Crofelemer

Crofelemer
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Rabin Bista, M.B.B.S. [2]

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Overview

Crofelemer is a anti-diarrheal that is FDA approved for the treatment of non-infectious diarrhea in adult patients with HIV/AIDS. Common adverse reactions include upper respiratory tract infection, bronchitis, cough, flatulence and increased bilirubin.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

FULYZAQ is indicated for symptomatic relief of non-infectious diarrhea in patients with HIV/AIDS on anti-retroviral therapy.

Dosage

The recommended dose of FULYZAQ is one 125 mg delayed-release tablet taken orally two times a day, with or without food. FULYZAQ tablets should not be crushed or chewed. Tablets should be swallowed whole.

3 DOSAGE FORMS AND STRENGTHS FULYZAQ is a white, oval, enteric-coated 125 mg delayed-release tablet printed on one side with 125SLXP.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Crofelemer in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Crofelemer in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

The safety and effectiveness of FULYZAQ have not been established in pediatric patients less than 18 years of age.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Crofelemer in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Crofelemer in pediatric patients.

Contraindications

• None

Warnings

• Risks of Treatment in Patients with Infectious Diarrhea

If infectious etiologies are not considered, and FULYZAQ is initiated based on a presumptive diagnosis of non-infectious diarrhea, then there is a risk that patients with infectious etiologies will not receive the appropriate treatments, and their disease may worsen. Before starting FULYZAQ, rule out infectious etiologies of diarrhea. FULYZAQ is not indicated for the treatment of infectious diarrhea.

Adverse Reactions

Clinical Trials Experience

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

A total of 696 HIV-positive patients in three placebo-controlled trials received FULYZAQ for a mean duration of 78 days. Of the total population across the three trials, 229 patients received a dose of 125 mg twice a day for a mean duration of 141 days, 69 patients received a dose of 250 mg twice a day for a mean duration of 139 days, 102 patients received a dose of 250 mg four times a day for a mean duration of 14 days, 54 patients received a dose of 500 mg twice a day for a mean duration of 146 days, and 242 patients received a dose of 500 mg four times a day for a mean duration of 14 days.

Adverse reactions for FULYZAQ that occurred in at least 2% of patients and at a higher incidence than placebo are provided in Table 1.

Adverse reactions that occurred in between 1% and 2% of patients taking a 250 mg daily dose of FULYZAQ were abdominal pain, acne, increased aspartate aminotransferase, increased conjugated bilirubin, increased unconjugated blood bilirubin, constipation, depression, dermatitis, dizziness, dry mouth, dyspepsia, gastroenteritis, herpes zoster, nephrolithiasis, pain in extremity, pollakiuria, procedural pain, seasonal allergy, sinusitis and decreased white blood cell count.

Adverse reactions were similar in patients who received doses greater than 250 mg daily.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Crofelemer in the drug label.

Body as a Whole

Cardiovascular

Digestive

Endocrine

Hematologic and Lymphatic

Metabolic and Nutritional

Musculoskeletal

Neurologic

Respiratory

Skin and Hypersensitivy Reactions

Special Senses

Urogenital

Miscellaneous

Drug Interactions

Drug Interaction Potential

In vitro studies have shown that crofelemer has the potential to inhibit cytochrome P450 isoenzyme 3A and transporters MRP2 and OATP1A2 at concentrations expected in the gut. Due to the minimal absorption of crofelemer, it is unlikely to inhibit cytochrome P450 isoenzymes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and CYP3A4 systemically [see Clinical Pharmacology (12.3)].

7.2 Nelfinavir, Zidovudine, and Lamivudine

FULYZAQ administration did not have a clinically relevant interaction with nelfinavir, zidovudine, or lamivudine in a drug-drug interaction trial.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): 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.

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Crofelemer in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Crofelemer during labor and delivery.

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 FULYZAQ, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

• The safety and effectiveness of FULYZAQ have not been established in pediatric patients less than 18 years of age.

Geriatic Use

• Clinical studies with crofelemer did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently than younger patients.

Gender

There is no FDA guidance on the use of Crofelemer with respect to specific gender populations.

Race

There is no FDA guidance on the use of Crofelemer with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Crofelemer in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Crofelemer in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Crofelemer in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Crofelemer in patients who are immunocompromised.

CD4 Count and HIV Viral Load

No dose modifications are recommended with respect to CD4 cell count and HIV viral load, based on the findings in subgroups of patients defined by CD4 cell count and HIV viral load.

The safety profile of crofelemer was similar in patients with baseline CD4 cell count less than 404 cells/μL (lower limit of normal range) (N=388) and patients with baseline CD4 cell counts greater than or equal to 404 cells/μL (N=289).

The safety profile of crofelemer was similar in patients with baseline HIV viral loads less than 400 copies/mL (N = 412) and patients with baseline HIV viral loads greater than or equal to 400 copies/mL (N = 278).

Administration and Monitoring

Administration

• Oral

Monitoring

There is limited information regarding Monitoring of Crofelemer in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Crofelemer in the drug label.

Overdosage

• There has been no reported experience with overdosage of crofelemer.

Pharmacology

There is limited information regarding Crofelemer Pharmacology in the drug label.

Mechanism of Action

Structure

File:Crofelemer01.png

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Crofelemer in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Crofelemer in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Crofelemer in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Crofelemer in the drug label.

How Supplied

Storage

There is limited information regarding Crofelemer Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Crofelemer in the drug label.

Precautions with Alcohol

• Alcohol-Crofelemer interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• ®

Look-Alike Drug Names

• A® — B®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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