prednisone (Rx)

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

Contraindications

Untreated serious infections

Documented hypersensitivity

Varicella

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)

Cautions

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 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

Pregnancy Categories

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

Absorption

Bioavailability: 92%

Duration: Plasma, 60 min; biologic, 8-36 hr

Peak plasma time: PO (immediate release), 2 hr; PO (delayed release), 6.0-6.5 hr

Distribution

Protein bound: 65-91%

Metabolism

Extensively metabolized in liver; hydroxylated to active metabolite; conversion can be impaired in liver disease

Metabolite: Prednisolone (active)

Elimination

Half-life: 2.6-3 hr

Dialyzable: Hemodialysis, no

Excretion: Urine (mainly)