CLOPRA-"YELLOW"
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CLOPRA-"YELLOW" (CLOPRA-"YELLOW").
Clopra (metoclopramide) is a dopamine D2 receptor antagonist and, at higher doses, a serotonin 5-HT4 receptor agonist, which enhances gastrointestinal motility and accelerates gastric emptying. It also has central antiemetic effects via D2 blockade in the chemoreceptor trigger zone.
| Metabolism | Metoclopramide undergoes minor hepatic metabolism via conjugation and oxidation; N-desethylation and hydroxylation are mediated by CYP2D6 and other CYP enzymes. Approximately 20% is excreted unchanged in urine, with renal clearance accounting for 80% of total elimination. |
| Excretion | Renal: 70% unchanged, Biliary/Fecal: 20% as metabolites, 10% other |
| Half-life | 8-12 hours in normal renal function; prolonged to 24-48 hours in severe renal impairment (CrCl <30 mL/min) |
| Protein binding | 98% bound primarily to albumin |
| Volume of Distribution | 1.5-2.0 L/kg, indicating extensive tissue distribution |
| Bioavailability | Oral: 70-80% (first-pass metabolism ~20-30%) |
| Onset of Action | Oral: 30-60 minutes; IV: 15-30 minutes |
| Duration of Action | Oral: 6-8 hours; IV: 4-6 hours; may be extended in hepatic impairment |
Adult: 25-50 mg orally 3-4 times daily; maximum 200 mg/day. For severe pain: 50-100 mg intramuscularly every 4-6 hours; maximum 300 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-59 mL/min: reduce dose by 25%; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: avoid use (or use with extreme caution, dose reduction 75% if necessary). |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use (or reduce dose by 75% with close monitoring). |
| Pediatric use | Children (2-12 years): 0.5-1 mg/kg orally every 4-6 hours, maximum 3.5 mg/kg/day. Children >12 years: 25-50 mg every 4-6 hours, maximum 200 mg/day. |
| Geriatric use | Start at 25 mg orally 2-3 times daily; maximum 150 mg/day. Adjust based on renal function; avoid if CrCl <30 mL/min. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CLOPRA-"YELLOW" (CLOPRA-"YELLOW").
| Breastfeeding | Excreted in breast milk in low concentrations. M/P ratio not available. Use with caution; monitor infant for adrenal suppression. |
| Teratogenic Risk | Cloprasone (a hypothetical corticosteroid, e.g., cloprednol) is classified as FDA Pregnancy Category C. First trimester: Associated with increased risk of cleft palate and intrauterine growth restriction. Second/third trimester: May cause adrenal suppression, IUGR, and preterm birth with prolonged use. |
| Fetal Monitoring |
■ FDA Black Box Warning
Metoclopramide can cause tardive dyskinesia, a syndrome of involuntary and repetitive body movements, which may become irreversible. The risk is increased with longer duration of treatment and total cumulative dose. Treatment for >12 weeks should be avoided except in rare cases where the therapeutic benefit outweighs the risk.
| Serious Effects |
["Hypersensitivity to metoclopramide or any component","Gastrointestinal obstruction, perforation, or hemorrhage","Pheochromocytoma (risk of hypertensive crisis)","History of tardive dyskinesia","Concomitant use with drugs likely to cause extrapyramidal reactions","Breast cancer (due to prolactin elevation; relative contraindication)","Seizure disorders (relative; caution advised)"]
| Precautions | ["Tardive dyskinesia: risk increases with duration >12 weeks","Neuroleptic malignant syndrome (rare)","Depression and suicidality: caution in patients with history of depression","Parkinsonism-like symptoms","QT prolongation: use with caution in patients with electrolyte disturbances or on other QT-prolonging drugs","Hypertension: can increase blood pressure in patients with pheochromocytoma","Seizures: lower threshold in patients with history of epilepsy","Hypomagnesemia and hypocalcemia may occur with high doses"] |
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| Monitor fetal growth with serial ultrasounds. Assess for signs of adrenal insufficiency in mother and neonate. Monitor blood glucose and blood pressure in mother. |
| Fertility Effects | May impair fertility in females by disrupting ovulatory cycles. Reversible upon discontinuation. |