Diasek® (Diasec)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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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:

    Active substance: racecadotril - 100 mg;

    Excipients: corn starch, lactose monohydrate, silicon dioxide colloid (aerosil), talc;

    capsules, hard gelatinous: body and cap capsule - titanium dioxide, dye quinoline yellow, dye sunset yellow, gelatin.

    Description:

    Hard gelatin capsules No. 1 with a body and a lid of yellow color. The contents of capsules are white or almost white powder.

    Pharmacotherapeutic group:Antidiarrhoeic remedy
    ATX: & nbsp

    A.07.X.A.04   Racecadotril

    Pharmacodynamics:

    Racecadotril is a prodrug that is hydrolyzed to an 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 of 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.

    When receiving racecadotril 100 mg the peak plasma inhibiting enkephalinase is about 2 hour and 75 corresponds% inhibition. 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 enzyme isoforms CYP (3A4, 2D6, 2C9, 1F2, 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 enzyme isoforms CYP (3A, 2A6, 2B6 2C9 / 2C19, 1A, 2E1) and conjugated enzymes of uridine glucuronisyltransferase (UGTs) to a degree that can 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 indices TmOh (time to reach the maximum concentration in the blood) and T1 / 2 (half-life) and lower CmOh (maximum concentration in the blood), (-65%) and AUC (the 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 CmOh (-49%) and a higher indicator AUC (+ 16%) and T1 / 2 compared to healthy volunteers (creatinine clearance> 70 ml / min).

    FROMmOh 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:

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

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

    - Pregnancy and the period of breastfeeding.

    - 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 on pregnancy, embryonic development, delivery and postpartum development. However, due to the lack of clinical data, do not use Disek® during pregnancy.

    Breastfeeding period

    Due to the lack of information on the excretion of racecadotril into breast milk, do not use Diasek® 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 continue 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

    Older patients: correction of the dose of the drug for elderly patients is not required.

    Side effects:

    Reports of the following adverse reactions were noted with the use of racecadotril more often than with placebo or were received during the post-marketing period:

    Impaired nervous system: often (≥1 / 100, <1/10): headache.

    Disturbances from the skin and subcutaneous tissues: infrequently (≥1 / 1000, <1/100): skin rash, erythema; frequency is unknown (to assess the frequency of the available data is not enough): polymorphic erythema, edema of the tongue, 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 do not affect the kinetics of racecadotril in the joint use of these drugs.

    Special instructions:

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

    The presence of bloody or purulent discharge in the stool and high fever can serve as symptoms of an invasive bacterial infection that has caused diarrhea or other serious illness, 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 Diasek® does not affect or has a negligible effect on the ability to drive and operate machinery.
    Form release / dosage:Capsules, 100 mg.
    Packaging:

    By 9, 10, 18 or 20 capsules in a contour cell package from the film polyvinylchloride and aluminum foil printed lacquered.

    By 1, 2, 3, 4, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    Storage conditions:

    At a temperature of no higher than 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-004565
    Date of registration:29.11.2017
    Expiration Date:29.11.2022
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.01.2018
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