prednisolone (Rx)

Frequency Not Defined

Acne

Adrenal suppression

Delayed wound healing

Diabetes mellitus

GI perforation

Glucose intolerance

Hepatomegaly

Hypokalemic alkalosis

Increased transaminases

Insomnia

Menstrual irregularity

Myopathy

Neuritis

Osteoporosis

Peptic ulcer

Perianal pruritus

Pituitary adrenal axis suppression

Pseudotumor cerebri (on withdrawal)

Psychosis

Seizure

Ulcerative esophagitis

Urticaria

Vertigo

Weight gain

Contraindications

Documented hypersensitivity

Systemic fungal infection, varicella, superficial herpes simplex keratitis

Receipt 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 (replacement therapy)

Cautions

Use with caution in cirrhosis, diabetes, ocular herpes simplex, hypertension, diverticulitis, following myocardial infarction, thyroid disease, seizure disorders, hypothyroidism, myasthenia gravis, hepatic impairment, peptic ulcer disease, osteoporosis, ulcerative colitis, psychotic tendencies, untreated systemic infections, renal insufficiency, pregnancy

Thromboembolic disorders or myopathy may occur

Delayed wound healing is possible

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

Parenteral forms (prednisolone sodium phosphate) have been discontinued

Suppression of hypothalamic-pituitary-adrenal axis may occur particularly in patients receiving high doses for prolonged periods or in young children; discontinuation of therapy should be done through slow taper

Posterior subcapular cataract formation associated with prolonged use of corticosteroids

Prolonged use of corticosteroids may increase risk of secondary infections

Increase in intraocular pressure associated with prolonged use of corticosteroids

Long-term use associated with fluid retention and hypertension

Development of Kaposi's sarcoma associated with prolonged corticosteroid use

Acute myopathy associated with high dose of corticosteroids

Corticosteroid use may cause psychiatric disturbances

If product is used for 10 days or longer, intraocular pressure should be routinely monitored even though it may be difficult in children and uncooperative patients; steroids should be used with caution in the presence of glaucoma. Intraocular pressure should be checked frequently

Steroids after cataract surgery may delay healing and increase incidence of bleb formation

Use of ocular steroids may prolong course and may exacerbate severity of many viral infections of the eye (including herpes simplex)

Pregnancy

Prednisolone shown to be teratogenic in mice when given in doses 1-10 times human dose; dexamethasone, hydrocortisone, and prednisolone were ocularly applied to both eyes of pregnant mice five times per day on days 10 through 13 of gestation; a significant increase in the incidence of cleft palate observed in fetuses of treated mice; there are no adequate well-controlled studies in pregnant women; prednisolone should be used during pregnancy only if potential benefit justifies potential risk to fetus

Lactation

Not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk; systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects

Because of potential for serious adverse reactions in nursing infants from prednisolone, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account importance of drug to mother

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

Absorption

Duration: 18-36 hr

Peak plasma time: 5 min (IV); 1 hr (PO)

Distribution

Protein bound: 65-91% (lower in elderly)

Vd: 0.22-0.7 L/kg

Metabolism

Extensively metabolized in liver

Elimination

Half-life: 3.6 hr (normal renal function); 3-5 hr (end-stage renal disease)

Dialyzable: Hemodialysis, no

Renal clearance: 9.5 mL/min

Excretion: Urine (mainly)