section name header

Pronunciation ⬇

gra-NI-se-tron

Classifications ⬆ ⬇

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

Indications ⬆ ⬇

REMS


Action ⬆ ⬇

  • Blocks the effects of serotonin at receptor sites (selective antagonist) located in vagal nerve terminals and in the chemoreceptor trigger zone in the CNS.
Therapeutic effects:
  • Decreased incidence and severity of nausea and vomiting following emetogenic chemotherapy, radiation therapy, or surgery.

Pharmacokinetics ⬆ ⬇

Absorption: 50% absorbed following oral administration; transdermal enters systemic circulation via passive diffusion through intact skin. IV administration results in complete bioavailability.

Distribution: Distributes into erythrocytes; remainder of distribution is unknown.

Metabolism/Excretion: Mostly metabolized by the liver; 12% excreted unchanged in urine.

Half-Life: Patients with cancer: 10–12 hr (range 0.9–31.1 hr); healthy volunteers: 3–4 hr (range 0.9–15.2 hr); older adults: 7.7 hr (range 2.6–17.7 hr); SUBQ: 24 hr.

Time/Action Profile ⬆ ⬇

( plasma concentrations)

ROUTEONSETPEAKDURATION
POrapid60 min24 hr
IV1–3 min30 minup to 24 hr
TDunknown48 hrunknown
SUBQunknown12 hr7 days

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, QT interval prolongation

Derm: Topicalapplication site reactions, photosensitivity

GI: constipation, ↑liver enzymes, abdominal pain, diarrhea, dyspepsia.

Local: injection site reactions (SUBQ)

Neuro: headache, agitation, anxiety, CNS stimulation, dizziness, drowsiness, dysgeusia, headache, insomnia, weakness

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

Prevention of Nausea and Vomiting Due to Emetogenic Chemotherapy

Prevention of Nausea and Vomiting Associated with Radiation Therapy

Prevention and Treatment of Postoperative Nausea and Vomiting

Prevention of Acute and Delayed Nausea and Vomiting Due to Emetogenic Chemotherapy

Renal Impairment

Availability ⬆ ⬇

(Generic available)

Assessment ⬆ ⬇

Lab Test Considerations:

Implementation ⬆ ⬇

IV Administration:

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Kytril, Sancuso, Sustol

Code ⬆

NDC Code