Cytoprotective agents

• Cytoprotective agent overview


  medications that coat the mucosal wall to treat and prevent ulcer formation
• cytoprotective agents examples


  Sucralfate (Carafate)

  Misoprostol (Cytotec)
• Pharmacodynamics of cytoprotective agents

  sucralfate: Al salt that selectively binds to necrotic ulcer tissue and acts as a barrier to acid

  Misoprostol: methyl analog that inhibits histamine production of cAMP, inhibits gastric acid secretion. prostaglandin E binds to misoprostol causing higher production of mucus and bicarbonate
• Pharmacotherapeutics of cytoprotective agents

  Sucralfate has no contraindications

  Misoprostol: caution in renal impairment, caution in older adults

  pregnancy category X can induce uterine contractions

  excreted in breast milk
• Adverse drug reactions of cytoprotective agents

  Sucralfate: constipation

  Misoprostol: diarrhea, abdominal pain, flatulence, cramps, pregnancy complications
• Drug interactions of cytoprotective agents

  separate from other drugs by at least 2 hours
• Clinical use and dosing of cytoprotective agents

  Sucralfate: duodenal ulcers 1 hour before meals and at bedtime, combining with H2RA can increase effectiveness

  Misoprostol: for ulcers taken 200mcg 4 times a day with food and at bedtime
• Education of cytoprotective agents

  take as prescribed, do not double dose

  missed doses as soon as possible

  misoprostol should not be given to pregnant women
• Adverse reactions of cytoprotective agents

  GI bleeding

  misoprostol can cause spontaneous abortion

  nausea and vomiting
• sucralfate binds to ulcer tissue and acts as a barrier
• misoprostol inhibits cAMP formation and inhibits prostaglandin synthesis to increase mucus production
• Misoprostol can cause uterine contractions which may endanger pregnancy
• Misoprostol works within minutes whereas sucralfate takes about 30 min to onset
• first-line therapy of NSAID induced gastric ulcers is to discontinue the NSAID. Misoprostol is approved for prophylaxis of NSAID induced ulcers
• Sucralfate can be used for short term treatment of active ulcers

  1 g four times a day on an empty stomach

  maintenance is 1g twice a day
• Sucralfate is drug of choice in treatment of ulcers not induced by NSAID