crofelemer

General

Pronunciation:
kro-fel-e-mer


Trade Name(s)

  • Mytesi

Ther. Class.
antidiarrheals

Pharm. Class.
catechins

Indications

Symptomatic relief of non-infectious diarrhea in HIV-infected patients currently receiving antiretroviral therapy.

Action

  • A natural product derived from  Croton lechleri , a species of flowering plant.
  • Inhibits cyclic adenosine monophosphate (cAMP)-stimulated cystic fibrosis transmembrane conductance regulator (CTFR) chloride ion channels and the calcium-activated chloride channels on luminal membranes of enterocytes. Blocks chloride secretion and water loss by inhibiting chloride channels on the membranes of enterocytes.

Therapeutic Effect(s):

Decreased incidence and severity of diarrhea.

Pharmacokinetics

Absorption: Minimal absorption following oral administration.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: Unknown.

TIME/ACTION PROFILE

ROUTEONSETPEAKDURATION
POunknownunknownunknown

Contraindication/Precautions

Contraindicated in:

  • Lactation: Breastfeeding should be avoided in patients with HIV.

Use Cautiously in:

  • Infectious causes of diarrhea (evaluate and treat prior to use);
  • OB:  Safety not established in pregnancy;
  • Pedi:   Safety and effectiveness not established in children.

Adverse Reactions/Side Effects

CNS: anxiety

EENT: nasopharyngitis

GI: abdominal distention, flatulence, hemorrhoids, nausea, ↑ liver function tests

GU: urinary tract infection

MS: arthralgia, back pain, musculoskeletal pain

Resp: bronchitis, cough, upper respiratory tract infection

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

Due to minimal systemic absorption, interactions are unlikely.

Route/Dosage

PO (Adults): 125 mg twice daily.

Availability

Delayed-release tablets: 125 mg

Assessment

  • Assess for abdominal distention, presence of bowel sounds, and usual pattern of bowel function.
  • Assess color, consistency, and amount of stool produced.

Potential Diagnoses

Implementation

  • PO Administer tablets twice daily with or without food. Swallow tablets whole; do not crush, break, or chew.

Patient/Family Teaching

  • Instruct patient to take crofelemer as directed.
  • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding.

Evaluation/Desired Outcomes

Decreased incidence and severity of diarrhea.

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