FDA-filed SPL labeling · retrieved through openFDA

Crofelemer

Crofelemer is an anti-diarrheal medicine used to relieve non-infectious diarrhea in adults with HIV/AIDS who are on antiretroviral therapy.

Brand names FulyzaqMytesiCanalevia
Drug class Antidiarrheal
Rx Form 1 Route Oral
Dr. Brian Staiger, PharmD, BCPS
Reviewed by Last reviewed Jul 10, 2026
🧬 Where this information comes from Click to expand

The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 1 clinical label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →

At a glance
Linked label effectiveJul 31, 2026
AvailabilityRx
Earliest approval/marketing year 2012
FDA-listed product records 4
Boxed warningNone found in compared labels
How we combine label and product data →
No current FDA shortage listed · checked Sep 22, 2026
Crofelemer at a glance The quick version — the full detail is in the Patient Information Guide below.
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HelloPharmacist Editorial Team Bottom Line
Crofelemer (Mytesi) is a targeted, locally acting anti-diarrheal for adults with HIV/AIDS on antiretroviral therapy whose diarrhea is not caused by an infection. It works in the gut with minimal absorption into the rest of the body. Take it twice a day as directed, swallow the tablet whole, and check in with your doctor if symptoms don't improve.

📖 Crofelemer: Patient Information Guide

A plain-language walkthrough of Crofelemer — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.

🎯What it's used for

Crofelemer is approved for one specific use, tied to the brand Mytesi:

  • Mytesi (oral tablet): Symptomatic relief of non-infectious diarrhea in adults with HIV/AIDS who are on antiretroviral therapy.
⚙️How it works

Crofelemer blocks two types of chloride ion channels — the CFTR channel and the calcium-activated chloride channel (CaCC) — on the surface of intestinal cells. These channels normally regulate how much chloride and water move into the gut. When they are overactive, large amounts of fluid pour into the intestine, causing watery diarrhea. By blocking these channels, crofelemer reduces that excess fluid secretion and normalizes stool consistency.

Importantly, crofelemer is barely absorbed into the bloodstream after swallowing — it acts almost entirely within the gut itself. This means it does not significantly affect the rest of the body or most other medications you may be taking.

💊How it's taken

Mytesi is taken as an oral tablet twice a day. It can be taken with or without food, so you can fit it into your routine however works best for you.

  • Swallow the tablet whole — never crush or chew it.
  • Follow your prescriber's schedule exactly.
  • No specific dose adjustments are recommended based on CD4 cell count or HIV viral load.
🤒Side effects — in detail

The most commonly reported side effects with Mytesi (occurring in at least 2% of patients in clinical trials) include:

  • Upper respiratory tract infection (cold-like symptoms)
  • Bronchitis (inflammation of the airways)
  • Cough
  • Flatulence (gas)
  • Increased bilirubin (a liver-related marker in the blood)
  • Nausea
  • Back pain
  • Joint pain (arthralgia)
  • Urinary tract infection
  • Nasopharyngitis (inflammation of the nose and throat)

Contact your doctor if diarrhea worsens or does not improve, or if you notice any new or concerning symptoms after starting this medicine.

⚠️Warnings & precautions
  • Do not use for infectious diarrhea: Mytesi is only for diarrhea that is not caused by an infection. Your doctor must rule out infectious causes first. Using Mytesi when an infection is present could delay proper treatment and make the infection worse.
  • Pediatric use: Safety and effectiveness in children have not been established — Mytesi is approved for adults only.
  • Older adults: There is limited data on patients aged 65 and over; discuss any concerns with your prescriber.
🔀What it interacts with

Because crofelemer is minimally absorbed into the bloodstream, it has a low potential for systemic drug interactions. Studies have looked at a few specific combinations:

  • Nelfinavir and zidovudine (HIV medications): No clinically meaningful interaction was found with Mytesi.
  • Lamivudine (HIV medication): A small decrease in lamivudine exposure was seen in studies, but it was not considered clinically important.
  • Gut-level enzyme effects: Crofelemer may affect certain transporters in the intestine, but due to its minimal absorption, it is unlikely to interact with most drugs processed by the liver.

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

📋Before taking it
  • Infectious diarrhea must be ruled out by your doctor before you start Mytesi — using it for the wrong type of diarrhea can cause harm.
  • Pregnancy: Crofelemer is minimally absorbed, so exposure to the fetus is not expected. Still, tell your doctor if you are pregnant or planning to become pregnant.
  • Breastfeeding: Women with HIV should not breastfeed regardless of medication use, to avoid transmitting HIV to the baby. Do not breastfeed while taking Mytesi.
  • Children: Not approved for pediatric patients — safety and effectiveness are not established.
  • Older adults (65+): Limited clinical data are available for this age group; your prescriber will weigh the risks and benefits.
  • Low CD4 counts or high viral loads: No dose changes are needed based on these values, and the safety profile appeared similar regardless of CD4 count or viral load in clinical studies.
📡Pharmacodynamics — effects in the body

In clinical studies, crofelemer reduced stool chloride concentrations compared to placebo — consistent with its action of blocking chloride secretion in the gut. At a dose ten times the maximum recommended amount, crofelemer did not cause any clinically meaningful prolongation of the QTc interval (an electrical measurement of heart rhythm), suggesting it does not pose a significant cardiac risk at therapeutic doses.

🔬Pharmacokinetics — how your body processes it

Crofelemer is very poorly absorbed after swallowing — blood concentrations remain below measurable levels in both healthy adults and people with HIV. Because so little enters the bloodstream, standard measurements like half-life and peak concentration cannot be calculated. Food (including a high-fat meal) does not meaningfully increase systemic absorption. This minimal absorption also means crofelemer is unlikely to interact with liver enzymes that process most other medications.

📦How to store it

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

📄 Written from Crofelemer’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →

17

Supplements & herbs that interact with Crofelemer

17 supplements and herbal products have documented interactions with Crofelemer in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.

Severity mix
  • Major · 1
  • Moderate · 7
  • Minor · 9
Every supplement checked against Crofelemer — ranked by severity The full interaction hub: 1 major · 7 moderate · 9 minor · every one linked to its full report. Check Crofelemer against your exact supplements

Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.

🩺 Pharmacist Counseling Corner

Quick, plain-English answers to the questions patients ask most about Crofelemer — the kind of thing our pharmacy team would talk through with you at the counter.

What exactly is Mytesi for — can I take it for any stomach bug?
No — Mytesi is specifically for diarrhea that is NOT caused by an infection, in adults with HIV/AIDS who are on antiretroviral therapy. If your diarrhea is from a virus, bacteria, or parasite, Mytesi won't help and could actually delay you getting the right treatment. Your doctor will make sure an infection has been ruled out before starting you on it.
Will this medicine interfere with my HIV medications?
Based on studies, Mytesi did not have a meaningful interaction with common HIV drugs like nelfinavir or zidovudine. A small reduction in lamivudine levels was seen, but it wasn't considered clinically important. Because Mytesi is barely absorbed into your bloodstream, it generally has a low risk of interfering with other medications — but always keep your doctor and pharmacist updated on everything you take.
How do I take this tablet — does it matter if I have food?
You take Mytesi by mouth twice a day, and you can take it with or without food — whichever fits your routine. The most important thing is to swallow the tablet whole. Don't crush or chew it, because the tablet is designed to release the medicine in a specific way.
What side effects should I expect, and when should I call my doctor?
The most common side effects seen in studies include cold-like symptoms, cough, bronchitis, gas, mild nausea, back pain, and joint pain. Most people tolerate it reasonably well. Call your doctor if your diarrhea doesn't improve or gets worse — that can be a sign the cause wasn't properly identified and you may need a different treatment.
Can I take this if I'm pregnant or breastfeeding?
Because Mytesi is barely absorbed into your body, very little would reach a developing baby during pregnancy. That said, always tell your doctor you're pregnant so they can weigh everything carefully. As for breastfeeding — women with HIV are advised not to breastfeed at all, to avoid passing the virus to the baby. This applies regardless of which medications you're taking.
Is this medicine safe for my child or teenager with HIV?
Mytesi has only been studied and approved in adults. Its safety and effectiveness in children and teenagers have not been established, so it should not be used in pediatric patients unless a doctor specifically advises otherwise.
Is Crofelemer available over the counter?
Crofelemer is dispensed by prescription according to its FDA labeling, so it isn't sold over the counter. Your prescriber and pharmacist will determine if it's appropriate for you.
When was Crofelemer first available?
Crofelemer has been available in the United States since at least 2012, based on FDA approval history (Drugs@FDA) and product marketing records.
Who makes Crofelemer?
Crofelemer is supplied by 2 manufacturers listed in the FDA NDC Directory, including Napo Pharmaceuticals, Inc., Indena SpA.

💬 Answers drafted from Crofelemer’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →

🧰 Keep exploring

💊 How Crofelemer comes

Crofelemer is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.

Tablet

By mouth
Brands Mytesi
How this form is used
What it may be used for
  • Mytesi tablets are used to relieve non-infectious diarrhea in adults with HIV/AIDS who are on antiretroviral therapy.
Important instructions
  • Mytesi tablets are taken by mouth twice a day.
  • Mytesi can be taken with or without food.
  • Swallow Mytesi tablets whole — do not crush or chew them.
  • Before starting Mytesi, your doctor should confirm your diarrhea is not caused by an infection.
Available strengths 1 strength
3 FDA-listed product records

📊 Crofelemer across the U.S. market

How Crofelemer appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.

1
Dose forms
2
Manufacturers
1
Brand names
4
FDA-listed product records
2012
First marketed

Also listed with the FDA, not a patient dose form: Powder (1) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.

Napo Pharmaceuticals, Inc.75%
Indena SpA25%

Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.

📈 How widely Crofelemer is used

A general measure of how commonly Crofelemer is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.

Think of this as a proxy for how widely Crofelemer is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.

301
Medicaid prescriptions filled (Q1–Q4 2025)
$771,294 gross Medicaid reimbursement (before mandatory rebates — net cost is lower)

How commonly is Crofelemer prescribed? Of the 1,596 medications we measure, Crofelemer ranks #1,418 by Medicaid prescriptions — more than 11% of them.

Where Crofelemer ranks among the drugs we measure · Q1–Q4 2025 · neighbors ±5

Utilization by Crofelemer product

Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.

crofelemer 125 MG Delayed Release Oral Tablet

301 Medicaid prescriptions (Q1–Q4 2025) 100% of Crofelemer prescriptions shown $771,294 gross reimbursement (before rebates) ≈ $2,562 per prescription (gross)

Summed across the 1 of 1 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1364454

Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.

Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Crofelemer, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 1 of 1 listed Crofelemer NDCs with Medicaid activity.

🔍 Compare Crofelemer products

A representative set of FDA-listed product records for Crofelemer — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)

Strength Route Manufacturer / Labeler Category Details
💊Tablet
125 mg Oral Napo Pharmaceuticals, Inc. × 3 listings NDA View NDC →
💊Bulk drug substance
1 g/g Indena SpA BULK INGREDIENT View NDC →

Showing 4 of 4 products — FDA National Drug Code Directory. See every product, package size and price: browse all 4 Crofelemer NDCs →

RxNorm Concept Web — From Ingredient to Every Form and Strength

This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.

Ingredient (IN) Crofelemer RxCUI 1364449 1 dose form · 1 strength
  1. Dose form (SCDF) Delayed Release Oral Tablet RxCUI 1364453 No current FDA listing
    Clinical drug / strength (SCD) 125 MG RxCUI 1364454

Look up RxCUI 1364449 in the RxCUI Atlas →

RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.

🏷️ Sold under these brand names

Fulyzaq Mytesi Canalevia

🏭 Manufacturers & labelers

Napo Pharmaceuticals, Inc. 3 Indena SpA 1

RxNorm drug class

Crofelemer belongs to the Antidiarrheal class.

Pharmacologic class Antidiarrheal
Drug family (ATC) Other antidiarrheals

Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.

🔬 Where this comes from

Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.

📄
FDA-filed drug labels (SPL) Uses, dosing, warnings & side effects from SPL records retrieved through openFDA; the linked representative set can be verified on DailyMed. ✓ Linked label effective Jul 31, 2026
🏭
Forms, brands & labelersAggregated from ingredient-matched FDA National Drug Code Directory product records for Crofelemer.
📈
Real-world reportsThe FDA Adverse Event Reporting System (FAERS), served through openFDA.
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Recalls & shortagesopenFDA drug-enforcement reports and the FDA drug-shortage database.
🧾 Clinical label set — FDA-filed SPL labels retained for Crofelemer after exact ingredient or ingredient-combination matching and applicable route/form matching
Clinical labels in scope
1
NDC products indexed
4
Distinct labelers/manufacturers represented
2
Linked representative label
Napo Pharmaceuticals, Inc.
Linked label effective
Jul 31, 2026
Composite sections available
20
Linked SPL Set ID
45584fba-8081-4cd1-a21e-3ea8237f62ff
Linked SPL Document ID
f9b7d7cd-31ef-4030-ae3f-10ab635d0758
Open the linked representative label on DailyMed ↗

How we combine label and product data

HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 1 FDA-filed SPL label set within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.

For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Napo Pharmaceuticals, Inc. is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.

This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.