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60 Cards in this Set

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  • Back
Goals of drugs used in acid-peptic disease
Reduce intragastric acidity by manipulating systems controlling hydrogen acid secretion, promote mucosal defense, eradicated H. pylori
% of patients with duodenal ulcers due to H. pylori
80%
How do antacids work
weak bases that neutralize stomach acid by reacting with protons in the lumen of the gut and may also stimulate the protective functions of the gastric mucosa
Two popular antacids not absorbed in the bowel
magnesium hydroxide and aluminum hydroxide
Which has laxative effect?
magnesium hydroxide
Which has constipation effect?
aluminum hydroxide
Two weak bases that are absorbed from the gut
calcium carbonate and sodium bicarbonate
4 Examples of H2-receptor antagonists
cimetidine
ranitidine
famotidine
nizatidine
H2-receptor antagonists are effective in the treatment of?
GERD, PUD, nonulcer dyspepsia and in the prevention of stress-related gastritis
5 Examples of proton pump inhibitors?
omeprazole
esomeprazole
lansoprazole
pantoprazole
rabeprazole
MOA of proton pump inhibitors
undergo conversion to compounds that irreversibly inactivate the parietal cell H+/K+ ATPase (in parietal cell canaliculi)
first step of proton pump inhibitor action
lipophilic weak bases that diffuse into the parietal cell canaliculi, where they become protonated and concentrated more than 1000-fold
How do oral formulations avoid acid inactivation in the stomach?
enteric coating
where are proton pump inhibitors absorbed and metabolized?
absorbed- intestine
metabolized- liver
half life of proton-pump inhibitors
1-2 hours
duration of action of proton pump inhibitors
24 hours
adverse effects of proton pump inhibitors
diarrhea, abdominal pain, headache
chronic treatment with PPIs
hypergastrinemia
Sucralfate
aluminum sucrose sulfate
small, poorly soluble molecule
Where does sucralfate polymerize?
acid environment of stomach
MOA of sucralfate
binds to injured tissue and forms a protective coating over ulcer beds
misoprostol
analog of PGE1
MOA of misoprostol
increases mucosal protection and inhibits acid secretion
colloidal bismuth
formation of a protective coating on ulcerated tissue, stimulation of mucosal protective mechanisms, direct antimicrobial effects, sequestration of enterotoxins
Purpose of bismuth subsalicylate in infectious diarrhea
reduces stool frequency and liquidity
Antibiotic use in acid-peptic disease
eradication of H pylori
eradication of H pylori (PPI plus what?)
clarithromycin and amoxicillin
Use of drugs that stimulate upper gastrointestinal motility?
gastroparesis and postsurgical gastric emptying delay
treatment of hospitalized patients with acute large bowel distention
acetylcholinesterase inhibitor neostigmine
dopamine function in the enteric nervous system
inhibitor by inhibiting cholinergic stimulation of smooth muscle contraction
most effective antidiarrheal drugs
opiods and derivatives of opiods that have maximal antidiarrheal and minimal CNS effect
two meperidine analogs with weak analgesic effects
diphenoxylate and loperamide
how is diphenoxylate formulated to reduce the likelihood of abuse
formulated with antimuscarinic alkaloids
a naturally occurring hydrated magnesium alumninum silcate
kaolin
pectin
indigestible carbohydrate derived from apples
MOA of kaolin + pectin
absorbs bacterial toxins and fluid, resulting in decreased stool quantity
two anticholinergic drugs in IBS used as antispasmodics to relieve abdominal pain
dicyclomine and hyoscyamine
5-HT3 antagonist for treatment of women with IBS w/ diarrhea
alosetron
why is the use of alosetron restricted?
can cause constipation, including rare complications of severe constipation that require hospitalization or surgery, and rare cases of ischemic colitis
H1 histamine-blocking activity drugs useful as antiemetics
diphenydramine and several phenothiazines
antimuscarinic drug with antiemetic action
scopolamine
corticosteroid drug with antiemetic action
dexamethasone
cannabinoid receptor agonist with antiemetic action
dronabinol and nabilone
5-HT3 antagonists
ondansetron, granisetron, dolasetron, palonosetron
antagonist of neurokinin 1 receptor, used as an antiemetic
aprepitant
NK1 receptor location and mechanism of activation
area postrema of CNA and activated by substance P and other tachykinins
Tx of aprepitant
fatigue, dizziness, and diarrhea
how does aprepitant participate in other drug interactions
substrate and inhibitor of CYP3A4
largest group of drugs used in IBD
Aminosalicylates
chemical compound common to aminosalicylates
5-aminosalicylic acid
generic name for 5-ASA
mesalamine
site of absorption of mesalamine
small intestine
aminosalicylates with 5-ASA bound by an azo bone to an inert compound, another 5-ASA molecule or sulfapyridine
balsalazide, olsalazine, sulfasalazine
why does sulfalazine have a higher incidence of adverse effects
systemic absorption of sulfapyridine moiety
Tx of sulfsalazine
nausea, GI upset, headaches, arthralgias, myalgias, bone marrow suppression, malaise, severe hypersensitivity reactions
other groups of drugs used to treat UC and Crohns
antibiotics, glucocorticoids, immunosuppressive antimetabolites, anti-TNF drugs
Natalizumab
humanized monoclonal antibody that blocks integrins on circulating leukocytes
association of natalizumab limiting its use
multi-focal leukoencephalopathy; only used in severe refractory Crohns diseas
pancreatic lipase replacement
pancrelipase, pancreatin from pigs
protection from digestion of pancreatic lipase replacement
taken as enteric-coated capsules