Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 2.5mg/mL (2-mL or 4-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 (≥30 mL/min/1.73 m2): No dosage adjustment necessary
- Severe (<30 mL/min/1.73 m2): Avoid use; known to be substantially excreted by kidneys and patients with severe renal impairment may have increased systemic exposure and an increased risk of adverse reactions
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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
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)
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.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])
Administration
IV Compatibilities
Sterile water for injection
Dextrose 5% (D5W)
0.9% NaCl
Lactated Ringer (LR)
IV Administration
Dilution not required
Infuse over 1-2 min
May flush IV line before or after administration with sterile water for injection, D5W, LR, 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
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