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605 Pharmacology > Glucocorticoids > Flashcards

Glucocorticoids Flashcards

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1
Q

Hypothalamic Pituitary Adrenal Axis (HPAA)

A

hypothalamus secretes corticotropin releasing hormone (CRH) which stimulates the anterior pituitary to produce adrenocorticotropic hormone (ACTH) which tells the adrenal cortex to release cortisol

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2
Q

Cortisol Effect on Hypothalamus and Anterior Pituitary

A

negative feedback loop to decrease release of CRH and ACTH

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3
Q

ACTH effect on Hypothalamus

A

negative feedback loop to decrease release of CRH

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4
Q

3 General Effects of Cortisol

A
  1. Physiologic
  2. Pharmacologic
  3. Adverse
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5
Q

When we use glucocorticoids, what effects of cortisol are we targeting?

A

pharmacologic

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6
Q

4 Systems Affected by Glucocorticoids

A
  1. Renal (Kidney)
  2. Cardiovascular
  3. Immune
  4. Metabolic
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7
Q

Renal Effects of Glucocorticoids

A

increase blood pressure (d/t sodium retention and volume expansion); inhibit ADH release so urine becomes less concentrated

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8
Q

Cardiovascular Effects of Glucocorticoids

A

increase blood pressure (d/t increase vasoconstriction), decreases vascular permeability

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9
Q

Immune Effects of Glucocorticoids

A

inhibits phospholipase A2 (PLA2) therefore decreasing prostaglandins, decreases cell-mediated immunity

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10
Q

Excess Glucocorticoid Effect on Immune System?

A

anti-inflammatory and immunosuppression

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11
Q

Metabolic Effects of Glucocorticoids

A

increases gluconeogenesis, glycogenolysis, and lipolysis (diabetes risk)

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12
Q

2 Major Endogenous Glucocorticoids

A
  1. Cortisol (majority of species)
  2. Corticosterone (a few species)
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13
Q

Are we typically administering endogenous or synthetic steroids?

A

synthetic!

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14
Q

3 Ways to Classify Pharmacologic Steroids

A
  1. Glucocorticoid Potency
  2. Mineralocorticoid Potency
  3. Duration of Action
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15
Q

Relationship between Prednisone and PredniSOlone?

A

prednisone is a prodrug of predniSOlone

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16
Q

We talk about glucocorticoid potency in relation to what drug?

A

Prednisone

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17
Q

Short-Acting (<12 hours) Glucocorticoids (2)

A
  1. Cortisone
  2. Hydrocortisone
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18
Q

Intermediate-Acting (12-36 hours) Glucocorticoids (4)

A
  1. Prednisone
  2. PredniSOlone
  3. Methylprednisone
  4. Triamcinolone
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19
Q

Long-Acting (>48 hours) Glucocorticoids (3)

A
  1. Flumethasone
  2. Dexamethasone
  3. Betamethasone
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20
Q

Which intermediate-acting glucocorticoid is not mineralocorticoid potent?

A

triamcinolone

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21
Q

Which glucocorticoids are most mineralocorticoid potent - short or long acting?

A

SHORT (long acting have no mineralocorticoid potency)

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22
Q

Glucocorticoid Esters

A

chemical groups that can be added to steroid base to alter onset and/or duration

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23
Q

Ester Effect on Onset

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A

increases water solubility to hasten absorption, therefore a faster onset

24
Q

Ester Effect on Duration

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A

decrease solubility to allow depot formation, then bond must be hydrolyzed to be absorbed, resulting in longer duration

25
4 Pharmacologic Indications for Use of Glucocorticoids
1. Physiologic Replacement 2. Anti-inflammatory 3. Anti-neoplastic 4. Immunosuppressive
26
Dosing Range Effect on Function
we use DIFFERENT dosing ranges to have different effects, and they can be highly dependent on the individual patient
27
Physiologic Replacement Dosing Range
0.1 - 0.25mg/kg/day [prednisone equivalent]
28
Anti-Inflammatory Dosing Range
0.5 - 1 mg/kg/day [prednisone equivalent]
29
Anti-Neoplastic Dosing Range
1 - 2 mg/kg/day [prednisone equivalent]
30
Immunosuppressive Dosing Range
2 [- 4] mg/kg/day [prednisone equivalent]
31
Does continuing to increase does become more immunosuppressive?
no, it has a limit, and generally closer to the lower end of the range
32
Indications for Physiologic Replacement
Hypoadrenocorticism (Addisons) or other insufficiency; to prevent hypotension, shock, hypoglycemia, bradycardia (so essentially death, don't die k)
33
Anti-Inflammatory Indications
pruritic ear/skin diseases mainly; prevents PLA2 formation, also prevents histamine release
34
Can you use steroids as an anti-inflammatory medication all willy-nilly?
no, please rule out primary infectious cause first as steroids can sometimes make these worse
35
Anti-Neoplastic Indications
lround cell tumors (such as lymphoma or MCTs); causes apoptosis of [some] lymphocytes (lympholytic effect)
36
Why do we use steroids with neoplasms?
more for quality of life rather than survival, best used in combination with chemotherapy
37
Immunosuppressive Indications
for various anemias, cytopenias, opathys, meningitis, whatever; acts by many mechanisms of action, including inhibiting macrophages, poor cell adhesion, T cell apoptosis, etc
38
Which indications require tapering?
mainly in immunosuppressive (but depending on practice will taper in other uses as well)
39
Most Common Adverse Effects (in dogs)
PU/PD, polyphagia (excessive hunger), weight gain, muscle loss, hair loss
40
Cardiovascular and Renal Adverse Effects
PU/PD, hypertension, proteinuria
41
Musculoskeletal Adverse Effects
pot-belly, muscle wasting, ligament/tendon weakness, osteoporosis; also laminitis in horses
42
CNS Adverse Effects
polyphagia, panting, aggression or other behavior change; also masks disease progression
43
Metabolic Adverse Effects
weight gain, diabetes mellitus, iatrogenic Addison's d/t quick withdrawal
44
just a cool table to look at
look at it
45
Cutaneous Adverse Effects
hair loss, thin skin, poor wound healing
46
Skin Fragility Syndrome
in cats, skin tearing, yikes
47
Gastrointestinal Adverse Effects
gastritis and ulceration WHEN USED IN COMBINATION with other drugs like NSAIDs (generally not a problem on their own)
48
Calcinosis Cutis
calcium deposition in the skin, very very itchy
49
What glucocorticoid is ineffective in cats?
PREDNISONE (surprise, they don't have the necessary enzyme to break it down into prednisolone)
50
Dosing Steroids in Cats
round UP - generally require more as they are more "resistant" than other species
51
If cats get diabetes mellitus from steroid administration, is it reversible?
sometimes
52
Iatrogenic Addison's
d/t rapid withdrawal of steroids; signs include dullness/depression/fatigue, GI signs, and unthrifty appearance
53
Local Glucocorticoids
topical, OTIC, or eye preparations; can still have systemic effects d/t lipophilia (easily absorbed)
54
Soft Glucocorticoids
have a very high first pass effect and are rapidly absorbed by the liver, so they have very minimal systemic effects
55
Examples of Soft Steroids
budesonide PO (chronic enteropathy), fluticasone (asthma)

605 Pharmacology (11 decks)

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