Racecadotril

Oral
Acute diarrhoea
Adult: As cap: Initially, 100 mg to be taken regardless of the time of the day, then 100 mg tid, preferably before main meals. Continue treatment until 2 normal stools are recorded. Max duration of treatment: 7 days. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Child: In combination with oral rehydration: As granules/powder for oral susp: Recommended dose: 1.5 mg/kg tid. Max: Approx 6 mg/kg daily. Usual doses: Infants (>3 months) <9 kg: 10 mg; 9-<13 kg: 20 mg; Children 13-27 kg: 30 mg; >27 kg: 60 mg. All doses to be taken tid. Continue treatment until 2 normal stools are recorded. Max duration of treatment: 7 days. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Granules/ powder for oral susp: May be taken with or without food. May be added to food or dispersed in a glass of water or in the feeding bottle. Mix well & take immediately after prep. Powder may be administered directly into mouth.
Cap: May be taken with or without food. Swallow whole, do not open/break/chew. Administer initial cap at any time of the day. Subsequent cap, preferably taken prior to meals.

Diarrhoea associated with fever and/or bloody or purulent stools; antibiotic-associated diarrhoea. Patients who have experienced angioedema with ACE inhibitors.

Patient with history of angioedema of any other aetiology. Administer racecadotril in combination with rehydration therapy. Avoid use in case of prolonged vomiting. Concomitant use with ACE inhibitors. Renal and hepatic impairment; avoid use in children with hepatic or renal impairment. Infants and children.

Significant: Hypersensitivity or angioedema. Nervous system disorders: Headache. Respiratory, thoracic and mediastinal disorders: Tonsillitis (particularly in infants or children). Skin and subcutaneous tissue disorders: Rash, erythema nodosum, erythema multiforme, urticaria, papular rash, prurigo, pruritus.
Potentially Fatal: Rarely, severe skin reactions.

May increase the risk of angioedema with ACE inhibitors (e.g. captopril, enalapril).

Delayed peak activity by 1-1.5 hours when given with food.

Racecadotril is a prodrug of thiorphan, which is an inhibitor of enkephalinase, a cell membrane peptidase enzyme that aids in the hydrolysis of exogenous peptides and the breakdown of endogenous peptides (e.g. enkephalins). Inhibition of enkephalinase enzymatic degradation prolongs peptide action at enkephalinergic synapses in the small intestine and decreases hypersecretion without affecting basal secretion.
Duration: Enkephalinase inhibition: Approx 8 hours.
Absorption: Rapidly absorbed. Delayed time to peak activity by 1-1.5 hours with food.
Distribution: Plasma protein binding: 90%, mainly to albumin (thiorphan).
Metabolism: Rapidly hydrolysed to thiorphan glycine (active metabolite), which is further metabolised to inactive metabolites.
Excretion: Mainly via urine (81.4%); faeces (approx 8%); as active and inactive metabolites. Elimination half-life: Approx 3 hours (racecadotril).

Oral: Store below 30°C.

Antidiarrheals

A07XA04 - racecadotril ; Belongs to the class of other antidiarrheals.