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GI/Nutrition > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

omeprazole

A

class: proton pump inhibitor
MoA: prodrug, weak base activated by acid, forms disulfide bond with cysteine residue on proton pump to irreversibly inhibit its action; ideally given 30 minutes before meals to coordinate with maximum pump expression/activity
uses: healing of peptic ulcers, GERD, erosive esophagitis, ulcers associated with H. pylori, Zollinger-Ellison syndrome
side effects: nausea, abdominal pain, constipation, flatulence, diarrhea
other: inhibits CYP2C19 (prevents activation of clopidogrel)

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2
Q

esomeprazole

A

class: proton pump inhibitor
MoA: prodrug, weak base activated by acid, forms disulfide bond with cysteine residue on proton pump to irreversibly inhibit its action; ideally given 30 minutes before meals to coordinate with maximum pump expression/activity
uses: healing of peptic ulcers, GERD, erosive esophagitis, ulcers associated with H. pylori, Zollinger-Ellison syndrome
side effects: nausea, abdominal pain, constipation, flatulence, diarrhea
other:

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3
Q

lansoprazole

A

class: proton pump inhibitor
MoA: prodrug, weak base activated by acid, forms disulfide bond with cysteine residue on proton pump to irreversibly inhibit its action; ideally given 30 minutes before meals to coordinate with maximum pump expression/activity
uses: healing of peptic ulcers, GERD, erosive esophagitis, ulcers associated with H. pylori, Zollinger-Ellison syndrome, recurrent NSAID-associated gastric ulcers
side effects: nausea, abdominal pain, constipation, flatulence, diarrhea
other:

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4
Q

cimetidine

A

class: H2 receptor antagonist
MoA: reversibly and competitively inhibits H2 receptors; predominantly inhibits basal acid secretion
uses: healing of peptic ulcers, GERD, stress ulcer prevention
side effects: diarrhea, headache, drowsiness, CNS effects (rare)
other: less potent than PPIs, but good for nocturnal acid secretion; inhibits P450 metabolism (prolongs half-life of warfarin, gynecomastia in men)

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5
Q

ranitidine

A

class: H2 receptor antagonist
MoA: reversibly and competitively inhibits H2 receptors; predominantly inhibits basal acid secretion
uses: healing of peptic ulcers, GERD, stress ulcer prevention
side effects: diarrhea, headache, drowsiness, CNS effects (rare)
other: less potent than PPIs, but good for nocturnal acid secretion

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6
Q

aluminum hydroxide

A 
class: antacid
MoA: weak base, reacts with gastric HCl to form salt and water and neutralize acid; stimulates protective functions of mucosa
uses: indigestion
side effects: constipation
other:
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7
Q

calcium carbonate

A

class: antacid
MoA: weak base, reacts with gastric HCl to form salt and water and neutralize acid; stimulates protective functions of mucosa
uses: indigestion
side effects: gastric distention, belching, metabolic alkalosis
other:

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8
Q

magnesium hydroxide

A 
class: antacid
MoA: weak base, reacts with gastric HCl to form salt and water and neutralize acid; stimulates protective functions of mucosa
uses: indigestion
side effects: osmotic diarrhea
other:
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9
Q

sucralfate

A

class: sucrose salt
MoA: unknown; forms paste-like substance in base of ulcers or erosion; stimulates mucosal prostaglandin and bicarbonate secretion
uses: short-term management of duodenal ulcers, NSAID mucosal damage, stress ulcer prevention
side effects: constipation (rare)
other: very small amount of drug is absorbed into systemic circulation

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10
Q

misoprostol

A

class: prostaglandin analog
MoA: stimulates EP3 on parietal cells –> decrease cAMP –> decreased acid production; also EP3 –> promotes mucin and bicarbonate secretion
uses: replacement therapy for prevention of NSAID-associated ulcers
side effects: diarrhea, abortifacient
other:

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11
Q

bismuth subsalicylate

A

class: bismuth salt
MoA: unknown; binds base of ulcer, promotes mucin and bicarbonate production, antibacterial effects, anti-inflammatory effects
uses: peptic ulcers, traveler’s diarrhea, episodic diarrhea, gastroenteritis
side effects: black stool, Reye’s syndrome
other: salicylate is absorbed but bismuth is not

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12
Q

H. pylori treatment

A

initial treatment: PPI + amoxicillin + clarithromycin
penicillin allergy: PPI + metronidazole + clarithromycin
retreatment or clarithromycin resistance: omeprazole + bismuth subcitrate + metronidazole + tetracycline

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13
Q

scopolamine

A

class: anticholinergic
MoA: competitively antagonizes ACh receptors
uses: motion sickness prophylactic, nausea prophylaxis during recovery from anesthesia
side effects: dry mouth, drowsiness, blurred vision
other: transdermal patch; most effective as prophylactic agent (4-6 hrs before exposure to stressor)

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14
Q

dimenhydrinate

A

class: antihistamine
MoA: competitively inhibits H1 receptors, anticholinergic, blocks chemoreceptor trigger zone, diminishes vestibular stimulation
uses: motion sickness (off-label: nausea and vomiting during pregnancy)
side effects: sedation
other:

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15
Q

ondansetron

A

class: 5-HT3 antagonist
MoA: blocks peripheral 5-HT3 receptors on extrinsic intestinal vagal and spinal afferent nerves
uses: anti-emetic (prevention), hyperemesis gravidarum
side effects: headache, dizziness, constipation, QT prolongation
other: oral; hepatic metabolism by conjugation and P450s (effect prolonged with liver disease)

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16
Q

granisetron

A

class: 5-HT3 antagonist
MoA: blocks peripheral 5-HT3 receptors on extrinsic intestinal vagal and spinal afferent nerves
uses: anti-emetic (prevention), hyperemesis gravidarum
side effects: headache, dizziness, constipation, QT prolongation
other: transdermal patch (48 hrs to peak concentration)

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17
Q

prochlorperazine

A

class: dopamine antagonist
MoA: blocks postsynaptic dopaminergic D2 receptors in chemoreceptor trigger zone; anticholinergic, antihistaminergic, and alpha-adrenergic antagonist
uses: management of surgical and non-surgical nausea and vomiting, opioid-induced PONV
side effects: sedation, dystonia, tradeoff dyskinesia, elderly pts with dementia-related psychosis at increased risk of death
other:

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18
Q

dronabinol

A

class: cannabinoid
MoA: synthetic form of THC, acts on CB1 receptors in CNS, exact mechanism unknown
uses: nausea and vomiting in chemotherapy pts who are refractory to conventional antiemetic treatments
side effects: vertigo, dry mouth, hypotension, dysphoria (esp. in older pts)
other: CYP450 metabolism

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19
Q

dexamethasone

A

class: corticosteroid
MoA: mechanism of antiemetic action is unknown
uses: adjunctive vomiting prophylaxis in chemotherapy, postoperative nausea/vomiting prophylaxis
side effects: insomnia, increased energy, mood changes
other:

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20
Q

aprepitant

A

class: neurokinin receptor antagonist
MoA: crosses blood-brain barrier, antagonizes substance P at NK1 receptors in vomiting reflex center of brain
uses: prevention of nausea due to chemotherapy (in combination with 5-HT3 receptor antagonists and corticosteroids) or post-op
side effects: fatigue, dizziness, diarrhea
other: metabolized by CYP3A4 (inhibits metabolized by CYP3A4, i.e. warfarin)

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21
Q

metoclopramide

A

class: prokinetic
MoA: 5-HT4 receptor antagonist, vagal and central 5-HT3 antagonist, sensitization of muscarinic receptors on smooth muscle; results in coordinated contractions that enhance transit (primarily effective in upper GI tract)
uses: GERD, diabetic gastroparesis, propylaxis for nausea and vomiting with chemotherapy, prophylaxis for post-op nausea and vomiting
side effects: extrapyramidal effects, tradeoff dyskinesia, galactorrhea
other: first-pass hepatic metabolism (at least in part by P450s)

22
Q

erythromycin

A

class: macrolide antibiotic
MoA: prokinetic, effects mimic motilin
uses: diabetic gastroparesis (off-label)

23
Q

loperamide

A

class: opioid
MoA: mu opioid receptor agonist; inhibits peristalsis, prolongs transit time, reduces fecal volume, increases stool viscosity
uses: traveler’s diarrhea, chronic diarrhea
side effects: dizziness, constipation, abdominal cramping, nausea
other:

24
Q

diphenoxylate

A

class: opioid
MoA: mu opioid receptor agonist; inhibits peristalsis, prolongs transit time, reduces fecal volume, increases stool viscosity
uses: traveler’s diarrhea, chronic diarrhea
side effects: penetrates CNS at high doses (abuse potential)
other: some preparations contain sub-therapeutic doses of atropine to discourage abuse

25
Q

octreotide

A

class: somatostatin analog
MoA: inhibits secretion of 5-HT and other GI peptides
uses: severe secretory diarrhea due to hormone-secreting tumors, chemotherapy, HIV, diabetes, gastric surgery
side effects: nausea, bloating, injection site pain; long-term may cause gallstones or hypo-/hyperglycemia
other:

26
Q

kaolin + pectin

A

class: aluminum silicate clay + plant polysaccharide
MoA: binds water to increase stool bulk, alters stool viscosity
uses: mild diarrhea, IBS
side effects:
other:

27
Q

magnesium hydroxide

A

class: saline laxative
MoA: osmotic retention of water due to lack of absorption of magnesium; possibly induces production of inflammatory mediators
uses: constipation
side effects:
other: use with caution in pts with renal insufficiency, cardiac disease, or preexisting electrolyte abnormalities

28
Q

lactulose

A

class: non-digestible sugar
MoA: synthetic disaccharide of galactose and fructose, hydrolyzed to short-chain fatty acids in colon, stimulates propulsive motility, osmotically draws water into lumen, lowers lumenal pH, traps ammonia by conversion to ammonium ion
uses: opioid-induced constipation, constipation in the elderly, chronic constipation
side effects: gas, cramping, abdominal distention (first 24-48 hrs)
other:

29
Q

polyethylene glycol

A 
class: laxative
MoA: poorly absorbed, osmotically retains water in intestinal lumen
uses: colonic cleansing, constipation
side effects:
other:
30
Q

docusate salts

A 
class: laxative
MoA: anionic surfactant, lowers stool surface tension to permit easier defecation
uses: constipation, colonic cleansing
side effects:
other:
31
Q

bisacodyl

A

class: stimulant/irritant laxative
MoA: prodrug activated by endogenous esterases in bowel; has direct effects on enterocytes, enteric neurons, and GI smooth muscle; induces low-grade inflammation; produces giant migrating colonic contractions, induces water and electrolyte secretion
uses: constipation

32
Q

senna

A

class: stimulant/irritant laxative
MoA: has direct effects on enterocytes, enteric neurons, and GI smooth muscle; induces low-grade inflammation; produces giant migrating colonic contractions, induces water and electrolyte secretion
uses: constipation

33
Q

lubiprostone

A

class: laxative
MoA: poorly absorbed, activates chloride channels by activating EP4 receptors linked to adenylyl cyclase
uses: chronic constipation, IBS
side effects: nausea, headache, diarrhea, allergic reactions, dyspnea

34
Q

linaclotide

A

class: laxative
MoA: synthetic peptide, poor absorption, activates guanylate cyclase C receptor on luminal surface of intestinal epithelium to stimulate cGMP production; leads to Cl- and bicarbonate secretion; may also reduce pain-sensing nerve activity
uses: chronic idiopathic constipation, IBS
side effects: diarrhea, abdominal pain
other:

35
Q

methylnaltrexone

A

class: opioid antagonist
MoA: acts peripherally to block mu opioid receptor
uses: opioid-induced constipation in pts with advanced illness and inadequate response to conventional laxative regimens
side effects: abdominal pain, gas, nausea
other: limited ability to cross blood-brain barrier, orally active

36
Q

alvimopan

A

class: laxative
uses: restricted - postoperatve ileus post-bowel resection

37
Q

dietary fiber

A

lignin (bran): unfermented, has laxative effect
pectins, hemicelluloses (fruits and vegetables): fermented, less effective than lignin, can cause bloating and gas
fiber also effective against diarrhea (mild diarrhea, IBS); binds water to add bulk to stool

38
Q

alosetron

A

class: serotonin antagonist
MoA: antagonizes 5-HT3 receptor; decreases gut contractility, decreases colonic transit, increases fluid absorption; may also blunt visceral sensation
uses: diarrhea-predominant IBS
side effects: ischemic colitis

39
Q

prednisone

A

class: corticosteroid
MoA: dampens inflammatory response
uses: moderate to severe episodes of IBD
side effects: increased hunger, weight gain, sleep disturbance, behavioral changes, irritability, increased BP
other: pts may be responsive, dependent, or unresponsive; treatment aims to limit duration and dose of use

40
Q

budesonide

A

class: corticosteroid (enteric release synthetic)
MoA: dampens inflammatory response
uses: mild to moderate Crohn’s disease
side effects: minimal (less than prednisone) - increased hunger, weight gain, sleep disturbance, behavioral changes, irritability, increased BP
other: enteric release delivers therapy to bowel while minimizing side effects

41
Q

mesalamine

A

class: 5-aminosalicylate
MoA: inhibits IL-1 and TNF-a, lipoxygenase pathway, free radical and oxidant scavenging, possibly NF-kB (not related to COX inhibition)
uses: mild to moderate ulcerative colitis (first-line)
side effects: infrequent and minor - headache, dyspnea, skin rash
other: contraindicated in pts allergic to salicylates; delayed-release (active throughout s. and l. bowel) and pH-sensitive (active in ileum and colon) formulations available

42
Q

olsalazine

A

class: 5-aminosalicylate
MoA: inhibits IL-1 and TNF-a, lipoxygenase pathway, free radical and oxidant scavenging, possibly NF-kB (not related to COX inhibition)
uses: mild to moderate ulcerative colitis (first-line)
other: contraindicated in pts allergic to salicylates, active in colon

43
Q

sulfasalazine

A

class: 5-aminosalicylate
MoA: prodrug, activated by colonic bacteria; inhibits IL-1 and TNF-a, lipoxygenase pathway, free radical and oxidant scavenging, possibly NF-kB (not related to COX inhibition)
uses: mild to moderate ulcerative colitis (first-line)
side effects: fever, malaise, vomiting, headache
other: contraindicated in pts allergic to salicylates, active in colon

44
Q

6-mercaptopurine

A

class: immunosuppressant
MoA: impairs purine biosynthesis, inhibits cell proliferation
uses: maintenance of remission of IBD, Crohn’s-related fistulas, prophylaxis against recurrence of Crohn’s following surgical resection
side effects: bone marrow suppression, vomiting, jaundice, pancreatitis
other:

45
Q

azathioprine

A

class: immunosuppressant
MoA: impairs purine biosynthesis, inhibits cell proliferation
uses: maintenance of remission of IBD, Crohn’s-related fistulas, prophylaxis against recurrence of Crohn’s following surgical resection
side effects: bone marrow suppression, vomiting, jaundice, pancreatitis
other:

46
Q

methotrexate

A

class: immunosuppressant
MoA: inhibits dihydrofolate reductase, thereby blocking DNA synthesis and causing cell death
uses: steroid-resistance or steroid-dependent IBD
side effects: bone marrow suppression, vomiting, jaundice, pancreatitis
other:

47
Q

infliximab

A

class: biologic (antibody)
MoA: neutralizes TNF-a
uses: moderate to severe Crohn’s disease, Crohn’s-related fistulas, acute flares, maintains remission
side effects: fever, chills, anaphylaxis, lupus-like symptoms, risk of respiratory infection, reactivation of TB, non-Hodgkin’s lymphoma
other: contraindicated in pts with severe congestive heart failure

48
Q

adalimumab

A

class: biologic (antibody)
MoA: neutralizes TNF-a
uses: induce remission in mild to moderate, severe, and fistulizing Crohn’s disease
side effects: fever, chills, anaphylaxis, lupus-like symptoms, risk of respiratory infection, reactivation of TB, non-Hodgkin’s lymphoma
other: contraindicated in pts with severe congestive heart failure

49
Q

certolizumab pegol

A

class: biologic (pegylated Fab fragment)
MoA: neutralizes TNF-a
uses: moderate to severe Crohn’s disease
side effects: hepatotoxicity, hypersensitivity reaction
other: contraindicated with other immune-modulating drugs (risk of progressive multifocal leukoencephalopathy)

50
Q

natalizumab

A

class: biologic (antibody)
MoA: neutralizes alpha4-integrin (VLA-4), reduces migration of leukocytes to sites of inflammation
uses: moderate to severe Crohn’s disease
side effects: hepatotoxicity, hypersensitivity reaction
other: contraindicated with other immune-modulating drugs (risk of progressive multifocal leukoencephalopathy)

GI/Nutrition (3 decks)

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