GI Drugs Flashcards
Aluminum Hydroxide and Magnesium Hydroxide: ROA (1) MOA (1) A&E (1) Use (1) AE (2) Contraindications (2) PLR
Oral (suspension, liquid)
React with gastric HCl to form salt and water (Al(OH)3 slow, Mg(OH)2 fast, usually
administered together)
Reduce intragastric acidity
Nonprescription remedy for treatment of intermittent heartburn and dyspepsia
Al salts cause diarrhea; Mg salts cause constipation
Precautions with other oral drugs; should not be taken within two hours of doses of tetracyclines, fluoroquinolones,
itraconazole, and Fe compounds
C/precaution (safety unknown)
Calcium Carbonate: ROA (1) MOA (1) A&E (1) Use (4) AE (1) Contraindications (3) PLR
Oral (suspension, tablet, chewable)
React with gastric HCl to form salt and water
Reduce intragastric acidity
Nonprescription remedy for treatment of intermittent heartburn and dyspepsia, hypocalcemia, osteoporosis, hyperphosphatemia
Milk-alkali syndrome (alkalosis, hypercalcemia, renal insufficiency)
Precautions with other oral drugs; should not be taken within two hours of doses of tetracyclines, fluoroquinolones,
itraconazole, and Fe compounds; hypophosphatemia, nephrolithiasis, hypercalcemia, hypercalciuria, digoxin toxicity
PLR–C/safe
Sodium Bicarbonate, Aspirin and Citric Acid: ROA (1) MOA (2) A&E (2) Use (1) Contraindications (3) PLR
Oral (effervescent tablet)
React with gastric HCl to form salt and water, aspirin irreversibly inhibits COX-1 and -2
Reduce intragastric acidity, analgesic
Nonprescription remedy for treatment of intermittent heartburn and dyspepsia
Precautions with other oral drugs; should not be taken within two hours of doses of tetracyclines, fluoroquinolones,
itraconazole, and Fe compounds; hypochloremia, respiratory alkalosis, hypocalcemia
C/precaution (safety unknown)
Cimetidine ROA (4) MOA (2) A&E (3) Use (4 oral, 2 IM/IV/IO) AE (6) PLR
Oral (solution, tablet), IV, IM, IO
Competitive inhibitors of H2-receptors on gut parietal cells (GPCRs that stimulate
production of cAMP upon histamine binding); inhibits several enzymes of Cyt-P450 cascade (binding of dihydrotestosterone)
Suppresses basal and meal-stimulated gastric acid secretion; reduces volume of gastric secretion and pepsin and reduces histamine-stimulated (nocturnal); gastrin- and cholinomimetic agent-mediated gastric acid secretion
Oral use – PUD, erosive GERD, heartburn, pathological hypersecretory conditions
IV, IM, IO use – upper GI bleeding, duodenal ulcer
IV infusions may cause bradycardia, hypotension, gynecomastia, galactorrhea, loss of libido, impotence
PLR – B/not recommended
Famotidine ROA (2) MOA (2) A&E (3) Use (3 oral, 3 IV) AE (6) PLR
Oral (suspension, tablets, chewable, disintegrating), IV
Competitive inhibitors of H2-receptors on gut parietal cells (GPCRs that stimulate
production of cAMP upon histamine binding)
Suppresses basal and meal-stimulated gastric acid secretion; reduces volume of gastric secretion and pepsin; reduces histamine-stimulated (nocturnal), gastrin- and cholinomimetic agent-mediated gastric acid secretion
Oral – GERD, PUD, hypersecretory conditions
IV – acute treatment of duodenal ulcer, hypersecretory conditions, gastric ulcer
IV infusions may cause bradycardia, hypotension, headache, constipation, diarrhea,
dizziness, decreased libido, hepatitis, arrhythmia, toxic epidermal necrolysis
B/not recommended
Rantidine: ROA (3) MOA (1) A&E (3) Use (5) AE (8) Contraindication (1) PLR
Oral (syrup, tablet, capsule, effervescent tablet), IM, IV
Competitive inhibitors of H2-receptors on gut parietal cells (GPCRs that stimulate
production of cAMP upon histamine binding)
Suppresses basal and meal-stimulated gastric acid secretion; reduces volume of gastric secretion and pepsin; reduces histamine-stimulated (nocturnal) gastrin- and cholinomimetic agent-mediated gastric acid secretion
GERD, PUD, erosive esophagitis, hypersecretory conditions, prevention of Mendelson’s syndrome
IV infusions may cause bradycardia, hypotension, headache, alopecia, anemia,
necrotizing enterocolitis, pancreatitis, thrombocytopenia
Breastfeeding women
B/not recommended
Esomeprazole: ROA (2) MOA (1) A&E (2) Use (8 oral, 1 IV) AE (4) Contraindication (1) PLR
Oral (capsule, suspension), IV
Irreversible, suicide inhibition of H+/K+ ATPase
Inhibits fast-acting and meal-stimulated gastric secretion, increases serum gastrin levels
1.2- to 2-fold
Oral use – GERD, PUD, NSAID-associated ulcers, rebleeding of peptic ulcers, nonulcer dyspepsia, prophylaxis for stress-related mucosal bleeding, gastrinoma and other hypersecretory conditions
IV use – GERD (if patient is unable to swallow)
Hospital-acquired pneumonia, clostridum difficile-associated diarrhea, fractures,
inflammation hyperplasia of ECL cells
Hepatic disease substantially reduces clearance
C/not recommended
Omeprazole: ROA (1) MOA (1) A&E (2) Use (8 oral, 1 IV) AE (4) Contraindication (1) PLR
Oral (packet, suspension, tablet, capsule, capsule with NaHCO3, chewable with Mg(OH)2 or NaHCO3, suspension with NaHCO3)
Irreversible, suicide inhibition of H+/K+ ATPase
Inhibits fast-acting and meal-stimulated gastric secretion, increases serum gastrin levels
1.2- to 2-fold
Oral use – GERD, PUD, NSAID-associated ulcers, rebleeding of peptic ulcers, nonulcer dyspepsia, prophylaxis for stress-related mucosal bleeding, gastrinoma and other hypersecretory conditions
IV use – GERD (if patient is unable to swallow)
Hospital-acquired pneumonia, clostridum difficile-associated diarrhea, fractures,
inflammation hyperplasia of ECL cells
Hepatic disease substantially reduces clearance
C/not recommended
Sucralfate: ROA (1) MOA (1) A&E (1) Use (2ish) PLR
Oral (tablet, suspension)
Forms viscous, tenacious paste in water that binds selectively to ulcers or erosions
Forms physical barrier over ulcer
Reduces incidence of clinically-significant upper GI bleeding, prevention of stress-related
bleeding, PUD, stress ulcer epidermolysis bullosa, oral complications of chemotherapy in bone marrow transplant
B/precaution (safety unknown)
Misoprostol: ROA (3) MOA (1) A&E (4) Use (5 oral, 1 vaginal, 1 rectal) AE (BBW) Contraindications (3) PLR
Oral (tablet), vaginal, rectal
Agonist of several prostaglandin receptors
Stimulates mucus, electrolyte, bicarbonate and fluid secretion in GI system; enhances mucus flow; reduces histamine-stimulated cAMP productions and gastric acid secretion; stimulates intestinal motility and uterine contractions
Oral use – NSAID-induced ulcers, PUD, early abortion, intrauterine fetal death, fat absorption in CF patients
Vaginal use – induction of labor
Rectal use – postpartum hemorrhage
Black Box Warning – Misoprostol administration to women who are pregnant can cause abortion, premature birth or birth defects
Women of childbearing age; oral and written warning (strong precaution); negative serum pregnancy test, compliant with effective contraceptive measures, given informed consent, at beginning of menstrual period
X/strong precaution (safety unknown)
Bismuth Subsalicylate: ROA (1) MOA (1) A&E (4) Use (8) AE (7) Contraindications (8) PLR (2)
Oral (chewable, caplet, suspension)
Unclear, coats ulcers and erosions, creates protective layer
Antisecretory effects, antimicrobial effects, binds enterotoxins, reduces stool frequency
Dyspepsia, gas, indigestions, heartburn, nausea, acute diarrhea, traveler’s diarrhea
(prevention), treatment of H. pylori infections
Nausea, melena, blackened tongue, black stool, neurotoxicity, Reye syndrome, salicylate
toxicity
Hypersensitivity to aspirin or salicylates, infectious diarrhea, high fever, von Willebrand disease, hemorrhage, ulcer or GI bleeding with black or bloody stool, hemophilia, viral illness
C (D in 3rd trimester)/precaution
D/contraindicated for bismuth subsalicylate/tetracycline/metronidazole combination formulation
Erythromycin: ROA (1) MOA (1) A&E (1) Use (2) AE (8)
IV
Direct stimulation of motilin receptors on GI smooth muscle
Promotes onset of migrating motor complex
Gastroparesis, promotion of gastric emptying of blood before endoscopy in patients with
acute upper GI hemorrhage
Superinfection, C. difficile associated diarrhea, hepatitis, QT prolongation, ventricular
arrhythmias, torsade de pointes, Stevens-Johnson syndrome, reversible hearing loss
Metoclopramide: ROA (3) MOA (1) A&E (3) Use (4 oral, 4 IM/V) AE (6 and BBW) Contraindications (4) PLR
Oral (syrup, tablet), IV, IM
Dopamine D2-receptor antagonist
Enhances gastric emptying, increases peristalsis and LES pressure
Oral use – chemotherapy-induced nausea or vomiting, diabetic gastroparesis, advancement of nasoenteric feeding tubes, GERD
IV or IM use – chemotherapy-induced nausea or vomiting, diabetic gastroparesis, small bowel movement intubation, post-operative nausea or vomiting
Tardive dyskinesia, extrapyramidal symptoms, galactorrhea, gynecomastia, impotence,
hematological abnormalities
Black Box Warning – Potential risk of development of tardive dyskinesia
Pheochromocytoma, seizure disorder, GI bleed/perforation/obstruction, other drugs causing extrapyramidal symptoms
B/precaution (safety unknown)
Pancreatic Enzyme Supplements (Pancrealipase): ROA (1) MOA (1) A&E (1) Use (1) AE (5) Contraindications (1) PLR
Oral (delayed-release capsule, tablet)
Displays enzymatic activity proper to each enzyme
Breakdown of target bio-macromolecules in food in GI lumen
Treatment of exocrine pancreatic insufficiency
Abdominal cramping, headache, fibrosing colonopathy, intestinal obstruction, recurrence of pre-existing carcinoma
Hypersensitivity to pork protein
C/precaution (safety unknown)
Name the three different drug regimens to treat H. pylori infections.
- 14 d “triple therapy”
Amoxicillin/metronidazole, clarithromycin, es/omeprazole - 10d “sequential”
d 1-5= Amoxicillin + PPI (es/omeprazole)
d 6-10= PPI (es/omeprazole) + clarithromycin, tinidazole - 14 days
Bismuth subsalicylate, PPI (es/omeprazole) x2
metronidazole, tetracycline x4
Name the Antacids
Aluminum hydroxide and magnesium hydroxide
Calcium carbonate
Sodium bicarbonate, aspirin and citric acid
Name the H2-Receptor Antagonists
Cimetidine
Famotidine
Rantidine
Name the Proton Pump Inhibitors
Esomeprazole
Omeprazole
Name the Mucosal Protective Agents
Sucralfate
Misoprostol
Bismuth subsalicylate
Name the Prokinetics
Ethryromycin
Metoclorpramide