GI Drugs Flashcards
Learn Class, MOA, Adverse Effects/Unique Features
Aluminum salts
Class: Low-systemic antacid
MOA: binds luminal H+ to produce H2O, CO2, or Cl- salts
Adverse Effects: Constipation, Hypophospatemia
Calcium salts
Class: Low-systemic antacid
MOA: binds luminal H+ to produce H2O, CO2, or Cl- salts
Adverse Effects: Constipation, hypercalcemia, hypophosphatemia, calcium-based kidney stones
Magnesium salts
Class: Low-systemic antacid
MOA: binds luminal H+ to produce H2O, CO2, or Cl- salts
Adverse Effects: Diarrhea, hypermagnesemia
Sodium salts
Class: high-systemic antacid
MOA: Binds luminal H+ to produce H2O, CO2, or Cl- salts
Adverse Effects: Gas/flatulence, hypernatremia, metabolic alkalosis
Simethicone
Class: Supplemental antacid
MOA: surfactant that decreases surface tension of gas bubbles in the GI tract to create one, easily passable gas bubble
Adverse Effects: none listed
Cimetidine
Class: H2 receptor antagonist
MOA: Reversibly inhibits H2-receptors on the basolateral membrane of parietal cells
Adverse Effects: Nausea, diarrhea, constipation, headache
Unique characteristics: gynechomastia in men, galactorrhea in women, neutropenia, thrombocytopenia, prototypical CYP450 inhibitor
Famotidine
Class: H2 receptor antagonist
MOA: Reversibly inhibits H2-receptors on the basolateral membrane of parietal cells
Adverse Effects: Nausea, diarrhea, constipation, headache
Nizatidine
Class: H2 receptor antagonist
MOA: Reversibly inhibits H2-receptors on the basolateral membrane of parietal cells
Adverse Effects: Nausea, diarrhea, constipation, headache
Ranitidine
Class: H2 receptor antagonist
MOA: Reversibly inhibits H2-receptors on the basolateral membrane of parietal cells
Adverse Effects: Nausea, diarrhea, constipation, headache
Lansoprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Dexlansoprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Omeprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Unique Characteristics: prototypical CYP450 inhibitor
Esomeprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Pantoprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Rabeprazole
Class: Proton pump inhibitors
MOA: irreversibly binds sulfhydryl groups of H/K-ATPase at parietal cell secretory sites, inhibiting gastric acid secretion
Adverse Effects: Nausea, diarrhea, dyspepsia, increased risk for C diff infection, HA, dizziness
Sucralfate
Class: Surface acting anti-ulcer agent
MOA: cross-links w/ itself in response to stomach acid to create a sticky polymer that adheres to epithelial cells around the ulcer’s crater
Adverse Effects: Constipation d/t conjugated Al(OH)3
Misoprostol
Class: misoprostol
MOA: reduces gastric acid release from parietal cells and stimulates cytoprotective actions of gastric mucosa
Adverse Effects: diarrhea, cramping, HA, dizziness
Bismuth subsalicylate
Class: bismuth antiulcer agents
MOA: prevents microbial attachment to mucosa, inactivates enterotoxins, disrupts bacterial cell wall
Adverse Effects: constipation, black regularly formed stools
Dolasetron
Class: Serotonin Receptor Antagonist
MOA: blocks serotonin receptors at vagal nerve terminals and block signal transmission to CTZ
Adverse Effects: HA, constipation/diarrhea, serotonin syndrome, QT prolongation, Torsade de pointes
Granisetron
Class: Serotonin Receptor Antagonist
MOA: blocks serotonin receptors at vagal nerve terminals and block signal transmission to CTZ
Adverse Effects: HA, constipation/diarrhea, serotonin syndrome, QT prolongation, Torsade de pointes
Unique characteristic: sustained-release allows for once daily administration
Ondansetron
Class: Serotonin Receptor Antagonist
MOA: blocks serotonin receptors at vagal nerve terminals and block signal transmission to CTZ
Adverse Effects: HA, constipation/diarrhea, serotonin syndrome, QT prolongation, Torsade de pointes
Palonosetron
Class: Serotonin Receptor Antagonist
MOA: blocks serotonin receptors at vagal nerve terminals and block signal transmission to CTZ
Adverse Effects: HA, constipation/diarrhea, serotonin syndrome, QT prolongation, Torsade de pointes
Unique Characteristic: sustained-release allows for once daily administration
Aprepitant
Class: neurokinin-1 receptor antagonist
MOA: blocks NK1 receptors in the CTZ and vomit center
Adverse effects: dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence
Unique Characteristic: given up to 3 hours prior to anesthesia induction to control vomiting
Fosaprepitant
Class: neurokinin-1 receptor antagonist
MOA: blocks NK1 receptors in the CTZ and vomit center
Adverse effects: dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence
Netupitant
Class: neurokinin-1 receptor antagonist
MOA: blocks NK1 receptors in the CTZ and vomit center
Adverse effects: dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence
Unique characteristic: longer half-life
Fosnetupitant
Class: neurokinin-1 receptor antagonist
MOA: blocks NK1 receptors in the CTZ and vomit center
Adverse effects: dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence
Unique characteristic: longer half-life
Rolapitant
Class: neurokinin-1 receptor antagonist
MOA: blocks NK1 receptors in the CTZ and vomit center
Adverse effects: dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence
Diphenhydramine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Dimenhydrinate
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Hydroxyzine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Promethazine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Meclizine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Cyclizine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Doxylamine
Class: Histamine-1 Receptor Antagonist
MOA: blocks H1 receptors in the VC and vestibular system
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, decreased BP
Chlorpromazine
Class: Phenothiazine Dopamine-2 receptor antagonist
MOA: blocks D2 receptors in the CTZ
Adverse Effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, arrhythmias
Perphenazine
Class: Phenothiazine Dopamine-2 receptor antagonist
MOA: blocks D2 receptors in the CTZ
Adverse Effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, arrhythmias
Prochlorperazine
Class: Phenothiazine Dopamine-2 receptor antagonist
MOA: blocks D2 receptors in the CTZ
Adverse Effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, arrhythmias
Metoclopramide
Class: Dopamine-2 receptor antagonist
MOA: blocks D2 receptors in the CTZ
Adverse Effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision, arrhythmias
Scopolamine
Class: Muscarinic-1 receptor antagonist
MOA: blocks M1 receptors in neural pathways from the vestibular nuclei in the inner ear to the brain stem and from the reticular formation to the VC
Adverse effects: Drowsiness, dry mouth, constipation, urinary retention, blurred vision
Dronabinol
Class: Cannabinoids
MOA: stimulation of CB1 and CB2 receptors in VC/CTZ to minimize release of serotonin from vagal afferent terminals
Adverse effects: euphoria, irritability, vertigo, sedation, drowsiness, impaired cognition, memory, hallucinations, distorted sense of time, xerostomia, increased HR and BP, appetite stimulation
Unique Characteristic: schedule III drug, large first-pass effect
Nabilone
Class: Cannabinoids
MOA: stimulation of CB1 and CB2 receptors in VC/CTZ to minimize release of serotonin from vagal afferent terminals
Adverse effects: euphoria, irritability, vertigo, sedation, drowsiness, impaired cognition, memory, hallucinations, distorted sense of time, xerostomia, increased HR and BP, appetite stimulation
Unique characteristic: schedule II drug, metabolized to several active metabolites
Sulfasalzine
Class: 5-ASA
MOA: inhibition of prostaglandin and leukotriene formation via arachidonic acid pathway, reduction in macrophage chemotaxis
Adverse effects: aspirin allergy
Unique characteristic: sulfa drug
Mesalamine
Class: 5-ASA
MOA: inhibition of prostaglandin and leukotriene formation via arachidonic acid pathway, reduction in macrophage chemotaxis
Adverse effects: aspirin allergy
Unique characteristic: single 5-ASA molecule
Olsalazine
Class: 5-ASA
MOA: inhibition of prostaglandin and leukotriene formation via arachidonic acid pathway, reduction in macrophage chemotaxis
Adverse effects: aspirin allergy
Unique characteristic: 2 5-ASA molecules
Balsalazine
Class: 5-ASA
MOA: inhibition of prostaglandin and leukotriene formation via arachidonic acid pathway, reduction in macrophage chemotaxis
Adverse effects: aspirin allergy
Unique characteristic: inert carrier + 5-ASA
Tofacitinib
Class: JAK inhibitor
MOA: sequestration of free-floating and bound JAK-1 and JAK-3 to inhibit gene transcription and cytokine release
Adverse Effects: lymphopenia, neutropenia, anemia, fatigue, increased LDL and HDL
Adalimumab
Class: TNF-α inhibitor
MOA: binds and neutralizes membrane-associated and soluble TNF-α to block leukocyte migration
Adverse Effects: reactivation of TB, liver injury, HA, arthralgia, fatigue
Golimumab
Class: TNF-α inhibitor
MOA: binds and neutralizes membrane-associated and soluble TNF-α to block leukocyte migration
Adverse Effects: reactivation of TB, liver injury, HA, arthralgia, fatigue
Unique Characteristic: only indicated for ulcerative colitis
Certolizumab
Class: TNF-α inhibitor
MOA: binds and neutralizes membrane-associated and soluble TNF-α to block leukocyte migration
Adverse Effects: reactivation of TB, liver injury, HA, arthralgia, fatigue
Unique Characteristic: only indicated for Crohn disease
Infliximab
Class: TNF-α inhibitor
MOA: binds and neutralizes membrane-associated and soluble TNF-α to block leukocyte migration
Adverse Effects: reactivation of TB, liver injury, HA, arthralgia, fatigue
Vedolizumab
Class: α4 Integrin inhibitor
MOA: limits integrin-associated cell adhesion and subsequent trans-endothelial migration of leukocytes
Adverse Effects: Infusion-related side effects, anti-medication antibody formation
Unique characteristics: increased risk for malignancies
Natalizumab
Class: α4 Integrin inhibitor
MOA: limits integrin-associated cell adhesion and subsequent trans-endothelial migration of leukocytes
Adverse Effects: Infusion-related side effects, anti-medication antibody formation
Unique characteristics: progressive multifocal leukoencephalopathy (infection w/ JC virus)
Ustekinumab
Class: IL-12/-23 Inhibitors
MOA: Binds to p40 subunit of IL-12/-23 to block activation and differentiation of naive T cells and NK cell activation
Adverse Effects: reactivation of TB, infusion/injection-related allergic reactions, HA, arthralgia, fatigue
Loperamide
Class: opioid agonist
MOA: interferes w/ peristalsis via direct action on circular and longitudinal muscles of intestinal wall
Adverse Effects: dizziness, fatigue, drowsiness, urinary retention
Unique characteristics: cardiac toxicities that can lead to death
Diphenoxylate
Class: opioid agonist
MOA: exerts local and central effect on GI smooth muscle cells to inhibit GI motility and slow excess GI propulsion
Adverse Effects: dizziness, fatigue, drowsiness, urinary retention
Unique characteristic: opioid agonist + atropine (to curb abuse)
Eluxadoline
Class: opioid agonist
MOA: mu and kappa receptor agonist in GI tract to slow peristalsis, delta receptor antagonist to decrease stomach/pancreas/biliary secretions
Adverse Effects: dizziness, fatigue, drowsiness, urinary retention
Unique Characteristic: hepatic/pancreatic toxicity
Alosetron
Class: Serotonin receptor antagonist
MOA: selective blockade of GI serotonin receptors to regulate visceral pain, colonic transit, and GI secretions
Adverse Effects: Ischemic colitis
Unique characteristics: requires special prescriber program, only indicated in chronic severe IBS-D that is not responsive to other conventional therapies
Crofelemer
Class: Chloride channel inhibitor
MOA: inhibition of chloride anion secretion by blocking CFTR and calcium-activated chloride channels
Adverse Effects: abd distention, elevated AST/ALT/bilirubin, respiratory/urinary infections
Unique characteristics: indicated in non-infectious diarrhea for HIV/AIDS pts
Methylnaltrexone
Class: peripheral opioid antagonist
MOA: peripheral mu receptor blockade increases GI motility
Adverse Effects: abd pain, diarrhea, N/V
Naloxegol
Class: peripheral opioid antagonist
MOA: peripheral mu receptor blockade increases GI motility
Adverse Effects: abd pain, diarrhea, N/V
Alvimopan
Class: peripheral opioid antagonist
MOA: peripheral mu receptor blockade increases GI motility
Adverse Effects: abd pain, diarrhea, N/V
Unique Characteristics: increased risk for MI w/ use; only used in post-op ileus prevention
Linaclotide
Class: Guanylate Cyclase-C agonists
MOA: binds GC-C on luminal surface of intestinal epithelium to increase cGMP stimulation of chloride/bicarb secretion
Adverse Effects: diarrhea, GERD, dyspepsia, N/V
Unique characteristic: indicated in IBS-C and chronic idiopathic constipation
Lubiprostone
Class: selective chloride channel activators
MOA: PGE-1 analog that increases activation of GI specific chloride channels (CIC-2) in luminal cells of intestinal epithelium
Adverse Effects: Nausea, dyspepsia, dizziness
Bisacodyl
Class: stimulant laxative
MOA: irritates enterocytes, GI smooth muscle cells to promote water and electrolyte accumulation in the lumen, prompting peristalsis to remove irritants
Adverse Effects: abdominal cramping, urine discoloration, fluid/electrolyte disturbances, perforated bowel (in GI obstruction)
Unique characteristics: faster onset (0.5 - 2 hours)
Castor oil
Class: stimulant laxative
MOA: irritates enterocytes, GI smooth muscle cells to promote water and electrolyte accumulation in the lumen, prompting peristalsis to remove irritants
Adverse Effects: abdominal cramping, urine discoloration, fluid/electrolyte disturbances, perforated bowel (in GI obstruction)
Glycerin
Class: stimulant laxative
MOA: irritates enterocytes, GI smooth muscle cells to promote water and electrolyte accumulation in the lumen, prompting peristalsis to remove irritants
Adverse Effects: abdominal cramping, urine discoloration, fluid/electrolyte disturbances, perforated bowel (in GI obstruction)
Unique characteristics: faster onset (0.5 - 2 hours)
Senna
Class: stimulant laxative
MOA: irritates enterocytes, GI smooth muscle cells to promote water and electrolyte accumulation in the lumen, prompting peristalsis to remove irritants
Adverse Effects: abdominal cramping, urine discoloration, fluid/electrolyte disturbances, perforated bowel (in GI obstruction)
Na+ picosulfate
Class: stimulant laxative
MOA: irritates enterocytes, GI smooth muscle cells to promote water and electrolyte accumulation in the lumen, prompting peristalsis to remove irritants
Adverse Effects: abdominal cramping, urine discoloration, fluid/electrolyte disturbances, perforated bowel (in GI obstruction)
Lactulose
Class: Osmotic laxative
MOA: osmotically attracts and retains water in the colon to increase moisture, softness, and volume/bulk of stools
Adverse effects: electrolyte disturbances, N/V, diarrhea
Unique characteristic: used to trap ammonia in liver disease
Magnesium citrate
Class: Osmotic laxative
MOA: osmotically attracts and retains water in the colon to increase moisture, softness, and volume/bulk of stools
Adverse effects: electrolyte disturbances, N/V, diarrhea
Polyethylene glycol (PEG)
Class: Osmotic laxative
MOA: osmotically attracts and retains water in the colon to increase moisture, softness, and volume/bulk of stools
Adverse effects: electrolyte disturbances, N/V, diarrhea
Unique Characteristics: used as pre-surgical bowel prep
Sorbitol
Class: Osmotic laxative
MOA: osmotically attracts and retains water in the colon to increase moisture, softness, and volume/bulk of stools
Adverse effects: electrolyte disturbances, N/V, diarrhea
Magnesium Hydroxide
Class: Saline cathartic
MOA: create hyperosmolar solutions that pull fluid into the stool and inhibits reabsorption of water in the GI tract to increase stool volume, shortening transit time
Adverse Effects: electrolyte imbalance, hypernatremia
Na+ phosphate
Class: Saline cathartic
MOA: create hyperosmolar solutions that pull fluid into the stool and inhibits reabsorption of water in the GI tract to increase stool volume, shortening transit time
Adverse Effects: electrolyte imbalance, hypernatremia
Dietary fiber
Class: bulk forming cathartic
MOA: increase bulk volume and water content to increase GI motility, supports colonic bacteria fermentation and digestion
Adverse effects: bloating, obstruction
Psyllium
Class: bulk forming cathartic
MOA: increase bulk volume and water content to increase GI motility, supports colonic bacteria fermentation and digestion
Adverse effects: bloating, obstruction
Unique characteristics: many drug interactions
Methylcellulose/carboxymethylcellulose
Class: bulk forming cathartic
MOA: increase bulk volume and water content to increase GI motility, supports colonic bacteria fermentation and digestion
Adverse effects: bloating, obstruction
Unique characteristics: many drug interactions
Calcium polycarbophil
Class: bulk forming cathartic
MOA: increase bulk volume and water content to increase GI motility, supports colonic bacteria fermentation and digestion
Adverse effects: bloating, obstruction
Docusate
Class: stool softener
MOA: increases fluid secretion and inhibits water reabsorption to soften and lubricate already formed stool
Adverse Effects: N/V/D
Mineral Oil
Class: stool softener
MOA: increases fluid secretion and inhibits water reabsorption to soften and lubricate already formed stool
Adverse Effects: N/V/D
Hyoscyamine
Class: antimuscarinic agents
MOA: competitive inhibition of muscarinic receptors to decrease GI motility and spasms
Adverse Effects: dry mouth, urinary retention, constipation, drowsiness, mental confusion, blurred vision
Dicyclomine
Class: antimuscarinic agents
MOA: competitive inhibition of muscarinic receptors to decrease GI motility and spasms
Adverse Effects: dry mouth, urinary retention, constipation, drowsiness, mental confusion, blurred vision
Clidinium/chlordiazepoxide
Class: antimuscarinic agents
MOA: competitive inhibition of muscarinic receptors to decrease GI motility and spasms
Adverse Effects: dry mouth, urinary retention, constipation, drowsiness, mental confusion, blurred vision
Drugs to treat CDI
Vancomycin
Metronidazole
Fidaxomicin
H. Pylori Treatments
Bismuth subsalicylate
Metronidazole
Tetracycline
Omeprazole
E. histolytica treatment
Metronidazole
Tinidazole
Paromomycin
Iodoquinol
Giardia lamblia treatment
Tinidazole
Metronidazole
Nitazoxanide
C. parvum treatment
Nitazoxanide
Nematodes treatment
Albendazole Mebendazole Ivermectin Thiabendazole Pyrantel pamoate
Schistosoma treatment
Praziquantel
Cestode treatments
Praziquantel
Niclosamide
Albendazole