CorticosteroidsRx

Trade Names
Oral
Prednisone: Deltasone, Rayos (delayed release)
Prednisolone: Orapred, Millipred
Methylprednisolone: Medrol
Dexamethasone: Decadron
Parenteral
Methylprednisolone sodium succinate: Solu-Medrol
Hydrocortisone: Solu-Cortef
Dexamethasone: Decadron
Intraarticular
Methylprednisolone acetate suspension: Depo-Medrol
Triamcinolone acetonide suspension: Kenalog
Triamcinolone diacetate suspension: Aristocort Forte
Triamcinolone hexacetonide suspension: Aristospan Intra-articular

Drug Class: Glucocorticoid

Preparations
Oral
Prednisone: 1-, 2.5-, 5-, 10-, 20-, 50-mg tablets
Prednisolone: 2-, 4-, 8-, 16-, 24-mg tablets
Dexamethasone: 0.25-, 0.5-, 0.75-, 1-, 1.5-, 2-, 4-, 6-mg
Parenteral
Methylprednisolone sodium succinate injection: 40, 125, 500, 1,000, 2,000 mg
Hydrocortisone injection: 50, 100, 250, 500 mg
Dexamethasone: 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6 mg
Intraarticular
Methylprednisolone acetate suspension: 20, 40, 80 mg/mL
Triamcinolone acetonide suspension: 10 and 40 mg/mL
Triamcinolone diacetate suspension: 40 mg/mL
Triamcinolone hexacetonide suspension: 20 mg/mL

Dose: Varies according to the indication; adult dose ranges from 2 to 80 mg/day. For serious inflammatory disease,  a common approach is to give  1 mg/kg/day of prednisone or equivalent initially and titrate down according to response. Approximate equivalent doses for glucocorticoid efficacy: 0.75 mg dexamethasone = 4 mg methylprednisolone = 5 mg prednisone or prednisolone = 20 mg hydrocortisone. Intraarticular doses of depot steroid depend on the size of the joint.

Indications: Anti-inflammatory or immunosuppressant therapy in a wide range of diseases including inflammatory arthritis, inflammatory muscle disease, vasculitis, SLE, and RA.

Mechanism of Action: A wide range of effects on numbers of inflammatory cells, their migration, and production of inflammatory mediators

Contraindications: Known hypersensitivity to a glucocorticoid preparation

Precautions: Use caution in diabetes, atherosclerosis, immunosuppression, hypertension, osteoporosis, infection, peptic ulcer, and cirrhosis. Because of dose-related adverse effects, the minimum effective dose should be used. After prolonged glucocorticoid therapy, acute adrenal insufficiency may occur if the glucocorticoid is discontinued abruptly. After discontinuation of glucocorticoid therapy, the hypothalamus-pituitary-adrenal axis may remain suppressed for as long as a year, so supplementary doses of glucocorticoid are required during acute stress such as surgery. Increased risk of infections including tuberculosis.

Monitoring: Monitor for adverse effects with long-term therapy; consider monitoring potassium and glucose concentrations and bone density and consider osteoporosis prophylaxis or treatment (with long-term use).

Pregnancy Risk: C

Adverse Effects: Most are dose related. Almost all patients on high doses for more than a few weeks experience adverse effects, including cushingoid appearance, weight gain, skin fragility, bruising, impaired wound healing, edema, hypertension, diabetes, hypokalemia, atherosclerosis, cataracts, infection, insomnia, mood swings, psychosis, GI ulceration with NSAIDs, myopathy, osteoporosis, fractures, and pancreatitis. Suppression of the hypothalamus-pituitary-adrenal axis and acute adrenal insufficiency may occur if therapy is discontinued suddenly or with severe physiologic stress (major surgery) after therapy has been discontinued.

Drug Interactions
Hepatic enzyme inducers (rifampin, phenytoin, phenobarbitone): Decreased effect of corticosteroids
Diuretics: Increased potassium depletion

Patient Instructions: Corticosteroids should not be discontinued suddenly. Before a procedure or surgery, notify your surgeon or doctor that you are receiving corticosteroids. Careful attention to diet is necessary to avoid significant weight gain.

Comments: Marked leukocytosis and neutrophilia occur after even a single dose of glucocorticoid, and if the cause is not recognized, an unnecessary infection workup results. Adverse effects are related to dose and duration of therapy. Once disease control has been established, high doses of steroids can often be tapered relatively rapidly with 5- to 10-mg decrements at doses between 40 and 60 mg. Lower doses require a more gradual taper. Between 20 and 40 mg, taper in 5-mg decrements; between 10 and 20 mg, taper in 2.5-mg decrements, and <10 mg, taper in 1-mg decrements. A common error is tapering high doses too slowly and low doses too fast, resulting in adverse effects and disease flare, respectively.

Triamcinolone hexacetonide is the least soluble intraarticular preparation and has the longest duration of action. Triamcinolone or other fluorinated corticosteroid preparations should not be used for injection of soft tissue or bursae because marked atrophy of soft tissue may result.

Clinical Pharmacology: Prednisone is inactive until metabolized to prednisolone. Hepatic conversion is rapid and complete. Plasma half-life of prednisone/prednisolone is 3–4 hours, but the biologic effect lasts 18–36 hours. Rayos is a delayed release brand of prednisone whose pharmacokinetic profile is  delayed about 4 hours compared to immediate release prednisone. It is more  expensive than immediate release prednisone. Dexamethasone has almost no mineralocorticoid effect. It is more potent than prednisone/prednisolone but more difficult to titrate clinically. Depot injection preparations, either intraarticularly or intramuscularly, provide low plasma concentrations of steroid for 2–4 weeks.

Cost: $ (generic)

BIBLIOGRAPHY

Weinstein RS. Clinical practice. Glucocorticoid-induced bone disease. N Engl J Med 2011;365:62-70. PMID:21732837

Lavelle W, Lavelle ED, Lavelle L. Intra-articular injections. Med Clin North Am. 2007;91:241-50. PMID:17321284