Granisetron
KYTRIL
Pronunciation: gra-NI-se-tron
“Granny tron's Kite trail”
5-HT3 antagonist color theme (ondansetron, alosetron)
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
- nausea/vomiting (1993)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prevention of chemotherapy-induced nausea/vomiting | Adults | 2 mg QD or 1 mg BID, up to 1 h before chemo | 2 mg QD or 1 mg BID (2nd dose 12 h after 1st) | |
| Prevention of radiation-induced nausea/vomiting | Adults | 2 mg QD within 1 h of radiation | 2 mg QD |
Renal No adjustment needed
Hepatic No adjustment needed
Instructions
- Give up to 1 h before chemotherapy or within 1 h of radiation
- Administer only on day(s) of chemotherapy/radiation; continued dosing off-therapy not useful
Available strengths
- tab 1 mg
- sol 2 mg/10 mL
- inj 0.1, 1 mg/mL
- patch 3.1 mg/24 hr
Cautions
- QT prolongation reported
- Hypersensitivity reactions (including anaphylaxis) reported
Adverse reactions
- Headache
- Constipation
- Asthenia
- Diarrhea
- Abdominal pain
- Dyspepsia
Pregnancy Category B; animal studies show no fetal harm; use only if clearly needed
Lactation Undefined
Cost
| Strength | #/mo | generic $ | CostPlus | |
|---|---|---|---|---|
| 1 mg | tab | 30 qd | $39.15/mo | offered |
| 2 mg/10 mL | sol | per unit | not offered | |
| 0.1 mg/mL | inj | per unit | not offered | |
| 1 mg/mL | inj | per unit | not offered |
Generic entryLong generic
NO BOXED WARNINGS
Principal riskIt does not cover delayed emesis
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySedation, QT prolongation, extrapyramidal symptoms or anticholinergic toxicity vary by receptor target.
Serotonicity
This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.
5-HT3 antagonists block a serotonin receptor and are not Gillman-type serotonin-toxicity triggers.
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
Non-elevating action5-HT3 antagonist
Evidence confidenceHigh
Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.
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