GI System Drugs Flashcards
Mechanism: Misoprostol
PGE1 analog:
- Increases production and secretion of gastric mucous barrier
- Decreases acid production
All antacids can cause ___
Hypokalemia
Class: Polyethylene glycol
Osmotic laxative
Class: Magnesium hydroxide
Antacid
Osmotic laxative
Mechanism:
Loperamide
Diphenoxylate (+ atropine)
Agonist at mu-opioid receptors → slows gut motility
Loperamide: Poor CNS penetration (low addictive potential)
Diphenoxylate: Slight diffusion across BBB (atropine added to reduce abuse)
Clinical use: Sulfasalazine
- Ulcerative colitis (UC)
- Crohn disease (colitis component)
Adverse effects: Ondansetron
- Headache
- Constipation
- QT interval prolongation
- Serotonin syndrome (when used with other serotonergic drugs)
Adverse effects: Stimulant laxative
Senna
- Diarrhea
- Melanosis coli (dark brown/black discoloration of colon due to pigment deposition in lamina propria)
Adverse effects: Osmotic laxatives
Magnesium hydroxide
Magnesium citrate
Polyethylene glycol
Lactulose
- Diarrhea
- Dehydration
- May be abused by bulimics
Adverse effects: Bulk-forming laxatives
Psyllium
Methylcellulose
- Bloating
Overuse: Calcium carbonate (antacid)
- Hypercalcemia (milk-alkali syndrome)
- Rebound acid increase
Clinical use: Octreotide
- Acute variceal bleeds
- Acromegaly
- VIPoma
- Carcinoid tumors
Adverse effects: PPIs
- C. difficile infection
- Pneumonia
- Decreaes serum Mg2+ with long-term use
Adverse effects: Misoprostol
- Diarrhea
- Contraindicated in women of childbearing potential (abortifacient)
Mechanism: Emollient laxative
Docusate
Osmotic draw into lumen → increases water absorption by stool
Adverse effects: Octreotide
- Steatorrhea
- Increase risk of cholelithiasis due to CCK inhibition
- Nausea
- Cramps
Clinical use: Ondansetron
- Controlling post-op vomiting
- Cancer chemotherapy
Adverse effects:
Loperamide
Diphenoxylate
- Constipation
- Nausea
Class: Senna
Stimulant laxative
Adverse effects: Orlistat
- Steatorrhea
- Decrease absorption of fat-soluble vitamins
Mechanism: Orlistat
Inhibits gastric and pancreatic lipase → decreases breakdown and absorption of dietary fats
Mechanism: H2 blockers
Cimetidine
Ranitidine
Famotidine
Nizatidine
Reversible block of histamine H2-receptors → decreasing H+ secretion by parietal cells
Mechanism: Stimulant laxative
Senna
Enteric nerve stimulation → colonic contraction
Clinical use: H2 blockers
- Peptic ulcer
- Gastritis
- Mild esophageal reflux
Mechanism: Ondansetron
5-HT3 antagonist
Decrease vagal stimulation
Powerful central-acting antiemetic
Adverse effects:
Metoclopramide
Prochlorperazine
- Parkinsonian effects
- Tardive dyskinesia
- Restlessness
- Drowsiness/fatigue
- Depression
- Diarrhea
Mechanism: Octreotide
Long-acting somatostatin analog
Inhibits secretion of various splanchnic vasodilatory hormones
Overuse: Aluminum hydroxide (antacid)
- Constiaption
- Hypophosphatemia
- Proximal muscle weakness
- Osteodystrophy
- Seizures
___ is a potent P-450 inhibitor
It also has antiandrogenic effects (prolactin, release, gynecomastia, importence, decreased libido in males)
Can cross BBB and placenta
Cimetidine
___ can chelate and decrease effectiveness of other drugs (e.g., tetracyclines)
Calcium carbonate
Laxatives are indicates for ___ or ___
Constipation
Patients on opiates requiring bowel regimen
Mechanism: Osmotic laxatives
Magnesium hydroxide
Magnesium citrate
Polyethylene glycol
Lactulose
Provide osmotic load to draw water into GI lumen
___ is an osmotic laxative that also treats hepatic encephalopathy because gut flora degrade it into metabolites (lactic acid, acetic acid) that promote nitrogen excretion as NH4+
Lactulose
Metoclopramide and Prochlorperazine cause drug interactings with ___ and ___
Digoxin
Diabetic agents
Clinical use:
Loperamide
Diphenoxylate
- Diarrhea
Class: Docusate
Emollient laxative
Clinical use: PPIs
- Peptic ulcer
- Gastritis
- Esophageal reflux
- Zollinger-Ellison syndrome
- Component of H. pylori triple therapy
- Stress ulcer prophylaxis
Clinical use:
Aprepitant
Fosaprepitant
(-pitant)
- Antiemetic for chemotherapy-induced N/V
Class: Magnesium citrate
Osmotic laxative
Clinical use:
Bismuth
Sucralfate
- Increase ulcer healing
- Travelers’ diarrhea
Metoclorpramide and Prochlorperazine are contraindicated in patients with ___ or ___ (due to D2-receptor blockade)
Small bowel obstruction
Parkinson disease
Mechanism:
Metoclopramide
Prochlorperazine
D2 receptor antagonists - increases:
- Resting tone
- Contractility
- LES tone
- Motility
- Promotes gastric emptying
Does not influence colon transport time
Clinical use:
Metoclopramide
Prochlorperazine
- Diabetic and post-surgical gastroparesis
- Antiemetic
- Persistent GERD
Mechanism: PPIs
(-prazole)
Irreversibly inhibit H+/K+ ATPase in stomach parietal cells
Class: Lactulose
Osmotic laxative
Overuse: Magnesium hydroxide
- Diarrhea
- Hyporeflexia
- Hypotension
- Cardiac arrest
Antacid use can affect absorption, bioavailability, or urinary excretion of other drugs by altering ___ or by ___
Gastric and urinary pH
Delaying gastric emptying
Adverse effects: Emollient laxative
Doxusate
- Diarrhea
Mechansm:
Aprepitant
Dosaprepitant
(-pitant)
Substance P antagonist:
Blocks neurokinin-1 (NK1) receptors in brain
Mechanism:
Bismuth
Sucralfate
Bind to ulcer base providing physical protection and allowing HCO3- secretion to reestablish pH gradient in the mucous layer
Require acidic environment
Usually not given with PPIs or H2 blockers
___ and ___ are H2 blockers that decrease renal excretion of creatinine
Other H2 blockers are relatively free of these effects
Cimetidine
Ranitidine
Class: Methylcellulose
Bulk-forming laxative
Clinical use: Orlistat
Weight loss
Clinical use: Misoprostol
- Prevention of NSAID-induced peptic ulcers (NSAIDs block PGE1 production)
- Off-label: Induction of labor (ripens cervix)
Mechanism: Sulfasalazine
Combination:
- Sulfapyridine (antibacterial)
- 5-aminosalicylic acid (anti-inflammatory)
Activated by colonic bacteria
Adverse effects: Sulfasalazine
- Malaise
- Nausea
- Sulfonamide toxicity
- Reversible oligospermia
Class: Psyllium
Bulk-forming laxative
Mechanism: Bulk-forming laxatives
Psyllium
Methylcellulose
Soluble fibers: Draws water into gut lumen, forming a viscous liquid that promotes peristalsis