Cerekinon 20%
Cerekinon 20% Uses, Dosage, Side Effects, Food Interaction and all others data.
Cerekinon 20% maleate is a noncompetitive spasmolytic agent. It possesses moderate opiate receptor affinity and has marked anti-serotonin activity especially on 'mu' receptors. It induces regulation of spontaneous activity and increases synchronization between electrophysiological spikes and contractions in isolated guinea pig strips of colon and ileum. However, it does not alter normal motility, but regulates abnormal intestinal activity.
Cerekinon 20% 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 . Cerekinon 20% mediates a local anesthetic action by acting as a weak agonist at mu opioid receptors.
| Trade Name | Cerekinon 20% |
| Generic | Trimebutine |
| Trimebutine Other Names | Trimébutine, Trimebutine, Trimebutino |
| Type | |
| Formula | C22H29NO5 |
| Weight | Average: 387.476 Monoisotopic: 387.204573038 |
| Protein binding | Protein binding is minimal with 5% in vivo and in vitro to serum albumin . |
| Groups | Approved |
| Therapeutic Class | Anticholinergics |
| Manufacturer | |
| Available Country | Japan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Treatment and relief of symptoms associated with irritable bowel syndrome (spastic colon). Postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.
Cerekinon 20% is also used to associated treatment for these conditions: Irritable Bowel Syndrome (IBS), Gastrointestinal spasms, Postoperative paralytic ileus
How Cerekinon 20% works
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 . Cerekinon 20% 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 . Cerekinon 20% 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 .
Dosage
Cerekinon 20% dosage
For adults: 100 mg to 200 mg, 3 times per day before meals.
Side Effects
Cerekinon 20% maleate is generally well tolerated. The infrequently reported adverse effects are as follows: dry mouth, foul taste, diarrhea, dyspepsia, epigastric pain, nausea, constipation, drowsiness, fatigue, dizziness, hot/cold sensations, headache etc.
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. Cerekinon 20% is not reported to display teratogenic, mutagenic or carcinogenic potential .
Precaution
Elderly, pregnancy and lactation
Interaction
Cerekinon 20% maleate increases the duration of d-tubocurarine-induced curarization. No other druginteractions have been observed during clinical trial or otherwise reported.
Food Interaction
- Take before a meal.
Volume of Distribution
Cerekinon 20% is most likely to be accumulated in the stomach and the intestinal walls in highest concentrations. The fetal transfer is reported to be low .
Elimination Route
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 .
Elimination Route
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 .
Pregnancy & Breastfeeding use
Although teratological studies have not shown any drug related adverse effects on the course and outcome of pregnancy, the use of trimebutine maleate in pregnant women is not recommended.
Elderly, pregnancy and lactationIt is not known if trimebutine maleate passes into breast milk. This medication should be used while breast feeding only if the potential benefits outweigh risks to the nursing infants.
Contraindication
Patients with known hypersensitivity to trimebutine maleate or any excipient.
Acute Overdose
No evidence of overdosage have been reported to date. However, if overdosage should occur following oral administration, gastric lavage is recommended. Treatment should be made according to the symptoms observed.
Storage Condition
Store in a cool and dry place, protected from light and moisture. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Cerekinon 20%
Cerekinon 20% contains Trimebutine see full prescribing information from innovator Cerekinon 20% Monograph, Cerekinon 20% MSDS, Cerekinon 20% FDA label
FAQ
What is Cerekinon 20% used for?
It is used to treat symptoms of irritable bowel syndrome (spastic colon). Cerekinon 20% is also used to restart the movement of the gut after abdominal surgery and to prevent intestinal blockage.
How safe is Cerekinon 20%?
Cerekinon 20% is by no means a harmless drug, contrary to the impression given by the limited safety data available.
What are the common side effects of Cerekinon 20%?
The common side effects of Cerekinon 20% are include:
Dry mouth, heartburn, nausea, diarrhea, constipation, drowsiness, dizziness, tiredness or headache may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
How does Cerekinon 20% work?
Cerekinon 20% works by slowing down or normalizing the abnormal movements of the bowel. It is used to treat irritable bowel syndrome (spastic colon). This condition is caused by overactive movements of the bowels.
Is Cerekinon 20% safe during pregnancy?
The use of Cerekinon 20% by pregnant women is not recommended. If you become pregnant while taking this medication, contact your doctor immediately.
Is Cerekinon 20% safe during breastfeeding?
It is not known if Cerekinon 20% passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
Can I drink alcohol with Cerekinon 20%?
Consuming alcohol may intensify the effect of this product. If you choose to drink alcohol, do so in moderation.
Can I drive after taking Cerekinon 20%?
This drug may make you dizzy or drowsy. Alcohol can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
When is the best time to take Cerekinon 20%?
Best time to take Cerekinon 20% by mouth as directed before meals usually three times a day.
Who should not take Cerekinon 20%?
Cerekinon 20% should not be taken by anyone who is allergic to Cerekinon 20% or to any of the ingredients of the medication.
Can I take Cerekinon 20% for a long time?
Do not increase the dose, take it more often or continue taking this for longer than prescribed.
How long does Cerekinon 20% stay in my system?
The elimination half life is approximately 1 hour following a single oral dose of 2mg/kg 3, and 2.77 hours following a single oral dose 200 mg 8.
Is Cerekinon 20% a narcotic?
Cerekinon 20% is a drug with antimuscarinic and weak mu opioid agonist effects.
What happens if I miss a dose?
If you miss a dose, take it as soon as remembered, do not take it if it is near the time for the next dose, instead, skip the missed dose and resume your usual dosing schedule. Do not "double-up" the dose to catch up.
What happens if I overdose?
If overdose is suspected, contact your local poison control center or emergency room immediately. Cases of serious accidental or intentional trimebutine overdose have been reported in infants and young adults, leading to neurological disordersand cardiac .
How should I use Cerekinon 20%?
The adult recommended dose consists of up to 600 mg daily taken in 3 divided doses (200 mg 3 times daily) before meals.
Can Cerekinon 20% used for children?
Cerekinon 20% is not recommended for use by children under 12 years of age.
