Loperamide

What is Loperamide?

• Loperamide (Imodium) is a synthetic opioid antidiarrheal for oral use.

Loperamide

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What are the uses of this medicine?

• Loperamide (Imodium) is used for the control and symptomatic relief of acute nonspecific diarrhea in patients 2 years of age and older and of chronic diarrhea in adults associated with inflammatory bowel disease.
• It is also used to reduce the amount of fluid in people with ileostomies (surgery to create an opening for waste to leave the body through the abdomen).

• Nonprescription loperamide is used to control acute diarrhea (loose stools that come on suddenly and usually lasts less than 2 weeks), including travelers' diarrhea.

How does this medicine work?

• Loperamide (loe per’ a mide) is a synthetic piperidine derivative that acts as a mild opiate receptor agonist (predominant µ type receptors), but is used largely for the treatment of diarrhea rather than pain.
• Loperamide is not structurally related to morphine or codeine and has minimal or no euphoric or analgesic effects, apparently because it is poorly absorbed orally and is actively transported out of the central nervous system.
• Loperamide acts as a potent opiate agonist in the intestine and reduces intestinal motility, causing a slowing of intestinal transport and increased resorption of water and electrolytes, actions that are helpful in treating diarrhea.

Who Should Not Use this medicine ?

This medicine cannot be used in:

• pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions.
• 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.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• antibiotics such as clarithromycin (Biaxin, in PrevPac) and erythromycin (E.E.S., Ery-Tab, Eryc, others)
• certain antifungals such as itraconazole (Onmel, Sporanox) and ketoconazole
• cimetidine (Tagamet), gemfibrozil (Lopid)
• quinine (Qualaquin), ranitidine (Zantac), ritonavir (Norvir, in Kaletra), or saquinavir (Invirase).

Is this medicine FDA approved?

• Loperamide was approved for use in the United States in 1976 and is still widely used to treat acute diarrhea caused by gastroenteritis, as well as the chronic diarrhea of inflammatory bowel disease.

How should this medicine be used?

Recommended dosage: For Acute Diarrhea:

In Adults and Pediatric Patients 13 Years and Older:

• The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool.
• The maximum daily dose is 16 mg (eight capsules).
• Clinical improvement is usually observed within 48 hours.

In Pediatric Patients 2 to 12 Years of Age:

• In pediatric patients 2 to 5 years of age (20 kg or less), the non-prescription liquid formulation of loperamide (1 mg/5 mL) should be used.
• For ages 6 to 12, either loperamide hydrochloride capsules or the non-prescription liquid formulation of loperamide may be used.

Recommended First Day Dosage Schedule:

• Two to five years (13 kg to 20 kg): 1 mg three times daily.
• Six to eight years (20 kg to 30 kg): 2 mg twice daily.
• Eight to twelve years (greater than 30 kg): 2 mg three times daily.

• Following the first treatment day, it is recommended that subsequent loperamide hydrochloride capsules doses (1 mg/10 kg body weight) be administered only after a loose stool.

For Chronic Diarrhea: In Adults:

• The recommended initial dose is 4 mg (two capsules) followed by 2 mg (one capsule) after each unformed stool until diarrhea is controlled, after which the dosage of loperamide hydrochloride capsules should be reduced to meet individual requirements.
• The average daily maintenance dosage in clinical trials was 4 mg to 8 mg (two to four capsules per day). The maximum daily dosage is 16 mg (eight capsules per day).

Administration:

• Loperamide comes as a tablet, capsule, and as a suspension or solution to take by mouth.
• If you are giving loperamide to your child, read the package label carefully to make sure that it is the right product for the age of the child. Loperamide should not be given to a child younger than 2 years of age.
• If you are taking loperamide liquid, do not use a household spoon to measure your dose. Use the measuring cup that came with the medication or use a spoon made especially for measuring liquid medication.
• If you are taking loperamide for acute diarrhea and your symptoms get worse or if your diarrhea lasts longer than 48 hours, stop taking this medication and call your doctor.
• Nonprescription loperamide usually is taken immediately after each loose bowel movement but not more than the 24-hour maximum amount described on the label.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet, capsule, and as a suspension or solution (liquid)

This medicine is available in fallowing brand namesː

• Imodium
• Imodium AD
• Imotil
• K-Pek II
• Kao-Paverin
• Kaopectate 1-D
• Maalox Anti-Diarrheal
• Pepto Diarrhea Control

What side effects can this medication cause?

The most common side effects of this medicine include:

• Constipation
• Dizziness
• nausea
• vomiting
• headache
• meteorism
• abdominal pain
• abdominal cramp
• colic

Additional side effects may include:

• Cardiac Disorders: QT/QTc-interval prolongation, Torsades de Pointes, other ventricular arrhythmias, cardiac arrest, syncope, and death.

• Skin and Subcutaneous Tissue Disorders: Rash, pruritus, urticaria, angioedema, and extremely rare cases of bullous eruption including erythema multiforme, Stevens-Johnson syndrome and Toxic Epidermal Necrolysis.

• Immune System Disorders: severe hypersensitivity reactions including anaphylactic shock and anaphylactoid reactions have been reported with the use of loperamide hydrochloride capsules.

• Gastrointestinal Disorders: Dry mouth, abdominal pain, distention or discomfort, nausea, vomiting, flatulence, dyspepsia, constipation, paralytic ileus, megacolon; including toxic megacolon.

• Renal and Urinary Disorders: Urinary retention

• Nervous System Disorders: Drowsiness, dizziness

• General Disorders and Administrative Site Conditions: Tiredness

What special precautions should I follow?

• Cases of prolongation of the QT/QTc interval, Torsades de Pointes, other ventricular arrhythmias, cardiac arrest, some resulting in death, have been reported in adults with use of higher than recommended doses per day of loperamide hydrochloride capsules.
• Loperamide hydrochloride is contraindicated in pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions. Avoid loperamide hydrochloride capsules dosages higher than recommended in adults and pediatric patients 2 years of age and older due to the risk of serious cardiac adverse reactions.
• Fluid and electrolyte depletion often occur in patients who have diarrhea. The use of loperamide hydrochloride capsules does not preclude the need for appropriate fluid and electrolyte therapy.
• Patients with AIDS treated with loperamide hydrochloride capsules for diarrhea should have therapy stopped at the earliest signs of abdominal distention.
• Treatment of diarrhea with loperamide hydrochloride capsules is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate.
• Loperamide hydrochloride capsules should be used with special caution in pediatric patients because of the greater variability of response in this age group. Dehydration, particularly in pediatric patients less than 6 years of age, may further influence the variability of response to loperamide hydrochloride capsules.
• Extremely rare allergic reactions including anaphylaxis and anaphylactic shock have been reported.
• Loperamide has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.
• Use of a higher than prescribed dosage is not recommended. Report to a healthcare facility if you or someone you are caring for taking loperamide hydrochloride capsules experiences a fainting episode, a rapid or irregular heartbeat or becomes unresponsive.
• For patients with acute diarrhea, that if clinical improvement is not observed in 48 hours, discontinue loperamide hydrochloride capsules and contact their healthcare provider.
• Advise to contact their healthcare provider if they see blood in their stools, or if they develop a fever or abdominal distention.
• Loperamide hydrochloride may make you drowsy and dizzy. Do not drive a car or operate machinery until you know how this drug affects you.

What to do in case of emergency/overdose?

Symptoms of overdosage may include: Cardiac effects:

• 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.

CNS and Respiratory Depression:

• Altered mental status, stupor, coordination disorders, somnolence, miosis, muscular hypertonia, respiratory depression, hypotension, urinary retention, and paralytic ileus.

Management of overdosage:

• 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.
• 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.
• 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.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well controlled studies in pregnant women.
• Loperamide hydrochloride capsules should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• 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.
• Loperamide hydrochloride capsules should be used with special caution in pediatric patients because of their greater variability of response. Dehydration, particularly in pediatric patients less than 6 years of age.
• The safety and effectiveness of loperamide hydrochloride capsules in pediatric patients with chronic diarrhea have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• LOPERAMIDE HYDROCHLORIDE

Inactive Ingredients:

• FERROSOFERRIC OXIDE
• SILICON DIOXIDE
• GELATIN, UNSPECIFIED
• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• MICROCRYSTALLINE CELLULOSE
• FERRIC OXIDE RED
• SODIUM LAURYL SULFATE
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• TITANIUM DIOXIDE
• FERRIC OXIDE YELLOW
• D&C YELLOW NO. 10
• FD&C BLUE NO. 1
• FD&C BLUE NO. 2
• FD&C RED NO. 40
• PROPYLENE GLYCOL
• SHELLAC

Who manufactures and distributes this medicine?

Manufactured for:

• Mylan Pharmaceuticals Inc.
• Morgantown, WV U.S.A.

Manufactured by:

• Auro PR Inc.
• RD 156 Caguas West Industrial Park, Lot 24
• Caguas, PR U.S.A.

What should I know about storage and disposal of this medication?

• Store at 20° to 25°C (68° to 77°F).
• Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

Full and partial opiod agonists:

• Alfentanil
• Butorphanol
• Codeine
• Diphenoxylate
• Fentanyl
• Heroin
• Hydrocodone
• Hydromorphone
• Levorphanol
• Loperamide
• Meperidine
• Methadone
• Morphine
• Opium
• Oxycodone
• Oxymorphone
• Pentazocine
• Remifentanil
• Sufentanil
• Tramadol

Opiate antagonists:

• Nalmefene
• Naloxegol
• Naloxone
• Naltrexone

• Dailymed label info on Loperamide
• FDA Loperamide

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