Crofelemer

Crofelemer is a prescription medication indicated for the treatment of noninfectious diarrhea in patients with HIV/AIDS on antiretroviral therapy.

• Crofelemer is available under the following different brand names: Mytesi

Common side effects of Crofelemer include:

• upper respiratory tract infection
• bronchitis
• cough
• gas
• increased bilirubin
• nausea
• back pain
• joint pain
• urinary tract infection
• runny or stuffy nose
• musculoskeletal pain
• hemorrhoids
• giardiasis
• anxiety
• increased alanine aminotransferase
• abdominal bloating

Serious side effects of Crofelemer include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• dark urine, jaundice (yellowing of the skin or eyes)
• wheezing, chest tightness, trouble breathing
• worsening diarrhea

Rare side effects of Crofelemer include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet, delayed-release

• 125 mg

Noninfectious diarrhea

Adult dosage

• 125 mg orally two times a day

Dosage Considerations – Should be Given as Follows:

• See "Dosages"

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Crofelemer has severe interactions with no other drugs
• Crofelemer has serious interactions with the following drugs:
  • lonafarnib
  • sulbactam/durlobactam
• Crofelemer has moderate interactions with at least 177 other drugs
• Crofelemer has minor interactions with no other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See "What Are Side Effects Associated with Using Crofelemer?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Crofelemer?"

Cautions

• Not indicated for infectious diarrhea; before initiating, rule out infectious etiologies of diarrhea
• If initiated based on a presumptive diagnosis of noninfectious diarrhea, then there is a risk that patients with infectious etiologies will not receive the appropriate treatments, and their disease may worsen
• In vitro studies have shown that crofelemer has the potential to inhibit CYP3A4 and transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed

Pregnancy and Lactation

• The drug is minimally absorbed systemically by the oral route of administration and maternal use is not expected to result in fetal exposure to the drug
• Lactation
  • The CDC recommend that mothers infected with HIV-1 should not breastfeed infants to avoid risking postnatal transmission of HIV-1
• There are no data on the presence of drugs in human milk, its effects on the breastfed infant, or milk production; because of the potential for HIV transmission and adverse effects on breastfed infants, instruct mothers not to breastfeed if they are receiving therapy