GI motility drugs Flashcards

1
Q

Location of emesis center

A

Medulla

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2
Q

Afferents of the emesis center

A

CTZ in area postrema
Vestibular apparatus
Vagal afferents via solitary tract nucleus

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3
Q

Activating receptors on the CTZ

A

Serotonin
5-HT3
Dopamine D2
Muscarinic M1

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4
Q

Substances released by vestibular apparatus to activate vomiting center

A

Ach
Histamine

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5
Q

Drug class of Hyoscine

A

Anticholinergic antiemetic

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6
Q

Drug class of scopolamine

A

Anticholinergic antiemetic

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7
Q

Drug class of dicyclomine

A

Anticholinergic antiemetic

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8
Q

Most effective drug for motion sickness

A

Hyoscine

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9
Q

Side effects of anticholinergic antiemetics

A

Sedation and dry mouth

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10
Q

Use of anticholinergic antiemetics

A

Motion sickness

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11
Q

H1 antihistamine with significant antimuscarinic acitivity

A

Promethazine

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12
Q

Drug class of promethazine

A

H1 antihistamine and D2 blocker

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13
Q

Drug class of Doxylamine

A

H1 antihistamine

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14
Q

Drug class of meclizine

A

H1 antihistamine

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15
Q

H1 antihistamine that is less sedative and has a longer duration of action

A

Meclizine

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16
Q

Duration of action of meclizine

A

24 hrs

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17
Q

Antiemetic available in a slow-release patch that lasts 72 hrs

A

Scopolamine

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18
Q

Drug class of cinnarizine

A

H1 antihistamine

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19
Q

Use of meclizine

A

Sea sickness

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20
Q

Uses of cinnarizine

A

Vertigo
Motion sickness

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21
Q

General uses of H1 antihistamine antiemetics

A

Motion sickness

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22
Q

General side effects of H1 antihistamine antiemetics

A

Sedation and dry mouth –> anticholinergic action

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23
Q

Drug class of chlorpromazine

A

D2 blocker (neuroleptic) antiemetic

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24
Q

Drug class of domperidone

A

D2 blocker (neuroleptic) antiemetic

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25
Q

Mechanism of D2 blocker antiemetics

A

D2 receptor antagonist that primarily acts on CTZ, as it does not cross the BBB

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26
Q

Drug class of ondansetron

A

First generation 5-HT3 antagonist

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27
Q

Drug class of Granisetron

A

First generation of 5-HT3 antagonist

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28
Q

Drug class of dolasetron

A

First generation 5-HT3 antagonist

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29
Q

Use and administration of first generation 5-HT3 antagonists

A

Given 3-5 days after chemotherapy for N/V

Also used for postoperative nausea

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30
Q

Drug class of palonosetron

A

Second generation 5-HT3 antagonist

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31
Q

5-HT3 antagonist with a longer duration of action

A

Palonosetron

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32
Q

Antiemetic that may prevent N/V for up to 7 days after chemotherapy, approved for treating both acute and delayed N/V

A

Palonosetron

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33
Q

Antiemetic drug class that prevents both peripheral and central stimulation of the vomiting center

A

5-HT3 antagonists

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34
Q

Drug class of aprepitant

A

NK1 receptor antagonist

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35
Q

Drug that blocks the emetic action of substance P at NK1 receptor

A

Aprepitant

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36
Q

Drug used for delayed phase vomiting (days 2-5) from cisplatin and for pts undergoing multiple chemotherapy cycles

A

Aprepitant

37
Q

Adjuvant antiemetics

A

Dexamethasone
Cannabinoids

38
Q

Drug class that is an agonist of CB1 receptor

A

Cannabinoids

39
Q

Types of cannabinoids

A

Dronabinol
Nabilone

40
Q

Drug class of metoclopramide

A

Prokinetic

41
Q

Drug used for gastroparesis or postop emptying delay that speeds up gastric emptying by enhancing coordinated propulsive motility

A

Metoclopramide

42
Q

Actions of metoclopramide

A

D2 antagonism
5-HT3 antagonism
5-HT4 agonism

43
Q

Drug that increases the release of Ach from cholinergic motor neurons in the enteric nervous system

A

Metoclopramide

44
Q

Main side effects of metoclopramide

A

Sedation
Dizziness
Loose stools
Muscle dystonias (children)

45
Q

Possible effects of long-term use of metoclopramide

A

Parkinsonism
Galactorrhea
Gynecomastia

46
Q

Macrolides used to promote gastric motility by stimulating motilin receptors

A

Erythromycin

47
Q

Anticancer drugs with high emetogenic potential

A

Cisplatin
Cyclophosphamide
Dacarbazine

48
Q

High emetic risk CINV acute phase treatment regimen

A

Combination of:
NK1 receptor antagonist
5-HT3 receptor antagonist
Dexamethasone

49
Q

Moderate and high emetic risk CINV delayed phase treatment

A

NK1 receptor antagonist
Dexamethasone

50
Q

Low and moderate emetic risk CINV acute phase treatment regimen

A

Combination of:
5-HT3 receptor antagonist
Dexamethasone

51
Q

NT that plays a vital role in promoting GI motility

A

Serotonin

52
Q

First line treatment for constipation

A

Diet and lifestyle modifications:
-Increased fiber intake
-Adequate fluid intake
-Regular exercise

53
Q

Examples of bulk-forming laxatives

A

Psyllium
Methylcellulose
Polycarbophil

54
Q

Preferred drug class for the management of chronic constipation because they can be used for a long time without noticeable side effects

A

Bulk-forming laxatives

55
Q

Examples of stool-softening laxatives

A

Docusate
Glycerin
Mineral oil

56
Q

Examples of osmotic laxatives

A

Magnesium oxide
Sorbitol
Lactulose
Magnesium citrate
Sodium phosphate
Polyethylene glycol

57
Q

Laxative used in hepatic encephalopathy associated with elevated blood ammonia levels

A

Lactulose

58
Q

Risk of excessive use of osmotic laxatives

A

Significant electrolyte and fluid loss

59
Q

Examples of stimulant/secretory laxatives

A

Aloe
Senna
Cascara
Castor oil
Bisacodyl

60
Q

Agent used for evacuating the bowel before surgery or examination that is available as a suppository

A

Bisacodyl

61
Q

Adverse effects of stimulant/secretory laxatives

A

Abdominal cramping
Significant electrolyte and fluid loss (long-term use)

62
Q

Examples of chloride channel activator laxatives

A

Lubiprostone
Linaclotide

63
Q

Example of opioid receptor antagonists used as laxatives

A

Methylnaltrexone
Alvimopan

64
Q

Examples of colloidal bulk forming substances used for diarrhea

A

Psyllium hydrophilic mucilloid
Calcium polycarbophil
Methyl cellulose

65
Q

Do colloidal bulk forming substances reduce water and electrolyte loss?

A

No

66
Q

Uses of colloidal bulk forming substances

A

Constipation and diarrhea phases of IBS

67
Q

Drug class of diphenoxylate and its brand name

A

Antimotility drug

Lomotil

68
Q

Drug class of loperamide and its brand name

A

Antimotility drug

Imodium

69
Q

Synthetic opioid that is chemically related to pethidine and mu opiate receptor agonist. Used exclusively as a constipating agent.

A

Diphenoxylate

70
Q

Adjuvant to diphenoxylate to discourage abuse by taking several tablets

A

Atropine

71
Q

Rare side effects of diphenoxylate

A

Respiratory depression
Paralytic ileus
Toxic megacolon (children)

72
Q

Mu opiate receptor agonist with poor water solubility limiting its intestinal absorption.

A

Loperamide

73
Q

Most effective antimotility drug for diarrhea that is available OTC.

A

Loperamide

74
Q

Adverse effects of loperamide

A

Paralytic ileus
Toxic megacolon (children <4 yo)

75
Q

Drug class contraindicated for use in acute infective diarrheas because they delay the clearance of pathogens from intestine

A

Antimotility drugs

76
Q

Drug class of racecadotril

A

Antisecretory antidiarrheal

77
Q

Enkephalinase inhibitor that prevents degradation of ENKs, which act as agonists on mu opioid receptors

A

Racecadotril

78
Q

Use of racecodotril

A

Acute secretory diarrheas

Can be used in children

79
Q

Disease characterized by progressive degeneration of ganglion cells in the myenteric plexus of the esophageal wall causing failure of LES relaxation and loss of peristalsis in distal esophagus

A

Achalasia

80
Q

Drugs used for treatment of achalasia

A

Nitrates
Nifedipine –> Ca channel blocker
Botox into LES

81
Q

A rare, acquired, premalignant disorder of the stomach characterized by large gastric folds due to overgrowth of mucous cells

A

Menetrier’s disease

82
Q

Symptoms of Menetrier’s disease

A

Epigastric pain
Hypoalbuminemia

83
Q

Possible associations of Menetrier’s disease

A

CMV
H pylori infection

84
Q

Monoclonal antibody used to treat Menetrier’s disease that blocks EGFR

A

Cetuximab

85
Q

Treatment options for Menetrier’s disease

A

PPI or H2 blocker
Albumin transfusion
Cetuximab
Treatment of underlying disease if present
Octreotide

86
Q

Somatostatin analogue that reduces EGFR signaling, used to treat Menetrier’s disease

A

Octreotide

87
Q

Antivirals used for treatment of CMV related Menetrier’s disease

A

Ganciclovir
Foscarnet

88
Q

Mechanism of Ganciclovir

A

Nucleoside analogue that inhibits DNA synthesis via chain termination

89
Q
A