ATC categoryGastroenterology. Hepatology
Each capsule contains:
active ingredient: loperamide hydrochloride – 2 mg;
excipients: microcrystalline cellulose, sodium starch glycolate, magnesium stearate.
Loperamide binds to the opiate receptor in the gut wall, reducing propulsive peristalsis and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter.
In a double blind randomised clinical trial in 56 patients with acute diarrhoea receiving loperamide, onset of anti-diarrhoeal action was observed within one hour following a single 4 mg dose. Clinical comparisons with other antidiarrhoeal drugs confirmed this exceptionally rapid onset of action of loperamide.
About 40% of a dose of loperamide is reported to be absorbed from the gastrointestinal tract to undergo first-pass metabolism in the liver and excretion in the faeces via the bile as inactive conjugate; there is slight urinary excretion. Little intact drug reaches the systemic circulation. The elimination half-life is reported to be about 10 hours.
In acute diarrhoea the usual initial dose for adults is loperamide hydrochloride 4 mg followed by 2 mg after each loose stool to a maximum of 16 mg daily; the usual daily dose is 6 to 8 mg.
Child 8–12 years – 2 mg 4 times daily for up to 5 days.
Child 12–18 years initially 4 mg, then 2mg after each loose stool for up to 5 days (usual dose 6–8 mg daily; max. 16 mg daily).
Abdominal pain or bloating, nausea, constipation, dry mouth, dizziness, fatigue, and hypersensitivity reactions including skin rashes have been reported. Loperamide has been associated with paralytic ileus, particularly in infants and young children, and deaths have been reported. Depression of the CNS, to which children or those with hepatic impairment may be more sensitive, may be seen in overdosage; constipation and urinary retention also occur.
• patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients.
• children less than 4 years of age.
Loperamide should not be used when inhibition of peristalsis is to be avoided, in particular where ileus or constipation occur, and should be avoided in patients with abdominal distension, acute inflammatory bowel disease, or antibiotic-associated colitis. Loperamide should not be used alone in patients with dysentery.
Loperamide should be used with caution in patients with hepatic impairment because of its considerable first-pass metabolism in the liver. It should also be used with caution in young children because of a greater variability of response in this age group.
Pregnancy and lactation
Safety in human pregnancy has not been established although studies in animals have not demonstrated any teratogenic effects. As with other drugs, it is not advisable to administer Loperamide in pregnancy.
Small amounts of loperamide may appear in human breast milk. Therefore, Loperamide 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.
Use in elderly
No dose adjustment is required for the elderly.
No dose adjustment is required for patients with renal 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.
Effects on ability to drive and use machines
Tiredness, dizziness, or drowsiness may occur when diarrhoea is treated with Loperamide. Therefore, it is advisable to use caution when driving a car or operating machinery.
In case of overdose the following effects may be observed: constipation, urinary retention, ileus and neurological symptoms (miosis, muscular hypertonia, somnolence and bradypnoea). If intoxication is suspected, naloxone may be given as an antidote. Since the duration of action of loperamide is longer than that of naloxone, the patient should be kept under constant observation for at least 48 hours in order to detect any possible depression of the central nervous system. Children, and patients with hepatic dysfunction, may be more sensitive to CNS effects. Gastric lavage, or induced emesis and or enema or laxatives may be recommended.
Loperamide may increase the gastrointestinal absorption of desmopressin.
The capsules have a brown body and a pink cap, and cotains white or off white, odorless granules.
1 blister packet with 10 capsules in the cardboard box.
3 years. Do not use after the expiration date.
To be dispensed without prescription.
Store at a room temperature (15-250C), in a dry place, out of the reach of children. Protect from light.