Crofelemer (Oral)

A naturally-occurring botanical agent derived from the sap of the Croton lechleri plant, Crofelemer is particularly useful in treating non-infectious diarrhea.


Crofelemer is extracted from the red sap of the Croton lechleri, a plant which is indigenous to the South Americas. It is typically used for the treatment of non-infectious diarrhea associated with the use of certain anti-HIV medications like protease inhibitors and nucleoside analog reverse transcriptase inhibitors. It can also be used to treat diarrhea in children and patients with irritable bowel syndrome.

A purified form of oligomeric proanthocyanidin, Crofelemer alleviates the symptoms of diarrhea but is not suitable for treating the causes of infectious versions of the condition, such as those caused by the infection of the digestive system by parasites, viruses or bacteria.

This medicine was initially developed by Napo Pharmaceuticals and is licensed for use in over 140 countries. It was approved by the US Food & Drug Administration (FDA) in 2012.

Crofelemer is taken orally and functions by blocking two unrelated chloride channels within the gut, notably the calcium-activated chloride channel anoctamin 1 (with an inhibition of over 90 per cent) and the cystic fibrosis transmembrane conductance regulator (CFTR) with an in-vitro inhibition of approximately 60%. As a result of this channel inhibition, much fewer chloride ions are excreted into the gut, and this, in turn, results in a decreased excretion of sodium and water, which improves the consistency of stools and reduces the propensity for diarrhea.

Type of medicine

  • Diarrhea inhibitor

Conditions treated

  • Non-infectious diarrhea

Side effects

Like many medications, Crofelemer may cause some unwanted side effects along with its desired effects. The most commonly-reported effects by patients undergoing therapy with this medication are as follows: chills, cough, nasal congestion, body aches and pains, difficulty breathing, runny nose, sneezing, fever, headache, ear congestion, sore throat, unusual weakness or tiredness.

As the patient continues to undergo treatment with this medicine as prescribed by a doctor, many (if not all) of the previously mentioned side effects should lessen. If side effects continue to affect the patient over a prolonged period, he or she is advised to contact their doctor or healthcare provider.

Other side effects, which are experienced rarely (but often enough to warrant reporting) include the following: acidic or sour stomach, irritability, back pain, bladder pain, belching, loss of appetite, lower back or side pain, skin blemishes, bloody or cloud urine, muscular pain, bone pain, cracked/dry/scaly skin, difficulty moving, pain around the eyes/cheekbones, excess flatulence, difficulty sleeping, heartburn, indigestion, fear or nervousness, dry mouth, difficulty with bowel movements, a feeling of sadness or emptiness, and/or genital pain.

Patients who experience these rare symptoms are advised to contact their doctor, who may be able to advise on how to alleviate certain side effects usual natural or over the counter remedies for example, incidences of dry mouth can be alleviated by chewing sugar-free gum or regularly drinking ice cold water. In some instances, a doctor may advise discontinuing use of the Crofelemer and switching to an alternative drug.

While the majority of the previously mentioned symptoms are likely to cause mild discomfort only, patients who experience the following symptoms should contact their doctor or healthcare provider immediately: acute abdominal or stomach pain, bleeding after defecating, a feeling of bloatedness, pressure within the stomach, swelling or the stomach or abdomen, and/or uncomfortable swelling around the anus.


As with all drugs, it is imperative that patients only take Crofelemer as prescribed by a doctor. Patients should avoid taking any more of this medicine than recommended, either in terms of dose size or frequency. In addition to this, patients should cease taking Crofelemer if advised to by their doctor, even if they still have a supply of the medicine remaining.

Crofelemer can be taken with or without food. Tablets should not be crushed or chewed, and should instead be swallowed whole with a glass of water where possible. For non-infectious diarrhea in patients with HIV/AIDS who are receiving antiretroviral therapy, the recommended dose is 125mg, twice daily, taken orally.

Although the manufacturers of Crofelemer provide general dose instructions, it should be reiterated that these are mere recommendations which can be altered at the discretion of the patient's doctor. When determining the optimum dose, a doctor will take into account the height, weight, age, condition and general health of the patient.

Although the potential to overdose on Crofelemer is low in comparison to other drugs, patients who experience abdominal cramps, difficulty breathing, unconsciousness, seizures or loss of coordination should contact their local poison control center on 1800-222-1222 immediately, the emergency services on 911, or alternatively attend their local emergency room as soon as possible.


All drugs have the potential to interact with other chemicals and medication within the body, which can change the effects of each medicine. This could cause one medicine to become ineffective at treating the condition it was prescribed for, or it could cause dangerous or potentially fatal reactions in the patient. Because of these possibilities, it is important for patients to keep a fully detailed list of all medicines they are currently being treated with. This extends to complementary medicines, over the counter remedies, vitamins, and herbal supplements as well as prescription medications.

There are no known drugs which interact with Crofelemer. However, this does not mean that no interactions exist - it merely means that there have been no conclusive studies into interactions with this medicine. Patients who feel they may have experienced an interaction are advised to inform their doctor, and to report their findings to the FDA if they so choose.


Before taking Crofelemer, the patient must be certain that the diarrhea they are experiencing is non-infectious. Patients who are vomiting or show other signs of infection may be suffering from a gastrointestinal infection, and may need treatment with antibiotics or other medicines. Patients with infectious diarrhea are also at risk of deyhydration, and may require a larger intake of fluids and salts to counteract the effects of the condition.

To get the most from this medication, patients must take it regularly. To facilitate a regular dosing schedule, patients are advised to take Crofelemer at the same times every day. It may also take a number of months before the patient begins to feel the full benefit of this medication. Patients should contact their doctor if they do not feel any benefit, or notice that their condition has worsened.

Patients who are pregnant or intending on becoming pregnant soon should use this medicine only if the benefits clearly outweigh the risks, and should discuss this with their doctor prior to beginning treatment.

In some instances, a doctor may recommend dietary changes in conjunction with Crofelemer use, such as greater intake of fiber. Increased fiber intake is a great way of naturally achieving firmer stools, and while not a sufficient treatment for non-infectious diarrhea on its own, can contribute to an overall greater sense of health and wellbeing.

It is currently unknown whether this medication passes into breast milk, although in theory, it could cause constipation-like conditions. Breastfeeding mothers are therefore advised to consult their doctor or healthcare provider, who may recommend stopping breastfeeding while undergoing treatment with this medication.


Crofelemer should be stored in the package it was supplied in, at room temperature. The manufacturer recommends that this medication is kept away from sources of moisture and heat it is therefore unsuitable for storage in a bathroom cabinet, and should instead be kept in a dedicated medicine cabinet where possible. Like all medicines, it should be kept away from children and pets.

This medicine should be disposed of in a hygienic and safe manner. It must not be poured down a drain or flushed down a toilet. A local pharmacy or waste disposal company will be able to provide patients with advice on how best to dispose of unwanted, unused or expired medications, and many pharmacies will even offer free Ĺ“take-back programs, where they will dispose of or recycle medicines which would otherwise have been discarded.


Crofelemer is a greatly beneficial drug, however, it can pose a risk to patients who fail to communicate effectively with their healthcare providers. As a treatment designed to alleviate symptoms of non-infectious diarrhea caused by antiretroviral medicines, Crofelemer helps to firm up stools and prevent uncontrollable bowel movements. However, it can also cause several side effects which can impair the patient's day-to-day functioning.

Although Crofelemer is unlikely to interact with other medications, patients should be upfront with their doctor regarding their medical history, current health conditions and medication regimen, to rule out any potentially harmful issues.

When taken correctly, Crofelemer is effective in stopping the symptoms of diarrhea which may have previously been untreatable. In many instances, this provides patients with the means to live their lives with much more confidence and freedom. To achieve these results, patients are advised to work together to ascertain the optimum dosage and frequency of use.