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46 Cards in this Set

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What two properties of antacids make them useful for alleviating symptoms of the stomach associated with increase acid?

They are weak bases that react with HCl to increase the pH. They also may stimulate prostaglandin synthesis to increase the mucosal barrier (remember, NSAIDs inhibit prostaglandin synthesis)
What are some antacids?
Aluminum hydroxide, magnesium hydroxide, calcium carbonate, and sodium bicarbonate.
Magnesium hydroxide is associated with?
A strong laxative effect, causing diarrhea.

First, Mg2+ is poorly absorbed from the intestinal tract, so it draws water from the surrounding tissue by osmosis. Not only does this increase in water content soften the feces, it also increases the volume of feces in the intestine (intraluminal volume) which naturally stimulates intestinal motility.
Aluminum hydroxide is associated with?
Constipation.
What is sucralfate good for? What should it not be with and why?
Promoting the healing of duodenal ulcers by either up regulating prostaglandin synthesis (enhances the mucosal barrier) or forming a protective coating over ulcer beds. It requires an acid environment to become active; therefore, do not take with antacids, H2 blockers, or proton pump inhibitors.
What are some H2 receptor blockers?
Cimetidine, ranitidine, famotidine, and nizatidine
What is the MOA of H2 receptor blockers?
Blocks the binding of histamine to H2 receptor present on parietal cells. This leads to decrease activity of H+/K+ pump and decrease gastric acid.
What are H2 receptor blockers useful for?
GERD, peptic ulcer, and nonulcer dyspepsia and stress related gastritis.
What is a SE of H2 receptor blockers?
Gynecomastia
What are some proton pump inhibitors?
Omeprazole, lansoprazole, pantoprazole, and rabeprazole
What is the MOA of a proton pump inhibitor?
Binds directly to H+/K+ ATPase pump to suppress gastric acid secretion.
Proton pump inhibitors are more effective than H2 receptor blockers and equally effective with?
More effective with GERD and peptic ulcers. Equally effective for nonulcer dyspepsia and prevention of stress-related mucosal bleeding. PPI are also useful for Zollinger-Ellison syndrome.
SE of PPI?
Infrequently diarrhea, abdominal pain, and headache. Chronic treatment with hypergastrinemia.

Decrease absorption of B12, increase risk of respiratory and enteric infection.
What is misoprostol, and what is it useful for?
It is a prostaglandin (PGE1) analog. It increases mucosal protection and inhibits acid secretion. Also, increases uterine contractions. It is effective in reducing risk of ulcers with users of NSAIDs
SE of misoprostol
Can cause abortifacient in PTs treated with gastric ulcers.
What is bismuth (Pepto-Bismol) used for?
Formation of protectiving coating on ulcerated tissue, stimulation of mucosal protective mechanisms, direct antimicrobial effects, sequestration of enterotoxins.

Used to treat traveler's diarrhea to decrease frequency and liquidity.
What happens to the color of the stool with bismuth therapy?
Turns it black
What can neostigmine be useful for in relationship with GI disorder?
It is an acetylcholinesterase inhibitor and used for treatment of hospitalized PTs with acute large bowel distention to stimulate motility for gastroparesis and post surgical gastric emptying delay.
What function does dopamine serve in the enteric nervous system?
Inhibiting cholinergic stimulation of smooth muscle contraction.

Also, D2 activation leads to vomiting reflex pathway.
What is the MOA of metoclopramide and prochlorperazine?
They are D2 dopamine receptor antagonist.
What is the purpose of using metoclopramide and prochlorperazine?
By blocking dopamine, they can promote gastrointestinal motility and preventing emesis (not as efficient as ondansetron) after surgical anesthesia or chemotherapy.
SE of Metoclopramide and prochlorperazine?
Chronic use, can lead to parkinsonism, extrapyramidal effects, and hyperprolactinemia.
What is the MOA of Ondansetron and what is its purpose?

And its SE
Blocks 5-HT3 receptors. When 5-HT3 are activated in the GI tract by release of serotonin from damaged enterochromaffin cells, the signal is sent via the vagus nerve to the brainstem to induce vomiting. My using ondansetron, vomiting is decrease in PTs receiving chemotherapy.

May slow colonic transit or constipation.
Two H1 receptor antagonist and their function?
Promethazine and diphenhydramine. H1 receptors are found within the GI tract. By blocking these receptors, GI tract motility is decreased.

They are mainly a first generation antihistamine mainly used to treat allergies
PT with insulin-dependent diabetes of 40 years complains of severe bloating and abdominal distress, especially after meals. Evaluation is consistent with diabetic gastroparesis. What is the recommended prokinetic drug (motility inducer)?
Metoclopramide

Metoclopramide has as it is primarily used to treat gastric paresis (eg., in diabetes). It also helps as antiemetic.

Note: ondansetron is a stronger preventer of emesis.
A PT taking verapamil for hypertension and angina has constipation. What drug is an osmotic laxative that can be used?
Magnesium hydroxide. Verapamil blocks calcium channels (also present in smooth muscle), therefore, can cause constipation. By increasing bulk of the stool, magnesium hydroxide can help stimulate contraction.
Which drug accumulates in parietal cell canaliculi and undergoes conversion to a derivative that irreversibly inhibits H+/K+ ATPase?
Esomeprazole, a PPI. Also, omeprazole, lansoprazole, rabeprazole, pantoprazole.
How do laxatives cause BM?
By irritating or stimulation the bowel wall; bulk-forming to induce a reflex contraction; softening on hard or impacted stool; and lubricating effect.
What two drugs can inhibit the formation of cholesterol gallstones and primary biliary cirrhosis?
Ursodiol and Chenodiol

They inhibit cholesterol secretion into the bile.
What is the MOA of Ursodiol?
Inhibits HMG-CoA reductase; decreases intestinal reabsorption of cholesterol; and inhibits secretion of cholesterol into bile.
What drug is most likely to be useful in the treatment of inflammatory bowel disease? And its MOA?
Mesalamine (an aminosalicylates--5-ASA)

It inhibits eicosanoid inflammatory mediators (prostaglandin, prostacyclins, thromboxanes, leukotrienes) by inhibiting of COX.
What drug is most appropriate for the treatment of a PT with Zollinger-Ellison syndrome resulting from gastrinoma?
Gastrinomas increase HCl secretion producing GI ulceration and malabsorption. A PPI (e.g., omeprazole) would be effective. H2 antagonists result in suboptimal acid suppression.
A woman with IBS with diarrhea is not responsive to conventional therapies. Despite the small risk of severe constipation and ischemic colitis, the PT decides to begin therapy with alosetron, a drug that?
Is a 5-HT3 receptor antagonist. Serotonin plays a major regulatory role in the enteric nervous system.

While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products.
Feeling an attack of diarrhea is imminent, what drug can be purchase at a drugstore without a prescription even though it is chemically related to opioid-analgesic meperidine?
Loperamide (e.g., Imodium and Pepto). Diphenoxylate is similar to loperamide but requires a Rxn. Aluminum hydroxide is constipating, but not related to meperidine.
A PT with duodenal ulcer was treated with combination of duodenal ulcer was treated with a combination of drugs to heal mucosal damage and eradicate H. pylori. What is an antibacterial drug use for this purpose?
Clarithromycin, amoxicillin, tetracycline, and metronidazole. Bismuth also has antibacterial action.
A PT is receiving highly emetogenic chemotherapy for metastatic carcinoma. To prevent chemotherapy-induced nausea and vomiting, she is likely treated with?
Ondansetron, a 5-HT3 receptor antagonist is highly effective at preventing chemotherapy-induced nausea and vomiting.

It is more effective than metoclopramide and prochlorperazine for antiemetic
Management of steatorrhea is best accomplished with?
Pancrelipase or pancreatin (pancreatic lipase). Steatorrhea occurs with decreased fat absorption.
A small molecule that polymerizes in stomach acid and coats the ulcer bed, resulting in accelerated healing and reduction of symptoms.
Sucralfate
What is ann antiemetic and gastroprokinetic agent that causes extrapyramidal dysfunction, including tardive dyskinesia with chronic administration.
Metoclopramide (antagonist of dopamine receptors in the CNS)
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
H2 blocker that causes the most interactions with other drugs
Cimetidine
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
5HT-3 antagonist used in chemotherapeutic induced emesis
Ondansetron, alosetron, granisetron, and dolasetron (last three aren't in the mini-pharm or pharm-cards) From. Dr. K.\

They all end in "-setron"
5HT-3 antagonist that has been associated with QRS and QT prolongation and should not be used in patients with heart disease
Dolasetron
DOC of chemo induced nausea and vomiting
Odansetron
Prostaglandins that cause abortions
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha