Hydrasek, capsules 100 mg 10 pcs

Pharmacological group:
Antidiarrheals. Other antidiarrheal drugs. Racecadotril.

Pharmacodynamics:
Racecadotril is an inactive substance, as a result of hydrolysis it is converted to thiorfan, which has the property of inhibiting enkephalinase, a cell membrane peptidase localized in various tissues, especially in the epithelial cells of the small intestine. This enzyme is involved in the hydrolysis of exogenous peptides and the cleavage of endogenous peptides such as enkephalins. Consequently, racecadotril protects endogenous enkephalins, which are physiologically active at the level of digestive tract, prolonging their antisecretory action.

Racecadotril is a substance with antisecretory action, its activity is limited to small intestine mucosa. It reduces hypersecretion of water and electrolytes in the small intestine caused by cholera toxin or inflammation, it has no effect on basal secretory activity. Racecadotril has a rapid antidiarrheal effect, without affecting the duration of intestinal transit.

Racecadotril does not cause abdominal bloating. In clinical studies, the incidence of secondary constipation while taking racecadotril is comparable to the group that took placebo.

When taken orally, its activity appears exclusively at the peripheral level, with no effect on the central nervous system.

Pharmacokinetics:
Absorption. Racecadotril is rapidly absorbed when administered orally. Its pharmacological action of plasma enkephalinase inhibition begins after 30 minutes. The bioavailability of racecadotril is not altered by ingestion, but peak activity comes about an hour and a half later.

Distribution. After an oral dose of 14C-racecadotril, measured radiocarbon exposure in plasma was many times higher than in hemocytes and erythrocytes and 3 times higher than in whole blood. Thus, the drug does not bind to blood cells to any significant extent. The distribution of radiocarbon in other body tissues was moderate, the average apparent volume of distribution in plasma was 66.4 kg. 90% of the active metabolite of racecadotril, thiorphan (= (RS)-N-(1-oxo-2-(mercaptomethyl)-3-phenylpropyl) glycine), binds to plasma proteins, predominantly to albumin.

The pharmacokinetic properties of racecadotril are not altered by repeated doses in adults.

The duration and severity of action of ratsecadotril are dose dependent.

In children, maximum inhibition (90%) of plasma enkephalinase activity is achieved in approximately 2 hours at a dose of 1.5 mg/kg. In adults maximum inhibition of plasma enkephalinase activity also occurs after 2 hours and corresponds to 75% inhibition at a dose of 100 mg. The duration of plasma enkephalinase inhibition is approximately 8 hours.

Metabolism. The biological half-life as measured by the duration of plasma enkephalinase inhibition is approximately 3 hours.

Racecadotril is rapidly hydrolyzed to thiorphan, the active metabolite, which in turn is converted to inactive metabolites. Repeated administration of ratsecadotril does not cause cumulation in the body. In-vitro studies indicate that ratsecadotril/tiorphan and the four major inactive metabolites do not inhibit major CYP isoenzymes (3A4, 2D6, 2C9, 1A2 and 2C19) or stimulate CYP isoenzymes (3A family, 2A6, 2B6, 2C9/2C19, 1A family, 2E1) and glucoronyltransferase-conjugated enzymes to a clinically significant degree.

Racecadotril does not affect the degree of binding to plasma proteins of active agents that bind heavily to plasma proteins, such as tolbutamide, warfarin, niflumic acid, digoxin and phenytoin.

Excretion. Racecadotril is excreted mainly in the form of inactive metabolites in the urine and in small amounts in the feces. Excretion through the lungs is insignificant.

In patients with hepatic impairment (liver cirrhosis, class B according to Child-Pugh) the following features of the pharmacokinetic profile of the active metabolite of racecadotril compared to healthy individuals were revealed: Similar values of time to reach maximum concentration (Tmax) and half-life (T1/2), and lower values of maximum concentration (Cmax) and area under the curve (AUC) (-65% and -29%, respectively).

In patients with severe renal impairment (creatinine clearance (CK) 11-39 ml/min), the kinetic profile of the active metabolite of racecadotril showed lower maximum concentrations (Cmax) (-49%) and higher area under curve (AUC) values (+16%) and half-life (T1/2), compared to healthy individuals with CK greater than 70 ml/min.

In children the pharmacokinetic parameters are similar to those in adults, the time to reach Cmax was 2 h 30 min after taking the drug. It does not accumulate after repeated doses every 8 hours for 7 days.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Synopsis

The pathogens that cause acute diarrhea (viruses, bacteria, toxins) damage intestinal cells, which leads to disruption of water absorption by the body. As a result, excess fluid from our body is excreted into the intestines, thinning the stool.

Racecadotril, the active ingredient in Hydrasek, protects special peptides in the intestine which regulate the release of fluid into the intestinal lumen, prolonging their action and thereby preventing the stool from becoming liquefied. Racecadotril begins to have anti-diarrheal effect within 30 minutes after intake, without slowing down intestinal motility.

Hydrasek is indicated for symptomatic therapy of acute diarrhea of any etiology (viruses, bacteria, toxins) and does not require long-term course of treatment.

Hydrasek is compatible with other medicinal agents. Racecadotril may be used together with antibiotics as additional therapy of acute bacterial diarrhea.2

Hydrasek effectively relieves symptoms of acute diarrhea in older adults; no dose adjustment is necessary for older patients.

Contraindications

Side effects

Overdose

Pregnancy use