Pharmacology of Digestive System

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treatment approaches of PUD

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1

treatment approaches of PUD

eradicating H.P reducing gastric acid mucosal protective agents

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2

quadruple therapy for PUD H.P

bismuth, metronidazole, tetracycline, PPi

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3

triple therapy for PUD H.P

PPi, amoxicillin, clarithromycin

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4

while quadruple therapy is first line, when is triple therapy preferred for PUD

low resistance/exposure to atb

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5

endings of H2-r antagonists

"tidine"

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6

______ was the first H2-r antagonist but use is limited due to SE + DD interactions

cimetidine

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7

moa of H2-r antagonists

act selectively on H2 r in stomach, competitive antagonists + reversible

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8

cli of h2-r antagonists

PUD, acute stress ulcers (IV), GERD

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9

what drugs are preferred to h2-r antagonists

ppis

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10

pharmacokinetics of H2-r antagonists

distribute widely (milk + placenta), excreted in urine

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11

which h2-r antagonists are available iv and require dosage adjustments in renal dysfxn

cimetidine, ranitidine, famotidine

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12

SE h2-r antagonists

only cimetidine -> endocrine (gynecomastia + galactorrhea), CNS (confusion)

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13

_______ inhibits cytochrome p450 and can interfere w/ warfarin, phenytoin and clopidogrel

cimetidine

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14

PPis bind to __________ and suppresses secretion of _______ into gastric lumen

H+/k+-ATPase enzyme system acids

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15

ending of ppis

"prazole"

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16

moa ppi

prodrugs w/ acid-resistant enteric coat -> removed in duodenum -> covalent bond w/ proton pump -> inhibits 90% acid secretion

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17

an oral product containing ______ combined w/ _______ for faster absorption is available to decrease gastric acid secretion

omeprazole sodium bicarb

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18

cli ppi

GERD, erosive esophagitis, active duodenal ulcers, Zollinger-Ellison, prevention NSAID + stress ulcers

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19

pharmacokinetics of ppis

orally -> taken 30-60m before breakfast or largest meal of day, excreted in urine and feces

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20

which ppis are available iv

esomeprazole, lansoprazole, pantoprazole

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21

se ppis

omeprazole + esomeprazole decreases clopidogrel fractures, b12 + ca + mg deficiency, diarrhea + c. difficile colitis, pneumonia

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22

cli prostaglandins

NSAID gastric ulcers

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23

prostaglandins ending

"prostol"

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24

CO misoprostol

pregnancy (uterine contractions)

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25

SE PGs

diarrhea

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26

_____ reduce gastric acidity + pepsin activity

antacids

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27

when should antacids be taken

full stomach

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28

2 antacids used

aluminum OH magnesium OH

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29

cli antacids

symptoms of PUD, heartburn, GERD

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30

SE antacids

aluminum OH - constipation magnesium OH - diarrhea

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31

sucralfate

mucosal protective agent, aluminum OH + sucrose -> physical gel barrier

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32

cli sucralfate

duodenal ulcers, prevention stress ulcers

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33

why is sucralfate not used much

multiple daily dosing, DD interactions w/ PPis, H2 antagonists and antacids (needs acidic pH)

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34

bismuth

mucosal protective agent w/ antimicrobial action + coats ulcer

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35

which brainstem vomiting site is outside bbb

CTZ

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36

_____ functions mainly in motion sickness

vestibular system

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37

moa phenothiazines

block dopa r in CTZ

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38

phenothiazines cli

emetogenic chemo drugs

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39

__________ is a phenothiazine

prochlorperazine

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40

ending 5-H53-r blockers

"setron"

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41

moa 5-ht3-r blockers

block 5-ht3 r in periphery + CTZ

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42

cli 5-ht3-r blockers

for CINV, administered as single dose before chemo

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43

5-ht3 antagonists are metabolized by liver but only ________ need dosage requirements in hepatic insufficiency

ondansetron

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44

SE 5-ht3-r blockers

only ondansetron + dolasetron = qt prolongation

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45

the substituted benzamide, _______ is effective at high doses against chemo

metoclopramide

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46

metoclopramide moa + SE

inhibition of dopa in CTZ -> extrapyramidal symptoms

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47

metoclopramide cli

gastroparesis + CINV

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48

moa butyrophenones

blocking dopa r

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49

butyrophenones ending

"peridol" (droperidol + haloperidol)

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50

cli droperidol

sedation in interventions (antiemetic)

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51

why is droperidol last resort antiemetic

qt prolongation

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52

benzodiazepines ending

"zepam" (lorazepam + alprazolam)

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53

cli benzos

anticipatory vomiting

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54

corticosteroids such as _______ are used alone for CINV

dexamethasone, methylprednisolone

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55

substance p/neurokinin-1-r antagonists endings

"pitant"

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56

substance P antagonists are used for _____ in combo w/ ______

delayed phase CINV dexamethasone + 5-ht3 antagonist

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57

substance P antagonists undergo hepatic metabolism by

CYP4A4 (many DD interactions)

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58

SE substance P antagonists

hiccups

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59

antiemetic combo: corticosteroids are given with

metoclopramide, phenothiazine and butyrophenone/benzo

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60

antiemetic combo: metoclopramides are given in combo with

antihistamines (reduced extrapyramidal) or corticosteroids (reduced diarrhea)

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61

best antiemetic combo for delayed CINV

substance P antagonist + 5-HT3 antagonist + dexamethasone

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62

classes of antidiarrheal drugs

antimotility agents, adsorbents, drugs modifying fluid and electrolyte transport

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63

2 antimotility agents

diphenoxylate + loperamide

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64

moa of antimotility agents (diphenoxylate, loperamide)

opioid-like actions, activated presynaptic opioid receptors in enteric n system -> Ach inhibited -> less peristalsis

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65

loperamide cli

acute + traveler's diarrhea

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66

CO antimotility agent (diphenoxylate + loperamide)

children or colitis

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67

adsorbents for diarrhea

aluminum hydroxide + methylcellulose

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68

moa adsorbents

adsorb toxins/organisms + coat mucosa

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69

bismuth cli for diarrhea

traveler's diarhea

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70

SE bismuth

black tongue + stool

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71

stimulant laxatives

senna and bisacodyl

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72

opioid-induced constipation drug combo

senna + docusate

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73

bisacodyl pharmokinetics

suppository or enteric-coated tablet, acts directly on n

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74

irritant laxative

castor oil

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75

CO castor oil

pregnancy (uterine contractions)

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76

bulk laxatives

methylcellulose

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77

psyllium adverse efect

reduce drug absorption (for 2h)

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78

saline laxatives

magnesium citrate + OH

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79

saline laxatives (magnesium citrate + OH) moa

hold water in intestines

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80

PEG cli

colonic lavage for interventions

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81

lactulose

osmotic laxative

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82

cli lactulose

hepatic encephalopathy + constipation

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83

stool softeners

docusate (Na + Ca)

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84

cli docusate

prophylactic constipation

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85

CO stool softeners

mineral oil

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86

lubricant laxatives

mineral oil + glycerin suppositories

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87

how should mineral oil be taken

upright position

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88

Cl- channel activator

lubiprostone

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89

moa lubiprostone

activates Cl- channels to increase fluid secretion in lumen

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90

cli lubiprostone

chronic constipation + IBS-C

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91

IBD mild/moderation symptoms treatment

aminosalicylates/corticosteroids

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92

IBD chronic symptoms treatment

thiopurines, methotrexate, cyclosporin

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93

_______ is an atb infusion for IBD

infliximab

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