Katzung Chapter 62 Drugs Used in the Treatment of Gastrointestinal Diseases

Gastrin

Binds to gastrin/cholecystokinin receptor on parietal cells and causes the secretion of H+ ions thru the H+/K+ ATPase pump

Histamine

Binds to histamine type 2 receptors on parietal cells and causes the secretion of H+ ions thru the H+/K+ ATPase pump

Acetylcholine

Binds to muscarinic type 3 receptors on parietal cells and causes the secretion of H+ ions thru the H+/K+ ATPase pump

Antacids

Weak bases that react with gastric hydrochloric acid to form a salt and water for the treatment of intermittent heartburn and dyspepsia

Sodium bicarbonate

Antacid that couples with hydrochloric acid to form carbon dioxide and sodium chloride

Calcium carbonate

Antacid that couples with hydrochloric acid to form carbon dioxide and calcium chloride

Magnesium hydroxide

Antacid that couples with hydrochloric acid to form magnesium chloride and water

Aluminum hydroxide

Antacid that couples with hydrochloric acid to form aluminum chloride and water

H2-receptor antagonists

Reduce acid secretion stimulated by histamine, gastrin and acetylcholine by binding to histamine type 2 receptors for the treatment of GERD, peptic ulcer disease and bleeding from stress related gastritis

Cimetidine

H2-receptor antagonists

Ranitidine

H2-receptor antagonists

Famotidine

H2-receptor antagonists

Nizatidine

H2-receptor antagonists

Proton pump inhibitors

Form a covalent disulfide bond with the H+/K+-ATPase, irreversibly inactivating the protein

Omeprazole

Proton pump inhibitors

Esomeprazole

Proton pump inhibitors

Lansoprazole

Proton pump inhibitors

Dexlansoprazole

Proton pump inhibitors

Rabeprazole

Proton pump inhibitors

Pantoprazole

Proton pump inhibitors

Sucralfate

Negatively charged sucrose sulfate binds to positively charged proteins in the base of ulcers or erosion, forms a physical barrier and stimulates mucosal prostaglandin and bicarbonate secretion

Bismuth subsalicylate

Creates a protective layer against acid and pepsin in ulcers and erosions, reduces infectious diarrhea, direct antimicrobial effects and binds enterotoxins

Neostigmine

Acetylcholinesterase inhibitor, enhances gastric, small intestine, and colonic emptying to treat hospitalized patients with acute large bowel distention

Metoclopramide

Dopamine D2-receptor antagonists to treat impaired gastric emptying and an antiemetic

Macrolides

Directly stimulates motilin receptors on GI smooth muscle

Psyllium

Natural plant laxative (bulk forming)

Methylcellulose

Natural plant laxative (bulk forming)

Polycarbophil

Synthetic laxative (bulk forming)

Docusate

Stool softener

Glycerin

Osmotic laxative agent, soluble but nonabsorbable compounds

Mineral oil

Lubricates fecal material and retards water absorption

Magnesium hydroxide

Osmotic laxative agent, soluble but nonabsorbable compounds

Sorbitol

Osmotic laxative agent, soluble but nonabsorbable compounds

Lactulose

Osmotic laxative agent, soluble but nonabsorbable compounds

Magnesium citrate

Osmotic laxative agent, soluble but nonabsorbable compounds

Senna

Stimulant laxatives, direct stimulation of the enteric nervous system causing colonic electrolyte and fluid secretion

Bisacodyl

Stimulant laxatives, direct stimulation of the enteric nervous system causing colonic electrolyte and fluid secretion

Lubiprostone

Chloride channel activator laxative, stimulates the type 2 chloride channel in the small intestine that increases chloride-rich fluid secretion into the intestine and stimulates intestinal motility

Linaclotide

Minimally absorbed, 14-amino acid peptide that stimulates intestinal chloride secretion, approved for chroinc constipation and IBS

Methylnaltrexone bromide

Opioid receptor antagonists laxative

Alvimopan

Opioid receptor antagonists laxative

Loperamide

Opioid agonists, antidiarrheal agents

Diphenoxylate

Opioid agonists, antidiarrheal agents

Cholestyramine

Bile salt binding resins, may decrease diarrhea caused by excess fecal bile acids

Alosetron

Serotonin 5-HT3 receptor antagonists, approved for the treatment of severe IBS with diarrhea predominant in women

Dicyclomine

Antispasmodics (anticholinergics) used to treat IBS

Ondansetron

Serotonin 5-HT3 antagonists, used to treat nausea and vomiting

Granisetron

Serotonin 5-HT3 antagonists, used to treat nausea and vomiting

Dolasetron

Serotonin 5-HT3 antagonists, used to treat nausea and vomiting

Palonosetron

Serotonin 5-HT3 antagonists, used to treat nausea and vomiting

Aprepitant

Neurokinin 1 receptor antagonists (central blockade in the area postrema), prevention of acute and delayed nausea and vomiting from chemotherapeutic regimens

Fosaprepitant

Neurokinin 1 receptor antagonists (central blockade in the area postrema), prevention of acute and delayed nausea and vomiting from chemotherapeutic regimens

Prochlorperazine

Phenothiazines- antipsychotic agent with antiememtic actions

Promethazine

Phenothiazines- antipsychotic agent with antiememtic actions

Trimethobenzamide

Phenothiazines- antipsychotic agent with antiememtic actions

Droperidol

Butyrophenones- antipsychotic with antiemetic actions

Diphenhydramine

H1 Antihistamines, antiemetic

Dimenhydrinate

H1 Antihistamines, antiemetic

Meclizine

H1 Antihistamines, antiemetic

Scopolamine

H1 Antihistamines, antiemetic

Lorazepam

Benzodiazepines, antiemetic before the initiation of chemotherapy to reduce anticipatory vomiting or vomiting caused by anxiety

Dronabinol

Δ9-tetrahydrocannabinol-THC, antiemetic

Sulfasalazine

Aminosalicylates used to treat mild to moderate Crohn disease and ulcerative colitis

Mesalamine

Aminosalicylates used to treat mild to moderate Crohn disease and ulcerative colitis

Olsalazine

Aminosalicylates used to treat mild to moderate ulcerative colitis for patients intolerant of sulfasalazine

Balsalazide

Aminosalicylates used to treat mild to moderate ulcerative colitis

Prednisone

Corticosteroid used to treat acute episodes of Crohn disease or ulcerative colitis

Prednisolone

Corticosteroid used to treat acute episodes of Crohn disease or ulcerative colitis

Hydrocortisone

Corticosteroid used to treat acute episodes of ulcerative colitis

Budesonide

Corticosteroid used to treat acute episodes of mild to moderate Crohn disease or ulcerative colitis

Methylprednisolone

Corticosteroid used to treat acute episodes of Crohn disease or ulcerative colitis

Azathioprine

Purine anti-metabolites with immunosuppressive properties used for remission maintenance or steroid reduction in Crohn disease and ulcerative colitis

6-mercaptopurine

Purine anti-metabolites with immunosuppressive properties used for remission maintenance or steroid reduction in Crohn disease and ulcerative colitis

Infliximab

Monoclonal antibodies to human TNF used to treat inflammatory bowel disease

Adalimumab

Monoclonal antibodies to human TNF used to treat inflammatory bowel disease

Certolizumab

Monoclonal antibodies to human TNF used to treat inflammatory bowel disease

Golimumab

Monoclonal antibodies to human TNF used to treat inflammatory bowel disease

Natalizumab

Monoclonal antibodies to human integrin used to treat inflammatory bowel disease

Pancrelipse

Pancreatic enzyme supplements from procine containg amylase, lipases and proteases

Ursodiol

Reduces the secretion of cholesterol from the liver and reabsorption in the intestines used to treat gallstones

Tegaserod

Serotonin 5HT4 receptor partial agonist used to treat IBS with constipation predominant