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Pharmacology Exam 1 > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

characteristic of glucocorticoids

A

stress hormones
increase circulating glucose
potent anti-inflammatory effects

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2
Q

characteristics of mineralocorticoids

A

Na+ retention
increase blood volume
increase blood pressure

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3
Q

regulation of mineralocorticoid synthesis

A

anterior pituitary does not control the synthesis of mineralocorticoids

RAA-system does

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4
Q

transport of steroids

A

transported in plasma by plasma transport proteins
corticoid-binding globulin - glucocorticoids & progesterone
sex hormone binding globulin - testosterone and estradiol

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5
Q

where are steroids metabolized

A

metabolized in the liver to soluble forms

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6
Q

excretion of steroids

A

excreted in bile (estrogen) or in the urine (progesterone, androgen, and glucocorticoids)

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7
Q

what are GRes

A

Glucocorticoid Resposive Elements - DNA binding domains that are targets of activated dimers

GREs are upstream of steroid responsive genes

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8
Q

what do glucocorticoids upregulate

A

glucocorticoids upregulate enzymes for gluconeogenesis & anti-inflammatory proteins

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9
Q

what catalyzes the rate-limiting step in gluconeogenesis

A

phosphoenolpyruvate carboxykinase (PEPCK)

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10
Q

function of lipocortin 1

A

suppresses phospholipase A2, critical role in eicosanoid synthesis

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11
Q

mechanism of suppression by glucocorticoids

A

activated glucocorticoid Rs binds to NFkB and prevents binding of NFkB to its response element
transcription of cytokine genes are repressed

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12
Q

physiologic effects of cortisol on liver

A

increases gluconeogenesis in short-term fasting

inreases glycogen storage in long-term fasting

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13
Q

physiologic effect of cortisol on muscle

A

promote protein degradation
decrease protein synthesis
decrease sensitivity to insulin

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14
Q

physiologic effect of cortisol on adipose tissues

A

promote lipolysis

decrease sensitivity to insulin

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15
Q

physiologic effect of cortisol on immune system

A

block the synthesis of cytokines (immunosuppression)

inhibits the production of eicosanoids (anti-inflammatory)

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16
Q

addison’s disease

A

hypoadrenalism

decreased secretion of steroid hormone by the adrenal cortex

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17
Q

causes of addison’s disease

A

destruction of the cortex by tuberculosis or atrophy

decreased secretion of ACTH due to diseases of anterior pituitary

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18
Q

symptoms of addison’s disease

A

extreme weakness

anorexia, anemia, nausea, vomiting

low blood pressure (primary Addison’s only)

skin hyperpigmentation (primary Addison’s only)

mental depression

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19
Q

what is another possible cause of Addison’s-like symptoms

A

cessation of long-term system glucocorticoid therapy can lead to Addisonian symptoms

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20
Q

characteristics of primary addison’s disease

A

adrenal defect

high CRH, high ACTH, low cortisol, low aldosterone

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21
Q

characteristics of secondary addison’s disease

A

pituitary defect

high CRH, low ACTH, low cortisol, aldosterone not affected

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22
Q

characteristics of tertiary addison’s disease

A

hypothalamic defect

low CRH, low ACTH, low cortisol, aldosterone not affected

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23
Q

Cushing’s disease

A

hyperadrenalism

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24
Q

causes of Cushing’s disease

A
  • tumors in the adrnal cortex
  • increased production of ACTH due to pituitary carcinoma
  • ectopic production of ACTH due to non-pituitary carcinoma
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25
symptoms of Cushing's disease
increased protein catabolism (easy bruising, delayed wound healing, muscle wasting) and higher glucose osteoporosis opportunistic infections
26
what else can cause Cushing's symptoms
long-term therapeutic use of systemic glucocorticoids
27
characteristics of adrenal Cushing's disease
low CrH, low ACTH, high cortisol
28
characteristics of pituitary Cushing's disease
low CRH, high ACTH, high cortisol
29
characteristics of ectopic Cushing's disease
low CRH, low ACTH, high cortisol, high ectopic ACTH
30
characteristics of ketoconazole
antifungal at lower concentrations (block synth of ergosterol) inhibits P450scc, 17-alpha hydroxylase, and 11beta-hydroxylase can tx hyperglucocorticoid states may cause toxic side effects
31
therapeutic uses of corticosteroids
- primary adrenal insufficiency cause by atrophy of adrenal cortex - allergic rxns - inflammation & autoimmune diseases - asthma - immunosuppressive - anti-cancer
32
requirements for glucocorticoid activity
4,5-double bond C3 ketone 11-beta hydroxyl C17 hydroxyl
33
requirements for mineralcorticoid activity
4,5-double bond C3 ketone 11-beta hydroxyl less important C17 hydroxyl is NOT rquired
34
cortisol vs cortisone
oxidation of 11 hydroxyl to ketone inactivates glucocorticoid rxn catalyzed in liver by 11beta-hydroxysteroid DH (reversible)
35
in whom should cortisone not be used
in patients with impaired liver functions
36
short acting corticosteroids
t1/2 8-12 hrs hydrocortisone cortisone
37
intermediate acting corticosteroids
``` t1/2 12-36 hrs prednisone prednisolone methylprednisolone triamcinolone ```
38
long-acting corticosteroids
t1/2 36-54 hrs dexamethasone betamethasone
39
characteristics of fludrocortisone
9alpha-F greater glucocorticoid activity strong mineralocorticoid activity intense Na+ retention leading to edema
40
use for fludocortisone
used in mineralocorticoid replacement therapy
41
characteristics of prednisone/prednisolone
extra double bound C1-C2 more potent, stronger binding to R reduced mineralocorticoid act., interconvertable by 11beta-hydroxysteroid DH
42
characteristics of methylprednisolone
6alpha-methyl group potency similar to that of prednisolone reduced mineralocorticoid activity
43
characteristics of triamcinolone
``` 9alpha-F and 16alpha-OH GC act. similar to prednisone reduced MC act. increased hydrophilicty low oral bioavailability ```
44
characteristics of dexamethasone
16alpha-methyl group increased lipophilicity -> ups R binding, stronger effect increased stability in human plasma reduced MC activity
45
characteristics of betamethasone
enantiomer of dexamethasone at 16 | similar properties to dexamethasone
46
characteristics of 21-esters
hydroxyl group @ 21 can mod. to ester to control GC properties
47
if modified 21 hydroxyl to ester with acetate & butyrate
switching to acetate and butyrate -> increased lipophilicity, prolonged action upon IM
48
if modified 21 hydroxyl to ester with succinate
switch to succinate-> soluble, slow hydrolysis
49
if modified 21 hydroxly to ester with phosphate
increased solubility rapid hydrolysis by phosphatases IV or IM injection for emergency conditions
50
desired properties of topical GCs
high lipophilicity minimal systemic effect prolonged action halogenated are more potent
51
characteristics of topical GCs
once absorbed, metabolized primariy through the liver & excreted in the bile low potentcy GC are safest for chronic applications high potentcy GC for short term use
52
why do acetonide or eseter forms have better potency for topical applications
high lipophilicity eg traimcinolone acetonide > betamethasone valerate
53
21-chlorocorticoids
greatly enhances topical anti-inflammatory activity eg clobetasol proprionate, halobetasol proprionate, halcinonide
54
characteristics of topical corticosteroids
only medium potency for topical corticosteroids high lipophilicity and highest binding affinity but poor solubility poor dissolution into inflamed tissue
55
desired properties of inhaled GCs
high potency minimal systemic effects prolonged action
56
characteristics of inhaled GCs
high lipophilicity low oral bioavailability rapid clearance eg triamcinolone acetonide & beclomethasone diproprionate
57
characteristics of triamcinolone acetonide
acetonide is resistant to hydrolysis | 8x more potent than prednisolone
58
characteristics of beclomethasone diproprionate
converted rapidly to 17-monoproprionate by hydrolysis | 14x more potent than dexamethasone
59
characteristics of flunisolide
rapid absorption from nasal or lung tissue rapid metabolism by liver, extensive "first-path" metabolism minimal systemic adverse effect with long-term therapy
60
characteristics of budesonide
1:1 mixture of epimers at 16,17-butylacetal faster topical uptake low oral bioavailability extensive first-path metabolism
61
characteristics of mometasone furoate
``` highly potent more rapid onset of action negligible systemic availability rapid metabolism low oral bioavailability ```
62
characteristics of fluticasone proprionate
``` inactivated by hydrolysis of thioester rapid first-path metabolism highly lipophilic and insoluble highly potent poor absorption from GI rapid topical uptake ```
63
possible adverse crossover effects of corticoids
-crossover mineralocorticoid activity (Na+/H2O retention, HTN, correctible with synth. GCs)
64
adverse metabolic effects of corticoids
- metabolic effects (ups glucose produc) - -steroid myopathy - high doses cause wasting of prox muscles - -reduced long bone growth in kids-> premature closing of epiphyseal junction - -osteoporosis-inhibit osteoblasts, prevented by bisphosphonate - Cushing's like effects (redistrib. of fat) - impaired glucose tolerance
65
effects of corticoids on immune system
increased susceptibility to infections by suppressing immune system impair wound healing
66
corticoids on GI
greater peptic ulcer risk
67
corticoids on CNS
linked to glucose metabolism euphoria depression cataracts
68
adverse effects of corticoids on withdrawal
adrenal insufficiency (addisonian crisis)
69
symptoms of addisonian crisis
inability to withstand stress hypotension weakness

Pharmacology Exam 1 (7 decks)

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