From the Guidelines
Intermediate and long-acting synthetic corticosteroids are medications such as prednisone, methylprednisolone, triamcinolone, dexamethasone, betamethasone, and fluticasone, which provide anti-inflammatory and immunosuppressive effects over extended periods. These medications are designed to have a prolonged duration of action, with intermediate-acting options like prednisone and prednisolone lasting 12-36 hours 1, and long-acting options like dexamethasone and betamethasone lasting 36-72 hours. The duration of action is related to their half-life in the body, which determines how frequently they need to be dosed.
Key Characteristics of Intermediate and Long-Acting Synthetic Corticosteroids
- They work by binding to glucocorticoid receptors, which suppresses inflammatory pathways and immune responses.
- The dosing of these medications varies widely based on the condition being treated, with higher doses typically used for acute conditions and lower doses for chronic management.
- Common side effects include weight gain, mood changes, increased blood sugar, bone loss, and adrenal suppression, particularly with prolonged use.
- These medications should be tapered rather than stopped abruptly to prevent adrenal crisis, especially after extended treatment periods.
Clinical Considerations
- The choice of corticosteroid and its duration of use should be based on the specific clinical scenario, taking into account the potential benefits and risks, including the risk of side effects and the impact on morbidity, mortality, and quality of life.
- As noted in the guidelines for asthma management 1, the use of corticosteroids, particularly inhaled corticosteroids, is a key component of long-term control of asthma symptoms, highlighting the importance of these medications in specific therapeutic contexts.
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 acetate, which affords sustained activity, it can be inferred that betamethasone acetate is an example of a long-acting synthetic corticosteroid. However, the text does not provide a clear definition or list of intermediate and long-acting synthetic corticosteroids. 2
From the Research
Intermediate-Acting Synthetic Corticosteroids
- Intermediate-acting synthetic corticosteroids include prednisone and methylprednisolone, which are four to five times more potent than 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 phytohemagglutinin (PHA) stimulated peripheral lymphocytes (PBL) and T-lymphocytes 5.
Long-Acting Synthetic Corticosteroids
- Long-acting synthetic corticosteroids, such as dexamethasone, have a potency that is about 25 times greater than short-acting products like hydrocortisone 3.
- Dexamethasone is a highly potent corticosteroid with strong anti-inflammatory activity, but it can also cause significant side effects, including Cushing-like changes, decreased glucose tolerance, and osteoporosis 6.
- The industrial synthesis of long-acting synthetic corticosteroids, such as dexamethasone and betamethasone, involves a combination of chemistry and biotechnology, with diosgenin as the starting material 7.