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Upper GI
N/A
84
Pharmacology
Professional
04/27/2011

Additional Pharmacology Flashcards

 


 

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Term
aggressive factors
Definition
acid
pepsin
H. pylori
Term
protective factors
Definition
bicarbonate and mucus secretion
prostaglandin formation
Term
__________ and ________ inhibit prostaglandin synthesis
Definition
aspirin; NSAIDs
Term
Which COX-2 selective inhibitor has a lesser incidence of causing PUD?
Definition
celecoxib (Celebrex)
Term
risk factors for PUD
Definition
aspirin, NSAID use
alcohol (in excess)
smoking
H. pylori infection
Term
overall goals of therapeutic strategies
Definition
relief of symptoms
healing of ulcers
prevention of recurrence
prevention of complications
reduce aggressive factors
increase protective factors
Term
PPI mechanism of action
Definition
inhibit H+,K+,-ATPase proton pump by covalently binding to it
Term
PPIs _________ modify sulfhydryl groups on the proton pump which __________ inactivates H+ secretion.
Definition
covalently; irreversibly
Term
Why does a PPI need to be taken 30-60 min before a meal?
Definition
works best on actively secreting pumps
Term
PPIs have a _________ mechanism.
Definition
prodrug
Term
Enteric coating--release of prodrug in intestine

at neutral pH of intestine, prodrug is chemically stable, lipid soluble, and devoid of inhibitory activity

neutral weak base absorbed and carried by blood stream to parietal cells in stomach, diffuse into secretory canaliculi, acid pH causes protonation and trapping of drug near proton pump
Definition
Term
Which PPI may reduce the metabolism of phenytoin, warfarin, and diazepam?
Definition
omeprazole
Term
omeprazole (Prilosec)
Definition
PPI
Term
lansoprazole (Prevacid)
Definition
PPI
Term
rabeprazole (Achiphex)
Definition
PPI
Term
pantoprazole (Protonix)
Definition
PPI
Term
esomeprazole (Nexium)
Definition
PPI
Term
dexlansoprazole (Kapidex, Dexilant)
Definition
PPI
Term
cimetidine (Tagamet)
Definition
H2 blocker
Term
ranitidine (Zantac)
Definition
H2 blocker
Term
famotidine (Pepcid)
Definition
H2 blocker
Term
nizatidine (Axid)
Definition
H2 blocker
Term
Why are PPIs considered better drugs than H2 blockers?
Definition
H2 blocker significantly reduces the amount of acid throughout the day, but PPI keeps acid almost flat-lined.
Term
H2 blocker uses
Definition
duodenal and gastric ulcers
GERD
stress ulcers
hypersecretory states
preanesthetic to reduce the danger of aspiration pneumonitis
Term
Histamine activates ______________________ on parietal cells and stimulates ____________ activity and acid secretion into the lumen.
Definition
H2 subtype of receptor; H+,K+,-ATPase
Term
H2 blocker mechanism of action
Definition
competitively inhibits histamine-mediated acid secretion

blunts the response to gastrin and ACh
Term
Classic antihistamines, H1 blockers, do/do not inhibit acid secretion.
Definition
do not
Term
H2 blockers inhibit ______, _______, and ________ acid secretion.
Definition
basal; food-stimulated; nocturnal
Term
H2 blockers reduce both...
Definition
volume and H+ concentration of gastric secretions
Term
H2 blockers are equally ___________ but differ in ________.
Definition
efficacious; potency
Term
Which H2 blocker inhibits the activity of CYP450?
Definition
cimetidine
Term
If drug interactions need to be avoided, which H2 blocker should not be chosen?
Definition
cimetidine
Term
standard treatment for PUD not associated with H. pylori
Definition
PPI--1 hr before first and second meal for 2 months

H2 blocker--at bedtime (if breakthrough symptoms)

reduce PPI to once daily until all symptoms are gone
Term
triple therapy for H. pylori
Definition
PPI (BID)
clarithromycin (BID) (or metronidazole)
amoxicillin (BID) (or metronidazole)

14 days
Term
quadruple therapy for H. pylori
Definition
PPI (BID)
tetracycline (QID)
metronidazole (TID/QID)
pepto-bismol (QID)

14 days
Term
Prevpac
Definition
Prevacid (lansoprazole) PPI
clarythromycin
amoxicillin

combo drug used to treat H. pylori
Term
advantages/disadvantages of quadruple therapy for H. pylori
Definition
less expensive, but compliance issues
Term
Why do you need to wait one week after stopping PPI to retest for H. pylori?
Definition
PPI can cause false positive on stool antigen test
Term
What should be done for a patient taking a PPI for GERD if they are planning on traveling out of the country?
Definition
cut the dose in half (one every other day)
Term
antacid therapeutic use
Definition
simple dyspepsia
adjuncts to primary therapy with PPIs or H2 blockers
primary therapy in uncomplicated GERD
Term
antacid mechanism of action
Definition
weak bases that chemically neutralize acid

goal is to raise gastric pH above 4
Term
aluminum hydroxide
Definition
antacid
Term
magnesium hydroxide
Definition
antacid
Term
calcium carbonate
Definition
antacid
Term
sodium bicarbonate
Definition
antacid
Term
simethicone
Definition
antacid
Term
gaviscon
Definition
antacid
Term
major side effect of aluminum hydroxide
Definition
constipation
Term
major side effect of magnesium hydroxide
Definition
diarrhea
Term
Why are combinations of aluminum and magnesium hydroxides the most popular antacids?
Definition
combo minimizes disturbance of bowel motility
Term
dosing for antacids
Definition
1 and 3 hrs after a meal and at bedtime
Term
adverse effects of antacids
Definition
changes in bowel motility
alkalosis
Term
drug interactions with antacids
Definition
significant effects on the absorption of other drugs

do not take within 1-2 hrs of other drugs!
Term
What can occur with discontinuation of antacids?
Definition
rebound acidity
Term
mechanism of action for pepto-bismol
Definition
-enhances secretion of mucus and HCO3-
-inhibits pepsin activity
-chelates with proteins at the base of ulcers and forms a protective barrier against acid and pepsin
-may inhibit H. pylori
Term
uses of pepto-bismol
Definition
effective adjunct for treatment and prophylaxis of duodenal and gastric ulcers, GERD, and diarrhea
Term
pepto-bismol side effects
Definition
black tarry stools
blackened tongue (with long-term use)
Term
sucralfate (Carafate)
Definition
cytoprotective agent
Term
mechanism of action for sucralfate
Definition
forms sticky, viscous gel that adheres to gastric epithelial cells protecting them from acid and pepsin
Term
dosing for sucralfate
Definition
1 hr before meals and at bedtime promotes healing
Term
misoprostol (Cytotec)
Definition
cytoprotective agent
Term
mechanism of action for misoprotol
Definition
slowly metabolized analog of PGE1
stimulates mucus and HCO3- production
Term
Misoprostol is primarily used for patients who must use ________.
Definition
NSAIDs
Term
Misoprostol causes _________ in 30% of patients.
Definition
diarrhea
Term
misoprostol contraindications
Definition
pregnancy (aborts fetus)
Term
ondansetron (Zofran)
Definition
5-HT3 antagonist
antiemetic
Term
5-HT3 antagonists are most effective when combined with...
Definition
corticosteroid therapy (short-term)--dexamethasone
Term
aprepitant (Emend)
Definition
neurokinin 1 receptor antagonist
antiemetic
Term
primary use of aprepitant
Definition
combo with 5-HT3 antagonist and corticosteroid for prevention of chemotherapy induced nausea and vomiting
Term
aprepitant side effects
Definition
fatigue
dizziness
diarrhea
Term
metoclopramide (Reglan)
Definition
D2 antagonist
antiemetic and promotility agent
Term
Which D2 antagonist is also a weak 5-HT3 antagonist?
Definition
metoclopramide
Term
promethazine (Phenergan)
Definition
H1 blocker
antiemetic
Term
dimenhydrinate (Dramamine)
Definition
H1 blocker
antiemetic
Term
scopolamine
Definition
antimuscarinic agent
patch for motion sickness
Term
dronabinol (Marinol)
Definition
cannabinoid
antiemetic
Term
dronabinol uses
Definition
chemotherapy-induced nausea and vomiting
appetite stimulant
Term
dronabinol side effects
Definition
euphoria
dysphoria
sedation
hallucinations
Term
indications for antiemetics
Definition
motion sickness and vertigo
postoperative recovery
pregnancy
cancer chemotherapy
migraine
Term
metoclopramide mechanism of action as promotility agent
Definition
increases esophageal peristalsis
increases LES pressure
promotes gastric emptying

no effect on small intestine or colon
Term
metoclopramide side effects
Definition
hyperprolactinemia
anxiety
depression
tardive dyskinesia (typically limited to 2 week course)
Term
erythromycin
Definition
macrolide antibiotic that promotes motility (acts on motilin receptor)
Term
Erythromycin is used for __________, but tolerance develops.
Definition
gastroparesis
Term
Why are macrolide antibiotics used in acute GI hemorrhage?
Definition
promote emptying of gastric blood before endoscopy
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