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Kaopectate

Kaopectate is a brand-name over-the-counter used to treat and relieve associated symptoms of upset , including , , , gas, , and fullness. Its active ingredient, (524 mg per 30 mL dose in liquid form; 262 mg per 15 mL), works by coating the lining of the and intestines to protect against irritation, reducing , and exhibiting effects against certain that can cause . Originally introduced in 1936 as a combination of kaolin (a clay adsorbent) and pectin (a demulcent derived from fruits), Kaopectate was named after its key component, kaolin, and was marketed for noninfectious diarrhea and gastrointestinal upset. In the late 1980s, the formulation shifted to attapulgite clay as the primary adsorbent, and by 2003, it was reformulated to to enhance efficacy and comply with regulatory standards, including reductions in trace lead contaminants previously present in earlier versions. This change aligned Kaopectate more closely with similar products like Pepto-Bismol, while maintaining its focus on multi-symptom relief for conditions such as traveler's diarrhea and overindulgence in food or drink. The medication is available in forms including cherry- or vanilla-flavored liquids, caplets, and tablets, with dosing typically every 30 to 60 minutes as needed, up to eight doses in 24 hours for adults and children 12 years and older. Precautions include avoiding use in children under 12 without medical advice, and it is contraindicated for those with aspirin allergies, bleeding disorders, or certain infections due to the salicylate component. Over the years, ownership has transitioned from early manufacturers to Chattem Inc., then , and since 2020 to Consumer Healthcare, with distribution handled by entities like Laboratories.

Medical Uses

Indications

Kaopectate, an over-the-counter medication containing , is primarily indicated for the relief of mild, acute in adults and children 12 years of age and older. It provides temporary symptomatic relief by addressing nonspecific not associated with fever or systemic illness, typically resolving within 48 hours of use. The product is approved by the U.S. (FDA) for this purpose as a Category I over-the-counter agent. In addition to its primary role, Kaopectate is indicated for secondary gastrointestinal symptoms, including upset stomach due to overindulgence in food and drink, , , , gas, , and feelings of fullness. It is also used for the prevention and treatment of , particularly in scenarios involving dietary changes or exposure to unfamiliar water sources. These indications focus on short-term, self-limiting conditions, and the medication should not be used for more than two days without medical consultation. Kaopectate is not indicated for chronic diarrhea, which may signal an underlying condition requiring diagnostic evaluation, nor for cases involving bloody or mucoid stools, high fever, or , as these warrant immediate medical attention. Off-label applications include its use in combination with other antibiotics and acid-suppressing agents for the management of pylori-associated gastric ulcers, supported by clinical evidence demonstrating antimicrobial activity against the bacterium. It may also provide occasional relief for minor gastric discomfort in supervised settings, though such uses are not part of the official labeling.

Dosage and Administration

Kaopectate is administered orally in the form of , caplets, or tablets for the relief of and associated symptoms. The standard dosage for adults and children 12 years and older is 30 mL of oral or 2 caplets/tablets, equivalent to 524 mg of , taken every 30 to 60 minutes as needed. This regimen should not exceed 8 doses in any 24-hour period. For children under 12 years of age, consult a healthcare provider before use. Do not use in children or teenagers recovering from or flu-like symptoms unless directed by a , due to the risk of Reye's syndrome. The oral suspension must be shaken vigorously before each use to ensure even distribution of the . Caplets and tablets should be swallowed whole with water and not chewed. Therapy should be limited to no more than 2 days or until resolves, whichever occurs first; if symptoms persist beyond this duration, medical advice should be sought promptly. For prevention of , adults may take 524 mg (2 caplets/tablets or 30 mL of ) four times daily, starting 1 to 2 days before and continuing throughout the trip for up to 3 weeks.

Pharmacology and Mechanism

Mechanism of Action

Kaopectate, containing as its active ingredient, exerts its therapeutic effects primarily through multiple mechanisms that address the of and gastrointestinal upset. The compound's antisecretory action reduces intestinal fluid secretion by inhibiting the synthesis of prostaglandins, which are mediators that promote and hypersecretion in the gut; this inhibition occurs via blockade of enzymes. Additionally, demonstrates antimicrobial activity against common diarrhea-causing pathogens, such as and species, by binding to bacterial cell walls and disrupting their integrity, leading to bactericidal effects that limit bacterial proliferation and toxin production in the intestinal lumen. This binding occurs with sufficient affinity to effectively inhibit growth even at concentrations achievable in the , though the precise molecular interactions remain under study. The formulation also provides a protective on the intestinal mucosa, forming an insoluble complex that acts as a barrier to soothe , shield against further damage from irritants or pathogens, and thereby reduce local . The salicylate moiety contributes mild properties, alleviating associated abdominal cramps through its effects akin to those of other salicylates. Overall, these combined actions help normalize bowel function without significantly altering normal gut flora.

Pharmacokinetics

Bismuth subsalicylate (BSS), the active ingredient in Kaopectate, undergoes in the stomach to and upon . The component is almost completely absorbed from the , achieving peak concentrations of approximately 40 μg/mL within 1 to 2 hours following a standard dose. In contrast, absorption is minimal, with less than 1% entering the systemic circulation, resulting in levels typically below 5 ng/mL even after multiple doses; this limited uptake allows BSS to exert its effects primarily through local action within the . does not significantly alter the absorption profile of either component. Due to its poor systemic , bismuth exhibits minimal beyond the gastrointestinal , where it forms insoluble salts such as that contribute to its therapeutic activity. The salicylate moiety, once absorbed, distributes widely throughout the body, including into plasma and tissues, similar to other salicylates. Metabolism of occurs primarily through gastric into its and salicylate components; the itself is not further metabolized, while the absorbed salicylate is converted in the liver to and subsequent conjugates. Excretion of is predominantly fecal, reflecting its limited and retention in the gut, though trace amounts may be eliminated via and . Salicylate metabolites are primarily cleared through the kidneys into . The elimination of the salicylate component is approximately 2 to 5 hours. With multiple doses, can accumulate in the stool, often manifesting as darkened feces, but systemic accumulation is negligible in short-term use.

Side Effects and Safety

Common Side Effects

The most common side effect of Kaopectate, which contains as its , is the temporary blackening of the and stools, occurring due to the formation of bismuth sulfide when the drug reacts with produced by gut bacteria. This effect is very common, affecting 10% or more of users for black stools and 1% to 10% for black tongue, but it is harmless and fully reversible upon discontinuation of the medication. Other gastrointestinal side effects include , along with less frequent occurrences of or ; these are typically mild and self-limiting, resolving without intervention once the drug is stopped, though users should adhere to recommended dosages to minimize risks. Allergic reactions to Kaopectate are uncommon but may manifest as or itching in sensitive individuals, with severe being extremely rare. In cases of suspected , immediate medical attention is advised. Signs of overdose, primarily related to salicylate from excessive intake, can include , , seizures, and severe drowsiness. Management involves seeking emergency care, as these symptoms may progress to more serious complications if untreated.

Contraindications and Precautions

Kaopectate, containing , is contraindicated in individuals with a known to , salicylates, or aspirin, as it may provoke severe allergic reactions. It is also absolutely contraindicated in children and teenagers recovering from chicken pox or flu-like symptoms due to the risk of Reye's syndrome, a rare but serious condition involving liver and . Additionally, use is prohibited in patients with active peptic ulcers, bleeding disorders, or those experiencing bloody or black stools, as the salicylate component can worsen or mask underlying pathology. Precautions are necessary for certain populations where the salicylate in Kaopectate may pose risks. Patients with disorders, , or renal impairment should avoid or use it cautiously, as salicylates can increase tendencies, elevate levels, or accumulate in the body leading to . It is not recommended for self-treatment in cases of accompanied by fever or /blood in stools, and medical consultation is advised if symptoms persist beyond two days or if develops, which may signal salicylate overdose. Drug interactions with Kaopectate primarily stem from its salicylate and components. Concurrent use with anticoagulants like heightens the risk of bleeding due to additive effects on platelet function and clotting factors. can bind to tetracyclines in the , reducing their absorption by up to 34%; doses should be separated by at least two hours to minimize this effect. Administration with other salicylate-containing products, such as aspirin, should be avoided to prevent cumulative toxicity and enhanced adverse effects. Consultation with a healthcare provider is recommended if the patient is on medications for , , or , as interactions may alter therapeutic responses. Regarding special populations, current FDA labeling for advises use during only if clearly needed, as show risks and human data are limited; it should be avoided in the third due to salicylate-related risks such as increased , fetal harm, and . During , caution is warranted because salicylates are excreted into and may cause adverse effects in nursing infants, such as .

History and Formulation Changes

Original Development

Kaopectate was developed by the Company during the 1930s as an over-the-counter suspension combining kaolin, a natural clay adsorbent, and , a plant-derived , to alleviate symptoms of by absorbing excess fluids and soothing the intestinal lining. The formulation leveraged the protective properties of these naturally occurring substances, which had been used in folk remedies for gastrointestinal issues, to create a gentle, non-chemical alternative for mild treatment. The product was first commercialized and sold in the United States in under the brand name Kaopectate, a portmanteau derived from its primary ingredients, kaolin and pectin. Introduced prior to the full implementation of modern FDA regulatory frameworks under the Federal Food, Drug, and Cosmetic Act, Kaopectate entered the market as a safe, effective OTC remedy based on established pharmaceutical practices of the era, without requiring pre-market approval typical of later drugs. promoted it through detailing and direct advertising, emphasizing its suitability for everyday use in managing acute from dietary indiscretions or travel-related ailments. Early adoption was rapid, driven by the appeal of its all-natural composition amid growing consumer preference for non-synthetic medications during the post-Depression recovery period. Primarily targeted at human use for symptomatic relief of noninfectious , Kaopectate established itself as a staple in household medicine cabinets, contributing to Upjohn's reputation in the category.

Key Formulation Shifts

In the late 1980s, Kaopectate underwent a significant reformulation when its original active ingredients, kaolin and , were replaced by attapulgite clay, a magnesium aluminum noted for superior water adsorption and compared to the kaolin- combination. This shift, occurring around 1984 to early 1990s, was driven by attapulgite's enhanced performance in binding toxins and fluids in the , as well as improved availability of the . By 2003, regulatory scrutiny intensified when the U.S. (FDA) issued a final for over-the-counter drug products, prohibiting attapulgite due to insufficient and inconsistent evidence of its safety and efficacy from submitted studies. The FDA docket specifically highlighted the lack of substantial data demonstrating attapulgite's effectiveness in reducing duration or severity, leading to its exclusion as a ingredient effective April 19, 2004. In response, the manufacturer reformulated Kaopectate for the U.S. market in 2004, switching the active ingredient to , which had established efficacy for symptomatic relief of and associated symptoms like . This change aligned with FDA standards and mirrored the composition of competing products like Pepto-Bismol. In contrast, Canadian formulations retained attapulgite as the until a 2021 Health Canada of Children's Kaopectate Suspension due to elevated levels of , including and lead, exceeding acceptable limits in affected lots. This , issued on July 2, 2021, and affecting all available stock, ultimately led to the discontinuation of attapulgite-based Kaopectate in , disrupting supply and prompting a reevaluation of alternatives.

Ingredients and Availability

Current Formulations

In the United States, the current formulation of Kaopectate features as the active ingredient at a concentration of 262 mg per 15 mL of liquid or per caplet, providing an equivalent of approximately 525 mg per standard 30 mL or two-caplet dose for anti-diarrheal and upset stomach relief. This over-the-counter (OTC) medication is manufactured and distributed by Laboratories, a of Arcadia Consumer Healthcare, following the company's acquisition of the U.S. rights in 2020. Kaopectate maintains its OTC status, available without prescription for adults and children over 12 years old. For the liquid suspension, common inactive ingredients include (for color), carboxymethylcellulose sodium (as a suspending agent), , (preservative), sodium salicylate, , , and , with flavorings such as cherry, vanilla, or to improve palatability. The liquid variants contain sodium salicylate as an inactive ingredient in addition to the salicylate from the , which may pose risks for those sensitive to salicylates. Caplet formulations lack this additional sodium salicylate, featuring inactive components like croscarmellose sodium, crospovidone, hydrated silica, , , , , and povidone instead. These caplets offer a solid . Internationally, formulations vary by market; in , following the 2021 recall and discontinuation of attapulgite-based products due to heavy metal contamination, available Kaopectate products as of November 2025 primarily use as the active ingredient, similar to the U.S. version and often available in vanilla-flavored liquid form through importation. Attapulgite is no longer used in U.S. or Canadian bismuth-based formulations, though it persists in select international markets like for certain Kaopectate products. Overall, these current compositions prioritize for its dual action on and gastrointestinal symptoms, with inactive ingredients tailored for stability, taste, and ease of administration across liquid and caplet formats.

Historical Ingredients

The original formulation of Kaopectate, introduced in 1936 and used through the 1980s, consisted primarily of kaolin, a naturally occurring clay adsorbent, at a concentration of 90 grains per (approximately 197 /), and pectin, a plant-derived emollient, at 2 grains per (approximately 4.4 /). These ingredients worked by adsorbing bacterial toxins in the via kaolin's binding properties and providing a protective to the intestinal lining through pectin's action. The formula was marketed as a "natural" remedy, leveraging kaolin's origin and pectin's source from fruit peels, which aligned with early perceptions of gentle, non-chemical treatments for . In the 1980s, following FDA concerns over the of kaolin and —classified as Category III (insufficient evidence of ) in a 1986 review—the product was reformulated to replace kaolin with attapulgite, another adsorbent, at 1.2 g per dose, while was reduced or entirely removed in most versions. This attapulgite-based version, used in the United States until 2003, was promoted as an "advanced clay" formulation for improved toxin absorption and relief. However, attapulgite faced similar scrutiny; the FDA's 2003 final on drugs excluded it due to inadequate data from clinical studies. Discontinuation of these historical ingredients stemmed from safety and regulatory issues beyond efficacy alone. Kaolin's removal was partly influenced by potential natural contaminants in clay sources, though primary drivers were evidentiary gaps rather than acute risks. Attapulgite's phase-out accelerated due to lead contamination detected in products, prompting a 2003 reformulation agreement to eliminate the metal, which posed neurological risks especially in children. In Canada, where attapulgite persisted longer, a 2021 recall of Kaopectate suspension cited excessive heavy metals (arsenic and lead) exceeding safe limits, leading to its full discontinuation. These shifts marked the transition away from clay-based adsorbers toward more rigorously vetted alternatives.

Veterinary and Other Applications

Use in Animals

The original formulation of Kaopectate containing kaolin and pectin was permitted for use in organic livestock production, including food-producing animals such as cows and pigs, under USDA National Organic Program standards prior to the 2003 reformulation. The current bismuth subsalicylate version lacks FDA approval for veterinary use and is considered off-label when administered to animals. In veterinary practice, kaolin-pectin variants, including veterinary-specific formulations such as Kaolin/Pectin oral suspensions, remain commonly employed for supportive care of noninfectious diarrhea in species including dogs, cats, horses, and cattle, while the bismuth formulation is used cautiously in select cases under strict supervision. In dogs, Kaopectate or equivalent products are frequently recommended for short-term management of mild, uncomplicated , with a total daily dosage of 1–3 orally, divided into 2–4 doses every 6–12 hours as directed by a . PetMD guidelines as of 2023 endorse its use in dogs under veterinary supervision for acute gastrointestinal upset, emphasizing that it should not exceed without reassessment. However, administration requires professional oversight to monitor for potential interactions or underlying causes of . Use in cats requires extreme caution and strict veterinary supervision due to their sensitivity to salicylates, which can metabolize into aspirin-like compounds leading to toxicity, including . The 2023 PetMD recommendations caution against salicylate-containing formulations in felines without supervision, advising alternatives like kaolin-pectin if therapy is needed. Veterinary consultation is essential before any use, as cats may exhibit severe reactions even at low doses. Precautions include avoiding Kaopectate in dehydrated animals, where it may exacerbate fluid loss, or in those with gastrointestinal ulcers or bleeding disorders, as salicylates can worsen mucosal damage. It should not be used for severe, persistent, or infectious , and animals with concurrent conditions like renal impairment require adjusted dosing or alternatives. Always obtain veterinary approval to ensure safety and efficacy across species.

Non-Medical Uses

Kaopectate, containing bismuth subsalicylate, has been used anecdotally in home remedies to alleviate symptoms of minor food poisoning by coating the stomach lining and reducing irritation from toxins or pathogens. Users report it helps soothe nausea, cramping, and loose stools associated with mild cases, often self-administered without medical consultation as a first-line household intervention. Similarly, it is employed informally for relief, where its properties are believed to protect the against -induced inflammation, easing and . Anecdotal accounts suggest taking it after excessive drinking to mitigate upset and prevent , though effectiveness varies and relies on individual experiences rather than clinical validation. Historically, Kaopectate has appeared in and kits for managing wilderness-acquired , included as a compact anti-diarrheal option in lists for outdoor or scenarios. Such kits, recommended by organizations for remote travel or crises, stock it alongside hydration aids to address acute gastrointestinal distress from contaminated water or food in isolated settings. These non-medical applications lack formal endorsement from the FDA, which approves Kaopectate solely for relieving and associated upset stomach symptoms, not for mitigation or informal remedies. Misuse carries risks, including salicylate-related complications like or allergic reactions, particularly if symptoms indicate a more serious condition requiring professional care. No rigorous studies support its efficacy in these alternative contexts, emphasizing reliance on over .

Society and Culture

Brand Ownership and Marketing

Kaopectate was originally introduced in 1936 by Sharp & Dohme and acquired by in 1949, which then marketed it as an medication containing kaolin and . In 1995, merged with to form , which continued to own and promote the brand. acquired in 2003, thereby gaining ownership of Kaopectate. In 2006, sold the U.S. rights to Kaopectate to , Inc., as part of a broader divestiture of over-the-counter brands. acquired in 2010, integrating Kaopectate into its consumer healthcare portfolio. In March 2020, sold the U.S. rights to Consumer Healthcare (formerly Laboratories) in a transaction whose value was not publicly disclosed; announced plans to invest in marketing and innovation to drive growth for the brand. Throughout its history, Kaopectate has been marketed as a trusted provider of quick, multi-symptom relief for , upset stomach, , , and gas, often positioning itself as suitable for travelers, families, and those affected by overindulgence or causes. Advertising campaigns have emphasized the brand's long-standing reliability, with over 75 years of use by millions of , and its ability to target symptoms at the source despite formulation updates over time. The brand's promotional efforts include television commercials highlighting rapid action and ease of use, such as caplets for on-the-go convenience. Kaopectate is widely available over-the-counter in U.S. pharmacies, grocery stores, and online retailers in forms like liquids and caplets. Generic equivalents containing , the current active ingredient, are also readily accessible and often sold under store brands. Annual sales figures for Kaopectate specifically are not publicly reported, but it holds a significant share in the global OTC market, valued at $4.03 billion in 2025. Kaopectate has appeared in various forms of media, often as a humorous or practical reference to dealing with digestive issues. In the 1979 hip-hop track "Rapper's Delight" by , the lyrics describe seeking "quick relief from a bottle of Kaopectate" after overindulging in food, highlighting the product's role in everyday mishaps. This early mention helped embed the brand in culture during the rise of . Television shows have featured Kaopectate in comedic contexts related to stomach ailments. In the 1995 episode "The Weaker Sex" of , character mistakenly drinks a bottle of Kaopectate, believing it to be a shake, leading to a humorous revelation about his lunch. Similarly, in , the character consumes Kaopectate after misunderstanding its purpose for relief, adding to the show's absurd humor. These portrayals underscore Kaopectate's recognition as a go-to remedy in lighthearted depictions of bodily discomfort. In film, Kaopectate receives a brief but memorable nod in the 1996 comedy The Nutty Professor, where a character lists it alongside as an essential drugstore purchase for health woes. Literature also references the product in narratives involving travel and survival challenges. Stephen King's 2011 novel includes multiple instances where the protagonist relies on Kaopectate to manage stomach upset during time-travel adventures. Travel memoirs, such as Bob Shacochis's 2016 Kingdoms in the Air, evoke it as a staple for adventurers, noting that embarking on far-flung journeys often involves acquiring "a plane ticket and a bottle of Kaopectate." The brand's cultural footprint extends to parodies and informal references, particularly in humor and memes centered on "the runs," though it lacks major celebrity endorsements. Its household name status was bolstered by television commercials, such as the 1981 ad positioning it as "the specialist," which used catchy scenarios to make the product synonymous with rapid relief. In survivalist fiction, like Hoagland's 2013 Children Are Diamonds, Kaopectate appears as a aid distributed in crisis situations, emphasizing its practical ubiquity without dramatic flair.

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