Version May 2024
Postoperative nausea and vomiting: IV
Prevention: 5 mg as a single dose, at the time of anesthesia induction.
Treatment: 10 mg as a single dose after surgery (in patients who did not receive prophylaxis or received an agent of a different class).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
eGFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.
eGFR <30 mL/minute/1.73 m2 (not requiring dialysis): No dosage adjustment necessary.
Hemodialysis: There are no dosage adjustments provided in the manufacturer’s labeling.
There are no dosage adjustments provided in the manufacturer’s labeling.
Refer to adult dosing.
Amisulpride may cause dose- or concentration-dependent prolonged QT interval on ECG, predominately at supratherapeutic doses, as well as occasional treatment-emergent T-wave changes. However, in 2 randomized, crossover studies in healthy adult subjects using therapeutic doses (5 mg or 10 mg) of amisulpride intravenously, no clinically significant effects on the QT interval were observed (Ref)
Mechanism: Dose-related; blockade of the cardiac human ether-à-go-go-related gene (hERG) blockade channel is associated with QT prolongation; amisulpride has been shown to inhibit hERG current (Ref).
Onset: Rapid; within 5 minutes (Ref)
Risk factors:
Drug-induced QTc prolongation/torsades de pointes (TdP) (in general):
• Females (Ref)
• Age >65 years (Ref)
• Structural heart disease (eg, history of myocardial infarction or heart failure with a reduced ejection fraction) (Ref)
• History of drug-induced TdP (Ref)
• Genetic defects of cardiac ion channels (Ref)
• Congenital long QT syndrome (Ref)
• Baseline QTc interval prolongation (eg, >500 msec) or lengthening of the QTc by ≥60 msec (Ref)
• Electrolyte disturbances (eg, hypokalemia, hypocalcemia, hypomagnesemia) (Ref)
• Bradycardia (Ref)
• Hepatic impairment (Ref)
• Kidney impairment (Ref)
• Coadministration of multiple medications (≥2) that prolong the QT interval or increase drug interactions that increase serum drug concentrations of QTc prolonging medications (Ref)
• Substance use (Ref)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Cardiovascular: Procedural hypotension (3%)
Endocrine & metabolic: Hypokalemia (4%), increased serum prolactin (5%)
Gastrointestinal: Abdominal distention (2%)
Local: Infusion-site pain (6%)
Nervous system: Chills (4%)
Frequency not defined: Cardiovascular: Prolonged QT interval on ECG
Hypersensitivity to amisulpride or any component of the formulation.
Disease-related concerns:
• Renal impairment: Use caution in patients with mild or moderate renal impairment; avoid use in patients with severe renal impairment.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous [preservative free]:
Barhemsys: 5 mg/2 mL (2 mL); 10 mg/4 mL (4 mL)
No
Solution (Barhemsys Intravenous)
5 mg/2 mL (per mL): $27.00
10 mg/4 mL (per mL): $27.00
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
IV: Infuse over 1 to 2 minutes; flush line before and after administration with a compatible solution (eg, D5W, NS, LR, SWFI).
Postoperative nausea and vomiting: Prevention of postoperative nausea and vomiting (PONV), either alone or in combination with an antiemetic of a different class, in adults; treatment of PONV in adults who have received antiemetic prophylaxis with an agent of a different class or have not received prophylaxis.
Amisulpride may be confused with amitriptyline.
Substrate of BCRP/ABCG2, OCT1, OCT2, P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Anti-Parkinson Agents (Dopamine Agonist): Amisulpride (Injection) may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Risk X: Avoid combination
DroPERidol: Amisulpride (Injection) may enhance the QTc-prolonging effect of DroPERidol. Risk X: Avoid combination
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Levosulpiride: Benzamide Derivatives may enhance the adverse/toxic effect of Levosulpiride. Risk C: Monitor therapy
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Amisulpride crosses the placenta (Nandakumaran 1984).
Information related to the use of amisulpride in pregnancy is limited (Damkier 2018).
Amisulpride is present in breast milk.
Information related to amisulpride secretion into breast milk is available from case reports following oral dosing. The estimated exposure to the breastfeeding infant was 5% to 11% of the weight-adjusted maternal dose. Maternal doses ranged from 200 to 400 mg daily (Ilett 2010; O'Halloran 2016; Teoh 2011). Amisulpride was also detected in the serum of one of the breastfeeding infants (Ilett 2010).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Lactating women may consider expressing and discarding breast milk for a period of 48 hours after receiving amisulpride injection to minimize exposure to the breastfed infant.
ECG (preexisting arrhythmias or cardiac conduction disorders, electrolyte abnormalities, congestive heart failure; taking other medications known to prolong QTc interval) (monitor as appropriate).
Amisulpride is an atypical antipsychotic with selective binding to D2 and D3 dopamine receptors. Antagonism of D2 receptors in the chemoreceptor trigger zone relays inhibitory stimuli to the vomiting center. Antagonism of D3 receptors in the area postrema also inhibits emesis. Has minimal affinity for 5-HT2B and 5-HT7 receptors, and no affinity for any other receptor types.
Distribution: Vd: Healthy subjects: 171 L; surgical patients: 127 to 144 L.
Protein binding: Plasma: 25% to 30%.
Metabolism: Not metabolized via CYP pathway.
Half-life elimination: ~4 to 5 hours.
Time to peak: At end of infusion.
Excretion: Urine: 74% (58% as unchanged drug); feces: 23% (20% as unchanged drug).
Renal function: In patients with mild to moderate renal impairment (eGFR 30 to 89 mL/minute/1.73 m2) Cmax was not significantly different and AUC increased about 1.3-fold compared to healthy adults. In patients with severe renal impairment not requiring dialysis (eGFR <30 mL/minute/1.73 m2) Cmax was not significantly different and AUC increased about twice as high compared to healthy adults.
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