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Drugs reference index «Dolasetron Mesylate»

Dolasetron Mesylate

Pronunciation: (dahl-AH-set-rahn)Class: 5-HT 3 receptor antagonist

Trade Names:Anzemet- Injection 20 mg/mL- Tablets 50 mg- Tablets 100 mg

Pharmacology

Selective serotonin (5-HT 3 ) receptor antagonist that inhibits serotonin receptors in the GI tract and chemoreceptor zone.

Pharmacokinetics

Absorption

Parent drug rapidly eliminated and completely metabolized to hydrodolasetron (active). T max for hydrodolasetron is approximately 1 h (oral) and approximately 0.6 h (IV). Bioavailability is approximately 75% (determined by hydrodolasetron).

Distribution

Vd approximately 5.8 L/kg (hydrodolasetron). Hydrodolasetron is 69% to 77% protein bound.

Metabolism

Reduced to hydrodolasetron by carbonyl reductase. Subsequent hydroxylation due to CYP2D6 and N-oxidation due to CYP3A and flavin monooxygenase.

Elimination

Approximately 67% of dose recovered in the urine (61% as hydrodolasetron) and approximately 33% recovered in the feces.

t ½ less than 10 min for dolasetron (IV), approximately 7.3 h for hydrodolasetron (IV), and approximately 8.1 h (oral).

Cl approximately 9.4 mL/min/kg (IV) and approximately 13.4 mL/min/kg (oral) for hydrodolasetron.

Indications and Usage

Parenteral or oral

Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy; prevention of postoperative nausea and vomiting in patients at risk.

Parenteral only

Treatment of postoperative nausea and vomiting.

Unlabeled Uses

Radiotherapy-induced nausea and vomiting.

Contraindications

Standard considerations.

Dosage and Administration

Prevention of Chemotherapy-Induced Nausea and VomitingAdults and children older than 16 yr of age

PO 100 mg within 1 h before chemotherapy. IV 1.8 mg/kg (or 100 mg) infused rapidly over 30 sec or diluted and infused over 15 min, 30 min before chemotherapy.

Children 2 to 16 yr of age

PO 1.8 mg/kg (max 100 mg) within 1 h before chemotherapy. IV 1.8 mg/kg (max 100 mg) infused rapidly over 30 sec or diluted and infused over 15 min, 30 min before chemotherapy.

Prevention of Postoperative Nausea and Vomiting in Patients at RiskAdults and Children older than 16 yr of age

PO 100 mg within 2 h before surgery. IV 12.5 mg 15 min before cessation of anesthesia.

Children 2 to 16 yr of age

PO 1.2 mg/kg (max of 100 mg) within 2 h before surgery. IV 0.35 mg/kg (max of 12.5 mg) 15 min before cessation of anesthesia.

Treatment of Postoperative Nausea and VomitingAdults and Children older than 16 yr of age

IV 12.5 mg as a single dose as soon as nausea and vomiting presents.

Children 2 to 16 yr of age

IV 0.35 mg/kg as a single dose as soon as nausea and vomiting present.

General Advice

  • Dolasetron injection may be mixed with apple or apple-grape juice for oral administration in children. Use within 2 h of dilution.
  • Compatible IV fluids include: sodium chloride 0.9%, dextrose 5%, dextrose 5% and sodium chloride 0.45%, dextrose 5% and lactated Ringer injection, lactated Ringer injection and mannitol 10% injection.
  • Do not mix dolasetron injection with solution for which compatibility has not been established.
  • Do not mix dolasetron injection with other drugs.
  • Flush infusion line before and after administration of dolasetron injection.
  • Inspect injectable solutions for particulate matter or discoloration before use.

Storage/Stability

Diluted injection is stable for 24 h at room temperature or for 48 h if refrigerated. Store tablets and undiluted injection at room temperature protected from light.

Drug Interactions

Drugs that prolong the QTc interval (eg, quinidine)

Additive effects on conduction.

Atenolol

Increased serum levels of active metabolite (IV only).

Cimetidine

Increased serum levels of active metabolite.

Rifampin

Decreased serum levels of active metabolite.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia; bradycardia; flushing; hypertension; hypotension.

CNS

Headache; vertigo; dizziness agitation; drowsiness; sleep disorder; depersonalization.

Dermatologic

Rash; itching; sweating.

GI

Abdominal pain; constipation; diarrhea; dyspepsia; anorexia; taste perversion; abnormal liver function.

Genitourinary

Oliguria; urinary retention.

Miscellaneous

Fever; fatigue; pain; chills; shivering.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy in children younger than 2 yr of age not established.

Conditions predisposing to prolongation of cardiac conduction intervals (eg, electrolyte abnormalities, class 1A antiarrhythmias)

Use with caution.

ECG Changes

Can cause ECG interval change (PR, QTc, JT) prolongation and QRS widening) which could cause CV consequences, including heart block and arrhythmias. These changes are related in magnitude and frequency to the active metabolite.

Patient Information

  • Advise patient that headache is common adverse reaction.
  • Advise patient that medication will greatly reduce likelihood of nausea and vomiting but that these are still possible.

Copyright © 2009 Wolters Kluwer Health.

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