Hidrasec 10mg powder treatment for acute diarrhea in children (16 packs)

Thiorphan is an enkephalinase inhibitor, a cell membrane peptidase present in many different tissues, mainly epithelium of the small intestine. This enzyme is involved in both external hydrolysis and endogenous peptide destruction as enkephaline. Therefore, RaceCadotril protects endogenous enkephalins that have physiological activity in the gastrointestinal tract, prolonging their secretion effect in the gastrointestinal tract.

racecadotril is an anti -intestinal drug, which is limited to the small intestine. It reduces the secretion of water and electrolytes in the small intestine, caused by cholera or inflammatory toxins, and does not affect the basic excretory activity.

racecadotril quickly works anti -diarrhea without changing the time of the small intestine.

In 2 clinical studies in children, Racecadotril reduced by 40% and 46% of the fertilizer weight in the first 48 hours. It is also recognized that diarrhea and water compensation decrease significantly.

A data synthetic analysis study (9 random clinical trials of racecadotril compared to placebo, along with oral compensation) collected personal data from 1384 boys and girls with acute diarrhea at severe level and inpatient or outpatient.

Average age is 12 months old (about 6 - 39 months of age). A total of 714 patients under 1 year of age and 670 patients over 1 year of age. The average weight ranges from 7.4 kg to 12.2 kg. The total diarrhea time is 2.81 days for the placebo group and 1.75 days for the raceCadotril group.

The percentage of patients recovering in Racecadotril group is higher than the placebo [HR): 2.04; 95% CI: 1.85 - 2.32; p

For study in boarding patients (n = 637 patients), the average ratio of fertilizer of the group using racecadotril compared to the placebo is 0.59 (95% CI: 0.51 - 0.74); p

racecadotril does not cause bloating. During clinical research, Racecadotril causes secondary constipation at the ratio equivalent to placebo. When taken orally, the drug only acts on the periphery, without the influence on the central nervous system.

Dynamic pharmacokinetics

absorption

racecadotril is quickly absorbed after drinking. A plasma enzyme inhibitor begins after about 30 minutes. RaceCadotril's bioavailability is not replaced by food, but the peak concentration is slowered for about 1 hour and 30 minutes.

distribution

After taking 1 dose of Racecadotril is marked by C-14, the amount of exposure of radioactive carbon measured in plasma is many times higher than blood cells and 3 times higher than the total blood. Therefore, the drug is not attached to any blood cells. The distribution of radioactive carbon in other tissues of the body is moderate, expressed by the average appsed distribution in plasma of 66.4 kg.

90% of the active metabolites of racecadotril, thiorphan (= (rs) -N- (1-oxo-2- (mercaptomethyl) -3-phenylpropyl) glycine), are linked to plasma proteins, mainly with albumin.

The time and range of influence of racecadotril depends on the dose.

In children, the time to inhibit Enkephalinase peaks in plasma is approximately 2 hours and is equivalent to 90% of inhibition at a dose of 1.5 mg/kg. In adults, the time to inhibit Enkephalinase reaches a peak in plasma approximately 2 hours and is equivalent to 75% inhibition at a dose of 100 mg.

Enkephalinase inhibitor time is about 8 hours.

transformation

Racecadotril's biological waste time is calculated according to plasma Enkephalinase inhibition, approximately 3 hours.

racecadotril is quickly hydrolyzed into thiorphan, which is active, transformed back into non -activity metabolites. The repetition of raceCadotril does not cause the accumulation of drugs in the body.

In vitro data shows racecadotril/thiorphan and 4 non -active metabolites inhibit CYP enzymes such as 3A4, 2D6, 2C9, 1A2 and 2C19 to the level of clinical effects related.

In vitro data shows racecadotril/thiorphan and 4 main substances in the non -activity metabolism that does not activate CYP enzyme (family 3A, 2A6, 2B6, 2C9/2C19, family 1A, 2E1) and enzymes combine UGTS for clinical effects.

racecadotril does not change the protein attachment of active ingredients that strongly bond protein such as: Tolbutamide, Warfarin, Niflamic Acid, Digoxin or Phenytoin.

In patients with hepatic impairment [cirrhosis, the degree B of the Child-Pugh classification scale], the dynamic properties of metabolites with the activity of racecadotril have shown the similarities between TMAX and T and lower amounts than CMAX (-65%) and AUC (-29%) when compared to healthy objects.

In patients with severe renal impairment (Racecadotril 11 - 39 ml/minute ratio) The kinetic properties of Racecadotril's metabolism have shown that lower than CMAX (-49%) and higher than AUC (+16%) and T1/2 when compared to healthy volunteers (East ratio> 70 mL/minute).

In children, the pharmacokinetic results are similar to that of an adult, reaching the peak concentration after drinking 2 hours 30 minutes. Do not accumulate drugs when taking the dose repeated every 8 hours in 7 days.

Elimination

racecadotril is eliminated in the form of active and non -active metabolism, mainly through urine, and there is much less level through feces. Elimination through the lungs is not meaningful.