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

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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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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            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.