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GINME > Week 2: GI pharmacology > Flashcards

Week 2: GI pharmacology Flashcards

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

A
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22
Q

H3 receptor

A
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23
Q

H2 antagonists block what

A
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24
Q

H2 antagonists

A
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25
Q

Histamine H2 receptor antagonists prototypes and mechanism of action

A
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26
Q

H2 receptor antagonists pharmacokinetics

A
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27
Q

Therapeutic uses of H2 receptor antagonists

A
  • Promoting healing of gastric and duodenal ulcers
  • Treatment of GERD
28
Q

Adverse effects of H2 receptor antagonists

29
Q

Muscarinic receptor antagonists pathways blocked

30
Q

Muscarinic receptor antagonists receptor-targeted

A

most muscarininic antagonists are nonselective

the target to block acid secretion would be M1

31
Q

Selectivity of Muscarinic receptor antagonists

A

the only selective Muscarinic receptor antagonists in clinical use is pirenzipine for gastric ulcers

32
Q

Side effects of muscarinic antagonists

A

Significant cholinergic side effects so have largely been replaced by H2 receptor antagonists and H+ pump inhibitors

33
Q

Pirenzipine MOA

34
Q

Omeprazole brand name

35
Q

Omeprazole MOA

A

Proton pump inhibitor

36
Q

Structures of proton pump inhibitors

A

key structural feature is the Sulfer oxygen double bond

37
Q

Omeprazole activity/kinetics

A

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
Q

Parietal cell structure when at rest vs stimulated

A

when stimulated make a massive physical conformational change to form the intracellular caliculi to secrete

39
Q

Describe the accumulation of omeprazole

40
Q

Describe activation of omeprazole

A

low pH converts the prodrug to active form through proton catalyzed conversion

41
Q

Describe pump inhibition of omeprazole

A

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
Q

Omeprazole pathway

43
Q

The delivery system of omeprazole

A

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
Q

Absorption of Omeprazole

A

Rapid

Highly protein bound

45
Q

Metabolism of omeprazole

A

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
Q

Adverse effects of PPIs

47
Q

PPIs lableing change

48
Q

Emerging adverse effects of PPIs

49
Q

Mg2+ and PPIs

50
Q

PPIs vs H2 antagonists

51
Q

Drugs affecting gastric mucosal defense

52
Q

Misoprostol Brand

53
Q

Misoprostol MOA

54
Q

Adverse effects of Misoprostol

55
Q

Sucralfate MOA

56
Q

Adverse effects of sucralfate

57
Q

What is Bismuth Subsalicylate

A

Pepto-Bismol

58
Q

Pepto-Bismol drug name

A

Bismuth Subsalicylate

59
Q

Bismuth Subsalicylate MOA

60
Q

Bismuth Subsalicylate properties

61
Q

Uses of Bismuth Subsalicylate

A
  • Coats ulcers and erosions
  • Creates a protective layer against acid and pepsin
62
Q

Helicobacter pylori AKA

63
Q

H. pylori properties

64
Q

How are most ulcers cured?

A

Antibiotic therapy now cures most ulcers

65
Q

Therapy for H pylori

66
Q

GI Pharmacology summary

GINME (63 decks)

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