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

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

Derm:

Topical

application site reactions, photosensitivity

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

granisetron: Kytril, Sustol,

granisetron (transdermal): Sancuso

Code

NDC Code