Trimebutine maleate


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What is Trimebutine maleate?
Cas No.:34140-59-5
Appearance:white crystals or crystalline powder
Molecular Formula:C26H33NO9

Overview of Trimebutine maleate
 
Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects. The major product from drug metabolism of trimebutine in human beings is nortrimebutine,which comes from removal of one of the methyl groups attached to nitrogen. Trimebutine exerts its effects in part due to causing a premature activation of phase III of the migrating motor complex in the digestive tract.Both Trimebutine and its metabolite are commercially available.
 
Primary Characterstics of Trimebutine maleate
 
Molecular Structure of Trimebutine Maleate belongs to Aminobenzoate. It belongs to Alpha adrenergic agonist pharmacological group on the basis of mechanism of action and also classified in Gastrointestinal Anticholinergics/Antispasmodics and Antispasmodic Agent pharmacological group.The Molecular Weight of Trimebutine (Maleate) is 503.50.
 
Application of Trimebutine maleate
 
Trimebutine maleate is used to make the movement of the intestinal tract more normal. This medication slows down or speeds up the movement of the intestines if the gut is not working well. It does not affect a normally working gut. It is used to treat symptoms (e.g., abdominal pain/fullness, gas, diarrhea, constipation) of irritable bowel syndrome (spastic colon). Trimebutine is also used to restart the movement of the gut after abdominal surgery and to prevent intestinal blockage (paralytic ileus).
 
Storage instructions and handling of Trimebutine maleate
 
Store at room temperature.
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 12 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

The effect of trimebutine maleate on gastric emptying in patients with non-ulcer dyspepsia

The study was designed to investigate the effect of trimebutine maleate, a drug used in both hyperkinetic and hypokinetic motility disorders, on gastric emptying in patients with non-ulcer dyspepsia having prolonged gastric emptying rates and to compare the parameters used for the determination of the lag period observed during the emptying of solid foods from the stomach. Gastric emptying was measured by the radionuclide technique. Twenty normal volunteers and 43 patients with non-ulcer dyspepsia participated in the study. Radionuclide imaging was performed by using a solid meal labeled with 99mTc-tin colloid. Of the patients with non-ulcer dyspepsia, 20 had prolonged gastric emptying. They were given three weeks of oral treatment with trimebutine maleate and had their radionuclide gastric emptying study repeated. Treatment with trimebutine maleate resulted in reduction in duration of the lag period and less retention of food at 100 minutes (p < 0.0005). After treatment with trimebutine maleate, no significant difference has been observed in the mean symptom score of patients with prolonged gastric emptying. Among the parameters used for the determination of the lag period, lag period determined by a mathematical equation (TLAG) has been found to be longer than the lag 

Effect of trimebutine maleate on sinus node pacemaker activity of the rabbit

The electrophysiological effects of trimebutine maleate were studied on rabbit sinus node cells with the two-microelectrode voltage clamp method. Trimebutine (above 10 μM) produced a negative chronotropic effect accompanied by decreases in the maximum upstroke velocity at phase 0, slope of phase 4 depolarization and action potential amplitude. The effects on the current systems were depression of the slow inward current and a decrease in the current oscillations induced by elevating [Ca]0. It is concluded that trimebutine exerts a Ca2+ channel blocking effect on the sinus node pacemaker cells.

Efficacy of Trimebutine Maleate in the Treatment of Functional Dyspepsia in Childhood

Peripheral μ-, k- and δ-opioid agonist trimebutine maleate is considered to be an effective therapeutic drug for the treatment of functional gastrointestinal disorders. Ninety-two paediatric outpatients (12- 17 year-old) suffering from functional dyspepsia (epigastric pain and meal-induced dyspeptic symptoms) were enrolled in a prospective openlabel study. For ethical reasons, no placebo group was included. Patients were treated with trimebutine maleate (200 mg three times daily). After a 3-week treatment there was a significant decrease in scores of epigastric pain (p<0.05), postprandial fullness (p<0.05), early satiety (p<0.05), nausea (p<0.05) and belching (p<0.05). The treatment regimen was well tolerated and demonstrated a good compliance. In conclusion, we postulate that trimebutine maleate is an effective medication for relief of main symptoms associated with functional dyspepsia syndrome in childhood. Because of the limited data on therapeutic interventions in functional dyspepsia in childhood and increasing demand for therapies to treat this disorder, further evaluation of the efficacy of trimebutine treatment for children is certain.

Potency Reasearch on Trimebutine Maleate Compound Preparation

Objective: To observe the effect of trimebutine maleate compound preparation on gastric emptying,small intestine advancing and protein digestion as well as its role in acute toxicity.Method: Nutritional semi-solid filling regimens was adopted to test the gastric residual rate and small intestine advancing rate;biuret protein test was used to detect impact of protein digestion;improved Karber method was applied to test the acute toxicity.Result: Compared with model control group,trimebutine maleate compound preparation in each group significantly reduced the rate of gastric residue while increasing the small intestine advancing rate(P0.05);compared with the blank control group,the protein digestibility of trimebutine maleate compound preparation group increased significantly(P0.05);the mortality of 5 trimebutine maleate compound preparation groups with different doses were 0%,10%,40%,90% and 100%,respectively.Conclusion: Trimebutine maleate compound preparation can not only reduce the inhibition of gastrointestinal tract movement due to atropine,but can enhance the digestion of proteins.LD50 for oral administration of mice is(2.89±0.35) g/kg;95% confidence limit of 2.56~3.27 g/kg.

Curative effect of trimebutine maleate on gastric dynamic disorder in patients with cirrhosis

Aim To analyze the change of electrogastrogram(EGG) and estimate the efficacy of trimebutine maleate in treatment of gastric dynamic disorder in patients with cirrhosis.Methods 95 patients were divided into two groups by liver function.Patients with gastric dynamic disorder were examined with EGG before and after the treatment of trimebutine maleate and their symptoms were assessed simultaneously.Results There was significant difference between them.EGG examinations before and after meal showed that average frequency was reversed to normal level after treatment with trimebutine maleate.The symptoms of patients were also improved after the treatment(P0.05).Conclusion Trimebutine maleate can relieve symptoms and improve the average frequency of EGG in patients of cirrhosis with gastric dynamic disorder
A Case of Trimebutine-Induced Anaphylaxis

Trimebutine maleate [2-dimethylamino-2-phenylbutyl 3,4,5-trimethoxybenzoic acid] has been demonstrated to be active for relieving abdominal pain and it is widely used for patients with irritable bowel syndrome. Adverse drug reactions are mostly mild and well-tolerated. To our knowledge, only two cases of trimebutine induced hypersensitivity have been reported, and both were delayed type reactions. Here, we report the first case of trimebutine maleate-induced anaphylaxis.

A case of senile depression with dysarthria due to trimebutine maleate

Trimahutine maleate is a gastroenteric motor modulator which improves abnormal peristaltic movements through the direct effect on the smooth muscle cells. We examined a case of senile depression with dysarthria due to trimebutine maleate. The patient was a 67-year-old female. At the age of 65, she became depressive state without any causes and some nontricyclic antidepressants gave her no relief from the depression and induced side effects (drowsiness, dry mouth and dysarthria), When she was 66 years old, she was given trimebutine maleate (100mg) for her irritable colon syndrome. After several hours of the administration, she suffered from dysarthria and finger tremor. Quitting trimebutine maleate stopped the symptoms a few days later. The cranial CT findings before the occurrence of dysarthria showed cavum septi pellucidi, cavum Vergae, calcifications in bilateral basal gangilas and mild atrophy of cerebral cortices and the findings after the occurrence had no change. Cerebral hemorrhage and infarction were ruled out by her CT findings and the other drugs were unlikely to cause the dysarthria. Therefore, trimebutine maleate might induce the dysarthria which seemes to be the breakdown of the balance between dopaminergic and cholinergic systems in the brain. Moreover, it is speculated that her dispositional frailty of the central nervous system and the cerebral organic changes by cavum septi pellucidi, the calcifications and aging underlay the apperance of the dysarthria.

Effect of Trimebutine Maleate on Diabetic Diarrhea

Seven patients were studied to evaluate the effect of trimebutine maleate on diabetic diarrhea. All patients had severe autonomic neuropathy. Improvement was assessed on the basis of subjective symptoms (diarrhea score) after oral administration of trimebutine maleate (300 mg/day). Within two days, severe diarrhea was markedly reduced. No side effects were observed in any of the patients. The results of this study suggest that trimebutine maleate may serve as a useful drug in improving the symptom of diabetic diarrhea.


Effects of trimebutine maleate (TM-906) on the gastrointestinal motility in anesthetized dogs

Effects of trimebutine maleate (TM-906) on the spontaneous motility of the gastrointestinal tracts were investigated in anesthetized dogs by means of force transducers. TM-906, administrated intravenously or intraduodenally, produced an inhibition followed by a potentiation of the spontaneous motility in the stomach, and caused a potentiation of the spontaneous motility in the duodenum, jejunum, ileum and colon. These effects of TM-906 were observed also in the vagotomized dogs as in the intact dogs. From these results, it is suggested that TM-906 modulates the spontane-ous motility of the gastrointestinal tracts primarily through the peripheral mechanism.

Effects of trimebutine maleate on the gastrointestinal motility in conscious dogs

Trimebutine maleate is known to have beneficial effect in the treatment of gastrointestinal disorders. In conscious dogs with implanted force transducers, effects of trimebutine maleate on the gastrointestinal motility were investigated by intravenous injection, and the results were compared to those with metoclopramide and hyoscine-N-butylbromide. When trimebutine maleate was administered during the motor quiescence in the interdigestive state, contractions were evoked or the quiescent time was shortened in the gastrointestinal tract. In the digestive state, the gastric antral contractile activity was reduced, and duodenal activity was somehow suppressed by trimebutine maleate; but in the jejunum, ileum or colon, the activity was augmented. Injection of metoclopramide evoked a continuous contraction in the gastric antrum and duodenum during the period of motor quiescence in the interdigestive state. In the digestive state, metoclopramide caused a slight enhancement in the contractile activity of the gastric antrum. On the other hand, hyoscine-N-butylbromide produced no effect during the period of motor quiescence in the interdigestive state and suppressed the activity of the gastrointestinal tract during the digestive state. Thus, the pattern of action of trimebutine maleate was different from metoclopramide and hyoscine-N-butylbromide. It was concluded that trimebutine maleate produces dual actions, suppression and acceleration, on the gastrointestinal motility in conscious dogs.

trimebutine maleate pharmacology animal pharmacology

In isolated smooth muscle preparations, trimebutine maleate was shown to be anoncompetitive spasmolytic agent. It was found to be as active as papaverine againstacetylcholine, 

histamine, barium or serotonin on ‘D’ receptors; however, it was more active against nicotine or serotonin on ‘M’ receptors. This potent anti-serotonin activity is non-

specific and may be, at least partly, attributed to its local anaesthetic activity, as shown in comparative studies with lidocaine. Using membrane preparations of whole ratbrain 

and guinea pig intestine, trimebutine maleate was shown to bind to opiate receptors with moderate affinity.
Electrophysiological studies have shown that trimebutine maleate exerts a strong spasmolytic papaverine-like activity together with an evident, unusual stimulation of 

spontaneous activity. It induced a marked regularization of spontaneous activity with an increase in the amplitude of contractions. A clear synchronization with the appearance 

of large regular spikes closely coupled to the single contractions was also noted. However, unlike quinidine-like drugs, the membrane resistance was not concomitantly increased.
The effects of trimebutine maleate on the mechanical and electrical activity of the intestine are not prevented by atropine or hexamethonium, but the spasmolytic activity is 

counteracted by an increase in calcium concentration.
In vivo, trimebutine maleate did not alter normal intestinal transit time in mice and rats,but regularized abnormal intestinal activity by increasing transit time when 

abnormally low or by decreasing it when abnormally high, thus returning transit time towards normal values. A similar regularizing effect was noted on Oddi’s sphincter in 

rabbits. It was less active than atropine against the intestinal spasmogenic effect of methacholine, but more active than papaverine against other spasmogens such as barium or 

prostigmin in mice,rats and rabbits. 
The effect of trimebutine maleate administered orally or intravenously was studied in conscious or anaesthetized rabbits, dogs and sheep and the mechanical and/or electrical
activity was recorded in some or all of the following segments: stomach, duodenum,jejunum, ileum, and colon. Gastric activity remained unaltered or was slightly depressed;
the depressant effect was much less than that with N-butylscopolamine and atropine and more than with papaverine, while metoclopramide had the opposite effect. The activity
of the small intestine was markedly increased, more in the duodenum than in the jejunum and ileum and preferentially in those segments with irregular intestinal activity. This
effect was more pronounced with trimebutine maleate than with metoclopramide, while papaverine had a depressant effect. In dog colon, trimebutine maleate has a less
pronounced but more sustained effect which consisted of a stimulant action on circular muscles coupled with an inhibitory action on longitudinal muscles. In the rabbit, the
experimentally-induced hyperpolarization of the colon was decreased in amplitude or suppressed, while a facilitation effect on synaptic excitatory potentials was noted which
might have been related to an action on purinergic neurons. No other noticeable effects were observed on the gastrointestinal tract.Trimebutine maleate was shown to be a potent 

local anaesthetic with activity which is greater in magnitude and longer in duration than cocaine, procaine and lidocaine.On the central nervous system, trimebutine maleate 

dosed at 2-30 mg/kg i.v., 2-100mg/kg i.p. and 2-500 mg/kg p.o. in mice, rats and rabbits produced some of the following effects depending upon the species, the dosage and the 

route of administration: reduced spontaneous activity, hypotonia, slight sedation and impairment of cortical reactivity,increased sleep duration and decreased duration of 

induced hyperactivity, anticonvulsant activity and amidopyrine-like analgesia. Trimebutine maleate depressed respiration rate and amplitude and produced respiratory arrest at 

high doses.
In the cardiovascular system of dogs and rabbits, trimebutine maleate produced vasodilation as illustrated by increased coronary and femoral blood flow, and a dose related, but 

transient fall in systolic and diastolic blood pressure; ECG was not modified. 

trimebutine maleate pharmacokinetics

Metabolic studies in rat, dog and man showed the C14- trimebutine maleate or its free base is rapidly absorbed after oral administration. Peak plasma concentrations of
radioactivity were observed within one hour in man and rat and within 2-4 hours in the dog.
Plasma radioactivity in man indicated a kinetic model with central and peripheral compartments and a mean distribution half-life of 0.66 hour. Tissue distribution studies
showed high concentration of the radiolabelled drug in the stomach and the intestinal walls of rat and in the major organs of metabolism and excretion in mice. Placental
transfer without teratogenic effect was observed in the rat. Protein-binding was less than 5% in vivo (rat plasma) and in vitro (bovine serum albumin).
Urine was the main route of elimination in all species while a small percentage (5-12%) of radioactivity was detected in the faeces. The plasma half-life of trimebutine was 

short,but the elimination half-life of radioactivity was approximately 10-12 hours in man and rat. In the rat, an entero-hepatic circulation was also demonstrated.
Extensive metabolism of the parent compound was indicated since less than 2.4% of the urinary radioactivity was found as unchanged drug in all species. The livers of rat and
dog appeared to be the major site of hydrolysis of the ester and also capable of a “first pass” metabolism.
The main urinary metabolites in all species were 2-amino (I) or 2-methylamino (II) or 2-dimethylamino-2-phenylbutan-1-ol (III). These three metabolites plus mono-Ndesmethyl
trimebutine (IV) were also shown in plasma; the major component was III in rat and dog and IV in man. Sulphate and/or glucuronic acid conjugation was also shown to play an 

important role in metabolism. 

In a recent study involving 22 fasting healthy volunteers, the pharmacokinetic profile of trimebutine maleate 2 x 100 mg tablets was compared with 1 x 200 mg tablet to evaluate
the bioavailability of trimebutine from the two formulations.Analysis of the results indicated that the absorption of trimebutine from the two formulations was comparable. There 

were no statistically significant differences between the two formulations for any of the calculated bioavailability parameters for trimebutine.
It was therefore concluded that one 200 mg tablet of trimebutine maleate and two tablets of 100 mg strength appear to have comparable bioavailability. 
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Trimebutine maleate

Cas NO.:34140-59-5Molecular Formula:C26H33NO9Appearance:white crystals or crystalline powder

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