is normally [404:<400 copies/mL. 1 Specific Populations Pregnancy Category C. 1 Lactation Not known whether distributed into human milk. 1 Discontinue nursing or the drug. 1 Pediatric Use Safety and efficacy not established in pediatric patients> <18 years of age. 1 Geriatric Use Insufficient experience in patients 65 years of age to determine whether they respond differently than younger adults. 1 Common Adverse Effects Upper respiratory tract infection, bronchitis, cough, flatulence, increased bilirubin concentrations. 1 Interactions for Crofelemer Based on in vitro studies, potentially could inhibit CYP3A at concentrations expected in the gut. 1 Inhibition of CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, and 3A4 in the liver unlikely since systemic absorption is minimal following oral administration. 1 11 Does not induce CYP1A2, 2B6, or 3A. 11 Based on in vitro studies, potentially could inhibit multidrug resistance protein (MRP) 2 and organic anion transport protein (OATP) 1A2 at concentrations expected in the gut. 1 Specific Drugs Drug Interaction Comments HIV protease inhibitors (PIs) Nelfinavir: No effect on systemic exposure to nelfinavir 1 Nucleoside and nucleotide reverse transcriptase inhibitor antiretrovirals (NRTIs) Lamivudine: Decreased systemic exposure to lamivudine; not considered clinically important 1 Zidovudine: No effect on systemic exposure to zidovudine 1 Crofelemer Pharmacokinetics Absorption Bioavailability Acts locally in GI tract. 10 Minimal systemic absorption following oral administration in healthy or HIV-infected individuals. 1 10 11 AUC and peak plasma concentration not established because plasma concentrations generally undetectable following oral administration. 1 6 7 11 Food Administration with a high-fat meal in healthy individuals did not increase systemic exposure. 1 Distribution Distribution not determined. 1 Extent Not known whether distributed into human milk. 1 Elimination Metabolism Metabolites not identified in healthy or HIV-infected individuals. 1 Elimination Route Not identified in humans. 1 Half-life Not established because plasma concentrations generally undetectable following oral administration. 1 6 7 11 Stability Storage Oral Tablets 20 25 C (may be exposed to 15 30 C). 1 Actions A botanical drug product; 1 derived from red latex of Croton lechleri Müll. Arg, a tree found in western Amazonian region of South America. 1 2 3 4 5 Botanical raw material from the tree has been called dragon s blood (sangre de drago) or tree s blood (sangre de grado). 2 5 Oligomeric proanthocyanidin mixture consisting principally of catechin, epicatechin, gallocatechin, and epigallocatechin monomer units linked in a random sequence. 1 2 3 Exact mechanism of action in treatment of noninfectious diarrhea not fully elucidated; 6 7 8 appears to inhibit both cyclic adenosine-monophosphate (cAMP)-stimulated cystic fibrosis transmembrane conductance regulator (CFTR) chloride ion channel and calcium-activated chloride channel (CaCC) at luminal membrane of enterocytes. 1 2 3 4 8 CFTR chloride channel and CaCC regulate chloride and fluid secretion by intestinal epithelial cells. 1 6 7 Decreases chloride secretion and accompanying high volume water loss resulting in normalization of chloride and water flow in GI tract, decreased stool weight and frequency, and symptomatic relief of diarrhea. 1 2 6 7 8 Diarrhea in HIV-infected patients can be categorized as infectious (e.g., caused by opportunistic pathogens) or noninfectious (e.g., related to antiretroviral therapy, HIV enteropathy); 2 3 9 some noninfectious causes may involve secretory mechanisms. 2 3 7 9 Advice to Patients Advise patients that crofelemer may be administered without regard to meals. 1 Advise patients that crofelemer delayed-release tablets should be swallowed whole and not crushed or chewed. 1 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Crofelemer Routes Dosage Forms Strengths Brand Names Manufacturer Oral Tablets, delayed-release (enteric-coated) 125 mg Fulyzaq Salix AHFS DI Essentials. Copyright 2017, Selected Revisions January 2, 2014. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Salix Pharmaceuticals, Inc. Fulyzaq (crofelemer) delayed-release tablets prescribing information. Raleigh, NC; 2013 Feb. 2. Yeo QM, Crutchley R, Cottreau J et al. Crofelemer, a novel antisecretory agent approved for the treatment of HIV-associated diarrhea. Drugs Today (Barc) . 2013; 49:239-52. [PubMed 23616951] 3. Frampton JE. Crofelemer: A Review of its Use in the Management of Non-Infectious Diarrhoea in Adult Patients with HIV/AIDS on Antiretroviral Therapy. Drugs . 2013; 73:1121-9. [PubMed 23807722] 4. Tradtrantip L, Namkung W, Verkman AS. Crofelemer, an antisecretory antidiarrheal proanthocyanidin oligomer extracted from Croton lechleri, targets two distinct intestinal chloride channels. Mol Pharmacol . 2010; 77:69-78. [PubMed 19808995] 5. Food and Drug Administration. Center for Drug Evaluation and Research. Application number: 202292Orig1s000: Summary review. From FDA website. 6. Cottreau J, Tucker A, Crutchley R et al. Crofelemer for the treatment of secretory diarrhea. Expert Rev Gastroenterol Hepatol . 2012; 6:17-23. [PubMed 22149578] 7. Patel TS, Crutchley RD, Tucker AM et al. Crofelemer for the treatment of chronic diarrhea in patients living with HIV/AIDS. HIV AIDS (Auckl) . 2013; 5:153-62. [PubMed 23888120] 8. Crutchley RD, Miller J, Garey KW. Crofelemer, a novel agent for treatment of secretory diarrhea. Ann Pharmacother . 2010; 44:878-84. [PubMed 20388859] 9. MacArthur RD, DuPont HL. Etiology and pharmacologic management of noninfectious diarrhea in HIV-infected individuals in the highly active antiretroviral therapy era. Clin Infect Dis . 2012; 55:860-7. [PubMed 22700829] 10. Food and Drug Administration. Center for Drug Evaluation and Research. Application number: 202292Orig1s000: Medical review(s). From FDA website. 11. Food and Drug Administration. Center for Drug Evaluation and Research. Application number: 202292Orig1s000: Clinical pharmacology and biopharmaceutics review(s). From FDA website. Next Pregnancy Warnings Print this page Add to My Med List More about crofelemer Side Effects During Pregnancy Dosage Information Support Group En Español 0 Reviews Add your own review/rating Drug class: antidiarrheals Consumer resources Crofelemer Crofelemer (Advanced Reading) Professional resources Crofelemer (Wolters Kluwer) Other brands: Fulyzaq , Mytesi Related treatment guides Diarrhea> ] FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Antidiarrheals Related Drugs Diarrhea loperamide , Lomotil , Imodium , Acidophilus , atropine / diphenoxylate , neomycin , Florastor , lactobacillus acidophilus , Pepto-Bismol , bismuth subsalicylate , Florajen , saccharomyces boulardii lyo , Imodium A-D , Kaopectate , Anti-Diarrheal , Pedialyte , opium , Bacid (LAC) , Bismatrol , attapulgite , Flora-Q , RisaQuad , More... 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