CLOPRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CLOPRA (CLOPRA).
Clopra (metoclopramide) is a dopamine D2 receptor antagonist and a 5-HT4 receptor agonist, enhancing gastrointestinal motility and having antiemetic effects via central and peripheral actions.
| Metabolism | Metabolized by CYP2D6, CYP1A2, and CYP2C9; undergoes conjugation (glucuronidation, sulfation). |
| Excretion | Renal (50-70% as unchanged drug and metabolites); fecal (20-30%); biliary (minor ~5%) |
| Half-life | Terminal elimination half-life 6-8 hours (prolonged in renal impairment; up to 20 hours in severe CKD) |
| Protein binding | 80-90% (primarily to albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | 2.5-4.0 L/kg (suggests extensive tissue distribution) |
| Bioavailability | Oral: 50-70% (first-pass metabolism; reduced by food) |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-15 minutes |
| Duration of Action | 4-6 hours (dose-dependent; extended-release formulations 12 hours) |
Clopra (metoclopramide) 10 mg orally or intramuscularly 30 minutes before meals and at bedtime; maximum 30 mg/day. For intravenous administration, give 10 mg over 1-2 minutes.
| Dosage form | TABLET |
| Renal impairment | GFR 10-40 mL/min: reduce dose to 5 mg per dose. GFR <10 mL/min: reduce dose to 2.5 mg per dose or administer every 12 hours. |
| Liver impairment | Child-Pugh class A: no adjustment. Class B: reduce dose by 50%. Class C: avoid use or use with caution; no specific dose established. |
| Pediatric use | Children 2-18 years: 0.1 mg/kg per dose orally or intravenously, up to 10 mg per dose, 3-4 times daily. Maximum 0.5 mg/kg/day. |
| Geriatric use | Elderly patients (≥65 years): initiate at 5 mg orally 3 times daily; maximum 15 mg/day due to increased risk of tardive dyskinesia and extrapyramidal symptoms. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CLOPRA (CLOPRA).
| Breastfeeding | Cloprostenol is excreted in human milk; M/P ratio not determined. Due to potential for serious adverse reactions in nursing infants, contraindicated during breastfeeding. |
| Teratogenic Risk | Pregnancy Category C. First trimester: limited human data; animal studies show embryocidal effects but no consistent teratogenicity. Second and third trimesters: risk of premature closure of ductus arteriosus, oligohydramnios, and pulmonary hypertension in the neonate. Avoid in late pregnancy. |
| Fetal Monitoring |
■ FDA Black Box Warning
May cause tardive dyskinesia, often irreversible. Risk increases with duration of treatment and total cumulative dose. Discontinue if signs/symptoms appear. Use >12 weeks should be avoided except in patients with a severe, documented condition where benefit outweighs risk.
| Serious Effects |
Hypersensitivity, gastrointestinal hemorrhage/obstruction/perforation, pheochromocytoma, concurrent MAOIs, history of tardive dyskinesia, Parkinson's disease (relative), epilepsy (may lower seizure threshold).
| Precautions | Tardive dyskinesia, extrapyramidal symptoms, neuroleptic malignant syndrome, QT prolongation, electrolyte disturbances, depression and suicidality, Parkinsonism, hypotension, hypertensive crisis (with MAOIs), porphyria, use in epilepsy. |
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| Monitor uterine tone, fetal heart rate, and progression of cervical effacement/dilation during use in pregnancy. Assess for signs of uterine hyperstimulation or rupture. In high-dose scenarios, monitor maternal blood pressure and respiratory status. |
| Fertility Effects | Cloprostenol is a prostaglandin F2α analog used for luteolysis and induction of labor. In females, it may impair fertility by causing luteolysis and disruption of early pregnancy. No known effects on male fertility. |