DSA26 - Pharmacotherapy of GI Managements of NV, Diarrhea and Constipation

Loperamide MoA

Opioid (Peripherally-acting mu receptor agonist)

Loperamide Tx

Diarrhea, Traveler's Diarrhea, IBS-D

Loperamide S/E

Abdominal Pain, Nausea, Constipation

Eluxadoline MoA

Opioid (Mu agonist, Delta Antagonist)

Eluxadoline Tx

Diarrhea, IBS-D

Eluxadoline S/E

C/I = Biliary Disorders, Pancreatitis, No Gallbladder, Alcoholism + S/E = Abdominal Pain, Nausea, Constipation

Diphenoxylate + atropine MoA

Opioid

Diphenoxylate + atropine Tx

Diarrhea

Octreotide MoA

Somatostatin Analog; inhibits GI motiltiy and secretion

Octreotide Tx

Severe diarrhea (endocrine tumor or AIDS)

Octreotide S/E

Abdominal pain, nausea, headache, dizziness, arrhythmia, hyperglycemia

Bismuth Subsalicylate MoA

Anti-inflammatory/anti-microbial/anti-acid/anti-motility (increases water absorption + inhibits motility via ASA)

Bismuth Subsalicylate Tx

Diarrhea

Ciprofloxacin MoA

Abx

Ciprofloxacin Tx

Severe Traveler's Diarrhea, Inflammatory Bowel Disease

Metronidazole MoA

Abx

Metronidazole Tx

Inflammatory Bowel Disease

Rifaximin MoA

Abx

Rifaximin Tx

Severe Traveler's Diarrhea, IBS-D

Azithromycin MoA

Abx

Azithromycin Tx

Off-Label for Traveler's Diarrhea + Fluoroquinolone-resistant bacteria (Campylobacter)

Azithromycin S/E

Abdominal pain, nausea/vomiting, prolonged QT interval

Methylcellulose MoA

Bulk-Forming Laxative

Methylcellulose Tx

Simple Constipation

Psyllium MoA

Bulk-Forming Laxative

Psyllium Tx

Simple Constipation, IBS-C

Ca2+ polycarbophil MoA

Bulk-Forming Laxative

Ca2+ polycarbophil Tx

Simple Constipation

Bran MoA

Bulk-Forming Laxative

Bran Tx

Simple Constipation

Bisacodyl MoA

Stimulant Laxative; Stimulates ENS --> More AC activity --> more cAMP

Bisacodyl Tx

Bowel Prep for Surgery

Linaclotide MoA

Stimulant Laxative; Stimulates GC --> more cGMP

Linaclotide Tx

IBS-C Chronic Constipation

Linaclotide S/E

S/E = Diarrhea, Abd Pain; BBW = CI if < 6 yo, AVOID if < 18 yo

Senna MoA

Stimulant Laxative

Senna Tx

Occassional Constipation

Lubiprostone MoA

Stimulant Laxative; Increases Cl- Ion channel influx

Lubiprostone Tx

IBS-C Chronic Constipation

Lubiprostone S/E

Diarrhea, Nausea, Abd Pain

Mg2+ hydroxide/citrate MoA

Osmotic/saline Laxatives

Mg2+ hydroxide/citrate Tx

Simple Constipation

Sorbitol MoA

Osmotic/saline Laxative

Sorbitol Tx

Occassional Constipation (5-7% found in PRUNE JUICE)

Na+ phosphate MoA

Osmotic/saline Laxatives

Na+ phosphate Tx

Acute Constipation

Lactulose MoA

Osmotic/saline Laxatives

Lactulose Tx

Chronic Constipation --> Lactic/Acetic Acids

Polyethylene glycol-electrolyte solutions MoA

Osmotic/saline Laxatives

Polyethylene glycol-electrolyte solutions Tx

PEG; Complete Colon Cleaning

Docusate/Mineral Oil MoA

Surfactant/Stool Softeners

Docusate/Mineral Oil Tx

Acute Constipation - reduces straining (limited clinical use d/t lack of effectiveness)

Methylnaltrexone MoA

Opioid Antagonist

Methylnaltrexone Tx

Opioid Induced Constipation (OIC)

Ondansetron (+dexamethasone+aprepitant) MoA

5-HT3R Antagonist (target CTZ)

Ondansetron (+dexamethasone+aprepitant) Tx

Vomiting

Metoclopramide (central effect) MoA

D2R Antagonist(target CTZ)

Metoclopramide (central effect) Tx

Vomiting

Metoclopramide (central effect) S/E

S/E = Nausea, HA, Weak/Fatigue; BBW = Tardive Dyskinesia & Other Extrapyramidal Sx

Metoclopramide (peripheral pro-kinetic effect) MoA

D2R Antagonist (dis-inhibits PNS, increases esophageal sphincter tone, stimulates gastric emptying)

Metoclopramide (peripheral pro-kinetic effect) Tx

Diabetic gastroparesis, GERD, Post-OP & Chemo-induced N/V (Central anti-emetic)

Metoclopramide (peripheral pro-kinetic effect) S/E

S/E = Nausea, HA, Weak/Fatigue; BBW = Tardive Dyskinesia & Other Extrapyramidal Sx

Palonosetron MoA

5-HT3R Antagonist(target CTZ)

Palonosetron Tx

Vomiting

Promethazine MoA

H1R Antagonist

Promethazine Tx

Motion Sickness, Postop N/V

Promethazine S/E

S/E = Drowsiness; BBW = Fatal Resp Depression if < 2 yo

Meclizine MoA

H1R Antagonist

Meclizine Tx

Motion Sickness, Postop N/V, VERTIGO

Meclizine S/E

Xerostomina (Anti-ACh), Drowsiness

Diphenhydramine MoA

H1R Antagonist

Diphenhydramine Tx

Motion Sickness, Postop N/V

Dronabinol MoA

Cannabinoid

Dronabinol Tx

Chemo-induced N/V

Aprepitant MoA

Neurokinin 1 Receptor Antagonist

Aprepitant Tx

Chemo-induced AND Post-Op N/V (ADD to Ondasteron + Dexamethasone for added efficacy for Anti-Emetic effect)

Erythromycin MoA

Abx; Motilin Receptor Agonist

Erythromycin Tx

Vomiting

Erythromycin S/E

Abd Pain, N/V, Diarrhea, Arrhythmia, Tachycardia, QT Prolong

Dicyclomine MoA

Weak Anti-Muscarininc Agent (Anti-Spasmodic)

Dicyclomine Tx

IBS

5-aminosalicylic acid (Mesalamine) MoA

Inhibit inflammatory mediators, cytokines & immune cells, scavengers of reactive oxygen species

5-aminosalicylic acid (Mesalamine) Tx

Inflammatory Bowel Disease

5-aminosalicylic acid (Mesalamine) S/E

Hypersensitivity (rare)

Sulfasalazine (=mesalamine+sulfapyridine) MoA

Inhibit inflammatory mediators, cytokines & immune cells, scavengers of reactive oxygen species

Sulfasalazine (=mesalamine+sulfapyridine) Tx

Inflammatory Bowel Disease

Sulfasalazine (=mesalamine+sulfapyridine) S/E

D/t Sulfapyridine (Abd Pain, Diarrhea, Nausea, HA, Arthralgia, Myalgia, Infex + Hypersensitivty (Fever, Dermatitis, Pancreatitis, Pneumonitis, Hepatitis, Pericarditis); Inhibit Folate Absorption

Prednisone MoA

Corticosteroid

Prednisone Tx

Inflammatory Bowel Disease

Hydrocortisone MoA

Corticosteroid

Hydrocortisone Tx

Inflammatory Bowel Disease

Budesonide MoA

Corticosteroid

Budesonide Tx

Inflammatory Bowel Disease

Adalimumab MoA

Anti-TNF/Integrin Ab

Adalimumab Tx

Inflammatory Bowel Disease

Adalimumab S/E

BBW = Infex, Lymphoma

Infliximab MoA

Anti-TNF/Integrin Ab

Infliximab Tx

Inflammatory Bowel Disease

Infliximab S/E

BBW = Infex, Lymphoma

Vedolizumab MoA

Anti-Alpha-4-Beta-7 Integrin Ab: Inhibits lymphocyte traffic