Professional view

loperamide hydrochloride: prescribing and clinical use

Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.

loperamide hydrochloride: clinical details

Prescribing considerations

Treatment is symptomatic: assess the likely cause and address fluid and electrolyte depletion.
Investigate persistent or changing diarrhoea rather than continuing empirical antimotility treatment.
Use cautiously in hepatic impairment because reduced first-pass metabolism may increase systemic and CNS effects.
Avoid excessive supply or use in people at risk of misuse; very high exposure is associated with serious cardiac toxicity.
Licensing and minimum age differ between products, so verify the selected preparation's SmPC.

Contraindications and cautions

Hypersensitivity to loperamide or formulation excipients.
Acute dysentery with blood in stools and fever.
Acute ulcerative colitis.
Enterocolitis caused by invasive bacteria such as Salmonella, Shigella or Campylobacter.
Pseudomembranous colitis associated with broad-spectrum antibiotics.
Any situation where suppressing peristalsis risks ileus, megacolon or toxic megacolon.

Monitoring

Hydration status and electrolyte replacement needs.
Stool frequency and consistency, abdominal distension, constipation and signs of ileus.
New alarm features or failure of the clinical pattern to improve.
CNS toxicity in hepatic impairment or suspected overdose.
ECG and close observation following significant overdose or cardiac symptoms.

Clinical pharmacology

A peripherally acting opioid-receptor agonist that reduces propulsive peristalsis and gastrointestinal secretion while increasing transit time, water absorption and anal sphincter tone. Extensive hepatic first-pass metabolism, involving CYP3A4 and CYP2C8, keeps systemic availability low; loperamide is also a P-glycoprotein substrate.

Formulation and product differences

Selected products include hard capsules, standard tablets and orodispersible tablets.
Capsules require liquid; orodispersible tablets dissolve on the tongue and can be swallowed without liquid.
Some capsules and standard tablets contain lactose.
Orodispersible products contain aspartame and differ in flavouring and other excipients; check suitability in phenylketonuria and relevant excipient sensitivities.
The score line on the selected standard tablet facilitates swallowing and is not intended to produce equal portions.
Selected consumer-oriented products license acute diarrhoea from age 12 and IBS diarrhoea in adults; the selected prescription tablet has different age and chronic-diarrhoea indications.