159b Endo Pharm Flashcards Preview

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Flashcards in 159b Endo Pharm Deck (43):
1

Desmopressin - Rx?

ADH analog (much stronger antidiuretic than pressor)

longer half life

Rx -central DI, vWF disease

2

ADH receptors?

GPCR

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

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

3

ADH uses?

central diabetes insipidus (along with desmopressin)

stop bleeding from esophageal varices

hemophilia A and VW disease

4

ADH side effects

vasoconstriction via V1 --> careful in those with CAD

nausea, cramps, headaches, allergies

5

treatment of lithium induced/nephrogenic DI?

Thiazide diuretics (also increase Ca reabsorption)

6

SIADH treatment - mechanism and drug names?

ADH receptor antagonists

conivaptan
tolvaptan (V2>V1)

7

oxytocin - mechanism

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

increases prostaglandins and leukotriences

8

GH - replacement drugs?

somatropin --> identical to GH

somatrem --> longer half life

9

GH: + and - regulators

+ GHRH

- somatostatin, dopamine, GH, IGF-1

10

GH mechanism?

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

increases IGF-1 release from liver which causes most effects

11

oxytocin use

induce labor

pospartum to control uterine hemorrhage

12

oxytocin adeverse effects?

uterine rupture, fetal distress

high doses --> activates ADH receptors

13

GH action

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

14

IGF-1 agonists, use

Mecasermin (meca - sir - min)

mecasermin rinfabate - longer half life

GH resistance deficiencies

15

GH uses?

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

16

effects of octreotide

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

Rx for acromegaly, hormone-secrteting tumors, secratory diarrhea

17

Pegvisomant

modified GH

causes receptor dimerization but blocks activation of JAK-STAT pathway

Rx for acromegaly

18

dopamine agonists to treat GH excess?

bromocriptine
cabergoline

also inhibit prolactin

RX for acromegaly and prolactinoma

19

GH side effects

athralgias, myalgias
peripheral edema
carpal tunnel
increacranial htn
instulin resistance

20

generic names for TH

t4= levothroxine

t3=liothyronine

21

TH mechanism

nuclear receptor --> heterodimers --> regulate genes

unligated receptors acts a repressor at gene

22

IGF-1 agonists adverse effects

hypoglycemia, lipohypertrophy
scoloiosis
dont give to patients with cancer

23

adrenal steroids mechanisms

receptors in cytoplasm

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

24

liver glucocorticoids affects

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

25

glucocorticoid connect tissue affect and fat

decreases fibroblasts

decreases protein synthesis and increases breakdown --> need fuel for gluconeogenesis in liver

increases truncal obesity and fat redistribution

26

kidney affect of steroids

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

27

immune sytem - steroids

decreases Ab production

decrease lymphocytes, cytokines, prostaglandings

28

TH structure

idoinated peptides - from tyrosine residues on TG

29

CNS - steroids

euphoria, depression, psychoses, sleep issues

30

adrenal hyperfunction - rx drugs

somatostatin analogs (octreotide) --I ACTH

glucocorticoid synthesis inhibitors
metyrapone --I 11 hydroxylase
ketoconazole --I multiple steps

glucocorticoid receptor antagonist
mifepristone

31

non-endocrine glucocorticoid use

antiinflammaroty
immunisuppressive
anticancer actions

32

hyperthroidism Rx (drugs), radiation

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

33

methimazole and PTU side effects

PTU - hepatotoxicity so use methimazole

both - agranulocytotis (look for fever --> get blood count)

34

GI - steroids

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

35

stress response - steroids

increases CO, GFR

36

mineralocorticoid action

DCT and collecting duct

37

addison's disease

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

38

CAH causes

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

39

metyrapone

--I 11 hydroxylase

40

mifepristone

glucocorticoid receptor antagonist

41

ketoconazole

blocks glucocorticoid synthesis

42

somatostain

suppresses ACTH

43

glucocorticoid replacement

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

(gluco:mineralo activity)