dolasetron


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dolasetron

 [do-las´ĕ-tron]
a selective serotonin receptor antagonist, used as the mesylate salt for the prevention of nausea and vomiting associated with chemotherapy or occurring after surgery; administered orally and intravenously.

dolasetron

(dol-a-se-tron) ,

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.

dolasetron

/do·las·e·tron/ (do-las´ĕ-tron) a selective serotonin receptor antagonist, used as the mesylate salt for the prevention of nausea and vomiting associated with chemotherapy or occurring after surgery; administered orally and intravenously.

dolasetron

an antiemetic.
indications It is used to prevent the nausea and vomiting associated with cancer chemotherapy and radiotherapy, and to prevent postoperative nausea and vomiting.
contraindication Known hypersensitivity prohibits its use.
adverse effects Bronchospasm and arrhythmias are life-threatening effects of this drug. Other adverse reactions include constipation, increased AST and ALT, abdominal pain, anorexia, dizziness, fatigue, drowsiness, rash, urinary retention, oliguria, electrocardiogram changes, hypotension, tachycardia, and hypertension. Common side effects include diarrhea and headache.
References in periodicals archive ?
Our study forecasts individual revenues of eight top products: -- Palonosetron -- Ondansetron -- Granisetron -- Dolasetron -- Dronabinol -- Nabilone -- Metoclopramide -- Domperidone.
3] receptor antagonists (azasetron, dolasetron, granisetron, ondansetron, ramosetron, and tropisetron) are equally effective and toxic when used at the recommended doses, and differ only in terms of cost.
Also, Bock and colleagues18 reported that dolasetron 1 mg.
3] receptor antagonist: results of a phase III, single-dose trial versus dolasetron.
3]) receptor antagonists (ondansetron, granisetron, dolasetron, and palonosetron) approved by the US Food and Drug Administration between 1991 and 2003.
In 2006, the typical regimen--Camptosar (irinotecan), leucovorin, fluorouracil, dolasetron, and dex-amethasone--was $8.
Financial Support: Abbott Laboratories (Abbott Park, IL) provided 70 dolasetron 12.
3] receptor antagonists ondansetron, dolasetron (Anzemet), or granisetron (Kytril) prevent emesis in about 30% more men than women.
The following drugs were checked: granisetron, ondansetron, tropisetron, dolasetron, alizapride, zolpidem, tianeptine, methylprednisolone, fluoxetine, dextropropoxyphene, acetaminophen, enoxaparin, nifedipine, bromazepam, lorazepam, chlorazepate, levothyroxine, zopiclone, tinzaparin, cetirizine, simvastatin, famotidine, glibenclamide, and omeprazole.
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.
Analysis of Phase III Clinical Studies for Palonosetron, Ondansetron, Dolasetron and Granisetron in the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) Poster Session