Term
what does the parietal cell make? |
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Definition
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Term
what does the Enterochromaffin cell make? |
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Definition
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Term
What does the antral cell make? |
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Definition
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Term
What are the inputs to the parietal cells? |
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Definition
neural from vagus, endocrine from antral cells: Histamine, paracrine from ECL cells (Histamine) |
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Term
How does the parietal cell form acid? |
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Definition
H/K ATPase: pumps H into lumen |
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Term
What is the site of action of PPI's? |
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Definition
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Term
What is the critical regulator of acid production? |
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Definition
Histamine, through H2 receptors |
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Term
How does Histamine stimulate acid production? |
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Definition
H/K ATPase through the cAMP pathway |
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Term
How do Muscarinic and gastrin receptor activate acid? |
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Definition
through increases in Calcium |
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Term
What are the Histamine receptor antagonists? |
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Definition
Cimetidine, Ranitidine, Famotidine, Nizatidine |
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Term
What is the structure of Histamine receptor antagonists? |
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Definition
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Term
what is the prototype histamine receptor |
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Definition
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Term
which Histamine recepotr blocker is the most likely to have side effects? |
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Definition
cimetidine; blocks cyt P450 |
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Term
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Definition
what else does Cimetidine block?,androgen recepotrs and Estrogen metabolism; lead to Estrogen effects such as gynecomastia |
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Term
What are side effects of cimetidine? |
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Definition
may cause gynecomastia, decreased sperm count, galactorrhea |
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Term
what drugs does Cimetidine alter the metabolism of? |
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Definition
Warfarin, Quinidine, phenytoin, Beta Blockers |
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Term
Which Histamine antagonist has only 1/10 effect on p450 as Cimetidien? Which 2 are devoid of p450 effects? |
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Definition
Ranitidine. Famotidine and Nizatidine |
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Term
Histamine receptor antagonists not only block stimulated acid secretion |
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Definition
but also ____,basal secretion |
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Term
what suffix is a/w histamine receptor antagonists? |
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Definition
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Term
what are the uses of Histamine Receptor antagonists? |
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Definition
gastric and duodenal ulcers, suppression of nocturnal acid production, treatment of uncomplicated GERD, prophylaxis of stress ulcers. |
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Term
What are the Proton Pump Inhibitors? |
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Definition
Omeprazole, esomeprazole, Pantoprazole, Lansoprazole, Dexlansoprazole |
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Term
What is the MOA of PPI"s? |
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Definition
covalently interact and form disulfide bridge with H/K ATPase and inhibit the pump; IRREVERSIBLE! |
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Term
How are PPI's administered? |
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Definition
orally active in a delayed releae form so they are protected from stomach acid. |
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Term
What are adverse reactions of PPI's? |
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Definition
very insignificant; alter absorption of other drugs that require acid mileiu of stomach |
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Term
What drugs' absorption is affected by PPI's? |
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Definition
Ketoconazole or Ampicillin esters |
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Term
what are the uses of PPI's? |
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Definition
healing of gastric and duodenal ulcers, Tx of GERD, Zollinger Ellison, erosive esophagitis |
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Term
What is the MOA of Misoprostol to inhibit acid secretion? |
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Definition
PGE1 analog that acts on EP3 receptors of parietal cells to decrease cAMP, decrease acid secretion, increase mucin and bicarbonate |
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Term
How is Misoprostol administered |
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Definition
it is orally active and rapidly absorbed |
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Term
What is the approved use of Misoprostol that is GI-related? |
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Definition
approved for preventing mucosal injury caused by NSAIDs |
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Term
What is the one adverse effect of Misoprostol? |
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Definition
PG's cause smooth muscle contraction, so they cause diarrhea |
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Term
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Definition
for treatment of ulcers, contraindicated?,contraindicated in pregnancy |
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Term
What drug is used for prophylaxis of Stress-induced ulcers? |
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Definition
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Term
What are the two components of Sucralfate? |
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Definition
sucrose octasulfate and polyaluminum hydroxide |
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Term
What is the MOA of Sucralfate? |
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Definition
at pH 4 and below, undergoes cross-linking and adheres to form a protective coat on ulcers |
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Term
What is the adverse effect of Sucralfate? |
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Definition
constipation due to the Aluminum component |
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Term
Antacids are either ___ or ___ |
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Definition
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Term
What is the MOA of Antacids? |
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Definition
They are weak bases that neutralize acid |
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Term
Which 2 antacids are rapid acting? |
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Definition
Calcium carbonate and Magnesium Hydroxide |
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Term
What is the slow acting antacid? |
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Definition
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Term
What are side effects of Aluminum? |
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Definition
constipation, can bind drugs, toxic in individuals with reanl insufficiency: osteoporosis, encephalopathy, myopathy |
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Term
What are the effects of Magnesium? |
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Definition
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Term
Whcih antacid can lead to hypercalcemia? |
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Definition
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Term
What class of drugs is used in Europe for peptic ulcer disease by blocking acetylcholine activity of EC cells? |
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Definition
Anticholinergics: Pirenzipine and Telenzipine |
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Term
When are antibiotics used as acid regulators? |
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Definition
in treatment of H.pylori. used in combo with PPI's |
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Term
How are Prostaglandins 'bifunctional'? |
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Definition
1. inhibit acid secretion by decreasing cAMP. 2. increase mucus production |
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Term
What is the overall theme of prokinetic drugs? |
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Definition
ACH and activation of M3 receptor |
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Term
What is the effect of Dopamine on Gut motility? |
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Definition
inhibitory; inhibits the release of ACH through D2 receptors |
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Term
What is the effect of blocking Dopamine on Gut motility? |
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Definition
Dopamine inhibits gut motility, so inhibiting Dopamine activates gut smooth muscle. |
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Term
What is the bimodal effect of Serotonin on gut motility? |
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Definition
5HT3 and 4 increase motility, 5HT1 inhibits ACH release. |
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Term
what is a naturally occuring peptide taht stimulates the upper GI tract? |
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Definition
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Term
What is a Dopamine inhibitor that blocks D2 receptors |
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Definition
blocking the inhibitory effect of Dopamine on Gut Motility?,Metoclopramide |
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Term
What are the uses of Dopamine inhibitors? |
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Definition
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Term
What are adverse effects of Dopamine inhibitors? |
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Definition
crosses BBB causing Extrapyramidal side effects. also increases prolactin |
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Term
What are the 2 5HT4 agonists? |
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Definition
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Term
What are the adverse effects of 5HT4 agonists? |
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Definition
myocardial and CNS iscehmia/stroke |
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Term
What are 2 Motilin agonsits? |
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Definition
Erythromycin, Clarithromycin |
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Term
When is a Motilin agonist used? |
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Definition
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