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Trimebutine | CAS No: 39133-31-8 | GMP-certified suppliers
A medication that provides symptomatic relief in irritable bowel syndrome and postoperative paralytic ileus by modulating gastrointestinal motility and smooth muscle function.
Therapeutic categories
Primary indications
- Indicated for symptomatic treatment of irritable bowel syndrome (IBS) and treatment of postoperative paralytic ileus following abdominal surgery
Product Snapshot
- Trimebutine is available in multiple oral (tablet, capsule, suspension, granule), rectal (suppository), and injectable (intramuscular, intravenous) formulations
- It is primarily used for symptomatic treatment of irritable bowel syndrome (IBS) and postoperative paralytic ileus following abdominal surgery
- The product is approved for use in the Canadian market
Clinical Overview
Pharmacodynamically, trimebutine exerts a dual modulatory effect on gastrointestinal smooth muscle. At lower concentrations, it depolarizes resting membrane potentials via inhibition of outward potassium currents without significantly affecting contraction amplitude, thereby promoting motility. At higher concentrations, it inhibits inward calcium currents, particularly through L-type voltage-dependent calcium channels, leading to reduced spontaneous contractions and diminished peristaltic activity. Additionally, trimebutine activates T-type calcium channels and increases gastric emptying and GI contractility. Its weak agonist activity at mu opioid receptors contributes to a local anesthetic effect, mediated by selective binding with lower affinity compared to endogenous opioids. Metabolites such as nor-trimebutine also interact with mu opioid receptors on neural sites influencing gastrointestinal function.
The mechanism of action involves inhibition of extracellular calcium influx via high-affinity binding to the inactivated state of L-type calcium channels and suppression of calcium release from intracellular stores. Concomitant inhibition of delayed rectifier and calcium-dependent potassium channels induces contractile modulation. These combined effects restore normal bowel function by balancing excitatory and inhibitory influences on smooth muscle cells.
Trimebutine is classified chemically as a derivative of gallic acid and is commonly supplied as its maleate salt in pharmaceutical preparations. Although not approved by the U.S. Food and Drug Administration, it is marketed in Canada and various international markets. Safety profiles indicate typical antimuscarinic side effects, and the compound is associated in some reports with QTc interval prolongation, necessitating vigilance in patients with predisposing cardiac conditions.
For sourcing and quality control, trimebutine APIs should comply with established pharmacopeial standards where available, emphasizing high purity, consistent polymorphic form, and controlled residual solvents. Given its sensitivity to Ca2+ channel binding and potential metabolite activity, stability testing under relevant storage conditions is advisable to ensure bioequivalence and therapeutic reliability. Procurement should confirm supplier adherence to Good Manufacturing Practices (GMP) and provide comprehensive analytical documentation to support regulatory submissions and formulation development.
Identification & chemistry
| Generic name | Trimebutine |
|---|---|
| Molecule type | Small molecule |
| CAS | 39133-31-8 |
| UNII | QZ1OJ92E5R |
| DrugBank ID | DB09089 |
Pharmacology
| Summary | Trimebutine modulates gastrointestinal motility through concentration-dependent effects on ion channels and opioid receptors. It inhibits voltage-dependent L-type calcium channels and calcium-activated potassium channels in smooth muscle, reducing calcium influx and altering membrane depolarization to regulate contractility. Additionally, trimebutine acts as a weak mu-opioid receptor agonist, contributing to its spasmolytic and local anesthetic properties. |
|---|---|
| Mechanism of action | At high concentrations, trimebutine is shown to inhibit the extracellular Ca2+ influx in the smooth muscle cells through voltage dependent L-type Ca2+ channels and further Ca2+ release from intracellular Ca2+ stores [A19691, A19689]. Trimebutine is suggested to bind to the inactivated state of the calcium channel with high affinity. Reduced calcium influx attenuates membrane depolarization and decrease colon peristalsis. It also inhibits outward K+ currents in response to membrane depolarization of the GI smooth muscle cells at resting conditions through inhibition of delayed rectifier K+ channels and Ca2+ dependent K+ channels, which results in induced muscle contractions [A19691, A19695]. Trimebutine binds to mu opioid receptors with more selectivity compared to delta or kappa opioid receptors but with lower affinity than their natural ligands. Its metabolites (N-monodesmethyl-trimebutine or nor-trimebutine), are also shown to bind to opoid receptors on brain membranes and myenteric synaptosomes . |
| Pharmacodynamics | Trimebutine is a spasmolytic agent that acts directly on smooth muscle to modulate gastric motility. It shows a "dual function" that stimulates or inhibits spontaneous contractions depending on the concentration and prior contractile activity in the preparation. Targeting ion conductance that regulates GI motility, trimebutine inhibits the inward calcium currents and calcium-dependent potassium currents in a concentration-dependent manner . At lower concentrations (1-10uM), trimebutine depolarizes the resting membrane potential without affecting the amplitude of contractions, which is thought to be mediated by inhibition of outward potassium currents. It is also shown to activate T-type Ca2+ channel and increase gastric emptying, intestinal and colonic contractility . At higher concentrations (100-300uM), reduced amplitude of spontaneous contractions and action potentials is thought to be mediated by inhibition of L-type Ca2+ channels and inward calcium current . Trimebutine mediates a local anesthetic action by acting as a weak agonist at mu opioid receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | agonist |
| Voltage-dependent L-type calcium channel | Humans | inhibitor |
| Calcium-activated potassium channel | Humans | inhibitor |
ADME / PK
| Absorption | The free base form or salt form of trimebutine are rapidly absorbed after oral administration, with the peak plasma concentration reached after 1 hour of ingestion . The time to reach peak plasma concentration following a single oral dose of 200mg trimebutine is 0.80 hours . |
|---|---|
| Half-life | The elimination half life is approximately 1 hour following a single oral dose of 2mg/kg , and 2.77 hours following a single oral dose 200 mg . |
| Protein binding | Protein binding is minimal with 5% in vivo and in vitro to serum albumin . |
| Metabolism | Trimebutine undergoes extensive hepatic first-pass metabolism. Nortrimebutine, or N-monodesmethyltrimebutine, is the main metabolite that retains pharmacological activity on the colon. This metabolite can undergo second N-demethylation to form N-didesmethyltrimebutine. Other main urinary metabolites (2-amino, 2-methylamino or 2-dimethylamino-2-phenylbutan-1-ol) can be formed via hydrolysis of the ester bond of desmethylated metabolites or initial hydrolysis of the ester bond of trimebutine followed by sequential N-demethylation . Trimebutine is also prone to sulphate and/or glucuronic acid conjugation . |
| Route of elimination | Renal elimination is predominant while excretion into feces is also observed (5-12%). About 94% of an oral dose of trimebutine is eliminated by the kidneys in the form of various metabolites and less than 2.4% of total ingested drug is recovered as unchanged parent drug in the urine . |
| Volume of distribution | Trimebutine is most likely to be accumulated in the stomach and the intestinal walls in highest concentrations. The fetal transfer is reported to be low . |
Formulation & handling
- Trimebutine is a small molecule API primarily formulated for oral administration with multiple tablet and suspension forms, also available for intravenous and intramuscular injection. This compound exhibits low water solubility and a relatively high LogP of 4.11, which may affect formulation strategies for solubility enhancement and bioavailability. The API requires administration before meals, indicating potential sensitivity to food, which should be considered in dosing form design and patient instructions.
Regulatory status
| Lifecycle | The API's primary patent protections in Canada have expired, allowing for generic manufacturing and distribution. As a result, the product is in a mature market phase with multiple generic options available. |
|---|
| Markets | Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Trimebutine involves several originator companies supplying branded products primarily in Canada, with multiple formulations including tablets and injections. Branded presence is concentrated in the Canadian market, with limited indication of distribution in the US or EU. Patent expiry status suggests that generic competition is likely established or imminent, facilitating broader B2B sourcing opportunities. |
|---|
Safety
| Toxicity | Common gastrointestinal adverse effects include dry mouth, foul taste, diarrhea, dyspepsia, epigastric pain, nausea and constipation. Some CNS effects include drowsiness, fatigue, dizziness, hot/cold sensations and headaches. In case of overdosage, gastric lavage is recommended. Oral LD50 in mouse and rats is >5000 mg/kg and 2500 mg/kg in rabbits, respectively. Trimebutine is not reported to display teratogenic, mutagenic or carcinogenic potential . |
|---|
- Handle with care to avoid ingestion and inhalation due to potential gastrointestinal and CNS effects such as nausea, dizziness, and headache
- In cases of accidental overdose, gastric lavage is advised as an emergency intervention
- Oral LD50 values exceed 2500 mg/kg in animal models, indicating moderate acute toxicity
Trimebutine is a type of Motility inhibitors
Motility inhibitors are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are used to regulate and control the movement of the gastrointestinal tract. These inhibitors play a crucial role in treating conditions such as irritable bowel syndrome (IBS), gastroesophageal reflux disease (GERD), and other gastrointestinal disorders.
Motility inhibitors work by blocking the action of certain neurotransmitters and receptors in the gastrointestinal tract, thereby reducing the frequency and intensity of contractions in the smooth muscles. This leads to a decrease in the speed of food passage through the digestive system, providing relief from symptoms like abdominal pain, bloating, and diarrhea.
One commonly used motility inhibitor is metoclopramide, which acts by inhibiting dopamine receptors in the gastrointestinal tract. It enhances the contractions of the stomach and small intestine while relaxing the muscles of the pyloric sphincter, thus improving gastric emptying and reducing reflux.
Another important motility inhibitor is loperamide, which works by slowing down the muscular contractions of the intestines. It is commonly used to treat diarrhea by increasing the time it takes for stool to move through the digestive system.
Motility inhibitors are available in various forms, including tablets, capsules, and oral suspensions. They are generally well-tolerated, but like any medication, they can have side effects such as drowsiness, dizziness, and constipation.
In summary, motility inhibitors are an essential subcategory of pharmaceutical APIs used to manage gastrointestinal disorders by regulating the movement of the digestive tract. They provide relief from symptoms and improve overall digestive function, enhancing the quality of life for individuals suffering from these conditions.
Trimebutine (Motility inhibitors), classified under Gastrointestinal Agents
Gastrointestinal Agents belong to the pharmaceutical API category that focuses on treating disorders and ailments related to the digestive system. These agents play a crucial role in addressing various gastrointestinal conditions, such as acid reflux, ulcers, irritable bowel syndrome (IBS), and inflammatory bowel disease (IBD).
One of the key types of gastrointestinal agents is proton pump inhibitors (PPIs), which work by reducing the production of stomach acid. PPIs help in treating conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. Another essential class of agents is antacids, which neutralize excessive stomach acid, providing relief from heartburn and indigestion.
Gastrointestinal agents also include antispasmodics that alleviate abdominal cramps and spasms associated with conditions like IBS. These drugs work by relaxing the smooth muscles of the digestive tract. Additionally, there are drugs categorized as laxatives that aid in relieving constipation by promoting bowel movements.
Moreover, certain gastrointestinal agents act as antiemetics, effectively reducing nausea and vomiting. These drugs are particularly useful for patients undergoing chemotherapy or experiencing motion sickness.
Pharmaceutical companies develop and manufacture a wide range of gastrointestinal agents in various forms, including tablets, capsules, suspensions, and injections. These agents are typically formulated using active pharmaceutical ingredients (APIs) and other excipients to ensure their efficacy and safety.
In conclusion, gastrointestinal agents form a vital category of pharmaceutical APIs, providing relief from digestive disorders and improving overall gastrointestinal health. The availability of diverse agents catering to different conditions ensures that patients can receive targeted treatment for their specific gastrointestinal needs.
Trimebutine API manufacturers & distributors
Compare qualified Trimebutine API suppliers worldwide. We currently have 11 companies offering Trimebutine API, with manufacturing taking place in 6 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Edmond Pharma (Recipharm) | Producer | Italy | Italy | CoA, JDMF | 20 products |
| Isochem | Producer | France | France | CEP, CoA, FDA, GMP, USDMF | 12 products |
| Moehs | Producer | Spain | Spain | CEP, CoA, EDMF/ASMF, GMP | 50 products |
| PMC Isochem | Producer | France | France | CEP, CoA, GMP | 7 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Shiratori Pharmaceutical | Producer | Japan | Japan | CoA, JDMF | 9 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 762 products |
| Suanfarma | Distributor | Spain | European Union | CEP, CoA, GDP, GMP, ISO9001, USDMF | 13 products |
| Sumitomo Chemical | Producer | Japan | Japan | CoA, JDMF | 28 products |
| Zhejiang East Asia Pharma... | Producer | China | China | CoA, JDMF | 4 products |
| Zhejiang East-Asia Pharma | Producer | China | China | CEP, CoA, GMP, JDMF | 7 products |
When sending a request, specify which Trimebutine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Trimebutine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
