Loperamide

Registered South African indications:

• Diarrhoea

Contraindications

• Known hypersensitivity to the active ingredient or any of its excipients
• Children below 3 years  
• Acute dysentery
• Acute ulcerative colitis
• Bacterial enterocolitis caused by Salmonella, Shigella and Campylobacter
• Pseudomembranous colitis associated with the use of broad-spectrum antibiotics
• Do not use when peristalsis inhibition should be avoided due to potential for ileus, megacolon and/or toxic megacolon

Cautions

• Pregnancy
• Breastfeeding
• Hepatic impairment
• Elderly
• Fluid and electrolyte depletion
• Prolonged use
• HIV positive patients  
• Children
• Irritable bowel syndrome
• Low sodium diet (syr)
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery
• Risk for QT prolongation

Forms avail. in SA and covered in this monograph: tab, cap, syr, eft, dsp

Acute diarrhoea

• Oral (dsp, tab, eft, cap, syr): Loading dose: 4mg; Maintenance: 2mg, after each loose stool; Treatment duration: 48hrs; Max: 16mg/24hrs

Stop loperamide as soon as diarrhoea is under control

Orodispersable tablet should be placed on the tongue and allowed to dissolve

Chronic diarrhoea

• Oral (dsp, tab, eft, cap, syr): Initial: 4mg, dly; Maintenance: 2-12mg/day, in divided doses; Max: 16mg/24hrs

Individualise dose until 1-2 solid stools per day achieved

Orodispersable tablet should be placed on the tongue and allowed to dissolve

Paed. forms avail. in SA and covered in this monograph: tab, cap, syr, eft, dsp

Generally loperamide is not recommended for use in children

Acute diarrhoea

Oral (syr)

• Younger than 2 years: Not recommended for use
• Older than 2 years: Loading dose: 1mg/12.5kg; maintenance: 0.5mg/12.5kg, after each loose stool; Max: 3mg/12.5kg/24hrs; Treatment duration: 48hrs

Oral (dsp, tab)

• Younger than 6 years: Oral (tab): Not recommended for use; Oral (dsp): Contraindicated
• Between 6-12 years: Loading dose: 2mg; Maintenance: 2mg, after each loose stool; Max: Based on weight (see table)

Oral (cap)

• Younger than 6 years: Oral (cap): Not recommended for use
• Between 6-12 years: Loading dose: 2mg; Maintenance: 2mg, after each loose stool; Max: Based on weight (see table)

Oral (eft)

• Younger than 5 years: Not established for use
• Older than 5 years: Loading dose: 2mg; Maintenance: 2mg after each loose stool; Max: Based on weight (see table)

Stop loperamide as soon as diarrhoea is under control

Orodispersable tablet should be placed on the tongue and allowed to dissolve

Pregnancy

• Caution
• Safety in human pregnancy has not been established, although from animal studies there are no indications that loperamide 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

Breastfeeding

• Caution; not recommended
• Small amounts of loperamide may appear in human breast milk

Fertility

• The effect on human fertility has not been evaluated

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Somnolence
• Loss of consciousness
• Depressed level of consciousness
• Hypertonia
• Coordination abnormality
• Fatigue

Gastrointestinal Disorders

• Constipation
• Nausea and vomiting
• Flatulence
• Abdominal pain
• Dry mouth
• Dyspepsia
• Ileus 
• Megacolona
• Glossodynia
• Abdominal distension

Genitourinary Disorders

• Urinary retention

Skin and Subcutaneous Tissue Disorders

• Rash
• Bullous eruption
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis 
• Erythema multiforme
• Angioedema
• Urticaria
• Pruritus

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reaction
• Anaphylactic reaction 
• Anaphylactic shock
• Anaphylactoid reaction

Sensory Disorders

• Miosis

• P-glycoprotein inhibitors
• Itraconazole 
• Ketoconazole
• Gemfibrozil 
• Oral desmopressin
• Agents that affect intestinal motility

None routine. Specific cases may require

• Neurological examination

Tablet 2mg - EML (Primary)

Tablet melts 2mg, Capsule 2mg, Tablet effervescent 2mg, Syrup 1mg/5ml - Non-EML

Only take this medicine to treat acute episodes of diarrhoea associated with Irritable Bowel Syndrome if your doctor has previously diagnosed IBS 

If any of the following now apply, do not use the product without first consulting your doctor, even if you know you have IBS:

• If you are aged 40 or over and it is some time since your last IBS attack
• If you are aged 40 or over and your IBS symptoms are different this time
• If you have recently passed blood from the bowel
• If you suffer from severe constipation
• If you are feeling sick or vomiting 
• If you have lost your appetite or lost weight
• If you have difficulty or pain passing urine
• If you have a fever
• If you have recently travelled abroad

Loperamide binds to opiate receptors in the gut wall, reducing propulsive peristalsis, increasing intestinal transit time and enhancing resorption of water and electrolytes. Loperamide increases the tone of the anal sphincter, which helps reduce faecal incontinence and urgency.

Tablet 2mg 

• Adco-Prodium  (Adcock)
• Adco-Loperamide  (Adcock)
• Betaperamide  (Adcock)
• Cipla-loperamide (Cipla Medpro) (Discontinued: 25/08/2022)
• Dis-chem Anti-Diarrhoeal (Pharmacare)
• Gastron (Pharmacare)
• Imodium (Johnson & Johnson) originator
• Norimode (Pharmacare)

Tablet melts 2mg 

• Imodium Melts (Johnson & Johnson) originator

Tablet effervescent 2mg 

• Lopedium (Sandoz)

Capsule 2mg

• Imodium (Janssen) originator

Syrup (per 5ml) 1mg

• Adco-loperamide (Adcock)
• Gastron (Pharmacare)
• Imodium (Johnson & Johnson) originator
• Loperastat Syrup (Ranbaxy Pharmaceuticals)

COMBINATION PREPARATIONS

Loperamide/ Simethicone

Tablet 2mg/125mg

• Loperamide Plus (Johnson & Johnson) originator