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Prucalopride

Medically reviewed by Drugs.com. Last updated on Aug 20, 2020.

Pronunciation

(proo KAL oh pride)

Index Terms

  • Prucalopride Succinate
  • R093877
  • R108512

Dosage Forms

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)]

Brand Names: U.S.

  • Motegrity

Pharmacologic Category

  • Gastrointestinal Agent, Prokinetic
  • Serotonin 5-HT4 Receptor Agonist

Pharmacology

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.

Absorption

Rapid

Distribution

Vd: 567 L (IV administration)

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)

Excretion

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

Time to Peak

2 to 3 hours

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)

Protein Binding

~30%

Use: Labeled Indications

Chronic idiopathic constipation: Treatment of chronic idiopathic constipation in adults

Off Label Uses

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

Data from a phase II, randomized, double-blind, placebo-controlled study support the use of prucalopride in the treatment of opioid-induced constipation in noncancer, chronic pain patients. Prucalopride improved patient-rated severity of constipation and effectiveness of treatment [Sloots 2010]. Additional trials may be necessary to further define the role of prucalopride in this condition.

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

Dosing: Adult

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

Dosing: Geriatric

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).

Administration

Oral: Administer without regard to meals.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F). Store in original container to protect from moisture.

Drug Interactions

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

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

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

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

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

Adverse Reactions

>10%:

Central nervous system: Headache (19%)

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

1% to 10%:

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

Genitourinary: Pollakiuria (<2%)

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

<1%, postmarketing, and/or case reports: Amnesia (Anton 2017), dyspnea, facial edema, loss of balance (Anton 2017), palpitations (Anton 2017), pruritus, skin rash, suicidal ideation, suicidal tendencies, urticaria, vaginal hemorrhage, visual hallucination (Anton 2017)

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. Closely monitor patients for 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.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Elderly: Use with caution in the elderly (limited data); dose reductions may be necessary.

Monitoring Parameters

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

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.

Patient Education

What is this drug used for?

• It is used to treat constipation.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache

• Nausea

• Vomiting

• Diarrhea

• Abdominal pain

• Bloating

• Passing gas

• Dizziness

• Loss of strength and energy

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Behavioral changes

• Mood changes

• Depression

• Thoughts of suicide

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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