# 2nd Generation H2RAs ___ antagonist reduce gastric acid secretion in response to histamine, gastrin, acetylcholine ___ half life ( ___ vs BID dosing) fewer effects on ___ system greater ___ absorbed ___ to reduce parietal cell function

competitive longer, HS CYP450 potency quickly

GI Flashcards by Reagan Smith

drugs that affect gastric secretion (4)

antacids
H2 histamine receptor antagonists
proton pump inhibitors
protectants

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drugs that increase GI motility (2)

laxatives
prokinetic drugs

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drugs that reduce GI motility (2)

antidiarrheals
anti-emetics

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Zollinger-Ellison syndrome is

overactive tumors on pancreas secrete gastric and make too much gastirc acid

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G cells produce ___ in the lumen of the ___
gastrin travels through blood vessels and binds to ___ and ___ cells.
ECL cell releases ___ which binds to ___ cells
parietal cells exchange ___ for K+ using ATPases
this makes ___ acid more acidic
high acidity triggers __ cells to produce ___ to slow the release of gastrin

gastrin, antrum
ECL, parietal
histamine, parietal H+
luminal
D, somatostatin

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Prostaglandins like ___ and ___ work with ___ to maintain mucus layer. When NSAIDs like aspirin inhibit prostaglandins, this protection is compromised and ulcers can form

PGE2 and PGI2
NO

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antacids prevent ___ from being secreted from ___ cells
PPIs stop the whole ___

H+, parietal
ATPase

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All of the following antacids have high neutralizing capacity except:
A) NaHCO3
B) CaCO3
C) Al(OH)3
D) Mg(OH)2

CaCO3

only moderate

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Side effects

Al(OH)3: ___
Mg(OH)2: ___

constipation
diarrhea

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Antacid Brand Names

AlternaGEL

Al(OH)3

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Antacid Brand Names

Tums

CaCO3

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Antacid Brand Names

Maalox, Mylanta

Al(OH)3 and Mg(OH)2

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Antacid Brand Names

Rolaids

CaCO3 and Mg(OH)2

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Brand Names

Alka-Seltzer

ASA and NaHCO3

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Antacid Brand Names

Gaviscon

sodium alginate + antacids

viscous weak base

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H2RAs block H2 receptors on ___ cells

parietal

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H2RA

cimetidine (Tagamet)
* ___ antagonist
* reduce gastirc acid sectretion in response to histamine, ___ , and ____

competitive
gastrin, acetylcholine

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2nd Generation H2RAs (3)

ranitidine
nizatidine
famotidine

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2nd Generation H2RAs Brand Names

ranitidine

Zantac

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2nd Generation H2RAs Brand Names

nizatidine

Axid

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2nd Generation H2RAs Brand Names

famotidine

Pepcid

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2nd Generation H2RAs

___ antagonist
reduce gastric acid secretion in response to histamine, gastrin, acetylcholine
___ half life ( ___ vs BID dosing)
fewer effects on ___ system
greater ___
absorbed ___ to reduce parietal cell function

competitive
longer, HS
CYP450
potency
quickly

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PPI chemical structure name

benzimidazoles

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PPI Brand Names

esomeprazole

Nexium

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# PPI Brand Names omeprazole

Prilosec | racemic mixture

# PPI Brand Names lansoprazole

Prevacid

# PPI Brand Names rabeprzole

Aciphex

# PPI Brand Names pantoprazole

Protonix

# PPI Brand Names dexlansoprazole

Dexilant

T or F: esomeprazole is the R enantiomer that is more potent

False; S enantiomer

T or F: PPIs are prodrugs

True

# PPI Prodrug Steps * must be absorbed in the ___ , circulate and then be taken up by ___ cells. Leads to slow ___ * activated/protonated by ___ in the parietal cells * ___ inhibitor of __ ATPase (Cys ___ ) * short plasma half life, but long duration due to ___ inhibition and slow turnover of ___ * hypergastrinemia occurs, and may result in rebound ___ of gastric acid upon drug ___

* SI, parietal, onset * acidic pH * irreversible, H+/K+, Cys813 * covalent, proton pumps * hypersecretion, withdrawal

Hypergastrinemia definition

reduced gastric acid removes somatostatin's inhibition of gastrin secretion | D cells get lazy since they havent had to suppress in to long

T or F: tolerance to H2 antagonists can occur

True

# PPI associated fracture Known 1. PPI therapy causes profound acid suppression 2. leads to ___ 3. gastrin acts on ___ and leads to hyperplasia 4. leads to primary ____ 5. increase in ___ causes increased bone ___ Theory * PPIs decrease ___ absorption * leads to secondary ____

* hypergastrinemia * parathyroid gland * hyperparathyroidism * PTH, resorption * Ca2+ * hyperparathyroidism

T or F: PPIs have an increased risk of dementia

False; debunked, this study used a bunch of old people

Vonoprazan is a ___ competitive acid blocker (P-CAB) * faster ___ suppression * not a ___ * not influenced by ___ * very stable to ___ pH | only approved in Japan

* potassium * acid * prodrug * meals * low

# Mucosal Protective agents Sucralfate * Brand name ___ * ___ complex of sucrose * ___ and forms protective barrier at ___ site * ___ pH activates complex * poorly ___

* Carafate * aluminum hydroxide * polymerizes ulcer * acidic * absorbed

# Mucosal Protective agents Misoprostol * Brand name ___ * semi-synthetic ___ E1 derivative * reduced acid secretion in __ cells * cytoprotectant effects - enhanced ___ and ___ secretion * used in combination eith chronic ____ * Adverse effects: ___ and ___

* Cytotec * prostaglandin * parietal * mucus, bicarbonate * NSAIDs * diarrhea, abortifacient

# H. Pylori and Peptic Ulcers * converted to ___ salts and ___ acid in the GI tract * Bismuth subsalicylate has ___, antiviral, and antisecretory activity Uses: nausea, heartburn, indigestion, upset stomach, diarrhea * part of multi-drug therapy for ___ eradication * Brand Name ___

* bismuth, salicylic * antibacterial * H. pylori * Pepto-Bismol

# H. pylori Eradication therapy can consist of: * bismuth salt ( ___ ) * antibiotic (4) * H2 blocker or PPI * Tritec ( ___ bismuth citrate)

* PeptoBismol * metronidazole, tertracycline, amoxicillin, clarithromycin * ranitidine

H. pylori Eradication example

metronidazole (Flagyl) 500 mg BID + omeprazole (Prilosec) 20 mg BID + clarithromycin (Biaxin) 500 mg BID for 2 weeks

Which of the following antibacterial drugs is used commonly to eradicate intestinal H pylori? A) Cefazolin B) Ciprofloxaz C) Clarithromycin D) Clindamycin E) Vancomycin

Clarithromycin

* Enteric nervous system (ENS) - increased ___ * Extrinsic primary afferent - nausea, ___ , and pain (goes to brain) * intrinsic primary (goes to ENS)

* peristalsis * vomiting

# Bulk and Osmotic Laxatives * Fiber laxatives: psyllium ( ___ ), Methylcellulose ( ___ ), calcium polycarbophil ( ___ ) * PEG3350 ( ___ ) * isosmotic electrolyte solutions with PEG 3350 ( ___ )

* Metamucil * Citrucel * fiberCon * MiraLAX * GoLytely

# Bulk and Osmotic Laxatives * lactulose ( ___ ) is a non-absorbable sugar that has an ___ effect. Fermented by bacteria in the gut producing acetate which stimulates ___. * sugar free gummies have non-absorbable sugar alcohol called ___, Forms hydrophilic mass in the presence of water * increase water in the intestinal lumen by ___ force, leading to distention and an increase in ___

* Duphalac, osmotyic, peristalsis * maltitol * osmotic, peristalsis

# Stool Softeners * docusate sodium (Colace), mineral oil, glycerin * __ and lubricants * incorporate into stool to make passage easier and ___ water adsorption * ___ lower bowel to reduced fecal impaction * can decrease absorption of ___ soluble vitamins

* surfactants * decrease * lubricate * fat (ADEK)

# Secretory or Stimulant Laxatives * mechanism poorly understood * castor oil: hydrolyzed in the upper small intestine to ___ acid * diphenylmethan derivatives: bisacodyl ( ___ ) * anthraquinones: cascara, ___ , and aloes * irritation of the mucosa affects fluid secretion/absorption balance and induces ___

* ricinoleic * Dulcolax * senna * peristalsis

# Prokinetic Drugs and their receptors * Prucalopride and Tegaserod; ___ * Erythromycin; ___ * Bethanechol; ___ * Metoclopramide; ___ * Neostigmine; ___

* 5-HT4 * Motilin * M3 * D2 * AChE

# Metoclopramide * Brand name: ___ * Blockade of ___ receptors in the ___ plexus leads to increase ___ release * produced anti-___ effects * Promotes gastric ___ * can lead to acute ___ reactions

* Reglan * D2, myenteric, ACh * emetic * emptying * dystonic

# Prokinetic Drugs Opioid receptor antagonists: Centrally acting: anti-addictive agents (3)

* Naloxone (Narcan) * Naltrexone * Nalmefene

# Prokinetic Drugs Peripherally acting - cannot cross ___ (3)

BBB * Naloxegol (Movantik) * Alvimopan (Entereg) * Naldemedine (Symproic)

Opioid induced constipation can also be avoided by using a biased agonist such as ___ 1. decrease smooth muscle ___ 2. increase rectal sphincter ___ 3. decreases colonic mucosa ___

Oliceridine 1. contraction 2. tone 3. secretion

# Prokinetic Drugs Prucalopride * Brand name: ___ * __ agonist * ___ receptor, GPCR, Gas coupled activation leads to increased ___ production and ___ activation. Releases ___ * indicated for the treatment of chronic idiopathic ___ in adults

* Motegrity * 5HT4 * serotonin, cAMP, PKA, ACh * constipation

# Prokinetic Drugs Tegaserod * Brand Name: ___ * same mechanism as ___ * indicated for treatment of ___ in women under ___

* Zelnorm * Prucalopride * IBS-C, 65

# Prokinetic Drugs Chloride Channel Activators (3)

* Lubiprostone (Amatiza) * Linaclotide (Linzess) * Plecanatide (Trulace)

# Prokinetic Drugs - Chloride Channel Activators * increased chloride-rich fluid secretion into intestine * treatment of ___ * not absorbed ___

* IBS-C * systemically

# Prokinetic Drugs - Chloride Channel Activators Lubiprostone * Brand name: ___ * stimulation of type ___ chloride channel ___ activator in ___ Linaclotide and Plecanatide * Brand names: ___ and ___ * a ___ activator or ___ cyclase C ___

* Amatiza * 2, ClC-2, small intestine * Linzess, Trulance * peptide, guanylate, GC-C

# Prokinetic Drugs Tenapanor * ___ exchanger inhibitor * exhanger is expressed on the ___ side of small bowel and colonic epithelial cells * functions to absorb ___ from luminal contents * trapping Na+ in the gut leads to increased ___ in the gut acclerating transit of intestinal contents

* Na+/H+ (NHE3) * luminal * Na+ * water

Which of the following drugs in an osmotic laxative that could be used to treat constipation? A) aluminum hydroxide B) diphenoxylate C) magnesium hydroxide D) metoclopramide E) ranitidine

magnesium hydroxide

Which of these drugs irreversibly inhibits the H+/K+ ATPase in the parietal cells? A) cimetidine B) diphenoxylate C) esomeprazole D) metoclopramide E) sulfasalazine

esomeprazole

# Antidiarrheals Opiates (2) * slow ___ to increase water and electrolyte absorption * inhibits ___ cholinergic nerves

* diphenoxylate, loperamide * peristalsis * presynaptic

Diphenoxylate ( + atropine = ___ ) * active in the ___

* Lomotil * CNS

Loperamide ( ___ ) * poorly transverse the ___ * act ___ to delay gastric emptying

Imodium * BBB * locally

Loperamide ( ___ ) * poorly transverse the ___ * act ___ to delay gastric emptying

Imodium * BBB * locally

# Antidiarrheals Alosetron ( ___ ) * blocks visceral afferent pain sensation and decreases colon ___

Lotrinex * motility

# Anti-Emetics * ___ receptor antagonists "-setron" * block activity of ___ nerves from stomach and small intestine which activate the trigger center in the ___ * Side effect: ___

* 5-HT3 * afferent, CNS * Constipation

# Anti-Emetics * NK1 antagonists (3) * receptors in the ___ trigger zone * can be combined with ___. Example ( ___ is a combination of Netupitant and palonosetron)

* Aprepitant, Netupitantm Rolapitant * chemoreceptor * 5-HT3 * Akynzeo

# Anti-Emetics antihistamines/anticholinergics * Dimenhydrinate ( ___ ) = ___ - H1 antihistimine with anticholinergic properties + the stimulant chlorotheophylline in dramamine

* dramamine, diphenhydramine

# Anti-Emetics antihistamines/anticholinergics * Meclizine ( ___ ) - H1 antihistimine with minimal ___ properties

Antivert * anticholinergic

# Anti-Emetics antihistamines/anticholinergics * Scopolamine - ___ receptor antagonist with significant ___ effects

* muscarinic * anticholinergic

# Anti-Emetics Antipsychotics (4) * ___ receptor antagonists * ___ properties * also has ___ and ___ effects

* metoclopramide = Reglan * Prochlorperazine = Compazine * Promethazine = Phenergan * Droperidol = Inapsine * D2 dopamine * sedatice * antimuscarinic, antihistamine

GI Flashcards

(72 cards)