LOPERAMIDE HCL
Brand names: Anti Diarrheal, equaline loperamide hydrochloride, Anti-Diarrheal, loperamide hydrochloride, topcare loperamide hydrochloride, Loperamide HCl, leader anti diarrheal, foster and thrive anti diarrheal, anti diarrheal, Good Sense antidiarrheal, basic care loperamide hydrochloride, good neighbor pharmacy loperamide hydrochloride, Anti-Diarrheal, CVP HEALTH, Anti-diarrheal, CareOne Diarrhea Control, equate diarrhea control, Anti-Diarrheal, Caseys 4good, Loperamide hydrochloride, injoy diarrhea relief, DG Health Anti Diarrheal, LOPERAMIDE HYDROCHLORIDE, Equate Loperamide Hydrochloride, foster and thrive anti-diarrheal, ANTI-DIARRHEAL, Up and Up anti diarrheal, Leader Anti Diarrheal
Boxed warning
WARNING: TORSADES DE POINTES AND SUDDEN DEATH Cases of Torsades de Pointes, cardiac arrest, and death have been reported with the use of a higher than recommended dosages of loperamide hydrochloride (see WARNINGS and OVERDOSAGE). Loperamide hydrochloride is contraindicated in pediatric patients less than 2 years of age (see CONTRANIDICATIONS). Avoid loperamide hydrochloride dosages higher than recommended in adults and pediatric patients 2 years of age and older due to the risk of serious cardiac adverse reactions (see DOSAGE AND ADMINISTRATION).
Warnings
Warnings Allergy alert: Do not use if you have ever had a rash or other allergic reaction to loperamide HCl Heart alert: Taking more than directed can cause serious heart problems or death Do not use if you have bloody or black stool Ask a doctor before use if you have fever mucus in the stool a history of liver disease a history of abnormal heart rhythm Ask a doctor or pharmacist before use if you are taking a prescription drug. Loperamide may interact with certain prescription drugs. When using this product tiredness, drowsiness or dizziness may occur. Be careful when driving or operating machinery. Stop use and ask a doctor if symptoms get worse diarrhea lasts for more than 2 days you get abdominal swelling or bulging. These may be signs of a serious condition. If pregnant or breast-feeding, ask a health professional before use. Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center right away.
Contraindications
Loperamide hydrochloride capsules are contraindicated in: pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions (see WARNINGS). patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. patients with abdominal pain in the absence of diarrhea. patients with acute dysentery, which is characterized by blood in stools and high fever. patients with acute ulcerative colitis. patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter. patients with pseudomembranous colitis (e.g., Clostridium difficle) associated with the use of broad-spectrum antibiotics.
Overdose
The use of higher than recommended loperamide hydrochloride doses may result in life-threatening cardiac, CNS and respiratory adverse reactions. If over-exposure occurs, call your Poison Control Center at 1-800-222-1222 for current information on the management of poisoning or overdosage. Cardiac Effects Symptoms Cases of overdosage with loperamide hydrochloride (chronic ingestion of doses ranging from 70 mg to 1600 mg daily; 4 to 100 times the recommended dose) have resulted in life-threatening cardiac adverse reactions, including QT/QTc and QRS interval prolongation, Torsades de Pointes, Brugada syndrome and other ventricular arrhythmias, syncope, cardiac arrest, and death. Cases include patients who were abusing (using supratherapeutic doses in place of opioids to induce euphoria) or misusing (taking higher than recommended doses to control diarrhea or to prevent opioid withdrawal) loperamide. The following are representative cases that included cardiac adverse reactions: 25 year old abused loperamide and presented to the hospital on multiple occasions with symptoms of syncope, nausea, vomiting, bradycardia, hypotensive shock. The patient also experienced ventricular tachycardia, a prolonged QTc of 527 ms and QRS interval of 170 ms, frequent premature ventricular contractions, and subsequent cardiac arrest and death (elevated loperamide blood concentration of 32 ng/ml). 54 year old misused loperamide hydrochloride (up to 144 mg per day) as a self-treatment for chronic diarrhea for over 2 years. Signs of cardiac toxicity included syncope, prolonged QT of 500 ms sinus arrest with junctional escape rhythm, and polymorphic ventricular tachycardia, which required cardioversion and implantable cardioverter-defibrillator (ICD) management. 26 year old, with prior opioid abuse, presented to the hospital with recurrent syncope and developed Torsades de Pointes requiring electrical cardioversion. An ECG revealed a sinus rhythm with a heart rate of 85 bpm and a markedly prolonged QTc interval of greater than 700 ms. The patient reported ingesting 100 to 250 mg of loperamide hydrochloride with 400 mg of cimetidine daily for several months to simulate the euphoric sensation associated with opioids. Management Consider loperamide as a possible cause of cardiac arrhythmias in patients who may have a history of opioid abuse or recent ingestion of unknown drugs and in the differential diagnosis of unstable arrhythmias, prolonged QTc or QRS intervals, and Torsades de Pointes. If loperamide-induced cardiac toxicity is suspected, promptly discontinue the drug and initiate therapy to manage and prevent cardiac arrhythmias and serious outcomes. In many cases of loperamide overdosage, anti-arrhythmic medications (e.g., magnesium sulfate) were ineffective in resolving the arrhythmias and preventing further episodes of Torsades de Pointes. Electrical cardioversion and overdrive pacing, and isoproterenol continuous infusion were reported to manage QTc prolongation in the setting of overdose. Laboratory Testing Loperamide serum concentrations are not widely available or clinically useful to guide patient management. CNS and Respiratory Depression Symptoms Cases of loperamide overdose (including relative overdose due to hepatic dysfunction), may cause opioid toxic effects including CNS depression (e.g. altered mental status, stupor, coordination disorders, somnolence, miosis, muscular hypertonia, respiratory depression), hypotension, urinary retention, and paralytic ileus. Pediatric patients may be more sensitive to CNS effects, including respiratory depression, than adults. Management Loperamide non-cardiac arrhythmia overdosages should be treated as opioid overdosages. Naloxone may reverse the opioid-related toxicity, including CNS and respiratory depression, and hypotension, associated with loperamide overdosage. In adults and pediatric patients, naloxone may be administered intravenously. Appropriate doses of naloxone, via intranasal, intramuscular, intraosseus, or subcutaneous administration may be necessary if the intravenous route is not available. If the desired degree of opioid-related toxicity counteraction and improvement are not obtained, naloxone may be repeated at two- to three-minute intervals. If no response in opioid-related effects is observed after naloxone has been administered, then diagnosis of opioid-induced toxicity should be questioned. Refer to the naloxone prescribing information for complete information on initial and subsequent dosages. For patients whose adverse reactions are responsive to naloxone, monitor vital signs, neurologic and cardiopulmonary status for recurrence of opioid overdose symptoms for at least 24 hours after the last dose of naloxone, due to the prolonged intestinal retention of loperamide and the short duration (one to three hours) of naloxone. Patients with severe CNS or respiratory depression, and those who require multiple doses of naloxone to reverse symptoms, should be admitted to the hospital and may require intensive care. Laboratory Testing Standard drug screens for opioids do not include an assay for loperamide; such testing for opioids will yield negative results even in the presence of loperamide.
Uses
Use controls symptoms of diarrhea, including Travelers' Diarrhea
Dosage forms & strengths
Directions drink plenty of clear fluids to help prevent dehydration caused by diarrhea find right dose on chart. If possible, use weight to dose; otherwise, use age. adults and children 12 years and over 2 caplets after the first loose stool; 1 caplet after each subsequent loose stool; but no more than 4 caplets in 24 hours children 9-11 years (60-95 lbs) 1 caplet after the first loose stool; 1/2 caplet after each subsequent loose stool; but no more than 3 caplets in 24 hours children 6-8 years (48-59 lbs) 1 caplet after the first loose stool; 1/2 caplet after each subsequent loose stool; but no more than 2 caplets in 24 hours children 2-5 years (34-47 lbs) ask a doctor children under 2 years (up to 33 lbs) do not use
Ingredients
Active ingredient (in each caplet) Loperamide HCl 2 mg
Inactive ingredients corn starch, D&C yellow #10 aluminum lake, dibasic calcium phosphate dihydrate, FD&C blue #1 aluminum lake, magnesium stearate, microcrystalline cellulose, silicon dioxide
All identified pills
Side effects
Clinical Trial Experience The adverse effects reported during clinical investigations of loperamide hydrochloride are difficult to distinguish from symptoms associated with the diarrheal syndrome. Adverse experiences recorded during clinical studies with loperamide hydrochloride were generally of a minor and self-limiting nature. They were more commonly observed during the treatment of chronic diarrhea. The adverse events reported are summarized irrespective of the causality assessment of the investigators. 1) Adverse events from 4 placebo-controlled studies in patients with acute diarrhea The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on loperamide hydrochloride as on placebo, are presented in the table below. Acute Diarrhea Loperamide Hydrochloride Placebo No. of treated patients 231 236 Gastrointestinal AE% Constipation 2.6% 0.8% The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on loperamide hydrochloride, were: dry mouth, flatulence, abdominal cramp and colic. 2) Adverse events from 20 placebo-controlled studies in patients with chronic diarrhea The adverse events with an incidence of 1.0% or greater, which were reported at least as often in patients on loperamide hydrochloride as on placebo, are presented below in the table below. Chronic Diarrhea Loperamide Hydrochloride Placebo No. of treated patients 285 277 Gastrointestinal AE% Constipation 5.3% 0.0% Central and peripheral nervous system AE% Dizziness 1.4% 0.7% The adverse events with an incidence of 1.0% or greater, which were more frequently reported in patients on placebo than on loperamide hydrochloride were: nausea, vomiting, headache, meteorism, abdominal pain, abdominal cramp and colic. 3) Adverse events from seventy-six controlled and uncontrolled studies in patients with acute or chronic diarrhea The adverse events with an incidence of 1.0% or greater in patients from all studies are given in the table below. Acute Diarrhea Chronic Diarrhea All Studiesa No. of treated patients 1913 1371 3740 Gastrointestinal AE% 0.7% 3.2% 1.8% Nausea Constipation 1.6% 1.9% 1.7% Abdominal cramps 0.5% 3.0% 1.4% a. All patients in all studies, including those in which it was not specified if the adverse events occurred in patients with acute or chronic diarrhea. Postmarketing Experience The following adverse events have been reported: Cardiac disorders QT/QTc interval prolongation, Torsades de Pointes, other ventricular arrhythmias, cardiac arrest, syncope, and death (see WARNINGS, OVERDOSAGE). Skin and subcutaneous tissue disorders Rash, pruritus, urticaria, and angioedema and extremely rare cases bullous eruption including erythema multiforme, Stevens-Johnson syndrome and Toxic Epidermal Necrolysis have been reported with use of loperamide hydrochloride. Immune system disorders Isolated occurrences of allergic reactions and in some cases severe hypersensitivity reactions including anaphylactic shock and anaphylactoid reactions have been reported with the use of loperamide hydrochloride. Gastrointestinal disorders Dry mouth, abdominal pain, distention or discomfort, nausea, vomiting, flatulence, dyspepsia, constipation, paralytic ileus, megacolon; including toxic megacolon (see CONTRAINDICATIONS, WARNINGS). Renal and urinary disorders Urinary retention Nervous system disorders Drowsiness, dizziness General disorders and administrative site conditions Tiredness A number of the adverse events reported during the clinical investigations and post-marketing experience with loperamide are frequent symptoms of the underlying diarrheal syndrome (abdominal pain/discomfort, nausea, vomiting, dry mouth, tiredness, drowsiness, dizziness, constipation, and flatulence). These symptoms are often difficult to distinguish from undesirable drug effects.