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