma
Pregnancy & Lactation
Pregnancy category: C (immediate release); D (delayed release)
Drug may cause fetal harm and decreased birth weight; maternal corticosteroid use during first trimester increases incidence of cleft lip with or without cleft palate
Lactation: Of maternal serum metabolites, 5-25% are found in breast milk; not recommended, or, if benefit outweighs risk, use lowest dose
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Mechanism of Action
Glucocorticosteroid; elicits mild mineralocorticoid activity and moderate anti-inflammatory effects; controls or prevents inflammation by controlling rate of protein synthesis, suppressing migration of polymorphonuclear leukocytes (PMNs) and fibroblasts, reversing capillary permeability, and stabilizing lysosomes at cellular level; in physiologic doses, corticosteroids are administered to replace deficient endogenous hormones; in larger (pharmacologic) doses, they decrease inflammation
Duration: Plasma, 60 min; biologic, 8-36 hr
Peak plasma time: PO (immediate release), 2 hr; PO (delayed release), 6.0-6.5 hr
Protein bound: 65-91%
Extensively metabolized in liver; hydroxylated to active metabolite; conversion can be impaired in liver disease
Metabolite: Prednisolone (active)
Half-life: 2.6-3 hr
Dialyzable: Hemodialysis, no
Excretion: Urine (mainly)
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