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Granisetron

KYTRIL

What it is5-HT3 antagonist with hERG blockade; prevention of chemotherapy-associated nausea and vomiting.

Why this oneIts transdermal patch covers multiday chemotherapy, and QT effects are generally smaller than with ondansetron.

What limits itConstipation and headache are common; delayed emesis still needs a mechanistically different partner such as an NK1 antagonist.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Prevention of chemotherapy-induced nausea/vomitingAdults2 mg QD or 1 mg BID, up to 1 h before chemo2 mg QD or 1 mg BID (2nd dose 12 h after 1st)
Prevention of radiation-induced nausea/vomitingAdults2 mg QD within 1 h of radiation2 mg QD

Renal No adjustment needed

Hepatic No adjustment needed

Instructions

Cautions

Adverse reactions

Pregnancy Category B; animal studies show no fetal harm; use only if clearly needed

Lactation Undefined

NO BOXED WARNINGS

Principal riskIt does not cover delayed emesis

Cost, est. cash$300–$5,000/dose or month

Generic entryLong generic

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability1 / 4
QT / Torsades2 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilitySedation, QT prolongation, extrapyramidal symptoms or anticholinergic toxicity vary by receptor target.

Mechanism of action: Granisetron ballicule

Granisetron ballicule: receptor binding, kinetics and half-life diagram

Open Granisetron in the interactive console ↗

Memory aids: mascots and interaction avatars

Granisetron KYTRIL mascot mnemonic cartoon
“Granny tron's Kite trail”
5-HT3 antagonist color theme (ondansetron, alosetron)
Granisetron Box: minimal PK interactions avatar
Box: minimal PK interactions

Open Granisetron in the interactive console ↗