NeuroEndocrine/Adrenal/Thyroid Flashcards
Cabergoline
MOA:
D2 dopamine receptor agonist
Clinical uses:
hyperprolactinemia, Parkinson’s
toxicity:
GI disturbances, orthostatic hypotension, sleep disturbances
extra:
once weekly oral dopamine agonist, very effective, 90% achievement of normal prolactin and 85% impact on tumor reduction
Octreotide
MOA:
somatostatin receptor agonist
clinical uses:
growth hormone secreting tumors (acromegaly, gigantism), vasoactive intestinal peptide tumors
Toxicity:
GI disturbances, hypothyroidism, gall stones, CVS effects
Extra info:
synthetic somatostatin analogue
Somatropin
MOA:
growth hormone receptor agonist
Clinical uses:
GH deficiency, HIV wasting, short bowel syndrome
Toxicity:
edema, mylagia, arthralgia
Extra info;
recombinant form of human growth hormone
Pegvisomant
MOA:
growth hormone receptor antagonist
Clinical uses:
acromegaly
Toxicity:
liver toxicity, nausea
Extra info:
used when somatostatin analogues are unsuccessful, or pituitary tumor unresponsive to radiation or surgery
Mifepristone
MOA:
competitive progesterone receptor antagonist
Clinical uses:
Cushing’s syndrome, abortion
Toxicity:
vaginal bleeding, abdominal pain, GI disturbances, headache
extra info:
known as RU486
Metyrapone
MOA:
steroid 11B-hydroxylase inhibitor
Clinical uses:
Cushing’s syndrome, diagnosis of adrenal insufficiency
Toxicity:
GI disturbances, acute adrenocortical insufficiency
Extra info:
blocks cortisol synthesis, which stimulates ACTH secretion
Ketoconazole
MOA:
antisteroidogenic/ adrenolytic via inhibition of CYP11A1/CYP11B1
Clinical uses :
severe hypercortisolism
Toxicity:
side effects associated with decreased cortisol (headache, sedation, fatigue, nausea) and testosterone (gynecomastia, impotence) production
Extra info:
numerous DDIs via inhibition of CYP450 3A4, 1A2 and 2C9
Hydrocortisone
MOA
glucocorticoid receptor agonist
Clinical uses
inflammation reactions, organ transplantation, hematologic cancers
Toxicity:
adrenal suppression, growth inhibition, muscle wasting, osteoperosis, salt retention, glucose intolerance, behavioural changes
Extra info: Short acting (~12 h)
Prednisone
MOA
glucocorticoid receptor agonist
Clinical uses
inflammation reactions, organ transplantation, hematologic cancers
Toxicity:
adrenal suppression, growth inhibition, muscle wasting, osteoperosis, salt retention, glucose intolerance, behavioural changes
Extra info: Short acting (12-36 h)
Methlypredinsolone
MOA
glucocorticoid receptor agonist
Clinical uses
inflammation reactions, organ transplantation, hematologic cancers
Toxicity:
adrenal suppression, growth inhibition, muscle wasting, osteoperosis, salt retention, glucose intolerance, behavioural changes
Extra info: Short acting (12-36 h)
Dexamethasone
MOA
glucocorticoid receptor agonist
Clinical uses
inflammation reactions, organ transplantation, hematologic cancers
Toxicity:
adrenal suppression, growth inhibition, muscle wasting, osteoperosis, salt retention, glucose intolerance, behavioural changes
Extra info: Short acting (>48 h)
Fludrocortisone
MOA
glucocorticoid receptor agonist
Clinical uses Adrenal insufficiency (addison's disease)
Toxicity:
Na and H20 retention, CHF, glucocorticoid effects
Extra info:
long duration of action; strong mineralcorticoid activity, moderate glucocorticoid activity
Leveothyroxine (T4)
MOA:
synthetic thyroid T4 hormone, activates nuclear receptors
Clinical uses: hypothyroidism
Toxicity:
thyrotoxicosis symptoms
Extra info:
T4 converted to T3 in target cells
Liothyronine (T3)
MOA:
synthetic thyroid T3 hormone, activates nuclear receptors
Clinical uses hypothyroidism
Toxicitiy:
thyrotoxicosis symptoms
Extra info:
10x more potent than T4
Potassium iodide (KI(
MOA:
inhibits iodine organification and hormone release
Clinical uses:
reduces size and vascularity of thyroid gland, preparation for surgical thyroidectomy
Toxicity:
minimal
Extra info:
oral, onset of activity in 2-7 d