Hydrasek - instructions for use, doses, side effects, contraindications

Active substanceRacecadotrilRacecadotril

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Hydrasuke

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Abbott Laboratories, GmbH Germany

Diasek®

capsules inwards

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Dosage form: & nbspcapsules

Composition:

1 capsule contains:

Active substance: racecadotril - 100 mg.

Excipients: lactose monohydrate 41 mg, corn starch pregelatinized - 78 mg, magnesium stearate - 4 mg, silicon dioxide colloidal - 2 mg.

Hard gelatin capsule: ferric oxide yellow (E 172) 0.10%, titanium dioxide (E 171) 2.0%, gelatin to 100%.

Description:Hard gelatin capsules No. 2 of light yellow color. The contents of the capsules are a white powder with a characteristic odor.

Pharmacotherapeutic group:Antidiarrhoeic remedy

ATX: & nbsp

A.07.X.A.04 Racecadotril

Pharmacodynamics:

Racecadotril is a prodrug that is hydrolyzed to its active metabolite, thiophan, an inhibitor of enkephalinase, a surface peptidase (located on the cell membrane), localized in various tissues, especially in the epithelium of the small intestine. This enzyme is responsible simultaneously for the hydrolysis of exogenous peptides and for the cleavage of endogenous peptides, such as enkephalins. As a result, racecadotril protects endogenous enkephalins, which show physiological activity at the level of the digestive tract, prolonging their antisecretory action.

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 changing the transit time of intestinal contents through the intestine.

Racecadotril does not cause bloating.

In clinical studies, the incidence of secondary constipation when taking racecadotril was comparable to placebo.

Pharmacokinetics:

Suction

After oral administration racecadotril quickly absorbed. The time to initiation of inhibition of plasma enkephalinase is 30 minutes.

Eating does not affect the bioavailability of racecadotril, but after eating, the activity of the drug manifests itself with a delay of approximately one and a half hours.

Distribution

In plasma, after the use of radecadotrial radecadotril ¹⁴C, the content of radiocarbon 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 volume of its distribution in the plasma at a rate of 66.4 kg. 90% of the active metabolite racecadotril, (thiophane) ((RS) -N- (1-oxo-2- (mercaptomethyl) -3-phenylpropyl) glycine) binds to plasma proteins, mainly albumin. Racecadotril pharmacokinetic properties are not changed as a result of receiving repeated doses, and when assigning elderly patients.

The duration and effectiveness of the action of racecadotril depends on the dose of the drug. In adults, the time to peak plasma inhibiting enkephalinase is about 2 hour and 75 corresponds% inhibition when receiving a dose of 100 mg.

The inhibition time of plasma enkephalinase is approximately 8 hours.

Metabolism

The biological half-life of racecadotril, measured as the inhibition of plasma enkephalinase, is approximately 3 hours.

Racecadotril is rapidly hydrolyzed to thiorphan, the active metabolite, which is, in turn, is transformed into inactive metabolites. Reception of repeated doses of racecadotril does not lead to its accumulation in the body.Data from research in vitro, show that racecadotril / thiophane and the four major inactive metabolites do not inhibit the isoforms of the CYP enzyme (3A4, 2D6, 2C9, 1A2 and 2C19) to a degree that can be clinically significant.

Data from research in vitro, show that racecadotril / thiophane and the four major inactive metabolites do not induce isoforms of the CYP enzyme (3A, 2A6, 2B6, 2C9 / 2C19, 1A, 2E1) and conjugated enzymes of uridyllucuronosyltransferase (UGTs) to a degree that may be clinically significant.

Racecadotril does not affect the protein binding of such active substances as tolbutamide, warfarin, niflumic acid, digoxin or phenytoin.

In patients with hepatic insufficiency (class B according to the Child-Pugh classification), the kinetic profile of the active metabolite of racecadotril showed similar T_max (time to reach the maximum concentration in the blood) and T_1/2(half-life) and lower C_max (maximum concentration in the blood) (-65%) and AUC (area under the concentration-time curve) (-29%) compared to those in healthy people.

In patients with severe renal failure (creatinine clearance 11-39 ml / min), the kinetic profile of the active metabolite of racecadotril showed a lower C_max (-49%) and a higher AUC (+ 16%) and T_1/2compared with healthy volunteers (creatinine clearance> 70 ml / min.).

FROM_max is reached after 2 hours 30 minutes after application.

No cumulation was observed with repeated administration of the drug every 8 hours for 7 days.

Excretion

Racecadotril is excreted from the body in the form of active and inactive metabolites mainly through the kidneys, and much less - with feces. Excretion through the lungs is insignificant.

Indications:

Symptomatic treatment of acute diarrhea in adults.

Contraindications:

1 Hypersensitivity to the active substance or any other component of the drug.

2 Congenital intolerance of galactose, insufficiency of lactase, glucose-galactose malabsorption syndrome (due to the fact that the preparation contains lactose).

3 Pregnancy and the period of breastfeeding.

4 Children under 18 years of age (due to high content of active substance).

Pregnancy and lactation:

Pregnancy

Sufficient data on the use of racecadotril by pregnant women are not available. In animal studies, there were no direct or indirect adverse effects in terms of pregnancy, embryonic development, delivery, or postpartum development. However, due to the lack of clinical data, do not use Hydrasek during pregnancy.

Breastfeeding period

Due to the lack of information on the excretion of racecadotril into breast milk, do not use Hydrasek during breastfeeding.

Dosing and Administration:

For oral administration. The first capsule at the beginning of treatment is taken irrespective of the time of day. Next - one capsule three times a day before meals. Treatment should be continued until normalization of the stool (the appearance of normal feces up to two times), but not more than 7 days. It is not recommended to apply racecadotril a long time.

Special patient groups

Elderly patients: dosage adjustment for elderly patients is not required.

Side effects:

Reports of the following adverse reactions were noted when taking racecadotril more often,than when taking placebo or were received in the post-marketing period:

Disturbances from the nervous system

Often (≥ 1/100, <1/10): headache.

Disturbances from the skin and subcutaneous tissues

Infrequently (≥ 1/1000, <1/100): skin rash, erythema.

The frequency is unknown (to assess the frequency of cases, the available data is not enough): erythema polymorph, tongue edema, edema of the face, edema of the lips, edema of the eyelids, angioedema, urticaria, erythema nodosum, papular rash, prurigo, skin itch, toxic dermatitis.

Overdose:

At present, isolated cases of overdose without side effects are known.

In adults, taking a single dose of the drug more than 2 g, equivalent to a 20-fold therapeutic dose, did not cause adverse effects.

Interaction:

Currently, there is no data on interactions with other drugs. Loperamide or nifuroxazide does not affect the kinetics of racecadotril in the joint use of these drugs.

Special instructions:

The use of Hydrasek does not relieve oral rehydration when it is needed.

The presence of bloody or purulent discharge in the stool and high fever mayserve as symptoms of an invasive bacterial infection that caused diarrhea, or other serious disease, which is the basis for etiotropic therapy (for example, using antibiotics) or further research. Monotherapy with racecadotril for these conditions is contraindicated. As an additional therapy for acute bacterial diarrhea racecadotril can be used in conjunction with antibiotics.

Due to insufficient data, it is not recommended to use racecadotril with antibiotic-associated diarrhea and chronic diarrhea.

Due to insufficient data racecadotril should be used with caution in patients with renal and hepatic insufficiency.

The bioavailability of racecadotril can be reduced by repeated vomiting.

Effect on the ability to drive transp. cf. and fur:

The use of Hydrazec is not affected or has little effect on the ability to drive and machines.

Form release / dosage:

Capsules, 100 mg.

Packaging:

10 capsules per blister of PVC / PVDC / Al foil. For 1.2 blisters per pack of cardboard along with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004150

Date of registration:21.02.2017

Expiration Date:21.02.2022

The owner of the registration certificate:Abbott Laboratories, GmbHAbbott Laboratories, GmbH Germany

Manufacturer: & nbsp

SOPHARTEX France

Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia

Information update date: & nbsp21.03.2017

Illustrated instructions

Instructions

Hydrasuke (Hidrasec)