Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHRM 825 Steroids Exam 2 > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

How does the hypothalamus and pituitary regulate the biosynthesis of cortisol?

A

the hypothalamus sends CRH to the pituitary gland then produces ACTH that then stimulates the adrenal gland to produce cortisol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the regulation of glucocorticoid synthesis?

A
  1. Stress
  2. hypothalamus
  3. produce CRH
  4. Pituitary gland
  5. ACTH made
  6. Adrenal gland makes cortisol
  7. can either go back in a feedback loop or produce physiological responses
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what is the regulation of mineralocorticoid synthesis?

A
  1. liver
  2. angiotensinogen produced
  3. angiotensin 1
  4. angiotensin 2
  5. adrenal glands to produce aldosterone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what is a glucocorticoid and its structure?

A
  1. stress hormone
  2. inc. circulating glucose conc.
  3. potent anti-inflammatory effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is a mineralocorticoid and its structure?

A
  1. Na+ retention
  2. Inc. blood volume and BP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what are the two modes of actions of glucocorticoids?

A
  1. cortisol
  2. epinephrine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what is epinepherine’s mode of action?

A
  1. bind to GPCR
  2. initiate signal transduction pathway
  3. induce immediate response
  4. break down glycogen and release glucose
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what is cortisol’s mode of action?

A
  1. bind to nuclear hormone receptor
  2. regulate gene transcription –> translation/production
  3. induce long term response
  4. induce gluconeogenic enzymes
  5. inhibit pro-inflammatory response
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

where do glucocorticoids have physiologic effects?

A
  1. liver
  2. muscle
  3. adipose tissues
  4. immune system
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what are the effects of the liver?

A
  1. inc gluconeogenesis
  2. inc glycogen storage
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what are the effects of the muscle?

A
  1. promote muscle degradation
  2. dec protein synthesis
  3. dec sensitivity to insulin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what are the effects of adipose tissue?

A
  1. promote lipolysis
  2. decrease sensitivity to insulin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what are the effects of the immune system?

A
  1. block the synthesis of cytokines –> immunosuppression
  2. inhibit production of eicosanoids –> anti-inflammation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what do the liver/muscle/adipose tissue have in common?

A

increase blood glucose levels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what is the cause of addison’s disease?

A
  1. hypoadrenalism
  2. destruction of the cortex by tuberculorsis or atrophy
  3. dec. secretion of ACTH
  4. cessation of long-term steroid use
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How are each level of hormone affected by addison’s disease?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what is the cause of cushing’s disease?

A
  1. hyperaldreanlism
  2. tumors in adrenal cortex
  3. inc. production of ACTH due to pituitary carcinoma
  4. ectopic production of ACTH due to non-pituitary carcinoma
  5. long-term steroid use
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

how are each level of hormone affected by cushing’s disease?

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what systemic corticosteroids are short-acting?

A
  1. hydrocortisone
  2. cortisone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what systemic corticosteroids are intermediate-acting?

A
  1. prednisone
  2. prednisolone
  3. methylprednisolone
  4. triamcinolone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

what systemic corticosteroids are long-acting?

A
  1. dexmethasone
  2. betamethasone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what is fludrocortisone?

A
  1. F sub on carbon 9a
  2. greater glucocorticoid activity
  3. strong mineralocorticoid activity (Na+ retention –> edema)
  4. used in mineralocorticoid replacement therapy
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what is prednisone/prednisolone?

A
  1. extra double bond on carbon 1 & 2
  2. more potent glucocorticoid activity
  3. reduced mineralocorticoid activity
  4. interconvertable @ C11 with hydroxysteroid dehydrogenase
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

what is methylprednisolone?

A
  1. methyl group on C6a
  2. more potent glucocorticoid activity
  3. reduced mineralocorticoid activity
25
Q

what is triamcinolone?

A
  1. F on C9a and OH on C16a
  2. more potent glucocorticoid activity
  3. reduced mineralocorticoid activity
  4. inc. bioavailability
  5. low oral bioavailability
26
Q

what is dexmethasone?

A
  1. methyl on C16a
  2. inc. lipophilicity (receptor binding/ stronger)
  3. inc. stability in human plasma
  4. reduced MC activity
27
Q

what is betamethasone?

A
  1. enantiomer of demethasone
  2. similar properties to dexmethasone
28
Q

what do 21-esters do?

A

OH group can be modified to an ester to control the property of glucocorticoids
- prodrugs activated through hydrolysis by esterases

29
Q

what do acetates and butyrates do in terms of 21-ester position?

A
  1. inc. lipophilicty
  2. prolonged action upon IM or IA inj
30
Q

what do succinates do in terms of 21-ester position?

A
  1. soluble
  2. slow hydrolysis
31
Q

what do phosphates do in terms of 21-ester position?

A
  1. inc. solubility
  2. rapid hydrolysis by phosphatases
  3. IV or IM inj for EC
32
Q

what are the desired properties of inhaled glucocorticoids?

A
  1. high potency
  2. minimal systemic effects
  3. prolonged action
33
Q

what is triamcinolone acetonide?

A
  1. acetonide is resistant to hydrolysis
  2. 8x more potent than prednisolone
34
Q

what is beclomethasone dipropionate?

A
  1. 14x more potent than dexmethasone
  2. converted rapidly to 17 monopropionate by hydrolysis
35
Q

what is flunisolide?

A
  1. rapid absorption from nasal or lung tissue
  2. rapid metabolism by liver
    – first path metabolism
  3. minimal adverse effect from long term use
36
Q

what is budesonide?

A
  1. 1:1 mix of epimers 16,17 butylacetal
  2. faster topical uptake
  3. low oral bioavailability
  4. first path metabolism
37
Q

what is mometasone furoate?

A
  1. highly potent
  2. more rapid onset of action
  3. negligible systemic availability
    – rapid metabolism
    – low oral bioavailability
  4. poor solubility
38
Q

what is fluticasone propionate?

A
  1. inactivated by hydrolysis of thioester
    – rapid first path metabolism
  2. highly lipophilic and insoluble (poor)
    – high potent
    – poor absoprtion from GI
    – rapid topical uptake
39
Q

what is a potent topical glucocorticoid?

A

halogenated analogues

40
Q

what forms have better potency for topical applications due to high lipophilicity?

A

acetonide or ester forms

41
Q

what topical glucocorticoids have very high potency?

A

clobestasol propionate, halobetasol propionate

42
Q

what topical glucocorticoids have high potency?

A

halcinonide, triamcinolone acetonide, fluocinonide

43
Q

what topical glucocorticoids have medium potency?

A

betamethasone valerate, mometasone furoate, fluticasone propionate

44
Q

what does a 21-chlorocorticoid do?

A

substitution here of a Cl instead of OH enhances TOPICAL anti-inflammatory activity

45
Q

what are adverse effects of glucocorticoids?

A
  1. crossover mineralocorticoid activity
  2. metabolic effects
  3. cushing’s-like effects
  4. impaired glucose tolerance
  5. suppression of immune system
  6. GI
  7. CNS
  8. cataracts
  9. adrenal insufficiency upon withdrawal (addisonian crisis)
46
Q

describe crossover mineralocorticoid activity better of adverse effects for glucocorticoids?

A
  1. sodium and water retention
  2. development of HTN
  3. correctable with selective synthetic glucocorticoids
47
Q

describe the metabolic effects better of adverse effects for glucocorticoids?

A
  1. inc. glucose production
  2. steroid myopathy
  3. reduced long bone growth in children
  4. osteoporosis
48
Q

describe cushing’s-like effects of adverse effects for glucocorticoids?

A
  1. redistribution of fat
  2. moon face
  3. buffalo hump
49
Q

describe impaired glucose tolerance of adverse effects for glucocorticoids?

A
  1. hyperglycemia from gluconeogenesis
  2. dec. insulin response
    – may unmask diabetes
50
Q

describe suppression of immune system of adverse effects for glucocorticoids?

A
  1. inc. susceptibility to infections
  2. impaired wound healing
51
Q

describe GI of adverse effects for glucocorticoids?

A
  1. greater peptic ulcer risk
52
Q

describe CNS of adverse effects for glucocorticoids?

A
  1. linked to glucose metabolism
  2. euphoria
  3. depression
53
Q

describe adrenal insufficiency upon withdrawal of adverse effects for glucocorticoids?

A
  1. delayed recovery of HT and PT
  2. depressed ACTH release and adrenal response to ACTH
  3. directly related to dose/duration of therapy
  4. Symptoms
    – hypotension, weakness, inability to handle stress
  5. due to negative feedback
54
Q

what drugs are systemic corticosteroids?

A
  1. hydrocortisone
  2. cortisone
  3. prednisone
  4. prednisolone
  5. methylprednisolone
  6. betamethasone
  7. dexamethasone
55
Q

what drugs are systemic meneralocorticoids?

A
  1. fludrocortisone
56
Q

what drugs are inhaled glucocrticoids?

A
  1. traimcinolone acetonide
  2. beclomethasone dipropionate
  3. flunisolide
  4. budesonide
  5. mometasone furoate
  6. fluticasone propionate
57
Q

what drugs are topical glucocorticoids?

A
  1. triamcinolone acetonide
  2. fluocinonide
  3. betamethasone valerate
  4. clobestasol propionate
  5. halobetasol propionate
  6. halcinonide
58
Q

what are some strategies to minimize the adverse effects of glucocorticoids?

A
  1. no long term use
  2. no smoking/ alcohol
  3. maintain healthy lifestyle

PHRM 825 Steroids Exam 2 (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions