Although most acute nonspecific diarrhea in the United States is self-limiting, nonprescription antidiarrheal products may provide relief and will usually do no harm when used according to label instructions. Table Recommended Dosages of Antidiarrheal Agents for Acute Diarrhea lists dosage and administration guidelines for these agents. Scientific evidence that pharmacologic agents, with the exception of loperamide and Bismuth subsalicylate. reduce stool frequency or duration of disease in adults is lacking. Likewise, antidiarrheal drugs have not been shown to significantly improve clinical outcomes of acute nonspecific diarrhea in infants and children. Importantly, a change in stool consistency toward more formed stools does not necessarily indicate that antidiarrheal therapy has successfully treated the underlying problem.

Comparison of Electrolyte and Dextrose Concentrations of Household Fluids

Clear Liquids	Sodium (mEq/L)	Potassium (mEq/L)	Bicarbonate (mEq/L)	Dextrose (g/L)	Osmolarity (mOsm/L)
Cola	2	0.1	13	50-150 dextrose and fructose	550
Ginger ale	3	1	4	50-150 dextrose and fructose	540
Apple juice	3	20	0	10-150 dextrose and fructose	700
Chicken broth	250	5	0	0	450
Tea	0	0	0	0	5
Gatorade	20	3	3	45 dextrose and other sugars	330
Seven Up	7.5	0.2	0	80 dextrose and fructose	564

Recommended Dosages of Antidiarrheal Agents for Acute Diarrhea

	Adult Dosages
Medication	Dosage Forms	(Maximum Daily Dosage)	Pediatric Dosages	Duration of Use
Loperamide	Caplets (2 mg), liquid (1 mg/7.5 mL)	4 mg initially, then 2 mg after each loose stool (not to exceed 8 mg/day)	Consult product instructions; not recommended for children < 6 years except under medical supervision	48 hours
Bismuth subsalicylate	Tablets (262 mg), caplets (262 mg) liquids (262 mg/ 15 mL, 525 mg/ 15 mL)	525 mg every 30-60 minutes up to 4200 mg/day; (8 doses/day)	Not recommended for children < 12 years except under medical supervision	48 hours
Digestive enzymes (lactase)	Chewable tablets, caplets, liquids	5-15 drops placed in or taken with dairy product; 1-3 tablets or 1-2 capsules with first bite of dairy product	Same as adult dosage	Taken with each consumption of dairy product

Formed stools can have high water content, and substantial water losses may continue despite the change in consistency. Moreover, reliance on drugs shifts the focus away from management of fluids and electrolytes and dietary measures, increasing the risk for potentially dangerous side effects, such as toxic megacolon. without offering additional benefits. Because intestinal viruses are the leading cause of self-limiting acute gastroenteritis, antibiotics are not routinely recommended.

Loperamide

Loperamide is a popular, effective, and safe nonprescription antidiarrheal agent. It is a synthetic opioid agonist that produces antidiarrheal effects by stimulating micro-opioid receptors located on the intestinal circular muscles. This action slows intestinal morality, allowing absorption of electrolytes and water through the intestine. Stimulation of gastrointestinal micro-opioid receptors also decreases gastrointestinal secretion, which may contribute to the drug‘s antidiarrheal effects. Loperamide is approximately 50-fold more potent than morphine and two to three times more potent than diphenoxylate in its effects on gastrointestinal motility. However, loperamide penetrates the central nervous system (CNS) poorly and therefore has a lower risk for CNS side effects. Other pharmacologic mechanisms for loperamide’s antidiarrheal effects may include disruption of cholinergic and noncholinergic mechanisms involved in the regulation of peristalsis, inhibition of calmodulin function, and inhibition of voltage-dependent calcium channels. The effects on calmodulin and calcium channels may contribute to loperamide’s antisecretory effects.

Loperamide is used to provide symptomatic relief for acute, nonspecific diarrhea. Its therapeutic effects include reduction of daily fecal volume, increased viscosity, bulk volume, and reduced fluid and electrolyte loss. It may be used when the patient is afebrile or has a low-grade fever and does not have bloody stools. Current product information provides directions for use in children as young as 2 years. However, its use in children younger than 6 years is not recommended, because it produces only modest, clinically insignificant effects on stool volume and duration of illness, with an unacceptably high risk of side effects (including life-threatening side effects such as ileus and toxic megacolon).

Loperamide is also indicated as an antidiarrheal agent in travelers’ diarrhea (in combination with antibiotics), for chronic diarrhea associated with irritable bowel syndrome and inflammatory bowel disease, and for reduction of the volume of discharge from high-output ileostomies. Off-label uses of loperamide include control of chronic diarrhea secondary to diabetic neuropathy and other conditions, as well as control of toddler diarrhea (defined as diarrhea of at least 1 month duration in an otherwise healthy, active, well-nourished child, and in whom stool examination has revealed no bacterial, viral, or protozoal pathogens). All of these uses require medical supervision.

At usual doses, loperamide has few side effects other than occasional dizziness and constipation. Other infrequently occurring adverse effects include abdominal pain, abdominal distention. nausea, vomiting, dry mouth, fatigue, and hypersensitivity reactions. Loperamide is generally not recommended for use in patients with invasive (enteroinvasive E. coll, Salmonella, Sliigella, or C. jejuni) bacterial diarrhea or antibiotic-associated diarrhea (C. difficile), because it may (rarely) worsen diarrhea or cause toxic megacolon or paralytic ileus. However, there is no evidence that these complications occur in actual practice when loperamide is used with appropriate antimicrobial therapy. Patients with symptoms suggestive of infection with invasive organisms or antibiotic-associated diarrhea (i.e., fecal leukocytes, high fever, or blood or mucus in the stool) require evaluation by a primary care provider for proper management. If abdominal distention. constipation, or ileus occurs, loperamide should be discontinued. No significant drug-drug interactions are reported for loperamide.

Bismuth Subsalicylate

Bismuth subsalicylate is effective in the treatment of acute diarrhea, including travelers’ diarrhea, significantly reducing the number of diarrhea] stools.

Bismuth subsalicylate reacts with hydrochloric acid in the stomach to form bismuth oxychloride and salicylic acid. Bismuth oxychloride is insoluble and poorly absorbed from the gastrointestinal tract; less than 1% of the administered dose is absorbed systemically. The salicylate is readily and efficiently absorbed. Both moieties are pharmacologically active; each produces effects that reduce frequency of unformed stools, increase stool consistency, relieve abdominal cramping, and decrease nausea and vomiting in children and adults. In travelers’ diarrhea, the bismuth moiety exerts direct antimicrobial effects against ETEC and EAEC, C, jejuni, and other diarrhea] pathogens, whereas the salicylate moiety exerts antisecretory effects that reduce fluid and electrolyte losses in acute diarrhea. The antisecretory effects may be mediated by-several mechanisms, including inhibition of prostaglandin synthesis, inhibition of intestinal secretion through stimulation of sodium and chloride reabsorption. or disruption of calcium-mediated processes that regulate intestinal ion transport. Bismuth subsalicylate also directly binds to enterotoxins produced by E. coli and other diarrheal pathogens; however, the clinical significance of this effect in the treatment of diarrhea is not clear.

Bismuth subsalicylate is FDA-approved for management of acute diarrhea, including travelers’ diarrhea, in adults and children 12 years of age or older. Although previously labeled for children as young as 3 years, the product is not recommended for use in young children and no longer carries labeling for children younger than 12 years. Bismuth subsalicylate is also indicated for indigestion and as an adjuvant to antibiotics for treating H.pylori-associated peptic ulcer disease.

Table Recommended Dosages of Antidiarrheal Agents for Acute Diarrhea provides dosing information for Bismuth subsalicylate.

Bismuth subsalicylate dosage forms contain various amounts of salicylate. Methyl salicylate (oil of wintergreen) is used as a flavoring agent in the suspension dosage form and the original tablet formulation. The original suspension and cherry-flavored suspension dosage forms (262 mg/l 5 mL) contain 130 mg of salicylate. whereas the original tablets (262 mg) contain 102 mg of salicylate. The caplets (262 mg) and cherry-flavored tablets (262 mg) contain 99 mg of salicylate. If a patient is taking aspirin or other salicylate-containing drugs, toxic levels of salicylate may be reached even if the patient follows dosing directions on the label for each drug.

Mild tinnitus is a dose-related side effect that may be associated with moderate-to-severe salicylate toxicity. If tinnitus occurs, the product should be discontinued and the patient referred for medical evaluation. Salicylates may cause adverse effects that are independent of the dose. Children and adolescents who have or are recovering from chicken pox or influenza are at risk of Reye’s syndrome, a rare but serious illness associated with salicylates. These patients should not use Bismuth subsalicylate. In susceptible patients, salicylate-induced gout attacks have occurred. Patients who are sensitive to aspirin (resulting in asthmatic bronchospasm) should not use Bismuth subsalicylate.

Overdosage of bismuth products can cause neurotoxicity. Blood concentrations of bismuth greater than 50 mg/L have been associated with encephalopathy characterized by slow onset of tremors, postural instability, ataxia, myoclonus, and poor concentration. Confusion, memory impairment, seizures, visual and auditory hallucinations, psychosis, delirium, and depression may also develop. Most patients gradually recover after discontinuation of the bismuth preparation; however, some develop a permanent tremor and the encephalopathy has resulted in fatality, acquired immunodeficiency syndrome patients with acute diarrhea may be at particular risk for bismuth encephalopathy, perhaps resulting from altered gastrointestinal absorption.

Harmless black staining of stool may occur, which should not be confused with melena; in addition, harmless darkening of the tongue may also occur. These frequent effects occur in more than 10% of patients treated with Bismuth subsalicylate. Bismuth salts react with hydrogen sulfide produced by bacteria in the mouth and

colon. The resulting compound, bismuth sulfide, imparts the black discoloration. It is easily removed from the surface of the tongue by brushing the tongue with a soft-bristled brush; it may also be treated by discontinuing the bismuth product.

Bismuth subsalicylate is contraindicated for nursing or pregnant women and should therefore not be used without medical advice. It also should not be used in patients with acquired immunodeficiency syndrome because of the risk for neurotoxicity. Bismuth is radiopaque and may interfere with radiographic intestinal studies.

Bismuth subsalicylate may interact adversely with a number of other drugs, particularly those that potentially interact with aspirin. The salicylate moiety can increase the risk of toxicity with warfarin, valproic acid, and methotrexate by significantly decreasing plasma protein binding of these drugs in vivo. Salicylate can also increase the plasma concentration of methotrexate by decreasing its renal clearance. The uricosuric effects of probenecid may be inhibited by salicylate; the exact mechanism underlying this interaction is not known. The bismuth moiety is a bivalent cation and may decrease absorption of other medications. such as tetracycline and quinolone antibiotics, by forming complexes with them in the gastrointestinal tract. When ciprofloxacin is used to treat travelers’ diarrhea, the patient should be instructed to discontinue Bismuth subsalicylate. Solid dosage forms of Bismuth subsalicylate contain calcium carbonate, which may enhance the cation complex interaction.

Adsorbents

Gastrointestinal adsorbents (attapulgite, kaolin, and pectin) are no longer used to treat diarrhea. Evidence supporting the safety and effectiveness of attapulgite and pectin is lacking; products containing these adsorbents have either been reformulated or withdrawn from the market. Sufficient data support the effectiveness of kaolin in improving stool consistency within 24 to 48 hours, although it does not reduce the number of stools passed. Kaolin has been deemed to be a safe and effective antidiarrheal agent by the FDA, but no single-ingredient kaolin products are currently available in the United States.

Digestive Enzymes

For patients with lactase deficiency who are intolerant of milk products, lactase enzyme preparations (Table Selected Lactase Enzyme Products) may be taken with milk or other dairy products to prevent osmotic diarrhea.

Selected Lactase Enzyme Products

Trade Name	Primary Ingredient
Lactaid Caplets	Lactase enzyme 3000 FCC unitsVcaplet
Lactaid Fast Act Caplets	Lactase enzyme 9000 FCC unitsVcaplet
Lactrase Capsules	Lactase enzyme 250 mg/capsule

Product Selection Guidelines

Table Recommended Dosages of Antidiarrheal Agents for Acute Diarrhea provides a quick reference for recommended dosages and durations ol therapy for selected antidiarrheal agents. Tables Selected Lactase Enzyme Products and Selected Antidiarrheal Products list dosage forms and primary ingredients of selected trade-name products.

Special Populations

For young children (5 years or younger), self-treatment is limited to treating dehydration with oral rehydration solutions; antidiarrheal medications are not recommended. If oral rehydration solutions are ineffective, a primary care provider must be consulted.

Elderly patients (65 years or older) should be strongly cautioned against self-treatment with antidiarrheal medications. Diarrhea in these patients is more likely to be severe possibly fatal; therefore, these patients should be referred for medical evaluation.

Selected Antidiarrheal Products

Loperamide Products Imodium A-D Caplets	Loperamide HCI 2 mg
Imodium EZ Chews (Tablets)	Loperamide HCI 2 mg
Imodium Advanced Caplets	Loperamide HCI 2 mg; simethicone 125 mg
Imodium Advanced Chewable	Loperamide HCI 2 mg; simethicone 125 mg
Tablets	Loperamide HCI 1 mg/7.5 mL
Imodium A-D Liquid
Bismuth Subsalicylate	Products
Kaopectate Regular Flavor Liquid	Bismuth subsalicylate 262mg/15mL
Kaopectate Extra Strength Peppermint Flavor Liquid	Bismuth subsalicylate 525mg/15mL
Kaopectate Peppermint Flavor Liquid	Bismuth subsalicylate 62mg/15 mL
Kaopectate Cherry Flavor Liquid	Bismuth subsalicylate 262mg/15mL
Kaopectate Antidiarrheal Caplets	Bismuth subsalicylate 262 mg
Pepto-Bismol Caplets	Bismuth subsalicylate 262 mg
Pepto-Bismol Chewable Tablets	Bismuth subsalicylate 262 mg
Pepto-Bismol Cherry Chewable Tablets	Bismuth subsalicylate 262 mg
Pepto-Bismol Original Liquid	Bismuth subsalicylate 262mg/15mL
Pepto-Bismol Cherry Liquid	Bismuth subsalicylate 262mg/15mL
Pepto-Bismol Maximum Strength Liquid	Bismuth subsalicylate 525mg/15mL

Use of nonprescription antidiarrheals may be inappropriate during pregnancy; therefore, pregnant women should consult with a primary care provider before self-treating. Loperamide is a Pregnancy Category 15 drug. Although 13SS does not have an FDA Pregnancy Category rating. BSS-containing products should be used sparingly or not at all during pregnancy because of concerns that the salicylate component may inhibit platelet function and, in the third trimester, cause premature closure of the fetal ductUS arteriosus.

Patient Factors

Selection of antidiarrheal products for older children and adults should be based on factors such as the etiology of the diarrhea, if known, prominent symptoms, potential interactions with prescribed medications, and the applicable contraindications. For example. Bismuth subsalicylate is suggested to be the preferred agent when vomiting is the important clinical symptom of acute gastroenteritis. Furthermore, BSS should not be used to treat diarrhea in an immunocompromised patients (e.g., acquired immunodeficiency syndrome and transplant recipients), because they are at increased risk for bismuth encephalopathy.

A patient’s preference for a particular dosage form or a product that requires (ewer doses is another selection criterion.

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