Crofelemer

Crofelemer is an Anti-secretory belonging to an Antidiarrheal agent.

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.

The absorption of Crofelemer is minimal and Crofelemer concentrations in plasma are below the level of quantitation (50 ng/mL). The distribution of Crofelemer has not been determined. No metabolites of Crofelemer have been identified in healthy subjects or patients in clinical trials.

Crofelemer shows side effects like sneezing, or cough, tiredness, fever, chills, cough with mucus (sputum), or chest tightness, gas, nausea, swelling of the abdomen, hemorrhoids, back or joint pain, difficult, painful, or frequent urination, urine that is cloudy or discolored, back pain or pressure in the lower abdomen, anxiety.

Crofelemer is available in the form of Oral tablets.

Crofelemer is available in India, US, Russia, China, France, Italy, Singapore, and Australia.

Crofelemer belongs to the Antidiarrheal agent acts as an Anti-secretory.

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 inhibits both channels prevents water loss from diarrhea by inhibiting chloride secretion.

The Onset and duration of action of Crofelemer is not clinically established.

Crofelemer is used to control some types of diarrheas in patients with human immunodeficiency virus (HIV) infection who are being treated with certain medications. Crofelemer is in a class of medications called botanicals. It works by decreasing the amount of fluid that flows into the bowel which can cause diarrhea.

Crofelemer is approved for use in the following clinical indications

• Diarrhea, HIV/AIDS-related

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.

• Diarrhea, HIV/AIDS-related

Oral: 125 mg twice daily.

Crofelemer is available in various strengths as 125mg.

Crofelemer is available in the form of an Oral Tablet.

• HIV/AIDS

CD4 cell count and viral load do not have a clinical impact on Crofelemer treatment; no adjustments are necessary based on CD4 cell count or viral load.

• Infectious diarrhea

Crofelemer is not indicated for infectious diarrhea; there is a risk of inadequate or delayed treatment if used when infectious diarrhea is present. Rule out infectious causes for diarrhea prior to initiating treatment.

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 from Crofelemer, a decision should be made whether to discontinue nursing or to discontinue the drug, considering the importance of the drug to the mother.

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant the use of the drug in pregnant women despite potential risks. Use only if clearly needed.

Common

● Sneezing, or Cough, Tiredness, Fever, Chills, Cough with Mucus (sputum), or Chest tightness, Gas, Nausea, Swelling of the Abdomen, Hemorrhoids, Back or Joint pain, Difficult, Painful, or Frequent urination, Urine that is cloudy or discolored, Back pain or Pressure in the lower abdomen, Anxiety.

The common side effects of Crofelemer include the following

Common side effects

• Pregnancy

Pregnancy Category C

Reproduction studies performed with Crofelemer in rats at oral doses up to 177 times the recommended daily human dose of 4.2 mg/kg revealed no evidence of impaired fertility or harm to the fetus. In pregnant rabbits, Crofelemer at an oral dose of about 96 times the recommended daily human dose of 4.2 mg/kg, caused abortions and resorptions of fetuses. However, it is not clear whether these effects are related to the maternal toxicity observed. A pre-and postnatal development study performed with Crofelemer in rats at oral doses of up to 177 times the recommended daily human dose of 4.2 mg/kg revealed no evidence of adverse pre- and postnatal effects in offspring. There are, however, no adequate, well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug 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 from Crofelemer, a decision should be made whether to discontinue nursing or to discontinue the drug, considering the importance of the drug to the mother.

• Pediatric Use

The safety and effectiveness of Crofelemer have not been established in pediatric patients under 18 years of age.

• Geriatric Use

Clinical studies with Crofelemer did not include enough patients aged 65 and over to determine whether they respond differently than younger patients.

Pharmacodynamic

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.

Pharmacokinetics

• Absorption

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

• Distribution

The distribution of Crofelemer has not been determined.

• Metabolism and Excretion

No metabolites of Crofelemer have been identified in healthy subjects or patients in clinical trials.

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202292s000lbl.pdf
• https://medlineplus.gov/druginfo/meds/a613016.html
• https://reference.medscape.com/drug/mytesi-crofelemer-999806
• https://www.drugs.com/dosage/crofelemer.html
• https://go.drugbank.com/drugs/DB04941
• https://www.uptodate.com/contents/crofelemer-drug-information?search=crofelemer&source=panel_search_result&selectedTitle=1~3&usage_type=panel&kp_tab=drug_general&display_rank=1
• https://www.rxlist.com/fulyzaq-drug.htm#clinpharm