Anti-Inflammatory Steroids Flashcards
Stimulates adrenal cortex to secrete glucocorticoids, mineralocorticoids, and weak androgens.
Corticotropin (ACTH)
What is the prototype for glucocorticoids?
Cortisol
What is the prototype for mineralocorticoids?
Aldosterone
Prednisone/Prednisolone
Steroid
Inhibits phospholipase A2, resulting in less prostaglandins, leukotrienes
Anti-inflammatory
Name 2 fluorinated steroids.
Dexamethasone and triamcinolone
Where are glucocorticoid receptors found? What do they bind?
Intracellularly - translocate to cell nucleus and dimerize after steroid binding. Bind to HREs.
What are HRE’s?
Hormone responsive elements. DNA targets involved in regulation of specific gene promoters
Glucocorticoids induce synthesis of _____ which suppress activation of _____. As a result, release of ______ and production of pro-inflammatory eicosanoids are decreased.
Lipocortins
Phospholipase A2
Arachidonic acid
Glucocorticoids suppress _______ induction in inflammatory cells that are usually induced by pro-inflam stimuli like _____.
PGHS-2 (prostaglandin H synthase-2)
PGE2
Reduction of cytoprotective prostaglandin levels will lead to ______ and _____.
GI ulcerations and bleeds.
Prostaglandin that modulates gastric mucosal acid secretion, mucus levels, and blood flow.
PGE2
Prostaglandin with vasodilator actions that has cytoprotective properties.
PGI2
Prostaglandins that cause erythema.
PGD2, PGE1
PGE2, PGI2
Prostaglandins that cause systemic fever, local heat, and pain.
PGE2, PGI2
Prostaglandin that causes edema.
PGE2
Betamethasone
Most potent steroid
Anti-inflammatory
Hydrocortisone
Glucocorticoid
Increases plasma glucose/lipids/Na+
Anti-inflammatory
What are the 4 determinants of increased glucocorticoid duration of action?
- Protein binding – larger bound fraction correlates with extended duration
- 11β-HSD II binding affinity – lower affinity correlates with extended duration
- Lipophilicity – greater promotes adipose storage and extends duration
- Glucocorticoid Receptor Affinity – stronger binding extends duration of action
What is a disease of primary adrenal insufficiency? How do you treat it?
Addison’s Disease - hydrocortisone supplemented with a mineralocorticoid (fluorocortisone)
What is the correct treatment for secondary adrenal insufficiency?
Hydrocortisone alone (RAAAs provides enough mineralocorticoid)
Lympholytic effects of steroids have proven efficacious in treatment of _______ and _____.
Lymphocytic leukemia and multiple myeloma
T or F. Corticosteroids are curative drugs.
False! They suppress symptoms, but do not cure.
What syndrome involves adrenocorticotropin (ACTH) excess caused by pituitary or ectopic ACTH overproduction, adrenal tumors, or exogenous glucocorticoid administration?
Cushing’s syndrome
What are the symptoms of Cushing’s syndrome?
- Muscle weakness - due to decreased muscle mass
- Central fat deposition
- Moon face
- Purple abdominal striae
- Glucose intolerance
- Neuropsychiatric disorders
What are the effects of glucocorticoid therapy on gastric mucosa?
Peptic ulcers
What are possible skeletal effects of glucocorticoid therapy?
Osteoperosis and osteonecrosis
Name potential effects of glucocorticoid therapy on the following:
- Ophthalmic effects
- Fluid and electrolyte disturbances (fluorcortesol)
- Iatrogenic adrenal insufficiency
- Blood glucose levels
- Cataracts
- Na+ and water retention
- Suppression of hypothalamic and pituitary activity, leading to adrenal atrophy
- Hyperglycemia –> Diabetes
What are strategies for mgmt of adverse effects of glucocorticoid therapy?
- Intermittent dosing strategies
- Topical or inhaled administration
- Use lowest dose possible
What are potential issues after withdrawal from therapy?
- Flare-up of disease (most frequent)
- Acute adrenal insufficiency (most severe)
**sone
Inactive ketone form of steroid
***solone
Active hydroxyl form of steroid
Topical/inhaled steroids for rapid use
