amisulpride (Rx)

Brand and Other Names:Barhemsys
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 2.5mg/mL (2-mL, single-dose vial)

Postoperative Nausea & Vomiting

Prevention

  • Indicated for prevention of postoperative nausea and vomiting (PONV), either alone or in combination with an antiemetic of a different class
  • 5 mg as a single IV dose at time of anesthesia induction

Treatment

  • Indicated for treatment of PONV in adults who have received antiemetic prophylaxis with an agent of a different class or have not received prophylaxis
  • 10 mg as a single IV dose in the event of nausea and/or vomiting postoperatively

Dosage Modifications

Renal impairment

  • Mild-to-moderate (eGFR ≥30 mL/min/1.73 m2): No dosage adjustment necessary
  • Severe: Avoid use

Safety and efficacy not established

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Interactions

Interaction Checker

and amisulpride

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (1)

              • artemether

                artemether and amisulpride both increase QTc interval. Avoid or Use Alternate Drug.

              Monitor Closely (1)

              • albuterol

                albuterol and amisulpride both increase QTc interval. Use Caution/Monitor.

              Minor (0)

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                Adverse Effects

                1-10%

                Prevention of PONV

                • Increased blood prolactin (5%)
                • Chills (4%)
                • Hypokalemia (4%)
                • Procedural hypotension (3%)
                • Abdominal distension (2%)

                Treatment of PONV

                • Infusion site pain (6%)

                Postmarketing Reports

                Blood and lymphatic system disorders: Agranulocytosis

                Cardiac disorders: Bradycardia, torsades de pointes, ventricular tachycardia, prolonged QT by ECG

                General disorders: Neuroleptic malignant syndrome

                Immune system disorders: Angioedema, hypersensitivity, urticaria

                Hepatic disorders: Increased hepatic enzymes

                Nervous system disorders: Agitation, anxiety, dystonia, extrapyramidal disorder, seizure

                Psychiatric disorders: Confusional state, insomnia, somnolence

                Vascular disorders: Hypotension

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                Warnings

                Contraindications

                Hypersensitivity

                Cautions

                QT prolongation

                • May causes dose- and concentration-dependent prolongation of the QT interval
                • Avoid in patients with congenital long QT syndrome and in patients taking droperidol
                • ECG monitoring recommended with preexisting arrhythmias/cardiac conduction disorders, electrolyte abnormalities (eg, hypokalemia, hypomagnesemia), congestive heart failure, and in patients taking other drugs (eg, ondansetron) or with other medical conditions known to prolong the QT interval

                Drug interactions overview

                • Amisulpride inhibits MATE1 and MATE2-K transporters
                • Amisulpride is a substrate for P-gp, BCRP, OCT1, MATE1, and MATE2-K
                • Dopamine agonists
                  • Reciprocal antagonism of effects occurs between dopamine agonists (eg, levodopa)
                  • Avoid use
                • Drugs prolonging the QT interval
                  • Amisulpride causes dose- and concentration-dependent QT prolongation
                  • Avoid use with droperidol
                  • ECG monitoring recommended if coadministered with other drugs known to prolong QT interval (eg, ondansetron)
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                Pregnancy & Lactation

                Pregnancy

                Insufficient data available regarding use in pregnant women to establish a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

                Infertility

                • In animal fertility studies, administration of repeated doses of amisulpride over a 10­-day period to female rats resulted in infertility that was reversible

                Lactation

                Based on case reports in published literature, amisulpride is present in human milk at concentrations that are 11- to 20-fold higher than human plasma in patients taking multiple oral doses of amisulpride (200-400 mg/day)

                There are no reports of adverse effects on breastfed children and no information on effects of amisulpride on milk production

                May consider interrupting breastfeeding and pumping and discarding breast milk for 48 hr after administration to minimize drug exposure to a breastfed infant

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Selective dopamine-2 (D2) and dopamine-3 (D3) receptor antagonist

                D2 receptors are located in the chemoreceptor trigger zone (CTZ) and respond to the dopamine released from the nerve endings

                Activation of CTZ relays stimuli to the vomiting center, which is involved in emesis

                Absorption

                Peak plasma concentration

                • Healthy subjects: 200 ng/mL (5 mg); 451 ng/mL (10 mg)
                • Patients: 58-64 ng/mL (5 mg); 446 ng/mL (10 mg)

                AUC

                • Healthy subjects: 154 ng⋅hr/mL (5 mg); 136 ng⋅hr/mL (10 mg)
                • Patients: 204-260 ng⋅hr/mL (5 mg); 401 ng⋅hr/mL (10 mg)

                Distribution

                Vd: 127-144 L (surgical patients); 171 L (healthy subjects)

                Protein bound: 25-30%

                Metabolism

                No metabolites were detectable in plasma while 4 metabolites were identified in urine and feces

                Each metabolite accounts for <7% of the dose

                In vitro amisulpride is not metabolized by major cytochrome P450 enzymes

                Elimination

                Half-life: ~ 4-5 hr

                Clearance: 20.6 hr (surgical patients); 24.1 L/hr (healthy subjects)

                Renal clearance: 20.5 L/hr (healthy subjects)

                Excretion: Urine (74% [58% unchanged]), feces (23% [20% unchanged])

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                Administration

                IV Compatibilities

                Sterile water for injection

                Dextrose 5% (D5W)

                0.9% NaCl

                IV Administration

                Dilution not required

                Infuse over 1-2 min

                May flush IV line before or after administration with sterile water for injection, D5W, or 0.9% NaCl

                Storage

                Protect from light

                Unopened vials: Store at 20-25ºC (68-77ºF)

                Open vials: Administer within 12 hr of removal of the vial from the protective carton

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.