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Glucocorticoids Flashcards

1
Q

What are the receptors of glucocorticoid

A

Cytoplasmic since they are lipophilic they can pass the cell membrane

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2
Q

Primary adrenal insufficiency

A

There is low cortisol due to defect/dysfunction in the adrenal gland causing positive feedback increasing ACTH

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3
Q

Secondary adrenal insufficiency

A

A defect in pituitary gland causing decrease in ACTH hence decrease in Cortisol

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4
Q

Actions of cortisol

A 
Helps in metabolism of 
carbohydrates 
Proteins 
Fats
Also help ion transport and impact H2O electrolyte balance
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5
Q

Cortisol receptors

A

Glucocorticoid and mineralcorticod

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6
Q

Aldosterone receptors

A

Mineralcorticoid

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7
Q

What are the uses of corticosteroids

A

Anti inflammatory and immunosuppressive

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8
Q

How do corticosteroids work on immunosuppression and anti inflammation

A

By increasing the transcription of lipocortin-1 which inhibits phospho lipase A2 to prevent the change in membrane phospholipid

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9
Q

Other name for lipocortin-1

A

Annexin-1

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10
Q

What is used to decrease inflammatory mediators

A

Hydrocortisone hemisuccinate and acetate

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11
Q

Hydrocortisone hemisuccinate characteristics

A

Water soluble ester
Given IV or IM
Quick absorption and onset of action

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12
Q

Hydrocortisone acetate characteristics

A

Insoluble ester
Only given IM
Slow absorption and prolonged effects

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13
Q

List short acting GCS

A

Hydrocortisone and cortisone

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14
Q

List the Intermediate acting GCS

A

Prednisone (prodrug)

Prednisolone and methyprednisolone

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15
Q

List the king acting GCS

A

Dexamethasone and betamethasone

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16
Q

List the minerals corticosteroids

A

Fludocortisone

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17
Q

Mineralocorticoid potency

A

Cortisol 1
Cortisone 0.8
Prednisone and prednisilone 0.3
Fludocortisone 125

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18
Q

What is used in adrenal insufficiency

A

Cortisol and fludocortisone

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19
Q

Which GCS are used for long term treatment of antiallergic, anti inflammatory and immunosuppressive properties

A

Short and intermediate acting GCS

Short: Hydrocortisone and cortisone
Intermediate: Prednisone (prodrug)
Prednisolone and methyprednisolone

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20
Q

Which GCS is used in short term treatment in severe acute condition and when H2O retention is undesirable

A

Betamethasone

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21
Q

Which GCS is given to pregnant women and why

A

Prednisone as it is a prodrugs and when it passes to the fetal circulation it remains as a prodrug and when predinisilone passes to the fetal circulation it gets converted back to Prednisone

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22
Q

Therapeutic uses of glucocorticoids

A

In adrenal disorders as a replacement therapy( in primary and secondary adrenal insufficiency)
And in inflammatory and immunological conditions

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23
Q

In replacement therapy if chronic adrenal insufficiency what do we give to replace cortisol

A

We give hydrocortisone

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24
Q

In replacement therapy if chronic adrenal insufficiency what do we give to replace aldosterone

A

We give fludocortisone

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25
When in the day is replacement therapy always given
We always give 2/3 of the dose in the morning and 1/3 in the afternoon
26
Corticosteroids used in anaphylactic shock
Hydrocortisone Methylprednisilone Dexamethasone All give IV
27
What GCS is given for lung maturation and when do we give them
Betamethasone or dexamethasone given IM -> given in 2 :- - 48 hours prior to birth - 24 hours before delivery
28
What is Dexamethasone suppression test done for
To diagnose Cushing disease ( pituitary ACTH) or Cushing’s syndrome (cortisol or ectopic ACTH - done over 2 days
29
How to differentiate between Cushing disease and syndrome after Dexamethasone suppression test
- if patient has Cushing disease -> there is supression in normal HPA axis and Pituitary adenoma - if patient has Cushing syndrome-> no suppression in HPA axis and adrenal adenoma and ectopic ACTH secreting tumour
30
Adverse effect of GCS
Due to carbohydrate metabolism-> hyperglycaemia and resistance to insulin -diabetes like Due to protein metabolism-> muscle wasting and thinning of skin - central obesity moon face, buffalo hump And slim limbs -osteoporosis impaired wound healing and increased susceptibility to infections
31
More adverse effects of GCS
Diabetes mellitus, hypertension and PVD
32
Withdrawal symptoms of GCS
Adrenal insufficiency
33
How to reduce the risk of HPA axis suppression
- Use low dose of the drug - Follow daily rhythms, single morning does and alternate days therapy - short duration of therapy - use short and intermediate GCS - use topical route if administration
34
How to reduce osteoporosis from GCS
Physical activity and supplementation with Vitamin D and Ca
35
How to prevent preteen breakdown and muscle wasting with GCS
Physical activity and prevent hypokalemia
36
How to prevent GCS Increase risk of GI events
Take oral GCS with food and PPIs and eradication of H pylori
37
What is topical administration of glucocorticoids used for
Asthma Rhinitis Ocular diseases Dermatological conditions
38
Why are GCS given topical
To prevent systemic side effects
39
What do GCS do in asthma
Inhibit inflammatory reactions in airways but has no effect on acute bronchospasm
40
Topical asthma treatment with GCS side effects
Dry mouth, pharyngeal irritation and increased risk of oral candidiasis
41
How to reduce adverse effects of asthma GCS
Use spacer Rinsing the mouth after inhalation Use before meal Use low doses
42
What ocular diseases are given GCS
Posterior segment diseases - diabetic macular edema branch - retinal vein occlusion
43
What should be monitored when giving GCS to people with ocular diseases
Ocular pressure
44
Which dermatological conditions are treated with GCS
allergic dermatitis, urticaria, psoriasis and hives
45
Which GCS is given for dermatological confirmations
Betamethasone
46
GCS route if administration for rheumatoid arthritis
Oral and IM (depot)
47
GCS route if administration for osteoarthritis
Topical - intra articular injections
48
GCS route if administration for asthma
Inhalation (recommended) | Could be given oral and IV
49
GCS route if administration for anaphylactic shock
IV
50
GCS route if administration for allergic conjunctivitis
Topical eye drops
51
GCS route if administration for ants bite
Topical ointment
52
List the antagonists of adrenocortical agents
Aminoglutethimide Ketoconazole Metyrapone
53
Aminoglutethimide mechanism of action
Blocks the conversion of cholesterol to pregnenolone by inhibiting CHOLESTEROL DESMOLASE
54
Aminoglutethimide indications
Cushing syndrome due to Adrenocortical cancer and in breast carcinoma
55
Ketoconazole mechanism of action
Inhibits 17a hydroxylase which is used for adrenal and gonadal steroid synthesis
56
Ketoconazole indication
Cushing syndrome
57
Metylrapone mechanism of action
11 B hydroxylase inhibitor
58
Methrapone indication
Cushing syndrome
59
Which drug is used for pregnant women with Cushing syndrome
Metyrapone
60
What can cause acute adrenal insufficiency- adrenal crisis
``` Can be caused by Haemorrhage Sepsis Abrupt cessation of exogenous glucocorticoids Addison disease Challenged by stress or surgery ```
61
Treatment of adrenal crisis
Hydrocortisone succinate given as bolus then slow infusion | And dexamethasone

Pharmacology (33 decks)

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