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GI 1
Pharm
57
Medical
Kindergarten
04/27/2010

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Cards

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