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Therapeutics > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

Binds to Beta-adrenergic receptor (GPCR)
Initiates signal transduction cascade
Induces immediate response
Breaks down glycogen and release glucose

A

Epinephrine

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2
Q

Binds to glucocorticoid receptor
Regulates gene transcription and thus translation and protein production
Induces long term, persistent biological response
Induces gluconeogenic enzymes
Inhibit pro-inflammatory processes

A

Cortisol (hydrocortison)

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3
Q

Which part of the kidneys make glucocorticoids, mineralocorticoids, and androgens?

A

Cortex of the adrenal gland

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4
Q

Which part of the kidneys make epinephrine and norepinephrine?

A

Medulla of adrenal gland

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5
Q

Stress hormones
Increase circulating glucose concentration
Potent anti-inflammatory effects

A

Glucocorticoids

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6
Q

Adrenocorticoid that leads to Na+ retention and increased blood volume and pressure

A

Mineralocorticoids

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7
Q

Regulation of glucocorticoid synthesis

A

Stress -> Hypothalamus -> CRH -> ACTH -> Cortisol -> physiological responses

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8
Q

DNA-binding domains of activated dimers that bind to specific DNA sequences, upstream of steroid responsive genes

A

Glucocorticoid Responsive Elements (GRE)

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9
Q

Catalyzes the rate-limiting step in gluconeogenesis

A

PEP carboxykinase

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10
Q

Suppresses phospholipase A2, which has a critical role in eicosanoid synthesis

A

lipocortin I

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11
Q

Destruction of the cortex by tuberculosis or atrophy

A

Addison’s disease (primary)

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12
Q

What happens to CRH, ACTH, Cortisol and Aldosterone in Primary adrenal insufficiency?

A

Adrenal defect: Increased CRH and ACTH, decreased Cortisol and Aldosterone

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13
Q

What happens to CRH, ACTH, Cortisol and Aldosterone in Secondary adrenal insufficiency?

A

Pituitary defect: increased CRH and decreased ACTH, Cortisol, and not affected aldosterone

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14
Q

What happens to CRH, ACTH, Cortisol and Aldosterone in Tertiary adrenal insufficiency?

A

Hypothalamic defect: decreased CRH, ACTH, and Cortisol. Aldosterone not affected.

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15
Q

This condition has a few causes:
Tumors in the adrenal cortex
Increased production of ACTH due to pituitary carcinoma
Ectopic production of ACTH due to non-pituitary carcinoma

A

Cushing disease

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16
Q

What happens to CRH, ACTH and Cortisol in Adrenal affected Cushing disease?

A

Decreased CRH and ACTH, increased Cortisol

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17
Q

What happens to CRH, ACTH and Cortisol in Pituitary affected Cushing disease?

A

Decreased CRH and increased ACTH and Cortisol

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18
Q

What happens to CRH, ACTH and Cortisol in Ectopic affected Cushing disease?

A

Decreased CRH, ACTH and increased Cortisol and Ectopic ACTH

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19
Q

What is this glucocorticoid?

A

Cortisone

20
Q

How is cortisol inactivated?

A

Oxidation of 11 hydroxyl to ketone

21
Q

How is Cortisone activated?

A

Catalyzed by 11Beta-hydroxysteroid dehydrogenase in the liver

22
Q

What are the short-acting systemic corticosteroids (2)

A

(-sone): Hydrocortisone and cortisone

23
Q

What are the intermediate-acting corticosteroids? (4)

A

(-olone) Prednisone, Prednisolone, Methylprednisolone, and Triamcinolone

24
Q

What are the long-acting corticosteroids? (2)

A

(-methasone) Dexamethasone and Betamethasone

25
Q

Where is the Florine positioned at?
Greater glucocorticoid activity, strong mineralocorticoid activity (intense Na retention leading to edema)
Used in mineralocorticoid replacement therapy

A

Fludrocortisone: 9alpha-F

26
Q

Where is the altered ring structure?
More potent glucocorticoid activity, stronger binding to the glucocorticoid receptor
Reduced mineralocorticoid activity
Interconvertible by 11Beta-hydroxysteroid dehydrogenase

A

Prednisone/prednisolone
Double bond between C1 and C2

27
Q

Where is the methyl group located?
Potency similar to that for prednisolone
Reduced mineralocorticoid activity

A

Methylprednisolone: 6alpha-methyl group

28
Q

Where is the F and OH located at?
Glucocorticoid activity similar to prednisone
Reduced mineralocorticoid activity
Increased hydrophilicity
Low oral bioavailability

A

Triamcinolone: 9alpha-F and 16alpha-OH

29
Q

Where is the methyl group located?
Increased lipophilicity (increased receptor binding, significantly stronger effect)
Increased stability in human plasma
Reduced mineralocorticoid activity

A

Dexamethasone: 16alpha-methyl group

30
Q

Enantiomer of dexamethasone at what location?
Has similar properties as dexamethasone

A

Betamethasone: 16Beta instead of 16alpha (Dexamethasone)

31
Q

Which modifications of 21-esters increase lipophilicity and prolonged action upon IM or intra-articular injection

A

Acetate and butyrate

32
Q

Which modification of 21-esters is soluble and has slow hydrolysis (peak 30-40min)?

A

Succinate

33
Q

Which modification of 21-esters increases solubility, has rapid hydrolysis by phosphatases, and IV or IM injection for emergency use?

A

phosphate

34
Q

T/F: Glucocorticoids are are method of stopping an asthma attack while its happening?

A

FALSE

35
Q

Which type of glucocorticoid?
where acetonide is resistant to hydrolysis
8x more potent than prednisolone

A

Triamcinolone acetonide (Azmacort)
Inhaled

36
Q

Which type of glucocorticoid?
Converted rapidly to 17-monopropionate by hydrolysis
14x more potent than dexamethasone

A

Beclomethasone dipropionate
Inhaled

37
Q

Which type of glucocorticoid?
Rapid absorption from nasal or lung tissue
Rapid metabolism by the liver: extensive first-path metabolism, minimal systemic adverse effect with long-term therapy

A

Flunisolide (Aerobid)

38
Q

Which type of glucocorticoid?
1:1 mixture of epimers at 16, 17-butylacetal
Faster topical uptake
Low oral bioavailability
Extensive first-path metabolism

A

Budesonide (Pulmicort)
Inhaled

39
Q

Which type of glucocorticoid?
Highly potent, more rapid onset of action, negligible systemic availability (Rapid metabolism, low oral bioavailability)

A

Mometasone furoate (Asmanex)
Inhaled

40
Q

Which type of glucocorticoid?
Inactivate by hydrolysis of thioester (Rapid first-path metabolism)
Highly lipophilic and insoluble (highly potent, poor absorption from GI, rapid topical uptake)

A

Fluticasone propionate
Inhaled

41
Q

What are the three high potency topical glucocorticoids?

A

Triamcinolone acetonide, Fluocinonide, and Halcinonide

42
Q

What are two very high potency topical chlorocorticoids?

A

Clobetasol propionate and halobetasol propionate

43
Q

What are three medium potency topical glucocorticoids?

A

Betamethasone valerate, fluticasone propionate and mometasone furoate

44
Q

High lipophilicity
Minimal systemic effect
Prolonged action
Are desired properties of what?

A

Topical glucocorticoids

45
Q

High potency
Minimal systemic effects
Prolonged action
Are desired properties of what?

A

Inhaled glucocorticoids

Therapeutics (16 decks)

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