Each capsule also contains the following excipients: Lactose, maize starch, magnesium stearate and colloidal anhydrous silica. The capsule contains gelatin, titanium dioxide (E171) and yellow iron oxide (E172).
Pharmacology: Hidrasec is an inhibitor of enkephalinase, the enzyme responsible for breaking down enkephalins. It is a selective but reversible inhibitor and protects endogenous enkephalins which are physiologically active in the digestive tract.
Hidrasec is a pure intestinal antisecretory agent which has been shown to have no effect on gastrointestinal motility. It reduces intestinal hypersecretion of water and electrolytes caused by cholera toxin or inflammation without affecting basal secretion. There is therefore no effect in the normal intestine.
When given orally, enkephalinase inhibition is purely peripheral. Hidrasec does not affect central nervous system enkephalinase activity and has not been shown to produce habituation or central nervous stimulant or sedative effects.
Pharmacokinetics: Racecadotril is rapidly absorbed by the oral route. It is rapidly hydrolyzed to (RS)-N-[1-oxo-2-(mercaptomethyl)-3-phenylpropyl] glycine, its active metabolite, which is in turn converted into inactive metabolites which are eliminated through the kidneys, feces and lungs.
The extent and duration of action of racecadotril depends on the dose administered.
Activity against plasma enkephalinase starts within 30 min, with peak activity corresponding to 75% inhibition for a dose of 100 mg, occurring 1-3 hrs after administration. The biological half-life of racecadotril is 3 hrs. For a dose of 100 mg, the duration of activity against plasma enkephalinase is about 8 hrs.
(RS)-N-[1-oxo-2-(mercaptomethyl)-3-phenylpropyl] glycine, the active metabolite of racecadotril, is 90% bound to plasma proteins, mainly albumin. Tissue distribution only affects about 1% of the administered dose.
The pharmacokinetic properties of racecadotril are not changed by repeated administration or in elderly subjects. The bioavailability of racecadotril is not affected by food but the peak activity is delayed by 1½ hrs.
Toxicology: Preclinical Safety Data: No further information of relevance.
Adjunct treatment for adult diarrhea patient when oral rehydration therapy is not sufficient.
Hidrasec should be given in conjunction with oral or parenteral rehydration therapy in patients where dehydration has occurred or is suspected. Treatment should be initiated with a single 100 mg capsule given regardless of time. Further treatment is given approximately 8 hourly until cessation of diarrhea.
Individual doses of 2 g, ie 20 times the therapeutic dose for the treatment of acute diarrhea, have been administered in clinical trials without causing any harmful effects. No incident of accidental overdosage has been reported. No specific antidote has been identified, and management should follow recognized procedures for overdose.
Known hypersensitivity to racecadotril. In the absence of specific studies: Pregnancy and lactation.
HIDRASEC capsules are not recommended for use in children under 15 years. If the diarrhea persists for more than 3 days and in the case of severe diarrhea, the presence of blood in stool, fever or vomiting, further observation and evaluation is necessary.
In the absence of specific studies, Hidrasec is contraindicated during pregnancy and lactation.
A few cases of drowsiness have been reported during clinical trials. Nausea and vomiting, constipation, dizziness, headache and skin rash have also been reported rarely. The side-effects have been mild, and equivalent in nature, frequency and intensity to those reported to with placebo. Post marketing surveillance has indicated side-effects are extremely rare in general use.
No specific studies in humans have been performed. Racecadotril does not inhibit or induce Cytochrome P450 in animal models.
A07XA04 - racecadotril ; Belongs to the class of other antidiarrheals.