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Pharmacology > Glucocorticoids > Flashcards

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
Q

When in the day is replacement therapy always given

A

We always give 2/3 of the dose in the morning and 1/3 in the afternoon

26
Q

Corticosteroids used in anaphylactic shock

A

Hydrocortisone
Methylprednisilone
Dexamethasone
All give IV

27
Q

What GCS is given for lung maturation and when do we give them

A

Betamethasone or dexamethasone given IM -> given in 2 :-

  • 48 hours prior to birth
  • 24 hours before delivery
28
Q

What is Dexamethasone suppression test done for

A

To diagnose Cushing disease ( pituitary ACTH) or Cushing’s syndrome (cortisol or ectopic ACTH
- done over 2 days

29
Q

How to differentiate between Cushing disease and syndrome after Dexamethasone suppression test

A
  • 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
Q

Adverse effect of GCS

A

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
Q

More adverse effects of GCS

A

Diabetes mellitus, hypertension and PVD

32
Q

Withdrawal symptoms of GCS

A

Adrenal insufficiency

33
Q

How to reduce the risk of HPA axis suppression

A
  • 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
Q

How to reduce osteoporosis from GCS

A

Physical activity and supplementation with Vitamin D and Ca

35
Q

How to prevent preteen breakdown and muscle wasting with GCS

A

Physical activity and prevent hypokalemia

36
Q

How to prevent GCS Increase risk of GI events

A

Take oral GCS with food and PPIs and eradication of H pylori

37
Q

What is topical administration of glucocorticoids used for

A

Asthma
Rhinitis
Ocular diseases
Dermatological conditions

38
Q

Why are GCS given topical

A

To prevent systemic side effects

39
Q

What do GCS do in asthma

A

Inhibit inflammatory reactions in airways but has no effect on acute bronchospasm

40
Q

Topical asthma treatment with GCS side effects

A

Dry mouth, pharyngeal irritation and increased risk of oral candidiasis

41
Q

How to reduce adverse effects of asthma GCS

A

Use spacer
Rinsing the mouth after inhalation
Use before meal
Use low doses

42
Q

What ocular diseases are given GCS

A

Posterior segment diseases

  • diabetic macular edema branch
  • retinal vein occlusion
43
Q

What should be monitored when giving GCS to people with ocular diseases

A

Ocular pressure

44
Q

Which dermatological conditions are treated with GCS

A

allergic dermatitis, urticaria, psoriasis and hives

45
Q

Which GCS is given for dermatological confirmations

A

Betamethasone

46
Q

GCS route if administration for rheumatoid arthritis

A

Oral and IM (depot)

47
Q

GCS route if administration for osteoarthritis

A

Topical - intra articular injections

48
Q

GCS route if administration for asthma

A

Inhalation (recommended)

Could be given oral and IV

49
Q

GCS route if administration for anaphylactic shock

A

IV

50
Q

GCS route if administration for allergic conjunctivitis

A

Topical eye drops

51
Q

GCS route if administration for ants bite

A

Topical ointment

52
Q

List the antagonists of adrenocortical agents

A

Aminoglutethimide
Ketoconazole
Metyrapone

53
Q

Aminoglutethimide mechanism of action

A

Blocks the conversion of cholesterol to pregnenolone by inhibiting CHOLESTEROL DESMOLASE

54
Q

Aminoglutethimide indications

A

Cushing syndrome due to Adrenocortical cancer and in breast carcinoma

55
Q

Ketoconazole mechanism of action

A

Inhibits 17a hydroxylase which is used for adrenal and gonadal steroid synthesis

56
Q

Ketoconazole indication

A

Cushing syndrome

57
Q

Metylrapone mechanism of action

A

11 B hydroxylase inhibitor

58
Q

Methrapone indication

A

Cushing syndrome

59
Q

Which drug is used for pregnant women with Cushing syndrome

A

Metyrapone

60
Q

What can cause acute adrenal insufficiency- adrenal crisis

A 
Can be caused by 
Haemorrhage 
Sepsis 
Abrupt cessation of exogenous glucocorticoids 
Addison disease 
Challenged by stress or surgery
61
Q

Treatment of adrenal crisis

A

Hydrocortisone succinate given as bolus then slow infusion

And dexamethasone

Pharmacology (33 decks)

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