Granisetron: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

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.

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.

Pregnancy Category (US FDA)

IV/Parenteral/PO/SC/Transdermal: B

Patient Counseling Information

Avoid prolonged exposure to heat (transdermal patch).

Monitoring Parameters

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:
Mechanism of Action: 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

Storage

Tab/oral soln/inj: Store between 15-30°C. Protect from light. Patch: Store between 20-25°C.

MIMS Class

Antiemetics / Supportive Care Therapy

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.

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