REGLAN ODT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REGLAN ODT (REGLAN ODT).
Metoclopramide, the active ingredient, is a dopamine D2 receptor antagonist and also sensitizes tissues to acetylcholine by facilitating cholinergic transmission in the myenteric plexus. It enhances upper gastrointestinal motility without stimulating gastric secretions.
| Metabolism | Primarily metabolized by CYP2D6, with minor contributions from CYP1A2, CYP3A4, and CYP2C19. Undergoes sulfation and glucuronidation. |
| Excretion | Renal (85% as unchanged drug and conjugates, 5% as unchanged metoclopramide), fecal (10%). |
| Half-life | Terminal elimination half-life is 5-6 hours in patients with normal renal function. Prolonged in renal impairment (up to 15 hours in severe cases). |
| Protein binding | 30% primarily to albumin. |
| Volume of Distribution | 3.5 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral (tablet or ODT): 80% (due to first-pass metabolism); intramuscular: 74-96%; intravenous: 100%. |
| Onset of Action | Oral (tablet or ODT): 30-60 minutes; intramuscular: 10-15 minutes; intravenous: 1-3 minutes. |
| Duration of Action | Oral: 1-2 hours; parenteral: 1-2 hours. Clinical effect may persist up to 2 hours for gastrointestinal effects. |
10 mg orally 4 times daily (30 minutes before meals and at bedtime)
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | CrCl 40-60 mL/min: 5 mg orally 4 times daily; CrCl <40 mL/min: 5 mg orally 2 times daily; ESRD: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: not recommended |
| Pediatric use | 0.1 mg/kg/dose orally up to a maximum of 0.5 mg/kg/day; administer 30 minutes before meals and at bedtime |
| Geriatric use | Initiate at 5 mg orally 2-3 times daily; titrate cautiously due to increased risk of tardive dyskinesia |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REGLAN ODT (REGLAN ODT).
| Breastfeeding | Metoclopramide is excreted into breast milk with a milk-to-plasma (M/P) ratio of approximately 1.0. The estimated infant dose is about 1-6% of the maternal dose, which is generally considered low. However, metoclopramide can increase prolactin levels and may cause mild adverse effects in breastfed infants (e.g., drowsiness, gastrointestinal effects). Monitoring for extrapyramidal symptoms in the infant is recommended, especially with prolonged maternal use. |
| Teratogenic Risk | Metoclopramide (REGLAN ODT) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies exist in first trimester. Use in second and third trimesters is generally considered low risk, though high doses near term may cause neonatal extrapyramidal symptoms (dystonia, tardive dyskinesia) due to placental transfer. Limited data suggest no significant increase in major congenital malformations with first-trimester exposure. |
■ FDA Black Box Warning
Tardive dyskinesia (TD) may develop with prolonged or high-dose treatment, especially in elderly women. Risk increases with cumulative duration of therapy. REGLAN ODT should not be used for longer than 12 weeks except in rare cases where benefit outweighs risk.
| Serious Effects |
["History of tardive dyskinesia","Parkinson's disease (relative contraindication due to dopamine antagonism)","Pheochromocytoma (risk of hypertensive crisis)","Breast cancer (metoclopramide can increase prolactin levels)","Concomitant use of monoamine oxidase inhibitors (MAOIs)","Gastrointestinal hemorrhage, obstruction, or perforation","Epilepsy (may increase seizure frequency)"]
| Precautions | ["Tardive dyskinesia: risk increases with duration and dose; discontinue if signs/symptoms appear","Neuroleptic malignant syndrome (NMS): potentially fatal; discontinue immediately","Parkinsonism-like symptoms: tremor, rigidity, bradykinesia","Depression: may be severe; monitor high-risk patients","QT prolongation: caution in patients with electrolyte disturbances or concomitant QT-prolonging drugs","Hypotension and hypertensive crisis","Porphyria: avoid in patients with porphyria"] |
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| Fetal Monitoring | Monitor maternal blood pressure and heart rate, as metoclopramide can cause hypotension or hypertension. Assess for development of tardive dyskinesia, dystonia, and other extrapyramidal symptoms, especially with long-term use. In pregnancy, monitor for signs of preeclampsia if used for gastroparesis. Fetal monitoring includes ultrasound for growth and amniotic fluid volume if used chronically. Neonatal monitoring for extrapyramidal symptoms after delivery if maternal use near term. |
| Fertility Effects | Metoclopramide elevates prolactin levels via dopamine D2 receptor blockade, which can suppress gonadotropin-releasing hormone (GnRH) and lead to menstrual irregularities, anovulation, and decreased fertility in women. Reversible upon discontinuation. In men, hyperprolactinemia may cause erectile dysfunction and reduced libido. No evidence of permanent impairment. |