Each tablet contains clebopride malate 0.68 mg equivalent to clebopride 0.5 mg.
Clebopride malate is N-(1'-benzyl-4'-piperidyl)-2-methoxy-4-amino-5-chlorobenzamide malate.
Pharmacology: Clast has 3 fundamental pharmacological properties: Antiemetic, regulator of gastrointestinal motility and selective blocker of emotional stress. The therapeutic activity of Clast is exerted at 3 different levels: Clast re-establishes normal gastrointestinal motility by inhibiting the action of dopamine at the level of the plexuses of Meissner and Auerbach; the mechanism of action is based on the effects of increasing the blood flow of gastric mucosa and the acceleration of the gastric emptying movement; Clast's dopamine receptor-blocking action in the limbic system guarantees a selective blockade of emotional stress and a very favourable effect against the somatic symptoms of anxiety.
Pharmacokinetics: Clebopride is rapidly absorbed after oral administration and no accumulation is observed upon continuous administration.
Blood Level (Single Administration): Oral administration of 1 or 2 tablets of clebopride (0.5 or 1 mg as clebopride) to healthy adults resulted in a peak blood level after 1.5-1.6 hrs, with the mean concentration being 0.88 and 2.56 ng/mL, respectively. The serum half-lives were 36.5 hrs and 26.5 hrs, respectively.
Blood Level in Case of Continuous Administration: Using the formula for the simulation curve obtained by applying the 2-compartment model to the blood level after single administration of 1 tablet (clebopride 0.5 mg), the pattern of change in the blood level was obtained by integration when 1 tablet was administered 3 times daily for 5 consecutive days. The results showed that a steady state was maintained from around the 5th day after administration with no accumulation.
Clebopride does not influence drug-metabolizing enzyme activity of liver or metabolism of other drugs directly. Clebopride was administered in large doses to rats (25, 50 or 100 mg/kg); the weight of the liver, microsomal protein amount and the effect on hepatic drug-metabolizing enzymes were investigated.
As a result, in every dose group, no differences were observed from the control group for any of these parameters. It was, thus, confirmed that clebopride exerted no effect on the hepatic drug-metabolizing enzyme activities.
Treatment of peptic ulcer and gastroduodenitis. Reestablishing normal gastrointestinal motility, dyspepsia, anorexia, aerophagia and meteorism, gastritis, reflux oesophagitis, gastritis caused by chronic alcoholism. Vomiting and nausea. Vomiting caused by anticancer drugs and radiotherapy, intestinal obstruction, neurosurgery post-anesthesia, postoperative hiccup, morphological alterations (pyloric stenosis). Vomiting in acute gastroenteritis, uremia, chronic alcoholism. Vomiting associated with acetonemia, post-infectious states (pertussis, respiratory and meningeal infections).
Adults: 1 tab 3 times daily.
Administration: Clast tablet is orally administered 30 min before meals.
Not to be administered to patients in whom stimulation of gastric motility may be harmful (haemorrhage, obstruction, perforation). Patients with proven tardive dyskinesia to neuroleptics.
Children, the first 3 months of pregnancy, lactation. During treatment, situations requiring a special state of alertness (eg, driving vehicles or operating dangerous machinery).
Caution should be exercised if used during the first 3 months of pregnancy and lactation.
Large doses may cause extrapyramidal symptoms which normally disappear immediately after the cessation of Clast; drowsiness, breast tension, dizziness.
Co-administration with phenothiazines and other antidopaminergic drugs should be avoided since their effects on CNS may be potentiated.
Sedative symptoms may appear if administered at the same time with tranquilizers, hypnotics, narcotics and alcohol.
Keep at room temperature and free from moisture.
A03FA06 - clebopride ; Belongs to the class of propulsives. Used in the treatment of functional gastrointestinal disorders.
Coated tab 0.5 mg x 10 x 10's.