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GINME > Week 2: GI pharmacology > Flashcards

Week 2: GI pharmacology Flashcards

(66 cards)

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1
Q

Objectives

A
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2
Q

Cl- and HCO3 antiporter

A
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3
Q

What powers the HCO3 Cl- antiporter

A
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4
Q

Cellular mechanism of acid production

A
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5
Q

Stimulants of gastric acid secretion

A
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6
Q

Therapeutic targets to inhibit gastric acid secretion

5 listed

A
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7
Q

What are some common antiacids?

4 listed

A
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8
Q

Antacids that can cause belching

A

CaCO3

NaHCO3

because CO2 is produced

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9
Q

CaCO3 antacid brand name

A

TUMS

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10
Q

How much Ca2+ is absorbed by taking tums

A

10% of the Ca2+ is absorbed

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11
Q

Too much CaCo3 can result in?

A

Hypercalcemia can lead to kidney failure

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12
Q

NaHCO3 brand name

A

Alka Seltzer

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13
Q

NaHCO3 benefits

A
  • Very soluble, very fast-acting
  • Rapidly removed from the gut
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14
Q

Too much NaHCO3 can result in?

A
  • Systemic alkalosis
  • fluid retention
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15
Q

Al(OH)3 benefits

A

Insoluble aluminum chloride salt formed after neutralizing acid

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16
Q

Too much Al(OH)3 can result in?

A

Constipation

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17
Q

Mg(OH)2 benefits

A
  • Relatively insoluble
  • longer acting in stomach
  • relatively little absorption of Mg2+
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18
Q

Too much Mg(OH)2 can result in?

A

Laxative effect

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19
Q

Maalox and Mylanta are?

A

Al(OH)3 + Mg(OH)2 mixed together to neutralize the constipation and laxative effects each would have alone respectively

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20
Q

H1 receptor

A
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21
Q

H2 receptor

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22
Q

H3 receptor

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23
Q

H2 antagonists block what

A
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24
Q

H2 antagonists

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25
Histamine H2 receptor antagonists prototypes and mechanism of action
26
H2 receptor antagonists pharmacokinetics
27
Therapeutic uses of H2 receptor antagonists
* Promoting healing of gastric and duodenal ulcers * Treatment of GERD
28
Adverse effects of H2 receptor antagonists
29
Muscarinic receptor antagonists pathways blocked
30
Muscarinic receptor antagonists receptor-targeted
most muscarininic antagonists are nonselective the target to block acid secretion would be M1
31
Selectivity of Muscarinic receptor antagonists
the only selective Muscarinic receptor antagonists in clinical use is pirenzipine for gastric ulcers
32
Side effects of muscarinic antagonists
Significant cholinergic side effects so have largely been replaced by H2 receptor antagonists and H+ pump inhibitors
33
Pirenzipine MOA
34
Omeprazole brand name
Prilosec
35
Omeprazole MOA
Proton pump inhibitor
36
Structures of proton pump inhibitors
key structural feature is the Sulfer oxygen double bond
37
Omeprazole activity/kinetics
Is a prodrug so it enters parietal cell from circulation Omeprazole is a weak base and will accumulate in acidic environments such as the secretory canaliculi
38
Parietal cell structure when at rest vs stimulated
when stimulated make a massive physical conformational change to form the intracellular caliculi to secrete
39
Describe the accumulation of omeprazole
40
Describe activation of omeprazole
low pH converts the prodrug to active form through proton catalyzed conversion
41
Describe pump inhibition of omeprazole
covalent modification is nonreversible so the cell must endocytose the covalently inhibited pump and perform de novo synthesis 18hrs on average Cysteine 813 irreversible modification
42
Omeprazole pathway
43
The delivery system of omeprazole
important that the capsule only dissolves at an alkaline pH which would allow it to be absorbed in the small intestine and not degraded in the stomach or esophagus because it would be wasted
44
Absorption of Omeprazole
Rapid Highly protein bound
45
Metabolism of omeprazole
Extensively metabolized in the liver by cytochrome p450 Plasma half-life is 1-2 hrs but durations of action is much longer due to the irreversible inhibition
46
Adverse effects of PPIs
47
PPIs lableing change
48
Emerging adverse effects of PPIs
49
Mg2+ and PPIs
50
PPIs vs H2 antagonists
51
Drugs affecting gastric mucosal defense
52
Misoprostol Brand
Cytotec
53
Misoprostol MOA
54
Adverse effects of Misoprostol
55
Sucralfate MOA
56
Adverse effects of sucralfate
57
What is Bismuth Subsalicylate
Pepto-Bismol
58
Pepto-Bismol drug name
Bismuth Subsalicylate
59
Bismuth Subsalicylate MOA
60
Bismuth Subsalicylate properties
61
Uses of Bismuth Subsalicylate
* Coats ulcers and erosions * Creates a protective layer against acid and pepsin
62
Helicobacter pylori AKA
H pylori
63
H. pylori properties
64
How are most ulcers cured?
Antibiotic therapy now cures most ulcers
65
Therapy for H pylori
66
GI Pharmacology summary

GINME (63 decks)

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