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Pharmacology > GI > Flashcards

GI Flashcards

1
Q

Scopolamine is a

A

Cholinergic Antagonist

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2
Q

Scopolamine can come in what forms?

A

patch and injectable

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3
Q

Scopolamine mechanism of action

A

Blocks the acetylcholine at parasympathetic sites (smooth muscle, secretary glands, CNS)

Reduces histamine and serotonin activity

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4
Q

Scopolamine onset and duration

A

onset - 6-8 hours
duration - 72 hours

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5
Q

Scopolamine side effects

A

similar effect to atropine - bradycardia then tachycardia, flushing, orthostatic hypotension, cognitive impairment, psychosis and hallucinations

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6
Q

Scopolamine is contraindicated in

A

narrow angle glaucoma

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7
Q

Phenothiazines
Butyrophenones
Benzamides are all

A

Dopamine receptor antagonists

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8
Q

Phenothiazine include

A

Prochlorperazine

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9
Q

Butyrophenones include

A

Haloperidol
Droperidol

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10
Q

Benzamides include

A

Metoclopramide
Thrimethobenzamide

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11
Q

MOA for Dopamine receptor antagonists

A

acts primarily on the CTZ and afferent pathways in the gut
Antagonize D2 dopamine receptors in area postrema and peripheral sites
M1-muscarinic and H1-histamine blocking effects
Metoclopramide has weak 5-HT3 blockage at higher doses

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12
Q

Side effects of Dopamine receptor antagonists

A

Extrapyramidal reactions (Dystonia), tardive dyskinesia, QT prolongation, CNS/psych effects, hyperprolactinemia, Hypotension

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13
Q

Prochlorperazine onset and duration

A

onset - PO = 30-40 min
rectal approximately 60 min

Duration = 3-4 hours oral, 3-12 rectal

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14
Q

Metoclopramide duration

A

1-2 hours

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15
Q

Ondansetron and Granisetron are

A

Serotonin receptor antagonists

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16
Q

Ondansetron MOA

A

Blocks serotonin centrally and peripherally

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17
Q

Ondansetron onset and peak

A

onset = approx 30 min
peak = 1-2 hours

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18
Q

Ondansetron side effects

A

QT prolongation, dizziness, confusion, SOB, constipation

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19
Q

Ondansetron major interactions

A

amiodarone
QT prolonging agents
CYP3A4

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20
Q

Cannabinoids MOA

A

activates cannabinoid receptors

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21
Q

Cannabinoids onset, peak, duration

A

onset - 30-60 min
peak - 2-4 hours
duration - 4-6 hours

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22
Q

Cannabinoids side effects

A

euphoria
CNS changes
abdominal pain
vomiting
flushing
palpitations
hypotension
xerostomia
vertigo

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23
Q

Promethazine
Meclizine
Dimenhydrinate

A

Histamine antagonists

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24
Q

Promethazine MOA

A

blocks mesolimbic dopaminergic receptors in postsynaptic sites
Blocks the release of hormones from the hypothalamus
Blocks histamine 1 receptors in the brainstem

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25
Q

Promethazine Onset and duration

A

onset - IV ~5 min, PO/IM ~ 20 min
duration - 4-6 hours

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26
Q

Promethazine Side effects

A

EKG changes, anticholinergic effects, CNS depression, orthostatic hypotension

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27
Q

Meclizine MOA

A

Blocks HI histamine receptor and prevents vasodilation, increased capillary permeability, bronchoconstriction and spasmodic contraction of GI smooth muscles
depresses labyrinth excitability and vestibular stimulation

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28
Q

Meclizine onset and duration

A

onset - 1 hour
duration - ~24 hours

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29
Q

Meclizine side effects

A

sedation
HA
vomiting
blurred vision

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30
Q

Meclizine avoid in

A

glaucoma, asthma, urinary retention, or pyloric/duodenal obstruction

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31
Q

Dimenhydrinate MOA

A

binds to H1 receptor sites in peripheral sites including GI tract, resp tract, and blood vessels
blocks chemoreceptor trigger zones
Depresses labyrinthine function and vestibular stimulation
Central anticholinergic activity

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32
Q

Dimenhydrinate onset and duration

A

onset = up to 30 min for IM and PO
duration = 4-6 hours

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33
Q

Dimenhydrinate rarely causes

A

SJS

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34
Q

Dimenhydrinate do not use with

A

abx that are known to cause ototoxicity

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35
Q

Opioid Agonists
Serotonin receptor modulators
bile acid sequestrants
anti-spasmodics
antimicrobial agents
Can all be used for

A

Diarrhea and IBS-D

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36
Q

MOA Opioid Agonists

A

Activation of opioid receptors in the smooth muscle of the GI tract. Alters peristalsis by preventing smooth muscle contraction and relaxation. Reduces stool volume and can prevent electrolyte depletion

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37
Q

before using opioid agonists you should correct any

A

fluid/electrolyte imbalances

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38
Q

Do not use opioid agonists with

A

infectious diarrhea/toxic megacolon

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39
Q

Loperamide
Diphenoxylate/Atropine
Octreotide
Eluxadoline are all

A

opioid compound drugs

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40
Q

MOA Loperamide

A

also increases IAS and EAS tone

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41
Q

Diphenoxylate/ atropine - why does it contain atropine

A

contains small amount of atropine to prevent abuse

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42
Q

Octreotide MOA

A

Inhibits serotonin release
inhibits secretion of gastrin, VIP, insulin, glucagon, secretin, motilin and pancreatic polypeptide

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43
Q

MOA Eluxadoline

A

Binds to mu, kappa and delta opioid receptors in the intestinal lumen
decreases intestinal motility without causing constipation

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44
Q

Eluxadoline considerations

A

can cause acute pancreatitis in pts with cholecystectomy
Do not give to pts with EtOH abuse
do not use in pts with h/o intestinal obstruction
can cause CNS depression

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45
Q

Alosetron
Tegaserod are

A

serotonin receptor modulators

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46
Q

Alosetron is used for

A

chronic >6 months severe IBS-D

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47
Q

Alosetron MOA

A

selective 5-HT3 agonist
acts on receptors in the enteric neurons in addition to receptors in other locations centrally and peripherally
affects visceral pain, colonic transit, and alters secretions in the GI tract

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48
Q

Alosetron can rarely cause

A

ischemic colitis
do not use in pts with h/o GI obstruction, crohns, diverticulitis, vasculopathy, thrombophlebitis, hypercoagulable conditions

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49
Q

Alosetron instructions

A

take on an empty stomach to increase absorption

50
Q

MOA of bile acid sequestrants

A

Bind to bile salts in the intestine
inhibits reuptake of bile salts
increases fetal loss of bile salt bound LDL cholesterol

51
Q

Bile acid sequestrants instructions

A

do not administer within 4-6 hours of other medications - may interfere with absorption

52
Q

Rifaximin
Metronidazole
Ciprofloxacin
Amoxicillin
Neomycin

A

Antimicrobials

53
Q

Hyoscyamine
Dicyclomine are

A

anti-spasmodics

54
Q

MOA anti-spasmodics

A

Blocks acetylcholine at parasympathetic receptors
Antagonist of histamine and serotonin

55
Q

Contraindications of anti-spasmodics

A

MG
hypersensitivity to delladonna
UC
myocardial ischemia

56
Q

Isosmotic
Hyperosmotic
stimulant laxatives are all types of

A

bowel preps

57
Q

Isosmotic Preps are the

A

PEG (polyethylene glycol) based electrolyte lavage solutions

58
Q

PEG MOA

A

the osmotic effect of PEG causes water to be retained in colon –> produces watery stool - think fluid overload
does not work on the nerves or muscles of the gut
no permeation of cell membranes

59
Q

Advantages of PEG-based preps

A

no mucosal damage
minimal osmotic fluid shifts
safer than sodium phosphate based solutions in pts with impaired renal function, cirrhosis, etc

60
Q

Disadvantages of PEG based preps

A

large volume of fluids
unpalatable taste if not flavored

61
Q

Hyperosmotic Preps contain a higher concentration of

A

salts and other dissolved materials than normal tissues

62
Q

MOA of hyperosmotic preps

A

increases intraluminal water (pulls water into the intestine) by promoting the passage of extracellular fluid across the bowel wall (significant fluid and electrolyte shifts)
High Na concentration –> osmotic retention of water in the bowel –> causing a watery diarrhea

63
Q

Advantages Hyperosmotic preps

A

small volume (though additional fluids must be consumed as well)
more palatable than PEG - based solutions

64
Q

Disadvantages of hyperosmotic preps

A

potential for causing fluid and electrolyte shifts by drawing water into the intestine
renal damage

65
Q

Risks of NaP Bowel Preps

A

Acute phosphate nephropathy - form of renal insufficiency characterized by calcium phosphate deposition within the kidneys

66
Q

Stimulant laxatives MOA

A

increased smooth muscle activity (peristalsis)

67
Q

Examples of stimulant laxatives

A

senna, bisacodyl, sodium picosulfate

68
Q

Senna MOA

A

increases rate of motility –> enhances colonic transit and inhibits water and electrolyte secretion

69
Q

Senna is often used as adjunct to

A

PEG regimens

70
Q

Bisacodyl MOA

A

stimulation of small intestinal enzyme secretion and increased motor activity within the colon

71
Q

Clenpiq MOA

A

prodrug - metabolized in the gut by gut bacteria, stimulating peristalsis

72
Q

Contraindications of Clenpiq

A

creatinine clearance < 30 ml/min (mild to moderate kidney disease)

73
Q

Split dose regimen is

A

part of the purgative is taken the evening before and the remainder is taken the morning of the procedure - has been demonstrated to be more effective and better tolerated than single dose taken the evening before the procedure

74
Q

Contraindications for NaP bowel preps

A

peds
elderly pts
liver failure
CHF
bowel obstruction
renal insuff or failure

75
Q

Colonoscopy should be performed within

A

8 hours of the last dosing

76
Q

Diet before colonoscopy

A

~ 2 days before = eat low-fiber
day before = don’t eat solid foods, consume only clear fluids
day of = clear fluids only, don’t eat or drink anything 2 hours before the procedure

77
Q

GERD antacids MOA

A

Neutralize acid (increase pH)

78
Q

Calcium based - calcium hydroxide
Aluminum based - aluminum hydroxide
Magnesium based - magnesium hydroxide
are all

A

antacids

79
Q

GERD: surface agents MOA

A

coats esophageal/gastric mucosa, creates physical barrier between mucosa and acid
short term management of GERD sx’s, swallow after meals, avoid drinking/eating afterwards

80
Q

Sucralfate
Sodium alginate
Bismuth
are all

A

surface agents

81
Q

GERD: H2RAs MOA

A

block stimulation of gastric parietal cells by competing with histamine at H2 receptors
less effective than PPIs, not effective for h. pylori

82
Q

GERD: H2RAs you can develop

A

tolerance within 4-6 weeks

83
Q

Crimetidine
rantidine
famotidine
are all

A

GERD: H2RAs

84
Q

GERD: PPIs MOA

A

block the gastric H/L-ATPase, inhibiting gastric acid secretion
most effective acid suppressing med, use for GERD, dyspepsia, PUD, H. pylori

85
Q

Omeprazole
Pantoprazole
Lansoprazole
Dexlansolprazole
Esomeprazole
Rabeprazole
are all

A

PPIs

86
Q

Risks of PPIs

A

malabsorption of some minerals and vitamins (mag, calcium, B12)
risk of diarrheal illnesses - C. diff
increased bacterial pneumonia
gastric polyps

87
Q

PUD/ H. pylori: Bismuth MOA

A

stimulates prostaglandin/ mucous/ bicarbonate production in the stomach
mild antimicrobial activity against H. pylori
reduces inflammation

88
Q

Bismuth subsalicylate or Pylera (combo bismuth + metronidazole + tetracycline) used for

A

PUD/ H. pylori

89
Q

PUD: Misoprostol MOA

A

synthetic prostaglandin E1 analog
Prostaglandins inhibit acid secretion by reducing the ability of parietal cells to respond to histamine

90
Q

Use for Misoprostol

A

prevention of NSAID-induced gastric ulcers

91
Q

Example of a misoprostol

A

Cytotec

92
Q

Caution of Misoprostol (cytotec)

A

can induce uterine contractions

93
Q

Metoclopramide
Doperidone
Erythromycin
are all

A

prokinetic agents

94
Q

MOA of metoclopramide

A

dopamine antagonist
enhances upper GI tract response to Ach to enhance motility; increases colon motility and shortens transit time

95
Q

Metoclopramide BBW

A

can cause tardive dyskinesia

96
Q

Misoprostol BBW

A

contraindicated in pregnancy or women of childbearing age (can cause birth defects, premature birth, abortion, uterine rupture)

97
Q

Domperidone MOA

A

Peripheral dopamine antagonist
increases esophageal peristalsis, gastric motility, gastric emptying decreases small bowel transit time

98
Q

Domperidone BBW

A

increased risk of cardiac arrhythmias or sudden cardiac death
contraindicated for pts with prolactinomas

99
Q

erythromycin MOA

A

macrolide antibiotic
motilin agonist - increases gastric contractions

100
Q

Erythromycin caution with…

A

Myasthenia gravis - may exacerbate or cause symptoms

101
Q

Neostigmine MOA

A

acetylcholinesterase inhibitor

102
Q

Neostigmine Uses

A

acute colonic pseudo-obstruction (primarily used for MG)

103
Q

Flares of IBD treatment

A

Glucocorticoids - hydrocortisone, prednisone, budesonide
Aminosalicylates - 5-ASA, sulfasalazine, mesalamine

104
Q

Aminosalicylates MOA

A

work topically on affected/inflamed areas of mucosa; anti-inflammatory and immunosuppressive activity
Sulfasalazine - precursor to 5-ASA

105
Q

Thiopurines MOA and use

A

immunosuppressant
induce and maintain remission in both UC and Crohn’s

106
Q

Thiopurines BBW

A

chronic immunosuppression increases the risk of malignancy

107
Q

Thiopurines avoid use with

A

allopurinol –> leukopenia

108
Q

Methotrexate MOA

A

Immunosuppressant, anti-inflammatory for IBD
acts as a folate antagonist, inhibiting DNA synthesis, repair and cellular respiration

109
Q

Methotrexate use

A

induce and maintain remission in Crohn’s disease, less commonly used for UC

110
Q

Methotrexate BBW

A

serious toxic/fatal side effects
closely monitor for bone marrow, liver, lung, skin and kidney toxicity

Teratogenic

111
Q

Supplement with ________ when taking methotrexate

A

Folic acid

112
Q

IBD: biologics MOA

A

bind and sequester TNF to decrease inflammatory response

113
Q

Triple therapy for H. pylori

A

clarithromycin
amox (or metronidazole)
PPI

114
Q

Quad therapy for H. pylori

A

bismuth subsalicylate
tetracycline
metronidazole
PPI

115
Q

Biologic (“mab”s) use for IBD

A

maintenance for moderate - severe IBD (mostly for crohn’s, infliximab, vedolizumab also for UC)

116
Q

Glucocorticoids MOA

A

inhibits production of inflammatory cytokines and inhibits migration of inflammatory cells to affected area

117
Q

Glucocorticoid use

A

moderate-severe Crohn’s and UC, helpful in early treatment and during flares

118
Q

If giving Misoprostol to a women in childbearing age you need

A

a pregnancy test 2 weeks before and every month during the use of this drug

119
Q

Metoclopramide is for ______ term use only

A

short
< 12 weeks

120
Q

Erythromycin should only be used for a max of

A

4 weeks d/t tachyphylaxis

Pharmacology (7 decks)

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