METOZOLV ODT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for METOZOLV ODT (METOZOLV ODT).
Selective 5-HT3 receptor antagonist; blocks serotonin action at vagal nerve terminals and in the chemoreceptor trigger zone, inhibiting emetic reflex.
| Metabolism | Hepatic via CYP1A2, CYP3A4, and CYP2D6; extensive first-pass metabolism. |
| Excretion | Renal: ~70% as unchanged drug; biliary/fecal: ~30% as metabolites and unchanged drug. |
| Half-life | ~1.5–2 hours in normal renal function; prolonged to 10–20 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | ~5% bound to albumin; minimal binding. |
| Volume of Distribution | 0.3–0.5 L/kg; indicates distribution into total body water. |
| Bioavailability | Oral: ~95% (bioequivalent to conventional tablet). |
| Onset of Action | Orally disintegrating tablet: 15–30 minutes. |
| Duration of Action | 4–6 hours; may be extended in renal impairment. |
2.5 mg to 5 mg orally once daily, as disintegrating tablet; may increase to 10 mg if needed
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | eGFR 30-60 mL/min: no adjustment; eGFR 15-29 mL/min: initial 2.5 mg daily, max 5 mg; eGFR <15 mL/min: not recommended (no data) |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: initial 2.5 mg daily, max 5 mg; Child-Pugh C: not recommended (no data) |
| Pediatric use | Not recommended for pediatric patients (safety and efficacy not established) |
| Geriatric use | Initiate at 2.5 mg once daily; monitor renal function and electrolyte balance; increased sensitivity due to age-related decline in renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for METOZOLV ODT (METOZOLV ODT).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Use with caution due to potential for kernicterus in neonates, especially with glucose-6-phosphate dehydrogenase deficiency. Weigh benefits against risks. |
| Teratogenic Risk | First trimester: Risk of neural tube defects and cleft palate based on animal studies and limited human data; avoid if possible. Second/third trimester: No specific malformations reported; monitor fetal growth and amniotic fluid index due to potential for oligohydramnios. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Headache Nausea Dizziness |
| Serious Effects |
["Hypersensitivity to metoclopramide or any component (note: Metozolv ODT contains metoclopramide)","History of tardive dyskinesia","Concurrent use of MAO inhibitors","Gastrointestinal hemorrhage, obstruction, or perforation","Pheochromocytoma"]
| Precautions | ["Serotonin syndrome risk when used with other serotonergic drugs","QT interval prolongation, especially with electrolyte abnormalities or concurrent QT-prolonging drugs","Hypersensitivity reactions including anaphylaxis","Masking of progressive ileus and/or gastric distention in postoperative patients"] |
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| Maternal: CBC with differential, hepatic function, renal function tests, and urinalysis. Fetal: Serial ultrasound for growth and amniotic fluid volume; nonstress test or biophysical profile as clinically indicated. |
| Fertility Effects | Decreased spermatogenesis in males and menstrual irregularities in females reported; reversible upon discontinuation. No established effect on conception. |