Name | Prucalopride |
CAS number | 179474-81-8 |
Related CAS# | 179474-85-2 (Succinate); 179474-81-8 (free base); 179474-80-7 (HCl) |
EINECS number | 1312995-182-4 |
Synonym | R-108512; R 108512; R108512; R 093877; R-093877; R093877; R 93877; R-93877; R93877； Prucalopride; Prucalopride free base; Motegrity; Resolor; Resotran; 4-amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide |
Description | Prucalopride is a serotonin type 4 (5-HT4) receptor agonist that has potent prokinetic activity and is used as therapy for chronic idiopathic constipation. Prucalopride has applications in treating diabetic and idiopathic gastroparesis. |
Structure |  |
Molecular Formula | C18H26ClN3O3 |
Molecular Weight | 367.87 g/mol |
Appearance | Solid powder |
Quality Standard | USP Standard |
Assay | ≥98% |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Storage Condition | Store in cool place. Keep container tightly closed in a dry and well ventilated place. |
Shelf Life | >2 years if stored properly |
Sample package | Aluminium foil bag |
Commercial package | Aluminium Tin, Fiber drum |
Origin | China |
Prucalopride is a medication primarily used to treat chronic idiopathic constipation (CIC) in adults. As a selective serotonin receptor agonist, specifically targeting the 5-hydroxytryptamine receptor 4 (5-HT4), it enhances gastrointestinal motility by promoting the movement of waste through the bowel.
Mechanism of Action
Prucalopride acts as a 5-HT4 receptor agonist, which leads to increased gastrointestinal motility. By stimulating these receptors, prucalopride enhances the release of acetylcholine, a key neurotransmitter that facilitates smooth muscle contractions in the gastrointestinal tract. This action results in:
Increased synchronous contractions in the large intestine.
Decreased frequency of isolated contractions in the proximal colon.
Stimulation of giant migratory contractions, which are crucial for bowel movements
Applications
Prucalopride is mainly prescribed for:
Chronic Idiopathic Constipation (CIC): This condition is characterized by infrequent bowel movements and difficulty in passing stools lasting for three months or longer without an identifiable cause.
It may also be explored for other gastrointestinal disorders, but its primary indication remains CIC.
Routes of Administration
Prucalopride is administered orally in tablet form, typically taken once daily with or without food. It is crucial for patients to adhere to their prescribed dosage and schedule for optimal results.
Safety and Side Effects
Common Side Effects
The most frequently reported side effects include:
Diarrhea
Abdominal pain
Nausea
Headache
These effects often occur within the first few days of treatment and may resolve as the body adjusts.
Serious Side Effects
Serious adverse reactions can include:
Difficulty breathing
Rash or hives
Swelling of face, lips, tongue, or throat
Patients are advised to seek immediate medical attention if they experience severe abdominal pain, bloody diarrhea, or significant mood changes.
Long-term Safety
Clinical studies have indicated that prucalopride has a favorable safety profile with no significant cardiovascular risks observed compared to other prokinetic agents.
Pharmacokinetics
Absorption and Distribution
Prucalopride is well absorbed after oral administration, reaching peak plasma concentrations approximately 2.77 hours post-dose. The bioavailability is significant, allowing effective therapeutic action at recommended doses of 2 mg to 4 mg daily for adults, with a lower dose recommended for elderly patients (1 mg) due to altered pharmacokinetics related to renal function.
Metabolism and Excretion
The drug is primarily excreted unchanged through urine (about 60% of the dose), with minimal hepatic metabolism. It exhibits low potential for pharmacokinetic interactions with other drugs, making it relatively safe to use alongside various medications.
Special Populations
Pharmacokinetic parameters can vary based on age and renal function. In older adults or those with renal impairment, plasma concentrations may be higher than in younger individuals with normal renal function.
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