What are intermediate and long-acting synthetic corticosteroids?

From the Guidelines

Intermediate and long-acting synthetic corticosteroids are medications that include prednisone, prednisolone, methylprednisolone, dexamethasone, triamcinolone, and betamethasone, which provide sustained anti-inflammatory and immunosuppressive effects over extended periods. These medications are used to treat various conditions, including asthma, rheumatoid arthritis, inflammatory bowel disease, and autoimmune disorders.

• Intermediate-acting steroids like prednisone have a biological half-life of 12-36 hours, while long-acting options like dexamethasone can remain active for 36-72 hours 1.
• The dosing of these medications varies widely based on the condition being treated, with prednisone commonly prescribed at 5-60 mg daily, and dexamethasone at 0.5-10 mg daily 1.
• When using these medications, tapering is essential for courses longer than 1-2 weeks to prevent adrenal suppression, and patients should take them with food to minimize gastrointestinal irritation 1.
• Patients on these medications should be monitored for side effects including hyperglycemia, hypertension, mood changes, and increased infection risk 1.
• The treatment approach for conditions like idiopathic inflammatory myopathies involves initiating treatment with high-dose corticosteroids and a steroid-sparing agent, with prednisone typically started at a dosage of 0.5 to 1 mg/kg per day 1.
• The choice of steroid-sparing agent, such as methotrexate, azathioprine, or mycophenolate mofetil, depends on various factors, including the patient's response and potential adverse effects 1.

From the FDA Drug Label

CLINICAL PHARMACOLOGY Glucocorticoids, naturally occurring and synthetic, are adrenocortical steroids that are readily absorbed from the gastrointestinal tract. Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states Their synthetic analogs are primarily used for their anti-inflammatory effects in disorders of many organ systems. A derivative of prednisolone, betamethasone has a 16β-methyl group that enhances the anti-inflammatory action of the molecule and reduces the sodium- and water-retaining properties of the fluorine atom bound at carbon 9 Betamethasone sodium phosphate, a soluble ester, provides prompt activity, while betamethasone acetate is only slightly soluble and affords sustained activity. The intermediate and long-acting synthetic corticosteroids are not explicitly defined in the provided text, but based on the information about betamethasone, it can be inferred that:

• Betamethasone acetate is an example of a long-acting synthetic corticosteroid, as it affords sustained activity 2. However, the text does not provide a clear definition or examples of intermediate-acting synthetic corticosteroids.

From the Research

Intermediate-Acting Synthetic Corticosteroids

• Intermediate-acting synthetic corticosteroids, such as prednisone and methylprednisolone, are four to five times more potent than short-acting products like hydrocortisone 3.
• These corticosteroids have been used in the treatment of numerous medical conditions, including chronic inflammatory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and rheumatoid arthritis 4.
• The immunosuppressive potency of intermediate-acting synthetic corticosteroids, such as prednisolone and methylprednisolone, has been tested in vitro on lymphocyte cultures, showing high potency in suppressing lymphocyte proliferation 5.

Long-Acting Synthetic Corticosteroids

• Long-acting synthetic corticosteroids, such as dexamethasone, have a potency about 25 times greater than short-acting products like hydrocortisone 3.
• Dexamethasone is a highly potent anti-inflammatory and immunosuppressive drug, commonly used in the treatment of chronic inflammatory diseases and autoimmune disorders 4.
• The use of long-acting synthetic corticosteroids, such as dexamethasone, can be associated with significant side effects, including Cushing-like changes, decreased glucose tolerance, and osteoporosis 6.