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First Aid Step 1 material > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

Treatment regimen for Cushings Disease (3 pharm)

A

Surgery is main option
A Aminoglutethimide
K Ketoconazole
M Metyrapone

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2
Q

Aminoglutethimide inhibits what CYP?

A

CYP11A1

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3
Q

Mechanism of Aminoglutethimide

A

inhibits CYP11A1 resulting in inhibition of corticosteroid synthesis

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4
Q

Aminoglutethimide side effects

A

adrenal insufficiency

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5
Q

Aminoglutethimide drug interaction

A

increased metabolism of other drugs such as

warfarin, theopyylline and digitoxin

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6
Q

Ketoconazole Mechanism (3)

A

high doses - inhibits CYP17, inhibiting glucocorticoid and androgen synthesis
even higher doses - inhibits CYP11A1, inhibiting all steroidogenesis
also reduces ACTH secretion at therapeutic doses

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7
Q

Another name for CYP11A1 and action

A

Cholesterol Desmolase

converts Cholesterol to Pregnenolone

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8
Q

Use for Ketoconazole?

A

Treat Cushing’s Disease and fungal infections

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9
Q

Drug Interaction of Ketoconazole (2)

A

inhibits multiple CYPs, many potential interactions

inhibits P-glycoprotein so may increase levels of P-gp substrates

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10
Q

Metyrapone mechanism

A

selective inhibitor of CYP11B1 reducing the biosynthesis of cortisol

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11
Q

What CYP does Metyrapone inhibit?

A

CYP11B1

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12
Q

Metyrapone clinical use?

A

hypercorticism

diagnostic test for Cushings

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13
Q

Metyrapone main side effect and why it occurs?

A

Hirsutism - due to increased synthesis of adrenal androgens upstream from the enzymatic block

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14
Q

Mifepristone (RU-486) mechanism (2)

A

Inhibits the release of the glucocorticoid receptor from the chaperone proteins
Also competitive inhibitor of progestins at progesterone receptors

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15
Q

Mifepristone (RU-486) clinical use (2)

A

controlling hypercortisolism in patients with Cushing’s syndrome due to inoperable ectopic ACTH secreting tumors

abortion pill

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16
Q

Mifepristone (RU-486) main side effect

A

Heavy vaginal bleeding

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17
Q

Mifepristone (RU-486) drug interaction

A

increased metabolism of other drugs such as warfarin, theopyylline and digitoxin

18
Q

Cosyntropin test is used for what?

A

Determining primary vs secondary adrenal insufficiency

19
Q

Primary Adrenal Insufficiency treatment

A

hydrocortisone or cortisone

supplementation with fludrocortisone for mineralocorticoid effect

20
Q

Secondary Adrenal Insufficiency treatment

A

hydrocortisone, cortisone or prednisone

mineralocorticoids are not necessary.

21
Q

Why are Mineralocorticoids only given once a day

A

because their release does not show circadian

effects normally.

22
Q

Most common cause of Congenital Adrenal Hypoplasia

A

Deficiency in CYP21

23
Q

Presentation of Congenital Adrenal Hypoplasia males vs females

A

Males normal at birth precocious puberty

females psedudohermaphroditism

24
Q

Spironolactone Mechanism

A

Blocks renal aldosterone receptors

Also progesterone agonist and androgen antagonist

25
Q

Spironolactone clinical use

A

treatment of aldosteronism for non-surgical candidates

26
Q

Spironolactone side effects

A

breast tenderness and menstrual irregularities in women

impotence, decreased libido, and gynecomastia in men

27
Q

Glucocorticoids have excellent ___ activity and are they curative?

A

Excellent anti-inflammatory activity

Underlying cause is still present

28
Q

What occurs if you rapidly withdraw glucocorticoids?

A

adrenal insufficiency, must wean off

29
Q

What demographic must you be careful about with glucocorticoids?

A

post-menopausal women and osteoporosis patients

30
Q

Corticosteroids inhibit what transcription factor?

A

NF-kB

31
Q

What does cortisol bind to in blood and what raises the protein’s levels?

A

90% of cortisol binds to corticosteroid binding globulin (CBG) & albumin in the plasma

Pregnancy and estrogen therapy

32
Q

Metabolism of corticosteroids?

A

first pass hepatic conjugation and then renally excreted

33
Q

Why should people with infections or AIDS avoid corticosteroids?

A

they are highly immunosuppressive

34
Q

What must you supplement post-menopausal woman with when giving corticosteroids?

A

Vitamin D and Calcium with high protein diet

35
Q

Why use caution giving glucocorticoids to psychotic patients?

A

may exacerbate condition - side effect of drugs

36
Q

Which corticosteroid can induce cleft palate and still birth

A

Dexamethasone

37
Q

Why recommend no breast feeding in systemic steroid treatment.

A

can redistribute in breast milk

38
Q

Why be cautious in treating diabetics with steroids?

A

induces hyperglycemia

39
Q

Why be cautious in treating heart patients with steroids?

A

due to potential weight gain and hypertension and hyperlipidemia induced by steroids

40
Q

Hepatic microsomal enzyme inducers (barbiturates, carbamazepine, phenytoin) do what to corticosteroid metabolism?

A

promote corticosteroid metabolism.

First Aid Step 1 material (10 decks)

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