Steroids Flashcards
MOA of Glucocorticoids
3 things
- Effects mediated by glucocorticoid recepters
- Hormone enters cell and binds receptor -> transported to nucleus -> affects RNA transcription and protein synthesis
- Feedback suppression for ACTH
ADME of Glucocorticoids
- A/D: 75% bound to corticosteroid-binding protein (CBG), 5% bound to albumin, 20% free
- M: half-life 60-90 minutes
Dosage of Glucocorticoids
4 things
- Regimen based on seriousness of disease, amount required for desired effect, duration of therapy
- Lowest possible dose
- Do NOT stop abruptly
- Alternate day dosing: increase in efficacy and decrease in ADRs (useful when large doses are required for prolonged periods)
ADRs of Glucocorticoids
- Metabolic (5)
- Catabolic (2)
- Anti-inflammatory (4)
- CNS (5)
- Dermatologic (5)
- GI (3)
- Renal (3)
- Other (3)
- Metabolic: increase activities for gluconeogenesis, increaed serum glucose, lipolysis, and insulin*, muscle catabolism increases AA availability,
- Catabolic: decreased muscle mass and weakness, osteoporosis
- Anti-inflammatory: decreases prostaglandins, inhibits leukocytes and tissue macrophages, causes vasoconstriction
- CNS: can decrease seizure threshold, NO increase in intracranial pressure, anxiety, insomnia, steroid psychosis
- Derm: SQ fat redistribution (moon face), skin thinning, acne, impaired wound healing, fungal infections
- GI: increased acid and pepsin, increased fat absorption, decreased calcium absorption (through vit. D)
- Renal: decreased GFR, excess water retention, adrenal suppression (when used more than 2-3 days)
- Other: suppresion of ACTH, TSH, and FSH, increased platelets and RBCs, surfactant production in unborn babies
Endogenous Glucocorticoids
Cortisol (made from cholesterol and released under influence of ACTH)
Short/Medium acting glucocorticoids (3)
- Hydrocortisone
- Prednisone
- Prednisolone (methylprednisolone)
Intermediate/Long acting glucocorticoids (3)
- Triamcinolone
- Betamethasone
- Dexamethasone
Intra-articular injections (glucocorticoids)
5 things
- Treat joint disease (esp. RA)
- Fast impact on pain and stiffness
- Painful, may cause flushing, deterioration, HTN
- Do NOT repeat more than every 3 months (leads to necrosis)
- Drugs used: betamethasone, dexamethasone, methylprednisolone, triamcinolone
Epidural injections (glucocorticoids) 3 things
- Treat leg or back pain
- Not first line treatment
- Drugs used: hydrocortisone, methylprednisolone, triamcinolone)
Dose packs (glucocorticoids) 2 things
- High dose initially, then tapers off
- Drugs used: methylprednisolone, dexamethasone, betamethasone, triamcinolone
Topical (glucocorticoids)
3 things
- Very affective for skin disease
- Absorption increased by increased skin temperature and hydration
- Ointment better than creams
Opthalmic (glucocorticoids)
3 things
- For eye disease
- Systemic absorption is rare
- Not for glaucoma or cataracts
Enemas (glucocorticoids)
2 things
- For ulcerative colitis
- Drugs used: hydrocortisone
Aerosols (glucocorticoids)
2 things
- For asthma and allergic rhinitis
- Local effect only, first pass effect decreases systemic absorption
Stimulation of Lung Maturation in the Fetus
If premature newborn is under 34 weeks, betamethasone can be given to stimulate surfactant production in the lungs.