Contraindications
Hypersensitivity to the active substance or any of the excipients.
Patients who have developed angioedema while using angiotensin-converting enzyme inhibitors (such as captopril, enalapril, lisinopril, perindopril, ramipril) should not use racecadotril.
Due to the presence of sucrose, Hydrasec is contraindicated for use in patients with rare hereditary fructose intolerance, glucose-galactose malabsorption syndrome or sucrase-isomaltase deficiency.
Mode of application
Hydrasec is used orally with oral medications to restore water balance.
Hydrasec, 10 mg granules, is used for children weighing up to 13 kg.
Hydrasec, 30 mg granules, is used for children weighing over 13 kg.
The recommended dose is calculated by body weight: 1.5 mg/kg body weight 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 weighing from 9 kg to 13 kg – 2 sachets (10 mg) 3 times a day.
Children weighing from 13 kg to 27 kg - 1 sachet (30 mg) 3 times a day.
Children weighing over 27 kg – 2 sachets (30 mg) 3 times a day.
In clinical studies involving children, the duration of treatment was 5 days.
Treatment should be continued until 2 cases of normal stool are recorded.
The duration of treatment should not exceed 7 days.
Long-term treatment with racecadotril is not recommended.
Clinical studies have not been conducted in children under 3 months of age.
Hydrasec granules can be added to food, dissolved in a glass of water or in a feeding bottle, stirring well. After this, the drug should be used immediately.
Hidrasec
Suction
After oral administration, racecadotril is rapidly absorbed. The time until plasma enkephalinase inhibition begins is 30 minutes.
Eating does not affect the bioavailability of racecadotril, but after eating, the drug's activity appears with a delay of approximately one and a half hours.
Distribution
In the blood plasma, after the use of racecadotril, labeled with the radioactive isotope 14C, the radiocarbon content was many times higher than in blood cells, and 3 times higher than in whole blood. Thus, the drug slightly binds to blood cells. Radiocarbon is moderately distributed in other tissues of the body, as evidenced by its apparent volume of distribution in plasma of 66.4 kg. 90% of the active metabolite of racecadotril, (thiorphan) ((RS)-N-(1-oxo-2-(mercaptomethyl)-3-phenylpropyl) glycine), is bound to plasma proteins, predominantly albumin. The pharmacokinetic properties of racecadotril do not change as a result of repeated doses, or when administered to elderly patients.
The duration and effectiveness of racecadotril depend on the dose of the drug. In adults, the time to peak inhibition of plasma enkephalinase is approximately 2 hours and corresponds to 75% inhibition at a dose of 100 mg.
The inhibition time of plasma enkephalinase is approximately 8 hours.
Metabolism
The biological half-life of racecadotril, measured as plasma enkephalinase inhibition time, is approximately 3 hours.
Racecadotril is rapidly hydrolyzed to thiorphan, an active metabolite, which in turn is transformed into inactive metabolites. Taking repeated doses of racecadotril does not lead to its accumulation in the body. Data obtained from in vitro studies indicate that racecadotril/thiorphan and the four major inactive metabolites do not inhibit the CYP enzyme isoforms (3A4, 2D6, 2C9, 1A2 and 2C19) to an extent that may be clinically significant.
Data obtained from in vitro studies indicate that racecadotril/thiorphan and the four major inactive metabolites do not induce CYP enzyme isoforms (ZA, 2A6, 2B6, 2C9/2C19, 1A, 2E1) and uridine glucuronosyltransferase conjugate enzymes (UGTs) to a degree which may be clinically significant.
Racecadotril does not affect the protein binding of active substances such as tolbutamide, warfarin, niflumic acid, digoxin or phenytoin.
In patients with hepatic impairment (Child-Pugh class B), the kinetic profile of the active metabolite racecadotril showed similar Tmax (time to maximum blood concentration) and T1/2 (half-life) and lower Cmax (maximum blood concentration) values. (-65%) and AUC (area under the concentration-time curve) (-29%) compared with these indicators in healthy people.
In patients with severe renal impairment (creatinine clearance 11-39 ml/min), the kinetic profile of the active metabolite racecadotril demonstrated a lower Cmax (-49%) and higher AUC (+16%) and T1/2 compared to healthy volunteers ( creatinine clearance >70 ml/min.).
Cmax is reached 2 hours 30 minutes after application.
No accumulation was observed when the drug was repeated every 8 hours for 7 days.
Removal
Racecadotril is excreted from the body in the form of active and inactive metabolites primarily through the kidneys, and to a much lesser extent in the feces. Excretion through the lungs is negligible.
Features of application
The use of the drug Hydrasec does not change the usual regime for restoring water balance.
Diabetes patients should note that each sachet contains:
Hydrasec, granules 10 mg - 0.966 g of sucrose;
Hydrasec, granules 30 mg - 2.899 g of sucrose.
If the amount of sucrose (sources of glucose and fructose) in the daily dose of Hydrasec exceeds 5 g per day, this should be taken into account in the daily sugar intake.
The drug should not be used in infants under 3 months of age as clinical studies have not been conducted in this population.
Use during pregnancy or breastfeeding
There are no adequate data on the use of racecadotril in pregnant women. Animal studies do not indicate any direct or indirect harmful effects on pregnancy, embryofetal development, labor or postnatal development. However, since no specific clinical studies have been conducted, racecadotril should not be used during pregnancy.
Due to insufficient information about the excretion of Hydrasec into breast milk, it should not be used during breastfeeding.
Children
Hydrasec, 10 mg granules, is used for infants and children from 3 months to 2 years.
Hydrasec, 30 mg granules, is used for children over 2 years old.
The ability to influence the reaction rate when driving vehicles or other mechanisms
Racecadotril has no or negligible effect on the ability to drive and operate machinery.
Gidrasec Instructions for use
Pharmacodynamics
Racecadotril is a prodrug that is hydrolyzed to its active metabolite, thiorphan, which is an inhibitor of enkephalinase, a surface peptidase (located on the cell membrane) localized in various tissues, especially the epithelium of the small intestine. This enzyme is responsible for both the hydrolysis of exogenous peptides and the breakdown of endogenous peptides such as enkephalins. As a result, racecadotril protects endogenous enkephalins, which exhibit physiological activity at the level of the digestive tract, prolonging their antisecretory effect.
Racecadotril is an intestinal antisecretory substance. It reduces intestinal hypersecretion of water and electrolytes caused by cholera enterotoxin or inflammation and does not affect basal intestinal secretion.
Racecadotril has a rapid antidiarrheal effect without altering the transit time of intestinal contents through the intestines.
Racecadotril has a rapid antidiarrheal effect without altering the transit time of intestinal contents through the intestines.
Racecadotril does not cause bloating.
In clinical studies, the incidence of secondary constipation with racecadotril was comparable to placebo.
Pharmacokinetics
Suction
After oral administration, racecadotril is rapidly absorbed. The time until plasma enkephalinase inhibition begins is 30 minutes.
Eating does not affect the bioavailability of racecadotril, but after eating, the drug's activity appears with a delay of approximately one and a half hours.
Distribution
In the blood plasma, after the use of racecadotril, labeled with the radioactive isotope 14C, the radiocarbon content was many times higher than in blood cells, and 3 times higher than in whole blood. Thus, the drug slightly binds to blood cells. Radiocarbon is moderately distributed in other tissues of the body, as evidenced by its apparent volume of distribution in plasma of 66.4 kg. 90% of the active metabolite of racecadotril, (thiorphan) ((RS)-N-(1-oxo-2-(mercaptomethyl)-3-phenylpropyl) glycine), is bound to plasma proteins, predominantly albumin. The pharmacokinetic properties of racecadotril do not change as a result of repeated doses, or when administered to elderly patients.
The duration and effectiveness of racecadotril depend on the dose of the drug. In adults, the time to peak inhibition of plasma enkephalinase is approximately 2 hours and corresponds to 75% inhibition at a dose of 100 mg.
The inhibition time of plasma enkephalinase is approximately 8 hours.
In patients with hepatic impairment (Child-Pugh class B), the kinetic profile of the active metabolite racecadotril showed similar Tmax and T½ and lower Cmax (- 65%) and AUC (area under the concentration-time curve) (-29%) compared with these indicators in healthy people.
In patients with severe renal impairment (creatinine clearance 11-39 ml/min), the kinetic profile of the active metabolite racecadotril demonstrated a lower Cmax (-49%) and higher AUC (+16%) and T½ compared with healthy volunteers (clearance creatinine >70 ml/min).
Cmax is achieved 2 hours 30 minutes after application.
No accumulation was observed when the drug was repeated every 8 hours for 7 days.
Removal
Racecadotril is excreted from the body in the form of active and inactive metabolites primarily through the kidneys, and to a much lesser extent in the feces. Excretion through the lungs is negligible.
Overdose
Isolated cases of overdose without adverse reactions have been reported in infants and children. The doses taken were 7 times higher than the required dose.
In adults, single doses of more than 2 g, that is, 20 times the therapeutic dose, did not cause harmful effects.
Interaction with other drugs and other types of interactions
Angiotensin-converting enzyme inhibitors (such as captopril, enalapril, lisinopril, fosinopril, perindopril, ramipril) can cause angioedema. This risk may be increased in the presence of racecadotril.
Concomitant use of racecadotril with loperamide or nifuroxazide in humans does not alter the kinetics of racecadotril.
Description of the drug HIDRASEK®
After oral administration, racecadotril is rapidly absorbed. The time until plasma enkephalinase inhibition begins is 30 minutes. Cmax is achieved 2.5 hours after application. Eating does not affect the bioavailability of racecadotril, but after ingestion the activity of the drug appears with a delay of approximately 1.5 hours.
In the blood plasma after the use of racecadotril, labeled with the radioactive isotope 14C, the radiocarbon content was many times higher than in blood cells and 3 times higher than in whole blood. Thus, the drug slightly binds to blood cells. Radiocarbon is moderately distributed in other tissues of the body, as evidenced by the apparent plasma Vd of 66.4 kg. 90% of the active metabolite of racecadotril (thiorphan) ((RS)-N(1-oxo-2-(mercaptomethyl)-3-phenylpropyl) glycine) is bound to plasma proteins, mainly albumin.
When taking racecadotril at a dose of 100 mg, the time of peak inhibition of plasma enkephalinase is approximately 2 hours and corresponds to 75% inhibition. The duration and effectiveness of racecadotril depends on the dose. In adults, the time to peak inhibition of plasma enkephalinase is approximately 2 hours and corresponds to 75% inhibition at a dose of 100 mg. Plasma enkephalinase inhibition time is approximately 8 hours.
Racecadotril is rapidly hydrolyzed to thiorphan, an active metabolite, which in turn is transformed into inactive metabolites. Taking repeated doses of racecadotril does not lead to its accumulation in the body. Data obtained from in vitro studies indicate that racecadotril/thiorphan and the four major inactive metabolites do not inhibit the CYP enzyme isoforms (3A4, 2D6, 2C9, 1F2, and 2C19) to an extent that may be clinically significant. Data obtained from in vitro studies indicate that racecadotril/thiorphan and the four major inactive metabolites do not induce CYP enzyme isoforms (3A, 2A6, 2B6 2C9/2C19, 1A, 2E1) and conjugated uridine glucuronyl transferase enzymes (UGTs) to an extent that may be clinically significant.
The biological T1/2 of racecadotril, measured as the inhibition time of plasma enkephalinase, is approximately 3 hours. Racecadotril is excreted from the body in the form of active and inactive metabolites, primarily by the kidneys, and to a much lesser extent in the feces. Excretion through the lungs is negligible.
In patients with hepatic impairment (Child-Pugh class B), the kinetic profile of the active metabolite racecadotril demonstrated similar Tmax and T1/2 and lower Cmax (-65%) and AUC (-29%) compared with those in healthy people.
In patients with severe renal impairment (creatinine clearance 11–39 ml/min), the kinetic profile of the active metabolite racecadotril demonstrated a lower Cmax (-49%) and higher AUC (+16%) and T1/2 compared to healthy volunteers ( CC >70 ml/min).
Adverse reactions
Infections and infestations – uncommon: tonsillitis.
Skin and subcutaneous tissue disorders: uncommon: rash, erythema. Frequency unknown: erythema multiforme, swelling of the tongue, swelling of the face, swelling of the lips, swelling of the eyelids, angioedema, urticaria, erythema nodosum, papular rash, prurigo, pruritus.
Severe skin reactions (including angioedema) have been reported in patients treated with racecadotril. The incidence of these reactions is unknown, but if they occur, racecadotril treatment should be discontinued and appropriate alternative therapy should be instituted. In these cases, patients should be informed to avoid repeated doses of racecadotril.
Note!
Description of the drug Hydrasec gran. d/oral. susp. 10 mg sachet No. 16 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
