Adrenal Steroids Flashcards
What is mifepristone?
A progestational and glucocorticoid hormone antagonist
What are the indications of mifepristone?
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
The anti-progestational activity of mifepristone results from
The competitive interaction with progesterone at progesterone-receptor sites. The compound inhibits the activity of endogenous or exogenous progesterone. The termination of pregnancy results
In the treatment of Cushing’s syndrome, mifepristone blocks the
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
What are some of the adverse effects of mifepristone?
Heavy menstrual bleeding, abdominal pain, uterine cramping, nausea, vomiting and diarrhea
what is metyrapone?
Inhibitor of the enzyme steroid 11-beta monooxygenase
What is metyrapone used for?
As a diagnostic drug for testing the hypothalamic-pituitary ACTH function and ocasionally for Cushing’s disease
What is the mechanism of action of metyrapone?
Inhibits the 11-beta-hydroxylation reaction of the adrenal cortex, reducing cortisol and corticosterone production
What is an adverse effect of metyrapone?
Increase in ACTH production by the pituitary
There is marked increase of what compounds and their metabolites while using metyrapone?
11-desoxycortisol and desoxycorticosterone
The metabolites of 11-desoxycortisol and of desoxycoticosterone are determined by measuring what?
Urinary 17-hydroxycorticosteroids or 17-ketogenic steroids
urinary 17-OHCS is used as a
Index of pituitary ACTH responsiveness
Metyrapone also supresses the biosynthesis of
Aldosterone resulting in mild natiuresis
What are some overdose symptoms of metyrapone?
Cardiac arrythmias, hypotension, dehydration, anxiety, confusion, weakness, impairment of conciousness, nausea, vomiting, epigastric pain, and diarrhea
Which is the mineralcorticoid receptoe gene?
NR3C2
The mineralcorticoid receptor gene expressed two proteins which are?
Alfa MR and Beta MR
What is fludocortisone?
Synthetic mineralcorticoid with anti-inflammatory activity
What is fludocortisone for?
Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome
What is the mechanism of action of fludocortisone?
Binds to the mineralcorticoid receptor
What are some adverse effects of fludrocortisone?
Cardiac edema, increased blood volume, hypertension, cardiac arrythmias, enlargment of the heart, headaches and weakness of the extremities
What is cosyntropin?
A synthetic peptide that is identical to the 24- amino acid segment at the N terminal of adrenocorticotropic hormone
Cosyntropin is inficated for?
Used as a diagnostic agent in the screening of patients presumed to have adrenalcortical insufficiency
What is the MOA of cosyntropin?
Combines with a specific receptor in the adrenal cell plasma membrane and in patients with normal adrenocortical function
What is the target of cosyntropin?
ACTH receptor agonist
