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therapeutics > 61-62: GI protectants > Flashcards

61-62: GI protectants Flashcards

1
Q

Drugs that increase GI motility

A

-laxatives
-prokinetic drugs

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1
Q

Drugs affecting gastric secretion

A

-Antacids
-H2 histamine receptor antagonists
-Proton Pump Inhibitors
-Protectants

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2
Q

Drugs that reduce GI motility

A

-antidiarrheals
-anti-emetics

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3
Q

Acid-peptic disease

A

-non-ulcer dyspepsia (indigestion)
-gastric and duodenal ulcers
-GERD
-hypersecretory states (Zollinger syndrome)

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4
Q

Physiologic control of GI secretions

A

-slide 10-13

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5
Q

Antacids

A

-systemically absorbed: NaHCO3 and CaCO3
-minimally absorbed: Al(OH)3 and Mg(OH)2

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6
Q

NaHCO3

A

-systemic
-high efficacy
-alkalosis, fluid retention, gas)
-alkaseltzer

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7
Q

CaCO3

A

-systemic
-moderate efficacy
-hypercalcemia, nephrolithiasis, milk-alkali syndrome, CO2
-Tums and Rolaids

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8
Q

AlOH3

A

-minmally absorbed
-high efficacy
-contipation, hypophosphatemia
-encephalopathy if absorbed
-AlternaGEL and Maalox

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9
Q

MgOH2

A

-minimal absorption
-high efficacy
-diarrhea
-CNS toxicity if absorbed
-Maalox and Rolaids

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10
Q

AlternaGEL

A

-AlOH3
-antacid
-minimal absorbed

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11
Q

Tums

A

-CaCO3
-systemic
-mod efficacy
-antacid

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12
Q

Maalox/Mylanta

A

-AlOH3 and MgOH
-minimally absorbed

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13
Q

Rolaids

A

-CaCO3 and MhOH
-antacid

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14
Q

Alka-seltzer

A

-ASA and NaHCO3

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15
Q

Gaviscon

A

-sodium alginate + antacids
-viscous, weak base
-prevents reflux
-effective in GERD

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16
Q

Commercial antacids

A

-AlternaGEL
-Tums
-Maalox.Mylanta
-Rolaids
-Alka-seltzer
-Gaviscon

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17
Q

Histamine Receptor Antagonists

A

-slide 16-19

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18
Q

Cimetidine (tagamet)

A

-competative antagonist of H2
-reduce gastric secretion in response to histamine, gastrin, acetylcholine

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19
Q

2nd gen H2 blockers

A

-Rantidine (NO_
-Nizatidine
-Famotidine

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20
Q

Nizatidine (axid) and famotidine (pepcid

A

-2nd gen H2 antagonists
-reduce acid secretion in response to histamine, gastrin, acetylcholine
-longer hlaf life
-fewer CYP effects
-greater potency
-absorbed quickly to reduce parietal cell function

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21
Q

Proton Pump inhibitors

A

mech slide24-25

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22
Q

PPI drugs

A

-Benzimidazoles
-six ring next to 5 ring

-or Vonoprazan (P-CAB)

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23
Q

Benzimidazoles (PPI drugs)

A

-Esomeprazole (nexium)
-omeprazole (prilosec)
-lansoprazole (prevacid)
-rabeprazole (aciphex)
-pantoprazole (protonix)
-dexlansoprazole (dexilant)

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24
Q

Omeprazole (prilosec) vs eSomeprazole (nexium

A

-omeprazole racemic
-eSomeprazole is S enantiomer
-more potent

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25
Q

PPI action

A

-must be absorbed in SI, circulate and then be taken up by parietal cells = SLOW onset
-prodrugs activated by acidic pH in parietal cell
-irreversible inhibitor of H/K ATPase
-short plasma half-life (1 hour) but long duration of action due to covalent inhibition (>24 hours) and slow turnover of proton pumps
-hypergastrinemia occurs and may result in rebound hypersecretion of gastric acid upon drug withdrawal

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26
Q

Acid rebound

A

-inc acid secretion upon withdrawal of acid suppressing medications
-reduced gastric acid removes somatostatin’s inhibition of gastrin secretion (HYPERgastrinemia)
-tolerance to H2 antagonists can occur

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27
Q

PPI risks

A

-inc risk of infection
-vitamin b12 deficiency
-dec Ca absorption/inc bone fractures
-dementia?

-maybe bc calcium is dec and PTH is inc which takes Ca out of bone to replace blood levels

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28
Q

Vonoprazan

A

-PPI
-K-competative acid blocker (P-CAB)
-adbantages: faster acid suppresion, not prodrug, not influenced by meals, very stable in low pH

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29
Q

Mucosal Protective Agents

A

-Sucralfate (Carafate)
-Misoprostol (Cytotec)

-affect secretion

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30
Q

Sucralfate (carafate)

A

-mucosal protective agent
-al hydroxide complex of sucrose
-polymerices and forms protective barrier at ULCER site
-acidic pH activates complex
-poorly absorbed (big ugly charged molecule)

31
Q

Misoprostol

A

-semi-synthetic prostaglandin E1 derivative
-reduce acid secretion pariteal cell
-cytoprotectant effects (enhance musuc and bicarbonate secretion)
-used in combo w chronic NSAIDs
-diarrhea, abortifacient

32
Q

Ulcers

A

-failure of mucosal protection
-many associated w H. pylori infection (gram-neg)

33
Q

H. Pylori eradication

A

-bismuth subsalicylate
-antibiotic (metro, tetra, amox, clar)
-H2 blocker or PPI

-combo them

34
Q

Bismuth subslicylate

A

-converted to bismuth salts and salicylic acid in GI tract
-antibacterial/viral/secretory
-treat nausea, heartburn, indigestion, upset stomach, diarrhea
-part of multi-drug therapy for H. pylori eradication

35
Q

Drugs that INCREASE GI motility

A

-laxative
-prokinetic drugs

36
Q

Intrinsic nerve plexuses

A

-myenteric
-submucosal
-idk man watch the vid

37
Q

Bulk and Osmotic ? Laxatives

A

-cellulose, agar, bran, linseed complex
-form hydrophillic mass in presence of water
-inc water in intestinal lumen by osmotic force = inc distension = inc peristalisis

38
Q

Bulk and osmotic laxative

A

-fibers
-PEG3350 (miraLAX)
-isosmotic electrolyte solutions with PEG 3350 (GoLytely) produce similar effects
-Lactulose
-Maltitol in some sugar free gummies

39
Q

Fiber laxatives

A

-bulk and osmotic
-psyllium (metamucil)
-methylcellulose (citrucel)
-calcium polycarbophil (fiberCon)

40
Q

Types of laxatives

A

-bulk and osmotic
-stool softeners
-secrectory/stimulant

41
Q

Lactulose

A

-non aborbable sugar
-osmolytic effect
-also fermeted by gut flora which inc peristalisis

42
Q

Stool softener mech

A

-inc into stool to ease passage
-dec water absorption
-lube lower bowel
-can dec absorption of fat-soluble vitamins

43
Q

Stool softeners

A

-docusate sodium (Colace)
-mineral oil
-glycerin
-surfactants and lubricants

44
Q

Secretory/Stimulant laxatives mech

A

-poorly understood
-irritation of mucosa affects fluid secretion/absorption balance and induces peristalsis

45
Q

Secretory/stimulant laxatives

A

-castor oil
-diphenylmethane derivatives (bisacodyl dulcolax)
-anthraquinones (cascara, senna, aloes)

46
Q

Castor oil

A

-stimulant lax
-hydrolyzed in upper SI to ricinoleic acid

47
Q

Common GI HYPOmotility disorders

A

-gastroparesis
-ileus
-opioid-induced constipation

48
Q

Gastroparesis

A

-neuropathy during diabetes or Parkinson’s disease

49
Q

Ileus

A

-small bowels don’t recover after surgery

50
Q

Prokinetic drugs

A

-Metoclopramide (reglan)
-Prucalopride (motegrity)
-Tegaserod (Zelnorm)
-Tenapanor
-opioid ANTAgonists
-chloride channel activators

51
Q

Metoclopramide (Reglan)

A

-D2 ANTAgonist
-block D2 in myenteric plexus
=inc aCH release
=anti-emetic effects
-promotes gastric emptying to facilitate small bowel intubation, post-op and diabetic gastroparesis, GERD
-can lead to acute dystonic reactions

52
Q

Opioid ANTAgonists

A

-Central: Naloxone (Narcan), Naltrexone, nalmefene
-Peripheral: nalozegol, alvimopan, naldemedine

53
Q

Prucalopride (Motegrity)

A

-5HT4 AGONIST
-serotonin receptor = GPCR = inc cAMP = release AcH
-treat chronic idiopathic constipation in adults

54
Q

Tegaserod (Zelnorm)

A

-5HT4 AGONIST
-treat IBS with constipation in WOMEN UNDER 65

55
Q

Chloride channel activators

A

-prokinetic
-inc chloride-rich fluid secretion into intestine
-treat IBS + constipation
-not systemic
-lubiprostone and linaclotide

56
Q

Lubiprostone

A

-type 2chloride channel activator in small intestine

57
Q

Linaclotide and Plecanatide

A

-peptide activator of guanylate cyclase C

58
Q

Sodium/hydrogen exchanger inhibition

A

-prokinetic
-Tenapanor or enema
-dec Na absorption = inc Na in gut
-Na in gut leads to inc water, accelerating poop

59
Q

Tenapanor

A

-Sodium/H exchanger inhibition
-prokinetic drug
-inc Na and water in gut

60
Q

Slide 70

A

prac question

61
Q

Drugs that REDUCE GI motility

A

-antidiarrheals
-anti-emetics

62
Q

Anti-diarrheals

A

-slow peristalsis to inc water and electrolyte absorption
-opiates
-5HT3 ANTAgonist

63
Q

Anti-diarrheal opiates

A

-inhibit presynaptic cholinergic nerves
-Diphenoxylate active in the CNS
-Loperamide (poorly cross BBB, act locally)

64
Q

5HT3 ANTAgonist

A

-anti-diarrheal
-alosetron
-ondansetron, franisetron, dolasteron, palonosetron
-blocks visceral afferent pain and dec motility
-contipation, ischemic colitis side effects

65
Q

Intrinsic primary

A
66
Q

Extrinsic prim afferent neuron

A

-nausea, vomiting, pain

67
Q

ENS neuron

A

-inc peristalsis

68
Q

-setrons (5th3 ANTAagonists) use

A

-nausea, vomiting associated w chemo
-seide effects constipation

69
Q

Anti-emetics

A

-NK1 ANTAgonists
-Antihistamines/anticholinergics

70
Q

NK1 ANTAgonists

A

-Aprepiant
-Netupitant
-Rolapitant
-receptors in chemo trigger zone
-combined w 5-HT2 ANTAgonists

71
Q

Antihistamines/anticholinergics

A

-H1 ANTAgonists and one muscarinic receptor antagonist
-PREVENT motion sickness
-anti-emetic

72
Q

H1 ANTAgonist anti-emetics

A

-dimenhydraminate (dramamine
-Meclizine (antivert)
-promethazine

73
Q

Scopolamine

A

-muscarinic receptor ANTAgonist
-PREVENT motion sickness with his H ANTAgonist buddies

74
Q

Anti-emetic drugs

A

-antihistamines/anticholinergics
-D2 ANTAgonists

75
Q

D2 ANTAgonists

A

-anti-emetic and sedative
-antimuscarinic and antihistamine effects
-can cause acute distonic reactions
-Metoclopramide (Reglan)
-Prochlorperazine = Compazine
-Droperidol (Inapsine)

76
Q

Opioid-induced constipation can also be avoided by using a biased agonist

A

-activation of opioid recptors in myenteric plexus
-dec smooth musc contractin
-inc rectal sphinter tone
-dec secretion
-block B arrestin inc analgesia

therapeutics (78 decks)

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