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Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypertension, QT interval prolongation.

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

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:

Availability

(Generic available)

Route/Dosage

see Calculator

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

US Brand Names

Kytril, Sustol

granisetron (Transdermal): Sancuso

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

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

Patient/Family Teaching

Pronunciation

gra-NI-se-tron audio

Code

NDC Code*