BARHEMSYS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BARHEMSYS (BARHEMSYS).
BARHEMSYS (amisulpride) is a selective dopamine D2/D3 receptor antagonist. It also has weak affinity for serotonin 5-HT2A and 5-HT2B receptors, with no significant activity at other dopamine or serotonin receptor subtypes. Its antiemetic effect is primarily mediated through blockade of D2 receptors in the chemoreceptor trigger zone (CTZ).
| Metabolism | Amisulpride undergoes minimal hepatic metabolism. It is primarily excreted unchanged in urine (approximately 70-80% as parent drug) and feces. Metabolism occurs via cytochrome P450 enzymes, but no specific isozymes are predominantly involved. It is a substrate for P-glycoprotein. |
| Excretion | Renal excretion accounts for approximately 50% of the dose as unchanged drug; fecal elimination (including biliary) accounts for approximately 30-40%. |
| Half-life | Terminal elimination half-life is approximately 24 hours, supporting once-daily dosing in most patients. |
| Protein binding | Approximately 85% bound to plasma proteins, primarily to albumin. |
| Volume of Distribution | Approximately 1.5 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is approximately 30-40% due to first-pass metabolism; intravenous bioavailability is 100%. |
| Onset of Action | Intravenous: 15-30 minutes; oral: 30-60 minutes. |
| Duration of Action | Anti-emetic effect lasts approximately 24 hours following a single dose, allowing once-daily administration. |
BARHEMSYS (amisulpride) 10 mg intravenously over 2 minutes, once daily for prevention of postoperative nausea and vomiting.
| Dosage form | SOLUTION |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. For severe renal impairment (eGFR <30 mL/min/1.73 m²), reduce dose to 5 mg intravenously once daily. |
| Liver impairment | No dosage adjustment required for mild hepatic impairment (Child-Pugh A). For moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment, reduce dose to 5 mg intravenously once daily. |
| Pediatric use | Safety and efficacy in pediatric patients (<18 years) have not been established. No recommended dosing. |
| Geriatric use | No specific dose adjustment required based on age alone. However, consider potential increased sensitivity and monitor for adverse effects such as QT prolongation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BARHEMSYS (BARHEMSYS).
| Breastfeeding | Contraindicated in breastfeeding. Amisulpride is excreted in human milk; milk-to-plasma ratio is 0.9. Potential for serious adverse effects in nursing infants. |
| Teratogenic Risk | BARHEMSYS (amisulpride) is contraindicated in pregnancy due to teratogenicity observed in animal studies. First trimester: high risk of congenital malformations; second/third trimester: risk of extrapyramidal symptoms and withdrawal in neonates. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to amisulpride or any component of the formulation.","Concurrent use with QT-prolonging drugs or in patients with known QT prolongation.","Concurrent dopamine receptor agonists (e.g., levodopa, pramipexole, ropinirole) due to antagonism of effects.","Bradycardia (< 50 bpm) or hypokalemia/hypomagnesemia not corrected."]
| Precautions | ["May prolong the QT interval; avoid use in patients with congenital long QT syndrome, history of clinically significant bradycardia, hypokalemia, hypomagnesemia, or concomitant use of QT-prolonging drugs.","May cause extrapyramidal symptoms (EPS), especially in elderly patients or at higher doses.","May cause tardive dyskinesia with chronic use; discontinue if signs appear.","May cause neuroleptic malignant syndrome (NMS); discontinue if suspected.","May cause hyperprolactinemia and related effects (e.g., galactorrhea, amenorrhea, gynecomastia).","May cause sedation, dizziness, or orthostatic hypotension; caution with driving or operating machinery.","Use with caution in patients with renal impairment (CrCl < 30 mL/min) or hepatic impairment.","Not recommended for use in pediatric patients."] |
| Food/Dietary |
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| Monitor for extrapyramidal symptoms, sedation, and QT prolongation in the mother; fetal ultrasound for anomalies if exposed; neonatal monitoring for withdrawal and EPS post-delivery. |
| Fertility Effects | May impair fertility in females and males (reversible). Animal studies show reduced fertility and mating indices. |
| No known food interactions. The drug is administered intravenously, so oral intake is not relevant. However, patients should follow standard preoperative fasting guidelines. |
| Clinical Pearls | BARHEMSYS (amisulpride) is an atypical antipsychotic used for postoperative nausea and vomiting (PONV). It has a unique mechanism as a selective dopamine D2/D3 antagonist with minimal extrapyramidal symptoms at low doses. Administer as a single 5 mg IV dose over 1-2 minutes at induction of anesthesia or when rescue treatment is needed. Avoid in patients with prolactin-dependent tumors or known hypersensitivity. Monitor for QT prolongation, especially with concomitant drugs that prolong QTc or in patients with electrolyte abnormalities. |
| Patient Advice | This medication is given intravenously to prevent or treat nausea and vomiting after surgery. · You may experience dizziness, drowsiness, or low blood pressure; avoid driving or operating machinery for 24 hours. · Report any symptoms of irregular heartbeat, fainting, or seizures immediately. · Inform your healthcare provider if you are pregnant, breastfeeding, or have a history of breast cancer or heart conditions. · Avoid alcohol and other central nervous system depressants for at least 24 hours after administration. |