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What is Crofelemer?[edit | edit source]

  • Crofelemer (Mytesi) is an anti-diarrheal used to treat noninfectious diarrhea in HIV positive patients on antiretroviral therapy.
  • Crofelemer is an antidiarrheal agent derived from the red sap of the South American plant Croton lechleri.

Crofelemer skeletal

What are the uses of this medicine?[edit | edit source]

How does this medicine work?[edit | edit source]

  • Crofelemer (kroe fel' e mer) is a botanical antidiarrheal agent that is used to treat noninfectious diarrhea in HIV seropositive patients taking antiretroviral medications.
  • Crofelemer is derived from the red sap of the South American plant Croton lechleri, which has been used for centuries to treat diarrheal illness.
  • The active antidiarrheal product in crofelemer appears to be a large macromolecular, oligomeric proanthocyanidin which has been shown to decrease chloride secretion in the intestine by inhibition of the cystic fibrosis transmembrane conductance regulator (CFTR), as well as calcium-activated chloride channels.
  • In large clinical trials, daily therapy with crofelemer was found to decrease watery bowel movements and improve stool consistency in patients with HIV infection receiving antiretroviral therapy, and who had persistent diarrhea that could not be attributed to an infectious cause.

Who Should Not Use this medicine ?[edit | edit source]

  • This medicine have no usage limitations.

What drug interactions can this medicine cause?[edit | edit source]

Is this medicine FDA approved?[edit | edit source]

  • Crofelemer was approved for use in the United States in 2012, the first herbal medication to be approved for a specific medical use and first agent approved for therapy of noninfectious diarrhea in HIV positive patients.

How should this medicine be used?[edit | edit source]

  • Before starting Mytesi, rule out infectious etiologies of diarrhea.

Recommended dosage:

  • The recommended adult dosage is 125 mg taken orally twice a day, with or without food.


  • Do not crush or chew Mytesi tablets.
  • Swallow whole.

What are the dosage forms and brand names of this medicine?[edit | edit source]

This medicine is available in fallowing doasage form:

  • As Delayed-Release Tablets: 125 mg

This medicine is available in fallowing brand namesː

  • Mytesi

What side effects can this medication cause?[edit | edit source]

The most common side effects of this medicine include:

What special precautions should I follow?[edit | edit source]

  • Before starting Mytesi, rule out infectious etiologies of diarrhea. Mytesi is not indicated for the treatment of infectious diarrhea.
  • Instruct patients that Mytesi tablets may be taken with or without food.
  • Instruct patients to swallow Mytesi tablets whole and not to crush or chew the tablets.

What to do in case of emergency/overdose?[edit | edit source]

  • In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

Can this medicine be used in pregnancy?[edit | edit source]

  • Crofelemer is minimally absorbed systemically by the oral route of administration and maternal use is not expected to result in fetal exposure to the drug

Can this medicine be used in children?[edit | edit source]

  • The safety and effectiveness of Mytesi have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?[edit | edit source]

Active ingredient: CROFELEMER

  • Inactive ingredients:


Who manufactures and distributes this medicine?[edit | edit source]

  • Manufactured by Patheon, Inc. for

Napo Pharmaceuticals, Inc., San Francisco, CA

What should I know about storage and disposal of this medication?[edit | edit source]

  • Store at 20°C-25°C (68°F-77°F); excursions permitted between 15°C-30°C (59°F-86°F).

Antidiarrheal agents[edit source]

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents


Cannabinoid Receptor Agonists

Serotonin 5-HT3 Receptor Antagonists

Substance P/Neurokinin 1 Receptor Antagonists


Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

Immunosuppressive Agents

Tumor Necrosis Factor Antagonists


Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod


Crofelemer Resources
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