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Granisetron Hydrochloride

Pronouncation: (gran-IH-SEH-trahn)
Class: 5-HT ₃ receptor antagonist

Trade Names:
Kytril
- Injection 1 mg/mL
- Tablets 1 mg

Pharmacology

Feedback for Granisetron HCl

As a treatment for...	Avg User Ratings [?]
Nausea/Vomiting -- Chemotherapy Induced	0 comments Rate it!	10
Nausea/Vomiting -- Postoperative	Be the first to rate it 0 comments
Nausea/Vomiting -- Radiation Induced	Be the first to rate it 0 comments

Compare with other drugs.

Selective 5-HT ₃ receptor antagonists. 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. Clearance is predominantly by hepatic metabolism, and plasma protein binding is approximately 65%.

Pharmacokinetics

Absorption

Mean C _max is 64 ng/mL.

Distribution

Vd is about 3 L/kg. Protein binding is 65%.

Elimination

Mean t _{1/ 2} is 5 h. Mean Cl is 0.79ߙL/h/kg.

Peak

5 to 30 sec (injection).

Special Populations

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.

Indications and Usage

Adults

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.

Contraindications

Standard considerations.

Dosage and Administration

Chemotherapy-Induced Nausea and Vomiting
Adults

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.

Chemotherapy-Induced Nausea and Vomiting
Adults

PO 1 mg twice daily. Give the first oral dose up to 1 h before chemotherapy and the second dose 12ߙh later. Give granisetron only on day(s) of chemotherapy. Alternately, a single 2 mg dose may be given up to 1 h before chemotherapy.

Children

IV 10 mcg/kg, given up to 30 min before starting chemotherapy. Give only on day(s) of chemotherapy.

Radiation-Induced Nausea and Vomiting
Adults

PO 2 mg once daily. Give the dose up to 1 h before radiation therapy. Give granisetron only on day(s) of radiation therapy.

Prevention/Treatment Postoperative Nausea and Vomiting
Adults

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.

Drug Interactions

CYP-450 enzymes

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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension; hypotension.

CNS

Headache; somnolence; agitation; anxiety; mood changes; insomnia.

Dermatologic

Rash.

GI

Constipation; diarrhea; elevated AST and ALT; decreased appetite.

Musculoskeletal

Asthenia.

Miscellaneous

Fever; taste disorder; shivers; alopecia.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy of the injection in children younger than 2 yr of age not established.

Delayed nausea and vomiting

Granisetron is not consistently effective for treating delayed nausea and vomiting.

Patient Information

Advise patient, family, or caregiver that IV medication will be prepared and administered by health care professional in a medical facility.
Review dosing schedule with patient. Caution patient taking oral medication that tablets or solution must be taken no more than 1 h before chemotherapy administration or radiation therapy to provide greatest protection against nausea and vomiting.
Advise patient that medication will greatly reduce likelihood of nausea or vomiting but these are still possible.
Instruct patient to inform health care provider if medication does not prevent nausea or vomiting.
Advise patient to report any of the following to their health care provider: intolerable headache; persistent or intolerable constipation or diarrhea; persistent weakness.