159b Endo Pharm

Question 1

Desmopressin - Rx?

Answer 1

ADH analog (much stronger antidiuretic than pressor)

longer half life

Rx -central DI, vWF disease

Question 2

ADH receptors?

Answer 2

GPCR

V1 –> PLC –> Ca –> vasoconstriction, CNS side effects

primary V2 –> adenylate cyclase –> increase cAMP –> aquaporin + clotting factors (VIII and vWF)

Question 3

ADH uses?

Answer 3

central diabetes insipidus (along with desmopressin)

stop bleeding from esophageal varices

hemophilia A and VW disease

Question 4

ADH side effects

Answer 4

vasoconstriction via V1 –> careful in those with CAD

nausea, cramps, headaches, allergies

Question 5

treatment of lithium induced/nephrogenic DI?

Answer 5

Thiazide diuretics (also increase Ca reabsorption)

Question 6

SIADH treatment - mechanism and drug names?

Answer 6

ADH receptor antagonists

conivaptan
tolvaptan (V2>V1)

Question 7

oxytocin - mechanism

Answer 7

G-prtn –> PLC –> increases Ca –> contraction
of uterus and myoepithleial

increases prostaglandins and leukotriences

Question 8

GH - replacement drugs?

Answer 8

somatropin –> identical to GH

somatrem –> longer half life

Question 9

GH: + and - regulators

Answer 9

+ GHRH

• somatostatin, dopamine, GH, IGF-1

Question 10

GH mechanism?

Answer 10

tyrosine-kinase linked receptors –> dimerize –> JAK activation –> STAT proteins

increases IGF-1 release from liver which causes most effects

Question 11

oxytocin use

Answer 11

induce labor

pospartum to control uterine hemorrhage

Question 12

oxytocin adeverse effects?

Answer 12

uterine rupture, fetal distress

high doses –> activates ADH receptors

Question 13

GH action

Answer 13

stimulates long bones
increases muscle mass
decreases central fat
reduces sensitivity to insulin

Question 14

IGF-1 agonists, use

Answer 14

Mecasermin (meca - sir - min)

mecasermin rinfabate - longer half life

GH resistance deficiencies

Question 15

GH uses?

Answer 15

kids with deficiency
short stature (turner, prader-willi, etc.)
AIDS wasting

Question 16

effects of octreotide

Answer 16

inhibits GH
inhibits TSH, ACTC, glucagon, gastrin, insulin

Rx for acromegaly, hormone-secrteting tumors, secratory diarrhea

Question 17

Pegvisomant

Answer 17

modified GH

causes receptor dimerization but blocks activation of JAK-STAT pathway

Rx for acromegaly

Question 18

dopamine agonists to treat GH excess?

Answer 18

bromocriptine
cabergoline

also inhibit prolactin

RX for acromegaly and prolactinoma

Question 19

GH side effects

Answer 19

athralgias, myalgias
peripheral edema
carpal tunnel
increacranial htn
instulin resistance

Question 20

generic names for TH

Answer 20

t4= levothroxine

t3=liothyronine

Question 21

TH mechanism

Answer 21

nuclear receptor –> heterodimers –> regulate genes

unligated receptors acts a repressor at gene

Question 22

IGF-1 agonists adverse effects

Answer 22

hypoglycemia, lipohypertrophy
scoloiosis
dont give to patients with cancer

Question 23

adrenal steroids mechanisms

Answer 23

receptors in cytoplasm

release hsp90 –> exposes dna binding domain and translocation to nucleus

Question 24

liver glucocorticoids affects

Answer 24

conservation of glucose –> promote glycogen synthesis (anabolic) and gluconeogenesis to protect brain

Question 25

glucocorticoid connect tissue affect and fat

Answer 25

decreases fibroblasts decreases protein synthesis and increases breakdown --> need fuel for gluconeogenesis in liver increases truncal obesity and fat redistribution

Question 26

kidney affect of steroids

Answer 26

increases Ca excretion, mineral corticoid activity --> K and H excretion, H retention

Question 27

immune sytem - steroids

Answer 27

decreases Ab production decrease lymphocytes, cytokines, prostaglandings

Question 28

TH structure

Answer 28

idoinated peptides - from tyrosine residues on TG

Question 29

CNS - steroids

Answer 29

euphoria, depression, psychoses, sleep issues

Question 30

adrenal hyperfunction - rx drugs

Answer 30

somatostatin analogs (octreotide) --I ACTH glucocorticoid synthesis inhibitors metyrapone --I 11 hydroxylase ketoconazole --I multiple steps glucocorticoid receptor antagonist mifepristone

Question 31

non-endocrine glucocorticoid use

Answer 31

antiinflammaroty immunisuppressive anticancer actions

Question 32

hyperthroidism Rx (drugs), radiation

Answer 32

thionamide durgs propylthiouracil (PTU) --I TPO and 5'-deidonase methimazole --I TPO I131--> beta particles cause necrosis of cells; dont use in pregnant or nursing women B-blockers (stops tachycardia, htn, a fib) propranolol also weakly --I t4-->t3 KI --> inhibits hormone release, TPO, prevents radioactive uptake of I to prevent throid cancer

Question 33

methimazole and PTU side effects

Answer 33

PTU - hepatotoxicity so use methimazole both - agranulocytotis (look for fever --> get blood count)

Question 34

GI - steroids

Answer 34

thinning of mucus, increase pepsin and acid secretion, decrease Ca absoprtion

Question 35

stress response - steroids

Answer 35

increases CO, GFR

Question 36

mineralocorticoid action

Answer 36

DCT and collecting duct

Question 37

addison's disease

Answer 37

adrenal doesn't produce steroids--> weakness and hypotension

Question 38

CAH causes

Answer 38

deficient hydroxylases --> low glucocoritcoids --> no feedback --> high ACTH

Question 39

metyrapone

Answer 39

--I 11 hydroxylase

Question 40

mifepristone

Answer 40

glucocorticoid receptor antagonist

Question 41

ketoconazole

Answer 41

blocks glucocorticoid synthesis

Question 42

somatostain

Answer 42

suppresses ACTH

Question 43

glucocorticoid replacement

Answer 43

cortisol/hydrocortisone (100:1) prednisone (400:0.8) dexamethasone (2500:0) (gluco:mineralo activity)