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Tsis-4-Amino-5-hlor-N-[spent on drink 1-[3 (4-ftorfenoks)] - 3-metoksi-4-пиперидинил] - 2-metoksibenzamid
Substance represents white crystal powder which is badly dissolved in water, methyl alcohol, but we will well dissolve in acetone.
The laxative stimulating motility and a tone of a gastrointestinal tract.
Pharmacodynamics and pharmacokinetics
Substance excites 5-HT4 receptors of serotonin, thus, stimulating development of acetylcholine in mezenterialny neuroplex and increasing sensitivity to this neuromediator of the m-holinoretseptorov located in smooth muscles of intestines. The food moves ahead on intestines quicker, the tone of an ezofagealny sphincter raises, there is a decrease in enteral clearance.
After reception of means inside it is quickly soaked up from a stomach, reaching the maximum concentration within an hour. The effect of drug can also be noticed in one or one and a half hours. Biological availability of substance makes about 35-40%. At the raised hydrogen indicator of a gastric juice absorbing capacity of drug decreases.
Tsizaprid for 98% contacts proteins of a blood plasma. At peroral reception the elimination half-life makes from 6 to 12 hours, at intravenous injections – till 20 o'clock. Substance is exposed to a metabolism, reactions of dealkylation in liver tissues, with P450 cytochrome enzyme participation. The inactive metabolite nortsizaprid is as a result formed. Substance with a stake and urine is removed, about 10% of means are left by a gastrointestinal tract in not changed look.
Indications to use
Medicine is appointed:
- at spontaneous paresis of a stomach;
- for stimulation of digestion at dyspepsia;
- at the stomach paresis caused by a diabetic neuropathy, a gastroektomiya or vagisection;
- to patients with a gastroesophageal reflux or a reflux esophagitis;
- at a chronic idiopathic lock;
- to newborn children with regurgitation;
- at functional pseudo-impassability of intestines;
- for preparation for X-ray contrast researches gastrointestinal tract for stimulation of a vermicular movement of intestines.
Means is contraindicated:
- at an allergy to active ingredient;
- to patients with bleedings in a stomach or intestines;
- at mechanical intestinal impassability;
- to pregnant women and the feeding women;
- at perforation of intestines or stomach;
- sick, inclined to emergence of gastric arrhythmias, extension of an interval of QT;
- to premature children till 3 months.
It is necessary to be careful at diseases of a liver and kidneys, it is recommended to modify a dosage.
After reception of this substance can arise:
- spasms and discomfort in intestines, diarrhea, a liver failure, an abdominal murmur, nausea, hepatitis, vomiting;
- the allergic reactions which are shown in the form of skin rashes and an itch;
- leukopenia, aplastic anemia, thrombocytopenia, granulocytopenia, pancytopenia;
- tremor, dizziness, spasms, drowsiness, headache, extrapyramidal frustration, migraine;
- the speeded-up urination;
- arrhythmia, lengthening of an interval of QT, tachycardia and fibrillation;
- pharyngitis, mialgiya, xerostomia, puffiness.
Tsizaprid, application instruction (Way and dosage)
As a rule to accept medicine inside, orally.
The recommended single dose for the adult – from 5 to 20 mg of means.
Children from 6 to 12 years for once can accept 2,5 - 5 mg of drug. Aged till 6 flyings – 200 mkg on kg of weight of the child.
The mode of dosing is defined individually.
Usually adult appoint on 3-4 drug intakes a day (3 of them before meal, 1 – before going to bed).
For children frequency rate of reception – from 2 to 3 times a day.
Duration of treatment depends on many factors and is defined by the doctor.
As treatment wash out a stomach, appoint absorbent carbon or other enterosorbents, provide maintenance of the vital functions of an organism, normalize a cordial rhythm.
The concomitant use of this substance and Cyclosporine leads to increase of plasma concentration of both substances.
Combined use of Tsizaprid and diazepam can lead to increase in speed of absorption of the last of a digestive tract, strengthening of sedation.
At a combination with ketokonazoly, Flukonazoly, itrakonazoly, Miconazolum and other antifungal derivatives of an azol; with makrolidny antibiotics, erythromycin, klaritromitsiny, troleandomitsiny; HIV protease inhibitors, ritonaviry, indinaviry, nefadozony and other means oppressing activity of CYP3A4 enzyme, slow down Tsizaprid's metabolism. Its plasma concentration increases, and the risk of development of life-threatening disturbances from cardiovascular system increases.
Anticholinergics reduce efficiency of this medicine.
The combined reception of means with Disopyramidum can lead to development of the additive cardiotoxicity.
Tsizaprid's drugs at a combination with amantadiny strengthen a tremor.
Also exert impact on cardiotoxicity of substance: Amiodaronum, Disopyramidum, quinidine, amitriptyline, astemizol, Chlorpromazinum, Pimozidum, bepridit, sparfloksatsin, insulin, loopback diuretics, bretylium tosylate, procaineamide, Sotalol, lithium carbonate, terfenadin, a haloperidol, tiodazin, Maprotilinum, thiazide diuretics.
The combined administration of drug and ranitidine increases absorbing capacity of ranitidine, however reduces its AUC. Medicine exerts impact on efficiency of warfarin and an atsenokumarol.
At a drug combination to digoxin, concentration and efficiency of cardiac glycoside decreases.
The case when diltiazem in combination with Tsizaprid caused increase in an interval QT and a loss of consciousness is described.
It is necessary to consider that drug increases plasma concentration of substances from dosage forms with the slowed-down release.
Extremely it is not recommended to raise the recommended dosage.
If in the course of treatment at the patient severe diarrhea developed, then it is necessary to lower a drug dosage.
Extra care should be observed at treatment of children 3 months are more senior.
At pregnancy and a lactation
Medicine is not recommended to be used during pregnancy (especially on the 3rd trimester) and when feeding by a breast. As it is proved that Tsizaprid is allocated with milk.
Drugs in which contains (Tsizaprid's Analogues)
Coincidence on the ATH code of the 4th level:
As at the moment it is not possible to buy drug in the territory of the Russian Federation, it is not enough reviews of use of drugs on the basis of Tsizaprid, however from those that are available – all positive.
The price on Tsizaprid where to buy
It is almost impossible to buy Tsizaprid in the territory of Russia. Registration of substance ended in 2001.
Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance use Tsizaprid surely consult with the attending physician.