Prucalopride

ESRD requiring dialysis: Contraindicated. Severe (GFR <30 ml/min/1.73 m²): 1 mg once daily.

Severe (Child-Pugh class C): Initially, 1 mg once daily, may be increased to 2 mg if necessary. Dosage recommendations may vary among individual products and between countries (refer to specific product or local guidelines).

May be taken with or without food.

Intestinal perforation or obstruction due to structural or functional disorder of the gut wall; obstructive ileus; severe inflammatory conditions of the gastrointestinal tract (e.g. Crohn's disease, ulcerative colitis and toxic megacolon or megarectum). ESRD requiring dialysis.

Patient with history of arrhythmia, ischaemic heart disease; severe and clinically unstable concomitant disease (e.g. cancer, AIDS, lung or other CV disease; neurological, psychiatric, and other endocrine disorders). Renal and severe hepatic impairment (Child-Pugh class C) impairment. Elderly. Pregnancy and lactation.

Significant: Severe diarrhoea; suicide, suicide attempts, and suicide ideation (including cases of self-injurious ideation and new or worsening depression).
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Abdominal pain, nausea, vomiting, flatulence, dyspepsia, abnormal bowel sounds, abdominal distension, rectal haemorrhage.
General disorders and administration site conditions: Fatigue, fever, malaise.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Dizziness, headache, tremors, migraine.
Renal and urinary disorders: Pollakiuria.

This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery. Women of childbearing potential must use effective contraception during treatment.

Monitor for improvement and frequency of bowel movements. Closely monitor for new onset or persistent worsening of depression or the emergence of suicidal thoughts and behaviours.

Symptoms: Nausea, headache, diarrhoea. Management: Symptomatic and supportive treatment. In cases of excessive fluid loss, correcting electrolyte disturbances may be necessary.

Description:
Mechanism of Action: Prucalopride, a dihydrobenzofurancarboxamide, is a selective, high-affinity type 4 serotonin (5-HT₄) receptor agonist with prokinetic properties. It enhances bowel motility by binding with high affinity to 5-HT₄ receptors, thereby promoting the release of acetylcholine to increase the amplitude of contractions and stimulate colonic peristalsis.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: >90%. Time to peak plasma concentration: 2-3 hours.
Distribution: Extensively distributed. Enters breast milk. Plasma protein binding: Approx 30%.
Metabolism: Metabolised very slowly in the liver.
Excretion: Mainly via urine (84.2%; 60-65% as unchanged drug); faeces (13.3%; 5% as unchanged drug). Elimination half-life: Approx 24 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3052762, Prucalopride. https://pubchem.ncbi.nlm.nih.gov/compound/Prucalopride. Accessed Jan. 27, 2025.

Store between 15-30°C. Protect from moisture.

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A06AX05 - prucalopride ; Belongs to the class of other laxatives.

Anon. Prucalopride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 22/11/2024.

Brayfield A, Cadart C (eds). Prucalopride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 26/12/2024.

Joint Formulary Committee. Prucalopride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/11/2024.

Mercury Pharma (NZ). Resotrans 1 mg and 2 mg Film Coated Tablet data sheet 23 January 2023. Medsafe. http://www.medsafe.govt.nz. Accessed 22/11/2024.

Motegrity Tablet, Film Coated (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 22/11/2024.

Prucalopride 1 mg Film-coated Tablets (DHP Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 22/11/2024.

Prucalopride. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 22/11/2024.

Resolor (DKSH Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 22/11/2024.