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Pharmacological properties

racecadotril is a prodrug that requires hydrolysis to form an active metabolite of tiorphan, which is an inhibitor of enkephalinase, a peptidase of cell membranes that is located in different tissues, especially in the epithelium of the small intestine. this enzyme promotes both the hydrolysis of exogenous and the cleavage of endogenous peptides such as enkephalins. thus, racecadotril protects endogenous enkephalins, physiologically active at the level of the digestive tract, prolonging their antisecretory function.

Racecadotril is an antisecretory substance that acts exclusively in the intestinal mucosa. It reduces intestinal hypersecretion of water and electrolytes caused by cholera toxins or inflammation, and does not affect basal secretory activity. Racecadotril exhibits rapid antidiarrheal action without changing the duration of intestinal transit.

Racecadotril does not cause bloating. In clinical trials, the incidence of secondary constipation with racecadotril was similar to that observed in the placebo group.

When administered orally, the drug exhibits exclusively peripheral activity, without affecting the central nervous system.

In two clinical trials in children, racecadotril reduced stool weight during the first 48 hours by 40 and 46%, respectively. There was also a significant decrease in the duration of diarrhea and the need to restore water balance.

In a meta-analysis of individual patient data (9 randomized clinical trials of racecadotril compared with placebo, in addition to oral rehydration solution), individual patient data were collected (1384 boys and girls) with acute diarrhea of ​​varying severity who were hospitalized or outpatient. The average age was 12 months (interquartile latitude - from 6 to 39 months). Of these, 714 patients were under the age of 1 year, 670 patients - under the age of 1 year. The average body weight fluctuated during the study from 7.4 to 12.2 kg. The total average duration of diarrhea after inclusion was 2.81 days in the placebo group and 1.75 days in the racecadotril group. The percentage of patients who recovered was higher in the racecadotril groups compared with placebo [Hazard Ratio (HR): 2.04; 95% CI: 1.85 to 2.32; p0.001; Cox Proportional Hazards Regression]. The results were very similar for infants (1 year old) (HR: 2.01; 95% CI: 1.71 to 2.36; p0.001) and preschool children (1 year old) (HR: 2.16; 95 % CI: 1.83 to 2.57; p0.001). For inpatients (n = 637), the ratio of the average stool mass in the racecadotril group to that in the placebo group was 0.59 (95% CI: 0.51 to 0.74); p0.001). For outpatients (n = 695), the ratio of the average number of bowel movements for diarrhea in the racecadotril group to that for diarrhea in the placebo group was 0.63 (95% CI: from 0.47 to 0.85); p0.001).

Pharmacokinetics

Suction. Racecadotril is rapidly absorbed after oral administration. The initial time to inhibition of plasma enkephalinase is 30 minutes. The bioavailability of racecadotril does not change as a result of eating, but reaching maximum activity is delayed by about 1.5 hours.

Distribution. Following an oral dose of labeled 14With racecadotril, the measured concentration of the radioactive carbon isotope in blood plasma was many orders of magnitude higher than in blood cells, and 3 times higher than in the entire blood volume. Thus, the drug does not significantly bind to blood cells. The distribution of the radioactive isotope of carbon in other tissues of the body is moderate, which proves the average apparent distribution volume in plasma is 66.4 kg.

90% of the active metabolite of racecadotril, tiorphan (= (RS) -N- (1-oxo-2- (mercaptomethyl) -3-phenylpropyl) glycine) binds to blood plasma proteins, mainly albumin.The pharmacokinetic properties of racecadotril do not change with repeated use or when used in elderly patients.

The duration and extent of action of the racecadotril is dose dependent.

In children, the time to peak suppression of plasma enkephalinase is approximately 2 hours and corresponds to 90% suppression when taking a dose of 1.5 mg / kg body weight. In adults, the time to peak suppression of plasma enkephalinase is approximately 2 hours and corresponds to a 75% suppression when taking a dose of 100 mg.

The duration of plasma enkephalinase suppression is about 8 hours.

Metabolism. Biological T½ racecadotril, based on the degree of inhibition of plasma enkephalinase, is approximately 3 hours

Racecadotril is rapidly hydrolyzed to tiorphan, an active metabolite, which, in turn, turns into inactive metabolites.

Repeated use of racecadotril does not lead to the accumulation of compounds in the body.

In vitro data indicate that racecadotril / tiorphan and 4 major inactive metabolites do not inhibit the major CYP enzyme isoforms 3A4, 2D6, 2C9, 1A2 and 2C19 to a clinically significant degree.

In vitro data indicate that racecadotril / tiorphan and 4 major inactive metabolites do not stimulate CYP enzyme isoforms (3A class, 2A6, 2B6, 2C9 / 2C19, class 1A, 2E1) and UGT conjugating enzymes to a clinically significant degree.

Racecadotril does not affect protein binding of active substances that are significantly associated with proteins, such as tolbutamide, warfarin, niflumic acid, digoxin or phenytoin.

In patients with impaired liver function [cirrhosis, grade B according to the Child-Pugh classification], the kinetics profile of the active metabolite of racecadotril was observed Tmax and T½similar to those noted in healthy volunteers, but less Cmax (–65%) and AUC (–29%).

In patients with severe renal failure (creatinine clearance 11–39 ml / min), the kinetics profile of the active metabolite of racecadotril was noted to be lowermax (–49%) and large values ​​of AUC (+ 16%) and T½than in healthy volunteers (creatinine clearance 70 ml / min).

In children, pharmacokinetic parameters are similar to those in adults, reaching Cmax 2.5 hours after administration. No accumulation is observed after repeated doses every 8 hours for 7 days.

Racecadotril is excreted in the form of both active and inactive metabolites. The drug is excreted mainly by the kidneys, to a much lesser extent - with feces. Pulmonary excretion is negligible.

Indications

Auxiliary symptomatic treatment of acute diarrhea in infants (from the age of 3 months) and children in combination with oral rehydration and the usual supportive measures, when only these measures are not enough to control the clinical condition, and in the case when etiotropic treatment is impossible.

If etiotropic treatment is possible, racecadotril can be used as adjunctive therapy.

Application

Hidrasec is administered orally along with oral restoration of the water balance (see special instructions).

Hidrasec 10 mg is used in children weighing up to 13 kg.

The recommended dose is calculated by body weight: 1.5 mg / kg per dose. This amounts to 1-2 sachets of the appropriate dosage, which are taken 3 times a day at regular intervals.

Children weighing up to 9 kg: 1 sachet (10 mg) 3 times a day.

Children with a body weight of 9 to 13 kg: 2 sachets (10 mg) 3 times a day.

Children with a body weight of 13 to 27 kg: 1 sachet (30 mg) 3 times a day.

Children weighing 27 kg or more: 2 sachets (30 mg) 3 times a day.

In clinical trials involving children, the duration of treatment was 5 days.

Treatment should be continued until 2 cases of the normal nature of the stool are recorded.

The duration of treatment should not exceed 7 days.

Long-term treatment with racecadotril is not recommended.

Clinical studies involving children under 3 months of age have not been conducted.

Special patient groups.A study involving infants or children with renal or hepatic insufficiency has not been conducted (see SPECIAL INSTRUCTIONS).

Use the drug with caution in patients with renal or hepatic insufficiency.

Hidrasec granules can be added to food, dissolved in a glass of water or in a bottle for feeding, mixing well. After this, the drug should be used immediately.

Contraindications

Hypersensitivity to the active substance or to any of the excipients.

Due to the presence of sucrose, Hidrasec is contraindicated in patients with rare hereditary fructose intolerance, glucose-galactose malabsorption syndrome, or sucrose-isomaltase deficiency.

Patients who develop angioedema with ACE inhibitors should not use racecadotril.

Side effects

The following are adverse reactions to the drug, which were noted in the racecadotril group more often than in the placebo group, or registered in the post-registration period. by frequency, adverse reactions were divided into: very often (≥1 / 10), often (≥1 / 100 to 1/10), infrequently (≥1 / 1,000 to 1/100), rarely (≥1 / 10,000 to 1 / 1000), very rarely (1/10 000), of unknown frequency (it is impossible to determine from the available data).

Infections and infestations: infrequently - tonsillitis.

Disorders from the skin and subcutaneous tissue: infrequently - rash, erythema; unknown frequency - polymorphic erythema, swelling of the tongue, swelling of the face, swelling of the lips, swelling of the eyelids, angioedema, urticaria, erythema nodosum, papular rash, prurigo, itching.

special instructions

The use of the drug Hidrasec does not change the usual regime of restoring water balance.

Restoring water balance is extremely important in the treatment of acute diarrhea in children. To restore the water balance and the way to achieve it, it is necessary to take into account the patient’s age and body weight, as well as the condition and severity of the patient, especially in case of severe or prolonged diarrhea, accompanied by significant vomiting or loss of appetite. It is also important not to interrupt regular meals (including breastfeeding) and to control the intake of a sufficient amount of fluid.

Bloody or purulent stools and fever may indicate either the presence of invasive bacteria as the cause of diarrhea, or another serious illness requiring etiotropic treatment (e.g. antibiotics) or further investigation. Therefore, racecadotril should not be used in such cases. Racecadotril can be used with antibiotics in case of acute diarrhea of ​​bacterial etiology as an additional therapy.

The use of racecadotril in case of diarrhea caused by antibiotic treatment and chronic diarrhea is not recommended due to insufficient data.

Diabetes patients should consider that each sachet contains:

Hidrasec 10 mg: 0.966 g of sucrose;

30 mg Hidrasec: 2.899 g of sucrose.

If the amount of sucrose (a source of glucose and fructose) in the daily dose of Hidrasec exceeds 5 g / day, this should be taken into account in the daily sugar diet.

The drug should not be used in newborns under the age of 3 months, since clinical studies have not been conducted in this population.

The drug should not be used in children with impaired renal or hepatic function of any severity due to limited information on this population.

Due to a possible decrease in bioavailability, the drug should not be used in case of prolonged or uncontrolled vomiting.

Use during pregnancy and lactation

Pregnancy. There is no adequate data on the use of racecadotril in pregnant women. Animal studies do not indicate the presence of direct or indirect harmful effects on the course of pregnancy, embryofetal development, the course of childbirth or postnatal development.However, since no special clinical studies have been conducted, racecadotril should not be used during pregnancy.

Lactation. Due to insufficient information on the release of the drug Hidrasec into breast milk, it should not be used during lactation.

Children. Hidrasec, granules of 10 mg, are used in infants and children aged 3 months to 2 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Racecadotril does not affect or has a slight effect on the ability to drive a car and work with mechanisms.

Interactions

Interactions with other drugs in humans have not been recorded to date. the simultaneous use of racecadotril with loperamide or nifuroxazide in humans does not change the kinetics of racecadotril.

Overdose

Cases of overdose are not registered. in adults, single doses of more than 2 g, that is, 20 times the therapeutic dose, did not cause negative effects.

Storage conditions

At a temperature not exceeding 25 ° c. Keep out of the reach of children.

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