pharm gi 10

jaimes quizlet

H2 blockers are very effective what time of day

nighttime acid secretion, raises pH to 4-5

H2 blockers have a moderate impact on?

meal stimulated acid secretion

H2 blockers have little extra benefit when used with

PPI, need to alternate with H2 at night and PPI during the day if using both together

cemetidine interferes with

CYPP450 drugs

these H2 antagonists have very little drug interactions

famotidine and nizatidine

drugs that help reduce gastric activity

antacids
H2 receptor antagonists
PPI
potassium-competitive acid blocker

mucosal protective agents

sucralfate
prostaglandin analogs
colloidal bismuth compounds

aluminum hydroxide causes

constipation

mag. hydroxide causes

diarrhea

sodium bicarb causes

makes CO2 and NaCl and causes fluid overload

calcium carbonate causes

makes CO2 and CaCl, causes constipation, and can replace calcium

in PPIs the prodrug becomes concentrated in the parietal cell more than

1000 fold by henderson hasselbach trapping

PPIs form what kind of bond

covalent disulfide bond w/ H, K, ATPase which is irreversible

PPI dosing?
how long?
when do we use different dosing time?

start QD 30 min prior to 1st meal of the day
only use 8 weeks, taper to avoid acid rebound
use forever for Barret's esophagus or refractory GERD

vonoprazan moa

potassium-competitive acid blocker that suppresses acid secretion by blocking potassium binding to the proton pump, both active and inactive pumps

vonoprazan use:

treatment of H Pylori in adults and erosive esophagitis

vonoprazan is also made as a codrug with

amoxicillin or amoxicillin/clarithromycin

H pylori is a common infection that causes?

dyspepsia, ulcers, cancer

how do we treat H pylori

PPI + bismuth + metronidazole + tetracycline is the 1st line treatment

how does sucralfate work

it makes a thick paste when used with water or gastric acid that will bind to ulcers and erosions for 6 hours

sucralfate use

PUD

adverse sucralfate

constipation

interaction of sucralfate

antacids will make it less effective at binding

bismuth subsalicylate works how

rapidly breaks down, salicylate is absorbed and the bismuth coats the stomach, also has antibacterial effects

use of bismuth

H pylori, traveler's diarrhea

adverse for bismuth

black tongue and stool

contra for bismuth

intestinal blockage

what should we not use bismuth with/interactions

aspirin

why do we not give kids bismuth

reyes syndrome

misoprostol is a

analogue of PGE1 that stimulates gastric production or mucous and bicarb and enhances blood flow

misoprostol use

prevention of NSAID ulcers

misoprostol contra

pregnancy, casues contractions,

how does metoclopramide work

increases esophageal amplitude, increases LES pressure,and enhances gastric emptying

metaclopramide use

GERD, impaired gastric emptying, dyspepsia, vomiting

metoclopramide adverse

dystonic reactions, tardive dyskinesia, extrapyramidal symptoms

metoclopramide contra

pheochromocytoma, seizures,

metoclopramide interactions:

counteracts levodopa
increaseas risk w/ use of phenothiazines-prochlorperazine,chlorpromazine,promethazine

metaclopramide black box

tardive dyskenisia risk

lubiprostone class

chloride channel activator of type 2 channels in the small intestine

lubiprostone SE

gastroparesis, and nausea

lubriprostone use

chronic constipation, IBS, Opioid induced constipation

lubiprostone moa

increases chloride-rich fluid secretion into the small bowel and peristalsis

macrolide antiobiotics like erythromycin work by

stimulating motilin receptors on GI smooth muscles and promote onset of migrating motor complex. We can use azithryomycin if we need to avoid CYP450 interactions

amisulpride use

prevention and treatment of postop NV

amisulpride moa

D2 receptor antagonist which blocks dopamine signaling in the chemoreceptor trigger zone

amisulpride SE

dizziness, blurred vision, confusion, faintness

plecanitide class and moa

guanylate cyclase c agonist-increases cyclic GMP within epithelial cell
increases chloride rich fluid secretion into the small bowel and peristalsis-causing diarrhea

plecanitide use

IBS-c and constipation

plecanitide SE

diarrhea, bloating, abd pain

methylnaltrexone use

opioid induced constipation

methylnaltrexone is given how frequently

SQ every 2 days

methylnaltrexone works how

opiod receptor antagonist at intestinal mu-opioid receptors but won't cross blood brain barrier

naldemedine use

opioid constipation

naldemedine SE

abd pain, ND

naldemedine moa

antagonist at mu opioid receptor in the gut, large polar side chain that minimizes CNS absorption
derivative of naltrexone

naloxegel use

opioid constipation

naloxegel moa

peripheral mu-opioid receptor antagonist

naloxegel is what kind of drug

pegylated derivative of naloxone
pegylation reduces the ability to cross the BBB

alvimopan class

peripheral mu-opioid receptor antagonist

alvimopan use

postop ileus in bowel resection

alvimopan can only be used how long

7 days due to MI risk

prucalopride class and moa

5-HT 4 agonist
increases strength and number of high-amplitude propagating contractions

prucalopride use

constipation

prucalopride SE

abd pain, ND

osmotic laxatives

nonabsorbable salts:
mag oxide-causes hypermagnesesmia in renal dz
sorbitol or lactulose-makes you gassy

stimulant laxatives are aka?
how do they work

cathartics
directly stimulate enteric nervous system

stimulant laxatives are used on

neurologically impaired or bed-bound pts

loperamide(opiod agonist) is aka as?
what will it not do

poor man's methadone
doesn't cross the BBB if used correctly

diphenoxylate(opiod agonist) does not do what?
high levels will?

cross the BBB
high doses lead to opioid dependence

how do we reduce abuse of diphenoxylate

combine it with 0.025mgof atropine

cholestyramine moa

bile salt binding resin

cholestyramine use

hypercholesterolomia, itching from biliary obstruction, bile salt diarrhea

cholestyramine interactions

absorption of fat-soluble vitamins(ADEK)

cholestyramine SE

GI: constipation, bloating, gas

octreotide moa

-inhibits secretion of gastrin, CCK, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, vasoactive intestinal peptide, serotonin
-reduces intestinal fluid secretion and slows GI motility and GB contractions
-reduces portal and splanchic blood flow

dicyclomine is what kind of drug

antimuscarinic

dicyclomine use?
SE

IBS diarrhea
GI obstruction, obstructive uropathy, and glaucoma

dicyclomine interactions

potentiated by amantadine

linaclotide moa

guanylate cyclase c agonist-activates cystic fibrosis transmembrane conductance regulatr ion channel increasing intestinal secretions and making transit faster

linaclotide use?
SE?

IBS-c in adults
may cause diarrhea

rifaximin class and moa

antiobiotic
alters gut flora in a way that reduces IBS symptoms

rifaximin use

IBS-d

tenapanor class and moa

NHE3 inhibitor-sodium hydrogen 3 exchanger inhibitor which increases sodium absorption in the gut increasing fluid secretion and faster transit

tenapanor use?
side effect?

IBS-c in adults
casues diarrhea

ondansetron class and moa

selective 5 HT3 receptor antagonist which causes 5 HT3 receptor blockade in intestinal vagal afferents, as well as central 5 HT3 receptors in the VC and chemoreceptor trigger zones

ondansetron is not effective for

for motion sickness

trimethobenzamide moa

substituted benzmide that is a dopamine receptor blocker with weak antihistamine activity

trimethobenzamide use?
contra

use:NV
contra: premies and infants

trimethobenzamide adverse:
contra:

adverse: parkinson's like symptoms
interacts with alcohol

meclizine moa

H1 blocker w/ little anticholinergic properties w/out sedation effects

meclizine use and contra

use: vertigo and motion sickness
contra:asthma

meclizine SE and interactions

SE:sleepiness
interacts: avoid with alcohol

scopalomine moa

prototypic muscarinic receptor antagonist

scopalomine use and contra

use:motion sickness
contra:angle-closure glaucoma

scopalomine adverse:

blurred vision, increased IOP

scopalomine is available as a

patch for 72 hours

nabilone moa and class

THC analogue-moa not understood

nabilone use and SE

use: treatment of chemotherapy induced nausea and vomiting
SE: dry mouth, sedation, dizziness, orthostatic hypotension,

sulfasalazine use:
contra:

use: ulcerative colitis
contra: sulfa allergy, salicylate allergy

sulfasalazine SE:
interactions:

se: anorexia, HA, rash, hemolytic anemia
interactions: reduces absorption of folic acid and digoxin