Palonosetron

ALOXI

Open Palonosetron in the interactive console ↗

Pronunciation: pal-oe-NOE-se-tron

Palonosetron ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Palonosetron ballicule

What it isLong-acting second-generation 5-HT3-receptor antagonist; prevention of chemotherapy-induced nausea and vomiting.

Why this oneIts unusually durable receptor effect extends protection into delayed chemotherapy nausea, where older setrons fade.

What limits itIt has little QT effect compared with dolasetron or ondansetron; constipation, headache, and cost remain.

Palonosetron molecular structure (skeletal formula) — Molecular structure: Palonosetron

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
CINV - moderately emetogenic chemo (acute & delayed) and highly emetogenic chemo (acute)	Adults	0.25 mg IV single dose	single dose ~30 min before chemo (infuse over 30 sec)	0.25 mg
Postoperative nausea and vomiting (up to 24 h post-surgery)	Adults	0.075 mg IV single dose	immediately before anesthesia induction (over 10 sec)	0.075 mg
CINV - emetogenic chemo incl. HEC (acute)	Pediatric 1 month to <17 years	20 mcg/kg IV single dose (max 1.5 mg)	single dose ~30 min before chemo (infuse over 15 min)	1.5 mg

Renal Undefined

Hepatic Undefined

Instructions

Supplied ready for IV use at 0.05 mg/mL; do not mix with other drugs
Flush infusion line with normal saline before and after administration
Inspect for particulate matter/discoloration; discard unused portion
CINV: give ~30 min before chemotherapy (adults infuse over 30 sec; pediatrics over 15 min)
PONV: give over 10 sec immediately before induction of anesthesia

Available strengths

inj 0.05 mg/mL

Cautions

Hypersensitivity reactions incl. anaphylaxis/anaphylactic shock (may occur with or without known hypersensitivity to other 5-HT3 antagonists); do not reinitiate after a reaction
Serotonin syndrome, especially with concomitant serotonergic drugs

Adverse reactions

Headache
Constipation
QT prolongation (PONV)
Bradycardia (PONV)

Pregnancy No human data; animal reproduction studies showed no embryo-fetal harm at doses far above the human IV dose.

Lactation No data on presence in human milk, effects on the infant, or milk production; weigh benefits against risk.

Cost

Palonosetron (ALOXI)

Strength		#/mo	generic $/unit	CostPlus
0.05 mg/mL	inj	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Palonosetron is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Available combined with: Netupitant (AKYNZEO)

NO BOXED WARNINGS

Principal riskConstipation and headache; cost

Classes and tags

Antiemetics

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Defining liabilityConstipation, headache and rare anaphylaxis

Serotonicity

This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.

Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.

Retarded orgasm
Efficacy in OCD and cataplexy
Clonus and hyperreflexia in single-drug overdose
Serotonin toxicity when combined with an MAOI

Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.

Open Palonosetron in the interactive console ↗