Dolasetron


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Nausea and vomiting associated w/ cancer chemotherapy 100 or 200 mg once daily w/in 1 hr before chemotherapy. Duration of treatment: 4-7 days/cycle. Prophylaxis of post-op nausea and vomiting 50 mg at the induction of anaesthesia, or 100 mg w/in 2 hr before surgery. IV Treatment and prophylaxis of post-op nausea and vomiting 12.5 mg once daily over 30 seconds or 15 min; given as soon as symptoms present (treatment) or approx 15 min before cessation of anaesthesia (prophylaxis).
Dosage Details
Intravenous
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 12.5 mg once daily as IV push over 30 seconds or via infusion over 15 min; given as soon as nausea or vomiting present (treatment) or approx 15 min before cessation of anaesthesia (prophylaxis).

Oral
Nausea and vomiting associated with cancer chemotherapy
Adult: 100 or 200 mg once daily w/in 1 hr before chemotherapy. Duration of treatment: 4-7 consecutive days/chemotherapy cycle.

Oral
Prophylaxis of postoperative nausea and vomiting
Adult: 50 mg at the induction of anaesthesia, or 100 mg w/in 2 hr before surgery.
Reconstitution
IV infusion: Dilute in 50 ml of a compatible soln (i.e. NaCl 0.9%, dextrose 5%, Lactated Ringer’s soln, dextrose 5% and Lactated Ringer’s soln, dextrose 5% and NaCl 0.45%, and mannitol 10% inj).
Incompatibility
Incompatible w/ aciclovir, alemtuzumab, aminocaproic acid, aminophylline, amphotericin B, ampicillin Na, carmustine, cefazolin Na, chloramphenicol Na succinate, clindamycin phosphate, dexamethasone, K phosphate, thiopentone Na, 5-fluorouracil, heparin Na, methylprednisolone succinate, Na bicarbonate, pantoprazole, trimethoprim w/ sulfamethoxazole.
Contraindications
Complete heart block (w/o pacemaker), congenital QT syndrome.
Special Precautions
Patient w/ history of abnormal heart rhythms, structural heart disease, sick sinus syndrome, AF w/ slow ventricular response, myocardial ischemia, electrolyte abnormalities (i.e. hypokalaemia, hypomagnesemia). IV admin is not intended for prophylaxis of chemotherapy-associated nausea and vomiting. Pregnancy and lactation.
Adverse Reactions
Significant: PR, QRS, and QT prolongation.
Nervous: Dizziness, headache, drowsiness, fatigue, syncope, flushing, paraesthesia, tremor, ataxia, twitching, agitation, anxiety, sleep disorder, depersonalization, confusion, abnormal dreaming.
CV: Bradycardia, HTN, orthostatic hypotension, tachycardia, peripheral oedema and ischaemia, phlebitis.
GI: Diarrhoea, dyspepsia, flatulence, taste disturbance, constipation, abdominal pain, anorexia, pancreatitis.
Resp: Bronchospasm, dyspnea, epistaxis.
Genitourinary: Oliguria, dysuria, polyuria, acute renal failure, urinary retention, hematuria.
Haematologic: Anemia, hematoma, thrombocytopenia, prolonged partial thromboplastin time (PTT) and prothrombin time.
Musculoskeletal: Myalgia, arthralgia.
Ophthalmologic: Abnormal vision, photophobia.
Otic: Tinnitus.
Dermatologic: Pruritus, urticaria, increased sweating, rash.
Others: Chills, fever, pain, pain at inj site.
Potentially Fatal: Serotonin syndrome. Rarely, cardiac arrest, 2nd or 3rd degree AV block, serious ventricular arrhythmia (e.g. torsade de pointes).
IV/Parenteral/PO: B
MonitoringParameters
Monitor ECG, serum K and Mg concentration.
Overdosage
Symptoms: Severe hypotension, dizziness; PR, QRS, and QT prolongation. Management: Symptomatic and supportive treatment. Monitor cardiac function.
Drug Interactions
Increased risk of QT prolongation w/ other QT prolonging agents (e.g. pimozide, ziprasideone) and drugs known to cause electrolyte imbalance (e.g. diuretics). Decreased blood levels and therapeutic effects w/ rifampicin. Increased blood levels and effects w/ atenolol and cimetidine. Increased risk of conduction abnormalities when concurrently used w/ antiarrhythmic agents (e.g. verapamil, flecainide, quinidine).
Action
Description: Dolasetron, a selective serotonin (5-HT3) receptor antagonist, has antiemetic actions similar to ondansetron. It blocks serotonin both peripherally at the GI tract (main site of action) and centrally at the chemoreceptor trigger zone.
Pharmacokinetics:
Absorption: Rapid and completely absorbed (oral). Bioavalability: Approx 75%. Time to peak plasma concentration: Hydrodolasetron: Approx 1 hr (oral); 0.6 hr (IV).
Distribution: Widely distributed in the body. Volume of distribution: 5-7.9 L/kg. Plasma protein binding: 69-77%.
Metabolism: Rapidly metabolised hepatically via reduction by carbonyl reductase to hydrodolasetron (active metabolite); further metabolised by CYP2D6, CYP3A, and flavin monooxygenase enzymes.
Excretion: Via urine (approx 67%); faeces (approx 33%). Elimination half-life: Dolasetron: ≤10 min (IV); hydrodolasetron: 8.1 hr (oral); 7.3 hr (IV).
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Dolasetronum, CID=3033818, https://pubchem.ncbi.nlm.nih.gov/compound/Dolasetronum (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
A04AA04 - dolasetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
References
Anon. Dolasetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/02/2017.

Anzemet Injection (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/02/2017.

Anzemet Tablet, Film Coated (Validus Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/02/2017.

Buckingham R (ed). Dolasetron Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com . Accessed 27/02/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Dolasetron Mesylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 27/02/2017.

Disclaimer: This information is independently developed by MIMS based on Dolasetron from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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