Palonosetron

Registered South African indications:

• Nausea and vomiting

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Pregnancy
• Breastfeeding
• Severe renal impairment
• Patients on haemodialysis
• History of constipation  
• Suspected subacute intestinal obstruction  
• Personal or family history of QT prolongation
• Electrolyte abnormalities
• Hypokalaemia
• Hypomagnesemia
• Congestive heart failure
• Bradyarrhythmias
• Conduction disturbances
• Use in the days following chemotherapy  
• May impair ability to drive and operate machinery  

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

Prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy
Prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy

• IV: 250μg, as single bolus over 30sec, 30min prior to chemotherapy

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The efficacy of palonosetron in the prevention of nausea and vomiting induced by highly emetogenic chemotherapy may be enhanced by the addition of a corticosteroid administered prior to chemotherapy

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Repeated dosing within a seven-day interval is not recommended

Not established for use in children younger than 18 years in South Africa

Pregnancy

• Caution
• For palonosetron no clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect
  harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Only
  limited data from animal studies are available regarding the placental transfer
• There is no experience of palonosetron in human pregnancy. Therefore, palonosetron should not be used in pregnant
  women unless it is considered essential by the physician

Breastfeeding

• Caution; not recommended 
• As there are no data concerning palonosetron excretion in breast milk, breast-feeding should be discontinued during
  therapy

Fertility

• There are no data concerning the effect of palonosetron on fertility

Renal Impairment 

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended 
• Haemodialysis: Caution; no information available

Hepatic Impairment 

• No dose adjustment recommended 

Elderly  

• No dose adjustment recommended 

Porphyria

• Probably not porphyrinogenic (PNP) 

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Headache
• Dizziness
• Somnolence
• Insomnia
• Paraesthesia
• Hypersomnia
• Peripheral sensory neuropathy
• Anxiety
• Euphoria
• Asthenia

Cardiovascular Disorders

• Tachycardia
• Bradycardia
• Supraventricular extrasystoles
• Myocardial ischaemia
• Sinus arrhythmia
• Hypotension
• Hypertension
• Vein discolouration
• Vein distention 
• Electrocardiogram QT prolongation

Respiratory Disorders

• Hiccups

Gastrointestinal Disorders

• Constipation
• Diarrhoea
• Dyspepsia
• Abdominal pain
• Dry mouth
• Flatulence

Hepatobiliary Disorders

• Hyperbilirubinaemia
• Increased transaminases

Genitourinary Disorders

• Urinary retention
• Glycosuria

Endocrine and Metabolic Disorders

• Hyperkalaemia
• Hypocalcaemia
• Anorexia
• Hyperglycaemia
• Decreased appetite
• Metabolic disorders

Musculoskeletal Disorders

• Arthralgia

Skin and Subcutaneous Tissue Disorders ,7

• Allergic dermatitis
• Pruritic rash
• Injection site reaction
  - Burning
  - Induration
  - Discomfort
  - Pain

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
• Anaphylactoid reactions
• Anaphylactic shock
• Fever
• Influenza-like illness

Sensory Disorders

• Eye irritation
• Amblyopia
• Motion sickness
• Tinnitus

• Serotonergic agents  
• Selective serotonin reuptake inhibitors (SSRIs)
• Serotonin noradrenalin reuptake inhibitors (SNRIs)
• Anti-arrhythmic agents
• QT prolonging agents
• Agents resulting in electrolyte abnormalities

None routine

Palonosetron is a selective serotonin subtype 3 (5HT3) receptor antagonist. It blocks serotonin on vagal nerve terminals in the periphery, and centrally in the chemoreceptor trigger zone.  

Injection (per ml) 50μg

• Onicit (Pfizer) originator

Injection (per 5ml) 250μg

• Tronson (Eurolab)