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Sota
Omoigui's
Anesthesia Drug Handbook
3rd Edition:
:
Dolasetron Mesylate
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SECTION
ONE:
Uses, Dosing,
Elimination
SECTION TWO:
Preparation, Pharmacology, Pharmacokinetics
SECTION THREE:
Interactions, Toxicity
Guidelines/Precautions
Principal Adverse Reactions
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Uses
prevention and treatment of chemotherapy-induced and postoperative nausea and vomiting
Dosing
Chemo/Radiotherapy induced Nausea/Vomiting :
Adults PO/Slow IV 100 mg
Children: Slow IV 1.8 mg/kg (max.100 mg) within 30 mins before chemo or radiotherapy
Administer first dose 30 mins-2 hours before start of Chemo or Radiotherapy and for 1-2 days after Chemo or Radiotherapy. Administer IV dose over 30 seconds. Injection preparation mixed in apple or apple-grape juice may be used for oral dosing in pediatric patients.
Children: PO 1.2 mg/kg (max.100 mg)
No dose adjustment is recommended in elderly patients or patients with renal or hepatic impairment.
Postoperative Nausea - Oral Premedication :
Adults: PO 100 mg
Children: PO 1.2 mg/kg (max.100 mg)
Administer 1-2 hours before surgery.
Postoperative Nausea - Prevention/Treatment
Adults: IV 12.5 mg.
Children: IV 0.35 mg/kg (max.12.5 mg)
Dolasetron may be administered by direct IV injection (at a rate no greater than 100 mg/30 seconds) or as an intravenous infusion (dilute and administer over 15 mins). For prevention of postoperative nausea, administer IV dose, 15 minutes before cessation of anesthesia
Elimination
hepatic
How supplied
Injection: 12.5 mg./0.625 ml, 100 mg/5 ml
Tablets: 50 mg,, 100 mg
Storage
Temperature between 2-30 degrees Celsius. Protect from light.
DILUTION FOR INFUSION: Dilute in 50 mls of D5W, NS, LR.
Pharmacology
Dolasetron is a selective serotonin 5-HT3 receptor antagonist. The drug is rapidly metabolized by carbonyl reductase to the active form hydrodolasetron, which is 50-fold more potent than dolasetron. 5-HT3 receptors are present both peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates the 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex. Dolasetron may antagonize the emetic effects of serotonin at either or both receptor sites. Dolasetron does not antagonize dopamine receptors. The active metabolites of dolasetron may block sodium channels and produce dose-dependent reversible EKG changes e.g. QRS widening. Dolasetron is comparable in anti-emetic efficacy with ondansetron. A single intravenous dose of 1.8 mg/kg was comparable with a single intravenous dose of 32 mg of ondansetron in prevention of cancer chemotherapy induced nausea and vomiting. Transient increases in hepatic transaminase levels may occur following therapy. The drug may cross the placenta and may be excreted in breast milk. It should be used with caution in pregnant and nursing mothers. .
Pharmacokinetics
ONSET: IV < 30 minutes
PEAK EFFECT: IV variable
DURATION: IV 12-24 hours
Interactions
serum levels may be altered with concomitant administration of phenytoin, phenobarbital and rifampin
Guidelines
(1) Dolasetron does not stimulate gastric or intestinal peristalsis. It should not be used in place of a nasogastric tube. As with other antiemetics, the use of dolasetron in abdominal surgery may mask a progressive ileus and/or gastric distension.
(2) Dolasetron can cause EKG changes (PR, QTc, JT prolongation and QRS widening. These changes are self limiting and related in magnitude and frequency to the blood levels of the active metabolite. Dolasetron should be used with caution in patients who have or may develop prolongation of cardiac conduction intervals, particularly QTc. These include patients with hypokalemia or hypomagnesemia, patients taking diuretics with potential for inducing electrolyte abnormalities, patients with congenital QT syndrome, patients taking anti-arrhythmic drugs or other drugs, which lead to QT prolongation and cumulative high dose anthracycline therapy.
(3) Dolasetron is contraindicated in patients known to be hypersensitive to the drug.
Principal Adverse Reactions
CVS: hypotension, bradycardia, tachycardia, angina, bundle branch block (left and right), atrial flutter/fibrillation, T wave change, poor R-wave progression, second degree heart block
PULM: bronchospasm, shortness of breath
CNS: headache, dizziness, paresthesias, tremors, depersonalization, agitation
GI: constipation, dyspepsia, diarrhea, abdominal pain, hepatic dysfunction, rarely-pancreatitis
OTHER: blurred vision, pain and redness at site of injection
Reactions
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Address:
4019 W. Rosecrans Ave., Hawthorne, CA 90250-7913
Toll-Free: (800) 9-MEDIC-9, Phone: (310) 675-9121,
Fax: 310 675-7989, E-mail: medicinechief@aol.com
NOTICE:
Every effort has been made to ensure that the drug dosage schedules
herein are accurate and in accord with the standards accepted
at the time of publication. As new research and experience broaden
our knowledge, changes in treatment and drug therapy occur. The
medications described do not necessarily have specific approval
by the Food and Drug Administration for use in the situations
and the dosages for which they are recommended. This information
is advisory only. The package insert should be consulted for use
and dosage as approved by the FDA, for any changes in indications
and dosages and for added warnings and precautions. The ultimate
responsibility lies with the prescribing physician.
No part of this information may be reproduced or transmitted electronically
in any information storage or retrieval system, or within any
monitoring system without prior permission in writing from S.O.T.A.
Technologies (Electronic Publishers).
The Universal Drug Infusion Slide Ruler (patent pending) is now
available. It incorporates an infusion data guide and enables
infusion calculations for any drug at any dose and at any concentration.
It may be obtained by calling S.O.T.A Technologies (800 9-MEDIC-9)
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COMPOUNDED
TOPICAL MEDICATIONS MAY BE ORDERED (BY PRESCRIPTION ONLY) FROM L.A.
PAIN CLINIC. CALL 310 675-9121 or 1 800 9-MEDIC-9. |
Copyright 2000. Sota Omoigui, M.D. All rights reserved.
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