Granisetron


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Nausea and vomiting associated w/ cancer chemotherapy 1-2 mg w/in 1 hr prior to start of chemotherapy, then 2 mg/day as a single or in 2 divided doses for up to 1 wk after chemotherapy. Max: 9 mg/day. Prophylaxis of nausea and vomiting associated w/ radiation therapy 2 mg once daily w/in 1 hr of irradiation. IV Nausea and vomiting associated w/ cancer chemotherapy or radiotherapy 1-3 mg 5 min prior to start of therapy; further doses may be given at least 10 min apart. Max: 9 mg/day. Treatment and prophylaxis of post-op nausea and vomiting 1 mg before induction of anaesth. Transdermal Nausea and vomiting associated w/ cancer chemotherapy Apply 1 patch at the upper arm 24-48 hr prior to chemotherapy; remove at least 24 hr after the end of chemotherapy. May be worn for up to 7 days.
Dosage Details
Intravenous
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 1 mg over 30 sec, to be given before induction of anaesth. May be repeated up to max of 3 mg in 24 hr.

Intravenous
Nausea and vomiting associated with cancer chemotherapy
Adult: 1-3 mg 5 min prior to start of chemotherapy, by infusion over 5 min or by bolus inj over at least 30 sec. Further doses may be given at least 10 min apart. Max: 9 mg daily.
Child: 2-16 yr 10-40 mcg/kg (max: 3,000 mcg) by infusion over 5 min to be given prior to start of chemotherapy. An additional dose may be given w/in 24 hr, at least 10 min after the 1st infusion.

Intravenous
Prophylaxis of nausea and vomiting associated with radiation therapy
Adult: 1-3 mg 5 min prior to start of radiotherapy, by infusion over 5 min or by bolus inj over at least 30 sec. Further doses may be given at least 10 min apart. Max: 9 mg daily.

Oral
Nausea and vomiting associated with cancer chemotherapy
Adult: 1-2 mg w/in 1 hr prior to start of chemotherapy, then 2 mg daily as a single or in 2 divided doses for up to 1 wk after chemotherapy. Max: 9 mg daily.

Oral
Prophylaxis of nausea and vomiting associated with radiation therapy
Adult: 2 mg once daily w/in 1 hr of irradiation.

Transdermal
Nausea and vomiting associated with cancer chemotherapy
Adult: As patch releasing 3.1 mg/24 hr: Apply 1 patch at the upper arm 24-48 hr prior to chemotherapy; remove at least 24 hr after the end of chemotherapy. May be worn for up to 7 days depending on the duration of the chemotherapy regimen.
Administration
May be taken with or without food. Take up to 1 hr before chemotherapy.
Reconstitution
IV infusion: Dilute in dextrose 5% or NaCl 0.9% inj to a total vol of 20-50 mL.
Incompatibility
Y-site: Amphotericin B. Syringe: Ceftriaxone.
Special Precautions
Patient w/ cardiac co-morbidities, on cardiotoxic chemotherapy and/or w/ concomitant electrolyte abnormalities. May mask progressive ileus and/or gastric distention. Childn. Pregnancy and lactation.
Adverse Reactions
Headache, insomnia, constipation, diarrhoea, elevated hepatic transaminases; QT prolongation; bradycardia, palpitations, sick sinus syndrome, chest pain. Application site reactions (transdermal): Rash, pain, erythema, pruritus, irritation, burn, vesicles, urticaria, discolouration; patch non-adhesion.
IV/Parenteral/PO/SC/Transdermal: B
Patient Counseling Information
Avoid prolonged exposure to heat (transdermal patch).
MonitoringParameters
Monitor for signs of subacute intestinal obstruction; ECG and clinical abnormalities.
Overdosage
Symptoms: Mild headache. Management: Symptomatic treatment.
Drug Interactions
Induced metabolism w/ phenobarbital. Risk of serotonin syndrome w/ other serotonergic agents e.g. SSRIs, and serotonin and norepinephrine reuptake inhibitors (SNRIs). Altered clearance w/ CYP enzyme inducers or inhibitors. Concomitant use w/ drugs known to prolong QT interval may result in clinical consequences.
Action
Description: Granisetron is a highly selective 5-HT3-receptor antagonist w/ little or no affinity for other serotonin receptors. It blocks serotonin peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone.
Duration: Up to 24 hr.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 60%. Time to peak plasma concentration: Approx 2 hr.
Distribution: Widely distributed throughout the body. Volume of distribution: Approx 3 L/kg. Plasma protein binding: Approx 65%.
Metabolism: Hepatically metabolised via N-demethylation and aromatic ring oxidation followed by conjugation.
Excretion: Via urine (<20% as unchanged drug), and the remainder in the urine and faeces (as metabolites). Elimination half-life: 6 hr (oral); approx 9 hr (IV).
Chemical Structure

Chemical Structure Image
Granisetron

Source: National Center for Biotechnology Information. PubChem Database. Sancuso, CID=5284566, https://pubchem.ncbi.nlm.nih.gov/compound/Sancuso (accessed on Jan. 23, 2020)

Storage
Tab/oral soln/inj: Store between 15-30°C. Protect from light. Patch: Store between 20-25°C.
ATC Classification
A04AA02 - granisetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.
References
Anon. Granisetron. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 26/10/2015.

Buckingham R (ed). Granisetron. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com/mc/martindale/2009/ms-3385-h.htm. Accessed 26/10/2015.

Granisetron Hydrochloride Injection, Solution (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/10/2015.

Granisetron hydrochloride Tablet (Ascend Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 26/10/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Granisetron hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 26/10/2015.

Sancuso. U.S. FDA. https://www.fda.gov/. Accessed 26/10/2015.

Disclaimer: This information is independently developed by MIMS based on Granisetron 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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