Brand Names
Zofran
Broad Category
Antiemetic
Pharmacological class
selective 5-HT3 receptor antagonist
MOA
Selectively blocks serotonin 5-HT3 receptors (ligand gated ion channel), with little to no effect on dopamine receptors
- located in CTZ area postrema and the nucleus tactus solitarius
- also located peripherally on abdominal vagal afferents in the GI tract
Blocks emetogenic stimuli arising from the GI tract
Indications / Clinical uses
Perioperative use
- rescue treatment and prophylaxis for PONV
Rescue and prophylaxis for chemo-induced N/V
Adult dosing
4 mg IV
Pediatric Dosing
50-100 mcg/kg (MAX 4 mg)
Optimal timing?
End of surgery/procedure
Long procedure: 20-30 mins before end
Onset
˜10 mins
Duration
4-6 hours
Most Common SE
HA and Diarrhea
CV effects
QT prolongation (massive doses)
- black box warning: torasades de pointes (after doses of 32 mg given lol)
Precautions
Hepatic impairment
- Prolongs clearance
CYP2D6 poor metabolizers (prolongs)
QT prolongation (cautious - leads to torsades)
Drug to drug interactions
May precipitate serotonin syndrome when given with 2 or more other serotonergic meds
- SSRIs
- MAOIs
- fentanyl
- meperidine
- linezolid
Metabolism
Hepatic CYP450
- CYP3A4
- CYP2D6
- CYP1A2
Conjugation
Elimination
Primarily: Renal and Biliary
Vd considerations
Moderate - Large
- extensive tissue distribution
- moderate lipophilicity
Clearance Considerations
Reduced Clearance with severe hepatic impairment
Protein binding
70-76%