The International unlicensed
name Ratsekadotril Lekarstvennaya a form
Solid gelatin capsules of 100 mg
One capsule contains a trade name of Gidrasek®:
active agent – ratsekadotrit 100 mg,
excipients: lactose, starch corn prezhelatinizirovanny, magnesium stearate, silicon dioxide colloidal anhydrous
structure of a cover of the capsule: gland (III) oxide yellow (E172), titan dioxide (E171), gelatin.
Solid gelatin capsules, No. in size 2, with the body and a lid of color of ivory. Contents of capsules – powder of white color with a strong sulfuric smell.
Antidiarrheal drugs. Other anti-diarrheal drugs. Ratsekadotril.
ATX A07XA04 code
Pharmacokinetics Absorption properties. At intake ratsekadotrit quickly it is soaked up. Its pharmacological action on inhibition of an enkefalinaza of plasma begins in 30 minutes. The bioavailability of a ratsekadotril does not change at meal, but the peak activity comes later approximately on an hour and a half.
Distribution. After intake of a dose of a 14C-ratsekadotril the measured influence of radio carbon in plasma was many times higher, than in haemocytes and erythrocytes and 3 times above, than in whole blood. Thus, drug does not contact blood cells substantially. Distribution of radio carbon in other body tissues was moderate, the average seeming distribution volume in plasma was 66.4 kg. 90% of an active metabolite of a ratsekadotril – a tiorfan (= (RS) – N-(1-okso-2-3-fenilpropit (mercaptomethyl)) glycine), contacts proteins of plasma, mainly albumine.
Pharmacokinetic properties of a ratsekadotril do not change at reception of repeated doses at adults.
Duration and expressiveness of action of a ratsekadotril are dose-dependent.
At children the maximum suppression (90%) of activity of a plasma enkefalinaza is reached approximately in 2 hours at a dose of 1.5 mg/kg. At adults the maximum inhibition of activity of a plasma enkefalinaza in plasma also comes in 2 hours and corresponds to 75% inhibition at a dose of 100 mg. Duration of inhibition of a plasma enkefalinaza is about 8 hours.
Metabolism. Time of biological semi-removal measured by plasma enkefalinaza inhibition duration, about 3 hours.
Ratsekadotril is quickly hydrolyzed in tiorfan – an active metabolite which, in turn, will be transformed to inactive metabolites. Repeated reception of a ratsekadotril does not cause cumulation in an organism. The researches in-vitro specify that ratsekadotrit / tiorfan and four main inactive metabolites do not inhibit the main CYP isoenzymes (3A4, 2D6, 2S9, 1A2 and 2S19) and do not stimulate CYP isoenzymes (3A family, 2A6, 2B6, 2C9/2C19, 1A family, 2E1) and the glyukoroniltransferaz-conjugated enzymes to clinically significant degree.
Ratsekadotril does not influence extent of linking with proteins of plasma of active agents which to a large extent contact proteins of plasma, such as tolbutamide, warfarin, niflumovy acid, digoxin and Phenytoinum.
Removal. Ratsekadotril is brought mainly in the form of inactive metabolites with urine and also in small amounts with excrements. Removal through lungs is insignificant.
At patients with a liver failure (cirrhosis, class B on Chayld-Pyyu) the following features of a pharmacokinetic profile of an active metabolite of a ratsekadotril in comparison with healthy faces were revealed: similar values of time of achievement of the maximum concentration (Tmax) and elimination half-life (T1/2), and value of the maximum concentration (Cmax) and the area under curve (AUC) – lower (-65% and – 29%, respectively).
At patients with a heavy renal failure (clearance of creatinine (CC) of 11-39 ml/min.) the kinetic profile of an active metabolite of a ratsekadotril showed lower maximum concentration (Smakh) (-49%) and higher values of the area under curve (AUC) (+16%) and elimination half-life (T1/2), in comparison with healthy faces which KK have more than 70 ml/min.
At children the pharmacokinetic indicators are similar to that at adults, time of achievement of Cmax was 2 h 30 min. after administration of drug. Does not collect after repeated doses through everyone 8 hours within 7 days.
Ratsekadotril is inactive substance, as a result of hydrolysis he turns in tiorfan which has property to inhibit an enkefalinaza, the peptidase of a cellular membrane localized in various fabrics, especially in epithelial cells of a small intestine. This enzyme participates in hydrolysis of exogenous peptides and splitting of endogenous peptides, such as enkephalins. Therefore, ratsekadotrit protects endogenous enkephalins which are physiologically active at the level of a digestive tract, prolonging their anti-secretory action.
Ratsekadotril represents substance with anti-secretory action, its activity is limited mucous a small intestine. It reduces the hypersecretion of water and electrolytes in a small intestine caused by cholera toxin or inflammation does not affect basal secretory activity. Ratsekadotril quickly shows anti-diarrheal action, without influence on duration of intestinal transit.
Ratsekadotril does not cause an abdominal distension. In clinical trials the frequency of a secondary constipation at reception of a ratsekadotril is comparable with the group accepting placebo.
At intake its activity is shown only at the peripheral level, without impact on the central nervous system.
– symptomatic treatment of acute diarrhea at adults
to Accept the Route of administration and doses inside.
Adults: an initial dose – one Гидрасек® 100 capsule of mg irrespective of time of day. Then on one capsule 3 times a day, are preferable before the main meal. Treatment is continued to 2 cases of the issued chair, but by no more than 7 days. Long administration of drug is not recommended. If after 3 days of treatment there does not occur improvement, then it is necessary to consult with the doctor.
Special groups of patients:
Children: there is a special dosage form in the form of granules for preparation of suspension for intake intended for use for babies, children and teenagers.
Elderly: dose adjustment is not required from patients of old age.
Exist data of pharmacological and clinical trials with participation of 2714 patients accepting ratsekadotrit and 496, the accepting placebos. The general frequency of by-effects was 13.6% at the patients receiving ratsekadotrit also 22% in group of placebo. The headache (1.8% and 1.6%), nausea (1.5% and 2.4%), and a constipation (1.3% and 1.4%) was most often noted.
Side reactions which were observed at reception of a ratsekadotril more often than at intake of placebo are listed below, or recorded in
Often (& gt, 1/100, & lt, 1/10)
– a headache
Infrequently (& gt, 1/1000, & lt, 1/100)
– rash, an erythema
Frequency is unknown
– a multiformny erythema, a paraglossa, a face edema, hypostasis of lips, the century, a Quincke’s disease, urticaria, a knotty erythema, papular rash, a prurigo, an itching, a toxic epidermal necrolysis swelled.
According to messages, at the babies or children receiving ratsekadotrit, tonsillitis as side effect seldom developed. But for this age group there is a special dosage form of Gidrasek – a granule for preparation of suspension for intake.
– hypersensitivity to active or to any of drug excipients
– congenital intolerance of a galactose, deficiency of Lappa lactase or disturbance of absorption of glucose galactose
– children’s and teenage age up to 18 years
– pregnancy and the period of a lactation
does not exist messages about medicinal interactions of a ratsekadotril at the person Today. It is known that the concomitant use with nifuroksazidy and loperamide does not change kinetics of a ratsekadotril.
At treatment by Gidrasek it is necessary to observe the rehydration mode.
Presence at a chair of impurity of blood or pus and/or temperature increase can indicate bacterial intestinal infection as the cause of diarrhea, or presence of other serious disease demanding etiological therapy (antibiotic) and further inspection. In such cases Gidrasek is not recommended to appoint. In acute bacterial diarrhea it is possible to accept Gidrasek together with an antibiotic as additional treatment.
Gidrasek’s use in chronic diarrhea and an antibiotic – the associated diarrhea is not recommended because of insufficient data.
At patients with a renal and liver failure the data on use are limited. Therefore to appoint with care.
Decrease in bioavailability of a ratsekadotril in long vomiting is possible.
Â¿ñÓáßÑ¬® 100 mg of the capsule contain lactose. Patients with rare congenital states as intolerance of a galactose, deficiency of Lappa lactase or disturbance of absorption of glucose galactose should not accept Гидрасек® 100 mg of the capsule.
Pregnancy and the period of a lactation
does not exist sufficient data on use of Gidrasek®100 of mg of capsules for pregnant women. Preclinical trials did not show direct or indirect harmful effects of a ratsekadotril on a pregnancy course, development of an embryo and a fruit, a course of childbirth and a puerperal period. However Gidrasek’s reception by pregnant women is not recommended.
Гидрасек® the women nursing as there are not enough data on excretion of a ratsekadotril with breast milk should not accept.
Features of influence of medicine on ability to run the vehicle or potentially dangerous
Гидрасек® 100 mechanisms of mg of the capsule do not influence (or influence insignificant) ability to drive the car and to work with potentially dangerous equipment.
does not exist messages about Gidrasek’s overdose. Adults have a single dose in a dose 2 g that is equivalent to 20 therapeutic doses, did not cause negative effect.
Symptoms: strengthening of side effect is possible.
The form of release and packing
On 10 capsules place in blister strip packaging from a film polyvinylchloride / polietilenpolivinildikhloridnoy (PVC/PE/PVDC).
On 1 planimetric packing together with the instruction for medical use in the state and Russian languages put in a pack from cardboard bandbox.
To Store storage conditions in the dry, protected from light place at a temperature not above 25 °C.
To store out of children’s reach!
not to apply a period of storage after an expiration date!
of Proizvoditel Laboratories of Sofartex, France