prucalopride succinate

Contraindicated in:

Hypersensitivity;
Renal impairment requiring dialysis;
Intestinal obstruction/perforation (structural or functional), obstructive ileus, severe gastrointestinal inflammatory disease, including Crohn's disease, ulcerative colitis, toxic megacolon/megarectum;
Galactose intolerance, Lapp lactase deficiency or glucose/galactose malabsorption (tablets contain lactose);
OB: Not recommended for use during pregnancy;
Lactation: Not recommended for use while breastfeeding;
Pedi: Safety and effectiveness not established; not recommended for use.

Use Cautiously in:

Severe/clinically stable concurrent chronic diseases including liver, cardiovascular or lung disease, neurological or psychiatric disorders, cancer, AIDS or other disorders or insulin-dependent diabetes mellitus;
History of arrhythmias or cardiovascular disease, ischemic heart disease, pre-excitation syndromes (including Wolff-Parkinson-White syndrome, Lown-Ganong-Levine syndrome, or AV nodal disorders (↑ risk of arrhythmias);
Severe renal impairment (↓ dose recommended);
Geri: Due to age-related ↓ in renal function, ↓ dose is recommended.

Adv. Reactions/Side Effects ⬆ ⬇

CNS: headache, dizziness, fatigue

CV: ↓PR interval, palpitations, tachycardia

GI: abdominal pain, diarrhea, nausea, vomiting

Interactions ⬆ ⬇

Drug-drug:

Severe diarrhea may ↓ effectiveness of oral hormonal contraceptives; additional method of contraception recommended.
Blood levels and effects are ↑ by concurrent CYP3A4 and P-gp inhibitors including ketoconazole, verapamil, cyclosporine, and quinidine.
Beneficial effects may be ↓ by concurrent use of anticholinergics.

Availability ⬆ ⬇

Tablets (contain lactose): 1 mg; 2 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 2 mg once daily. If no bowel movement occurs in 3–4 days, add-on laxatives should be considered. If benefit is not obtained after 4 wk, prucalopride succinate should be discontinued.
PO (Adults >65 yr): 1 mg once daily.

Renal Impairment

PO (Adults ): GFR <30 mL/min/1.73m²: 1 mg once daily.

Action ⬆ ⬇

Acts as a serotonin (5–HT₄) receptor agonist with prokinetic properties. Enhances peristalsis and gastrointestinal propulsion.

Therapeutic effects:

Laxative effect.

Classifications ⬆ ⬇

Therapeutic Classification: prokinetic agents

Pharmacologic Classification: dihydrobenzofurancarboxamides

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed (90%) following oral administration.

Distribution: Rapidly and extensively distributed, enters breast milk.

Metabolism/Excretion: 60% excreted unchanged in urine, 3–8% unchanged in feces, minor amounts are extensively metabolized.

Half-Life: 24 hr.

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(normalization of bowel movements)

ROUTE	ONSET	PEAK	DURATION
PO	3–4 days	1–4 wk	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take prucalopride succinate as directed.
Caution the patient to discontinue the medication and notify health care professional with occurrence of severe diarrhea, signs of heart attack, black tarry stools, vomiting of blood or material that looks like coffee grounds.
Advise patient on a nutritional regimen and hydration, and exercise to decrease constipation.
Inform patient that if no bowel movement within 3 days of treatment, a "rescue" laxative may be added occasionally while taking prucalopride succinate.
Rep: Advise females of reproductive potential who are taking prucalopride succinate to use an effective method of birth control during treatment. If pregnancy occurs while taking this medication, contact health care professional immediately.

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Indications ⬇

Contraind./Precautions ⬆ ⬇