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Pharmacodynamics > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

What are corticosteroids?

A

Hormones derived from cholesterol, produced in the adrenal gland

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2
Q

What are the main corticosteroids?

A
  • Cortisol

- Aldosterone

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3
Q

2 categories of corticosteroids that cortisol and aldosterone split into?

A 
Glucocorticoid = Cortisol
Mineralocorticoid = Aldosterone
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4
Q

Where does cortisol act?

A

Acts via glucocorticoid receptors

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5
Q

Where does Aldosterone act?

A

Acts via mineralocorticoid receptors

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6
Q

What is the role of cortisol?

A

Acts upon carbohydrates and protein metabolism

Has regulatory effects on host defence mechanisms

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7
Q

What is the role of aldosterone?

A

Regulates water and electrolyte balance

Sodium conservation in sweat and renal glands.

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8
Q

How is glucocorticoid release regulated?

A

Regulated by the Hypothalamic - Pituitary - Adrenal (HPA) axis.

-Negative feedback control

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9
Q

Explain the Hypothalamic - pituitary - adrenal axis (HPA) regulation

A

The hypothalamus releases Corticotropin releasing hormone (CRH), +ve stimulatory effect on:

Anterior Pituitary which releases adrenocorticotropic hormone (ACTH), which causes stimulatory effects on the release of glucocorticoids from the adrenal gland.

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10
Q

What is Cushing’s syndrome?

A

A result of excessive levels of endogenous glucocorticoids.

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11
Q

What is Addison’s syndrome?

A

(Adrenal insufficiency)

A result of little levels of corticosteroids in the body.

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12
Q

What is Metyrapone?

A

A competitive inhibitor involved with glucocorticoid release.

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13
Q

What is the role of Metyrapone?

A

Reduces glucocorticoids when there’s overload.

This inhibits beta - hydroxylase which inhibits cortisol.

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14
Q

Symptoms of Cushing’s syndrome:

A

Easy bruising
Thinning of skin
Hypertension

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15
Q

What are the two molecular mechanisms of action for glucocorticoids

A

Upregulate transcriptional machinery (TM)

Repress the activity of transcriptional factors

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16
Q

The molecular mechanism of action of glucocorticoids:

A

Dimerized glucocorticoids bind to recognition sites on DNA.

17
Q

Up regulation of transcriptional machinery?

A

Glucocorticoids bind to glucocorticoid receptor = Ligand binding results in a nuclear receptor being activated.

18
Q

What is gene transpression?

A

One protein represses the activity of second protein.

Results in silencing pro-inflammatory genes.

19
Q

What happens as a result to repressing the activity of transcription factors?

A

This influences multiple signal transductions.

Switching off multiple activated inflammatory genes via the inhibition of HDAC2 and HAT.

20
Q

What action occurs on inflammatory cells?

A

Decreased no. of neutrophils from blood vessels and reduced activation of neutrophils / macrophages / mast cells.

Theres decreased activation of T-helper cells
Decreased fibroblast function

21
Q

Examples of natural glucocorticoids therapeutically?

A

Cortisol

22
Q

Which glucocorticoid is the most potent and has the least mineralocorticoid activity?

A

Dexamethasone

23
Q

The mechanism of synthetic glucocorticoids?

A

They bind to albumin, not to transcortin.

They are more slowly metabolised in the liver giving them a longer duration of action.

24
Q

Mechanism of Hydrocortisone?

A

Binds to corticosteroid-binding globulin and to albumin in the blood, and is extensively metabolised in the gut wall liver.

25
Q

Examples of therapeutically used synthetic glucocorticoids.

A

Cortisone
Prednisone
Betamethasone
Dexamethasone

26
Q

Mechanism of cortisol glucocorticoids?

A

Binds to corticosteroid-binding albumin and this is extensively metabolised in the gut wall

27
Q

Diseases that benefit from glucocorticoids therapy?

A

Myeloma
Bronchial Asthma
Organ transplantation

28
Q

Administration of glucocorticoids?

A

Topical Administration

29
Q

Benefits of Topical administration of glucocorticoids?

A

They can deliver high concentrations to the target site.

They achieve the desired concentration without adversely/ excessively increasing systemic side effects.

30
Q

What are the side effects of glucocorticoid therapy?

A

Cushing’s syndrome
Osteoporisis
Muscle wasting
Euphoria

31
Q

The difference between Cushing’s syndrome and Addison’s syndrome?

A 
Cushing's = Too much hormones
Addison's = Too little hormones

Pharmacodynamics (18 decks)

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