KG -Pharm 2 Exam 3, Corticosteroids Flashcards

1
Q

corticosteroids include ___ & ___

A

mineralcorticosteroids (Aldo) & glucocorticosteroids (cortisol)

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2
Q

Aldo is regulated by ___

A
  • reg by AT II & K+ (NOT ACTH)

- increases sodium and water retention, increases potassium secretioni

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3
Q

Cortisol is regulated by ___

A
  • reg by release of ACTH
  • STRESS HORMONE
  • nuclear receptor
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4
Q

glucocorticoids - effects on carbs/protein/fat

A
  • increases levels of GLUCOSE, FFAs, AAs
  • ANTAGONIZES INSULIN (bc insulin would get rid of glucose)
  • redistribute body fat to central body
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5
Q

glucocorticoids - CV effects

A
  • INCREASE VASCULAR RESPONSE TO SYMPATHETIC STIM (increase epi/norepi/dopamine)
  • some Na+/H2O RETENTION (less than mineralcorticoid)
  • increase CO
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6
Q

glucocorticoid - endocrine effects

A
  • DECREASE Ca2+ DEPOSITION INTO BONE (inhibits actions of vitamin D)
  • INCREASE Ca2+ LOSS FROM BONE (increase PTH)
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7
Q

glucocorticoid - immune system effects

A
  • IMMUNOSUPPRESSIVE (decr WBCs, leukocyte function)
  • BLOCKS ALL STEPS IN INFLAMMATION (heat, erythema, swelling, tenderness)
  • SUPPRESSION WOUND HEALING (edema, fibrin, collagen synthesis)
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8
Q

glucocorticoid - CNS effects

A
  • MOOD ELEVATION
  • INSOMNIA, RESTLESSNESS
  • ANXIETY
  • DEPRESSION
  • PSYCHOSIS
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9
Q

glucocorticoid - GI effects

A

peptic ulcer development

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10
Q

how to get glucocorticoid excess?

A
  • cushing’s dz/syndrome
  • ACTH excess - tumor
  • cortisol exccess - tumor or exogenous glucocorticoids
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11
Q

how to get adrenocortical insufficiency?

A
  • addison’s dz
  • adrenal malfunction
  • pituitary malfunction
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12
Q

symptoms of addison’s dz

A
  • weakness, anorexia, weight loss
  • hyperpigmentation
  • hypotension
  • GI problems
  • hypoglycemia, salt craving
  • poor response to stress
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13
Q

addisonian crisis?

A

ACUTE ADRENAL INSUFFICIENCY

  • circulatory collapse, dehydration, vomiting, hyperK+
  • fatal
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14
Q

why use glucocorticoids?

A

replacement and anti-inflammation

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15
Q

hydrocortisone?

A

CORTISOL

  • replacement therapy for adrenal insufficiency
  • mineralcorticoid + glucocorticoid properties
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16
Q

fludrocortisone?

A
  • combined w/ glucocorticoid for replacement when needed

- mineralcorticoid

17
Q

cortisone?

how is it different from hydrocortisone?

A
  • MUST FIRST BE CONVERTED TO HYDROCORTISONE IN THE LIVER IN ORDER TO BE ACTIVE
18
Q

prednisone & prednisolone?

A
  • gluco > mineral
  • PREDNISONE MUST BE CONVERTED TO PRENISOLONE IN LIVER IN ORDER TO BE ACTIVE
  • prednisone = most commonly prescribed oral glucocorticoid
19
Q

triamcinolone & methylprednisolone?

A
  • no mineral activity
  • high gluco activity
  • MOST NEW GLUCOCORTICOID DRUGS ARE LIFE THESE
  • diff duration/potency
20
Q

prep for long term therapy?

A

oral

21
Q

prep for emergency or depot admin?

A

injection

22
Q

prep for asthma/rhinitis?

A

inhalation/intranasal

23
Q

differences in topical preps?

A
  • fairly insoluble (prevent absorption)
  • more potent for thick skin
  • skin damage/thin skin = incr absorption
  • repeated app for depot effect
24
Q

adrenocorticosteroids - therapeutic uses?

A
  • 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
25
Q

corticosteroids - therapeutic guidelines?

A
  • use only as long as necessary
  • LOWEST EFFECTIVE DOSE (then taper down)
  • LOCALLY when possible (topical, injection to joint, inhaled)
  • give on ALTERNATE DAYS
26
Q

what is best way to give corticosteroids so as not to cause serious problems?

A
  • SHORT TERM THERAPY (1-2) WKS
    (chronic can leave HPA screwed up for months)
  • MANY ADVERSE EFFECTS W/ LONG TERM, HIGH DOSES
27
Q

corticosteroids - adverse effects?

A
  • 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
28
Q

corticosteroids & osteoporosis?

A
  • MOST DAMAGING & LIMITING EFFECT
  • 30-50% get fracture (vertebral/rib)
  • treat w/ vit D, Ca2+, bisphosphonates
29
Q

corticosteroids & iatrogenic adrenal insufficiency?

A
  • > 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
30
Q

corticosteroids & cushing-oid effects?

A
  • ACNE, striae
  • TRUNCAL OBESITY
  • BUFFALO HUMP
  • MOON FACE
  • dysmenorrhea
  • skin atrophy/thinning
31
Q

corticosteroids - contraindications?

A

NONE FOR ADRENAL INSUFFICIENCY!!!!! (necessary for life!)

  • INFECTION
  • poorly controlled DIABETES
  • OSTEOPOROSIS
  • HEART DZ/HTN w/ CHF
  • IMMUNOSUPPRESSED pt
  • CHILDHOOD
  • pregnancy
32
Q

corticosteroids - what to monitor?

A
  • hyperglycemia/glycosuria
  • Na+ retention (if edematous)
  • hypoK+
  • peptic ulcer
  • osteoporosis
  • infections
  • children = growth/development
  • pregnancy = teratogenic
33
Q

aminoglutethimide?

A
  • BLOCKS ADRENAL & GONADAL steroid synthesis
  • must give corticosteroids to suppress ACTH
  • not on market anymore
34
Q

ketoconazole?

A
  • antifungal that inhibits steroid synthesis (in high doses)
  • NON SELECTIVE
  • preoperative suppression
35
Q

mifepristone (RU486)?

A
  • ANTAGONIST of GLUCOCORTICOID & PROGESTERONE RECEPTORS

- for inoperable cushing’s pts

36
Q

spironolactone?

A
  • MINERALCORTICOID receptor ANTAGONIST
  • K+ sparing diuretic
  • for HYPERALDOSTERONISM & HIRSUTISM