Tsizaprid (cisapride)


TSIZAPRID (Cisapride).
     tsis-4- Amino hlor-N- [1-[3-(para-ftorfenoksi) propyl] -3-methyl piperidil] - ortho anizamid.
     Synonyms: Koordinaks, Periperid, Peristil, Sizapro, Tsisap, Tsisapid, Tsisaprid, Cisap, Cisapid, Cisapro, Coordinax, Peristil, Prepulsid.
      Crystalline powder. Nerastvorim water poorly soluble in methanol, soluble in acetone.
     Holinomimeticheskoe substance other than on the structure of atsetilholinopodobnyh compounds.
     Mechanism of binding of acetylcholine increased allocation from the end postganglionarnyh holinergicheskih nerves, especially bryzheechnyh eye ulcers. Increases tone and motor activity of the bowel and sphincter tone oesophagus, stomach contents warns Abandonment of oesophagus. Speeding up empty stomach and duodenal ulcer.
     As of tsizaprid close to metoclopramide (see) and domperidonu (see), but the molecular mechanisms of these drugs vary: tsizaprid a stimulant holinergicheskih processes, and metoclopramide and Domperidone-antagonists dofaminovyh (D2) receptor.
     A faster and stronger than metoclopramide and Domperidone.
     Quickly absorbed in the digestive, bioavailability of 35-40%, C max 1-1,5-h, T 1 / 2 (oral introduction), 6-12 h; Being biotransformation in the liver derived from urine and faeces in the form of metabolites.
     Assign paresis in the stomach, reflux ezofagite, atony bowel (chronic zaporah), dyspepsia, to accelerate peristalsis in ZHKT ray study.
     Apply inside and parenteral transmission.
     Inside (for 15 minutes before eating) designate an adult as tablets of 0,005-0,015 grams (up to 0.02 g), or 10 mL of 0.1% suspensions 3-4 times a day.
     "Standards for the diagnosis and treatment of patients with diseases of the digestive system" tsizaprida recommend the application of integrated therapy postholetsistektomicheskogo syndrome and holetsistitov (at 0.01 g 3-4 times per day for 2 weeks or more).
     Children designated as suspensions: aged 1 to 5 years of 0.0025 g (2.5 mg), the older of 0,005-0,01 g (5-10 mg) 2-3 times a day.
     Possible side effects: headaches, convulsions, arrhythmia, kserostomiya, dispersion, hepatitis, joints, swelling, blood oppression, allergic reactions.
     Contraindications: gastrointestinal bleeding, expressed functional kidneys and liver, pregnancy, breast-feeding.
     Method of production: tablets of 0,005 and 0.01 g (5 and 10 mg) (N. 20, 30); 0.1% suspension for receiving inside in vials of 60 ml and 100; 0.2% and 0, 5% solution for injection of 2 ml ampoule.
     Storage: List B.

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