ENTEREG
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ENTEREG (ENTEREG).
Selective 5-HT4 receptor agonist; enhances gastrointestinal motility by increasing peristalsis and accelerating colonic transit.
| Metabolism | Primarily metabolized by cytochrome P450 3A4 (CYP3A4); also involves CYP2D6 and CYP2C9 to a lesser extent. |
| Excretion | Primarily hepatobiliary excretion; unchanged drug and major metabolite (alvimopan) undergo extensive biliary elimination with fecal excretion accounting for >90% of total elimination. Renal excretion is minimal (<5% as unchanged drug). |
| Half-life | Terminal half-life is approximately 10–17 hours in healthy subjects. Clinically, the half-life may be prolonged in severe hepatic impairment but is not significantly altered in renal impairment. |
| Protein binding | Approximately 80–90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is about 30 L (approximately 0.4 L/kg), indicating distribution into extracellular fluid and tissues. |
| Bioavailability | Oral bioavailability is approximately 6–10% due to extensive first-pass metabolism; the drug is administered orally for local gastrointestinal activity. |
| Onset of Action | Oral administration: onset within 15–30 minutes for acceleration of gastrointestinal recovery after bowel resection. |
| Duration of Action | Duration of effect is approximately 12–24 hours; multiple dosing is typically used for up to 7 days postoperatively to maintain effect. |
Adults: 12 mg orally twice daily for up to 15 days, initiated within 30 minutes prior to surgery and continued postoperatively.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended for severe renal impairment (CrCl <30 mL/min) or dialysis. |
| Liver impairment | No dose adjustment for mild to moderate hepatic impairment (Child-Pugh A or B). Caution in severe hepatic impairment (Child-Pugh C); no specific dose recommendation. |
| Pediatric use | Not FDA-approved for pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to potential increased sensitivity and renal function decline. Monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ENTEREG (ENTEREG).
| Breastfeeding | No data on presence in human milk; caution advised; M/P ratio unknown. |
| Teratogenic Risk | No human data; animal studies at doses up to 10 mg/kg/day in rats and rabbits showed no teratogenicity at exposures lower than human dose; risk cannot be excluded due to lack of adequate human studies. |
| Fetal Monitoring | Monitor for gastrointestinal adverse effects in mother; fetal monitoring not specifically recommended; standard prenatal care. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to prucalopride or any excipients","Renal impairment requiring dialysis","Intestinal obstruction or perforation"]
| Precautions | ["May cause diarrhea, leading to electrolyte disturbances or hypovolemia","Use with caution in patients with severe renal impairment","Avoid use in patients with a history of mechanical gastrointestinal obstruction, perforation, or severe inflammatory bowel disease"] |
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| Fertility Effects | No human data; in animal studies at high doses, no adverse effects on fertility observed. |