Corticosteroids Flashcards
What do glucocorticoids do?
Stress hormones
Increase circulating glucose
Anti-inflammatory effects
What do mineral corticoids do?
Na+ retension
Increase blood volume
Increase blood pressure
Aldosterone is an example of a _______ while cortisol is an example of a___________
Mineralcorticoid
Glucocorticoid
________ stimulates the production of aldosterone from in the adrenal glands
Angiotensin II
Steroid hormones are synthesized from________ via_______
Cholesterol
CYP11AI
Corticoid-binding globulin (transcortin) binds_______
Glucocorticoids and Progesterone
Sex hormone binding globulin(SHBG) binds_______
Testosterone and estradiol
_______Is excreted on bile.
Estrogen
Progesterone, androgen and glucocorticoids are excreted via______
Urine
Glucocorticoids bind__________
Glucocorticoid Responsive Elements (GRE) and regulate transcription of genes.
____________Catalyzes the rate-limiting step in gluconeogenesis
Phosphoenolpyruvate carboxykinase (PEPCK)
Lipocortin suppresses ________
Phospholipase A2
How do glucocorticoids perform immunosuppression?
They bind thier receptors which together bing NFkB preventing NFkB from transcribing inflammatory aagents.
What is addison’s disease?
Hypoadrenalism caused by decreased secretion of hormones by the adrenal cortex
What can cause Addison’s disease?
Destruction of adrenal cortex by TB
Decreased secretion of ACTH by the anterior pituitary.
What are the symptoms of Addison’s disease?
Extreme weakness.
Low blood pressure
Hyperpigmentation
Mental depression
What is cushing’s disease?
Hyperadrenalism (Increased ACTH production by the adrenal cortex)
What are the symptoms of Cushing’s disease?
Increased protein catabolism
Osteoporosis
Opportunistic infections
Longterm use of systemic glucocorticoids can lead to Cushing’s symptoms
Ketokonazole is an antigungal that inhibits P450scc, __________ and __________
17a-hydroxylase
11B-hydroxylase
Ketokonazole can be used to treat_________
Hyperglucocorticoid state (Cushing’s syndrome)
Cortisol (hydrocotisone) is _______ while cortisone is_____
Active
Inactive
Name two short acting Corticosteroids (8-12hrs)
Hydrocortisone
Cortisone
Name 4 intermediate acting systemic corticosteroids (12-36hrs)
Prednisone
Prednisolone
Methylprednisolone
Triamcinolone
Name two long acting systemic corticosteroids
Dexamethasone
Betamethasone
Which corticosteroid has the most mineralocorticoid activity?
Fludrocortisone (Leads to Na+ retention and edema)
has a 9a-F
21 ester acetates on glucocorticoid________lipophilicity
Increase
Succinate replacement at the 21 position causes _______
Slow hydrolysis
Phosphate substitution at the 21 position of glucocorticoids causes___________
Increased solubility and rapid hydrolysis
Name tro topical glucocorticoids
Triamcinolone acetonide (High potency) Betamethasone Valerate (medium potency)
Substitution of the 21-hydroxyl group for a Chlorine greatly enhances topical____________
Anti-inflammatory activity.
Name 3 anti-inflammatory topical corticosteroids
Clobetasol propionate (very high potency) Halobetasol proprionate (Very high potency) Halcinonide (High potency)
Name two topical corticostetroids
Fluticasone propionate
Mometasone furoate
Fluticasone propionate and mometasone furoate have ad _________lipophilicity and _________binding affinity but________solubility
High
Highest
Poor
Name 6 inhaled glucocorticoids
Triamcinolone acetonide Beclomethasone dipropionate Flunisolide Budesonide Mometasone Furoate Fluticasone Propionate
Name a few adverse effects of corticoids
Sodium and H2O retention Hypertension Steroid myopathy Reduced long bone growth Osteoporosis Cushing's-like effects Hyperglycemia Immuosupression Peptic ulcer CNS (depression, euphoria, depression) Cataracts Addisonian Crisis (negative feed back on hypthalamus)
