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GI Clinical Therapeutics Flashcards

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1
Q

What do PPIs do?

A

Decrease daily production of acid, both basal and stimulated

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2
Q

PPIs require activation by

A

H+ ion

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3
Q

What do PPIs bind to?

A

Irreversibly bind to sulfhydryl groups of cysteines in H+ K+ ATPase pumps

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4
Q

What are examples of PPIs?

A

Omeprazole, lasoprazole, rabeprazole, pantoprazole, dexlansoprazole

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5
Q

What are clinical indications for PPIs?

A
  • Tx of peptic ulcer disease, GERD
  • Used in conjugation with antibiotics to eradicate H. Pylori infections
  • Tx of pathological hypersecretory conditions (Zollinger-Ellisons)
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6
Q

How are PPIs eliminated?

A

By liver- need to monitor pts with hepatic disease

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7
Q

What are adverse effects of PPIs?

A

Nausea, abdominal pain, constipation, flatulence, diarrhea

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8
Q

PPIs have ______ adverse effects and a _____ TI

A

few; high

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9
Q

What are some drug-drug interactions with PPIs?

A
  • Warfarin
  • Diazepam
  • Methotrexate

(PPIs inhibit elimination)

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10
Q

Chronic treatment with PPIs can decrease the absorption of which vitamin?

A

B12

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11
Q

What type of patients will need twice daily dosing of a PPI?

A

Those with severe symptoms and nocturnal acid breakthrough

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12
Q

Severe GERD can cause

A

noncardiac chest pain, asthma, laryngitis, chronic cough, ear/nose/throat conditions, barretts esophagus

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13
Q

Chronic treatment of a PPI can elevate gastrin
production which can significantly elevate

A

histamine release from the ECL cell

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14
Q

Once the PPI is withdrawn, what can occur?

A

Excessive acid secretion (rebound acid hypersecretion)

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15
Q

Chronic treatment of PPIs has been associated with:

A
  • Increased risk of bone fracture
  • Increased susceptibility to certain infections
  • Hypergastrinemia
  • Hypomagnesemia
  • Chronic kidney disease
  • Dementia
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16
Q

Histamine from the ECL cell will bind to H2R and cause

A

increase in cAMP

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17
Q

H2R antagonists are

A

reversible and lower cAMP production

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18
Q

What are H2R antagonist examples?

A

Cimetidine, Famotidine and Nizatidine

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19
Q

H2R antagonists block the production of cAMP and lower the

A

H+K+ ATPase pumps on apical membrane of parietal cells

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20
Q

What is the MOA of H2R antagonists?

A

Block histamine action of H2R on parietal cells

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21
Q

What is the absorption of H2R antagonists like?

A

rapid and very little of drug is protein bound in plasma

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22
Q

How are H2R antagonists excreted?

A

In kidneys by filtration and renal tubular secretion

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23
Q

What are clinical indications for the use of H2R antagonists?

A
  • Promote mucosal healing from gastric and duodenal ulcers (H. pylori)
  • Uncomplicated GERD
  • Prevent stress ulcers
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24
Q

What are typical side effects of H2R antagonists?

A

Diarrhea, headache, fatigue, muscular pain and constipation

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25
H2R antagonists can cross the
placenta and are excreted in breast milk
26
Cimetidine inhibits
CYPs and can icnrease level of a variety of drugs
27
How do cytoprotectives work by?
Promoting prostaglandins or somatostatin to help increase bicarb secretion, mucus production and inhibition of acid secretion
28
What are cytoprotective examples?
Misoprostol and sucralfate
29
Misoprostol, dinoprostone is used to prevent what?
NSAID induced mucosal injury
30
Misoprostol, dinoprostone binds to what receptor?
EP3 on parietal cells to stimulate Gi pathway
31
Misoprostol, dinoprostone helps to increase
mucin production, bicard secretion and mucosal blood flow
32
What are adverse effects of Misoprostol, dinoprostone?
Diarrhea, exacerbated IBD, DONT USE IN PREGNANCY (UTERINE CTXS)
33
What are the MOAs of sucralfate?
- Reacts with HCl to form cross links and make acid buffer - Acts as protective barrier to prevent damage by acid, pepsin, bile
34
What are clinical indications for sucralfate?
Short term treatment of active duodenal ulcers
35
What are adverse effects of sucralfate?
Constipation, block absorption of other drugs, may promote bezoars in some
36
Ocreotide (somatostatin analog) can inhibit
intestinal and pancreatic secretions
37
What is octreotide used for?
Tx of severe diarrhea associated with metastatic carcinoid tumor in adults. ALso acromegaly, acute variceal bleeding, GI fistula and acute pancreatitis
38
What are adverse effects of octreotide?
Nausea, abdominal cramping, steatorrhea and gall stones
39
Antacids neutralize
gastric acid and inhibit pepsin activity
40
Antacids have rapid action by neutralizing
gastric Hcl and increasing gastric pH
41
Antacids are composed of
inorganic salts
42
Aluminum only based antacids can cause
constipation
43
Magnesium only based antacids can cause
diarrhea
44
Simethicone is a surfactant that can
reduce the surface tension of gas bubbles and can be found in most antacids
45
Absorbable bicarbonate can increase blood and urine pH causing transient
metabolic alkalosis
46
What type of drug is amoxicillin?
Beta lactam (inhibits cross linkage of peptidoglycan polymer chains to disrupt bacterial wall synthesis)
47
What type of drug is clarithromycin?
Macrolide
48
Decreasing acid production in stomach, can allow for
bacterial overgrowth
49
Patients on PPIs have icnreased risk of developing
community acquired pneumonia
50
Zollinger Ellison Syndrome has increased _______ secretion due to___
gastric acid; gastrin releasing tumor
51
What are tx for ZOllinger Ellison Syndrome?
- Surgery to remove gastrinoma is best - Chronic PPIs
52
Drugs used to treat symptoms of gastroparesis include
- Dopamine antagonists - Macrolide antibiotics (erythromycin) - Cholinomimetics or acetylcholinesterase inhibitors
53
Erythromycin can ast as a
motilin mimetic
54
Erythromycin can be used to induce antral contractions and used short term in patients with
gastroparesis
55
What are adverse effects of erythromycin?
Prolonged QT interval (abnormal heart rhythms need to be monitored)
56
Bethanechol increases smooth muscle tone in the GI tract via what receptors?
M3
57
Bethanechol is typically used following what?
Abdominal surgery (also used to tx urinary retention)
58
Bethnechol does not have any
nicotinic action
59
Who should bethanechol not be used on?
Pts with a bowel obstruction or patient with IBD
60
Neostigmine is a
reversible AchE inhibitor
61
What is neostigmine used for?
Paralytic ileus and urinary bladder atony
62
Dopamine inhibits
motility in upper GI
63
Dopamine stimulates
motility in colon
64
What are adverse effects of dopamine?
anxiety, confusion, dystonia and tardive dyskinesi
65
What are other effects of dopamine?
elevate prolactin levels and induce galactorrhea, gynecomastia, amenorrhea and impotence
66
In patients with enterohemorrhagic E. coli, antibiotics need to be avoided due to risk of
hemolytic uremic syndrome
67
What can be used for traveler's diarrhea?
- Fluoroquinolone antibiotics - Azithromycin, rifaximin, trimethoprim Bismuth subsalicylate - Azithro for children
68
What is an adverse effect of bismuth subsalicylate?
Dark stool and black staining of tongue due to the sulfur
69
Why shpould children not take bismuth subsalicylate?
It can cause Reye syndrome and CNS effects like hearing loss and tinnitus
70
Opioids can cause constipation and they do this through inhibiting
intestinal motility, intestinal secretion or absorption
71
Diphenoxylate, difenoxin, and loperamide are examples of
opioids used in diarrhea
72
In patients with active IBD, loperamide should be used with great caution to avoid development of
toxic megacolon
73
Diphenoxylate and difenoxin are listed as
schedule V controlled substances
74
Crofelemer is only used in
Tx of diarrhea associated with ART for HIV/AIDS
75
How does crofelemer work?
Blocking Cl channels on enterocyte and reduces water loss associated with Cl secretion
76
What are adverse effects of crofelemer?
Upper respiratory tract infection, bronchitis, cough, flatulence, nausea
77
Antispasmodics are useful in the treamtent of
IBS-D
78
Antispasmodics are
muscarinic antagonists (M1 and M2)

Systems 1 (40 decks)

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