Anzemet

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.

See 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.

dolasetron

(dol-a-se-tron) dolasetron,

Anzemet

(trade name)

Classification

Therapeutic: antiemetics
Pharmacologic: five ht3 antagonists
Pregnancy Category: B

Indications

Oral: Prevention of nausea and vomiting associated with emetogenic chemotherapy. Intravenous: Prevention and treatment of postoperative nausea/vomiting.

Action

Blocks the effects of serotonin at receptor sites (selective antagonist) located in vagal nerve terminals and in the chemoreceptor trigger zone in the CNS.

Therapeutic effects

Decreased incidence and severity of nausea/vomiting associated with emetogenic chemotherapy or surgery.

Pharmacokinetics

Absorption: Well absorbed but rapidly metabolized to hydrodolasetron, the active metabolite.Distribution: Unknown.Metabolism and Excretion: 61% of hydrodolasetron is excreted unchanged by the kidneys.Half-life: Hydrodolasetron—8.1 hr (shorter in children).

Time/action profile (antiemetic effect)

ROUTEONSETPEAKDURATION
POunknown 1–2 hrup to 24 hr
IVunknown15–30 minup to 24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity;Prevention of nausea and vomiting associated with emetogenic chemotherapy (for IV only) (may ↑ risk of QT interval prolongation);Congenital long QT syndrome;Complete heart block (unless pacemaker present).Use Cautiously in: Patients with risk factors for cardiac conduction abnormalities (underlying structural heart disease, sick sinus syndrome, atrial fibrillation and slow ventricular rate, myocardial ischemia, concurrent beta-blocker, verapamil, diltiazem, or antiarrhythmic therapy);Hypokalemia, hypomagenesemia, concurrent therapy with diuretics, or history of cumulative high-dose anthracycline therapy; Geriatric: ↑ risk for cardiac conduction abnormalities; Obstetric / Lactation: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • headache (increased in cancer patients)
  • dizziness
  • fatigue
  • syncope

Cardiovascular

  • cardiac arrest (life-threatening)
  • torsade de pointes (life-threatening)
  • ventricular arrhythmias (life-threatening)
  • bradycardia
  • heart block
  • hypertension
  • hypotension
  • PR interval prolongation
  • QRS interval prolongation
  • QT interval prolongation
  • tachycardia

Gastrointestinal

  • diarrhea
  • dyspepsia

Genitourinary

  • oliguria

Dermatologic

  • pruritus

Miscellaneous

  • chills
  • fever
  • pain

Interactions

Drug-Drug interaction

Concurrent diuretic or antiarrhythmic therapy or cumulative high-dose anthracycline therapy may ↑ risk of conduction abnormalities.Blood levels and effects of hydrodolasteron are ↑ by atenolol and cimetidine.Blood levels and effects of hydrodolasetron are ↓ by rifampin.↑ risk of QT interval prolongation with other agents causing QT interval prolongation.

Route/Dosage

Prevention of Chemotherapy-Induced Nausea/Vomiting Oral (Adults) 100 mg given within 1 hr before chemotherapy.Oral (Children 2–16 yr) 1.8 mg/kg given within 1 hr before chemotherapy (not to exceed 100 mg).Prevention/Treatment of Postoperative Nausea/Vomiting Intravenous (Adults) Prevention or treatment—12.5 mg given 15 min before cessation of anesthesia (prevention) or as soon as nausea or vomiting begins (treatment).Intravenous (Children 2–16 yr) Prevention or treatment—0.35 mg/kg (up to 12.5 mg) given 15 min before cessation of anesthesia (prevention) or as soon as nausea or vomiting begins (treatment).

Availability

Tablets: 50 mg, 100 mg Injection: 12.5 mg/0.625 mL (in single-use vials and Carpujects), 20 mg/mL

Nursing implications

Nursing assessment

  • Assess patient for nausea, vomiting, abdominal distention, and bowel sounds before and after administration.
  • Monitor vital signs after administration. IV administration may be followed by severe hypotension, bradycardia, and syncope.
  • Monitor ECG in patients with HF, bradycardia, underlying heart disease, renal impairment, and elderly patients.
  • Lab Test Considerations: Monitor serum potassium and magnesium prior to and periodically during therapy.

Potential Nursing Diagnoses

Imbalanced nutrition: less than body requirements (Indications)

Implementation

  • Do not confuse Anzemet with Avandamet.
  • Oral: Administer within 1 hr before chemotherapy.
    • Injectable dolasetron may be mixed in apple or apple-grape juice for oral dosing for pediatric patients. Recommended oral dose in patients 2 to 16 yr of age is 1.2 mg/kg (maximum 100 mg) given within 2 hr before surgery. The diluted product may be kept up to 2 hr at room temperature before use. May be stored at room temperature for 2 hr before use.
  • Intravenous Administration
  • Correct hypokalemia and hypomagnesemia before administering.
  • Intravenous: Administer 15 min before cessation of anesthesia, or postoperatively if nausea and vomiting occur shortly after surgery.
  • Diluent: May be administered undiluted.Concentration: 20 mg/mL.
  • Rate: Administer 100 mg over at least 30 sec.
  • Intermittent Infusion: Diluent: May be diluted in 50 mL of 0.9% NaCl, D5W, dextrose/saline combinations, D5/LR, LR, or 10% mannitol solution. Solution is clear and colorless. Stable for 24 hr at room temperature or 48 hr if refrigerated after dilution.
  • Rate: Administer each dose as an IV infusion over up to 15 min.
  • Y-Site Compatibility: acetaminophen, alfentanil, amifostine, amikacin, amiodarone, anidulafungin, argatroban, aztreonam, bivalirudin, bleomycin, bumetanide, buprenorphine, busulfan, butorphanol, calcium chloride, calcium gluconate, carboplatin, carmustine, caspofungin, ceftazidime, chlorpromazine, ciprofloxacin, cisplatin, clindamycin, cyclophosphamide, cyclosporine, cytarabine, daptomycin, dacarbazine, dactinomycin, daptomycin, daunorubicin, dexmedetomidine, dexrazoxane, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxacurium, doxorubicin hydrochloride, doxycycline, enalaprilat, ephedrine, epinephrine, epirubicin, epfitibatide, ertapenem, erythromycin, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fludarabine, gemcitabine, gentamicin, haloperidol, hetastarch, hydromorphone, idarubicin, ifosfamide, imipenem/cilastatin, irinotecan, isoproterenol, leucovorin caclium, levofloxacin, levorphanol, lidocaine, linezolid, lorazepam, magnesium sulfate, mannitol, mechlorethamine, meperidine, mesna, methotrexate, metoclopramide, metronidazole, midazolam, milrinone, mitomycin, mitoxantrone, morphine, moxifloxacin, mycophenolate, nalbuphine, naloxone, nesiritide, nicardipine, nitroglycerin, nitroprusside, octreotide, oxaliplatin, oxytocin, paclitaxel, pamidronate, pancuronium, pemetrexed, pentamidine, phenylephrine, potassium acetate, potassium chloride, procainamide, prochlorperazine, promethazine, propranolol, quinupristin/dalfopristin, ranitidine, rocuronium, sodium acetate, streptzocin, sufentanil, tacrolimus, teniposide, theophylline, thiopental, thiotepa, tigecycline, tirofiban, tobramycin, vancomycin, vecuronium, verapamil, vinblastine, vincristine, vinorelbine, voriconazole, zidovudine, zoledronic acid
  • Y-Site Incompatibility: Manufacturer recommends not admixing with other medicationsacyclovir, alemtuzumab, aminocaproic acid, aminiphylline, amphotericin B colloidal, amphotericin B lipid complex, amphotericin B liposome, pantoprazole

Patient/Family Teaching

  • Advise patient to notify health care professional if nausea or vomiting occurs.
  • Advise patient to notify health care professional symptoms of abnormal heart rate or rhythm (racing heart beat, shortness of breath, dizziness, fainting) occur.

Evaluation/Desired Outcomes

  • Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy.
  • Prevention and treatment of postoperative nausea and vomiting.

Anzemet™

Dolasetron mesylate An antiemetic for postoperative and chemotherapy-related N&V