Active ingredient: Loperamide hydrochloride 2 mg.
Excipients/Inactive Ingredients: Lactose monohydrate, maize starch, talc, magnesium stearate, empty capsule.
Components of empty capsule: Gelatin, FD&C Blue 1, Quinoline Yellow, FD&C Yellow 6, Titanium Dioxide, FD&C Red 40, printing ink.
Components of printing ink (WHITE SB-0007P): Shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, sodium hydroxide, povidone, titanium dioxide.
For the symptomatic treatment of acute diarrhoea in adults and children aged 12 years and over.
For the symptomatic treatment of acute episodes of diarrhoea associated with Irritable Bowel Syndrome (IBS) in adults aged 18 years and over following initial diagnosis by a doctor.
Administration: Oral use. The capsules should be taken with liquid.
Dosage: Acute diarrhoea: Adults and children over 12: 2 capsules (4 mg) initially followed by 1 capsule (2 mg) after every loose stool. The maximum daily dose should not exceed 6 capsules (12 mg).
Symptomatic treatment of acute episodes of diarrhoea associated with Irritable Bowel Syndrome (IBS) in adults aged 18 years and over: Two capsules (4 mg) to be taken initially, followed by 1 capsule (2 mg) after every loose stool, or as previously advised by the doctor. The maximum daily dose should not exceed 6 capsules (12 mg).
Paediatric population: Loperamide is contraindicated in children less than 12 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 should be used with caution in such patients because of reduced first pass metabolism.
Symptoms: In case of overdose (including relative overdose due to hepatic dysfunction), CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia and respiratory depression), constipation, urinary retention and ileus may occur. Children, and patients with hepatic dysfunction, may be more sensitive to CNS effects.
In individuals who have ingested overdoses of loperamide HCl, cardiac events such as QT interval prolongation, torsades de pointes, other serious ventricular arrhythmias, cardiac arrest and syncope have been observed. Fatal cases have also been reported. Overdose can unmask existing Brugada syndrome.
Management: In cases of overdose, Electrocardiogram (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.
This medicine is contraindicated: Hypersensitivity to the active substance or to any of the excipients; In children less than 12 years of age; In patients with acute dysentery, which is characterised 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 must 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 must be discontinued promptly when ileus, constipation or abdominal distension develop.
Only take this medicine to treat acute episodes of diarrhoea associated with IBS if the doctor has previously diagnosed IBS.
If any of the following now apply, do not use the product without first consulting the doctor, even if aware of having IBS: If aged 40 or over and it is some time since the last IBS attack; If aged 40 or over and the IBS symptoms are different this time; If recently passed blood from the bowel; If suffering from severe constipation; If feeling sick or vomiting; If lost appetite or lost weight; If having difficulty or pain passing urine; If with fever; If recently travelled abroad.
Consult the doctor if new symptoms develop, or if symptoms worsen, or the symptoms have not improved over two weeks.
Treatment of diarrhoea with loperamide is only symptomatic. Whenever an underlying etiology can be determined, specific treatment should be given when appropriate. The priority in acute diarrhoea is the prevention or reversal of fluid and electrolyte depletion. This is particularly important in young children and in frail and elderly patients with acute diarrhoea. Use of this medicine does not preclude the administration of appropriate fluid and electrolyte replacement therapy.
Since persistent diarrhoea can be an indicator of potentially more serious conditions, this medicine should not be used for prolonged periods until the underlying cause of the diarrhoea has been investigated.
In acute diarrhoea, if clinical improvement is not observed within 48 hours, the administration of loperamide should be discontinued and patients should be advised to consult their doctor.
Patients with AIDS treated with this medicine for diarrhoea 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 hydrochloride.
Although no pharmacokinetic data are available in patients with hepatic impairment, this medicine should be used with caution in such patients because of reduced first pass metabolism, as it may result in a relative overdose leading to central nervous system (CNS) toxicity.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine because it contains lactose.
If patients are taking this medicine to control episodes of diarrhoea associated with Irritable Bowel Syndrome (IBS) previously diagnosed by their doctor, and clinical improvement is not observed within 48 hours, the administration of loperamide HCl should be discontinued and they should consult with their doctor. Patients should also return to their doctor if the pattern of their symptoms changes or if the repeated episodes of diarrhoea continue for more than two weeks.
Cardiac events including QT prolongation and torsades de pointes have been reported in association with overdose. Some cases had a fatal outcome. Patients should not exceed the recommended dose and/or the recommended duration of treatment.
Effects on ability to drive and use machines: Loss of consciousness, depressed level of consciousness, tiredness, dizziness, or drowsiness may occur when diarrhoea is treated with this medicine. Therefore, it is advisable to use caution when driving a car or operating machinery.
Pregnancy: Safety in human pregnancy has not been established, although from animal studies there are no indications that loperamide HCl possesses any teratogenic or embryotoxic properties. As with other drugs, it is not advisable to administer this medicine in pregnancy, especially during the first trimester.
Lactation: Small amounts of loperamide may appear in human breast milk. Therefore, this medicine is not recommended during breast-feeding.
Women who are pregnant or breast feeding infants should therefore be advised to consult their doctor for appropriate treatment.
The frequency categories use the following convention: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); and very rare (<1/10,000).
Common: Nervous system disorders: Headache.
Gastrointestinal disorders: Constipation, nausea, flatulence.
Uncommon: Nervous system disorders: Dizziness, somnolence.
Gastrointestinal disorders: Abdominal pain, abdominal discomfort, dry mouth, abdominal pain upper, vomiting, dyspepsia.
Skin and subcutaneous tissue disorders: Rash.
Rare: Immune system disorders: Hypersensitivity reaction, anaphylactic reaction (including anaphylactic shock), anaphylactoid reaction.
Nervous system disorders: Loss of consciousness, stupor, depressed level of consciousness, hypertonia, coordination abnormality.
Eye disorders: Miosis.
Gastrointestinal disorders: Ileus (including paralytic ileus), megacolon (including toxic megacolon), abdominal distension.
Skin and subcutaneous tissue disorders: Bullous eruption (including Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme), angioedema, urticaria, pruritus.
Renal and urinary disorders: Urinary retention.
General disorders and administration site conditions: 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 in a well-closed container, in a dry place. Do not store above 30°C.
A07DA03 - loperamide ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.
Loperamide Stella hard cap 2 mg
5 × 10's
Sign Out
