Loperamide, 2 mg capsules

Drug formCapsules

ATC categoryGastroenterology. Hepatology

ATC subcategoryAntidiarrheals

Brand nameLoperamide

Generic nameLoperamide


Each capsule contains:

active ingredient: loperamide hydrochloride – 2 mg;

excipients: microcrystalline cellulose, sodium starch glycolate, magnesium stearate.

Pharmacological group and ATC code
Antiperistaltic antidiarrhea agent; A07DA03.
Chemical name and CAS number
4-(4-p-Chlorophenyl-4-hydroxypiperidino)-NN-dimethyl-2,2-diphenylbutyramide hydrochloride;

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.

Uses and administration
Loperamide is a synthetic derivative of pethidine that inhibits gut motility and may also reduce gastrointestinal secretions. It is given by mouth as an antidiarrhoeal drug as an adjunct in the management of acute and chronic diarrhoeas and may also be used in the management of colostomies or ileostomies to reduce the volume of discharge.

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.

Acute diarrhoea

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).

Adverse effects

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.

Loperamide is contraindicated in:

  • 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.

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.

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.

Drug interactions

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.

Expiry date

3 years. Do not use after the expiration date.

Prescription status

To be dispensed without prescription.

Storage conditions

Store at a room temperature (15-250C), in a dry place, out of the reach of children. Protect from light.