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Pharm 3 Module 2: GI > pharm exam 2 GI meds > Flashcards

pharm exam 2 GI meds Flashcards

1
Q

What are the Antiemetic drugs

A

Scopolamine
Prochlorperazine
metocloperamide
Ondansetron
Dronabinol
Promethazine
Meclizine
Dimenhydrinate

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2
Q

What are the CTZ activation medications

A

Serotonin 5-HT2
Dopamine D2
Muscarinic M1 receptors

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3
Q

what are the drug categories for nausea and vomiting

A

cholinergic/muscarinic antagnoist
dopamine receptor antagonists
serotonin receptor antagonists
cannabinoids
histamine antagonists

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4
Q

What is the cholinergic antagonist

A

scopolamine

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5
Q

what is the MOA of Scopolamine

A

blocks Ach at parasympathetic sites (smooth muscle, secretory glands, CNS)
also reduced histamine and serotonin activity

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6
Q

what is the PK of Scopolamine

A

SubQ or transdermal
change patch every 3 days
onset: 3-4 hours, duration: 72 hours
hepatic metabolism

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7
Q

what are the AE of scopolamine

A

tachy, fushing, dry mouth, blurred vision
cognitive imapirement
psychosis and hallucinations

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8
Q

what are the contraindications of scopolamine

A

narrow-angle glaucoma or with other agents containing belladonna

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9
Q

what are the D2 receptor antagonists

A

prochlorperazine
metocloperamide

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10
Q

what is the MOA of prochlorperazine

A

antagonizes D2 receptors in the CTZ and gut
also clocks M1 and H1 receptors

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11
Q

what is the PK of prochlorperazine

A

oral or rectal
duration: 1-2 hours oral, 3-12 hours rectal

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12
Q

what are the AE of prochlorperazine

A

extrapyramidal effects
tardive dyskinesia
hypotension
long QT
CNS effects

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13
Q

what are the uses of metocloperamide

A

chemo induced and post op N/V
documented gastroparesis
off label: tx of hiccups and n/v in early pregnancy

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14
Q

what is the MOA of metocloperamide

A

antagonizes D2 receptors in CTZ and gut
also blocks M1 and H1 receptors
weakly blocks 5-HT3 at high doses

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15
Q

what is the PK of metocloperamide

A

oral or IV
duration: 1-2 hours, dosed 3-4x/day
CYP2D6

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16
Q

what is the AE of metocloperamide

A

extrapyramidal effects
tardive dyskinesia
hypotension
long QT
CNS effects
hyperprolactinemia

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17
Q

what are the serotonin receptor antagonists for nausea/vomiting

A

Ondansetron

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18
Q

what are the uses of ondansetron

A

chemo induced N/V, mgmt of post-op N/V
effective alone or in combo with Dexamethasone

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19
Q

what is the MOA of ondansetron

A

selectively blocks 5-HT3 receptors in the periphery and brain

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20
Q

what is the PK of ondansetron

A

Oral or IV admin
onset: 30 min, peak 1-2 hours
extensively metab by liver, CYP
dose adjust in hepatically impairment

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21
Q

what are the AE of ondansetron

A

HA, dizziness, confusion, SOB, constipation, Long QT
monitor EKG and watch sings of serotonin syndrome

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22
Q

What is the Cannabinoids

A

Dronabinol

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23
Q

what is the use of dronabinol

A

second line for chemo-induced N/V
stimulate appetite in pts with AIDS

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24
Q

what is the MOA of Dronabinol

A

activates cannabinoid receptors

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25
Q

what is the PK of dronabinol

A

oral admin
onset: 30-60 min, peak 2-4 hours, duration 4-6 hours
hepatic metabolism

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26
Q

what are the AE of dronabinol

A

euphoria, CNS changes, abd pain, vomiting, flushing, hypotension, vertigo

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27
Q

what are the contraindications of Dronabinol

A

contra in psych disorders + SUB
monitor HR and BP, cannabis hyperemesis

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28
Q

What are the histamine antagonists

A

promethazine
meclizine
dimenhydrinate

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29
Q

what are the uses of promethazine

A

reduces emesis associated with surgery, chemo, and toxins
widely used in young children
motion sickness

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30
Q

what is the MOA of promethazine

A

blocks D2 receptors in CTZ
blocks H1 receptor in brainstem

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31
Q

what is the PK of promethazine

A

oral, IM or IV
duration 4-6 hours
CYP metabolism

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32
Q

what is the AE of promethazine

A

extramyramidal sx,
anticholinerigic effects
hypotension
sedation
EKG changes
photosensitivity
tissue injury

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33
Q

what is the use of Meclizine

A

OTC antihistamine
motion sickness

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34
Q

what is the MOA of meclizine

A

blocks H1 and M1 receptor - depresses labrynth excitability and vestibular stimulation

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35
Q

what is the PK of meclizine

A

oral onset: 1 hr, duration 24 hours
hepatic metabolism

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36
Q

what are the AE of meclizine

A

sedation, HA, vomiting, blurred vision
avoid in glaucoma, asthma, urinary retentions, pyloric/duodenal obstruction

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37
Q

what is the use of Dimenhydrinate

A

OTC antihistamine
motion sickness

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38
Q

what is the MOA of dimenhydrinate

A

blocks H1 receptors in peripheral sites and CTZ
has central anticholinergic activity

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39
Q

what is the PK of dimenhydrinate

A

oral and IM
onset 30 min, duration 4-6 hours
hepatic metabolism

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40
Q

what are the AE of dimenhydrinate

A

tachycardia
anorexia
epigastric distress
sedation
dizziness
xerostomia
blurred vision
SJS
CNS changes

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41
Q

what are the drug categories used for diarrhea and IBS-D

A

opioid agnosts
serotonin receptor modulators
bile acid sequestrants
anti-spasmodics
antimicrobial agents

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42
Q

what are the antidiarrheal medications

A

loperamide
diphenoxylate/atropine
octreotide
eluxadoline
alosetron
tegeserod
bile acid sequestrants
Rifaximin
hyoscyamine/dicyclomine

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43
Q

what are the opioid compund drugs

A

loperamide
diphenoxylate/atrophine
octreotide
eluxadoline

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44
Q

what is the MOA of opioid antagonists

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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45
Q

What are the uses of Loperamide

A

structural analog of peperidine
tx of diarrhea and reduce volume of discharge from ileostomies

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46
Q

what are the MOA of loperamide

A

activate opioid receptors in smooth muscle of the GI tract, alters peristalsis, reduces stool volume and prevents electrolyte depletion
increase IAS and EAS tone

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47
Q

what are the PK of loperamide

A

oral tablets or liquid admin
poorly absorbed and does not cross BB
Hepatic metabolism

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48
Q

what are the SE of loperamide

A

constipation, dizziness, abd pain and cramping
cardiac arrest when used in large doses

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49
Q

what are the uses of diphenoxylate/atropine

A

diarrhea

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50
Q

what are the MOA of diphenoxylate/atropine

A

activate opioid receptors in GI tract
atropine prevents abuse

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51
Q

what are the PK of diphenoxylate/atropine

A

tablet or liquid
hepatic metabolism
onset: 45 min, half life 2.5 hours

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52
Q

what are the SE of diphenoxylate/atropine

A

flushing, tachy, CNS effects, xeroderma, vomiting, toxic megacolon, urinary retention

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53
Q

what is octreotide used for

A

diarrhea

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54
Q

what is the MOA of octreotide

A

inhibits serotonin release and has some effect on opioid receptors
inhibits secretion of gastrin, VIP, insulin, glucagon, motilin, pancreatic polypeptide

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55
Q

what is the PK of octreotide

A

oral
duration 6-12 hours
hepatic metabolism

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56
Q

what are the AE of octreotide

A

brady, fatigue, HA, dizziness, pruitis, hyperglycemia, hypothyroidism
cholelithiasis, abd pain, diarrhea, constipation, biliary obstruction, URI, arrhythmia, depression

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57
Q

what is the use of Eluxadoline

A

approved for IBS-D

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58
Q

what is the MOA of Eluxadoline

A

blocks kappa, and delta opioid receptors in the intestinal lumen; activates mu receptors -> decrease intestinal motility without causing constipation

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59
Q

what are the PK of Eluxadoline

A

oral and half life of 4-6 hours

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60
Q

what are the AE of Eluxadoline

A

dizziness, drowsiness, nausea, abd pain, vomiting, elevated LFTs, URI

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61
Q

when is Eluxadoline contraindicated

A

alcohol abuse, hx of intestinal obstruction

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62
Q

what are the serotonin receptor modulators used for diarrhea

A

Alosetron and Tegaserod

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63
Q

what is the use of Alosetron

A

chronic (>6mo) severe IBS-D

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64
Q

what is the MOA of alosetron

A

selective serotonin antagonist
acts on receptors in enteric neurons and in other locations centrally and peripherally

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65
Q

what is the PK of Alosetron

A

oral admin, absorption rapid but incomplete
take on an empty stomach
extensive P450 metabolism

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66
Q

what are the AE of Alosetron

A

constipation, HA, fatigue, abdominal pain, nausea

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67
Q

when is Alosetron contraindicated

A

hx GI obstruction, Crohn’s disease, diverticulitis, vasculopathy, thrombophelbitis, hypercoagu conditions

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68
Q

what is Tegaserod used for

A

only available for emergency investigational drug purposes due to risk of cardiac arrest

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69
Q

what is the use of bile acid sequestrants

A

bile acid diarrhea

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70
Q

what is the MOA of bile acid sequestrants

A

bind to bile salts in the intestines, inhibit re-uptake of bile salts

71
Q

what is the PK of bile acid sequestrants

A

no absorption, excretion in feces

72
Q

what are the AE of bile acid sequestrants

A

abdominal pain, bloating, biliary colic, gallbladder calcifications, melena, vomiting, dental erosions, abnormal LFTs, tinnitus, bleeding issues

73
Q

what antimicrobial meds are used for diarrhea

A

Rifaximin
metronidazole
ciprofloxacin
amoxicillin
neomycin

74
Q

what is the use of Rifaximin

A

small intestinal bowel overgrowth syndrome
IBS-D
travelers diarrhea

75
Q

what is the MOA of Rifaximin

A

binds to bacterial DNA-dependent RNA polymerase -> inhibits RNA synthesis

76
Q

what is the PK Rifaximin

A

oral admin
hepatic CYP metabolism

77
Q

what are the AE of Rifaximin

A

peripheral edema
dizziness
fatigue
ascites
nausea
HA
prurits
can cause pseudomembranous colitis

78
Q

what are the anti-spasmodic agents

A

Hyoscyamine/dicyclomine

79
Q

what is the use of Hyosccyamine/dicylomine

A

acute attacks of IBS-D with bloat and discomfort

80
Q

what is the MOA of Hyoscyamine/dicyclomine

A

blocks ACH at parasympathetic receptors
antagonists of histamine and serotonin

81
Q

what is the PK of hyoscyamine/dicylomine

A

onset 2-3 min, duration 4-6 hours
hepatic metabolism

82
Q

what are the AE of hyoscyamine/dicyclomine

A

tachy, mental status changes, abd pain, impotence, blurred vision, urinary retention, increased IOP

83
Q

when is hyoscyamine/dicylomine contraindicated

A

MG
hypersensitivity to belladonna
UC
myocardial ischemia

84
Q

what are the medication categories for constipation and IBS-C

A

stool softeners
bulking laxatives
osmotic laxatives
stimulant laxatives
selective opioid antagonists
guanylate cyclase-C agonists

85
Q

what is docusate sodium/docusate calcium

A

surfactant laxatives - stool softener
often used for prophylaxis instead of tx

86
Q

what is the MOA of docusate sodium/docusate calcium

A

lowers surface tension -> facilitates penetration of water into feces
may also inhibit fluid absorption into the intestinal wall

87
Q

what is the PK of docusate sodium/calcium

A

capsules, tablets, liquid, syrup admin
take with full glass of water

88
Q

what are the AE of docusate sodium/calcium

A

throat irritation
no major interactions

89
Q

what are the bulking laxatives

A

methylcellulose
psyllium

90
Q

what is the use of bulking laxatives

A

preferred for temporary constipation
used widely in diverticulosis and IBS

91
Q

what is the MOA of bulking laxatives

A

absorb and retain water in the intestine -> increase mass of stool promotes peristaliss
same effect as dietary fiber

92
Q

what is the PK of bulking laxatives

A

powder added to water 1-3 times/day or water

93
Q

what are the AE of bulking laxatives

A

systemic symptoms rare
esophageal obstruction possible when swallowed without water
bloating, flatulance, GI distress

94
Q

what are the osmotic laxatives

A

magnesium oxide/ sodium phosphate
lactulose
polyethylene glycol
glycerin

95
Q

what is the MOA of saline laxatives (mag oxide, sodium phosphate)

A

retains water in the intestines-> increase intraluminal pressure and promotes peristalsis

96
Q

what are the AE of saline laxatives

A

bloating, abdominal pain, apthous stomatitis, hypokalemia, hypophosphtemia

97
Q

what is lactulose

A

semi synthetic disaccharide, osmotic laxative
relieving constipation but more expensive than other drugs
reserved for patients who do not respond to bulk-forming agents

98
Q

what is the MOA of lactulose

A

promotes fluid retention in intestine, thus increasing intraluminal pressure and promoting prestalsis

99
Q

what is the SE of lactulose

A

flatulence, cramping, dehyrdration, hypernatremia, hypokalemia, blaoting, nausea, abdominal cramping, diarrhea
electrolyte imbalances

100
Q

what is the gold standard for bowl prep for colonoscopies

A

polyethylene glycol

101
Q

what is the MOA of PEG

A

nonabsorbable compound that retains water int he intestinal lumen, causing fecal mass to soften and swell
fluid overload

102
Q

what are the AE of PEG

A

Nausea, bloating, cramping, flatulance, electrolyte imbalances, diarrhea
major interactions with digoxin

103
Q

what is the MOA of glycerin suppository

A

facilitating the passage of hard stools

104
Q

what is the AE of glycerin suppository

A

can cause rectal burning
abdominal cramping, bloating, irritation, diarrrhea, tenesmus

105
Q

what are the stimulant laxatives

A

naloxgol and methynaltrexone

106
Q

what is the MOA for stimulant laxatives

A

block mu opioid receptors in the GI tract
naloxegol- bound to PEG to prevent crossing BBB

107
Q

what is the AE of stimulant laxatives/opioid antagonists

A

abdominal pain, flatulence, nausea, dizziness, diarrhea, muscle spasms, tremor, hot flashes
contra in mechanical GI obstruction

108
Q

what are the IBS-C medications

A

lubiprostone and linaclotide

109
Q

what is the MOA of lubiprostone

A

opens Cl- channels to increase fluid secretion in the intestinal lumen -> eases passage of stools

110
Q

what is the AE of Lubiprostone

A

N/D/V, abd distention/pain, gas, HA, chest pain, edema, dyspnea, syncope

111
Q

what is the MOA of linaclotide

A

acts on guanylate cyclase on the epithelium of the intestine -> increase cGMP -> stim Cl- and bicarb secretion promoting peristalsis

112
Q

what is the AE of linaclotide

A

HA, diarrhea, fatigue, abdominal pain

113
Q

what are treatment options for GERD

A

anatacids
surface agents
H2 receptor antagonists (H2RAs)
Proton pump inhibitors (PPI)

114
Q

what are the Anacids

A

Aluminum hydroxide
calcium carbonate/hydroxide
aluminum hydroxide/magnesium hydroxide

115
Q

what is the MOA of antacids

A

neutralize acid (increase pH)

116
Q

what are the SE of antacids

A

constipation

117
Q

what are the surface agents

A

sucralfate
bismuth

118
Q

what is the MOA of surface agents

A

coats esophageal/gastric mucosa, creates physical barrier between mucosa and acid

119
Q

what are the SE of Bismuth

A

black stools, black tongue (reversible)
neurotoxicity; encephalopathy, spetic meningitis, seizures

120
Q

what are the SE of Sucralfate

A

constipation, renal failure (aluminum toxicity)
caution with renal failure, DM

121
Q

what are the H2RA medications

A

Cimetidine
Famotidine

122
Q

what is the us of H2RA meds

A

GERD, dyspepsia, PUD, first line for infrequent symtpoms
less effective than PPIs, not effective for H/ pylori

123
Q

what is the MOA of H2RA medicatios

A

competitively block the binding of histmaine to H2 receptors in the stomach -> reduce secretion of gastric acid

124
Q

what are the SE of H2RA medications

A

gynecomastia and galactorrhea (cimetidine)
HA, dizziness, diarrhea, constipation
Prolonged use: B12 deficiency

125
Q

What are PPI medications

A

Omeprazole
esomeprazole
lansoprazole
pantoprazole

126
Q

what is the MOA of PPIs

A

Blocks gastric H+/K+ ATPase -> inhibiting gastric acid secretion

127
Q

what is the PK of PPIs

A

oral or admin 30-60 min before first meal of the day

128
Q

what are the AE of PPis

A

HA, nausea, abdominal pain, diarrhea
increased risk for fractures, malabsorption and some minerals, C.diff, PNA, AIN, CKD

129
Q

what is triple therapy

A

amoxicillin (metronidazole if PCN allergy) + clarithromycin, and PPI
used for treatment of H. pylori

130
Q

what is the MOA of triple therapy

A

antibiotic kills H.pylori, PPI reduces gastric acid

131
Q

what is the PK of triple therapy

A

2 week duration
confirm eradication 4 weeks after stopping abx

132
Q

what are the AE of triple therapy

A

diarrhea, abnormal stools, nausea, HA, SJS, hepatic impairment
intracranial HTN, photsensitivity

133
Q

what is quadruple therapy

A

Bismuth + metronidazole, tetracycline _ PPI

134
Q

what are the SE of Quadruple therapy

A

diarrhea, abnormal stools, nausea, HA, SJS, hepatic impairment

135
Q

What is the use of Misoprostol

A

PUD
Prevention of NSAID-induced gastric ulcers

136
Q

what is the MOA misoprostol

A

analog of prostaglandin E1 -> inhibits acid secretion by reducing partial cells ability to respond to histamine

137
Q

what are the AE of misoprostol

A

diarrhea, nausea, abdominal pain, HA
contra: Pregnancy

138
Q

what are the prokinetic agents

A

metocloramide
domperidone
erythromycin
neostigmine

139
Q

what is the use of metoclopramide

A

gastroparesis, persistent GERD, N/V
off label: tx of hiccups and N/V of early pregnancy
short term use only d/t TD
also an anti-emetic

140
Q

what is the MOA of metoclopramide

A

antagonizes D2 receptors
enhances upper GI tract response to Ach to enhance motility; increased colon motility and shortens transit time

141
Q

what are the AE of metoclopramide

A

extrapyramidal effects
tardive dyskinesia
hyptension
long QT
CNS effects
hyperprolactinemia

142
Q

what is the use of Domperidone

A

gastroparesis
motility disorders
N/V
not available in the US

143
Q

what is the MOA of Domperidone

A

peripheral Dopamine antagonists, increase esophageal peristalsis, gastric motility and gastric emptying
Decrease small bowel transit time

144
Q

what are the SE of Domperidone

A

HA, migraine, xerostomia, may increase prolactin levels
increase risk of arrythmias and sudden cardiac death

145
Q

when is domperidone contraindicated

A

prolactinomas

146
Q

what is the use of Erythromycin

A

macrolide abx
primarily used as abx but can be used for gastroparesis

147
Q

what is the MOA of erythromycin

A

macrolide abx, motilin agonist -> increase gastric contractions

148
Q

what is the SE of erythromycin

A

arrhythmias, long QT, superinfection
caution with MG
use for max of 4 weeks

149
Q

what is the use of neostigmine

A

acute colonic psuedo-obstruction
primariy use for MG

150
Q

what is the MOA of neostigmine

A

acetylcholinesterase inhibitor

151
Q

what are the SE of neostigmine

A

arrhythmias, esp bradycardia, dizziness, drowsiness, diarrhea
caution with CV disease

152
Q

what are meds for IBD flares

A

glucocorticoids
aminosalicylates

153
Q

what are the glucocorticoids used for IBD flares

A

prednisone, budesonide, methyprednisolong, hydrocortisone

154
Q

what are the aminosalicylates

A

sulfasalazine
mesalamine

155
Q

what is sulfasalazine

A

aminosalicylate
used to treat mild to moderate UC and Crohns disease to maintain remission after symptoms have subsided
RA

156
Q

what is the MOA of sulfasalazine

A

metab by intestinal bacteria into 5-ASA and sulfapyridine -> reduce inflammation
ASA: responsible for efficacy, sulfapyridine resp for SE

157
Q

what is the AE of sulfasalazine

A

Ha, nausea, fever, rash, fatigue, arthralgia, hematologic disorders
may impair male fertility

158
Q

what is mesalamine

A

aminosalicylates made of single 5-ASA molecules enclosed with in an enteric coat
mild to moderate UC (flares, maintenacne), mild Crohns dz

159
Q

what is the MOA of masalamine

A

anti-inflam and immunosuppression properties due to inhib of cytokines, leukotriene, and prostaglandin synthesis, savenging of free radicals etc

160
Q

what are the SE of mesalamine

A

HA, nausea, diarrhea, abdominal pain, nephrotoxicity, interstitial nephritis
caution in severe renal and hepatic impairment

161
Q

what is the use of glucocorticoids

A

mod-sever crohns and UC flares

162
Q

what is the MOA of glucocorticoids

A

inhibits production of inflammatory cytokines

163
Q

what are the AE of glucocortiocids

A

hyperglycemia, adrenal supp, peptic ulcers, immunosupp, anxiety, fluid retention

164
Q

what are the biologics used for IBD

A

adalimumab/infliximab

165
Q

what are the immunomodulators

A

Aianx and methotrexate

166
Q

what is the use of Ainx

A

induce and maintain remission in both UC and Crohns disease
cannot be used for acute tx
can help reduce steroid use

167
Q

what is the MOA of Aianx

A

immunosuppressant

168
Q

what are the SE of Aianx

A

N/V, pancreatitis, neutropenia, liver toxicity
monitor CBC and LFTs

169
Q

what is Methotrexate

A

induce and maintain remission in Crohn’s dz
less common in UC

170
Q

what is the MOA of methotrexate

A

Folic acid antagonist that inhibits cytokines production and purine nucleotide biosynthesis -> immunsuppression and anti-inflammatory effects

171
Q

what are the AE of methotrexate

A

cytotoxic in high doses
diarrhea, N/V, alopecia, bone marrow suppression, mucositis

contra in pregnancy

172
Q

what are adalimumab/infliximab

A

biologics
moderate to severe UC and CD, generally used as second line agents
adalimumab better for Crohn’s
infliximab better for UC

173
Q

what is the MOA of the biologics

A

TNF-alpha inhibitors -> helps mitigate overactive immune response

174
Q

what are the SE of biologics

A

infusion reactions

caution with heart disease and liver disease

Pharm 3 Module 2: GI (4 decks)

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