Crofelemer

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[edit] BRAND NAMES

[edit] MECHANISM OF ACTION

Crofelemer is a botanical drug substance (oligomeric proanthocyanidin) extracted from the stem bark latex of the Croton lechleri tree.

It is a first-in-class antidiarrheal agent that simultaneously targets two distinct channels, the cystic fibrosis conductance regulator (CFTR) and calcium-activated chloride channel (CaCC), responsible for chloride (Cl) and fluid secretion in the GI tract.

Crofelemer acts by blocking Cl secretion and accompanying high volume water loss in diarrhea, normalizing the flow of Cl and water in the gastrointestinal tract.

[edit] INDICATIONS

Crofelemer is an anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy

[edit] DOSAGE

One 125 mg delayed-release tablet taken orally twice a day, with or without food

[edit] CONTRAINDICATIONS

None

[edit] WARNINGS AND PRECAUTIONS

Before starting Crofelemer, rule out infectious etiologies of diarrhea. Crofelemer is not indicated for the treatment of infectious diarrhea.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). 'Crofelemer' should be used during pregnancy only if clearly needed.
  • Nursing Mothers: It is not known whether 'Crofelemer' is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

[edit] SIDE EFFECTS

Most common adverse reactions (incidence ≥ 3%) are upper respiratory tract infection, bronchitis, cough, flatulence and increased bilirubin.

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[edit] BIBLIOGRAPHY

[edit] REFERENCES