MOTEGRITY PRUCALOPRIDE 1 mg Tablet, Film Coated, 30-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Serotonin-4 Receptor Agonist class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Prucalopride is used to treat chronic idiopathic constipation (CIC; difficult or infrequent passage of stools that lasts for 3 months or longer and is not caused by a disease or a medication). Prucalopride is in a class of medications called serotonin receptor agonists. It works by increasing the movement of waste through the bowel.
Read the full MedlinePlus article ↗- 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:
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💊 What it looks like
Where does this data come from?
🧪 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.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII 0WZ8WG20P6
Hypromellose 2910 is a plant-based cellulose derivative that acts as a thickener, binder, and film-coating agent. It helps control how quickly the medicine dissolves and protects the tablet or capsule from moisture and light.
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Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII SA1B764746
A synthetic polymer commonly used as a solvent and binder in medicines. It helps dissolve active ingredients, improve texture, and ensure consistent tablet or capsule formation.
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Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
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Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.
8 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
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Can inactive ingredients matter?
💲 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 | $17.725 | $531.74 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $17.75 | $532.52 / 30 tablets |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Prucalopride 1 mg 00054-0749-13 | Hikma | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 00406-6301-03 | SpecGx | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 00781-8158-31 | Sandoz | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 31722-0391-30 | Camber | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 60505-4806-03 | Apotex | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 69097-0218-02 | Cipla | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 69238-2698-01 | Amneal | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride succinate 1 mg 70069-0821-01 | Somerset | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 70748-0389-01 | Lupin | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 70954-0596-10 | ANI | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Prucalopride 1 mg 72205-0218-30 | Novadoz | 30 tablets | $0.653 | AB | Availability likely | save 96% |
| Motegrity 1 mgthis 54092-0546-01 | Takeda | 30 tablets | $17.725 | AB | Availability likely | — |
| 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?
⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Code | What it grants | Expires |
|---|---|---|
| M-14 | New indication / labeling change (3-year) | Jul 10, 2028 |
| M-14 | New indication / labeling change (3-year) | Jul 10, 2028 |
Is there a generic version of MOTEGRITY 1 MG TABLET?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
Why do different websites show different generic release dates?
What does “FDA listed” mean?
What does a patent or protection date mean here?
What does “current Orange Book estimate” mean?
Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
What is the difference between patents and exclusivity?
Why are there multiple patent dates?
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 54092-0546-01 You're viewing this | 30 TABLET, FILM COATED in 1 BOTTLE (54092-546-01) | 2018-12-14 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE MOTEGRITY ® is indicated for the treatment of chronic idiopathic constipation (CIC) in adults. MOTEGRITY is 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 MOTEGRITY 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 MOTEGRITY Tablets: 1 mg prucalopride: White to off-white, round, biconvex film-coated tablet debossed with "PRU 1" on one side and no debossing on the other side. 2 mg prucalopride: Pink, round, biconvex film-coated tablet debossed with "PRU 2" on one side and no debossing on the other side. Tablets: 1 mg, 2 mg of prucalopride. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS MOTEGRITY is contraindicated in patients with: A history of hypersensitivity to MOTEGRITY. 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 MOTEGRITY. ( 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 MOTEGRITY 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 MOTEGRITY [see Adverse Reactions (6.1 , 6.2) ] . A causal association between treatment with MOTEGRITY and an increased risk of suicidal ideation and behavior has not been established.
Monitor all patients treated with MOTEGRITY 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 MOTEGRITY 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 Takeda Pharmaceuticals at 1-800-828-2088 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 MOTEGRITY 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 MOTEGRITY 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 MOTEGRITY and a rate higher than patients receiving placebo. in Double-Blind Placebo-Controlled Trials of CIC of at least 12 Weeks Duration Adverse Reaction MOTEGRITY 2 mg Once Daily N=1,251 Includes 93 patients who started on MOTEGRITY 1 mg and increased to MOTEGRITY 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 MOTEGRITY 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 MOTEGRITY 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 MOTEGRITY 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 MOTEGRITY 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% MOTEGRITY, 1% placebo), headache (1% MOTEGRITY, 1% placebo), diarrhea (1% MOTEGRITY, <1% placebo), or abdominal pain (1% MOTEGRITY, 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 MOTEGRITY at doses including 0.5 mg, 1 mg, 2 mg, or 4 mg per day in adult patients with CIC (the recommended dosage of MOTEGRITY for CIC is 2 mg once daily). The total exposure in the double-blind trials was 565 patient-years in the MOTEGRITY group, 384 patient-years in the placebo group, and 2,769 patient-years in the double-blind and open-label clinical trials.
Cardiovascular Safety Analysis In an evaluation by an independent adjudication comm…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to MOTEGRITY during pregnancy. Healthcare providers are encouraged to register patients by contacting MotherToBaby Pregnancy Studies conducted by the Organization of Teratology Information Specialists (OTIS) at 1-877-311-8972 or visiting https://mothertobaby.org/pregnancy-studies/ . 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 MOTEGRITY and any potential adverse effects on the breastfed child from MOTEGRITY 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 MOTEGRITY have not been established in pediatric patients. MOTEGRITY was evaluated in a 12-week randomized, double-blind, placebo-controlled study, followed by a 36-week double-blind extension study in patients 6 months to 17 years with functional constipation. The interim analysis of the primary endpoint showed that the number of spontaneous bowel movements per week over 12 weeks was similar between the MOTEGRITY and placebo groups, indicating that the study was unlikely to demonstrate effectiveness.
Therefore, the study was terminated early for futility. Adverse reactions reported in pediatric patients in this study were similar to those reported in adults.
8.5 Geriatric Use Of the 2,484 patients treated…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to MOTEGRITY during pregnancy. Healthcare providers are encouraged to register patients by contacting MotherToBaby Pregnancy Studies conducted by the Organization of Teratology Information Specialists (OTIS) at 1-877-311-8972 or visiting https://mothertobaby.org/pregnancy-studies/ . 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 MOTEGRITY have not been established in pediatric patients. MOTEGRITY was evaluated in a 12-week randomized, double-blind, placebo-controlled study, followed by a 36-week double-blind extension study in patients 6 months to 17 years with functional constipation. The interim analysis of the primary endpoint showed that the number of spontaneous bowel movements per week over 12 weeks was similar between the MOTEGRITY and placebo groups, indicating that the study was unlikely to demonstrate effectiveness.
Therefore, the study was terminated early for futility. Adverse reactions reported in pediatric patients in this study were similar to those reported in adults.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 2,484 patients treated with MOTEGRITY 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 MOTEGRITY 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, MOTEGRITY 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 average…
🧬 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 MOTEGRITY tablets containing 1 mg prucalopride are white to off-white, round, biconvex film-coated tablets debossed with "PRU 1" on one side and no debossing on the other side. They are supplied as: NDC 54092-546-01: HDPE bottle of 30 tablets, with child-resistant closure. MOTEGRITY tablets containing 2 mg prucalopride are pink, round, biconvex film-coated tablets debossed with "PRU 2" on one side and no debossing on the other side.
They are supplied as: NDC 54092-547-01: HDPE bottle of 30 tablets, with child-resistant closure. Store MOTEGRITY at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (between 59°F to 86°F) [see USP Controlled Room Temperature]. Store MOTEGRITY in the original container to protect from moisture.
📦 Storage and Handling ▾
Store MOTEGRITY at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (between 59°F to 86°F) [see USP Controlled Room Temperature]. Store MOTEGRITY in the original container to protect from moisture.
📋 Description ▾
11 DESCRIPTION MOTEGRITY (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-dihydrobenzofuran-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 MOTEGRITY contains 1 mg of prucalopride (equivalent to 1.32 mg prucalopride succinate), and the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, and microcrystalline cellulose.
The coating for the 1-mg tablet contains hypromellose, lactose monohydrate, polyethylene glycol 3000, titanium dioxide, and triacetin. Each 2-mg film-coated tablet of MOTEGRITY contains 2 mg of prucalopride (equivalent to 2.64 mg prucalopride succinate), and the following inactive ingredients: colloidal silicon dioxide, lactose monohydrate, magnesium stearate, and microcrystalline cellulose. The coating for the 2-mg tablet contains hypromellose, lactose monohydrate, polyethylene glycol 3000, titanium dioxide, triacetin, red iron oxide, yellow iron oxide, and FD&C Blue #2.
Chemical Structure
💬 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 MOTEGRITY. 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 MOTEGRITY immediately and contact their healthcare provider if any of these symptoms occur [see Warnings and Precautions (5.1) ] . Pregnancy: Advise patients that there is a pregnancy registry that monitors pregnancy outcomes in women exposed to MOTEGRITY during pregnancy [see Use in Specific Populations (8.1) ]. Storage Advise patients to keep MOTEGRITY in the original container to protect from moisture.