Adult: As oral solution: Initially, 4-8 mg daily in divided doses, may be adjusted depending on the severity. Doses may be given bid when patient’s daily maintenance dose is established. Max: 16 mg daily.
Oral Acute diarrhoea
Adult: As cap, orodispersible tab: Initially, 4 mg, followed by 2 mg after each loose stool. Usual dose: 6-8 mg daily. Max: 12 mg daily. As oral solution: Initially, 4 mg, followed by 2 mg after each loose stool. Max dose: 16 mg daily. Investigate cause of diarrhoea if clinical improvement is not observed within 2 days. Child: As cap, orodispersible tab: ≥12 years Same as adult dose. As oral solution: 4-8 years 1 mg 3 or 4 times daily for up to 3 days. >8-12 years 2 mg 4 times daily for up to 5 days. Investigate cause of diarrhoea if clinical improvement is not observed within 2 days.
Administration
May be taken with or without food.
Contraindications
Conditions when peristalsis inhibition should be avoided (e.g. constipation, abdominal distension, ileus). Acute ulcerative colitis, acute dysentery characterised by bloody stools and high fever, bacterial enterocolitis caused by Salmonella, Shigella, and Campylobacter; antibiotic-associated colitis, abdominal pain without diarrhoea. Children <4 years (oral solution); <12 years (cap, orodispersible tab); <18 years (patient with irritable bowel syndrome).
Special Precautions
Patients with AIDS, glaucoma, urinary bladder neck obstruction, pyloric obstruction, significant gastric retention, or intestinal statis, risk factors for QT interval prolongation (e.g. congenital long QT syndrome, history of cardiac arrhythmias or other heart conditions, electrolyte abnormalities). Not recommended for long-term treatment. Hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Ileus, constipation, abdominal distension, abdominal pain, bloody stool, syncope, ventricular tachycardia. Eye disorders: Rarely, miosis. Gastrointestinal disorders: Flatulence, nausea, dyspepsia, dry mouth, vomiting. General disorders and admin site conditions: Rarely, fatigue. Immune system disorders: Rarely, urticaria, angioedema. Musculoskeletal and connective tissue disorders: Hypertonia. Nervous system disorders: Headache, dizziness, somnolence, stupor, depressed level of consciousness, loss of consciousness, coordination abnormality. Renal and urinary disorders: Rarely, urinary retention. Skin and subcutaneous tissue disorders: Rash. Rarely, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis. Potentially Fatal: Megacolon, toxic megacolon, cardiac events e.g. QT interval and QRS complex prolongation, torsades de pointes, cardiac arrest. Rarely, anaphylaxis and anaphylactic shock.
This drug may cause dizziness, drowsiness, or tiredness, or depressed level of consciousness, if affected, do not drive or operate machinery.
MonitoringParameters
Assess for the cause of diarrhoea prior to treatment. Monitor for signs of CNS toxicity (in patients with hepatic impairment).
Overdosage
Symptoms: CNS depression (stupor, coordination abnormality, somnolence, miosis, muscular hypertonia and respiratory depression), constipation, urinary retention, ileus, or cardiac events like syncope, QT interval and QRS complex prolongation, torsades de pointes, other serious ventricular arrhythmias, and cardiac arrest. Management: If vomiting has occurred spontaneously, administration of activated charcoal. If vomiting has not occurred, may perform gastric lavage followed by administration of activated charcoal through gastric tube. Administer repeated treatment of naloxone as an antidote if CNS symptoms occur. Monitor patient closely for at least 48 hours to detect possible CNS depression.
Drug Interactions
Increased plasma concentrations with quinidine, ritonavir, gemfibrozil, ketoconazole, and itraconazole. May increase plasma levels of oral desmopressin. May enhance the QTc prolongation and ventricular arrhythmia of QT-prolonging agents.
Action
Description: Loperamide, an opioid agonist, binds to the opioid receptor directly in the gut wall on the circular and longitudinal intestinal muscles thereby, reduces propulsive peristalsis and prolong transit time, and enhances resorption of water and electrolytes. It also increases the tone on the anal sphincter. Pharmacokinetics: Absorption: Poorly absorbed in the gastrointestinal tract. Bioavailability: Approx 0.3%. Time to peak plasma concentration: 2.5 (oral solution); approx 5 hours (cap). Distribution: Poorly distributed into the brain. Enters breast milk (small amounts). Plasma protein binding: Approx 95%, mainly to albumin. Metabolism: Almost completely metabolised in the liver via oxidative N-demethylation mainly by CYP2C8 and CYP3A4 isoenzymes, and to a lesser extent by CYP2B6 and CYP2D6 isoenzymes to form desmethylloperamide. Undergoes significant first-pass effect. Excretion: Mainly via faeces (as unchanged drug and metabolites); urine. Elimination half-life: Approx 10 hours.
Chemical Structure
Loperamide Source: National Center for Biotechnology Information. PubChem Database. Loperamide, CID=3955, https://pubchem.ncbi.nlm.nih.gov/compound/Loperamide (accessed on Jan. 22, 2020)
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