Gastrointestinal Pharmacology

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jknell
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206920
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Gastrointestinal Pharmacology
Updated:
2013-03-12 22:33:40
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  1. H2 Blockers
    • Cimetidine
    • Ranitidine
    • Famotidine
    • Nizatidine

    "Take H2 blockers before you dine. Think Table 2"

    • Mechanism:
    • -Reversible block of histamine H2 receptors
    • -decreases H+ secretion by parietal cells

    • Clinical Use:
    • -Peptic ulcer
    • -gastritis
    • -mild esophageal reflux

    • Toxicity (Cimetidine):
    • -potent inhibitor of cytochrome P450 (multiple drug interactions
    • -antiandrogenic effects (prolactin release, gynecomastia, impotence, decreased libido in males)
    • -can cross BBB (confusion, dizziness, HA) and placenta
    • -decreased renal excretion of Cr (Ranitidine as well)

    **other H2 blockers are relatively free of these effects
  2. Proton Pump Inhibitors
    • Omeprazole
    • Lansoprazole
    • Esomeprazole
    • Pantoprazole
    • Dexlansoprazole

    • Mechanism:
    • -irreversibly inhibit H+/K+ ATPase in stomach parietal cells

    • Clinical Use:
    • -peptic ulcer
    • -gastritis
    • -esophageal reflux
    • -Zollinger-Ellison syndrome

    • Toxicity:
    • -increased risk of C. difficile infection and pneumonia
    • -Hip fractures
    • -Decrease serum Mg2+ with long term use
  3. Bismuth, sucralfate
    • Mechanism:
    • -bind to ulcer base, providing physical protection and allowing HCO3- secretion to reestablish pH gradient in the mucous layer

    • Clinical Use:
    • -increase ulcer healing
    • -traveler's diarrhea
  4. Misoprostol
    • Mechanism:
    • -PGE1 analog
    • -increases production and secretion of gastric mucous barrier
    • -decrease acid production

    • Clinical Use:
    • -prevention of NSAID-induced peptic ulcers
    • -maintenance of patent ductus arteriosus
    • -also used to induce labor (ripens cervix)

    • Toxicity:
    • -diarrhea
    • -CI in women of child bearing potential (abortifactant)
  5. Octreatide
    • Mechanism:
    • -long-acting somatostatin analog

    • Clinical use:
    • -acute variceal bleeds
    • -acromegaly
    • -VIPoma
    • -carcinoid tumors

    • Toxicity:
    • -Nausea
    • -Cramps
    • -Steatorrhea
  6. Antacid use
    -can affect absorption, bioavailability or urinary excretion of other drugs by altering gastric and urinary pH or by delaying gastric emptying

    -all can cause hypokalemia

    -overuse can cause specific problems
  7. Aluminum hydroxide
    Hypokalemia

    • Toxicity:
    • -constipation
    • -hypophosphatemia
    • -proximal muscle weakness
    • -osteodystrophy
    • -seizures

    "Aluminimum amount of feces"
  8. Magnesium hydroxide
    Hypokalemia

    • Toxicity:
    • -diarrhea
    • -hyporeflexia
    • -hypotension
    • -cardiac arrest

    "Mg = Must go to the bathroom"
  9. Calcium Carbonate
    Hypokalemia

    • Toxicity:
    • -hypercalcemia
    • -rebound increase in acid
    • -can chelate and decrease the effectiveness of other drugs (tetracycline)
  10. Osmotic Laxatives
    • Magnesium hydroxide
    • Magnesium citrate
    • Polyethylene glycol
    • Lactulose

    • Mechanism:
    • -provide osmotic load to draw water out
    • -lactulose: also treats hepatic encephalopathy (gut flora degrade it into metabolites that promote nitrogen excretion as NH4+)

    • Clinical use:
    • -constipation

    • Toxicity:
    • -diarrhea
    • -dehydration
    • -may be abused by bulimics
  11. Infliximab
    • Mechanism:
    • -monoclonal antibody to TNFa

    • Clinical Use:
    • -Crohn's disease
    • -ulcerative colitis
    • -rheumatoid arthritis

    • Toxicity:
    • -infection (including reactivation of latent TB)
    • -fever
    • -hypotension
  12. Sulfasalazine
    • Mechanism:
    • -combination of sulfapyridine (antibacterial) and 5-aminosalicylic acid (anti-inflammatory)
    • -activated by colonic bacteria

    • Clinical use:
    • -ulcerative colitis
    • -Crohn's disease

    • Toxicity:
    • -malaise
    • -nausea
    • -sulfa toxicity
    • -reversible oligospermia
  13. Ondansetron
    • Mechanism:
    • -5HT3 antagonist
    • -powerful central acting anti-emetic

    • Clinical use:
    • -control vomiting post-op and in patients with cancer chemotherapy

    • Toxicity:
    • -HA
    • -constipation

    "At a party but feeling queasy? Keep on dancing with ondansetron!"
  14. Metoclopramide
    • Mechanism:
    • -D2 receptor antagonist
    • -increases resting tone, contractility, LES tone, motility
    • -does not influence colon transport time

    • Clinical use:
    • -diabetic and post-surgery gastroparesis
    • -antiemetic

    • Toxicity:
    • -increased parkinsonian effects
    • -restlessness
    • -drowsiness
    • -fatigue
    • -depression
    • -nausea
    • -diarrhea
    • -drug interaction with digoxin and diabetic agents
    • -CI: patients with small bowel obstruction or Parkinson's Disease

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