EMETE-CON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EMETE-CON (EMETE-CON).
Antiemetic; dopaminergic antagonist at D2 receptors in the chemoreceptor trigger zone; also exhibits anticholinergic and antihistaminic properties.
| Metabolism | Hepatic via CYP2D6; excreted in urine and feces. |
| Excretion | Primarily hepatic metabolism (CYP2D6, CYP3A4) with <5% excreted unchanged in urine. Biliary/fecal excretion accounts for approximately 60-70% of metabolites, with renal elimination of metabolites constituting 25-35%. |
| Half-life | Terminal elimination half-life is 8-12 hours in adults with normal renal and hepatic function; may extend to 15-20 hours in elderly or patients with hepatic impairment. |
| Protein binding | Approximately 70-80% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 2.5-3.5 L/kg, indicating extensive tissue distribution beyond plasma volume. |
| Bioavailability | Oral bioavailability is approximately 60-70% due to first-pass metabolism; intramuscular bioavailability is near 100%. |
| Onset of Action | Intravenous: 1-3 minutes; Intramuscular: 10-15 minutes; Oral: 30-60 minutes. |
| Duration of Action | Duration of antiemetic effect is 4-6 hours following IV/IM administration, and 6-8 hours after oral dosing. Prophylactic effect may persist up to 12 hours in some patients. |
12.5 mg intravenously over 30 seconds as a single dose; may repeat once after 1 hour if necessary.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, use with caution; dose reduction to 6.25 mg recommended. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose to 6.25 mg. Child-Pugh Class C: Avoid use or reduce to 6.25 mg with close monitoring. |
| Pediatric use | Children ≥2 years: 0.125 mg/kg (max 12.5 mg) intravenously once; may repeat once after 1 hour. Not recommended for infants <2 years. |
| Geriatric use | No specific dose adjustment required, but consider starting at lower dose (6.25 mg) due to potential increased sensitivity to anticholinergic effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EMETE-CON (EMETE-CON).
| Breastfeeding | Excretion in human milk unknown; M/P ratio not determined. Due to potential for serious adverse reactions in nursing infants, discontinue breastfeeding or avoid use. |
| Teratogenic Risk | EMETE-CON (benzquinamide) is not recommended during pregnancy. No adequate human data; animal studies suggest potential risk. First trimester: avoid due to unknown teratogenic potential. Second/third trimesters: use only if maternal benefit outweighs fetal risk; may cause neonatal respiratory depression if used near term. |
■ FDA Black Box Warning
Not applicable.
| Serious Effects |
Hypersensitivity to the drug; comatose or severely depressed states; concurrent use with adrenergic agents; suspected pheochromocytoma.
| Precautions | May cause extrapyramidal symptoms, particularly in children and elderly; avoid in patients with Parkinson's disease; may lower seizure threshold; caution in patients with glaucoma or prostatic hypertrophy. |
| Food/Dietary | No specific food interactions have been reported. However, avoid alcohol as it may exacerbate central nervous system depression and dizziness. |
| Clinical Pearls |
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| Fetal Monitoring |
| Fetal heart rate monitoring during labor; maternal blood pressure, heart rate, and respiratory status; observe neonate for signs of sedation or respiratory depression if used near term. |
| Fertility Effects | Animal studies suggest possible impairment of fertility at high doses; human data insufficient to assess effect on fertility. |
| EMETE-CON (benzquinamide) is a parenteral antiemetic with antihistaminic and anticholinergic properties. Onset of action is 15 minutes via IM. Avoid extravasation due to irritant properties. Caution in patients with severe cardiovascular disease, as it may cause transient hypertension and tachycardia. Observe for extrapyramidal symptoms, especially in elderly. |
| Patient Advice | This medication is given by injection to prevent or treat nausea and vomiting. · Report any signs of allergic reaction, such as rash, itching, or difficulty breathing. · Avoid driving or operating heavy machinery until you know how this medication affects you as it may cause drowsiness or dizziness. · Inform your healthcare provider if you have heart problems, high blood pressure, or a history of seizures. · Do not consume alcohol while taking this medication as it can increase side effects. |