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JGR-GI
| Question | Answer |
|---|---|
| What ingredient of antacids causes constipation? Diarrhea? | Aluminum Hydroxide – May cause constipation (Amphojel®) Magnesium hydroxide – May produce diarrhea (Milk of Magnesia) –used as antacid or laxative |
| What antacid has less acid neutralizing capability compared to the other agents ? | Calcium Carbonate (Tums®) |
| Why should you avoid long term and excessive use of Sodium Bicarbonate? | Systemic alkalosis |
| What are the two major combination antacid products? | Magnesium Hydroxide, Aluminum Hydroxide and Simethicone (Maalox suspension and Mylanta liquid) Aluminum Hydroxide and Magnesium Trisilicate (Gaviscon® tablets & liquid) |
| What is the advantage to the combination product Maalox®? | The ingredients together normalize bowel function Simethicone relieves flatulence with defoaming action (gas bubbles combine and are more easily freed |
| What other ingredient is in Gaviscon®? | Alginic acid that creates a foamy layer above the stomach contents (reduces reflux) |
| What are two considerations when administering antacids? | DDI Sodium intake of patients with HTN and CHF |
| What is the MOA of H2 Blockers (Antisecretory Drugs)? | H2 Blockers – Competitively block the binding of histamine to H2 receptors whereby inhibiting gastric acid secretion induced by histamine. |
| What are the indications of H2 Blockers? | Peptic ulcers, Zollinger-Ellison syndrome, Acute stress ulcers, Gastroesophageal reflux disease (GERD) |
| List the four H2 Blockers | Cimetidine (Tagamet®) Ranitidine (Zantac®) Famotidine (Pepcid®) Nizatidine (Axid®) |
| Which H2 Blocker has the greatest efficacy? | None-they are all equal Selection is based on side effect profile and cost |
| What are the advantages of Cimetidine (Tagamet®) ? | Advantages -used to be much lower cost than the others, but now all of the others are also available as generics |
| What are the disadvantages of Cimetidine (Tagamet®)? | Disadvantages (outweigh the advantages) Drug/Drug Interactions – Inhibits cytochrome P-450 system TID and QID dosing compared to BID dosing for the others Endocrine side effects –anti-androgen causing gynecomastia , galactorrhea, and low sperm count |
| What is the H2 Blocker of choice for military facilities? Why? | Ranitidine (Zantac®) Low cost, few side effects, and good efficacy. |
| What are the advantages of Ranitidine (Zantac®) ? | Available as a generic, does not cause endocrine side effects Does not inhibit the cytochrome P450 system Requires BID dosing for most indications H2 blockers continued |
| What are the advantages of Famotidine (Pepcid®)? | It is also sold as a combination product OTC “Pepcid Complete®” it is an OTC item combining an H2 antagonist with an antacid It is to sell the combined benefits of antacids (fast acting) and the longer acting H2 blockers. |
| What is the advantage of Nizatidine (Axid®) ? | No advantage over Famotidine (Pepsid®) and Ranitidine (Zantac®) But much more expensive |
| What is the MOA of Proton Pump Inhibitors (Anti-secretory)? | MOA – Binds to the H+/K+ ATPase enzyme system (proton pump) of the cells suppressing secretion of hydrogen ions (Acid) |
| What are the indication for Proton Pump Inhibitors? | Indications – PUD, erosive esophagitis, Zollinger-Ellison syndrome, GERD, stress ulcer prophylaxis |
| What anti-secretory drugs are most effective, PPIs or H2 Blockers? | PPI are more effective than H2 blockers |
| What are the Adverse Reactions of Proton Pump Inhibitors? | Some GI discomfort nausea and diarrhea and headache/dizziness |
| What are the Drug/Drug interactions of PPIs? | Slight P450 inhibition |
| List the Proton Pump Inhibitors | Omeprazole (Prilosec®) -BCF Rabeprazole (Aciphex®) Lansoprazole (Prevacid®) Pantoprazole (Protonix®) Esomeprazole (Nexium®) –BCF |
| What PPIs are available OTC? | Omeprazole (Prilosec®) – BCF – Different salt (omeprazole magnesium) is now OTC for “intermittent heartburn” |
| What form does Omeprazole (Prilosec®) come in? | capsules and powder for oral suspension |
| What form does Lansoprazole (Prevacid®) come in? | Available as capsules, orally disintegrating tablet, granules for oral suspension and as an IV agent |
| What form does Pantoprazole (Protonix®) come in? | Available as tablets and as an IV agent |
| What is unique about Esomeprazole (Nexium®) - BCF? | S-isomer of omeprazole. No significant clinical difference compared to omeprazole. Available in capsules and IV form |
| What is the MOA of Antimuscarinic agents? | Decrease gastrointestinal motility (antispasmodic) and inhibit gastric acid secretion |
| What are the indications for antimuscarinic agents? | Peptic ulcer, irritable bowel and ulcerative colitis |
| What are the adverse reactions of antimuscarinic agents? | Anticholinergic side effects (Dry mouth, Urinary retention, mydriasis ) Cautions/Warnings – glaucoma, GI obstructive disease, and heat prostration in high temps |
| List the antimuscarinic agents | Hyoscyamine (Levsin®) |
| What is Hyoscyamine (Levsin®)’s place in therapy? | Rarely used and then as an adjunct agent to H2 blockers or PPIs |
| What are the Mucosal Protective Agents? | Misoprostol (Cytotec®) Sucralfate (Carafate®) |
| What is the MOA of Misoprostol (Cytotec®)? | Synthetic, oral prostaglandin E1 analog that has both antisecretory and mucosal protective properties |
| What are the indications for Misoprostol (Cytotec®)? | Very limited - Prevention of NSAID induced gastric ulcers Unlabeled Use – Cervical ripening ¼ of 100mg tablet placed vaginally |
| What are the adverse reactions of Misoprostol (Cytotec®) | Diarrhea 13-40% abdominal pain 7-20% Category X – May cause miscarriage |
| What is the MOA of Sucralfate (Carafate®)? | Covers the ulcer site and protects it against acid |
| What are the Adverse effects of Sucralfate (Carafate®)? | Not absorbed systemically, adverse effects are uncommon Take before meals and at bedtime – requires acidic pH for activation (Do not administer with agents that increase gastric pH) |
| What are the Prokinetic Agents? | Metoclopramide (Reglan®) Cisapride (Propulsid®) and Erythromycin |
| What is the MOA of Metoclopramide (Reglan®)? | Stimulates motility of the upper GI track without effecting secretions |
| What are the indications for Metoclopramide (Reglan®) ? | Gastroesophageal reflux, N/V from chemotherapy, diabetic gastroparesis |
| What are the Side effects of Metoclopramide (Reglan®)? | CNS effects drowsiness but may also cause restlessness drug induced Parkinsonism and tardive dyskinesis (It blocks dopamine receptors which is the reason behind its antiemetic effect and this side effect.) |
| What are the major causes of GERD? | Defective lower esophageal sphincter (LES) Delayed gastric emptying Irritant effects of refluxate |
| What are the steps of treatment for Gastroesophageal Reflux Disease (GERD)? | Phase I – lifestyles changes, OTC antacids and H2 antagonists Phase II – std/high dose anti-secretory Rx Phase III – surgical intervention Step-up/step-down Prokinetic agents |
| What are the treatment options for Gastroesophageal Reflux Disease (GERD)? | Antacids – effective but short duration H2 antagonists – OTC and prescription PPI – 83% improvement |
| 3 major causes of Peptic Ulcer Disease (PUD)? | Helicobacter pylori-most common NSAID Ingestion Unopposed hypergastrinemia Minor contributor to PUD: Inadequate mucosal defense against gastric acid |
| What are two treatment options for H. Pylori? | Clarithromycin +Amoxicillin + a PPI Bismuth subsalicylate + tetracycline + metronidazole + PPI Continue PPI or H2 antagonist therapy for 4-8 weeks after eradication therapy |
| Is there an empiric therapy for H. Pylori? | No, don’t treat without proof of infection |
| How long should treatment for H. Pylori last? | 10-14 days |
| How long should you continue PPI or anti-secretory drug after eradication of H. Pylori? | 4 weeks for duodenal 8 weeks for gastric |
| What are the four sources of stimulation of the medullary vomiting center? | 5-HT3 receptors Fibers of the vestibular system (histamine H1 and muscarinic cholinergic receptors) higher CNS centers Chemoreceptor trigger zone |
| Where are the 5-HT3 receptors located? | In afferent vagal and splanchnic fibers |
| What stimulates the 5-HT3 receptors? | Stimulated by biliary or GI distention, mucosal or peritoneal irritation and infection |
| How is the chemoreceptor trigger zone activated? | Zone is rich in opioid, Serotonin 5-HT3 and Dopamine D2 receptors Located outside the BBB – activated by drugs, toxins, hypoxia, acidosis |
| What causes acute vomiting? | Food poisoning, infectious gastroenteritis, drugs or systemic illness |
| What causes persistent vomiting? | Gastroparesis Gastric outlet obstruction Bulimia Psychogenic causes Pregnancy Uremia Alcohol Intake Increased Intracranial Pressure |
| List the Antiemetic drugs – 5HT3 antagonists | Ondansetron (Zofran®) Granisetron (Kytril®) Dolasetron (Anzemet®) |
| What is the Place in therapy for 5HT3 antagonists? | Antiemetic for cancer therapy N/V following surgery |
| What is used in conjunction with 5HT3 Seratonin Blockers? | Corticosteroids |
| What is the place in therapy for combination drug (5HT3 + corticosteroid)? | Used in chemotherapy-induced emesis with serotonin blockers (usually dexamethasone) |
| List the anti-emetic dopamine antagonists | Phenothiazines: Prochlorperazine (Compazine®) Promethazine (Phenergan®) Metoclopramide (Reglan®) |
| Which dopamine antagonist anti-emetic is indicated for motion sickness? | Promethazine (Phenergan®) |
| What is the MOA of dopamine antagonist anti-emetics? | Blocks dopamine receptors in CTZ (chemoreceptor trigger zone) of the CNS |
| What are the side effects of dopamine antagonist antiemetics? | hypotension, restlessness, extrapyramidal side effects (i.e. involuntary movements) and drowsiness |
| What are the antihistamines/anticholinergics indicated for nausea and vomiting due to motion sickness/vertigo? | Meclizine (Antivert®) Dimenhydrinate (Dramamine®) Diphenhydramine (Benadryl®) Trimethobenzamide (Tigan®) |
| What side effects do antihistamines/anticholinergics cause? | Drowsiness and anticholinergic side effects (actually beneficial for this indication) |
| What drug works in a similar fashion as antihistamines to prevent vomiting? | Scopolamine transdermal (Transderm-Scop®) |
| What is the oral med prescribed in conjunction with 5-HT3 and steroid for both the acute and delayed phases of cisplatin-induced emesis ? | Human substance P/neurokinin 1 (NK1) receptor antagonist - Aprepitant (Emend®) |
| What is prescribed to stop nausea and vomiting following chemotherapy when other drugs fail? | Cannabinoids: Dronabinol (Marinol®) |
| What drugs are given for anticipatory N/V ? | Benzodiazepines: Lorazepam (Ativan®) or alprazolam (Xanax®) |
| What is the empiric antibiotic therapy for diarrhea without blood/fever? All others? | Azithromycin or Rifamixin Flourquinolones |
| What two antibiotics cause diarrhea? | Metronidazole and vancomycin |
| What is the advantage to taking Loperamide (Imodium®) for diarrhea? | Does not cross the BBB and is considered less sedating and addicting than diphenoxylate |
| Which drugs should not be used as first line in acute diarrhea? | Loperamide (Imodium®) Diphenoxylate + atropine (Lomotil®) – C-IV |
| What drug is a Meperidine spin off, and will cause opioid activity at high doses so atropine is included to discourage abuse? | Diphenoxylate |
| What are the other antidiarrheal agents? | Absorbants: Kaolin Adsorb toxins and protect mucosa Bismuth subsalicylate – (Pepto-Bismol®)-antacid, anti-inflammatory and antibacterial |
| What are the treatment options for constipation? | Bulking Agents (Fiber Laxatives) Stool softeners Osmotic saline laxatives Irritants and stimulants Bowel evacuants Enemas |
| List the bulking agents | Psyllium (Metamucil®) Calcium polycarbophil (FiberCon®) Methylcellulose (Citrucel®) Bran powder |
| What treatment for constipation is most natural and safest? | Bulking agents |
| List the stool softeners | Docusate sodium (Colace®) Docusate calcium (Surfak®) Mineral Oil |
| List the osmotic saline laxative agents | Magnesium hydroxide (MOM) Magnesium sulfate (Epsom salts) Lactulose or 70% sorbitol PEG 3350 powder (Miralax®) – Unlike other polyethylene products this one is for chronic use |
| Who should not take Magnesium sulfate (Epsom salts)? | Patients with renal insufficiency |
| What is the MOA for osmotic/saline laxatives? | Holds water in intestine by osmosis |
| What is the MOA for stool softeners? | Draws water (and some fats) into stool to soften it |
| What are the adverse reaction of mineral oil? | Lipoid pneumonia if aspirated Can lower absorption of fat soluble vitamins |
| What is the MOA of mineral oil? | Slows the absorption of water from the stool by the colon (softens stool) and oil also acts as an intestinal lubricant |
| What are the indications for osmotic/saline laxatives? | May be used to soften stools. Used in older patients to prevent constipation and fecal impaction |
| List the stimulants? | Bisacodyl (Dulcolax®) Suppositories work in ~1 hour (15-60 minutes) Senna (Senokot®, ExLax®) Cascara (Nature’s Remedy®) Castor Oil |
| What is the MOA of bowel stimulants? | Stimulate secretion and motility of the bowel |
| List the bowel evacuants | • Polyethylene glycol (PEG) solutions CoLyte®, GoLYTELY® • Sodium phosphate – (Fleets®) Oral agent used in conjunction with bisacodyl suppository. • Magnesium citrate |
| List the enema drug. What is it indicated for? | Sodium Phosphate enema (Fleets®) For acute constipation and for prior to medical procedure |
| What is the quickest acting treatment for constipation? | Bisacodyl (Dulcolax®) suppositories |
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