GIMOTI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GIMOTI (GIMOTI).
GIMOTI (metoclopramide) is a dopamine D2 receptor antagonist and also sensitizes tissues to acetylcholine, enhancing gastric motility and accelerating gastric emptying.
| Metabolism | Primarily metabolized by CYP2D6; minor metabolism by CYP1A2 and CYP3A4; undergoes sulfation and glucuronidation; renal excretion of unchanged drug and metabolites. |
| Excretion | Primarily renal (60-70% unchanged); biliary/fecal 20-30% as metabolites. |
| Half-life | Terminal elimination half-life of 4-6 hours; prolonged in renal impairment (up to 10-14 hours). |
| Protein binding | 30-40% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd approximately 2.5-4.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 50-70% due to first-pass metabolism; intravenous: 100%. |
| Onset of Action | Intravenous: within 5 minutes; oral: 30-60 minutes. |
| Duration of Action | Duration of prokinetic effect 4-6 hours; may be prolonged in hepatic or renal impairment. |
10 mg orally three times daily.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for GFR ≥60 mL/min. For GFR 30-59 mL/min: 5 mg three times daily. For GFR 15-29 mL/min: 5 mg once daily. For GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 5 mg three times daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved in pediatric patients; safety and efficacy not established. |
| Geriatric use | Starting dose of 5 mg three times daily, with cautious titration, due to increased risk of QT prolongation and adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GIMOTI (GIMOTI).
| Breastfeeding | Metoclopramide is excreted into human breast milk. The milk-to-plasma ratio ranges from 1.1 to 2.6. Based on usual maternal doses, the estimated daily infant dose is about 0.1–0.2 mg/kg/day, which is less than the therapeutic dose for infants. However, potential adverse effects (e.g., dystonic reactions) warrant caution. Use only if clearly indicated and monitor infant for extrapyramidal symptoms. |
| Teratogenic Risk | GIMOTI (metoclopramide) is FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women. Available data do not suggest an increased risk of major birth defects or miscarriage with use during pregnancy, including first trimester. However, use should be limited to situations where clearly needed, especially in the first trimester. |
■ FDA Black Box Warning
Tardive dyskinesia (TD) may develop with prolonged or high-dose use, especially in elderly patients; risk increases with cumulative dose and treatment duration. Therapy should be discontinued if signs/symptoms of TD appear.
| Serious Effects |
["Hypersensitivity to metoclopramide","History of tardive dyskinesia","Parkinson's disease","Pheochromocytoma","Bowel obstruction, perforation, or hemorrhage","Concurrent use with drugs causing extrapyramidal reactions","Epilepsy"]
| Precautions | ["Tardive dyskinesia","Neuroleptic malignant syndrome (rare)","Parkinsonism and other extrapyramidal symptoms","Depression and suicidal ideation","Hypertension and fluid retention (especially with IV use)","QT prolongation (risk increases with electrolyte abnormalities, bradycardia, or concomitant QT-prolonging drugs)"] |
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| Fetal Monitoring | Monitor for extrapyramidal symptoms (EPS), tardive dyskinesia, neuroleptic malignant syndrome (NMS), depression, hypertension, and cardiac arrhythmias. In pregnancy, monitor maternal blood pressure and fetal heart rate if used near term due to potential oxytocin-like effects. Long-term use requires monitoring for tardive dyskinesia. |
| Fertility Effects | Metoclopramide may elevate prolactin levels, leading to galactorrhea, amenorrhea, and potential reversible infertility. In women, it can disrupt ovulatory cycles. In men, hyperprolactinemia may cause libido changes and erectile dysfunction. These effects are dose-dependent and reversible upon discontinuation. |