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lubiprostone

ClC-2 chloride channel activator; Prostanoid activator · Prosecretory agent; Laxative

ClC-2 chloride channel activator; Prostanoid activatorProsecretory agent; LaxativeATC A06AX03
CDSCO approvedATC A06AX03
EXCRETION
not curated
INTERACTIONS
none in our sources
PREGNANCY
not curated

Mechanism

Lubiprostone is a prostanoid activator of ClC-2 Cl– channels. It appears to bind to the EP4 prostaglandin receptor for PGE2, which couples to Gs, activating adenylyl cyclase and leading to enhanced apical Cl– conductance. This promotes the secretion of a chloride-rich fluid, improving stool consistency and promoting increased frequency by reflexly activating motility.

Indications

Constipation-predominant IBSChronic constipationOpioid-induced constipation

Dosing

Adult
8 μg twice daily (for constipation-predominant IBS). 24 μg twice daily (for chronic constipation and opioid-induced constipation).

Pharmacokinetics

Bioavailability
Poorly bioavailable (acts only in the bowel lumen)

Side effects

Common
Nausea (up to 30% of patients)HeadacheDiarrheaAllergic reactionsDyspnea

Related guidelines

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team