PROPULSID QUICKSOLV
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROPULSID QUICKSOLV (PROPULSID QUICKSOLV).
Selective serotonin 5-HT4 receptor agonist; enhances release of acetylcholine in the enteric nervous system, increasing gastrointestinal motility without increasing gastric acid secretion.
| Metabolism | Extensively metabolized via CYP3A4; also metabolized by CYP2C8 and CYP2C9. Main metabolites: norcisapride (active) and others. |
| Excretion | Approximately 60-70% of a dose is excreted in urine as unchanged drug and metabolites; ~30% in feces via biliary excretion. |
| Half-life | Terminal elimination half-life is approximately 6–12 hours in adults; prolonged in hepatic impairment (up to 20–30 hours) and elderly. |
| Protein binding | 97–98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd ≈ 2–4 L/kg (large, indicating extensive tissue distribution). |
| Bioavailability | Oral bioavailability is 40–50% due to first-pass metabolism; approximately 70% for the oral disintegrating tablet formulation. |
| Onset of Action | Oral (tablet or suspension): 30–60 minutes; oral disintegrating tablet (Quicksolv): 15–30 minutes. |
| Duration of Action | Duration of prokinetic effect is 8–12 hours; clinical effects on gastric emptying last up to 4–6 hours after single dose. |
10 mg orally three times daily before meals. Maximum 20 mg per dose.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | For GFR <40 mL/min: reduce dose to 5 mg three times daily. No adjustment for GFR ≥40 mL/min. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: 5 mg twice daily. Child-Pugh Class C: contraindicated. |
| Pediatric use | Not recommended for children due to risk of serious arrhythmias. |
| Geriatric use | Start at 5 mg three times daily and titrate cautiously due to decreased metabolism and increased risk of QT prolongation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROPULSID QUICKSOLV (PROPULSID QUICKSOLV).
| Breastfeeding | Present in human milk. Milk-to-plasma ratio (M/P) not established. Use with caution due to potential for cardiac effects in the infant, including QT prolongation. Monitor infant for arrhythmias, diarrhea, and extrapyramidal symptoms. Consider alternative with better safety profile. |
| Teratogenic Risk | First trimester: Human data limited but no increased risk of major malformations in case series. Animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: No known fetal risk; used for gastroparesis in pregnancy without reported adverse outcomes. However, theoretical risk of QT prolongation exists due to cisapride's proarrhythmic potential. |
■ FDA Black Box Warning
Cisapride is associated with serious cardiac arrhythmias including ventricular tachycardia, ventricular fibrillation, torsade de pointes, and QT prolongation. Use is contraindicated with certain drugs and medical conditions that increase risk of arrhythmias.
| Serious Effects |
Concomitant use of CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors, nefazodone); history of QT prolongation; uncorrected electrolyte disorders; significant bradycardia; concurrent use of other QT-prolonging drugs; known hypersensitivity.
| Precautions | Risk of QT prolongation and serious arrhythmias; hypokalemia, hypomagnesemia, bradycardia, and concomitant use of QT-prolonging drugs increase risk. Avoid in patients with structural heart disease. May cause extrapyramidal effects and diarrhea. |
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| Fetal Monitoring | Maternal: Baseline and periodic ECG to monitor QT interval; serum electrolytes (K+, Mg2+); hepatic function; renal function. Fetal: Ultrasound for growth and anatomy; fetal heart rate monitoring if maternal QT prolongation or arrhythmias occur. |
| Fertility Effects | No known effects on human fertility. Animal studies at high doses showed no impairment of fertility. Theoretical concern due to prolactin elevation (dopamine antagonist) but not reported in clinical use. |