Trade Names:Kytril- Injection 1 mg/mL- Tablets 1 mg
Trade Names:Sancuso- Transdermal 3.1 mg per 24 h (34.3 mg per 52 cm 2 )
Serotonin receptors of the 5-HT 3 type are located peripherally on vagal nerve terminals, enteric neurons in the GI tract, and centrally in the chemoreceptor trigger zone. During chemotherapy, mucosal enterochromaffin cells from the small intestine release serotonin, which stimulates the 5-HT 3 receptors. This evokes vagal afferent discharge, inducing vomiting.
Mean C max is 64 ng/mL.Transdermal
T max is 48 h. C max is 5 ng/mL. Mean AUC 0-168h is 527 ng•h/mL.
Vd is about 3 L/kg. Protein binding is 65%.
Involves N-demethylation and aromatic ring oxidation followed by conjugation.
Mean t 1/ 2 is 5 h. Mean Cl is 0.79 L/h/kg. Cl is predominately by hepatic metabolism.IV
Approximately 12% is excreted unchanged in the urine; the rest is excreted as metabolites, 49% in urine and 34% in feces.
5 to 30 sec (injection).
Cl not affected in patients with severe renal failure.Hepatic Function Impairment
Total Cl decreased by about 50%.Elderly
Mean C max is 57 ng/mL. Mean t 1/ 2 is 7.69 h. Mean Cl is 0.44 L/h/kg. Mean Vd is about 4 L/kg.Cancer patients
C max is 84 ng/mL. Mean t 1/ 2 is 9 h. Cl is 0.38 L/h/kg.
Prevention of chemotherapy-induced nausea and vomiting; prevention of radiation-induced nausea and vomiting (oral only); postoperative nausea and vomiting (injection only).Children (2 to 16 yr of age)
Prevention of chemotherapy-induced nausea and vomiting (injection only). Safety and efficacy not established in patients younger than 2 yr of age.
IV 10 mcg/kg (commonly rounded to nearest 1 mg), given up to 30 min before starting chemotherapy. Give only on day(s) of chemotherapy.Adults
PO 1 mg twice daily. Give the first oral dose up to 1 h before chemotherapy and the second dose 12 h later. Give granisetron only on day(s) of chemotherapy. Alternately, a single 2 mg dose may be given up to 1 h before chemotherapy.Adults
Transdermal 1 patch to the upper outer arm a minimum of 24 h before chemotherapy; may be applied up to a max of 48 h before chemotherapy, as appropriate. Remove the patch a minimum of 24 h after completion of chemotherapy. The patch can be worn for up to 7 days, depending on the duration of the chemotherapy regimen.Children
IV 10 mcg/kg, given up to 30 min before starting chemotherapy. Give only on day(s) of chemotherapy.Prevention/Treatment Postoperative Nausea and VomitingAdults
IV For prevention, use 1 mg, undiluted, administered over 30 seconds, before induction of anesthesia or immediately before reversal of anesthesia. For treatment, use 1 mg, undiluted, administered over 30 seconds, after surgery.Radiation-Induced Nausea and VomitingAdults
PO 2 mg once daily. Give the dose up to 1 h before radiation therapy. Give granisetron only on day(s) of radiation therapy.
Store transdermal patch at 59° to 86°F.
Granisetron does not induce or inhibit the CYP-450 system; however, it is metabolized partially by CYP-450 3A enzymes. Medications that induce or inhibit CYP-450 3A isoenzymes may alter granisetron metabolism.
None well documented.
Angina pectoris, atrial fibrillation, hypertension, hypotension, syncope.
Headache (3%); agitation, anxiety, asthenia, dizziness, mood changes, insomnia, somnolence.
Constipation (5%); abnormal pain, decreased appetite, diarrhea, elevated AST and ALT, nausea, vomiting.
Alopecia, fever, hypersensitivity reactions (eg, anaphylaxis, shortness of breath, urticaria), shivers, taste disorder.
Category B .
Safety and efficacy of the injection in children younger than 2 yr of age not established. Safety and efficacy of the transdermal patch in children younger than 18 yr of age not established.
Granisetron is not consistently effective for treating delayed nausea and vomiting.
May mask a progressive ileus and/or gastric distention.
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