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Prucalopride: Drug information

Prucalopride: Drug information
(For additional information see "Prucalopride: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Motegrity
Brand Names: Canada
  • APO-Prucalopride;
  • JAMP Prucalopride;
  • Resotran
Pharmacologic Category
  • Gastrointestinal Agent, Prokinetic;
  • Serotonin 5-HT4 Receptor Agonist
Dosing: Adult
Chronic idiopathic constipation

Chronic idiopathic constipation: Oral: 2 mg once daily; consider adjunctive laxative therapy if no bowel movement within ≥3 consecutive days (Camilleri 2008; Yiannakou 2015).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute: 1 mg once daily

ESRD requiring hemodialysis: Avoid use.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; compared to normal hepatic function, prucalopride AUC was increased 10% to 20% in moderate and severe impairment (clinically nonsignificant).

Dosing: Older Adult

Refer to adult dosing; use with caution due to increased likelihood of decreased renal function. In some clinical trials, patients >65 years of age were initiated on 1 mg/day with the option to increase to 2 mg/day if needed after 2 or 4 weeks of treatment (Yiannakou 2015).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as succinate:

Motegrity: 1 mg

Motegrity: 2 mg [contains fd&c blue #2 (indigotine)]

Generic Equivalent Available: US

No

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as succinate:

Resotran: 1 mg

Resotran: 2 mg [contains fd&c blue #2 (indigo carm) aluminum lake]

Generic: 1 mg, 2 mg

Administration: Adult

Oral: Administer without regard to meals.

Use: Labeled Indications

Chronic idiopathic constipation: Treatment of chronic idiopathic constipation in adults

Use: Off-Label: Adult

Opioid-induced constipation in patients with chronic pain (noncancer)

Medication Safety Issues
Sound-alike/look-alike issues:

Resotran may be confused with Restoril

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Gastrointestinal: Abdominal pain (16%), nausea (14%), diarrhea (13%; severe diarrhea: 2%)

Nervous system: Headache (19%)

1% to 10%:

Gastrointestinal: Abdominal distension (5%), abnormal bowel sounds (<2%), decreased appetite (<2%), flatulence (3%), vomiting (3%)

Genitourinary: Pollakiuria (<2%)

Nervous system: Dizziness (4%), fatigue (2%), migraine (<2%)

Postmarketing:

Cardiovascular: Facial edema, palpitations (Anton 2017)

Dermatologic: Pruritus, skin rash, urticaria

Nervous system: Amnesia (Anton 2017), anxiety, depression, insomnia, loss of balance (Anton 2017), nightmares, suicidal ideation, suicidal tendencies, visual hallucination (Anton 2017)

Respiratory: Dyspnea

Contraindications

Hypersensitivity to prucalopride or any component of the formulation; intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the GI tract (eg, Crohn disease, ulcerative colitis, toxic megacolon/megarectum).

Canadian labeling: Additional contraindications not in US labeling: Renal impairment requiring dialysis

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: May cause dizziness and fatigue; caution patients about performing tasks that require mental alertness (eg, operating machinery or driving).

• Diarrhea: May cause diarrhea, sometimes severe; most often reported during first week of treatment and typically resolved within a few days. If severe or persistent diarrhea occurs, discontinue therapy and advise patient to consult health care provider.

• Suicidal ideation/behavior: Suicide, suicide attempts, and suicide ideation have been reported, including cases of self-injurious ideation and new or worsening depression within the first few weeks of initiation of therapy. Closely monitor patients for new onset or persistent worsening of depression or the emergence of suicidal thoughts and behaviors and discontinue therapy immediately for any symptoms.

Disease-related concerns:

• Renal impairment: Use with caution in patients with renal impairment; prucalopride mainly undergoes renal elimination. Dose reduction is required in severe impairment; avoid use in patients requiring dialysis.

Special populations:

• Older adult: Use with caution in older adults (limited data); dose reductions may be necessary.

Metabolism/Transport Effects

Substrate of P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Anticholinergic Agents: May diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Fosfomycin: Gastrointestinal Agents (Prokinetic) may decrease the serum concentration of Fosfomycin. Risk C: Monitor therapy

Levosulpiride: Benzamide Derivatives may enhance the adverse/toxic effect of Levosulpiride. Risk C: Monitor therapy

Opioid Agonists: May diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Sirolimus (Conventional): Gastrointestinal Agents (Prokinetic) may increase the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy

Reproductive Considerations

Consider use of appropriate contraception in females of reproductive potential.

Pregnancy Considerations

Information related to use in pregnancy is limited; spontaneous abortions were observed in clinical trials; however, available data is insufficient to evaluate the risk of adverse maternal or fetal outcomes.

Data collection to monitor pregnancy and infant outcomes following exposure to prucalopride is ongoing. Health care providers are encouraged to enroll patients exposed to prucalopride during pregnancy in the Organization of Teratology Information Specialists (OTIS) MotherToBaby Pregnancy Study (1-877-311-8972 or https://mothertobaby.org/pregnancy-studies/).

Breastfeeding Considerations

Prucalopride is present in breast milk.

In a study of 8 lactating women taking prucalopride 2 mg once daily for 4 days, breast milk concentrations of prucalopride were ~6% of the maternal dose. Sampling occurred prior to dosing on days 1 and 4 and over 24 hours after the maternal dose on day 4. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Monitoring Parameters

Frequency of bowel movements; worsening of depression or emergence of suicidal thoughts and behavior

Mechanism of Action

Prucalopride is a selective, high affinity 5-HT4 receptor agonist whose action at the receptor site promotes cholinergic and nonadrenergic, noncholinergic neurotransmission by enteric neurons leading to stimulation of the peristaltic reflex, intestinal secretions, and gastrointestinal motility.

Pharmacokinetics

Absorption: Rapid

Distribution: Vd: 567 L (IV administration)

Protein binding: ~30%

Metabolism: Minor route of elimination; 8 metabolites produced (in vitro data suggest that 4 of 8 metabolites have lower or similar affinity to prucalopride for 5-HT4 receptor) (Resotran Canadian product labeling)

Bioavailability: >90%

Half-life elimination: ~24 hours; terminal half-life increases to 34, 43, and 47 hours in mild, moderate, and severe renal impairment, respectively (Resotran Canadian product labeling)

Time to peak: 2 to 3 hours

Excretion: Primarily as unchanged drug: Urine (84.2%); feces (13.3%)

Pricing: US

Tablets (Motegrity Oral)

1 mg (per each): $19.44

2 mg (per each): $19.44

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Constinon (EG);
  • Dosne (AR);
  • Ercanol (AR);
  • Prucal (AR);
  • Prucalex (CL);
  • Prucasoft (EG);
  • Pruval (CL);
  • Resolor (AE, AT, BE, BH, BR, CH, CN, CO, CY, CZ, DE, DK, EE, EG, ES, FI, FR, GB, GR, HK, HR, IE, IL, JO, KR, KW, LB, LT, LU, MT, NL, NO, PE, PH, PL, PT, QA, RO, RU, SE, SG, SK, TH, TR, VE, VN);
  • Resotrans (AU, CR, DO, GT, HN, MX, NI, NZ, PA, SV);
  • Vegaprat (RU)


For country code abbreviations (show table)
  1. Anton C, Crawford C. Adverse effects of laxatives: update. Wolters Kluwer Adverse Drug Reaction Bulletin. 2017;303.
  2. Camilleri M, Kerstens R, Rykx A, et al, “A Placebo-Controlled Trial of Prucalopride for Severe Chronic Constipation,” N Engl J Med, 2008, 358(22):2344-54. [PubMed 18509121]
  3. Motegrity (prucalopride) [prescribing information]. Lexington, MA: Takeda Pharmaceuticals America; November 2020.
  4. Prucalopride. In chronic constipation: poorly documented risks. Prescrire Int. 2011;20(116):117-120. [PubMed 21648173]
  5. Resotran (prucalopride) [product monograph]. Toronto, Ontario, Canada: Janssen Inc; February 2019.
  6. Sloots CE, Rykx A, Cools M, et al, “Efficacy and Safety of Prucalopride in Patients With Chronic Noncancer Pain Suffering from Opioid-Induced Constipation,” Dig Dis Sci, 2010, 55(10):2912-21. [PubMed 20428949]
  7. Yiannakou Y, Piessevaux H, Bouchoucha M, et al. A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial to Evaluate the Efficacy, Safety, and Tolerability of Prucalopride in Men With Chronic Constipation. Am J Gastroenterol. 2015;110(5):741-748. [PubMed 25869393]
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