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PHRM 825 > GI > Flashcards

GI Flashcards

1
Q

drugs that affect gastric secretion (4)

A
  • antacids
  • H2 histamine receptor antagonists
  • proton pump inhibitors
  • protectants
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2
Q

drugs that increase GI motility (2)

A
  • laxatives
  • prokinetic drugs
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3
Q

drugs that reduce GI motility (2)

A
  • antidiarrheals
  • anti-emetics
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4
Q

Zollinger-Ellison syndrome is

A

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

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5
Q
  1. G cells produce ___ in the lumen of the ___
  2. gastrin travels through blood vessels and binds to ___ and ___ cells.
  3. ECL cell releases ___ which binds to ___ cells
  4. parietal cells exchange ___ for K+ using ATPases
  5. this makes ___ acid more acidic
  6. high acidity triggers __ cells to produce ___ to slow the release of gastrin
A
  • gastrin, antrum
  • ECL, parietal
  • histamine, parietal H+
  • luminal
  • D, somatostatin
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6
Q

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

A
  • PGE2 and PGI2
  • NO
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7
Q
  • antacids prevent ___ from being secreted from ___ cells
  • PPIs stop the whole ___
A
  • H+, parietal
  • ATPase
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8
Q

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

A

CaCO3

only moderate

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9
Q

Side effects

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

A
  • constipation
  • diarrhea
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10
Q

Antacid Brand Names

AlternaGEL

A

Al(OH)3

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11
Q

Antacid Brand Names

Tums

A

CaCO3

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12
Q

Antacid Brand Names

Maalox, Mylanta

A

Al(OH)3 and Mg(OH)2

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13
Q

Antacid Brand Names

Rolaids

A

CaCO3 and Mg(OH)2

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14
Q

Brand Names

Alka-Seltzer

A

ASA and NaHCO3

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15
Q

Antacid Brand Names

Gaviscon

A

sodium alginate + antacids

viscous weak base

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16
Q

H2RAs block H2 receptors on ___ cells

A

parietal

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17
Q

H2RA

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

A
  • competitive
  • gastrin, acetylcholine
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18
Q

2nd Generation H2RAs (3)

A
  • ranitidine
  • nizatidine
  • famotidine
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19
Q

2nd Generation H2RAs Brand Names

ranitidine

A

Zantac

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20
Q

2nd Generation H2RAs Brand Names

nizatidine

A

Axid

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21
Q

2nd Generation H2RAs Brand Names

famotidine

A

Pepcid

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22
Q

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
A
  • competitive
  • longer, HS
  • CYP450
  • potency
  • quickly
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23
Q

PPI chemical structure name

A

benzimidazoles

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24
Q

PPI Brand Names

esomeprazole

A

Nexium

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25
Q

PPI Brand Names

omeprazole

A

Prilosec

racemic mixture

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26
Q

PPI Brand Names

lansoprazole

A

Prevacid

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27
Q

PPI Brand Names

rabeprzole

A

Aciphex

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28
Q

PPI Brand Names

pantoprazole

A

Protonix

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29
Q

PPI Brand Names

dexlansoprazole

A

Dexilant

30
Q

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

A

False; S enantiomer

31
Q

T or F: PPIs are prodrugs

A

True

32
Q

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 ___
A
  • SI, parietal, onset
  • acidic pH
  • irreversible, H+/K+, Cys813
  • covalent, proton pumps
  • hypersecretion, withdrawal
33
Q

Hypergastrinemia definition

A

reduced gastric acid removes somatostatin’s inhibition of gastrin secretion

D cells get lazy since they havent had to suppress in to long

34
Q

T or F: tolerance to H2 antagonists can occur

A

True

35
Q

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 ____

A
  • hypergastrinemia
  • parathyroid gland
  • hyperparathyroidism
  • PTH, resorption
  • Ca2+
  • hyperparathyroidism
36
Q

T or F: PPIs have an increased risk of dementia

A

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

37
Q

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

only approved in Japan

A
  • potassium
  • acid
  • prodrug
  • meals
  • low
38
Q

Mucosal Protective agents

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

A
  • Carafate
  • aluminum hydroxide
  • polymerizes ulcer
  • acidic
  • absorbed
39
Q

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 ___

A
  • Cytotec
  • prostaglandin
  • parietal
  • mucus, bicarbonate
  • NSAIDs
  • diarrhea, abortifacient
40
Q

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 ___
A
  • bismuth, salicylic
  • antibacterial
  • H. pylori
  • Pepto-Bismol
41
Q

H. pylori Eradication

therapy can consist of:
* bismuth salt ( ___ )
* antibiotic (4)
* H2 blocker or PPI
* Tritec ( ___ bismuth citrate)

A
  • PeptoBismol
  • metronidazole, tertracycline, amoxicillin, clarithromycin
  • ranitidine
42
Q

H. pylori Eradication example

A

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

43
Q

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

A

Clarithromycin

44
Q
  • Enteric nervous system (ENS) - increased ___
  • Extrinsic primary afferent - nausea, ___ , and pain (goes to brain)
  • intrinsic primary (goes to ENS)
A
  • peristalsis
  • vomiting
45
Q

Bulk and Osmotic Laxatives

  • Fiber laxatives: psyllium ( ___ ), Methylcellulose ( ___ ), calcium polycarbophil ( ___ )
  • PEG3350 ( ___ )
  • isosmotic electrolyte solutions with PEG 3350 ( ___ )
A
  • Metamucil
  • Citrucel
  • fiberCon
  • MiraLAX
  • GoLytely
46
Q

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 ___
A
  • Duphalac, osmotyic, peristalsis
  • maltitol
  • osmotic, peristalsis
47
Q

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
A
  • surfactants
  • decrease
  • lubricate
  • fat (ADEK)
48
Q

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 ___
A
  • ricinoleic
  • Dulcolax
  • senna
  • peristalsis
49
Q

Prokinetic Drugs and their receptors

  • Prucalopride and Tegaserod; ___
  • Erythromycin; ___
  • Bethanechol; ___
  • Metoclopramide; ___
  • Neostigmine; ___
A
  • 5-HT4
  • Motilin
  • M3
  • D2
  • AChE
50
Q

Metoclopramide

  • Brand name: ___
  • Blockade of ___ receptors in the ___ plexus leads to increase ___ release
  • produced anti-___ effects
  • Promotes gastric ___
  • can lead to acute ___ reactions
A
  • Reglan
  • D2, myenteric, ACh
  • emetic
  • emptying
  • dystonic
51
Q

Prokinetic Drugs

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

A
  • Naloxone (Narcan)
  • Naltrexone
  • Nalmefene
52
Q

Prokinetic Drugs

Peripherally acting - cannot cross ___
(3)

A

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

53
Q

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 ___

A

Oliceridine
1. contraction
2. tone
3. secretion

54
Q

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

A
  • Motegrity
  • 5HT4
  • serotonin, cAMP, PKA, ACh
  • constipation
55
Q

Prokinetic Drugs

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

A
  • Zelnorm
  • Prucalopride
  • IBS-C, 65
56
Q

Prokinetic Drugs

Chloride Channel Activators (3)

A
  • Lubiprostone (Amatiza)
  • Linaclotide (Linzess)
  • Plecanatide (Trulace)
57
Q

Prokinetic Drugs - Chloride Channel Activators

  • increased chloride-rich fluid secretion into intestine
  • treatment of ___
  • not absorbed ___
A
  • IBS-C
  • systemically
58
Q

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 ___

A
  • Amatiza
  • 2, ClC-2, small intestine
  • Linzess, Trulance
  • peptide, guanylate, GC-C
59
Q

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

A
  • Na+/H+ (NHE3)
  • luminal
  • Na+
  • water
60
Q

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

A

magnesium hydroxide

61
Q

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

A

esomeprazole

62
Q

Antidiarrheals

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

A
  • diphenoxylate, loperamide
  • peristalsis
  • presynaptic
63
Q

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

A
  • Lomotil
  • CNS
64
Q

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

A

Imodium
* BBB
* locally

64
Q

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

A

Imodium
* BBB
* locally

65
Q

Antidiarrheals

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

A

Lotrinex
* motility

66
Q

Anti-Emetics

  • ___ receptor antagonists “-setron”
  • block activity of ___ nerves from stomach and small intestine which activate the trigger center in the ___
  • Side effect: ___
A
  • 5-HT3
  • afferent, CNS
  • Constipation
67
Q

Anti-Emetics

  • NK1 antagonists (3)
  • receptors in the ___ trigger zone
  • can be combined with ___. Example ( ___ is a combination of Netupitant and palonosetron)
A
  • Aprepitant, Netupitantm Rolapitant
  • chemoreceptor
  • 5-HT3
  • Akynzeo
68
Q

Anti-Emetics

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

A
  • dramamine, diphenhydramine
69
Q

Anti-Emetics

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

A

Antivert
* anticholinergic

70
Q

Anti-Emetics

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

A
  • muscarinic
  • anticholinergic
71
Q

Anti-Emetics

Antipsychotics (4)
* ___ receptor antagonists
* ___ properties
* also has ___ and ___ effects

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

PHRM 825 (49 decks)

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