Prucalopride 1 mg Tablet, Film Coated, 30-count — NDC 0054-0749-13 (Billing 00054-0749-13)
This is a package of 30 tablets of Prucalopride 1 mg Tablet, Film Coated from Hikma Pharmaceuticals USA Inc, marketed since Jun 2025 and currently FDA-listed; retail pharmacies pay about $0.6393 per tablet (NADAC). It is this product's only package size.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification
- GSN (GCN sequence number): 066216
- GCN: 28446
- HICL (First Databank): 036920
- AHFS class code: 56:32.00.00
- RxCUI (RxNorm): 2107345
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Serotonin-4 Receptor Agonist class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
Clinical
- Chronic idiopathic constipation — or CIC — is ongoing constipation where doctors can't find a specific underlying cause. It's not constipation from a medication or another disease;...
- What exactly is chronic idiopathic constipation, and is that what this is for?
- Prucalopride reaches steady, stable levels in your bloodstream within about 3 to 4 days of once-daily dosing, so many people start to notice a difference within the first week. The...
- You can take prucalopride with or without food — it makes no difference to how well the medication is absorbed. Pick whatever time of day works best for your routine and stick with...
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Prucalopride — tap one for details:
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.639 | $19.18 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $1.16 | $34.69 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $3.13 | $93.93 / 30 tablets |
Where does this data come from?
- CMS NADAC weekly file · file of Sep 30, 2026
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · through Q1 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 00054-0749-13 You're viewing this Main listing | 30 TABLET, FILM COATED in 1 BOTTLE | 2025-06-24 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Prucalopride 1 mgthis 00054-0749-13 | Hikma | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 00406-6301-03 | SpecGx | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 00781-8158-31 | Sandoz | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 31722-0391-30 | Camber | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 60505-4806-03 | Apotex | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 69097-0218-02 | Cipla | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 69238-2698-01 | Amneal | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride succinate 1 mg 70069-0821-01 | Somerset | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 70748-0389-01 | Lupin | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 70954-0596-10 | ANI | 30 tablets | $0.639 | AB | Availability likely | — |
| Prucalopride 1 mg 72205-0218-30 | Novadoz | 30 tablets | $0.639 | AB | Availability likely | — |
| Motegrity 1 mg 54092-0546-01 | Takeda | 30 tablets | $17.731 | AB | Availability likely | +2673% |
| Prucalopride 1 mg 27241-0294-30 | Ajanta | 30 tablets | — | AB | FDA listed | — |
| prucalopride 1 mg 70771-1899-03 | Zydus | 30 tablets | — | AB | FDA listed | — |
| prucalopride 1 mg 72578-0221-06 | Viona | 30 tablets | — | AB | FDA listed | — |
| Prucalopride 1 mg 73190-0038-30 | AvKARE | 30 tablets | — | AB | FDA listed | — |
| Prucalopride 1 mg 83085-0005-30 | SKG | 30 tablets | — | AB | FDA listed | — |
| Prucalopride 1 mg 46708-0077-30 | Alembic | 30 tablets | — | AB | FDA listed | — |
| Prucalopride 1 mg 62332-0077-30 | Alembic | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Sep 3, 2026
- CMS NADAC weekly file · file of Sep 30, 2026
Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
- FDA Orange Book · refreshed Sep 3, 2026
What it looks like
Where does this data come from?
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Prucalopride tablets are indicated for the treatment of chronic idiopathic constipation (CIC) in adults. Prucalopride tablets are a serotonin-4 (5-HT 4 ) receptor agonist indicated for the treatment of chronic idiopathic constipation (CIC) in adults. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Prucalopride tablets can be taken with or without food. The recommended dosage by patient population is shown in Table 1. Table 1: Recommended Dosage Regimen and Dosage Adjustments by Population Population with CIC Recommended Oral Dose Regimen Adults 2 mg once daily Patients with severe renal impairment (creatinine clearance (CrCL) less than 30 mL/min) [see Use in Specific Populations ( 8.5 , 8.6 )] .
1 mg once daily • Take with or without food. ( 2 ) • Recommended dosage by patient population: Population with CIC Recommended Oral Dose Regimen Adults 2 mg once daily. ( 2 ) Patients with severe renal impairment (creatinine clearance (CrCL) less than 30 mL/min) 1 mg once daily.
( 2 , 8.5 , 8.6 )
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Prucalopride Tablets: • 1 mg prucalopride: White to off-white, round, biconvex film-coated tablet debossed with “54” on one side and “13” on the other side. • 2 mg prucalopride: Pink to light pink, round, biconvex film-coated tablet debossed with “54” on one side and “15” on the other side. Tablets: 1 mg, 2 mg of prucalopride. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Prucalopride is contraindicated in patients with: • A history of hypersensitivity to prucalopride. Reactions including dyspnea, rash, pruritus, urticaria, and facial edema have been observed [see Adverse Reactions ( 6.2 )] . • Intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the intestinal tract such as Crohn’s disease, ulcerative colitis, and toxic megacolon/megarectum. • Hypersensitivity to prucalopride ( 4 ) • Intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the intestinal tract such as Crohn’s disease, ulcerative colitis, and toxic megacolon/megarectum.
( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Suicidal Ideation and Behavior : Monitor patients for suicidal ideation and behavior as well as self-injurious ideation and new-onset or worsening of depression. Instruct patients to discontinue prucalopride immediately and contact their healthcare provider if they experience any unusual changes in mood or behavior, or they experience emerging suicidal thoughts or behaviors. ( 5.1 )
5.1Suicidal Ideation and Behavior In clinical trials, suicides, suicide attempts, and suicidal ideation have been reported. Postmarketing cases of suicidal ideation and behavior as well as self-injurious ideation and new onset or worsening of depression have been reported within the first few weeks of starting prucalopride [see Adverse Reactions ( 6.1 , 6.2 )] . A causal association between treatment with prucalopride and an increased risk of suicidal ideation and behavior has not been established.
Monitor all patients treated with prucalopride for new onset or worsening of depression or the emergence of suicidal thoughts and behaviors. Counsel patients, their caregivers, and family members of patients to be aware of any unusual changes in mood or behavior and alert the healthcare provider. Instruct patients to discontinue prucalopride immediately and contact their healthcare provider if they experience any of these symptoms.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Most common adverse reactions (≥2%) are headache, abdominal pain, nausea, diarrhea, abdominal distension, dizziness, vomiting, flatulence, and fatigue. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data described below represent 2,530 patients (1,251 received prucalopride 2 mg once daily and 1,279 received placebo) with CIC from 6 double-blind, placebo-controlled clinical trials of 12 weeks to 24 weeks in duration. In these trials overall, patients were primarily female (76%) and white (76%).
The mean age was 47 years (range 17 to 95 years) [see Clinical Studies ( 14 )] . Common Adverse Reactions Table 2 below summarizes the incidence (%) of common adverse reactions occurring in at least 2% of patients with CIC receiving either 2 mg of prucalopride once daily or placebo and at an incidence greater than in the placebo group from the six double-blind placebo-controlled trials described above. Table 2: Common Adverse Reactions Reported in ≥2% of patients receiving prucalopride and a rate higher than patients receiving placebo. in Double-Blind Placebo-Controlled Trials of CIC of at least 12 Weeks Duration Adverse Reaction Prucalopride 2 mg Once Daily N=1,251 Includes 93 patients who started on prucalopride 1 mg and increased to prucalopride 2 mg. % Placebo N=1,279 % Headache 19 9 Abdominal pain Includes abdominal pain, upper abdominal pain, lower abdominal pain, abdominal tenderness, abdominal discomfort, and epigastric discomfort.
16 11 Nausea 14 7 Diarrhea 13 5 Abdominal distension 5 4 Dizziness 4 2 Vomiting 3 2 Flatulence 3 2 Fatigue 2 1 Less Common Adverse Reactions Less common adverse reactions occurring in <2% of patients receiving prucalopride 2 mg once daily include: Gastrointestinal disorders: Abnormal gastrointestinal sounds Metabolism and nutrition disorders: Decreased appetite Nervous system disorders: Migraine Renal and urinary disorders: Pollakiuria Diarrhea Of the patients who reported diarrhea, 70% (110 out of 157) reported it in the first week of treatment.
Diarrhea typically resolved within a few days in 73% (80 out of 110) of those patients. Severe diarrhea was reported in 1.8% of patients treated with prucalopride 2 mg compared to 1% of patients in the placebo group, and had a similar onset and duration as diarrhea overall. Headache Of the patients who reported headache, 66% (157 out of 237) treated with prucalopride 2 mg once daily reported onset in the first 2 days of treatment.
Symptoms typically resolved within a few days in 65% (102 out of 157) of those patients. Adverse Reactions Leading to Discontinuation In the 6 clinical trials described above, 5% of patients treated with 2 mg of prucalopride once daily discontinued due to adverse reactions, compared to 3% of patients in the placebo group. The most common adverse reactions leading to discontinuation were nausea (2% prucalopride, 1% placebo), headache (1% prucalopride, 1% placebo), diarrhea (1% prucalopride, <1% placebo), or abdominal pain (1% prucalopride, 1% placebo).
Adverse Reactions of Special Interest Adverse reactions of special interest were evaluated in a pool of 28 completed clinical trials (19 double-blind and 9 open-label) for prucalopride at doses including 0.5 mg, 1 mg, 2 mg, or 4 mg per day in adult patients with CIC (the recommended dosage of prucalopride for CIC is 2 mg once daily). The total exposure in the double-blind trials was 565 patient-years in the prucalopride group, 384 patient-years in the placebo group, and 2,769 patient-years in the double-blind and open-label clinical trials.
Cardiovascular Safety Analys… [Excerpted — this section continues on DailyMed.]
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Available data from case reports with prucalopride use in pregnant women are insufficient to identify any drug-associated risks of miscarriage, major birth defects, or adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed with prucalopride administration during the period of organogenesis to pregnant rats and rabbits at doses up to approximately 390 times and 780 times, respectively, the recommended human dose of 2 mg/day (see Data) .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Data Animal Data In oral embryofetal development studies in rats and rabbits, prucalopride was administered to pregnant animals at doses of 5, 20, and 80 mg/kg/day throughout the period of organogenesis. No adverse embryofetal developmental effects were observed in either rats or rabbits up to the highest oral dose of 80 mg/kg/day (about 390 times and 780 times the recommended human dose of 2 mg/day, respectively, based on body surface area). In an oral pre- and post-natal development study in rats, prucalopride was administered at doses of 5, 20, and 80 mg/kg/day.
At the 80-mg/kg dose (about 390 times the recommended human dose of 2 mg/day, based on body surface area), a slight decrease in overall survival rate of pups after 7 days was observed, which could be due to maternal toxicity observed at this dose.
8.2Lactation Risk Summary Prucalopride is present in breast milk (see Data) . There are no data on the effects of prucalopride on the breastfed child or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for prucalopride and any potential adverse effects on the breastfed child from prucalopride or from the underlying maternal condition.
Data In an open-label study in 8 healthy lactating women in the weaning stage, plasma and milk samples were collected at predose (day 1 and 4), and then 2, 4, 8, 12, and 24 hours (day 4) after a 2-mg dose of prucalopride was administered once daily for 4 days. Prucalopride is excreted in breast milk with a milk to plasma AUC ratio of 2.65:1; the average amount passed to the infant was estimated to be 1.74 mcg/kg/day, which is about 6% of the maternal dose, adjusted for body weight. The prucalopride concentration detected in breast milk during weaning may not reflect the prucalopride concentration in breast milk during full milk production.
8.4Pediatric Use The safety and effectiveness of prucalopride have not been established in pediatric patients. Pediatric information describing a clinical study in which efficacy was not demonstrated is approved for Takeda Pharmaceuticals U.S.A., Inc’s MOTEGRITY (prucalopride) tablets. However, due to Takeda Pharmaceuticals U.S.A., Inc’s marketing exclusivity rights, this drug product is not labeled with that information.
8.5Geriatric Use Of the 2,484 patients treated with prucalopride 1 mg or 2 mg once daily in 6 controlled trials of at least 12-week duration in patients with CIC, 15% were 65 years of age and over, and 5% were 75 years of age and over [see Clinical Studies ( 14 )] . No overall differences in safety and effectiveness were observed between elderly and younger patients. In an additional 4-week double-blind, placebo-controlled dose escalation study in 89 elderly nursing home residents with CIC (PRU-USA-26, NCT00627692), no unanticipated safety issues were identified.
Elderly subjects had higher prucalopride exposure compared to younger subjects. However, the effect of age on the pharmacokinetics of prucalopride appeared to be rel… [Excerpted — this section continues on DailyMed.]
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Available data from case reports with prucalopride use in pregnant women are insufficient to identify any drug-associated risks of miscarriage, major birth defects, or adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed with prucalopride administration during the period of organogenesis to pregnant rats and rabbits at doses up to approximately 390 times and 780 times, respectively, the recommended human dose of 2 mg/day (see Data) .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Data Animal Data In oral embryofetal development studies in rats and rabbits, prucalopride was administered to pregnant animals at doses of 5, 20, and 80 mg/kg/day throughout the period of organogenesis. No adverse embryofetal developmental effects were observed in either rats or rabbits up to the highest oral dose of 80 mg/kg/day (about 390 times and 780 times the recommended human dose of 2 mg/day, respectively, based on body surface area). In an oral pre- and post-natal development study in rats, prucalopride was administered at doses of 5, 20, and 80 mg/kg/day.
At the 80-mg/kg dose (about 390 times the recommended human dose of 2 mg/day, based on body surface area), a slight decrease in overall survival rate of pups after 7 days was observed, which could be due to maternal toxicity observed at this dose.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of prucalopride have not been established in pediatric patients. Pediatric information describing a clinical study in which efficacy was not demonstrated is approved for Takeda Pharmaceuticals U.S.A., Inc’s MOTEGRITY (prucalopride) tablets. However, due to Takeda Pharmaceuticals U.S.A., Inc’s marketing exclusivity rights, this drug product is not labeled with that information.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 2,484 patients treated with prucalopride 1 mg or 2 mg once daily in 6 controlled trials of at least 12-week duration in patients with CIC, 15% were 65 years of age and over, and 5% were 75 years of age and over [see Clinical Studies ( 14 )] . No overall differences in safety and effectiveness were observed between elderly and younger patients. In an additional 4-week double-blind, placebo-controlled dose escalation study in 89 elderly nursing home residents with CIC (PRU-USA-26, NCT00627692), no unanticipated safety issues were identified.
Elderly subjects had higher prucalopride exposure compared to younger subjects. However, the effect of age on the pharmacokinetics of prucalopride appeared to be related to decreased renal function [see Clinical Pharmacology ( 12.3 )] . Adjust the dosage in elderly patients based on renal function [see Dosage and Administration ( 2 ), Use in Specific Populations ( 8.6 )] .
🆘 Overdosage ▾
10 OVERDOSAGE An overdose may result in appearance of symptoms from an exaggeration of the known pharmacodynamic effects of prucalopride and includes headache, nausea, and diarrhea. Specific treatment is not available for prucalopride overdose. Should an overdose occur, treat symptomatically and institute supportive measures, as required. Extensive fluid loss from diarrhea or vomiting may require correction of electrolyte disturbances.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Prucalopride, a selective serotonin type 4 (5-HT 4 ) receptor agonist, is a gastrointestinal (GI) prokinetic agent that stimulates colonic peristalsis (high-amplitude propagating contractions [HAPCs]), which increases bowel motility. Prucalopride was devoid of effects mediated via 5-HT 2A , 5-HT 2B , 5-HT 3 , motilin or CCK-A receptors in vitro at concentrations exceeding 5-HT 4 receptor affinity by 150-fold or greater. In isolated GI tissues from various animal species, prucalopride facilitated acetylcholine release to enhance the amplitude of contractions and stimulate peristalsis.
In rats and dogs, prucalopride stimulated gastrointestinal motility with contractions starting from the proximal colon to the anal sphincter.
12.2Pharmacodynamics High Amplitude Propagating Contractions Following a single 2-mg dose of prucalopride in patients with CIC, prucalopride increased the number of high amplitude propagating contractions (HAPCs) during the first 12 hours as compared with an osmotic laxative treatment. In addition, prucalopride 4 mg once daily (2 times the maximum human recommended dose of 2 mg) for 7 days increased the amplitude of HAPCs in healthy subjects without affecting colonic phasic activity as compared with placebo. Colonic Transit Time An integrated analysis of 3 randomized, placebo-controlled, dose-finding studies in 280 patients with CIC showed that after once daily treatment with 2 mg of prucalopride, the mean colonic transit time was reduced by 12 hours from a baseline of 65 hours for prucalopride 2 mg, compared to an increase of 0.5 hours from a baseline of 66 hours in the placebo group.
Cardiac Electrophysiology At a dose 5 times the maximum approved recommended dose, prucalopride does not prolong the QT interval to any clinically relevant extent.
12.3Pharmacokinetics The pharmacokinetics of prucalopride has been evaluated in healthy subjects and is dose-proportional within and beyond the therapeutic range (tested up to 20 mg, 10 times the maximum approved recommended dose). Prucalopride administered once daily displays time-independent kinetics during prolonged treatment. With once daily administration of 2 mg prucalopride, pharmacokinetic steady-state is attained within 3 to 4 days, and steady-state plasma concentrations fluctuate between trough and peak values of 2.5 and 7 ng/mL, respectively, with mean plasma AUC 0-24h of 109 ng•h/mL.
The accumulation ratio after once daily dosing ranged from 1.9 to 2.3. The terminal half-life is approximately 1 day. Pharmacokinetic parameters in patients with CIC are similar to those seen in healthy subjects.
Absorption Following a single oral dose of 2 mg prucalopride in healthy subjects, peak plasma concentrations are observed within 2 to 3 hours after administration. The absolute oral bioavailability is >90%. Effect of Food Concomitant intake with a high-fat meal (1,000 kcal total, 500 kcal from fat) does not influence the oral bioavailability of prucalopride [see Dosage and Administration ( 2 )] .
Distribution Prucalopride has a steady-state volume of distribution (V ss ) of 567 liters after intravenous administration. The plasma protein binding of prucalopride is approximately 30%. Elimination Renal excretion is the main route of elimination of prucalopride.
Non-renal elimination contributes up to about 35% of the total. The plasma clearance of prucalopride averages 317 mL/min. Metabolism Prucalopride is a substrate of CYP3A4, in vitro .
In an oral dose study with radiolabeled prucalopride in healthy subjects, prucalopride made up 92 to 94% of the total radioactivity in plasma. There are 7 different known minor metabolites, the most abundant metabolite (O-desmethyl prucalopride acid) represents 0 to 1.7% of the total plasma exposure. Excretion Following oral administration of radiolabeled prucalopride in healthy subjects, 60 to 65% of the administered dose is excreted unchanged in urine and about 5% in feces.
On av… [Excerpted — this section continues on DailyMed.]
🧬 Mechanism of Action ▾
12.1Mechanism of Action Prucalopride, a selective serotonin type 4 (5-HT 4 ) receptor agonist, is a gastrointestinal (GI) prokinetic agent that stimulates colonic peristalsis (high-amplitude propagating contractions [HAPCs]), which increases bowel motility. Prucalopride was devoid of effects mediated via 5-HT 2A , 5-HT 2B , 5-HT 3 , motilin or CCK-A receptors in vitro at concentrations exceeding 5-HT 4 receptor affinity by 150-fold or greater. In isolated GI tissues from various animal species, prucalopride facilitated acetylcholine release to enhance the amplitude of contractions and stimulate peristalsis.
In rats and dogs, prucalopride stimulated gastrointestinal motility with contractions starting from the proximal colon to the anal sphincter.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Prucalopride tablets containing 1 mg prucalopride are white to off-white, round, biconvex film-coated tablets debossed with “54” on one side and “13” on the other side. They are supplied as: • NDC 0054-0749-13: HDPE bottle of 30 tablets, with child-resistant closure. Prucalopride tablets containing 2 mg prucalopride are pink to light pink, round, biconvex film-coated tablets debossed with “54” on one side and “15” on the other side.
They are supplied as: • NDC 0054-0750-13: HDPE bottle of 30 tablets, with child-resistant closure. Store prucalopride tablets at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (between 59° to 86°F) [see USP Controlled Room Temperature]. Store prucalopride tablets in the original container to protect from moisture.
📋 Description ▾
11 DESCRIPTION Prucalopride tablets for oral use contain prucalopride succinate, a dihydrobenzofurancarboxamide that is a serotonin type 4 (5-HT 4 ) receptor agonist. The IUPAC name is: 4-Amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide succinate. The molecular formula is C 18 H 26 ClN 3 O 3 •C 4 H 6 O 4 and the molecular weight is 485.96.
The structural formula is: Prucalopride succinate is a white to almost white powder. It is highly soluble in acidic aqueous media and alkaline aqueous media up to a pH of approximately 9. Each 1-mg film-coated tablet of prucalopride contains 1 mg of prucalopride (equivalent to 1.32 mg prucalopride succinate), and the following inactive ingredients: mannitol, silicified microcrystalline cellulose, magnesium stearate, and Opadry II (White).
Opadry II (White) contains: titanium dioxide, polydextrose, hypromellose, triacetin, polyethylene glycol. Each 2-mg film-coated tablet of prucalopride contains 2 mg of prucalopride (equivalent to 2.64 mg prucalopride succinate), and the following inactive ingredients: mannitol, silicified microcrystalline cellulose, magnesium stearate, and Opadry II (Pink). Opadry II (Pink) contains: polydextrose, titanium dioxide, hypromellose, triacetin, polyethylene glycol, FD&C Red #40 Allura Red AC Aluminum Lake, FD&C Yellow #6 Sunset Yellow Aluminum Lake, FD&C Blue #2 Indigo Carmine Aluminum Lake. prucalopride-structural-formula-image
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). • Suicidal Ideation and Behavior : Inform patients, their caregivers, and family members that suicidal ideation and behavior, self-injurious ideation as well as new onset or worsening depression have been reported in patients treated with prucalopride. Advise them to be aware of any unusual changes in mood or behavior, new onset or worsening of depression, or the emergence of suicidal thoughts or behavior.
Instruct patients, caregivers, and family members to discontinue prucalopride immediately and contact their healthcare provider if any of these symptoms occur [see Warnings and Precautions ( 5.1 )] . Storage Advise patients to keep prucalopride tablets in the original container to protect from moisture. For more information, call Hikma Pharmaceuticals USA Inc. at 1-800-962-8364.
Distributed by: Hikma Pharmaceuticals USA Inc. Berkeley Heights, NJ 07922 C50001221/03 Revised: November 2025
🧬 Pharmacokinetics ▾
12.3Pharmacokinetics The pharmacokinetics of prucalopride has been evaluated in healthy subjects and is dose-proportional within and beyond the therapeutic range (tested up to 20 mg, 10 times the maximum approved recommended dose). Prucalopride administered once daily displays time-independent kinetics during prolonged treatment. With once daily administration of 2 mg prucalopride, pharmacokinetic steady-state is attained within 3 to 4 days, and steady-state plasma concentrations fluctuate between trough and peak values of 2.5 and 7 ng/mL, respectively, with mean plasma AUC 0-24h of 109 ng•h/mL.
The accumulation ratio after once daily dosing ranged from 1.9 to 2.3. The terminal half-life is approximately 1 day. Pharmacokinetic parameters in patients with CIC are similar to those seen in healthy subjects.
Absorption Following a single oral dose of 2 mg prucalopride in healthy subjects, peak plasma concentrations are observed within 2 to 3 hours after administration. The absolute oral bioavailability is >90%. Effect of Food Concomitant intake with a high-fat meal (1,000 kcal total, 500 kcal from fat) does not influence the oral bioavailability of prucalopride [see Dosage and Administration ( 2 )] .
Distribution Prucalopride has a steady-state volume of distribution (V ss ) of 567 liters after intravenous administration. The plasma protein binding of prucalopride is approximately 30%. Elimination Renal excretion is the main route of elimination of prucalopride.
Non-renal elimination contributes up to about 35% of the total. The plasma clearance of prucalopride averages 317 mL/min. Metabolism Prucalopride is a substrate of CYP3A4, in vitro .
In an oral dose study with radiolabeled prucalopride in healthy subjects, prucalopride made up 92 to 94% of the total radioactivity in plasma. There are 7 different known minor metabolites, the most abundant metabolite (O-desmethyl prucalopride acid) represents 0 to 1.7% of the total plasma exposure. Excretion Following oral administration of radiolabeled prucalopride in healthy subjects, 60 to 65% of the administered dose is excreted unchanged in urine and about 5% in feces.
On average, 84.2% of administered radioactive dose was recovered in urine and 13.3% of the dose was recovered in feces. Seven metabolites were recovered in urine and feces, with the most abundant metabolite (O-desmethyl prucalopride acid) accounting for 3.2% and 3.1% of the dose in urine and feces, respectively. None of the other metabolites accounted for more than 3% of the dose.
Renal elimination of prucalopride involves both passive filtration and active secretion. Use in Specific Populations Population pharmacokinetic analysis of a combined study population of 1,343 subjects indicated that there were no clinically significant differences in the pharmacokinetics of prucalopride based on age (17 to 95 years), sex, race (89% white, 7% black, 4% other), or body weight (37 to 161 kg), after accounting for the effect of renal function. Geriatric Patients After once daily dosing of 1 mg, peak plasma concentrations (C max ) and AUC of prucalopride in geriatric subjects were 26% to 28% higher than in younger adult subjects.
The effect of age appeared to be related to decreased renal function in the elderly. Additionally, a population pharmacokinetic analysis indicated that age was not a significant covariate, after accounting for the effect of renal function [see Use in Specific Populations ( 8.5 )] . Patients with Renal Impairment After a single 2-mg oral dose, the mean AUC 0-inf of prucalopride increased 1.23-fold in subjects with mild renal impairment (creatinine clearance 60 to ≤89 mL/min), 1.4-fold in subjects with moderate renal impairment (creatinine clearance 30 to ≤59 mL/min), and 2.38-fold in subjects with severe renal impairment (creatinine clearance 15 to ≤29 mL/min), compared to subjects with normal renal function.
The pharmacokinetics of prucalopride in patients with end-stage renal disease or undergoing dialysi… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacodynamics ▾
12.2Pharmacodynamics High Amplitude Propagating Contractions Following a single 2-mg dose of prucalopride in patients with CIC, prucalopride increased the number of high amplitude propagating contractions (HAPCs) during the first 12 hours as compared with an osmotic laxative treatment. In addition, prucalopride 4 mg once daily (2 times the maximum human recommended dose of 2 mg) for 7 days increased the amplitude of HAPCs in healthy subjects without affecting colonic phasic activity as compared with placebo. Colonic Transit Time An integrated analysis of 3 randomized, placebo-controlled, dose-finding studies in 280 patients with CIC showed that after once daily treatment with 2 mg of prucalopride, the mean colonic transit time was reduced by 12 hours from a baseline of 65 hours for prucalopride 2 mg, compared to an increase of 0.5 hours from a baseline of 66 hours in the placebo group.
Cardiac Electrophysiology At a dose 5 times the maximum approved recommended dose, prucalopride does not prolong the QT interval to any clinically relevant extent.
🔬 Clinical Studies ▾
14 CLINICAL STUDIES The efficacy of prucalopride for the treatment of CIC was evaluated in six double-blind, placebo-controlled, randomized, multicenter clinical trials in 2,484 adult patients (Studies 1 to 6; see Table 3 ). Studies 1 through 5 were 12-week treatment duration and Study 6 included 24 weeks of treatment. Patients less than 65 years were dosed with prucalopride 2 mg once daily.
In Studies 2 and 6, the geriatric patients started on prucalopride 1 mg once daily and, if necessary, the dose was increased to 2 mg after 2 or 4 weeks of treatment in the event of insufficient response at 1 mg; of these patients 81% increased to 2 mg. Overall, the majority of patients were female (76%) and white (76%), and also included Asian (19%) and black (3%). The mean adult age was 47±16 years (range 17 to 95 years) and the mean duration of constipation was 16±15 years with 28% of patients having chronic constipation for at least 20 years.
Table 3: Main Studies in the Prucalopride Clinical Program Study Number Duration Study 1 (PRU-CRC-3001, NCT01116206) 12 Weeks Study 2 (SPD555-302, NCT01147926) 12 Weeks Study 3 (PRU-INT-6, NCT00488137) 12 Weeks Study 4 (PRU-USA-11, NCT00483886) 12 Weeks Study 5 (PRU-USA-13, NCT00485940) 12 Weeks Study 6 (SPD-555-401, NCT01424228) 24 Weeks Eligible patients required a history of chronic constipation defined as having fewer than 3 spontaneous bowel movements (SBMs) per week that resulted in a feeling of complete evacuation (complete, spontaneous bowel movement [CSBM]) and 1 or more of the following symptoms for greater than 25% of bowel movements in the preceding 3 months, with symptoms onset more than 6 months prior to screening: • Lumpy or hard stools • Sensation of incomplete evacuation • Straining at defecation Patients who never had SBMs were eligible.
In Study 1, eligibility also included sensation of ano-rectal obstruction or blockade or the need for digital manipulation in more than 25% of bowel movements. In all studies, patients were excluded if constipation was due to secondary causes or suspected to be drug-induced. Efficacy was assessed using information provided by patients in a daily diary.
Primary Efficacy Results For the primary efficacy endpoint, a responder was defined as a patient with an average of 3 or more CSBMs per week, over the 12-week treatment period. In the Intent-to-Treat [ITT] population in the 6 trials, 1,237 received prucalopride 1 or 2 mg and 1,247 received placebo. Table 4 summarizes the results.
Table 4: Efficacy Responder Rates in Placebo-Controlled Studies of CIC: Proportion of Patients with an Average Weekly Frequency of ≥3 CSBMs per Week over 12 Weeks of Treatment (ITT Population) Study Prucalopride 1 or 2 mg Once Daily Placebo Treatment Difference (95% CI) p value N n (%) N n (%) Study 1 249 83 (33) 252 26 (10) 23 (16, 30) p<0.001 Study 2 177 67 (38) 181 32 (18) 20 (11, 29) p<0.001 Study 3 236 46 (19) 240 23 (10) 10 (4, 16) p=0.002 Study 4 190 55 (29) 193 25 (13) 16 (8, 24) p<0.001 Study 5 214 50 (24) 212 25 (12) 12 (4, 19) p<0.001 Study 6 171 43 (25) 169 34 (20) 5 (-4, 14) p=0.341 p-value based on a Cochran-Mantel-Haenszel test N = number of patients per treatment group n = number of responders In all studies, improvement in the frequency of CSBMs/week was seen as early as week 1 and was maintained through week 12.
Across the six studies, the median time to first CSBM after dosing of prucalopride on day 1 ranged from 1.4 to 4.7 days compared with 9.1 to 20.6 days in the placebo group. The median time to first SBM after dosing on day 1 ranged from 0.1 to 0.4 days in the prucalopride group compared with 1.0 to 1.6 days in the placebo group. Alternative Efficacy Endpoint Using an alternative efficacy endpoint, a responder was defined as a patient who had at least 3 CSBMs and an increase of at least 1 CSBM from baseline in a given week for at least 9 weeks out of the 12-week treatment period and for at least 3 of the last 4 weeks of the treatment period.
The diff… [Excerpted — this section continues on DailyMed.]
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis In a 2-year carcinogenicity study in mice, prucalopride was given by daily oral gavage at doses of 10, 20, and 80 mg/kg. An increased incidence of mammary gland adenocarcinomas was observed in female mice at 80 mg/kg/day. The finding is considered rodent-specific.
No significant neoplastic changes were seen in male mice dosed up to 80 mg/kg/day and in female mice dosed up to 20 mg/kg/day (exposure ratio of 219 and 24 times the human dosage of 2 mg per day in male and female mice, respectively, based on AUC). In a 2-year carcinogenicity study in rats, prucalopride was given by daily oral gavage at doses of 5, 20, and 80 mg/kg in males and 5, 10, and 40 mg/kg in females. In male and female rats there was a significant increase in the incidences of benign tumors, including hepatocellular adenomas, thyroid follicular adenomas, and mammary gland fibroadenomas.
An increased incidence of pituitary adenomas, pancreas islet cell adenomas, and adrenal gland benign pheochromocytomas was also seen in male rats. The increases in neoplastic changes occurred primarily at the high dose of 80 mg/kg/day in male rats and 40 mg/kg/day in female rats (exposure ratios 556 times (males) and 495 times (females) the human dosage of 2 mg per day, based on AUC). There was no significant increase in tumor incidence at doses up to 20 mg/kg/day in male rats and up to 10 mg/kg/day in female rats (exposure ratios of 63 and 40 times the human dosage of 2 mg per day in male and female rats, respectively, based on AUC).
In a 12-month carcinogenicity study in neonatal mice, prucalopride was administered by oral gavage at total dosages of 75, 150, and 300 mg/kg given across 2 doses on day 8 of age (one-third of total dosage) and day 15 of age (two-thirds of total dosage). Prucalopride was not tumorigenic at doses up to 300 mg/kg (>1,600 times the human exposure at 2 mg per day, based on AUC). Mechanistic studies demonstrated that the increase in tumor incidence in rodents related to stimulation of prolactin in endocrine tissues was associated with dopamine D2 antagonist activity.
The hepatic and thyroid tumors were due to induction of enzymes in liver and subsequent disruption of thyroid homeostasis. Mutagenesis Prucalopride was tested in a battery of assays, including the Ames bacterial mutation assay in Salmonella typhimurium and Escherichia coli , mouse lymphoma assay, chromosomal aberration assays in human lymphocytes, micronucleus test in mice, Vitotox test, and in vitro Unscheduled DNA Synthesis (UDS) studies. Prucalopride tested positive in the Ames bacterial mutation assay in the S. typhimurium TA100 strain, at concentrations ≥500 mcg/plate, both in the presence and absence of metabolic activation.
Prucalopride was negative in other assays evaluating mutagenesis, including in vitro mammalian-based assays (e.g., mouse lymphoma assay, chromosomal aberration assays in human lymphocytes) and in vivo tests (e.g., micronucleus test in mice, a UDS test, a gene mutation assay in Big Blue transgenic rats, and a 32 P-postlabeling study in target tissues identified in the carcinogenicity studies, including liver, mammary gland, thyroid, and adrenal tissues). Based on the weight of evidence, prucalopride does not appear to have a mutagenic potential.
Impairment of Fertility In an oral fertility and early embryonic development study performed in rats at doses of 5, 20, and 80 mg/kg/day, there was no evidence of adverse effects on fertility at doses up to 20 mg/kg. At the highest dose of 80 mg/kg (about 390 times the recommended human dose of 2 mg/day, based on body surface area), an increase in pre-coital interval, pseudo-pregnancies, and pre-implantation loss were seen. These effects could be secondary to increased prolactin secretion with prucalopride treatment.
13.2Animal Toxicology and/or Pharmacology In safety pharmacology studies, no relevant effects were observed… [Excerpted — this section continues on DailyMed.]
📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ▾
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis In a 2-year carcinogenicity study in mice, prucalopride was given by daily oral gavage at doses of 10, 20, and 80 mg/kg. An increased incidence of mammary gland adenocarcinomas was observed in female mice at 80 mg/kg/day. The finding is considered rodent-specific.
No significant neoplastic changes were seen in male mice dosed up to 80 mg/kg/day and in female mice dosed up to 20 mg/kg/day (exposure ratio of 219 and 24 times the human dosage of 2 mg per day in male and female mice, respectively, based on AUC). In a 2-year carcinogenicity study in rats, prucalopride was given by daily oral gavage at doses of 5, 20, and 80 mg/kg in males and 5, 10, and 40 mg/kg in females. In male and female rats there was a significant increase in the incidences of benign tumors, including hepatocellular adenomas, thyroid follicular adenomas, and mammary gland fibroadenomas.
An increased incidence of pituitary adenomas, pancreas islet cell adenomas, and adrenal gland benign pheochromocytomas was also seen in male rats. The increases in neoplastic changes occurred primarily at the high dose of 80 mg/kg/day in male rats and 40 mg/kg/day in female rats (exposure ratios 556 times (males) and 495 times (females) the human dosage of 2 mg per day, based on AUC). There was no significant increase in tumor incidence at doses up to 20 mg/kg/day in male rats and up to 10 mg/kg/day in female rats (exposure ratios of 63 and 40 times the human dosage of 2 mg per day in male and female rats, respectively, based on AUC).
In a 12-month carcinogenicity study in neonatal mice, prucalopride was administered by oral gavage at total dosages of 75, 150, and 300 mg/kg given across 2 doses on day 8 of age (one-third of total dosage) and day 15 of age (two-thirds of total dosage). Prucalopride was not tumorigenic at doses up to 300 mg/kg (>1,600 times the human exposure at 2 mg per day, based on AUC). Mechanistic studies demonstrated that the increase in tumor incidence in rodents related to stimulation of prolactin in endocrine tissues was associated with dopamine D2 antagonist activity.
The hepatic and thyroid tumors were due to induction of enzymes in liver and subsequent disruption of thyroid homeostasis. Mutagenesis Prucalopride was tested in a battery of assays, including the Ames bacterial mutation assay in Salmonella typhimurium and Escherichia coli , mouse lymphoma assay, chromosomal aberration assays in human lymphocytes, micronucleus test in mice, Vitotox test, and in vitro Unscheduled DNA Synthesis (UDS) studies. Prucalopride tested positive in the Ames bacterial mutation assay in the S. typhimurium TA100 strain, at concentrations ≥500 mcg/plate, both in the presence and absence of metabolic activation.
Prucalopride was negative in other assays evaluating mutagenesis, including in vitro mammalian-based assays (e.g., mouse lymphoma assay, chromosomal aberration assays in human lymphocytes) and in vivo tests (e.g., micronucleus test in mice, a UDS test, a gene mutation assay in Big Blue transgenic rats, and a 32 P-postlabeling study in target tissues identified in the carcinogenicity studies, including liver, mammary gland, thyroid, and adrenal tissues). Based on the weight of evidence, prucalopride does not appear to have a mutagenic potential.
Impairment of Fertility In an oral fertility and early embryonic development study performed in rats at doses of 5, 20, and 80 mg/kg/day, there was no evidence of adverse effects on fertility at doses up to 20 mg/kg. At the highest dose of 80 mg/kg (about 390 times the recommended human dose of 2 mg/day, based on body surface area), an increase in pre-coital interval, pseudo-pregnancies, and pre-implantation loss were seen. These effects could be secondary to increased prolactin secretion with prucalopride treatment.
📄 Patient Package Insert ▾
PATIENT INFORMATION Prucalopride (proo-KAL-oh-pride) Tablets, for oral use What are prucalopride tablets? Prucalopride tablets are a prescription medicine used in adults to treat a type of constipation called chronic idiopathic constipation (CIC). Idiopathic means the cause of the constipation is unknown.
It is not known if prucalopride tablets are safe and effective in children. Do not take prucalopride tablets if you: • are allergic to prucalopride tablets. Allergic reaction symptoms may include trouble breathing, rash, itching and swelling of your face, lips, tongue or throat. • have a tear in your stomach or intestinal wall (bowel perforation), a bowel blockage (intestinal obstruction) or serious conditions of the intestinal wall such as Crohn’s disease or ulcerative colitis.
Before taking prucalopride tablets, tell your healthcare provider about all of your medical conditions, including if you: • have or have had depression, suicidal thoughts or actions, or mood problems. • have kidney problems. Your healthcare provider may give you a lower dose of prucalopride tablets. • are pregnant or plan to become pregnant. It is not known if prucalopride tablets will harm your unborn baby. • are breastfeeding or plan to breastfeed.
Prucalopride can pass into your breastmilk. Talk with your healthcare provider about the best way to feed your baby if you take prucalopride tablets. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
How should I take prucalopride tablets? • Take 1 prucalopride tablet each day or as directed by your healthcare provider. • Take prucalopride tablets exactly as your healthcare provider tells you to take them. • Take prucalopride tablets with or without food. What are the possible side effects of prucalopride tablets? Prucalopride tablets may cause serious side effects, including: unusual changes in mood or behavior, thoughts of hurting yourself, trying to hurt yourself, or suicide.
Stop taking prucalopride tablets right away and tell your healthcare provider immediately if your depression gets worse, you feel sad, hopeless, begin to have thoughts of suicide, thoughts of hurting yourself or you have tried to hurt yourself or if you develop new depression. The most common side effects of prucalopride tablets include: • headache • nausea • dizziness • gas • stomach area (abdominal) pain or bloating • diarrhea • vomiting • fatigue These are not all the possible side effects of prucalopride tablets.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. How should I store prucalopride tablets? • Store prucalopride tablets at room temperature between 68° to 77°F (20° to 25°C). • Store prucalopride tablets in the original container to protect from moisture.
Keep prucalopride tablets and all medicines out of the reach of children. General information about the safe and effective use of prucalopride tablets. Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet.
Do not use prucalopride tablets for a condition for which they were not prescribed. Do not give prucalopride tablets to other people, even if they have the same symptoms that you have. They may harm them.
You can ask your pharmacist or healthcare provider for information about prucalopride tablets that is written for health professionals. What are the ingredients in prucalopride tablets? Active ingredient: prucalopride Inactive ingredients: mannitol, silicified microcrystalline cellulose, magnesium stearate.
In addition to the ingredients listed above, the 1 mg tablet contains Opadry II (White). Opadry II (White) contains titanium dioxide, polydextrose, hypromellose, triacetin, and polyethylene glycol. The 2 mg tablet contains Opadry II (Pink).
Opadry II (Pink) contains titanium dioxide, polydextrose, hypromellose, triacetin, polyethylene glycol, FD&C Re… [Excerpted — this section continues on DailyMed.]
📄 Package Label / Principal Display Panel ▾
PACKAGE/LABEL PRINCIPAL DISPLAY PANEL NDC 0054- 0749 -13 Prucalopride Tablets 1 mg 30 Tablets Rx only prucalopride 1 mg bottle label
PACKAGE/LABEL PRINCIPAL DISPLAY PANEL NDC 0054- 0750 -13 Prucalopride Tablets 2 mg 30 Tablets Rx only prucalopride 2 mg bottle label