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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
Omeprazole (prilosec) vs eSomeprazole (nexium
-omeprazole racemic -eSomeprazole is S enantiomer -more potent
25
PPI action
-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
26
Acid rebound
-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
27
PPI risks
-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
28
Vonoprazan
-PPI -K-competative acid blocker (P-CAB) -adbantages: faster acid suppresion, not prodrug, not influenced by meals, very stable in low pH
29
Mucosal Protective Agents
-Sucralfate (Carafate) -Misoprostol (Cytotec) -affect secretion
30
Sucralfate (carafate)
-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
Misoprostol
-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
Ulcers
-failure of mucosal protection -many associated w H. pylori infection (gram-neg)
33
H. Pylori eradication
-bismuth subsalicylate -antibiotic (metro, tetra, amox, clar) -H2 blocker or PPI -combo them
34
Bismuth subslicylate
-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
Drugs that INCREASE GI motility
-laxative -prokinetic drugs
36
Intrinsic nerve plexuses
-myenteric -submucosal -idk man watch the vid
37
Bulk and Osmotic ? Laxatives
-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
Bulk and osmotic laxative
-fibers -PEG3350 (miraLAX) -isosmotic electrolyte solutions with PEG 3350 (GoLytely) produce similar effects -Lactulose -Maltitol in some sugar free gummies
39
Fiber laxatives
-bulk and osmotic -psyllium (metamucil) -methylcellulose (citrucel) -calcium polycarbophil (fiberCon)
40
Types of laxatives
-bulk and osmotic -stool softeners -secrectory/stimulant
41
Lactulose
-non aborbable sugar -osmolytic effect -also fermeted by gut flora which inc peristalisis
42
Stool softener mech
-inc into stool to ease passage -dec water absorption -lube lower bowel -can dec absorption of fat-soluble vitamins
43
Stool softeners
-docusate sodium (Colace) -mineral oil -glycerin -surfactants and lubricants
44
Secretory/Stimulant laxatives mech
-poorly understood -irritation of mucosa affects fluid secretion/absorption balance and induces peristalsis
45
Secretory/stimulant laxatives
-castor oil -diphenylmethane derivatives (bisacodyl dulcolax) -anthraquinones (cascara, senna, aloes)
46
Castor oil
-stimulant lax -hydrolyzed in upper SI to ricinoleic acid
47
Common GI HYPOmotility disorders
-gastroparesis -ileus -opioid-induced constipation
48
Gastroparesis
-neuropathy during diabetes or Parkinson's disease
49
Ileus
-small bowels don't recover after surgery
50
Prokinetic drugs
-Metoclopramide (reglan) -Prucalopride (motegrity) -Tegaserod (Zelnorm) -Tenapanor -opioid ANTAgonists -chloride channel activators
51
Metoclopramide (Reglan)
-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
Opioid ANTAgonists
-Central: Naloxone (Narcan), Naltrexone, nalmefene -Peripheral: nalozegol, alvimopan, naldemedine
53
Prucalopride (Motegrity)
-5HT4 AGONIST -serotonin receptor = GPCR = inc cAMP = release AcH -treat chronic idiopathic constipation in adults
54
Tegaserod (Zelnorm)
-5HT4 AGONIST -treat IBS with constipation in WOMEN UNDER 65
55
Chloride channel activators
-prokinetic -inc chloride-rich fluid secretion into intestine -treat IBS + constipation -not systemic -lubiprostone and linaclotide
56
Lubiprostone
-type 2chloride channel activator in small intestine
57
Linaclotide and Plecanatide
-peptide activator of guanylate cyclase C
58
Sodium/hydrogen exchanger inhibition
-prokinetic -Tenapanor or enema -dec Na absorption = inc Na in gut -Na in gut leads to inc water, accelerating poop
59
Tenapanor
-Sodium/H exchanger inhibition -prokinetic drug -inc Na and water in gut
60
Slide 70
prac question
61
Drugs that REDUCE GI motility
-antidiarrheals -anti-emetics
62
Anti-diarrheals
-slow peristalsis to inc water and electrolyte absorption -opiates -5HT3 ANTAgonist
63
Anti-diarrheal opiates
-inhibit presynaptic cholinergic nerves -Diphenoxylate active in the CNS -Loperamide (poorly cross BBB, act locally)
64
5HT3 ANTAgonist
-anti-diarrheal -alosetron -ondansetron, franisetron, dolasteron, palonosetron -blocks visceral afferent pain and dec motility -contipation, ischemic colitis side effects
65
Intrinsic primary
66
Extrinsic prim afferent neuron
-nausea, vomiting, pain
67
ENS neuron
-inc peristalsis
68
-setrons (5th3 ANTAagonists) use
-nausea, vomiting associated w chemo -seide effects constipation
69
Anti-emetics
-NK1 ANTAgonists -Antihistamines/anticholinergics
70
NK1 ANTAgonists
-Aprepiant -Netupitant -Rolapitant -receptors in chemo trigger zone -combined w 5-HT2 ANTAgonists
71
Antihistamines/anticholinergics
-H1 ANTAgonists and one muscarinic receptor antagonist -PREVENT motion sickness -anti-emetic
72
H1 ANTAgonist anti-emetics
-dimenhydraminate (dramamine -Meclizine (antivert) -promethazine
73
Scopolamine
-muscarinic receptor ANTAgonist -PREVENT motion sickness with his H ANTAgonist buddies
74
Anti-emetic drugs
-antihistamines/anticholinergics -D2 ANTAgonists
75
D2 ANTAgonists
-anti-emetic and sedative -antimuscarinic and antihistamine effects -can cause acute distonic reactions -Metoclopramide (Reglan) -Prochlorperazine = Compazine -Droperidol (Inapsine)
76
Opioid-induced constipation can also be avoided by using a biased agonist
-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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