Oral ImmunosuppressantsOral Glucocorticoids- Anti-inflammatory, antimitotic, immunosuppressive, and vasoconstrictive properties; forms complex with intracellular receptors and modulates transcription of certain genes
- Effects
- ↓ Circulating lymphocytes/eosinophils/monocytes, ↓ macrophage response to lymphokines, ↓ Ab production, ↓ synthesis of proinflammatory molecules, ↓ fibroblast production of collagen
- ↑ Neutrophils, ↑ blood glucose (stimulates gluconeogenesis), ↑ protein catabolism, ↑ plasma fatty acids/ketone body formation, ↑ acid/pepsin secretion in stomach
- Side effects
- Cutaneous: atrophy, telangiectasias, striae, poor wound healing
- Other: ↑ appetite, peptic ulcers, pancreatitis, osteoporosis, Cushing’s syndrome, hyperglycemia, hypertriglyceridemia, sodium retention, cataracts, glaucoma, ↑ risk of infection, hypertension, hirsutism, HPA axis suppression, failure to thrive, aseptic necrosis of femoral head, muscle weakness, psychosis, pseudotumor cerebri
- Short-acting glucocorticoids → cortisone and hydrocortisone
- Greatest mineralocorticoid activity; lowest glucocorticoid activity
- Intermediate and long-acting glucocorticoids → methylprednisolone, triamcinolone, dexamethasone, betamethasone
- Virtually no mineralocorticoid activity; dexamethasone/betamethasone with highest glucocorticoid activity
- Dosing
- Single morning dose ↓ risk of HPA suppression
- Divided daily dosing may ↑ anti-inflammatory efficacy but also ↑ systemic toxicity
- Alternate day dosing reduces all complications except osteoporosis and cataracts
|
