Imodium

Loperamide HCl (Imodium) is a white powder filled in capsules with green cap and dark gray body.
Each capsule contains: Loperamide (as HCl) 2 mg.

Loperamide HCl (Imodium) is indicated for the symptomatic control of acute and chronic diarrhea. In patients with an ileostomy, it can be used to reduce the number and volume of stools and to harden their consistency.

Adults and pediatrics: Acute diarrhea: The initial dose is 2 capsules (4 mg) for adults and 1 capsule (2 mg) for children; followed by 1 capsule (2 mg) after every subsequent loose stool.
Chronic diarrhea: The initial dose is 2 capsules (4 mg) daily for adults and 1 capsule (2 mg) daily for children; this initial dose should be adjusted until 1-2 solid stools a day are obtained, which is usually achieved with a maintenance dose of 1-6 capsules (2 mg-12 mg) daily.
The maximum dose for acute and chronic diarrhea is 8 capsules (16 mg) daily for adults; in children it must be related to the body weight (3 capsules/20 kg) but should not exceed a maximum of 8 capsules per day.
Pediatrics (under 2 years of age): Loperamide HCl should not be used in children under 2 years of age.
Elderly: No dose adjustment is required for the elderly.
Renal impairment: No dose adjustment is required for patients with renal impairment.
Hepatic impairment: Although no pharmacokinetic data are available in patients with hepatic impairment, Loperamide HCl should be used with caution in such patients because of reduced first-pass metabolism.
Administration: The capsules should be taken with liquid.
What should the patient do if they miss a dose: Continue medication based on dosage and/or consult a doctor.

Signs and symptoms: In case of overdose (including relative overdose due to hepatic dysfunction), CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia, and respiratory depression), urinary retention and ileus may occur. Children may be more sensitive to CNS effects than adults.
In individuals who have intentionally ingested overdoses (reported in doses from 40 mg up to 792 mg per day) of loperamide HCl, QT interval and QRS complex prolongation and/or serious ventricular arrhythmias, including Torsade de Pointes, have been observed. Fatal cases have also been reported. Abuse, misuse and/or overdose with excessively large doses of loperamide, may unmask Brugada syndrome. Upon cessation, cases of drug withdrawal syndrome have been observed in individuals abusing, misusing or intentionally overdosing with excessively large doses of Loperamide.
Treatment: In cases of overdose, ECG monitoring for QT interval prolongation should be initiated.
If CNS symptoms of overdose occur, naloxone can be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone (1 to 3 hours), repeated treatment with naloxone might be indicated. Therefore, the patient should be monitored closely for at least 48 hours in order to detect possible CNS depression.
What to do when the patient has taken more than the recommended dosage: Consult a doctor if the patient has taken more than the recommended dosage.

Loperamide HCl is contraindicated in patients with a known hypersensitivity to Loperamide HCl or to any of the excipients.
Loperamide HCl should not be used in children under 2 years of age.
Loperamide HCl should not be used as the primary therapy: In patients with acute dysentery, which is characterized by blood in stools and high fever; in patients with acute ulcerative colitis; in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter; in patients with pseudomembranous colitis associated with the use of broad-spectrum antibiotics.
Loperamide HCl should not be used when inhibition of peristalsis is to be avoided due to the possible risk of significant sequelae including ileus, megacolon and toxic megacolon. Loperamide HCl must be discontinued promptly when constipation, abdominal distension or ileus develop.

Treatment of diarrhea with Loperamide HCl is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate.
In patients with diarrhea, especially in children, fluid and electrolyte depletion may occur. In such cases administration of appropriate fluid and electrolyte replacement therapy is the most important measure.
Loperamide HCl should not be given to children aged 2 to 6 years of age without medical prescription and supervision.
In acute diarrhea, if clinical improvement is not observed within 48 hours, the administration of Loperamide HCl should be discontinued and patients should be advised to consult their physician.
Patients with AIDS treated with Loperamide HCl for diarrhea should have therapy stopped at the earliest signs of abdominal distension. There have been isolated reports of obstipation with an increased risk for toxic megacolon in AIDS patients with infectious colitis from both viral and bacterial pathogens treated with Loperamide HCl.
Although no pharmacokinetic data are available in patients with hepatic impairment, Loperamide HCl should be used with caution in such patients because of reduced first-pass metabolism. This medicine must be used with caution in patients with hepatic impairment as it may result in a relative overdose leading to CNS toxicity.
Abuse and misuse of Loperamide, as an opioid substitute, have been described in individuals with opioid addiction.
When should the patient consult a doctor: If symptoms persist or worsen, or if new symptoms occur, stop use and consult a doctor.
Effects on Ability to Drive and Use Machines: Tiredness, dizziness, or drowsiness may occur in the setting of diarrheal syndromes treated with Loperamide HCl. Therefore, it is advisable to use caution when driving a car or operating machinery.

Pregnancy and Breast-feeding: It is not advisable to administer this medicine in pregnancy. Women who are pregnant or breast-feeding should therefore be advised to consult their doctor for appropriate treatment.

Clinical trial data: Adults and pediatrics: Acute diarrhea: Adverse effects associated with the use of Loperamide HCl are headache, constipation, flatulence, nausea, dizziness, dry mouth, abdominal pain, abdominal discomfort, abdominal pain upper, abdominal distention, rash, vomiting and somnolence.
Chronic diarrhea: Adverse effects associated with the use of Loperamide HCl are dizziness, flatulence, constipation, nausea, headache, abdominal pain, dry mouth, abdominal discomfort and dyspepsia.
Post-Marketing Data: Adverse effects associated with the use of Loperamide HCl are hypersensitivity reaction, anaphylactic reaction (including anaphylactic shock) and anaphylactoid reaction, coordination abnormality, depressed level of consciousness, hypertonia, loss of consciousness, somnolence, stupor, miosis, ileus (including paralytic ileus), megacolon (including toxic megacolon), angioedema, bullous eruption (including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme), pruritus, urticaria, urinary retention and fatigue.

Non-clinical data have shown that loperamide is a P-glycoprotein substrate. Concomitant administration of loperamide (16 mg single dose) with quinidine, or ritonavir, which are both P-glycoprotein inhibitors, resulted in a 2- to 3-fold increase in loperamide plasma levels. The clinical relevance of this pharmacokinetic interaction with P-glycoprotein inhibitors, when loperamide is given at recommended dosages, is unknown.
The concomitant administration of loperamide (4 mg single dose) and itraconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 3- to 4-fold increase in loperamide plasma concentrations. In the same study a CYP2C8 inhibitor, gemfibrozil, increased loperamide by approximately 2-fold. The combination of itraconazole and gemfibrozil resulted in a 4-fold increase in peak plasma levels of loperamide and a 13-fold increase in total plasma exposure. These increases were not associated with CNS effects as measured by psychomotor tests (i.e., subjective drowsiness and the Digit Symbol Substitution Test). The concomitant administration of loperamide (16 mg single dose) and ketoconazole, an inhibitor of CYP3A4 and P-glycoprotein, resulted in a 5-fold increase in loperamide plasma concentrations. This increase was not associated with increased pharmacodynamic effects as measured by pupillometry. Concomitant treatment with oral desmopressin resulted in a 3-fold increase of desmopressin plasma concentrations, presumably due to slower gastrointestinal motility.
It is expected that drugs with similar pharmacological properties may potentiate loperamide's effect and that drugs that accelerate gastrointestinal transit may decrease its effect.

Store at temperatures not exceeding 30°C.

Antidiarrheals

A07DA03 - loperamide ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.

Non-Rx