GI drugs

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Author:
bshin
ID:
88245
Filename:
GI drugs
Updated:
2011-05-29 03:09:07
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GI drugs
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GI drugs
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  1. Parietal cell receptors
    • -para (enteric NS)-->Ach--> M3--> Gq--> IP3
    • -food-->antrum G cells--> Gastrin-->CCKb receptor--> Gq-ECL cell--> Histamine--> H2 receptor--> Gs-->cAMP
    • -PGs-->Gi-->decrease cAMP
    • -Somatostatin-->Gi--> decrease cAMP
  2. Enterochromaffin like cells
    ECL cells

    -what receptors do they have?
    Para enteric NS--> Ach--> M1-->

    Somatostatin--> ST2 receptor--> (inhibitory)

    G-cells--> Gastrin--> CCKb receptor
  3. Parietal cell proton pump
    K/H-ATPase!

    • pump H+ out, K+ in
    • use ATP
  4. H2 blockers
    "--dine"

    • Cimetidine
    • Ranitidine
    • Famotidine
    • Nizatidine

  5. Cimetidine
    • H2 blocker
    • -reversible block H2 receptor--> decrease H+ release by parietal cells
    • -inhibit CYPs!!
    • -antiandrogenic!
    • -cross BBB, placenta!

    USE- peptic ulcer, gastritis, mild GERD

    • SE- antiandrogenic effect!- prolactin release, gynecomastia, impotence, decrease libido in males
    • -confusion, dizziness, headaches (cross BBB)
    • Decrease renal CRN excretion!
  6. Ranitidine
    • H2 blocker
    • -reversible block H2 receptor--> decrease H+release by parietal cells
    • -decrease CRN clearance!

    USE- peptic ulcer, gastritis, mild GERD

    SE-decrease renal CRN excretion!
  7. Famotidine
    • H2 blocker
    • -reversible block H2 receptor--> decrease H+release by parietal cells

    -USE- peptic ulcer, gastritis, mild GERD
  8. Nizatidine
    • H2 blocker
    • -reversible block H2 receptor--> decrease H+release by parietal cells

    -USE- peptic ulcer, gastritis, mild GERD
  9. Omeprazole
    • PPI
    • irreversibly inhibit H/K-ATPase in gastric parietal cells

    USE- Peptic ulcer, Gastritis, GERD, Zollinger Ellison Syndrome
  10. Lansoprazole
    • PPI
    • irreversibly inhibit H/K-ATPase in gastric parietal cells

    USE- Peptic ulcer, Gastritis, GERD, Zollinger Ellison Syndrome
  11. Bismuth
    • Bind to gastric ulcer base
    • -provide physical protection
    • -allow HCO3- secretion to reestablish pH gradient in mucosal layer

    USE- increase ulcer healing, traveler's diarrhea
  12. Sucralfate
    • Bind to gastric ulcer base
    • -provide physical protection
    • -allow HCO3- secretion to reestablish pH gradient in mucosal layer

    USE- increase ulcer healing, traveler's diarrhea
  13. Triple therapy regimen for H. pylori
    Metronidazole + Amoxicillin + Bismuth

    +/ PPI

    or (tetracycline instead of Amoxicillin)
  14. Misoprostol
    • PGE1 analog
    • -Increase production, secretion of gastric mucous barrier.
    • -Decrease acid production

    • USE- prevent NSAID-induced peptic ulcers
    • -maintain PDA! (Tetralogy of Fellot, Complete Transposition)
    • -Induce LABOR!

    • SE- Diarrhea
    • do NOT use in women of childbearing potential (abortifacient)
  15. Pirenzepine
    • Muscarinic antagonist
    • -block M1 on ECL cells--> decrease Histamine secretion
    • -block M3 on parietal cells--> decrease H+ secretion

    USE- Peptic ulcer (rarely used)

    • SE- tachycardia, dry mouth, cycloplegia
    • (3C's!)
  16. Propantheline
    • Muscarinic antagonist
    • -block M1 on ECL cells--> decrease Histamine secretion
    • -block M3 on parietal cells--> decrease H+ secretion

    USE- Peptic ulcer (rarely used)

    SE- tachycardia, dry mouth, cycloplegia (3C's!)
  17. Octreotide
    Somatostatin analog

    • USE- acute variceal bleeds, Acromegaly
    • - VIPoma, Carcinoid tumors

    SE- nausea, cramps, steatorrhea (malabsorption)
  18. Antacids
    • AlOH
    • MgOH
    • CaCO3
  19. -can affect absorption, bioavailability, urinary excretion of other drugs by:
    • -altering gastric and urinary pH
    • -delaying gastric emptying
    • -can chelate, decrease efficacy of drugs
    • (ex) Tetracycline
    • -can cause HYPOKALEMIA!!!!
  20. AlOH
    • Antiacid
    • -can affect absorption, bioavailability, urinary excretion of other drugs by:
    • -altering gastric and urinary pH
    • -delaying gastric emptying
    • -can chelate, decrease efficacy of drugs (ex) Tetracycline
    • -can cause HYPOKALEMIA!!!!

    • specific SE- Constipation, Hypophosphatemia
    • Proximal muscle weakness, osteodystrophy, seizures
  21. MgOH
    • Antiacid
    • -can affect absorption, bioavailability, urinary excretion of other drugs by:
    • -altering gastric and urinary pH
    • -delaying gastric emptying
    • -can chelate, decrease efficacy of drugs (ex) Tetracycline
    • -can cause HYPOKALEMIA!!!!

    specific SE- diarrhea, hyporeflexia, hypotension, cardiac arrest
  22. CaCO3
    • Antiacid
    • -can affect absorption, bioavailability, urinary excretion of other drugs by:
    • -altering gastric and urinary pH
    • -delaying gastric emptying
    • -can chelate, decrease efficacy of drugs (ex) Tetracycline
    • -can cause HYPOKALEMIA!!!!

    Specific SE- hypercalcemia, rebound acid increase
  23. Infliximab
    monoclonal antibody to TNF

    USE- Crohn's disease, Rheumatoid arthritis

    • SE- Resp infection (reactivation of latent TB)
    • fever, hypotension
  24. Sufasalazine
    • combo of Sufapyridine + 5-aminosalicylic acid
    • (antibiotic + anti-inflammatory)
    • -activated by colonic bacteria

    USE-Ulcerative colitis, Crohn's disease

    SE-Malaise, nausea, sulfonamide hypersensitivity, reversible oligospermia!
  25. Ondansetron
    • 5-HT3 antagonist
    • -powerful centrally acting antiemetic!

    USE- nausea/vomiting in post-op, chemotherapy

    SE- headache, constipation
  26. Metoclopramide
    • D2 receptor antagonist
    • -increase resting tone, contractility, Lower esophageal sphincter tone, mobility
    • -does NOT influence colon transport time

    USE- Diabetic neuropathy illeus, post-op gastroparesis

    • SE- parkinsonian effects! restlessness, drowsiness, fatigue, depression, nausea, diarrhea.
    • -drug interaction w/ Digoxin, DM agents
    • do NOT use in small bowel obstruction!

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