Pharmacology - GI Drugs I & II - Patsy Iannolo Flashcards
Class: Calcium carbonate (Rolaids, Tums)
Antacid
Class: Sodium bicarbonate
Antacid
Rarely used due to causing systemic alkalosis
Class: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)
Antacid
Class: Aluminum hydroxide (Alternagel)
Antacid
Use: Calcium carbonate (Rolaids, Tums)
Ulcer tx, GERD
Use: Sodium bicarbonate
Ulcer tx, GERD
Rarely used due to causing systemic alkalosis
Use: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)
Ulcer tx, GERD
Use: Aluminum hydroxide (Alternagel)
Ulcer tx, GERD
Side Effects: Calcium carbonate (Rolaids, Tums)
Milk-alkali syndrome, nephrocalcinosis,
“rebound” acidity,
digitalis antagonism,
constipation
Side Effects: Sodium bicarbonate
Systemic alkalosis;
Enhanced effects of amphetamine, quinidine, and cinchophen
Rarely used due to causing systemic alkalosis
Side effects: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)
Diarrhea;
Hypokalemia,
hypermagnesemia,
iron deficiency
Magnesium toxicity mostly in presence of renal disease; liquid-based, so act fast
Side effects: Aluminum hydroxide (Alternagel)
Phosphate depletion and sequelae (weakness, anemia, tetany, apnea);
Constipation
What antacid is safe for use in patients with renal failure?
Aluminum hydroxide
also eliminates phosphate
What antacid should not be used in patients that have renal failure?
Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)
Class: Cimetidine
Histamine (H2) receptor blocker
Class: Famotidine
Histamine (H2) receptor blocker
Class: Ranitidine
Histamine (H2) receptor blocker
Class: Nizatidine
Histamine (H2) receptor blocker
MOA: Histamine (H2) receptor blockers - Cimiidine, Ranitidine, Famotidine, Nizatidine
Inhibits 50-80% of 24 hour acid production
Use: Histamine (H2) receptor blockers - Cimiidine, Ranitidine, Famotidine, Nizatidine
Ulcer treatment (satisfy all 4 requirements); prophylactically for stress ulcers; GERD
Side Effects: Ulcer treatment (satisfy all 4 requirements); prophylactically for stress ulcers; GERD
Rebound acidity if stopped;
Uncommon; headache, lethargy, confusion, depression, and hallucination
Class: Omeprazole
H/K/ATPase inhibitor
Class: Lansoprazole
H/K/ATPase inhibitor
Class: Rabeprazole
H/K/ATPase inhibitor
Class: Pantoprazole
H/K/ATPase inhibitor
Class: Esomeprazole
H/K/ATPase inhibitor
MOA: H/K/ATPase inhibitors:
Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole
Inhibit >90% of 24 hour acid secretion (better than H2 antagonists);
requires acid environment to activate, selectively diffuse to acidic environments (don’t take with antacids)
**noncompetitive inhibitors
Uses: Omeprazole and Lansorazole
Ulcer treatment,
treatment for H. pylori;
GERD
Uses: Rabeprazole, Pantoprazole, Esomeprazole
Ulcer treatment; GERD
Side Effects: H/K/ATPase inhibitors:
Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole
Headache, gynecomastia, gastric hyperplasia in humans and carcinoid tumors in rats long term (do not use long-term)
What is Dexlansoprazole?
A rapid-formulation of slow release Lansoprazole
What is the only H/K ATPase inhibitor available for IV administration?
Pantoprazole
T/F: H/K ATPase inhibitors will heal H2 antagonist refractory ulcers.
True
Also, better pain relief and faster healing rates than with H2 antagonists.
What H/K ATPase inhibitor has no P450 interaction?
Pantoprazole
What is the only drug that is FDA approved for the prevention of NSAID-induced gastric ulcers?
Misoprostol
H2 antagonists and sucralfate are ineffective if NSAID
therapy is being continued.
Class: Misoprostol
Prostaglandin E analog
MOA: Misoprostol
Decrease acid production, increase mucous and bicarbonate secretion
Use: Misoprostol
Ulcer treatment when prostaglandin production decreased (RA patients taking lots of NSAIDs)
What antacid should not be used in pregnancy?
Misoprostol
Side effects: Misoprostol
Transient diarrhea
What is the therapy for H. Pylori infection?
Quadruple therapy:
A PPI twice a day
Tetracycline HCl 500 mg 4 times a day
Bismuth subsalicylate or subcitrate 4 times a day Metronidazole 500 mg 3 times a day
Class: Atropine sulfate
Anticholinergics
Class: Probantheline;
Metantheline bromide
Anticholinergics
MOA: Anticholinergics -
Atropine sulfate;
Probantheline;
Metantheline bromide
Reduce acid secretion;
reduce spasm
Use: Atropine sulfate
Ulcer treatment
Side effects: Anticholinergics -
Atropine sulfate;
Probantheline;
Metantheline bromide
Anticholinergic effects
What are the contraindications for Probantheline;
Metantheline bromide
Known pyloric obstruction, hiatal hernia, or peptic esophagitis (not used much)
What are the contraindications for Atropine sulfate?
Aspirin;
Belladonna;
known pyloric obstruction, hiatal hernia, or peptic esophagitis (not used much)
Use: Probantheline;
Metantheline bromide
Ulcer treatment (taken 15-30 minutes before meals, and before bed)
Class: Sucralfate (Carafate)
Mechanical protector
Class: Bismuth salts
Mechanical protector
MOA: Sucralfate
Coat the ulcer crater, increase mucosal resistance (requires acid environment)
MOA: Bismuth salts
Coat the ulcer crater, increase mucosal resistance
Side effects: Sucralfate
Aluminum toxicity possible in renal failure
Use: Sucralfate, Bismuth salts
Ulcer treatment, treatment for H. pylori
Side effects: Bismuth salts
Aluminum toxicity possible in renal failure; turns bowel movements (and sometimes tongues) black
Class: Ondansetron
Serotonin (5HT3) receptor antagonists
Class: Granesitron
Serotonin (5HT3) receptor antagonists
Class: Dolasetron
Serotonin (5HT3) receptor antagonists
Class: Promethazine
Phenothiazines (neuroleptic class)
Class: Prochlorperazine
Phenothiazines (neuroleptic class)
MOA: Prochlorperazine
Probable CNS interaction with dopaminergic receptor-antagonist (leading to reduction of stimulation in the CRTZ in the medulla)
Use:
Prochlorperazine;
Promethazine
Anti-emetic
MOA: Promethazine
Antihistamine (H1 receptor);
anticholinergic
Side effects: Prochlorperazine
Largely extra-pyramidal (torticollis!)
Side effects: Promethazine
Somnolence (esp in elderly)
MOA:
Ondansetron;
Granesitron;
Dolasetron
Blocks serotonin at 5HT3 receptor (in central CRTZ)
Use:
Ondansetron;
Anti-emetic
Use:
Granesitron;
Dolasetron
Post-op anti-emetic
Class: Metochlopramide
Promotility agent (dopamine antagonist)
MOA: Metochlopramide
Increase motor tone in lower esophageal sphincter (prevent reflux) and stomch (esp. antrum: improves gastric emptying); peripheral (stomach) and CNS (vomiting, via CRTZ) dopamine antagonist
Use: Metochlopramide
GERD, anti-emetic, gastroparesis
Side effects: Metochlopramide
Hand tremor if used 4X/day (optimum use); possible extra-pyramidal symptoms, but not so severe
Class: Domperidone
Promotility agent
MOA: Domperidone
Improves gastric tone
Use: Domperidone
Gastroparesis
An important complication of Cisparide is:
possibility of sudden cardiac death
Class: Cisparide
Promotility agent (dopamine agonist)
MOA: Cisparide
Increase motor tone in lower esophageal sphincter and stomach
Use: Cisparide
GERD, gastroparesis
Class: Lubiprostone
…
Class: Linaclotide
…
Class: Naloxegol
Mu receptor antagonist
MOA: Lubiprostone
acts on chloride channel
MOA: Linaclotide
cGMP
Use: Lubiprostone
Anti-constipation
MOA: Naloxegol
…
Use: Naloxegol
Anti-constipation;
effective in opioid addicted population
Class: Sulfasalazine
Anti-inflammatory
Class: Olsalazine
Anti-inflammatory
Class: Mesalamine
Anti-inflammatory
Class: Prednisone
Corticosteroid
Class: Azathioprine
Immunosuppressive
Class: Cyclosporine
Immunosuppressive
Class: Infliximab
MAb Immunisuppressive
MOA: Sulfasalazine
Work from lumen to reduce inflammation
MOA: Olsalazine
Work from lumen to reduce inflammation; 5-ASA dimer
Broken down into bowel by bacteria into 2 moleules of 5-ASA
MOA: Mesalamine
Work from lumen to reduce inflammation
Delayed release 5-ASA, for terminal ileum, colon
MOA: Azathioprine
Purine antimetabolite; interferes with DNA synthesis
MOA: Cyclosporine
Suppresses T helper and T suppressor lymphocytes
MOA: Infliximab
Binds and neutralized TNFa
Use:
Sulfasalazine;
Olsalazine;
Mesalamine
Acute IBD (UC)
Use: Prednisone
Acute and chronic IBD
Can be given systemically or as enemas
Use:
Azathioprine;
Cyclosporine;
Infliximab
Chronic IBD
Side Effects: Sulfasalazine
Toxicity coming from systemic absorption of sulfapyridine
T/F: Olsalazine has less toxicity that Sulfasalazine
True