KG -Pharm 2 Exam 3, Corticosteroids Flashcards
corticosteroids include ___ & ___
mineralcorticosteroids (Aldo) & glucocorticosteroids (cortisol)
Aldo is regulated by ___
- reg by AT II & K+ (NOT ACTH)
- increases sodium and water retention, increases potassium secretioni
Cortisol is regulated by ___
- reg by release of ACTH
- STRESS HORMONE
- nuclear receptor
glucocorticoids - effects on carbs/protein/fat
- increases levels of GLUCOSE, FFAs, AAs
- ANTAGONIZES INSULIN (bc insulin would get rid of glucose)
- redistribute body fat to central body
glucocorticoids - CV effects
- INCREASE VASCULAR RESPONSE TO SYMPATHETIC STIM (increase epi/norepi/dopamine)
- some Na+/H2O RETENTION (less than mineralcorticoid)
- increase CO
glucocorticoid - endocrine effects
- DECREASE Ca2+ DEPOSITION INTO BONE (inhibits actions of vitamin D)
- INCREASE Ca2+ LOSS FROM BONE (increase PTH)
glucocorticoid - immune system effects
- IMMUNOSUPPRESSIVE (decr WBCs, leukocyte function)
- BLOCKS ALL STEPS IN INFLAMMATION (heat, erythema, swelling, tenderness)
- SUPPRESSION WOUND HEALING (edema, fibrin, collagen synthesis)
glucocorticoid - CNS effects
- MOOD ELEVATION
- INSOMNIA, RESTLESSNESS
- ANXIETY
- DEPRESSION
- PSYCHOSIS
glucocorticoid - GI effects
peptic ulcer development
how to get glucocorticoid excess?
- cushing’s dz/syndrome
- ACTH excess - tumor
- cortisol exccess - tumor or exogenous glucocorticoids
how to get adrenocortical insufficiency?
- addison’s dz
- adrenal malfunction
- pituitary malfunction
symptoms of addison’s dz
- weakness, anorexia, weight loss
- hyperpigmentation
- hypotension
- GI problems
- hypoglycemia, salt craving
- poor response to stress
addisonian crisis?
ACUTE ADRENAL INSUFFICIENCY
- circulatory collapse, dehydration, vomiting, hyperK+
- fatal
why use glucocorticoids?
replacement and anti-inflammation
hydrocortisone?
CORTISOL
- replacement therapy for adrenal insufficiency
- mineralcorticoid + glucocorticoid properties
fludrocortisone?
- combined w/ glucocorticoid for replacement when needed
- mineralcorticoid
cortisone?
how is it different from hydrocortisone?
- MUST FIRST BE CONVERTED TO HYDROCORTISONE IN THE LIVER IN ORDER TO BE ACTIVE
prednisone & prednisolone?
- gluco > mineral
- PREDNISONE MUST BE CONVERTED TO PRENISOLONE IN LIVER IN ORDER TO BE ACTIVE
- prednisone = most commonly prescribed oral glucocorticoid
triamcinolone & methylprednisolone?
- no mineral activity
- high gluco activity
- MOST NEW GLUCOCORTICOID DRUGS ARE LIFE THESE
- diff duration/potency
prep for long term therapy?
oral
prep for emergency or depot admin?
injection
prep for asthma/rhinitis?
inhalation/intranasal
differences in topical preps?
- fairly insoluble (prevent absorption)
- more potent for thick skin
- skin damage/thin skin = incr absorption
- repeated app for depot effect
adrenocorticosteroids - therapeutic uses?
- REPLACEMENT in chronic adrenal deficiency
- -> w/ GLUCOCORTICOID ALONE or GLUCO + MINERAL
- increase w/ stress/infection
- ACUTE INSUFFICIENCY = FATAL
also:
- RA (not curative)
- ASTHMA (inhaled = first step tx, with b2 agonist, oral for uncontrolled w/ inhaled)
- INTRANASAL for rhinitis
- sle, allergies, shock, organ transplants, etc
corticosteroids - therapeutic guidelines?
- use only as long as necessary
- LOWEST EFFECTIVE DOSE (then taper down)
- LOCALLY when possible (topical, injection to joint, inhaled)
- give on ALTERNATE DAYS
what is best way to give corticosteroids so as not to cause serious problems?
- SHORT TERM THERAPY (1-2) WKS
(chronic can leave HPA screwed up for months) - MANY ADVERSE EFFECTS W/ LONG TERM, HIGH DOSES
corticosteroids - adverse effects?
- more SUSCEPTIBLE TO INFECTION
- HYPERGLYCEMIA (may unmask diabetes)
- CNS = RESTLESSNESS, INSOMNIA, PSYCHOSES, INCR APPETITE (even with ACUTE TX)
- OSTEOPOROSIS
- IATROGENIC ADRENAL INSUFFICIENCY
- CUSHING-OID EFFECTS
corticosteroids & osteoporosis?
- MOST DAMAGING & LIMITING EFFECT
- 30-50% get fracture (vertebral/rib)
- treat w/ vit D, Ca2+, bisphosphonates
corticosteroids & iatrogenic adrenal insufficiency?
- > 1-2 WKS HIGH DOSE THERAPY –> HPA DEPRESSION
- ABRUPT drug cessation can cause ACUTE ADRENAL INSUFFICIENCY
- need GRADUAL WITHDRAWAL
- STRESS can cause adrenal crisis in chronic its
- do alternate days/morning dosing
corticosteroids & cushing-oid effects?
- ACNE, striae
- TRUNCAL OBESITY
- BUFFALO HUMP
- MOON FACE
- dysmenorrhea
- skin atrophy/thinning
corticosteroids - contraindications?
NONE FOR ADRENAL INSUFFICIENCY!!!!! (necessary for life!)
- INFECTION
- poorly controlled DIABETES
- OSTEOPOROSIS
- HEART DZ/HTN w/ CHF
- IMMUNOSUPPRESSED pt
- CHILDHOOD
- pregnancy
corticosteroids - what to monitor?
- hyperglycemia/glycosuria
- Na+ retention (if edematous)
- hypoK+
- peptic ulcer
- osteoporosis
- infections
- children = growth/development
- pregnancy = teratogenic
aminoglutethimide?
- BLOCKS ADRENAL & GONADAL steroid synthesis
- must give corticosteroids to suppress ACTH
- not on market anymore
ketoconazole?
- antifungal that inhibits steroid synthesis (in high doses)
- NON SELECTIVE
- preoperative suppression
mifepristone (RU486)?
- ANTAGONIST of GLUCOCORTICOID & PROGESTERONE RECEPTORS
- for inoperable cushing’s pts
spironolactone?
- MINERALCORTICOID receptor ANTAGONIST
- K+ sparing diuretic
- for HYPERALDOSTERONISM & HIRSUTISM
