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Basic Pharmacology > Glucocorticoids and Mineralocorticoids > Flashcards

Glucocorticoids and Mineralocorticoids Flashcards

1
Q

what are some of the sex steroids?

A

estrogens
progesterone
testosterone

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2
Q

what do anabolic steroids promote?

A

protein synthesis and hence muscle mass
marginal success in stimulating bone marrow in anemic animals

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3
Q

do synthesized anabolic steroids used in medicine have reproductive side effects?

A

yes- fewer than testosterone

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4
Q

what are corticosteroids?

A

name implies steroids derived from adrenal cortex
mineralocorticoids and glucocorticoids

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5
Q

what are the two main steroid groups derived from the cortex?

A

mineralocorticoids: aldosterone
glucocorticoids: cortisol

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6
Q

when is cortisol released?

A

response to stress and low blood glucocorticoid levels

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7
Q

what are the functions of cortisol?

A

increase blood sugar through gluconeogenesis
suppress immune system
aid in fat, carbohydrate, and protein metabolism
reduce bone formation

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8
Q

what does an excess of cortisol lead to?

A

Cushing’s disease

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9
Q

what does a deficiency of cortisol lead to?

A

Addison’s disease

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10
Q

where does aldosterone act?

A

acts on distal tubules and collecting ducts of the nephron to resorb sodium and excrete potassium

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11
Q

what is the net effect of aldosterone?

A

increased water retention and blood pressure

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12
Q

what are two drugs that are intended for use as mineralocorticoids?

A

fludrocortisone
desoxycorticosterone pivalate

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13
Q

what drugs have pure glucocorticoid effects?

A

dexamethasone
betamethasone
flumethasone

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14
Q

what drugs have incidental or additive mineralocorticoid effects?

A

prednisolone
predef 2X (isoflupredone)

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15
Q

how do you convert a predisone dose to dexamethasone dose?

A

divide your pred dose by 7

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16
Q

the potency factor of pred is _____ times cortisol and dex is _____ times

A

4
30

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17
Q

what is the biological half-life of predisolone?

A

12-36 hours (intermediate)

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18
Q

what is the biological half-life of dexamethasone?

A

26-54 hours (long)

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19
Q

what describes IV drugs?

A

water soluble
can be given IV
duration controlled by biological half-life

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20
Q

what describes IM drugs?

A

water insoluble
given IM
duration controlled by rate of absorption (usually lasts 2-4 weeks)

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21
Q

what are the expected side effects of glucocorticoids?

A

PU/PD/PP (polyphasia)
panting
alopecia/hair thinning
increased ALP and vacuolar hepatopathy

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22
Q

what are unusual (important) adverse effects of glucocorticoids?

A

inhibit wound healing
increased susceptibility to infection
diabetes
laminitis in horses
GI ulceration
may cause abortion

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23
Q

in which species do we expect ALP to increase with glucocorticoids?

A

dogs
not cats

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24
Q

what is budesonide?

A

glucocorticoid

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25
Q

what does budesonide do?

A

dissolves in duodenum to provide local anti-inflammatory activity
suppresses HPA axis

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26
Q

what is oral budesonide good for orally?

A

gastrointestinal and potentially hepatic disease

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27
Q

what is fluticasone?

A

inhaled glucocorticoid in dogs and cats

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28
Q

what is important to think about with dosing cats on glucocorticoids?

A

much more resistant to side effects
require 2x dose as dog for same anti-inflammatory effect
dose not absorb predisone well (use prednisolone)

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29
Q

what is important to think about with horses on glucocorticoids?

A

does not absorb predisone well (use prednisolone)
certain steroids are more prone to predispose to laminitis

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30
Q

what is important to think about with cattle on glucocorticoids?

A

prone to abortion/induction of parturition from certain steroids in last half of gestation and especially in last month of gestation

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31
Q

what is desoxycorticosterone pivalate?

A

pure mineralocorticoid

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32
Q

how do you dose desoxycorticosterone pivalate?

A

pivalate repository formulation allows dosing every 21-30 days

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33
Q

what is desoxycorticosterone pivalate used to treat?

A

hypoadrenocorticism

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34
Q

what is fludrocortisone acetate (Florinef) used for?

A

oral mineralocorticoid as alternative to DOCP
also glucocorticoid action: PU/PD
hypoadrenocorticism

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35
Q

what are the adverse effects of mineralocorticoids?

A

few
PU/PD
hypertension
hypokalemia
DOCP, rare: anemia, anaphylaxis, injection site reaction

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36
Q

what happens in Addison’s disease?

A

adrenals do not produce enough of their intended steroid products: glucocorticoids, mineralocorticoids
often both, sometimes isolated

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37
Q

what do we supplement with Addison’s disease?

A

mineralocorticoids
glucocorticoids

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38
Q

what does mineralocorticoid supplementation replace?

A

aldosterone

39
Q

what does glucocorticoid supplementation mimic?

A

cortisol

40
Q

what can be given during initial stabilization of Addison’s disease that does not react with the cortisol assay?

A

dexamethasone

41
Q

what drug is preferred for glucocorticoid supplementation?

A

prednisolone

42
Q

what is the dosing range for prednisolone for Addison’s?

A

0.1-0.4 mg/kg
taper to no signs PU/PD/PP

43
Q

how are mineralocorticoid dosages adjusted for an addisonian?

A

based on serum Na and K

44
Q

what are glucocorticoid dosage adjustments based on in an addisonian?

A

clinical signs

45
Q

do you ever need to change the glucocorticoid dose for an Addison’s disease animal after finding a good dose?

A

yes: more glucocorticoids during times of stress
2-3x maintenance dose

46
Q

how do glucocorticoids have an anti-inflammatory effect?

A

increase production of inhibitory protein lipocortin which inhibits phospholipase A2 within arachidonic acid cascade
reduces inflammatory gene transcription
reduces macrophage phagocytosis
inhibits complement

47
Q

how do you dose dogs for anti-inflammatory therapy using glucocorticoids?

A

begin at 1 mg/kg/day, taper down until signs controlled
0.5-1 mg/kg pred usually

48
Q

what dose of prednisolone do cats usually need to accomplish anti-inflammatory therapy?

A

1-2 mg/kg

49
Q

what is immunosuppressive dosing used for?

A

used to treat most immune-mediated diseases

50
Q

when treating for immunosuppression, how do you dose a dog and a cat?

A

begin 2 mg/kg/day pred and taper over weeks to months
cats 2-4 mg/kg prednisolone may be needed to accomplish same thing

51
Q

why must a steroid be reduced gradually after being used for longer than a couple of weeks?

A

to avoid iatrogenic hypoadrenocorticism crisis

52
Q

how are steroids used for antineoplastic effects?

A

prednisone/prednisolone can be sole palliative treatment for lymphoma (different if doing chemo)
effective against other round cell tumors like multiple myeloma and mast cell tumor
palliative for other neoplasias, though NSAIDs often recommended for carcinomas

53
Q

when should you not give a patient steroids?

A

fungal and viral infections
gastrointestinal ulceration
osteoporosis
late pregnancy
corneal ulcers
diabetes mellitus (relative)
procoagulant states (relative)

54
Q

why should we not use steroids for a patient with a fungal infection (systemic mycoses)?

A

diseases held in check by cell-mediated immunity: severely inhibited by steroids

55
Q

why should we not use steroids in patients with gastrointestinal ulceration?

A

may result in ulcer development or aggravate an existing ulcer

56
Q

is it okay to use NSAIDs and steroids together?

A

no
significant risk of ulceration/perforation if used together

57
Q

what animals are most prone to steroid-induced abortion?

A

cattle
mid-gestation on, especially last month

58
Q

why should you be hesitant to use steroids in a patient with diabetes mellitus?

A

glucocorticoids have an anti-insulin effect
regulation of diabetic difficult

59
Q

what is an aldosterone antagonist?

A

spironolactone

60
Q

what antagonizes cortisol synthesis?

A

trilostane (vetoryl): inhibits enzyme in cortisol synthesis pathway
mitotane (lysodren): adrenolytic; cytotoxic to adrenal zona fasciculata and reticularis

61
Q

what is a dopamine agonist?

A

pergolide mesylate

62
Q

dexamethasone is __________ as potent as prednisone

A

7 times

63
Q

true/false: steroids are used to enhance wound healing

A

false

64
Q

are mineralocorticoids or glucocorticoids used primarily for hypoadrenocorticism?

A

mineralocorticoids

65
Q

what does corticotropin releasing hormone lead to?

A

adrenocorticotropic hormone and then cortisol

66
Q

what is aldosterone involved in?

A

maintaining electrolyte and fluid balance

67
Q

what is the potency of predisolone?

A

glucocorticoid: 4
mineralocorticoid: 0.8

68
Q

what is the potency of dexamethasone?

A

glucocorticoid: 30
mineralocorticoid: 0

69
Q

what is the biological half-life of prednisolone?

A

12-36hr

70
Q

what is the biological half-life of dexamethasone?

A

36-54hr

71
Q

what are some base words to show drugs are IM repository?

A

acetate
pivalate

72
Q

what are some other adverse effects of glucocorticoids? other than pu/pd/pp, panting, alopecia, increased ALP

A

inhibit wound healing
increased susceptibility to infection
decreased response to vaccination
diabetes
laminitis in horses
GI ulceration
may cause abortion
muscular weakness
calcinosis cutis
hypertension
CHF
worsen proteinuria
pancreatitis?

73
Q

what are the positives of budesonide as an alternative glucocorticoid?

A

potentially fewer systemic side effects
still suppresses HPA axis

74
Q

fluticasone causes suppression of HPA axis in _________________________

A

dogs, but not cats

75
Q

what diseases should you consider fluticasone for?

A

feline asthma
canine chronic bronchitis

76
Q

why do we think some steroids cause laminitis in horses?

A

not sure, but may be due to sensitization of alpha receptors in hoof wall

77
Q

what drugs are less likely to cause abortion in cattle?

A

prednisolone
isoflupredone

78
Q

does potency play a role in choosing a steroid for anti-inflammatory or immunosuppressive purposes?

A

no

79
Q

what should you choose a steroid for anti-inflammatory or immunosuppressive purposes by?

A

whether or not want mineralocorticoid effects
duration of action desired
if tissue distribution is an issue
species differences

80
Q

what mineralocorticoids are used in addison’s disease?

A

DOCP
fludrocortisone

81
Q

why is prednisolone preferred for the glucocorticoid in addison’s?

A

has mineralocorticoid activity: can reduce dose of DOCP or fludrocortisone

82
Q

what drugs increase production of lipocortin (which inhibits phospholipase A2)?

A

glucocorticoids

83
Q

what is the duration of therapy for anti-inflammatory therapy (short)?

A

2-3 days: control pruritis
single dose dexamethasone
one week of prednisolone

84
Q

what are the positives of doing alternate day therapy with long-term anti-inflammatory therapy?

A

less immunosuppression
less pituitary-adrenal axis suppression
any nonrepository steroid can be used early one

85
Q

why do we try to avoid repository injections?

A

highs are too high, lows too low
less control
more adrenal suppression
repeating infections prone to cause iatrogenic hyperadrenocorticism in dogs

86
Q

what is the dose of prednisolone for horses?

A

50-100mg IM/IV per horse
PO similar to dogs

87
Q

what is the dose of dexamethasone for cows?

A

5-20 mg IM/IV per cow
0.02-0.04 mg/kg IM for many indications

88
Q

how many half-lives should you wait between NSAIDs and steroids?

A

5 half-lives
if cannot: consider misoprostal

89
Q

what can happen with a pregnant bitch placed on high doses of steroids?

A

fetal death
reabsorption in first half of gestation or abortion thereafter

90
Q

why should you avoid steroids in animals predisposed to thromboembolism?

A

animals with hyperadrenocorticism are predisposed to sudden death from thromboembolism: evidence that this occurs with exogenous steroids as well

91
Q

what should you treat hyperaldosteronism with?

A

spironolactone: aldosterone antagonist

92
Q

what is the drug of choice for canine and feline cushings?

A

trilostane

93
Q

how is equine cushings treated?

A

dopamine agonists
pergolide mesylate

Basic Pharmacology (37 decks)

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