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Pharm Exam 3 > Exam 3: L24-25 ACTH And Adrenal Steroids > Flashcards

Exam 3: L24-25 ACTH And Adrenal Steroids Flashcards

1
Q

Hydrocortisone

A

Preferred replacement therapy for Adrenocortical
Insufficiency
Equal mineralocorticoid and glucocorticoid

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2
Q

Cortisone

A

Inactive and must convert to hydrocortisone in the liver

80% potency of hydrocortisone d/t metabolic loss

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3
Q

What is Fludrocortisone?

A

An oral synthetic adrenocortical steroid with mineralocorticoid and glucocorticoid activity

Fludrocortisone has high glucocorticoid effects but more significant mineralocorticoid properties.

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4
Q

What are the pharmacologic actions of Fludrocortisone similar to?

A

Aldosterone

Fludrocortisone mimics the actions of aldosterone in the body.

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5
Q

When is Fludrocortisone used in combination with glucocorticoids?

A

For replacement therapy in primary adrenocortical insufficiency

This is especially important in conditions where both cortisol and aldosterone are absent.

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6
Q

What is the most severe form of 21-hydroxylase deficiency that Fludrocortisone is indicated for?

A

Salt-losing adrenogenital syndrome

In this condition, both cortisol and aldosterone are virtually absent.

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7
Q

In what situation is Fludrocortisone given independently of glucocorticoids?

A

When only aldosterone replacement is necessary

This includes conditions like corticosterone methyloxidase deficiency (18-hydroxylase deficiency).

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8
Q

Fill in the blank: Fludrocortisone has high _______ effects but much more significant _______ properties.

A

glucocorticoid, mineralocorticoid

This highlights the dual activity of Fludrocortisone.

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9
Q

What type of effects do Prednisone and Prednisolone have?

A

More glucocorticoid effects than mineralocorticoid

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10
Q

What must happen for Prednisone to be active?

A

It must be converted to prednisolone in the liver

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11
Q

What is the most commonly prescribed oral glucocorticoid?

A

Prednisone

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12
Q

For what purposes is Prednisone typically used?

A

Anti-inflammatory purposes

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13
Q

How should Prednisone be administered for it to be effective?

A

Orally, not topically or injected locally

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14
Q

What are the anti-inflammatory effects of Triamcinolone, Methylprednisolone, and Betamethasone?

A

Highest anti-inflammatory effects with no salt-retaining effects

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15
Q

What type of activity do Triamcinolone, Methylprednisolone, and Betamethasone have?

A

Virtually no mineralocorticoid activity

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16
Q

What is the primary use of Triamcinolone, Methylprednisolone, and Betamethasone?

A

Typically only used for anti-inflammatory purposes

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17
Q

What is a key difference among newer glucocorticoid drugs compared to older ones?

A

Differences exist in duration of action and potency

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18
Q

Fill in the blank: Prednisone is similar to _______ and hydrocortisone.

A

cortisone

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19
Q

Does Dexamethasone have mineralocorticoid activity?

A

No

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20
Q

What type of activity does Dexamethasone have?

A

Very high glucocorticoid activity

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21
Q

For what purpose is Dexamethasone typically used?

A

Anti-inflammatory purposes

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22
Q

Why is Dexamethasone the preferred glucocorticoid for cerebral edema?

A

Because of its ability to enter the CNS

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23
Q

When is Dexamethasone used in relation to endogenous cortisol levels?

A

When endogenous cortisol levels have to be measured

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24
Q

What is a specific test that uses Dexamethasone?

A

Dexamethasone suppression tests

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25
Q

Fill in the blank: Dexamethasone is preferred for cerebral edema due to its ability to enter the _______.

A

CNS

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26
Q

What is Fluticasone commonly prescribed for?

A

Asthma: Inhaled and intranasal

Rhinitis: intranasal

May use oral if inhaled not working

Fluticasone is marketed under the brand names Flovent® and Flonase®.

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27
Q

Fluticasone is categorized as what type of medication?

A

Glucocorticoid

28
Q

What is Ketoconazole (Nizoral®)?

A

Orally active antifungal agent that also inhibits steroidogenesis at higher doses

Ketoconazole is primarily known for its antifungal properties but has significant effects on hormone synthesis.

29
Q

What is the mechanism of action of Ketoconazole?

A

Inhibits 17a-hydroxylase → decreased androgens first then cortisol

At even higher doses, it also inhibits the conversion of cholesterol to pregnenolone, thereby inhibiting all steroid synthesis.

30
Q

What are the primary therapeutic effects of Ketoconazole?

A

Typically first line inhibitor of steroid biosynthesis used in patients with Cushing’s

It is used off label for other conditions not approved by the FDA.

31
Q

What is a significant pharmacokinetic property of Ketoconazole?

A

Metabolized by and is a strong inhibitor of CYP3A4

This can lead to interactions with other medications that are metabolized by the same enzyme.

32
Q

What are some common adverse effects of Ketoconazole?

A

Reversible hepatotoxicity, gynecomastia, libido decrease, and impotence

These side effects are important to consider when prescribing the drug.

33
Q

What are the contraindications/precautions associated with Ketoconazole?

A

Potentially teratogenic, not first line drug in pregnancy

It is crucial to avoid its use in pregnant women due to potential risks to the fetus.

34
Q

What is the mechanism of action of Metyrapone?

A

Relatively selective inhibitor of 11ß1-hydroxylase, the terminal enzyme in cortisol synthesis

It also reduces deoxycorticosterone levels, and thus aldosterone.

35
Q

What cortisol precursor is increased by Metyrapone?

A

11-deoxycortisol

36
Q

What are the therapeutic indications for Metyrapone?

A
  • Tests of adrenal function
  • Short-term management of symptoms while cause of Cushing’s is being determined
  • Long-term treatment of Cushing’s disease (off-label)
37
Q

Which patient group can Metyrapone be given to that other drugs in its class cannot?

A

Pregnant women

38
Q

What are some adverse effects of Metyrapone?

A
  • GI disturbances
  • Sedation
  • Dizziness
  • Rash
  • Hirsutism (androgen shunt)
39
Q

True or False: Metyrapone is considered a first-line drug for long-term management in non-pregnant women.

40
Q

How does Metyrapone affect aldosterone function?

A

Increases 11-deoxycortisol, which sustains aldosterone functions

41
Q

What is a notable advantage of Metyrapone compared to mitotane?

A

Less toxicity

42
Q

What is Osilodrostat also known as?

A

Isturisa®

43
Q

When was Osilodrostat FDA approved?

A

March 2020

44
Q

What is the mechanism of action of Osilodrostat?

A

Inhibitor of 11ß1-hydroxylase and aldosterone synthesis

45
Q

What condition is Osilodrostat indicated for?

A

Cushing’s syndrome

46
Q

What is a key indication for using Osilodrostat?

A

When pituitary surgery is not an option or has not been curative

47
Q

What is significant about Osilodrostat in the context of Cushing’s disease?

A

First cortisol synthesis inhibitor to be FDA-approved for treatment

48
Q

How is Osilodrostat metabolized?

A

By multiple hepatic enzymes, including CYP3A4

49
Q

What dosage adjustment is necessary when combining Osilodrostat with ketoconazole?

A

Decreased dose

50
Q

What is a common adverse effect of Osilodrostat that affects 43% of patients?

A

Hypocortisolism leading to adrenal insufficiency

51
Q

List three adverse effects of Osilodrostat that occurred in more than 20% of patients.

A
  • Fatigue
  • Nausea
  • Headache
  • Edema
52
Q

What percentage of patients taking Osilodrostat experienced hypertension?

53
Q

What are two adverse effects associated with women taking Osilodrostat?

A
  • Hirsutism
  • Acne
54
Q

What are two potential serious adverse effects of Osilodrostat?

A
  • Hypokalemia
  • Prolonged QT interval
55
Q

Has Osilodrostat been tested in pregnant women?

A

No, but no problems in pregnant animals at normal doses

56
Q

What was the effect of high doses of Osilodrostat in pregnant animals?

A

Decreased fetal viability

57
Q

What is Mifepristone also known as?

A

RU 486, Mifeprix®

58
Q

What is the primary mechanism of action of Mifepristone?

A

Powerful antagonist of progesterone receptors, and at higher doses, glucocorticoid receptors

59
Q

What is Mifepristone approved for?

A

Inducing abortions

60
Q

What condition can Mifepristone help manage in inoperable patients?

A

Ectopic ACTH secretion or adrenal carcinoma who have failed to respond to other therapies

61
Q

What symptoms can Mifepristone provide rapid relief from?

A

Some hypercortisolemia symptoms like psychosis

62
Q

What are some contraindications or precautions for Mifepristone?

A

Abdominal pain, amenorrhea, fatigue, gastrointestinal upset, pregnancy

63
Q

What is Spironolactone also known as?

A

Aldactone®

64
Q

What is the mechanism of action of Spironolactone?

A

Competitive mineralocorticoid receptor antagonist

65
Q

What additional receptor antagonism properties does Spironolactone have?

A

Androgen and progesterone receptor antagonist properties

66
Q

What are the therapeutic uses of Spironolactone?

A
  • Potassium-sparing diuretic
  • Primary hyperaldosteronism (also for diagnosis)
  • Hypertension
  • Heart Failure
  • Treat ascites associated with cirrhosis
  • Decrease hirsutism in women
67
Q

What adverse effects can Spironolactone cause?

A
  • Hyperkalemia
  • Cardiac arrhythmias
  • Gynecomastia and impotence in men
  • Menstrual irregularities in women
  • Gastrointestinal upset
  • Sedation
  • Headache
  • Skin rashes

Pharm Exam 3 (4 decks)

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