Drug reference

Palonosetron

Antiemetic

AntiemeticATC A04AA05

CDSCO approvedATC A04AA05

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

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Mechanism

Palonosetron is a specific 5HT3-receptor antagonist which blocks 5HT3 receptors in the gastrointestinal tract and in the CNS.

Indications

Prevention of nausea and vomiting associated with moderately or highly emetogenic cytotoxic chemotherapyNauseasuppressing nausea and vomitingChemotherapy-induced nausea and vomiting (acute and delayed)Postoperative nausea and vomiting (PONV)Nausea secondary to upper abdominal irradiationHyperemesis of pregnancychemotherapy induced nausea and vomiting (CINV) (acute phase)delayed vomiting (approved by US-FDA for delayed CINV)Prevention of chemotherapy-induced nausea and vomiting

Dosing

Adult: Moderately emetogenic chemotherapy: Oral 500 micrograms, 1 hour before treatment; alternatively, IV 250 micrograms administered over 30 seconds, 30 minutes before treatment. Severely emetogenic chemotherapy: IV 250 micrograms for 1 dose, administered over 30 seconds, 30 minutes before treatment.

Pharmacokinetics

Half-life

About 40 h (after intravenous injection in adults)

Metabolism

Metabolized principally by CYP2D6

Excretion

Metabolized and unchanged forms excreted in urine in roughly equal proportions

Contraindications

History of constipation
Intestinal obstruction
Susceptibility to QT-interval prolongation (including electrolyte disturbances)

Side effects

Common

ConstipationHeadacheDiarrhoea (with intravenous use)Dizziness (with intravenous use)Electrolyte imbalance (with intravenous use)Metabolic disorder (with intravenous use)Constipation or diarrheaLight-headednessfatiguedizzinessabdominal pain

Serious

Amblyopia
Anxiety
Appetite decreased
Arrhythmias
Arthralgia
Asthenia
Drowsiness
Dry mouth
Dyspepsia
Euphoric mood
Eye irritation
Feeling hot
Fever
Flatulence
Glycosuria
Hiccups
Hyperbilirubinaemia
Hyperglycaemia
Hypertension
Hypotension
Influenza like illness
Motion sickness
Myocardial ischaemia
Paraesthesia
Peripheral neuropathy
QT interval prolongation
Skin reactions
Sleep disorders
Tinnitus
Urinary retention
Serotonin syndrome
additive Q-T prolongation (when given with moxifloxacin, erythromycin, anti-psychotics, antidepressants)
blurring of vision (rapid i.v. injection)