Peringatan Keamanan

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 L872.

Trimebutine

DB09089

small molecule approved

Deskripsi

Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders A19691. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not a FDA-approved drug, but it is available in Canada and several other international countries.

Struktur Molekul 2D

Berat 387.476
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is approximately 1 hour following a single oral dose of 2mg/kg [A19692], and 2.77 hours following a single oral dose 200 mg [L872].
Volume Distribusi 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 [A19692].
Klirens (Clearance) -

Absorpsi

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 A19692. The time to reach peak plasma concentration following a single oral dose of 200mg trimebutine is 0.80 hours L872.

Metabolisme

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 A19694. Trimebutine is also prone to sulphate and/or glucuronic acid conjugation L872.

Rute Eliminasi

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 A19692 and less than 2.4% of total ingested drug is recovered as unchanged parent drug in the urine L872.

Interaksi Makanan

1 Data
  • 1. Take before a meal.

Interaksi Obat

1722 Data
Ceritinib Trimebutine may increase the bradycardic activities of Ceritinib.
Ivabradine Trimebutine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Trimebutine.
Aclidinium The risk or severity of adverse effects can be increased when Trimebutine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Trimebutine.
Mirabegron The risk or severity of urinary retention can be increased when Trimebutine is combined with Mirabegron.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Trimebutine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Trimebutine.
Tiotropium The risk or severity of adverse effects can be increased when Trimebutine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Trimebutine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Trimebutine is combined with Umeclidinium.
Cimetidine The serum concentration of Trimebutine can be increased when it is combined with Cimetidine.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Trimebutine.
Efavirenz The serum concentration of Trimebutine can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Trimebutine can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Trimebutine can be decreased when used in combination with Nafcillin.
Nitroprusside Trimebutine may increase the hypotensive activities of Nitroprusside.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Trimebutine.
Lithium citrate The risk or severity of adverse effects can be increased when Trimebutine is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Trimebutine is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Trimebutine is combined with Lithium hydroxide.
Glycopyrronium The risk or severity of adverse effects can be increased when Trimebutine is combined with Glycopyrronium.
Boceprevir The serum concentration of Trimebutine can be increased when it is combined with Boceprevir.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Trimebutine is combined with Botulinum toxin type A.
Glucagon Trimebutine may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Trimebutine may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Trimebutine is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Trimebutine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Trimebutine is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Trimebutine is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Trimebutine is combined with Bezitramide.
Tramadol The risk or severity of adverse effects can be increased when Trimebutine is combined with Tramadol.
Morphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Morphine.
Hydromorphone The risk or severity of adverse effects can be increased when Trimebutine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Trimebutine is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Trimebutine is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Trimebutine is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Trimebutine is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Trimebutine is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Trimebutine is combined with Remifentanil.
Buprenorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Buprenorphine.
Hydrocodone The risk or severity of adverse effects can be increased when Trimebutine is combined with Hydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Trimebutine is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Trimebutine is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Trimebutine is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Trimebutine is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Trimebutine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Trimebutine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Trimebutine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Trimebutine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Dihydromorphine.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Trimebutine is combined with Tapentadol.
Ketobemidone The risk or severity of adverse effects can be increased when Trimebutine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Trimebutine is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Trimebutine is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Trimebutine is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Trimebutine is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Trimebutine is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Trimebutine is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Trimebutine is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Trimebutine is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Trimebutine is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Trimebutine is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Trimebutine is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Trimebutine is combined with Carfentanil, C-11.
Methadone The risk or severity of adverse effects can be increased when Trimebutine is combined with Methadone.
Codeine The risk or severity of adverse effects can be increased when Trimebutine is combined with Codeine.
Benzhydrocodone The risk or severity of adverse effects can be increased when Trimebutine is combined with Benzhydrocodone.
Levacetylmethadol The risk or severity of adverse effects can be increased when Trimebutine is combined with Levacetylmethadol.
Alfentanil The risk or severity of adverse effects can be increased when Trimebutine is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Trimebutine is combined with Fentanyl.
Meperidine The risk or severity of adverse effects can be increased when Trimebutine is combined with Meperidine.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Trimebutine is combined with Dextropropoxyphene.
Naloxegol The risk or severity of adverse effects can be increased when Trimebutine is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Trimebutine.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Trimebutine.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Trimebutine.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Trimebutine.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Trimebutine.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Trimebutine.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Trimebutine.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Trimebutine.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Trimebutine.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Trimebutine.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Trimebutine.
Benzquinamide The risk or severity of adverse effects can be increased when Benzquinamide is combined with Trimebutine.
Tropicamide The risk or severity of adverse effects can be increased when Tropicamide is combined with Trimebutine.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Trimebutine.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Trimebutine.
Cyclopentolate The risk or severity of adverse effects can be increased when Cyclopentolate is combined with Trimebutine.
Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Trimebutine.
Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Trimebutine.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Trimebutine.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Trimebutine.

Target Protein

Mu-type opioid receptor OPRM1
Voltage-dependent L-type calcium channel CACNA1C
Calcium-activated potassium channel KCNMA1
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Voltage-dependent T-type calcium channel CACNA1G

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26424038
    Radulovic M, Anand P, Korsten MA, Gong B: Targeting Ion Channels: An Important Therapeutic Implication in Gastrointestinal Dysmotility in Patients With Spinal Cord Injury. J Neurogastroenterol Motil. 2015 Oct 1;21(4):494-502. doi: 10.5056/jnm15061.
  • PMID: 21725804
    Lee HT, Kim BJ: Trimebutine as a modulator of gastrointestinal motility. Arch Pharm Res. 2011 Jun;34(6):861-4. doi: 10.1007/s12272-011-0600-7.
  • PMID: 9364286
    Delvaux M, Wingate D: Trimebutine: mechanism of action, effects on gastrointestinal function and clinical results. J Int Med Res. 1997 Sep-Oct;25(5):225-46.
  • PMID: 8220900
    Nagasaki M, Komori S, Ohashi H: Effect of trimebutine on voltage-activated calcium current in rabbit ileal smooth muscle cells. Br J Pharmacol. 1993 Sep;110(1):399-403.
  • PMID: 2571489
    Miura Y, Chishima S, Takeyama S: Studies of metabolic pathways of trimebutine by simultaneous administration of trimebutine and its deuterium-labeled metabolite. Drug Metab Dispos. 1989 Jul-Aug;17(4):455-62.
  • PMID: 21725819
    Tan W, Zhang H, Luo HS, Xia H: Effects of trimebutine maleate on colonic motility through Ca(2)+-activated K+ channels and L-type Ca(2)+ channels. Arch Pharm Res. 2011 Jun;34(6):979-85. doi: 10.1007/s12272-011-0615-0. Epub 2011 Jul 2.
  • PMID: 8389715
    Nagasaki M, Komori S, Tamaki H, Ohashi H: Effect of trimebutine on K+ current in rabbit ileal smooth muscle cells. Eur J Pharmacol. 1993 Apr 28;235(2-3):197-203.

Contoh Produk & Brand

Produk: 7 • International brands: 68
Produk
  • Apo-trimebutine
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo-trimebutine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Mint-trimebutine
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Mint-trimebutine
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Modulon
    Tablet • 200 mg • Oral • Canada • Approved
  • Modulon Inj 50mg/5ml
    Liquid • 10 mg / 1 mL • Intramuscular; Intravenous • Canada • Approved
  • Modulon Tab 100mg
    Tablet • 100 mg • Oral • Canada • Approved
International Brands
  • Altrip — Spedrog-Caillon, Argentina
  • Anytin — Ahngook, South Korea
  • Biorgan — Ivax, Argentina
  • Bumetin — Galeno
  • Butikinon — Towa Yakuhin
  • Cerekinon — Mitsubishi Tanabe Pharma
  • Cineprac — Liferpal, Mexico
  • Colixane — Sanitas, Argentina
  • Colonix — Grupo Farma, Ecuador
  • Colperin — Gedeon Richter, Romania

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