GI Pharmacology Flashcards
What are the different GI disorders?
Gastroesophageal Reflux Disease (GERD)
Peptic Ulcer Disease (PUD)
Duodenal Ulcer
Nausea
Emesis
IBS
Diarrhea
Constipation
Gastric Mucosal Barrier
- The alkaline-rich mucus produced by mucosa cells in the pyloric region that protects the epithelium of the stomach and duodenum from harsh acid conditions of the lumen
- These cells are stimulated by mechanical and chemical irritation and parasympathetic inputs.
- This protective mucus barrier can be damaged by bacterial and viral infection, certain drugs, and aspirin
GERD
- Backflow of stomach acid into the esophagus, which can cause scarring
- Usual symptom of heartburn (burning sensation behind the breastbone; MI is often mistaken for GERD)
- severe symptoms=difficulty swallowing and chest pain
- complications include esophageal erosions, esophageal ulcer and esophageal stricture (narrowing)
- ~10% pts, normal esophageal lining is replaced with Barrett’s epithelium (aka Barrett’s esophagus) and has been linked to cancer
- Precipitants include: fatty food, alcohol, caffiene, smoking, obesity, and pregnancy
—this is usually a chronic/relapsing course
Peptic Ulcer Disease
- Can be benign or malignant
- Benign: normal gastric acid production, but the mucosal barrier is weak
- Malignant: Excessive secretion of gastric acid that overwhelms the mucosal barrier
Treatments for GERD and PUD
- Antacids
- H2 Receptor Blockers
- Mucosal Protective Agents
- Proton Pump Inhibitors
- Anti-cholinergics
- Prostaglandin Analogs
- Anti-microbial Agents
Antacids
Systemic antacid: Sodium bicarbonate
Nonsystemic antacids: Aluminum Hydroxide+Mg Hydroxide (Maalox and Mylanta)
- Maalox and Mylanta are contraindicated in pts with impaired renal function and Mg may cause diarrhea
- Calcium carbonate (Tums): Ca may cause constipation
H2 Receptor Blockers
- Cimetidine
- Famotidine
- Ranitidine
- Nizatidine
- Inhibit secretion of gastric acid through competitive inhibition of Histamine H2 receptors
- Prevention and Tx of PUD, Esophagitis, GI bleeding, stress ulcers, and Zollinger-Ellison Syndrome
- May alter the effects of other drugs through interactions with CYP450 (especially cimetidine)
- Very few side effects (except for cimetidine which inhibits metabolism of estrogen which can cause breast tissue growth in men when taken long term)
- Suppresses 24 hour gastric secretion by 70%
Proton Pump Inhibitors (PPIs)
- Omeprazole
- Esomeprazole
- Rebeprazole
- Lansoprazole
- Pantoprazole
- Strong inhibitors of gastric acid secretion through irreversible inhibition of proton pump
- Prevents release or pumping of gastric acid (24 hr action)
- Indicated in PUD, Gastritis, GERD, & Zollinger-Ellison syndrome
- Faster relief and healing than H2 receptor blockers
- Decreases acid secretion by up to 95% for up to 48 hours -4-8 week course of treatment
Mucosal protecting agents
Sucralfate (carafate)
- -used to prevent and Tx PUD
- -requires an acidic pH to activate
- -forms a sticky polymer in the acidic environment & adheres to the ulcer site forming a barrier
Chelated Bismuth
- -protects the ulcer crater and allows healing -some activity against H. pylori
- -should not be used repeatedly or for more than 2 months at a time
- -can cause black stools and constipation
Anti-H. pylori therapy
>85% PUD caused by H. pylori Antibiotic Ulcer Therapy: Used in Combinations
- Bismuth: Disrupts bacterial cell wall
- Clarithromycin: Inhibits protein synthesis
- Amoxicillin: Disrupts cell wall
- Tetracycline: Inhibits protein synthesis
- Metronidazone: Used often due to bacterial resistance to amoxicillin and tetracycline, or due to intolerance
Anti-H. pylori therapy
Triple Therapy is a 7 day treatment 80-85% effective
-Proton pump inhibitor + amoxicillin/tetracycline + metronidazone/clarithomycin
Quadruple Therapy is a 3 day treatment and as efficacious as triple therapy
-Add Bismuth to triple therapy
Prostaglandins
Misoprostol
- PGE1 analog
- Stimulates GI pathway leading to a decrease in gastric acid release
- For treatment of NSAID induced injury
- Side effects include diarrhea, pain, and cramps (30%)
**Do not give to women of childbearing years unless a reliable method of birth control can be DOCUMENTED
**Can cause birth defects, and premature birth
Anticholinergics
Pirenzipine
- Muscarinic M1 Ach receptor antagonist
- Blocks gastric acid secretions
- About as effective as H2 blockers
- Rarely used, primarily as adjunct therapy
- Anticholinergic side effects (anorexia, blurry vision, constipation, dry mouth, sedation)
Inflammatory Bowel Disease
Ulcerative Colitis
- A diffuse mucosal inflammation limited to the colon
- Bloody diarrhea, colicky pain, urgency, tenesmus (feel like you have to use the bathroom even though bowels are empty) Crohn’s Disease
- Patchy transmural inflammation
- May affect any part of the GI tract
- Causes abdominal pain, diarrhea, weight loss, intestinal obstruction
Treatment for Inflammatory Bowel Disease
Goal of treatment is to resolve the acute episodes and prolong remission
- Aminosalicylates - for mild symptoms
- Corticosteroids - for moderate symptoms
- Thiopurines - for active and chronic symptoms
- Methotrexate - for active and chronic symptoms
- Cyclosporin - for active and chronic symptoms refractory to corticorsteroids- (significant side effects)
- Infliximab - antibody infusion