Crofelemer

Crofelemer Uses, Dosage, Side Effects, Food Interaction and all others data.

Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree Croton lechleri. It is marketed under the brand name Fulyzaq and indicated for the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy.

Crofelemer is an inhibitor of secretory diarrhea via inhibition of the CFTR chloride transporter. Crofelemer is not an antimicrobial, and therefore does not drive the emergence of resistance; it does not inhibit motility, and therefore does not cause constipation or rebound diarrhea; and it is not systemically absorbed, reducing the potential for adverse drug interactions and toxicity.

Table Of contents

• Crofelemer
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	Crofelemer
Availability	Prescription only
Generic	Crofelemer
Crofelemer Other Names	Crofelemer
Related Drugs	loperamide, Lomotil, Imodium, neomycin, Pepto-Bismol, bismuth subsalicylate
Weight	125mg
Type	Oral delayed release tablet
Protein binding	Since crofelemer is not significantly absorbed, protein binding was not quantified.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Crofelemer is an antidiarrheal agent used for the symptomatic relief of drug-induced non-infectious diarrhea in adult patients with HIV/AIDS receiving antiretroviral therapy.

For the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy.

Crofelemer is also used to associated treatment for these conditions: Non-infectious Diarrhea

How Crofelemer works

Crofelemer is an inhibitor of the cystic fibrosis transmembrane regulator chloride channel (CFTR), as evidenced by its activity on cell cultures, single cell patch clamps, single CFTR channels, and elaboration of mouse intestinal fluid secretion. Crofelemer also inhibits calcium activated chloride channels (CaCC), which in combination with CFTR, are expressed on the luminal side of intestinal cells. Crofelemer inhibition of both of these channels prevents water loss from diarrhea by inhibiting chloride secretion.

Toxicity

The most common adverse effects are cough, flatulence, upper respiratory tract infection, bronchitis, and increased bilirubin.

Food Interaction

• Take with or without food.

Volume of Distribution

Since crofelemer is not significantly absorbed, volume of distribution was not quantified.

Elimination Route

The absorption of crofelemer is minimal and crofelemer concentrations in plasma are below the level of quantitation (50 ng/mL).

Half Life

Since crofelemer is not significantly absorbed, the half life was not determined.

Clearance

Since crofelemer is not significantly absorbed, clearance was not determined.

Elimination Route

Since crofelemer is not significantly absorbed, the route of elimination has not been identified.

Innovators Monograph

You find simplified version here Crofelemer