L35- Steroid Pharmacology (cortisol + general) Flashcards
list the hormonal steroids + main purpose
Glucocorticoids- effects intermediary metabolism and immune function
Mineralocorticoids- salt retaining activity
Steroids: androgenic, estrogenic
cortisone = ______ pharmacologically
hydrocortisone
_______ are the names for hydrocortisone receptors
(cortisol)
receptor in cytoplasm –> nucleus –> receptor hormone complex binds GRE(dna) = glucocorticoid response elements
list the catabolic effects of hydrocortisone
[1) protein –> AA release]
2) CT, muscle, lymphoid, peripheral fat and skin ==> wasting at high concentrations (thinning of skin)
long-term therapy limits:
3) osteoporosis
4) children- growth retardation
list the immunosuppressive effects of hydrocortisone
1) Leukocytes
- inc neutrophils: inc in blood, dec migration from BVs
- dec lymphocytes (T/B cells), monocytes, eosinophils, basophils: inc migration to lymphoid tissue
2) vasoconstriction via mast cell degranulation suppression: dec His release and capillary permeability
list the anti-inflammatory effects of hydrocortisone (glucocorticoids)
1) inhibits phospholipase A2 (via **annexin I activation) –> blocks arachidonic acid release (for PGs mainly + LTs, Txs)
- dec COX2 synthesis (via **NF-(kappa)B inhibition) –> dec PGs, Txs
- activates MAPK phosphatase I (inhibits MAPK proinflammation signals)
Hydrocortisone, ‘other’ effects:
- (1) CNS
- (2) other hormones
- (3) GI
- (4) blood
- (5) renal
- (6) fetus
1- behavioral changes: insomnia, euphoria –> depression
2- suppresses ACTH, GH, TSH, LH (chronic use)
3- peptic ulcers: gastric acid stimulation (+ H pylori immune response suppression)
4- inc platelets, RBCs
5- improves function (impaired with cortisol deficiency)
6- fetal lung development
Hydrocortisone:
- (short/long) duration of action
- (good/poor) skin diffusion
- (good/poor) mucous diffusion
- (strong/weak/no) salt retaining effects
1- short
2- poor
3- good
4- weak
corticosteroid agonists =
glucocorticoids
mineralocorticoids
list the glucocorticoids
prednisone hydrocortisone dexamethasone beclomethasone triamcinolone methylprednisolone
list the mineralocorticoids
aldosterone
fludrocortisone
list the metabolic effects of hydrocortisone
1) Inc Gluconeogenesis and Glycogen Storage
- glycogen for availability in SNS activation for brain stores
- inc serum glucose
- inc insulin release, but inhibits muscle cell uptake
2) protein catabolism –> release of AAs
3) lipolysis –> fat deposition and redistribution + free FA and glycerol release
**Net- maintains glucose levels and stores for brain