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dolasetron (Rx)Brand and Other Names:Anzemet

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • 20mg/mL

tablet

  • 50mg
  • 100mg
more...

Cancer Chemotherapy Induced Nausea & Vomiting

Oral: 100 mg PO 1 hr before chemotherapy

Note: IV administration no longer indicated for CINV because of risk for QT prolongation

Post-op Nausea & Vomiting

Indicated for prevention and treatment of postoperative nausea and vomiting (PONV)

IV: 12.5 mg IV 15 minutes before cessation of anesthesia or as soon as N/V presents

Note: Oral tablet no longer indicated for PONV

Dosing considerations

Post-op nausea & vomiting

  • As with other antiemetics, routine prophylaxis is not recommended for patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively
  • In patients where nausea and/or vomiting must be avoided postoperatively, a 5-HT3 receptor antagonist is recommended even where the incidence of postoperative nausea and/or vomiting is low
  • When prophylaxis has failed, a repeat dose should not be initiated as rescue therapy

Dosage Forms & Strengths

injectable solution

  • 20mg/mL

tablet

  • 50mg
  • 100mg
more...

Cancer Chemotherapy Induced Nausea & Vomiting

<2 years: Safety and efficacy not established

2-16 years: 1.8 mg/kg PO 1 hr before chemotherapy; not to exceed 100 mg/dose 

IV may be administered PO in children aged 2-16 years: 1.8 mg/kg PO 1 hr before chemotherapy; not to exceed 100 mg/dose

Note: IV administration no longer indicated for CINV because of risk for QT prolongation

Postoperative Nausea & Vomiting

Indicated for prevention and treatment of post-op nausea and vomiting (PONV) in children ≥2 years

<2 years: Safety and efficacy not established

IV: 0.35 mg/kg 15 minutes before cessation of anesthesia or as soon as N/V develops; not to exceed 12.5 mg/dose 

IV may be administered PO in children aged 2-16 years: 1.2 mg/kg PO administered within 2 hr before surgery; not to exceed 100 mg/dose

Note: Oral tablet no longer indicated for PONV

Dosing considerations

Post-op nausea & vomiting

  • As with other antiemetics, routine prophylaxis is not recommended for patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively
  • In patients where nausea and/or vomiting must be avoided postoperatively, a 5-HT3 receptor antagonist is recommended even where the incidence of postoperative nausea and/or vomiting is low
  • When prophylaxis has failed, a repeat dose should not be initiated as rescue therapy

Administration

IV administered PO

  • Injectable solution may be given PO mixed in apple-grape or apple juice
  • Diluted product may be kept up to 2 hr at room temperature

Cancer chemotherapy induced nausea & vomiting

Oral: 100 mg PO 1 hr before chemotherapy

Note: IV administration no longer indicated for CINV because of risk for QT prolongation

Post-op nausea & vomiting

IV: 12.5 mg IV 15 minutes before cessation of anesthesia or as soon as N/V presents

Note: Oral tablet no longer indicated for PONV

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Interactions

Interaction Checker

dolasetron and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache

            Diarrhea

            1-10%

            Dizziness

            Drowsiness

            Fatigue

            Bradycardia

            HTN

            Hypotension

            Tachycardia

            Abdominal pain

            Dyspepsia

            Abnormal liver function

            Chills

            Fever

            Oliguria

            Urinary retention

            Pain

            Pruritus

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            Warnings

            Contraindications

            Hypersensitivity

            Coadministration with apomorphine; combination reported to cause profound hypotension and loss of consciousness

            IV administration for chemotherapy-induced nausea/vomiting (CINV) because of risk for QT, PR, and QRS prolongation

            Cautions

            Patients at risk for prolongation of cardiac conduction intervals, particularly long QTc interval, congenital long QT syndrome, uncorrected hypokalemia or hypomagnesemia, or receiving other QT-prolonging drugs

            Serotonin syndrome reported with 5-HT3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs including SSRIs, SNRIs, MAO inhibitors, lithium, tramadol, methylene blue IV, and mirtazapine

            Correct hypokalemia and hypomagnesemia before administration

            Use electrocardiogram (ECG) monitoring in patients with congestive heart failure, bradycardia, underlying heart disease, renal impairment, or who are elderly

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: not known whether distributed into breast milk, use caution

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Selective 5-HT3 receptor antagonist; dolasetron binds to 5-HT3 receptors located on vagal neurons in GI tract, blocking signal to vomiting center in the brain, thus preventing N/V

            Pharmacokinetics

            Half-life: parent compound <10 min, hydrodolasetron (active) 4-9 hr

            Peak plasma time: IV: 0.6 hr, PO: 1-1.5 hr

            Bioavailability: 59-80% (PO)

            Vd: 5.8-10 L/kg

            Protein binding: 69-77%

            Metabolism: dolasetron is metabolized to hydrodolasetron (active) by carbonyl reductase; hydrodolasetron is subsequently metabolized by CYP2D6 and CYP3A

            Metabolites: hydrodolasetron (active)

            Total body clearance: 9.4-13.4 mL/min/kg

            Renal clearance: 2.6-3.4 mg/kg

            Excretion: urine (53-61%); feces (25-33%)

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            Administration

            IV Preparation

            For infusion, dilute to 50 mL in NS/D5W/D5 in 0.5 NS/D5 in LR/LR/10% mannitol injection

            Store vial at room temp

            Dilution stable for 24 hr at room temp or 48 hr refrigerated

            IV Administration

            IVP 100 mg/30 sec OR

            Dilute as above and infuse over up to 15 min

            After dilution, use within 24 hr, or 48 hr if refrigerated

            Do not mix with other drugs

            Flush infusion line before and after administration

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            Images

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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.
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