GI drug List

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Author:
jknell
ID:
123674
Filename:
GI drug List
Updated:
2011-12-14 15:37:36
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Gastrointestinal Drug List
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GI drug List
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  1. Antacids
    • Mg(OH)2
    • Al(OH)3
  2. Mg(OH)2
    Mechanism: neutralize gastric acid

    Indications: Acid-peptic diseases

    Adverse Effects: diarrhea, hyermagnesemia (pts with kidney disease)

    • Other:
    • a. optimized efficacy with postprandial dosing
    • b. secondary mechanism: angiogenesis, suprresion of H pylori)
    • c. alter absorption of drugs with pH dependent F
    • d. chelate small drugs and decrease absorption
  3. Al(OH)3
    Mechanism: neutralize gastric acid

    Indications: anti-peptic diseases

    Adverse Effects: constipation

    • Other:
    • a. optimized efficacy with postprandial dosing
    • b. secondary mechanism: angiogenesis, suprresion of H pylori)
    • c. alter absorption of drugs with pH dependent F
    • d. chelate small drugs and decrease absorption
  4. H2 Receptor Antagonists
    -tidines

    Cimetidine
  5. Cimetidine
    Mechanism: blocks H2 receptors on basolateral membrane of parietal cells deceasing gastric acid secretion

    Indications: acid-peptic diseases

    Adverse Effects: endocrine side effects (galactorrhea in women, impotence in men), minor side effects (GI, headache etc)

    • Other:
    • a. decrease hepatic blood flow (increase duration of action of some drugs)
    • b. affect absorption of drugs with a pH dependent F
    • c. inhibits CYPs
    • d. competes with drugs and creatine for secretion in kidney
    • e. Tolerance can develop
    • f. Discontinuation --> rebound hypersecretion
  6. Proton Pump Inhibitors
    -prazoles

    Omeprazole
  7. Omeprazole
    Mechanism: inhibit K+-H+ ATPase on apical membrane of parietal cell, decreasing gastric acid secretion

    Indications: acid-peptic diseases

    Adverse Effects: minor side effects (GI, headache), nutritional concerns (decrease absorption of B12 and Ca), infection concerns (risk of enteric and respiratory infections)

    • Other:
    • a. most efficacious inhibitors of gastric acid
    • b. may alter absorption of drugs with pH dependent F
    • c. interacts with CYP2C19 (inhibits) and CYP1A2 (induces)
    • d. discontinuation can cause rebound acid hypersecretion
  8. Prostaglandin Analogs
    Misoprostol
  9. Misoprostol
    Mechanism: stimulates EP3 receptors on basolateral membrane of parietal cell --> decreasing gastric acid secretion. stimulates EP3 receptors on basolateral membrane of surface mucus cell --> increased mucus, HCO3- secretion

    Indications: NSAID induced ulcers and mucousal damage

    Adverse Effects: diarrhea, headache

    Other: contraindicated in pregnancy, four qd dosing (low adherence)
  10. Drugs that enhance mucosal defense
    1. Sucralfate (viscous paste that adheres to ulcers, seldom used)

    2. Bismuth subsalicylate = Peptobismol (coats uclers, HCO3- secretions, antibacterial) --> can turn tongue and stool black
  11. D2 Antagonists
    Metoclopramide
  12. Metoclopramide
    Mechanism: blocks D2 receptors on excitatory motor neurons in ENS --> increased motility, stimulates presynaptic 5-HT4 receptors on IPANs --> increased motility

    Indications: gastroparesis, Nausea/Vomiting

    Adverse Effects: Extra Pyramidal Symptoms (black box warning)
  13. Peripherally restricted opiods
    • 1. Loperamide (immodium)
    • 2. Diphenoxylate
  14. Loperamide
    Mechanism: stimulates u and o opoid receptors on enteric neurons --> increased segmental contractions, decreased peristaltic contractions and increased tone of anal sphinter and dessication of bowel contents

    Indications: diarrhea

    Adverse Effects: abdominal pain, abdominal distention, constipation

    Other: more effective than diphenoxylate
  15. Diphenoxylate
    • Mechanism: stimulates u and o opoid receptors on enteric neurons -->
    • increased segmental contractions, decreased peristaltic contractions and
    • increased tone of anal sphinter and dessication of bowel contents

    Indications: diarrhea

    Adverse Effects: abdominal pain, abdominal distention, constipation

    Other: mAChR antagonist side effects at high doses
  16. Peripherally restricted opioid antagonists
    Methylnaltrexone
  17. Methylnaltrexone
    Mechanism: Block u opioid receptors in ENS --> decrease opioid-induced constipation

    Indications: opioid induced constipation

    Adverse Effects: abdominal pain, flatulence, nausea, dizziness, diarrhea

    Other: unable to cross BBB so does not block analgesic effects of opiods
  18. Antispasmodics (no names)
    Mechanism: block mAChRs in ENS and on GI SM --> decreased GI motility

    Indications: IBS

    Adverse Effects: mAChR antagonist effects

    Other: evidence limited, contraindicated in pt with GI or UT obstruction
  19. Laxatives and Cathartics
    1. Luminally active agents

    2. Stimulant (irritant) laxatives

    3. Prosecretory Laxatives
  20. Luminally active agents
    1. bulk forming laxatibes (indigestible, absorb water, bulky gel, reflex increase in motility)

    2. osmotic agents (soluble, nonabsorbable compounds that retain fluid in lumen, reflex increase in motility)

    3. stool softeners (decrease stool surface tension, increase fluid/electrolyte secretion)
  21. Stimulant (irritant) laxatives
    direct effects on enterocytes, enteric neurons and GI smooth muscle --> increase fluid/electrolyte secretion and increased motility

    Castor oil: ricinoleic acid (metabolite) causes increase fluid/electrolyte secretion and increased motility --> can be toxic!
  22. Proscretory Laxatives
    Stimulate EP4 receptors on GI epithelial cells --> activates chloride channels and increases fluid/electrolyte secretion, reflex increase in motility
  23. Antidiarrheal Agents
    1. Bile salt-binding resins

    2. Somatostatin analogs
  24. Bile Salt-binding Resins
    Cholestyramine
  25. Cholestyramine
    Mechanism: Bind BAs in lumen of small intestine and interrupt enterohepatic recycling, more BAs reach colon, increases fluid and electrolyte secretion

    Indications: Bile salt- induced diarrhea

    Adverse Effects: bloating, flatulence, constipation
  26. Somatostatin analogs
    Octreotide
  27. Octreotide
    Mechanism: stimulates SST receptors --> decreased secretion of GI mediators (VIP), decreased GI motility, decreased pancreatic secretion, decreased fluid/electrolyte secretion

    Indications: diarrhea caused by hormone secreting tumors (VIPoma)

    Adverse Effects: Nausea, bloating, steatorrhea, gallstones with long term use

    Other: also used in tx of diarrhea of other etiolgies etc
  28. Pharmacotherapy of Nausea/emesis
    1. 5-HT3 antagonists (-setrons)

    2. D2 antagonists

    3. mAChR antagonist

    4. H1 antihistamine

    5. NK1 antagonists

    6. Corticosteroids

    7. Cannabinoids

    8. Benzodiazepines

    9. Alternative therapies (B6 and ginger)
  29. 5-HT3 Antagonists
    Ondansetron

    -setrons
  30. Ondansetron
    Mechanism: blocks 5-HT3 receptors on EPANs in ENS, CTZ and EC/NTS

    Indications: CINV, RINV, PONV, Gastroenteritis induced NV

    Adverse Effects: minor

    Other: most efficacious antiemetics in prevent of CINV (better when combined with NK1 antagonists and corticosteriods)
  31. D2 antagonists
    1. Metocloprimide

    2. Prochlorperazine
  32. Metocloprimide/Prochlorperazine
    Mechanism: block D2 receptors in CTZ and in EC/NTS

    Indications: PONV, GINV, Migraine induced NV, GI motility induced NV, CINV

    Adverse Effects: EPS (black box warning)

    Other: good general purpose antiemetics
  33. mAChR Antagonists
    Scopolamine
  34. Scopolamine
    Mechanism: block mAChR on vestibular afferents and in EC/NTS

    Indications: motion sickness, PONV

    Adverse Effects: mAChR side effects

    Other: contraindication in GI or UT obstruction
  35. H1 Antihistamine (first generation)
    Diphenhydramine (benedryl)
  36. Diphenhydramine
    Mechanism: blocks H1 receptors on vestibular afferents and in EC/NTS

    Indications: motion sickness, PONV

    Adverse Effects: mAChR side effects

    Other: mAChR contraindications
  37. NK1 Antagonists
    Aprepitant
  38. Aprepitant
    Mechanism: blocks NK1 receptors in EC/NTS

    Indications: CINV (with 5-HT3 antagonists and corticosteroid)

    Adverse Effects: GI side effects, fatigue, asthenia
  39. Corticosteroids
    Dexamethasone
  40. Dexamethasone
    Mechanism: ?

    Indications: CINV (with 5-HT3 antagonists and NK1 antagonist), PONV

    no adverse effects b/c duration of therapy is short
  41. Cannabinoids
    Dronabinol
  42. Dronabinol
    Mechanism: Stimulates CB1 receptors in EC/NTS

    Indications: CINV

    Adverse Effects: CNS effects

    Other: controlled substance
  43. Benzodiazepines
    Mechanism: bind to allosteric site on GABA receptors, increase GAPA mediated IPSPs???

    Indications: CINV, PONV

    Adverse Effects: sedation

    Other: adjunctive therapy only, weak effects when adminstered alone
  44. Alternative therapies
    Vitamin B6, ginger

    Mechanism unknown

    Indications: any NV

    Other: especially useful in pregnancy

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