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INTRODUCTION

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granisetron (gra-nees-e-tron)

Kytril

granisetron (transdermal) (gra-nees-e-tron)

Sancuso

Classification

Therapeutic: antiemetics

Pharmacologic: 5-HT3 antagonists

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Indications
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Prevention of nausea and vomiting due to: emetogenic chemotherapy, radiation therapy. Prevention and treatment of postoperative nausea and vomiting.

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Action
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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.

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Adverse Reactions/Side Effects
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CNS: headache, agitation, anxiety, CNS stimulation, drowsiness, weakness. CV: hypertension. GI: constipation, diarrhea, elevated liver enzymes, taste disorder. Derm: application-site reactions, photosensitivity. Misc: anaphylactoid reactions, fever.

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PHYSICAL THERAPY IMPLICATIONS

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Examination and Evaluation
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  • Monitor improvements in GI symptoms (decreased nausea and vomiting, increased appetite) to help document whether drug therapy is successful.

  • Monitor signs of allergic and anaphylactoid reactions, including pulmonary symptoms (tightness in the throat and chest, wheezing, cough, dyspnea) or skin reactions (rash, pruritus, urticaria). Notify physician or nursing staff immediately if these reactions occur.

  • Assess blood pressure (BP) and compare to normal values (See Appendix F). Report a sustained increase in BP (hypertension).

  • Monitor personality changes, including agitation, anxiety, or other signs of CNS excitation. Notify physician if these changes become problematic.

  • If applied transdermally, monitor the application site for local irritation or inflammation. Report excessive application-site reactions to the physician.

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Patient/Client-Related Instruction
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  • Instruct patient to report bothersome side effects such as severe or prolonged headache, drowsiness, weakness, fever, or GI problems (diarrhea, constipation, abnormal taste).

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Pharmacokinetics
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Absorption: 50% absorbed following oral administration.

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

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

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Half-life: Patients with cancer—8–9 hr (range 0.9–31.1 hr); healthy volunteers —4.9 hr (range 0.9–15.2 hr); geriatric patients—7.7 hr (range 2.6–17.7 hr).

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TIME/ACTION PROFILE

ROUTE ONSET PEAK DURATION
PO rapid 60 min 24 hr
IV rapid 30 min up to 24 hr
TD unknown 48 hr unknown

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Contraindications/Precautions
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Contraindicated in: Hypersensitivity; Some products contain benzyl alcohol; avoid use in neonates.

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Use Cautiously in: OB/Lactation: Safety not established; Pedi: Children <2 yr (safe use of IV route not established); Pedi: Children <18 yr (safe use of PO route not established).

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Interactions
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Drug-Drug: ↑ risk of extrapyramidal reactions with other agents causing extrapyramidal reactions.

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Route/Dosage
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Prevention of Nausea and Vomiting Due to Emetogenic Chemotherapy
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PO (Adults): 1 mg twice daily; 1st dose given at least 60 min prior to chemotherapy and 2nd ...

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