Systemic Therapy Program

Search Again

Date



Disease Group



Cancer Type

Document Type

Drug Monographs
Treatment Regimens

Scientific Name:
DOLASETRON
Brand Name(s):
Anzemet

Drug Monograph

Pharmacology

Mechanism of Action

Selective serotonin receptor (5-HT3) antagonist, blocking serotonin both peripherally (primary site of action) and centrally at the chemorecptor trigger zone.

Pharmacokinetics

Oral Absorption
yes,well absorbed, but rapid and complete metabolism
Distribution
not found to be distributed extensively to blood cells; excretion in breast-milk unknown
cross blood brain barrier? No information
Vd: Hydrodolasetron: 5.8 L/kg 
PPB: high (69 to 77%); to a1-acid-glycoprotein: 50%
Metabolism
liver, by means of the ubiquitous enzyme, carbonylreductase to a reduced alcohol (hydrodolasetron); active metabolite: MDL 74 156
further hydroxylation by P450 CYP 2D6 and further N-oxidation by both CYP 3A and flavin monooxygenase
Excretion  no information, renal?
t½ dolasetron: 10 min; MDL 74 156: 8 hours
Cl: oral: hydrodolasetron: 13.4 mL/min/kg I.V.: 9.4 mL/min/kg

Side Effects

IMMEDIATE ONSET (hours to days)
   headache (31%), dizziness, lightheadness (23%)
EARLY ONSET (days to weeks)
   diarrhea (50%), increased appetite (27%)
   cardiovascular: Hypertension, hypotension (6.3%), EKG abnormalities, prolonged P-R, QRS and QTc intervals

Therapeutics

Approved Indications

Oral:
• 100mg po given 1 hour prior to chemotherapy; some oncologists prefer to give 200mg po prechemo
Injection:
• 1.8mg/Kg or ‘flat’ dose of 100mg IV, 30 minutes before chemotherapy
• May be given as iv push over 30 seconds, or diluted in 50mL NS or D5W and infused over 15 minutes
• Dolasetron should not be admixed with any other drugs
Pediatric
Intravenous:
• 1.8mg/Kg IV as a single dose before chemotherapy for children 2-16 years
Oral:
• 1.8mg/Kg (up to 100mg) PO 30 minutes before chemotherapy, using tablet or IV solution for oral administration (mixed in apple or apple-grape juice)

Routes

Oral:
• 100mg po given 1 hour prior to chemotherapy; some oncologists prefer to give 200mg po prechemo
Injection:
• 1.8mg/Kg or ‘flat’ dose of 100mg IV, 30 minutes before chemotherapy
• May be given as iv push over 30 seconds, or diluted in 50mL NS or D5W and infused over 15 minutes
• Dolasetron should not be admixed with any other drugs
Pediatric
Intravenous:
• 1.8mg/Kg IV as a single dose before chemotherapy for children 2-16 years
Oral:
• 1.8mg/Kg (up to 100mg) PO 30 minutes before chemotherapy, using tablet or IV solution for oral administration (mixed in apple or apple-grape juice)

IV Compatibility

• Prevention of nausea & vomiting from emetogenic chemotherapy

Dose Adjustment Criteria

• Dose may be given through side arm of a free-flowing IV, over 30-60 seconds (administering nurse should be certified to administer IV push chemotherapy agents and other vesicant agents)
• May be mixed in 50mL minibag (5% Dextrose, Normal Saline); Give over 15 minutes

Antiemetic Risk

normal saline, 5% dextrose

Monitoring

Product Information

Commercial Product Description

Brand Name: Anzemet® Vials with 100mg/5mL Pink tablets with 50mg & 100mg

Note

HANDLING RISK LEVEL:
RECOMMENDED CRITERIA
NO RECOMMENDED TOXICITY RATINGS
SUGGESTED CRITERIA
NO ADDITIONAL TOXICITY RATINGS

SERIOUS WARNINGS:
CYP 2D6 and 3A3/4 enzyme substrate products
cimetidine, rifampin, atenolol
drugs causing QTc interval prolongation

Availability & Funding



© 2017 Cancer Care Nova Scotia    Sitemap | Privacy                                                                                                        Report broken links and errors to nshealth.ca