Drug reference
crofelemer
CFTR and Ca2+-activated chloride channel inhibitor · Antidiarrheal
CFTR and Ca2+-activated chloride channel inhibitorAntidiarrhealATC A07XA06
CDSCO approvedATC A07XA06
EXCRETION
—
not curated
INTERACTIONS
—
none in our sources
PREGNANCY
—
not curated
Mechanism
Crofelemer inhibits the cystic fibrosis transmembrane conductance regulator (CFTR, a cyclic AMP–stimulated Cl– channel) and Ca2+-activated chloride ion channels on the luminal aspect of the enterocyte, thereby reducing water loss associated with chloride secretion into the lumen.
Indications
Diarrhea associated with antiretroviral therapy for HIV/AIDS (not approved for infectious or other diarrheas)
Dosing
- Adult
- 125 mg orally twice daily.
Pharmacokinetics
Bioavailability
Minimal systemic absorption
Side effects
Common
Upper respiratory tract infectionsCoughFlatulenceNauseaJoint painBack painOther GI effects
Related guidelines
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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team