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
what is the PK of dronabinol
oral admin onset: 30-60 min, peak 2-4 hours, duration 4-6 hours hepatic metabolism
26
what are the AE of dronabinol
euphoria, CNS changes, abd pain, vomiting, flushing, hypotension, vertigo
27
what are the contraindications of Dronabinol
contra in psych disorders + SUB monitor HR and BP, cannabis hyperemesis
28
What are the histamine antagonists
promethazine meclizine dimenhydrinate
29
what are the uses of promethazine
reduces emesis associated with surgery, chemo, and toxins widely used in young children motion sickness
30
what is the MOA of promethazine
blocks D2 receptors in CTZ blocks H1 receptor in brainstem
31
what is the PK of promethazine
oral, IM or IV duration 4-6 hours CYP metabolism
32
what is the AE of promethazine
extramyramidal sx, anticholinerigic effects hypotension sedation EKG changes photosensitivity tissue injury
33
what is the use of Meclizine
OTC antihistamine motion sickness
34
what is the MOA of meclizine
blocks H1 and M1 receptor - depresses labrynth excitability and vestibular stimulation
35
what is the PK of meclizine
oral onset: 1 hr, duration 24 hours hepatic metabolism
36
what are the AE of meclizine
sedation, HA, vomiting, blurred vision avoid in glaucoma, asthma, urinary retentions, pyloric/duodenal obstruction
37
what is the use of Dimenhydrinate
OTC antihistamine motion sickness
38
what is the MOA of dimenhydrinate
blocks H1 receptors in peripheral sites and CTZ has central anticholinergic activity
39
what is the PK of dimenhydrinate
oral and IM onset 30 min, duration 4-6 hours hepatic metabolism
40
what are the AE of dimenhydrinate
tachycardia anorexia epigastric distress sedation dizziness xerostomia blurred vision SJS CNS changes
41
what are the drug categories used for diarrhea and IBS-D
opioid agnosts serotonin receptor modulators bile acid sequestrants anti-spasmodics antimicrobial agents
42
what are the antidiarrheal medications
loperamide diphenoxylate/atropine octreotide eluxadoline alosetron tegeserod bile acid sequestrants Rifaximin hyoscyamine/dicyclomine
43
what are the opioid compund drugs
loperamide diphenoxylate/atrophine octreotide eluxadoline
44
what is the MOA of opioid antagonists
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
45
What are the uses of Loperamide
structural analog of peperidine tx of diarrhea and reduce volume of discharge from ileostomies
46
what are the MOA of loperamide
activate opioid receptors in smooth muscle of the GI tract, alters peristalsis, reduces stool volume and prevents electrolyte depletion increase IAS and EAS tone
47
what are the PK of loperamide
oral tablets or liquid admin poorly absorbed and does not cross BB Hepatic metabolism
48
what are the SE of loperamide
constipation, dizziness, abd pain and cramping cardiac arrest when used in large doses
49
what are the uses of diphenoxylate/atropine
diarrhea
50
what are the MOA of diphenoxylate/atropine
activate opioid receptors in GI tract atropine prevents abuse
51
what are the PK of diphenoxylate/atropine
tablet or liquid hepatic metabolism onset: 45 min, half life 2.5 hours
52
what are the SE of diphenoxylate/atropine
flushing, tachy, CNS effects, xeroderma, vomiting, toxic megacolon, urinary retention
53
what is octreotide used for
diarrhea
54
what is the MOA of octreotide
inhibits serotonin release and has some effect on opioid receptors inhibits secretion of gastrin, VIP, insulin, glucagon, motilin, pancreatic polypeptide
55
what is the PK of octreotide
oral duration 6-12 hours hepatic metabolism
56
what are the AE of octreotide
brady, fatigue, HA, dizziness, pruitis, hyperglycemia, hypothyroidism cholelithiasis, abd pain, diarrhea, constipation, biliary obstruction, URI, arrhythmia, depression
57
what is the use of Eluxadoline
approved for IBS-D
58
what is the MOA of Eluxadoline
blocks kappa, and delta opioid receptors in the intestinal lumen; activates mu receptors -> decrease intestinal motility without causing constipation
59
what are the PK of Eluxadoline
oral and half life of 4-6 hours
60
what are the AE of Eluxadoline
dizziness, drowsiness, nausea, abd pain, vomiting, elevated LFTs, URI
61
when is Eluxadoline contraindicated
alcohol abuse, hx of intestinal obstruction
62
what are the serotonin receptor modulators used for diarrhea
Alosetron and Tegaserod
63
what is the use of Alosetron
chronic (>6mo) severe IBS-D
64
what is the MOA of alosetron
selective serotonin antagonist acts on receptors in enteric neurons and in other locations centrally and peripherally
65
what is the PK of Alosetron
oral admin, absorption rapid but incomplete take on an empty stomach extensive P450 metabolism
66
what are the AE of Alosetron
constipation, HA, fatigue, abdominal pain, nausea
67
when is Alosetron contraindicated
hx GI obstruction, Crohn's disease, diverticulitis, vasculopathy, thrombophelbitis, hypercoagu conditions
68
what is Tegaserod used for
only available for emergency investigational drug purposes due to risk of cardiac arrest
69
what is the use of bile acid sequestrants
bile acid diarrhea
70
what is the MOA of bile acid sequestrants
bind to bile salts in the intestines, inhibit re-uptake of bile salts
71
what is the PK of bile acid sequestrants
no absorption, excretion in feces
72
what are the AE of bile acid sequestrants
abdominal pain, bloating, biliary colic, gallbladder calcifications, melena, vomiting, dental erosions, abnormal LFTs, tinnitus, bleeding issues
73
what antimicrobial meds are used for diarrhea
Rifaximin metronidazole ciprofloxacin amoxicillin neomycin
74
what is the use of Rifaximin
small intestinal bowel overgrowth syndrome IBS-D travelers diarrhea
75
what is the MOA of Rifaximin
binds to bacterial DNA-dependent RNA polymerase -> inhibits RNA synthesis
76
what is the PK Rifaximin
oral admin hepatic CYP metabolism
77
what are the AE of Rifaximin
peripheral edema dizziness fatigue ascites nausea HA prurits can cause pseudomembranous colitis
78
what are the anti-spasmodic agents
Hyoscyamine/dicyclomine
79
what is the use of Hyosccyamine/dicylomine
acute attacks of IBS-D with bloat and discomfort
80
what is the MOA of Hyoscyamine/dicyclomine
blocks ACH at parasympathetic receptors antagonists of histamine and serotonin
81
what is the PK of hyoscyamine/dicylomine
onset 2-3 min, duration 4-6 hours hepatic metabolism
82
what are the AE of hyoscyamine/dicyclomine
tachy, mental status changes, abd pain, impotence, blurred vision, urinary retention, increased IOP
83
when is hyoscyamine/dicylomine contraindicated
MG hypersensitivity to belladonna UC myocardial ischemia
84
what are the medication categories for constipation and IBS-C
stool softeners bulking laxatives osmotic laxatives stimulant laxatives selective opioid antagonists guanylate cyclase-C agonists
85
what is docusate sodium/docusate calcium
surfactant laxatives - stool softener often used for prophylaxis instead of tx
86
what is the MOA of docusate sodium/docusate calcium
lowers surface tension -> facilitates penetration of water into feces may also inhibit fluid absorption into the intestinal wall
87
what is the PK of docusate sodium/calcium
capsules, tablets, liquid, syrup admin take with full glass of water
88
what are the AE of docusate sodium/calcium
throat irritation no major interactions
89
what are the bulking laxatives
methylcellulose psyllium
90
what is the use of bulking laxatives
preferred for temporary constipation used widely in diverticulosis and IBS
91
what is the MOA of bulking laxatives
absorb and retain water in the intestine -> increase mass of stool promotes peristaliss same effect as dietary fiber
92
what is the PK of bulking laxatives
powder added to water 1-3 times/day or water
93
what are the AE of bulking laxatives
systemic symptoms rare esophageal obstruction possible when swallowed without water bloating, flatulance, GI distress
94
what are the osmotic laxatives
magnesium oxide/ sodium phosphate lactulose polyethylene glycol glycerin
95
what is the MOA of saline laxatives (mag oxide, sodium phosphate)
retains water in the intestines-> increase intraluminal pressure and promotes peristalsis
96
what are the AE of saline laxatives
bloating, abdominal pain, apthous stomatitis, hypokalemia, hypophosphtemia
97
what is lactulose
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
what is the MOA of lactulose
promotes fluid retention in intestine, thus increasing intraluminal pressure and promoting prestalsis
99
what is the SE of lactulose
flatulence, cramping, dehyrdration, hypernatremia, hypokalemia, blaoting, nausea, abdominal cramping, diarrhea electrolyte imbalances
100
what is the gold standard for bowl prep for colonoscopies
polyethylene glycol
101
what is the MOA of PEG
nonabsorbable compound that retains water int he intestinal lumen, causing fecal mass to soften and swell fluid overload
102
what are the AE of PEG
Nausea, bloating, cramping, flatulance, electrolyte imbalances, diarrhea major interactions with digoxin
103
what is the MOA of glycerin suppository
facilitating the passage of hard stools
104
what is the AE of glycerin suppository
can cause rectal burning abdominal cramping, bloating, irritation, diarrrhea, tenesmus
105
what are the stimulant laxatives
naloxgol and methynaltrexone
106
what is the MOA for stimulant laxatives
block mu opioid receptors in the GI tract naloxegol- bound to PEG to prevent crossing BBB
107
what is the AE of stimulant laxatives/opioid antagonists
abdominal pain, flatulence, nausea, dizziness, diarrhea, muscle spasms, tremor, hot flashes contra in mechanical GI obstruction
108
what are the IBS-C medications
lubiprostone and linaclotide
109
what is the MOA of lubiprostone
opens Cl- channels to increase fluid secretion in the intestinal lumen -> eases passage of stools
110
what is the AE of Lubiprostone
N/D/V, abd distention/pain, gas, HA, chest pain, edema, dyspnea, syncope
111
what is the MOA of linaclotide
acts on guanylate cyclase on the epithelium of the intestine -> increase cGMP -> stim Cl- and bicarb secretion promoting peristalsis
112
what is the AE of linaclotide
HA, diarrhea, fatigue, abdominal pain
113
what are treatment options for GERD
anatacids surface agents H2 receptor antagonists (H2RAs) Proton pump inhibitors (PPI)
114
what are the Anacids
Aluminum hydroxide calcium carbonate/hydroxide aluminum hydroxide/magnesium hydroxide
115
what is the MOA of antacids
neutralize acid (increase pH)
116
what are the SE of antacids
constipation
117
what are the surface agents
sucralfate bismuth
118
what is the MOA of surface agents
coats esophageal/gastric mucosa, creates physical barrier between mucosa and acid
119
what are the SE of Bismuth
black stools, black tongue (reversible) neurotoxicity; encephalopathy, spetic meningitis, seizures
120
what are the SE of Sucralfate
constipation, renal failure (aluminum toxicity) caution with renal failure, DM
121
what are the H2RA medications
Cimetidine Famotidine
122
what is the us of H2RA meds
GERD, dyspepsia, PUD, first line for infrequent symtpoms less effective than PPIs, not effective for H/ pylori
123
what is the MOA of H2RA medicatios
competitively block the binding of histmaine to H2 receptors in the stomach -> reduce secretion of gastric acid
124
what are the SE of H2RA medications
gynecomastia and galactorrhea (cimetidine) HA, dizziness, diarrhea, constipation Prolonged use: B12 deficiency
125
What are PPI medications
Omeprazole esomeprazole lansoprazole pantoprazole
126
what is the MOA of PPIs
Blocks gastric H+/K+ ATPase -> inhibiting gastric acid secretion
127
what is the PK of PPIs
oral or admin 30-60 min before first meal of the day
128
what are the AE of PPis
HA, nausea, abdominal pain, diarrhea increased risk for fractures, malabsorption and some minerals, C.diff, PNA, AIN, CKD
129
what is triple therapy
amoxicillin (metronidazole if PCN allergy) + clarithromycin, and PPI used for treatment of H. pylori
130
what is the MOA of triple therapy
antibiotic kills H.pylori, PPI reduces gastric acid
131
what is the PK of triple therapy
2 week duration confirm eradication 4 weeks after stopping abx
132
what are the AE of triple therapy
diarrhea, abnormal stools, nausea, HA, SJS, hepatic impairment intracranial HTN, photsensitivity
133
what is quadruple therapy
Bismuth + metronidazole, tetracycline _ PPI
134
what are the SE of Quadruple therapy
diarrhea, abnormal stools, nausea, HA, SJS, hepatic impairment
135
What is the use of Misoprostol
PUD Prevention of NSAID-induced gastric ulcers
136
what is the MOA misoprostol
analog of prostaglandin E1 -> inhibits acid secretion by reducing partial cells ability to respond to histamine
137
what are the AE of misoprostol
diarrhea, nausea, abdominal pain, HA contra: Pregnancy
138
what are the prokinetic agents
metocloramide domperidone erythromycin neostigmine
139
what is the use of metoclopramide
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
what is the MOA of metoclopramide
antagonizes D2 receptors enhances upper GI tract response to Ach to enhance motility; increased colon motility and shortens transit time
141
what are the AE of metoclopramide
extrapyramidal effects tardive dyskinesia hyptension long QT CNS effects hyperprolactinemia
142
what is the use of Domperidone
gastroparesis motility disorders N/V not available in the US
143
what is the MOA of Domperidone
peripheral Dopamine antagonists, increase esophageal peristalsis, gastric motility and gastric emptying Decrease small bowel transit time
144
what are the SE of Domperidone
HA, migraine, xerostomia, may increase prolactin levels increase risk of arrythmias and sudden cardiac death
145
when is domperidone contraindicated
prolactinomas
146
what is the use of Erythromycin
macrolide abx primarily used as abx but can be used for gastroparesis
147
what is the MOA of erythromycin
macrolide abx, motilin agonist -> increase gastric contractions
148
what is the SE of erythromycin
arrhythmias, long QT, superinfection caution with MG use for max of 4 weeks
149
what is the use of neostigmine
acute colonic psuedo-obstruction primariy use for MG
150
what is the MOA of neostigmine
acetylcholinesterase inhibitor
151
what are the SE of neostigmine
arrhythmias, esp bradycardia, dizziness, drowsiness, diarrhea caution with CV disease
152
what are meds for IBD flares
glucocorticoids aminosalicylates
153
what are the glucocorticoids used for IBD flares
prednisone, budesonide, methyprednisolong, hydrocortisone
154
what are the aminosalicylates
sulfasalazine mesalamine
155
what is sulfasalazine
aminosalicylate used to treat mild to moderate UC and Crohns disease to maintain remission after symptoms have subsided RA
156
what is the MOA of sulfasalazine
metab by intestinal bacteria into 5-ASA and sulfapyridine -> reduce inflammation ASA: responsible for efficacy, sulfapyridine resp for SE
157
what is the AE of sulfasalazine
Ha, nausea, fever, rash, fatigue, arthralgia, hematologic disorders may impair male fertility
158
what is mesalamine
aminosalicylates made of single 5-ASA molecules enclosed with in an enteric coat mild to moderate UC (flares, maintenacne), mild Crohns dz
159
what is the MOA of masalamine
anti-inflam and immunosuppression properties due to inhib of cytokines, leukotriene, and prostaglandin synthesis, savenging of free radicals etc
160
what are the SE of mesalamine
HA, nausea, diarrhea, abdominal pain, nephrotoxicity, interstitial nephritis caution in severe renal and hepatic impairment
161
what is the use of glucocorticoids
mod-sever crohns and UC flares
162
what is the MOA of glucocorticoids
inhibits production of inflammatory cytokines
163
what are the AE of glucocortiocids
hyperglycemia, adrenal supp, peptic ulcers, immunosupp, anxiety, fluid retention
164
what are the biologics used for IBD
adalimumab/infliximab
165
what are the immunomodulators
Aianx and methotrexate
166
what is the use of Ainx
induce and maintain remission in both UC and Crohns disease cannot be used for acute tx can help reduce steroid use
167
what is the MOA of Aianx
immunosuppressant
168
what are the SE of Aianx
N/V, pancreatitis, neutropenia, liver toxicity monitor CBC and LFTs
169
what is Methotrexate
induce and maintain remission in Crohn's dz less common in UC
170
what is the MOA of methotrexate
Folic acid antagonist that inhibits cytokines production and purine nucleotide biosynthesis -> immunsuppression and anti-inflammatory effects
171
what are the AE of methotrexate
cytotoxic in high doses diarrhea, N/V, alopecia, bone marrow suppression, mucositis contra in pregnancy
172
what are adalimumab/infliximab
biologics moderate to severe UC and CD, generally used as second line agents adalimumab better for Crohn's infliximab better for UC
173
what is the MOA of the biologics
TNF-alpha inhibitors -> helps mitigate overactive immune response
174
what are the SE of biologics
infusion reactions caution with heart disease and liver disease