PHRM 825 > GI System > Flashcards

GI System Flashcards

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1
Q

Which categories of drugs affect gastric secretion?

A
  • antacids
  • H2 histamine receptor antagonists
  • Proton pump inhibitors
  • Protectants
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2
Q

Which categories of drugs increase GI motility?

A
  • laxatives
  • prokinetic drugs
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3
Q

Which categories of drugs reduce GI motility?

A
  • antidiarrheals
  • anti-emetics
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4
Q

Which salts have high neutralizing capacities?

A
  • NaHCO3
  • Al(OH)3
  • Mg(OH)2
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5
Q

Which salt has a moderate neutralizing capacity?

A

CaCO3

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6
Q

What are the side effects from NaHCO3?

A
  • systemic alkalosis
  • fluid retention
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7
Q

What are the side effects of CaCO3?

A
  • hypercalcemia
  • nephrolithiasis (kidney stones)
  • milk-alkali syndrome
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8
Q

What are the side effects of Al(OH)3?

A
  • constipation
  • hypophosphatemia
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9
Q

What are the side effects of Mg(OH)2?

A

Diarrhea

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10
Q

What is the brand name of CaCO3?

A

Tums

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11
Q

What is the brand name of NaHCO3?

A

Alka-Seltzer

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12
Q

What is the brand name of Mg(OH)2 + Al(OH)3?

A

Maalox

Mylanta

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13
Q

What is the brand name of Al(OH)3?

A

AlternaGEL

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14
Q

What is the brand name of CaCO3 + Mg(OH)2?

A

Rolaids

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15
Q

What is the brand name of Al(OH)3 + MgCO3?

A

Gaviscon

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16
Q

List the 2nd generation H2 blockers?

A
  • ranitidine
  • nizatidine
  • famotidine
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17
Q

What are the benefits of the 2nd gen H2 blockers?

A
  • longer half-life (HS vs BID dosing)
  • greater potency
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18
Q

What is the brand name of cimetidine?

A

Tagamet

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19
Q

What is the brand name of ranitidine?

A

Zantac

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20
Q

What is the brand name of nizatidine?

A

Axid

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21
Q

What is the brand name of famotidine?

A

Pepcid

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22
Q

What does omeprazole have to be converted to in order to become active?

A

sulfenic acid

PPIs are prodrugs

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23
Q

What do PPIs inhibit?

A

H+,K+-ATPase

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24
Q

Explain the mechanism of action of PPIs:

A
  1. Prodrug diffuses into the parietal cells of the stomach
  2. Activated by formation of sulfenamide
  3. Activated form binds with the sulfhydryl groups of cysteines in the H+,K+-ATPase which irreversibly inactivates the pump
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25
What is the possible result of hypergastrinemia from PPI use?
- may result in rebound hypersecretion of gastric acid upon drug withdrawal
26
Why can long-term use of PPIs increase risk of infections?
The job of the acidic environment of the stomach is to sterilize things. Without the drops in pH, overgrowth can occur.
27
Why can long-term use of PPIs lead to B12 deficiency?
Gastric acid and pepsin are essential to liberate B12 from the proteins in food that bind it tightly.
28
Recognize the chemical structure of PPIs
--
29
List the mucosal protective agents:
- sucralfate (carafate) - misoprostol (cytotec)
30
What is the mechanism of action of sucralfate?
Polymerizes and forms protective barrier at ulcer site
31
what is the mechanism of action of misoprostol?
- misoprostol is a prostaglandin E1 derivative - it decreases gastric acid secretion and replaces the protective prostaglandins
32
Why are ulcers treated with antibiotics?
Many peptic ulcers are associated with infection of the gastric mucosa by H. pylori. | gram-negative bacilli
33
Which antibiotics are used for H. pylori infections?
- metronidazole - tetracycline - amoxicillin - clarithromycin
34
Brand name of omeprazole:
Prilosec
35
Brand name of esomeprazole:
Nexium
36
Brand name of lansoprazole:
Prevacid
37
Brand name of rabeprazole:
Aciphex
38
Brand name of pantoprazole:
Protonix
39
Brand name of dexlansoprazole:
Dexilant
40
What is bismuth subsalicylate used for?
- part of multi-drug therapy for H. pylori eradication - nausea - heartburn - indigestion - upset stomach - diarrhea
41
What are examples of bulk-forming laxatives?
- psyllium (metamucil) - methylcellulose (citrucel)
42
-What is the MOA of bulk-forming laxatives?
- indigestible, hydrophilic colloids that absorb water, forming a bulky, emollient gel that distends the colon and promotes peristalsis
43
List examples of stool softeners:
- docusate - mineral oil
44
What is the mechanism of action of stool softeners?
- incorporate into stool to make passage easier and decrease water absorption - lubricates lower bowel to reduce fecal impaction
45
What is the MOA of osmotic laxatives?
- increase water in the intestinal lumen by osmotic force, leading to distention and an increase in peristalsis
46
What is an example of an osmotic laxative?
PEG 3350 (MiraLAX)
47
What is an example of a stimulant laxative?
- Bisacodyl (Dolculax)
48
List an example of an anthraquinone laxative:
- Senna
49
What is the MOA of metoclopramide (a prokinetic drug)?
blockade of D2 receptors in the myenteric plexus leads to increase ACh release
50
What are examples of opioid receptor antagonists used for opioid-induced constipation?
- naloxegol - naldemedine
51
Explain the MOA of prucalopide (Motegrity): | This is also the mechanism for Tegaserod (Zelnorm).
- 5HT4 agonist - the serotonin receptor is a GPCR that is Gs coupled - Activation leads to increased cAMP --> PKA activation --> release of ACh
52
What is the MOA of the chloride channel activator lubiprostone?
- Drug binds to Gs coupled GPCR. - This leads to enhances apical Cl conductance. - The drug promotes the secretion of a chloride-rich fluid which thereby improves stool consistency, frequency, and activates motility.
53
What is the MOA of guanylate cyclase C prokinetic drugs?
Activates guanylate cyclase C (GC-C) which results in increased synthesis of cGMP. Increased cGMP results in enhanced chloride and bicarbonate secretion into the intestinal lumen which then leads to water secretion and enhanced motility. | linaclotide and plecanatide
54
What is the MOA of tenapanor?
Inhibits the Na+-H+ exchanger which reduces the absorption of Na+ and enhances intestinal fluid volume and transit
55
List the anti-diarrheal opiates:
- diphenoxylate + atropine (lomotil) - loperamide (imodium)
56
What is the MOA of anti-diarrheal opiates?
- inhibition of presynaptic cholinergic nerves to slow peristalsis
57
What is the MOA of alosetron (lotronex)?
- alosetron is a 5HT3 receptor antagonist that blocks visceral afferent pain sensation and decreases colon motility
58
What is the MOA of ondansetron?
block activity of afferent nerves from stomach and small intestine which activate the trigger center in the CNS
59
What is an example of NK1 antagonist anti-emetic?
aprepitant
60
What is an example of an antihistamine anti-emetic?
- dimenhydrinate - meclizine
61
What is an example of an anticholinergic anti-emetic?
- scopolamine
62
What is an example of an antipsychotic (D2 dopamine receptor antagonist) anti-emetic?
- metoclopramide - prochlorperazine - promethazine - droperidol
PHRM 825
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