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Pharmacology Block 9 > Adrenal Steroids > Flashcards

Adrenal Steroids Flashcards

1
Q

What is mifepristone?

A

A progestational and glucocorticoid hormone antagonist

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2
Q

What are the indications of mifepristone?

A

termination of intrauterine pregnancy through 49 days pregnancy

Control hyperglycemia secondary to hypercortisolism in adult patients with endogenous cushing’s syndrome who have type 2 diabetes mellitus or glucose intolerance and are not candidates for surgery or have had unsuccessful surgery

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3
Q

The anti-progestational activity of mifepristone results from

A

The competitive interaction with progesterone at progesterone-receptor sites. The compound inhibits the activity of endogenous or exogenous progesterone. The termination of pregnancy results

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4
Q

In the treatment of Cushing’s syndrome, mifepristone blocks the

A

Binding of cortisol to its receptor. It does not decrease cortisol production but reduces the effect of excess cortisol such as high blood sugar levels

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5
Q

What are some of the adverse effects of mifepristone?

A

Heavy menstrual bleeding, abdominal pain, uterine cramping, nausea, vomiting and diarrhea

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6
Q

what is metyrapone?

A

Inhibitor of the enzyme steroid 11-beta monooxygenase

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7
Q

What is metyrapone used for?

A

As a diagnostic drug for testing the hypothalamic-pituitary ACTH function and ocasionally for Cushing’s disease

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8
Q

What is the mechanism of action of metyrapone?

A

Inhibits the 11-beta-hydroxylation reaction of the adrenal cortex, reducing cortisol and corticosterone production

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9
Q

What is an adverse effect of metyrapone?

A

Increase in ACTH production by the pituitary

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10
Q

There is marked increase of what compounds and their metabolites while using metyrapone?

A

11-desoxycortisol and desoxycorticosterone

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11
Q

The metabolites of 11-desoxycortisol and of desoxycoticosterone are determined by measuring what?

A

Urinary 17-hydroxycorticosteroids or 17-ketogenic steroids

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12
Q

urinary 17-OHCS is used as a

A

Index of pituitary ACTH responsiveness

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13
Q

Metyrapone also supresses the biosynthesis of

A

Aldosterone resulting in mild natiuresis

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14
Q

What are some overdose symptoms of metyrapone?

A

Cardiac arrythmias, hypotension, dehydration, anxiety, confusion, weakness, impairment of conciousness, nausea, vomiting, epigastric pain, and diarrhea

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15
Q

Which is the mineralcorticoid receptoe gene?

A

NR3C2

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16
Q

The mineralcorticoid receptor gene expressed two proteins which are?

A

Alfa MR and Beta MR

17
Q

What is fludocortisone?

A

Synthetic mineralcorticoid with anti-inflammatory activity

18
Q

What is fludocortisone for?

A

Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome

19
Q

What is the mechanism of action of fludocortisone?

A

Binds to the mineralcorticoid receptor

20
Q

What are some adverse effects of fludrocortisone?

A

Cardiac edema, increased blood volume, hypertension, cardiac arrythmias, enlargment of the heart, headaches and weakness of the extremities

21
Q

What is cosyntropin?

A

A synthetic peptide that is identical to the 24- amino acid segment at the N terminal of adrenocorticotropic hormone

22
Q

Cosyntropin is inficated for?

A

Used as a diagnostic agent in the screening of patients presumed to have adrenalcortical insufficiency

23
Q

What is the MOA of cosyntropin?

A

Combines with a specific receptor in the adrenal cell plasma membrane and in patients with normal adrenocortical function

24
Q

What is the target of cosyntropin?

A

ACTH receptor agonist

25
Q

Does cosyntropin exhibit the full corticosteroidogenic activity of natural ACTH?

A

Yes

26
Q

What is the pharmacological effect of cosyntropin?

A

Stimulates the initial reaction involved in the synthesis of adrenal steroids from cholesterol by increasing the quantity of the substrate within the mitochondria

27
Q

What extra adrenal effects natural ACTH and cosyntropin have in common?

A

Melanotropic activity, increased growth hormone secretion, and adipokinetic effect

28
Q

Does cosyntropin significantly increase the plasma cortisol concentration in patients with primary and secondary adrenocortical insufficiency?

A

No

29
Q

What is eplerenone?

A

Aldosterone receptor antagonist similar to spironolactone

30
Q

What are the indications for eplerenone?

A

Improvement of survival of stable patients with left ventricular systolic dysfunction (ejection fraction less than 40%) and clinical evidence of congestive heart failure after an acute myocardial infarction

31
Q

What are other indications of eplerenone?

A

Hypertension

Less than 40% LVEF and chronic heart failure

32
Q

What is the mechanism of action of eplerenone?

A

Binds to the mineral corticoid receptor and thereby blocks the binding of aldosterone

33
Q

What are some adverse effects of eplerenone?

A

Hypotension and hyperkalemia

Pharmacology Block 9 (7 decks)

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