crofelemer

crofelemer

(kro-fel-e-mer) ,

Fulyzaq

(trade name)

Classification

Therapeutic: antidiarrheals
Pharmacologic: catechins
Pregnancy Category: C

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 effects

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
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Contraindications/Precautions

Contraindicated in: None noted.
Use Cautiously in: Infectious causes of diarrhea (evaluate and treat prior to use); Obstetric: Use during pregnancy only if clearly needed; Lactation: Breast feeding should be avoided by HIV-infected patients; Pediatric: Safe and effective use in children <18 yr has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • anxiety

Ear, Eye, Nose, Throat

  • nasopharyngitis

Respiratory

  • bronchitis
  • cough
  • upper respiratory tract infection

Gastrointestinal

  • abdominal distention
  • flatulence
  • hemorrhoids
  • nausea
  • ↑ liver function tests

Genitourinary

  • urinary tract infection

Musculoskeletal

  • arthralgia
  • back pain
  • muscuoloskeletal pain

Interactions

Drug-Drug interaction

Due to minimal systemic absorption, interactions are unlikely.

Route/Dosage

Oral (Adults) 125 mg twice daily.

Availability

Delayed-release tablets: 125 mg

Nursing implications

Nursing assessment

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

Potential Nursing Diagnoses

Diarrhea (Indications)

Implementation

  • Oral: 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.
  • Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Decreased incidence and severity of diarrhea.
References in periodicals archive ?
TM)] is a canine-specific formulation of crofelemer, an active pharmaceutical ingredient isolated and purified from the Croton lechleri tree, which is sustainably harvested.
There are four gastrointestinal agents: crofelemer (Fulyzaq; antidiarrheal), linaclotide (Linzess; laxative), teduglutide (Gattex; short bowel syndrome), and the combination of sodium picosulfate, magnesium oxide, and citric acid (Prepopik; osmotic laxative).
The option agreement with Forest Laboratories for the development of novel mPGES-1 inhibitors and the USFDA approval for Glenmark's in-licensed molecule - Crofelemer has come as a big boost and renewed validation for our world-class Drug Discovery capabilities.
The drug, Crofelemer 125 mg, is aimed at treating diarrhoea in patients with HIV/ AIDS and on anti- retroviral therapy.
According to the US Food and Drug Administration (FDA) the agency is to take some more time to review the Salix Pharmaceuticals' new drug application (NDA) for crofelemer 125 mg tablets, which is designed to provide symptomatic relief of non-infectious diarrhea in patients with HIV/AIDS on anti-retroviral therapy.
METOZOLVTM ODT (metoclopramide), crofelemer, budesonide foam and rifaximin for additional indications are under development.
Phase II trials were recently completed in the United States for crofelemer, a derivative obtained from the sap of the South American Croton lechleri tree.
Napo filed a lawsuit against Salix in New York on May, 2011 seeking to terminate its December 9, 2008 Collaboration Agreement with Salix for the Development, Manufacture and Commercialization of Napo's first-in-class anti-diarrheal drug, crofelemer (trade name FULYZAQ[sup.
Glenmark Pharmaceuticals Limited announced today that the US Food and Drug Administration has provided Marketing approval to its partner in US, Salix Pharmaceuticals Limited, for Crofelemer 125 mg delayed-release tablets for the symptomatic relief of non-infectious diarrhea in patients with human immunodeficiency virus (HIV)/ acquired immune deficiency syndrome (AIDS) on anti-retroviral therapy (ART).
surotomycin - Drug Profile 35 Product Description 35 Mechanism of Action 35 R&D Progress 35 crofelemer DR - Drug Profile 36 Product Description 36 Mechanism of Action 36 R&D Progress 36 fidaxomicin - Drug Profile 38 Product Description 38 Mechanism of Action 38 R&D Progress 38 cadazolid - Drug Profile 41 Product Description 41 Mechanism of Action 41 R&D Progress 41 fidaxomicin - Drug Profile 42 Product Description 42 Mechanism of Action 42 R&D Progress 42 AKT-10081 - Drug Profile 45 Product Description 45 Mechanism of Action 45 R&D Progress 45 MGB-BP-3 - Drug Profile 46 Product Description 46
Napo") seeking, among other things, a ruling that Glenmark's exclusive rights to develop, commercialise and distribute Crofelemer in 140 countries for treatment of diarrheal diseases includes the exclusive rights to distribute though relief agencies in these countries and an injunction prohibiting Napo from sharing confidential information concerning the manufacture of Crofelemer.