Gi Pharmacology

Front 1

Drugs for acid related disorders

Back 1

H2RA, PPI, Prostaglandin E analogue, Cytoprotective agents, anti H. pylori regimens

Front 2

Drugs for nausea/vomiting

Back 2

5HT antagonist, histamine H1 antagonist, Dopaminergic D2 antagonist, Benzodiazepines, corticosteroids, cannabinoids

Front 3

drugs for variceal hemorrhage

Back 3

somatostatin, octreotide, vasopressin

Front 4

list H2RAs (4)

Back 4

cemitidine (tagamet), ranitidine (Zantac), famotidine (pepcid), nizatidine (axid)

Front 5

H2RA MOA

Back 5

reversible, competitive inhibition of histamine-2 receptor

Front 6

which H2RA interferes with Cyt P450?

Back 6

cimetidine

Front 7

rare, serious side effects of H2RA?

Back 7

leukopenia, thrombocytopenia, anemia, bradycardia, hypotension

Front 8

clinical uses of H2RAs

Back 8

GERD, PUD, non-ulcer dyspepsia, stress gastritis prevention

Front 9

PPI agents available

Back 9

omeprazole (Prilosec), lansoprazole (Prevacid), rabeprazole (Aciphex), pantoprazole (Protonix), esomeprazole (Nexium)

Front 10

PPI MOA

Back 10

prodrugs, irreversibly bind H+/K+ atpase, concentrated 1000x in acidic canaliculi

Front 11

PPI pkinetics

Back 11

short serum t 1/2 ~1.5 hrs, but duration of action is 24h, takes 3-4 days before full potential is reached

Front 12

which PPI inhibits Cyt P450?

Back 12

omeprazole (Prilosec), lansoprazole (Prevacid), rabeprazole (Aciphex), pantoprazole (Protonix), esomeprazole (Nexium)

Front 13

Clinical uses of PPIs

Back 13

GERD, PUD, non-ulcer dyspepsia, stress gastritis prevention, Zollinger Ellison Sydrome

Front 14

what is the prostaglandin E analogue?

Back 14

misoprostol (Cytotec)

Front 15

how does misoprostol work?

Back 15

stims mucus and bicarb secretion and enhances mucosal blood flow

Front 16

problem with misoprostol?

Back 16

lots of side affects: diarrhea, uterine bleeding, abortion

Front 17

prokinetic agents?

Back 17

meoclopramide (Reglan), bethanechol, macrolides (erythromycin)

Front 18

metoclopramide MOA

Back 18

stims release of ach from myenteric neurons, increases LES pressure and enhances gastric emptying

Front 19

metoclopramide Side Effects:

Back 19

neuropsychiatric side effects in 10-20%, EPS

Front 20

uses of metoclopramide

Back 20

Gastroparesis, anti-emetic, GERD, non-ulcer dyspepsia

Front 21

where is the brainstem vomiting center?

Back 21

lateral medullary reticular formation

Front 22

what provides input into brainstem vomiting center?

Back 22

CTZ, vestibular system, pharynx, GI tract, cerebral cortex

Front 23

5HT3 serotonin antagonists

Back 23

ondansetron (zofran), granisetron (Kytril), dolasetron

Front 24

five types of laxatives

Back 24

bulk forming, stool surfactant, osmotics, PEGs, Stimulants

Front 25

what is a bulk forming laxative?

Back 25

indigestible substance that swells w/ water. Fiber: metamucil

Front 26

what is a stool surfactant agent?

Back 26

Colace: acts as detergent to soften stool

Front 27

what is an osmotic laxative?

Back 27

non-absorbable osmotically active agent: milk of magnesia

Front 28

list some stimulant laxatives:

Back 28

bisacodyl (ducolax), phenolphthalein (ExLax)

Front 29

list 3 anti-diarrheal agents

Back 29

loperamide (Immodium), diphenoxylate, octreotide

Front 30

mechanism of loperamide?

Back 30

slows motility through direct action on intestinal nerves

Front 31

diphenoxylate mechanism?

Back 31

opioid agonist

Front 32

Octreotide mechanism?

Back 32

synthetic peptide, mimics somatostatin

Front 33

Drugs used for IBS?

Back 33

antispasmodics and antidepressants, alosetron and tegaserod

Front 34

list some antispasmodics?

Back 34

Bentyl (dicylomine HCl), Levsin (hyocyamine sulfate)

Front 35

Mech of alosetron?

Back 35

selective 5ht3 antagonist, decreases visceral sensitivity

Front 36

mech of Tegaserod?

Back 36

5HT4 agonist, prokinetic effect

Front 37

5-ASA drugs

Back 37

pentasa, asacol, rowasa

Front 38

5-ASA mech?

Back 38

inhibits NFkB, transcription factor for pro-inflammatory cytokines

Front 39

key to 5-ASA delivery/bioavailability?

Back 39

works topically, so need to deliver high concentration

Front 40

when to use 5-ASA?

Back 40

first line against UC and CD

Front 41

which glucocorticoids used for IBD?

Back 41

prednisone and prednisolone

Front 42

glucorticoid MOA?

Back 42

anti-inflammatory and immunosuppresive: block TNF-a, IL-1, IL-8, NOS, phospholipase A2, cox2

Front 43

side effects of glucocorticoids?

Back 43

petechiae, bruising, striae, moon face, acne, HTN, ifxn

Front 44

how do you dose glucocorticoids?

Back 44

use high dose to induce remission, after stabilization, slowly taper dose

Front 45

Azathioprine MOA

Back 45

intracellular accumulation of 6-thioguanine tns inhibts pathways of purine synthesis/repair, causing inhibition of cell division

Front 46

p-kinetics of AZA/6MP

Back 46

AZA quickly metabolized to 6MP, 6MP inactivated by TPMT, converted to active 6TG by HGPRT

Front 47

problem with giving AZA?

Back 47

if px has TPMT deficiency, get toxic levels of drug

Front 48

adverse effects of AZA:

Back 48

allergic, dose related: BMS, anemia, leukocytopenia, thrombocytopenia

Front 49

methotrexate MOA

Back 49

inhibits DHFR, which is critical for production of thymidylate and purines

Front 50

MTX toxicities

Back 50

BMS, GI ulcer, stomatitis, alopecia, rescue with tetrahydrofolate

Front 51

which IBD benefits from MTX?

Back 51

CD, not UC

Front 52

what is infliximab?

Back 52

monoclonal anti-TNFa

Front 53

which IBD benefits from infliximab?

Back 53

UC and CD

Front 54

Drugs for IBD?

Back 54

5-ASA, prednisone, AZA, MTX, infliximab, abx, cyclosporine