2016 Lower GI Pharmacology

Mechanism of action

• Voltage-independent block of CFTR and anoctamin 1 (calcium-activated chloride channel)


• decreased Cl^- secretion → decreased sodium and water excretion → firmer stool


• very little systemic absorption


• purified from red latex from the South American "dragon's blood" tree

Therapeutic uses

• CROFELEMER is used to treat non-infectious diarrhea caused by anti-HIV drugs (e.g. nucleoside analog reverse transcriptase and protease inhibitors)

• Chloride secretion
  • CIC-2 stimulant
  • GC-C activator
  • CFTR Inhibitor
  • Somatostatin analogue
  • Bismuth subsalicylate
• Osmotic cathartics
• BABRs