Granisetron

Registered South African indications:

• Post-cytotoxic chemotherapy/radiotherapy nausea and vomiting
• Post-operative nausea and vomiting

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Pregnancy
• Breastfeeding
• Hepatic impairment
• Gastrointestinal obstruction
• Arrhythmias
• QT prolongation
• Risk factors for QT prolongation
• Paediatric population
• Risk factors for Serotonin Syndrome
• Galactose intolerance
• Lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab, inj

Prevention of post-cytotoxic chemotherapy nausea and vomiting

• IM: 3mg, 15min before start of chemotherapy
• IV: 1-3mg (10-40μg/kg), bolus given as a slow injection over 30sec before chemotherapy
  OR
• IV: 1-3mg (10-40μg/kg), as an infusion over 5min before chemotherapy
• Oral (tab): 1mg, 12hrly OR 2mg, dly; Treatment duration: For up to 1 week after chemotherapy

Oral: 1st dose to be given within 1hr before the start of therapy

Treatment of post-cytotoxic chemotherapy nausea and vomiting

• IM: 3mg, 15min before start of chemotherapy; Repeat dose twice within the next 24hrs if needed
• IV: 1-3mg (10-40μg/kg), bolus given as a slow injection over 30sec; Repeat as needed at intervals of at least 10min; Max: 9mg/24hrs
  OR 
• IV: 1-3mg (10-40μg/kg), as an infusion over 5min; Repeat as needed at intervals of at least 10min; Max: 9mg/24hrs

Prevention of post-radiotherapy nausea and vomiting

• Oral (tab): 2mg, dly; Treatment duration: For up to 1 week after radiotherapy

Oral: 1st dose to be given within 1hr before the start of therapy

• IV: 1-3mg (10-40μg/kg), bolus given as a slow injection over 30sec before chemotherapy
  OR
• IV:1-3mg (10-40μg/kg), as an infusion over 5min before radiotherapy

Post-operative nausea and vomiting
Prevention

• IV: 1mg, bolus given as a slow injection over 30sec before induction

Treatment

• IV: 1mg, bolus given as a slow injection over 30sec before induction; Repeat as needed; Max: 3mg/24hrs

Do not cut/crush/chew/dissolve tablets 

See additional prescribing points for administration directions

Paed. forms avail. in SA and covered in this monograph: inj

Prevention and treatment of post-cytotoxic chemotherapy nausea and vomiting

Younger than 2 years

• Not established for use

Older than 2 years

• IV: 10-40μg/kg, as an infusion over 5min before chemotherapy; Repeat dose once in 24hrs if required at an interval of at least 10min; Max single dose: 3mg

Do not cut/crush/chew/dissolve tablets 

See additional prescribing points for administration directions

Pregnancy

• Caution; no evidence of risk in studies
• There is limited amount of data from the use of granisetron in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of granisetron during pregnancy

Breastfeeding

• Caution; not recommended
• It is unknown whether granisetron or its metabolites are excreted in human milk. As a precautionary measure, breastfeeding should not be advised during treatment with granisetron

Fertility

• In rats, granisetron had no harmful effects on reproductive performance or ferility

Renal Impairment

• No dose adjustment recommended

Hepatic Impairment 

• Caution; no dose adjustment recommended 

Elderly

• No dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Headache
• Extrapyramidal reactions

Cardiovascular Disorders

• QT prolongation 

Gastrointestinal Disorders

• Constipation
• Diarrhoea

Hepatobiliary Disorders

• Increased transaminases

Skin and Subcutaneous Tissue Disorders

• Rash

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions

• QT prolonging agents
• Serotonergic agents
• Cardiotoxic chemotherapy
• Phenobarbital

ECG

Administration directions

IV infusion in adults

• Dilute in 20-50ml of normal saline or 5% dextrose-containing fluid
• Infuse over 5min

IV infusion in children

• Dilute dosage in 10-30ml of normal saline or 5% dextrose-containing fluid
• Infuse over 5min

Method of administration

The tablets should be swallowed whole with water

Granisetron is a potent selective antagonist of serotonin receptors in the vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema, which results in its antiemetic properties.

Film-coated tablet 1mg

• Granicip (Cipla)
• Granitril (Ranbaxy)

Tablet 1mg

• Aspen Granisetron (Pharmacare) 
• Kytril (Roche) originator

Film-coated tablet 2mg

• Granicip (Cipla)

Tablet 2mg

• Aspen Granisetron (Pharmacare) 
• Kytril (Roche) originator

Injection (per 1ml) 1mg

• Adco Granisteron (Adcock Ingram)
• Granicip (Cipla)
• Granisteron Fresenius (Fresenius) 
• Granisetron Teva (Teva)
• Granitril (Ranbaxy)
• Grantryl (Brimpharm)
• Kytril (Roche)
• Sandoz Granisetron (Sandoz)

Injection (per 3ml) 3mg

• Adco Granisteron (Adcock Ingram)
• Granisteron Fresenius (Fresenius) 
• Granisetron Teva (Teva)
• Grantryl (Brimpharm)
• Mylan Granisetron (Mylan)
• Sandoz Granisetron (Sandoz)