Buy Diasek capsules 100mg №10
  • Buy Diasek capsules 100mg №10

Diasec capsules 100mg №10

$26.19
Quantity

  • All payments are encrypted via SSL All payments are encrypted via SSL
  • Full Refund if you haven't received your order Full Refund if you haven't received your order


Mechanism of action

Racecadotril is a prodrug that hydrolyzes to an active metabolite, thiorphan, which is an inhibitor of enkephalinase, a surface peptidase (located on the cell membrane) located in various tissues, especially in the epithelium of the small intestine. This enzyme is simultaneously responsible for the hydrolysis of exogenous peptides and for the cleavage 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 action.

Racecadotril is an intestinal antisecretory agent. Reduces intestinal hypersecretion of water and electrolytes caused by cholera enterotoxin or inflammation, and does not affect the basal secretion of the intestine.

Racecadotril has a rapid antidiarrheal effect, without changing the time of passage of intestinal contents through the intestines.

Racecadotril does not cause bloating.

In clinical trials, the incidence of secondary constipation with racecadotril was comparable to placebo.

Pharmacokinetics

Suction

After oral administration, racecadotril is rapidly absorbed. The time before the start of inhibition of plasma enkephalinase is 30 minutes.

WITHmax is achieved after 2 h 30 min after application.

Eating does not affect the bioavailability of racecadotril, but after eating, the activity of the drug is delayed by about 1.5 hours.

Distribution

In blood plasma after administration of racecadotril, labeled with a radioactive isotope14C, radiocarbon content was many times higher than in blood cells, and 3 times higher than in whole blood. Thus, the drug is slightly associated with blood cells. Radiocarbon is moderately distributed in other tissues of the body, as evidenced by apparent Vd in plasma at a rate of 66.4 kg.

90% of the active metabolite of racecadotril (tiorfan) ((RS) -N (1-oxo-2- (mercaptomethyl) -3-phenylpropyl) glycine) binds to plasma proteins, mainly albumin.

The pharmacokinetic properties of racecadotril do not change as a result of receiving repeated doses, as well as when prescribing to elderly patients.

There was no cumulation with repeated use of the drug every 8 hours for 7 days.

When receiving 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 the action 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 time of inhibition of plasma enkephalinase is approximately 8 hours.

Metabolism

Racecadotril is rapidly hydrolyzed to thiorphan, an active metabolite that, in turn, is transformed into inactive metabolites. Reception of repeated doses of racecadotril does not lead to its accumulation in the body. Data obtained from in vitro studies show that racecadadotril / thiorfan and the four major inactive metabolites do not inhibit the isoform of the CYP enzyme (3A4, 2D6, 2C9, 1F2, and 2C19) to a degree that can be clinically significant.

The data obtained from in vitro studies show that racecadadotril / thiorfan and the four main inactive metabolites do not induce CYP isoforms (3A, 2A6, 2B6 2C9 / 2C19, 1A, 2E1) and conjugated uriding glucuronyl transferase (UGTs) enzymes in the degree of uriding glucuronyl transferase (UGTs) conjugated to the conjugated uriding enzyme transferase enzymes (UGTs) to a degree of conjugated uriding glucuronisyl transferase (UGTs) enzymes in the degree of urefluorosyl transferase (UGTs) conjugated to the conjugated uriding enzyme transferase enzymes (UGTs) to the extent of conjugated uriding glucuronyl transferase (UGTs) enzymes in the degree of UFTs conjugate to the degree of conjugated enzymes Uriding glucuronyl transferase (UGTs) and conjugated enzymes of uriding glucuronyl transferase (UGTs). be clinically relevant.

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

Removal

Biological T1/2 Racecadotril, measured as the time of plasma enkephalinase inhibition, is approximately 3 h.

Racecadotril is eliminated from the body in the form of active and inactive metabolites, mainly through the kidneys, and much less with feces. Removal through the lungs is negligible.

Pharmacokinetics in special clinical situations

In patients with hepatic insufficiency (Child-Pugh class B), the kinetic profile of the active metabolite of racecadotril showed similar T values.max and t1/2 and lower C scoresmax 
(-65%) and AUC (-29%) compared with these indicators in healthy people.

In patients with severe renal insufficiency (CC 11-39 ml / min), the kinetic profile of the active metabolite of racecadotril showed a lower C index.max(-49%) and higher AUC (+ 16%) and T1/2 compared with healthy volunteers (CC> 70 ml / min).

Indications of the drug Diasec

  • symptomatic treatment of acute diarrhea in adults.

Dosage and administration

For oral administration. The first capsule at the beginning of treatment is taken regardless of the time of day. Then - 1 capsule 3 times / day before meals.

Treatment should be continued until stool normalizes (normal stool appears up to two times), but not more than 7 days. It is not recommended to use racecadotril for a long time.

Dose adjustment forelderly patients not required.

Due to insufficient data, the drug should be used with caution.in patients with renal and hepatic impairment.

Side effect

Reports of adverse reactions listed below were noted when taking racecadotril more often than taking placebo or were received during post-marketing use.

Nervous system: often (≥1 / 100, <1/10) - headache.

Dermatological:infrequently (≥1 / 1000, <1/100) - skin rash, erythema; unknown frequency (for assessing the frequency of cases of available data is not enough) - erythema multiforme, tongue swelling, swelling of the face, lip swelling, eyelid edema, angioedema, urticaria, erythema nodosum, papular rash, prurigo, skin itch, toxic dermatitis

Contraindications

  • congenital intolerance to galactose, lactase deficiency, glucose-galactose malabsorption syndrome (due to the fact that the drug contains lactose);
  • pregnancy;
  • breastfeeding period;
  • age up to 18 years (due to the high content of the active substance);
  • Hypersensitivity to the active substance or any other component of the drug.

Use during pregnancy and lactation

Sufficient data on the use of racecadotril pregnant. In animal studies, no direct or indirect adverse effects on pregnancy, fetal development, childbirth and postpartum development were found. However, due to the lack of clinical data, do not use the drug Diasec® during pregnancy.

Due to the lack of information on the allocation of racecadotril with breast milk, do not use the drug Diasec® during breastfeeding.

Application for violations of the liver

Due to the lack of data, racecadotril should be used with caution in patients with hepatic insufficiency.

Application for violations of kidney function

In connection with the insufficiency of data, racecadotril should be used with caution in patients with renal insufficiency.

Use in children

The drug is contraindicated under the age of 18 years (due to the high content of the active substance).

Use in elderly patients

Correction of the drug dose for elderly patients is not required.

Special notes

The use of the drug Diasec® does not exempt from oral rehydration in cases where it is necessary.

The presence of bloody or purulent discharge in the stool and high fever can serve as symptoms of an invasive bacterial infection that caused diarrhea or another serious illness, which is the basis for etiotropic therapy (for example, using antibiotics) or further research. Monotherapy with racecadotril in 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.

The bioavailability of racecadotril can be reduced with repeated vomiting.

Influence on ability to drive motor vehicles and mechanisms

The use of the drug Diasec® does not affect or has a negligible effect on the ability to drive a car and machinery.

Overdose

Currently, isolated cases of overdose without side effects are known.

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

Drug interaction

Currently, data on the interaction with other drugs are not available.

Loperamide or nifuroxazide does not affect the kinetics of racecadotril when these drugs are used together.

Diasec storage conditions®

The drug should be stored out of the reach of children at a temperature not higher than 25 ° C.

Diasec shelf life®

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

Terms of implementation

The drug is available on prescription.