crofelemer

Action and Spectrum

Mechanism of action 

The exact mechanism of action crofelemer is not fully understood. Still, it is thought to work by inhibiting the transport of ions across the intestinal wall, which can help to reduce fluid loss and improve the consistency of the stool. 

It effectively treats diarrhea caused by various conditions, including HIV/AIDS, cancer, and inflammatory bowel disease. It is also used to treat diarrhea associated with certain medications, such as opioids. In addition, crofelemer is effective in reducing the symptoms of diarrhea in patients with cholera. 

Drug Interaction

Adverse Reaction

Frequency defined:  

1-10% 

Bronchitis 

Flatulence 

Nausea 

Arthralgia 

Nasopharyngitis 

Hemorrhoids 

Anxiety 

Abdominal distention 

Upper respiratory tract infections 

Cough 

Increased bilirubin 

Back pain 

Urinary tract infection 

Musculoskeletal pain 

Giardiasis 

Increased ALT 

Black Box Warning

Contraindication / Caution

Contraindications 

None 

Caution 

• Interactions with other medications: It may interact with other medications, particularly those metabolized by the cytochrome P450 enzyme system. Patients should inform their healthcare provider about their medications before starting crofelemer 
• Pregnancy and breastfeeding: There is currently not enough information available to determine the safety of crofelemer during pregnancy and breastfeeding. It is recommended that women who are pregnant or breastfeeding should avoid using crofelemer until more is known about its safety in these populations 
• Diarrhea associated with Clostridium difficile infection: It should not be used in patients with diarrhea associated with Clostridium difficile infection as it may worsen the condition. 
• Hypersensitivity: It should be avoided in patients with known hypersensitivity to the medication or its components 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: It is recommended that women who are pregnant or breastfeeding should avoid using crofelemer until more is known about its safety in these populations  

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology 

It is a selective inhibitor of the chloride channel protein CFTR. It acts on the apical membrane of the enterocytes to inhibit Cl- secretion and reduce the net secretion of water into the intestinal lumen. This results in a reduction of diarrhoea by slowing down intestinal transit and increasing the consistency of the stool. 

Pharmacodynamics 

It is a selective inhibitor of the chloride channel protein CFTR. It acts on the apical membrane of the enterocytes to inhibit Cl- secretion, which reduces the net secretion of water into the intestinal lumen. This leads to a reduction of diarrhoea by slowing down intestinal transit and increasing the consistency of the stool. 

Crofelemer does not affect the secretion of other ions, such as sodium or potassium; it specifically targets chloride ions. This specificity allows crofelemer to have a targeted effect on diarrhoea without causing other adverse effects. 

Pharmacokinetics 

The body does not easily absorb the drug (minimal absorption), its distribution within the body has not been determined, it does not appear to be metabolized (broken down) by the body, and its elimination from the body has not been identified. This suggests that the drug may stay in the body for a long time and may not be eliminated easily. It’s important to note that this information may change depending on the specific compound or drug being studied. 

Adminstartion

Administration 

The medication can be taken with or without food, which means that it does not interact with food and can be taken at any time, regardless of meals. It also instructs to swallow the tablet whole, which is essential because crushing, chewing, or dissolving the tablet can alter how the medication is released and absorbed by the body, potentially affecting its effectiveness or causing side effects 

Patient Information Leaflet

Patient information leaflet 

Generic Name: crofelemer 

Pronounced: [ kroe-FEL-e-mer ] 

Why do we use crofelemer? 

It is a medication used to treat diarrhea, specifically non-infectious diarrhea caused by certain medications in adult patients with HIV/AIDS who receive antiretroviral therapy. It works by slowing down the intestines’ movement, which helps reduce the frequency and urgency of bowel movements and also helps to prevent fluid loss