dolasetron mesylate

dolasetron mesylate

Anzemet

Pharmacologic class: Selective serotonin subtype 3 (5-HT3) receptor antagonist

Therapeutic class: Antiemetic

Pregnancy risk category B

Action

Blocks serotonin activation at receptor sites in vagal nerve terminals and in chemoreceptor trigger zone in CNS, decreasing the vomiting reflex

Availability

Injection: 12.5 mg/0.625-ml ampules, 20 mg/ml in 5-ml vials

Tablets: 50 mg, 100 mg

Indications and dosages

Chemotherapy-induced nausea and vomiting

Adults: 100 mg P.O. 1 hour before chemotherapy or 1.8 mg/kg I.V. 30 minutes before chemotherapy

Children ages 2 to 16: 1.8 mg/kg P.O. within 1 hour before chemotherapy or 1.8 mg/kg I.V. (not to exceed 100 mg) 30 minutes before chemotherapy

Prevention or treatment of postoperative nausea and vomiting

Adults: 100 mg P.O. within 2 hours before surgery or 12.5 mg I.V. 15 minutes before cessation of anesthesia (for prevention) or as soon as nausea or vomiting begins (for treatment)

Children ages 2 to 16: 1.2 mg/kg P.O. (up to 100 mg/dose) within 2 hours before surgery or 0.35 mg/kg I.V. (up to 12.5 mg) 15 minutes before cessation of anesthesia (for prevention) or as soon as nausea or vomiting begins (for treatment)

Contraindications

• Hypersensitivity to drug
• Arrhythmias

Precautions

Use cautiously in:
• risk factors for prolonged cardiac conduction intervals
• pregnant or breastfeeding patients (safety not established).

Administration

• Give oral dose at least 1 hour before chemotherapy for best results.
• To prevent postoperative nausea, give oral dose within 2 hours before surgery.
• If patient has difficulty swallowing tablet, injection solution may be mixed with apple or apple-grape juice and given orally.
• For I.V. use, give 100 mg single dose undiluted over 30 seconds. For I.V. infusion, dilute in normal saline solution, dextrose 5% in water, or lactated Ringer's solution to 50 ml, and give single dose over at least 15 minutes. Don't mix with other drugs.
• Flush I.V. line before and after infusion.

Adverse reactions

CNS: headache (increased in cancer patients), dizziness, fatigue, syncope

CV: bradycardia, tachycardia, ECG changes, hypertension, hypotension

GI: diarrhea, constipation, dyspepsia, abdominal pain

GU: urinary retention, oliguria

Skin: pruritus, rash

Other: chills, fever, decreased appetite

Interactions

Drug-drug.Antiarrhythmics, anthracycline (high cumulative doses), diuretics, drugs that prolong QTc interval: increased risk of conduction abnormalities

Drugs that affect hepatic microsomal enzymes: altered dolasetron blood level

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase: increased levels

Patient monitoring

• Monitor closely for excessive diuresis.

Watch for ECG changes, including prolonged PR interval and widened QRS complex, especially in patients receiving antiarrhythmics concurrently.

Patient teaching

• Instruct patient to take drug 1 to 2 hours before chemotherapy.
• Inform patient that drug commonly causes headache.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

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References in periodicals archive ?
Pooled analysis of three large clinical trials to determine the optimal dose of dolasetron mesylate needed to prevent postoperative nausea and vomiting.
Prophylactic oral dolasetron mesylate reduces nausea and vomiting after abdominal hysterectomy.
The additions are "other class Ia and III antiarrhythmics," mesoridazine, chlorpromazine, droperidol, gatifloxacin, halofantrine, mefloquine, pentamidine, arsenic trioxide, levomethadyl acetate, dolasetron mesylate, probucol, and tacrolimus.