PHARM: Overview of GI Pharm Flashcards

1
Q

Effect of SNS on walls of GI tract. (what receptors)

A

Relaxes via alpha-2, beta-2 (probably through presynaptic inhibition of parasympathetic activity)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Effect of SNS on sphincters of GI tract. (what receptors)

A

Contracts via alpha-1 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Effect of SNS on GI tract secretions.

A

NONE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Effect of PSNS on walls of GI tract. (what receptors)

A

Contracts via M3 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Effect of PSNS on sphincters of GI tract. (what receptors)

A

Relaxes via M3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Effect of PSNS on GI tract secretions. (what receptors)

A

increases via M3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is the predominant tone of the GI tract?

A

parasympathetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the major GI side effect of Cholinergic Agonists and Acetylcholinesterase inhibitors?

A

diarrhea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the major GI side effects of muscarinic antagonists?

A

constipation and decreased glandular secretions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Which type of muscarinic antagonists can cross the BBB? What is the consequence?

A

tertiary (confusion, delirium, etc.)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What controls the GI system?

A

enteric nervous system

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what are the two components of the enteric nervous system?

A

Myenteric Plexus

Submucosal Plexus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is another name for the Myenteric plexus?

A

Auerbach’s

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is another name for the submucosal plexus?

A

Meissner’s

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What plexus controls contraction and relaxation of the GI smooth muscle?

A

Myenteric (Auerbach’s)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What plexus is involved with secretory and absorptive functions of the GI epithelium, local blood flow, and neuro-immune activities?

A

Submucosal (Meissner’s)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is principle neurotransimtter of the enteric nervous system?

A

acetylcholine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is “enkephalin”?

A

opiod peptide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What do opiod peptides do in the ENS?

A

inhibit Ach release and peristalsis while possibly stimulating secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Other than Ach, what is an important transmitter at the neuron-to-neuron junctions in the ENS?

A

Serotonin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What receptors does serotonin use in the GI?

A

5HT-3 and 5HT-4

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What type of receptors are D2?

A

dopamine receptors on muscle

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Where are D2 muscular receptors located?

A

lower esophageal sphincter and the antrum/fundus of the stomach

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What are the actions of dopamine on the D2 receptors?

A

relaxes LES/antum/fundus AND it has indirect inhibitory effect on the musculature of the GI system

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

How does dopamine indirectly inhibit musculature of the GI system?

A

inhibiting Ach release from intrinsic cholinergic motor neurons by activating pre-junctional D2 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

How can you reverse the dopaminergic inhibition of GI musculature?

A

giving drug that has anti-domaminergic and serotonergic actions (have pre-junctional excitatory 5-HT4 receptors that will stimulate GI motility)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What drug has a mixed anti-dopaminergic and serotoninergic effect?

A

Metoclopramide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

What does Metoclopramide do?

A

increase lower esophageal tone and stimulate antral and small intestinal contractions

29
Q

Which receptors are inhibited by metoclopramide? What are their normal actions that are being inhibited by this drug?

A

5-HT3 (inhibits Ach release and relaxes SM)

D2 (inhibits cholinergic signals and decreases SM contraction)

30
Q

Which receptors are stimulated by metoclopramide? What are their normal actions that are sitmualted by this drug?

A

5-HT4 (stimulates Ach release and SM contraction)

31
Q

What is the major feature of UC?

A

disruption of physical barrier

32
Q

How do you treat UC?

A
  • Glucocorticoids
  • Infliximab
  • Adalimumab/Golimumab (as indicated)
33
Q

What is the underlying feature of Crohn’s disease?

A

microbe sensing dysfunction

34
Q

How do you treat Crohn’s disease?

A
  • Glucocorticoid/ Immunomodulator

- TNF-alpha mAb’s

35
Q

What type of inflammatory reaction is seen in IBD?

A

TNF-alpha mediated

36
Q

What do the TNF-alpha mAb’s do?

A

block the interaction between TNF-alpha molecules and the TNF-alpha type 1 and type 2 (and soluble) receptors to neutralize the pro-inflammatory signal and inhibit expression of inflammatory genes

37
Q

What is a major adverse effect of opiates?

A

constipation

38
Q

What should always be prescribed with opiates?

A

laxative agent (or opiate antagonists)

39
Q

What is the ONLY mu-specific opiod antagonist?

A

alvimopan

40
Q

What are the major pharmacological effects of opiods in the GI?

A

increase tone, increase absorption, decrease secretions (so constipation and cramping)

41
Q

True or false: GI tract events are the most common type of preventable adverse drug event in older ambulatory persons

A

TRUE

42
Q

What type of diarrhea is caused by: Medications draw water into GI tract

A

osmotic

43
Q

What type of diarrhea is caused by: Na+ absorption is impaired and Cl- and HCO3 ions are secreted into the GI lumen (pull in H2O)

A

secretory

44
Q

What type of diarrhea is caused by: Drugs affect cholinergic tone

A

disordered motility

45
Q

What type of diarrhea is caused by: Disruption of colonic flora precipitating C. difficile colitis or following direct damage of the gastric mucosa. Risk increases with duration of antibiotic exposure or NG tube.

A

inflammatory

46
Q

What type of diarrhea is caused by: Disrupting the acid-base environment or epithelial homeostasis

A

C. difficile diarrhea

47
Q

What type of diarrhea is caused by: Mal-digestion or absorption by virtue of a drug’s mechanism of action.

A

steatorrhea (fatty diarrhea)

48
Q

What type of diarrhea do the following drugs cause: Metformin, antibiotics, anticholinergics, NSAIDs, calcitonin

A

secretory diarrhea

49
Q

What type of diarrhea do the following drugs cause: Antibiotics, chemotherapy agents; immunosuppressants; PPIs; TKIs; SSRIs; NSAIDs

A

Inflammatory diarrhea

50
Q

What type of diarrhea do the following drugs cause: NSAIDS (direct epithelial damage and changes in Na+ permeability).

A

C. difficile diarrhea

51
Q

What type of diarrhea do the following drugs cause: alpha-glucosidase inhibitors

A

osmotic diarrhea

52
Q

What type of diarrhea do the following drugs cause: Metformin (decrease glucose absorption); Octreotide; Orlistat (Alli); Cholestyramine

A

Steatorrhea

53
Q

What type of diarrhea do the following drugs cause: Cholinergic drugs; macrolides

A

disordered motility

54
Q

Why is vancomycin good for treating C. difficile?

A

it gets very high in concentration in the GI tract (because it does not get absorbed)

55
Q

What is the name for the condition in which there is a feeling that a pill is stuck in throat +/- burning and retrosternal pain?

A

pill-induced esophagitis

56
Q

What is common among risk factors for pill-induced esophagitis?

A

decreased saliva (ex. old age, anticholinergics)

57
Q

What pills might give worse proglems with pill-induced esophagitis?

A

gelatin capsules and extended- or sustained-release products

58
Q

What two metabolic components are found in the intestinal wall where they modulate bioavailability and participate in the 1st pass metabolism of various drugs?

A

CYP3A and P-GP

59
Q

What is P-GP?

A

energy-dependent pump located in small intestine epithelial cells (kidney, BBB, placenta, etc.) and decreases bioavailability by pumping back into lumen.

60
Q

What happens when you decrease P-GP?

A

drug bioavailability will INCREASE (because drug is not being pumped back into lumen)

61
Q

What may control CYP3A?

A

P-gp/MDR1

62
Q

What is the connection between CYP3A and P-gp/MDR1 ?

A

P-gp/MDR1 works to pump drugs back into the lumen after passive absorption to be presented to CYP3A4 over and over (increasing the change it will be metabolized)

63
Q

Why do NSAIDs cause gastric ulcers?

A

decrease PGs and prevent the release of protective mucous by GI epithelial cells

64
Q

What are the 3 main drug classes for altering acidity?

A

Antacids
PPIs
H2 Histamine blockers

65
Q

What is the MOA of antacids?

A

alter pH and chelate (bind up and prevent absorption of drugs like antibiotics)

66
Q

What is the MOA of PPIs?

A

alter pH and inhibit CYP2C19

67
Q

What ist he MOA of H2 histamine blockers?

A

alter pH and inhibit CYPs (cimetidine)

68
Q

What substance has been indicated in the inflammatory response of migraine headaches?

A

CGRP