granisetron

REMS

PO: Prevention of nausea and vomiting due to emetogenic chemotherapy or radiation therapy.
IV: Prevention of nausea and vomiting due to emetogenic chemotherapy.
IV: Prevention and treatment of postoperative nausea and vomiting.
SC: Prevention of acute and delayed nausea and vomiting due to moderately emetogenic chemotherapy or anthracycline/cyclophosphamide combination chemotherapy (in combination with dexamethasone).
Prevention of nausea and vomiting due to moderately/highly emetogenic chemotherapy.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Some products contain benzyl alcohol; avoid use in neonates;
Severe renal impairment (SUBQ).

Use Cautiously in:

History of arrhythmias or conduction disorders;
Recent abdominal surgery (SUBQ);
Moderate renal impairment (↓ frequency of administration);
Lactation: Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children <18 yr (oral, SUBQ, or transdermal) or <2 yr (IV).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, QT interval prolongation

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

Derm: Topicalapplication 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:

↑risk of extrapyramidal reactions with other agents causing extrapyramidal reactions.
↑risk of QT interval prolongation with other agents causing QT interval prolongation.
Drugs that affect serotonergic neurotransmitter systems, including SSRIs, SNRIs, tricyclic antidepressants, MAO inhibitors, fentanyl, lithium, buspirone, tramadol, methylene blue, and triptans↑ risk of serotonin syndrome

Availability ⬆ ⬇

(Generic available)

Tablets: 1 mg
Solution for intravenous injection: 1 mg/mL
Solution for SUBQ injection (prefilled syringes): 10 mg/0.4 mL
Transdermal patch: 3.1 mg/24 hr

Route/Dosage ⬆ ⬇

Prevention of Nausea and Vomiting Due to Emetogenic Chemotherapy

PO (Adults ): 1 mg twice daily; 1st dose given at least 60 min prior to chemotherapy and 2nd dose 12 hr later only on days when chemotherapy is administered; may also be given as 2 mg once daily at least 60 min prior to chemotherapy.
IV (Adults and Children 2–16 yr): 10 mcg/kg given within 30 min prior to chemotherapy or 20–40 mcg/kg/day divided once or twice daily (maximum: 3 mg/dose or 9 mg/day).
Transdermal (Adults ): One patch applied up to 48 hr prior to chemotherapy, leave in place for at least 24 hr following chemotherapy, may be left in place for a total of 7 days.

Prevention of Nausea and Vomiting Associated with Radiation Therapy

PO (Adults ): 2 mg taken once daily within 1 hr of radiation therapy.

Prevention and Treatment of Postoperative Nausea and Vomiting

IV (Adults ): Prevention: 1 mg prior to induction of anesthesia or just prior to reversal of anesthesia; Treatment: 1 mg.
IV (Children ≥4 yr): 20–40 mcg/kg as a single dose (maximum: 1 mg).

Prevention of Acute and Delayed Nausea and Vomiting Due to Emetogenic Chemotherapy

SC (Adults ): 10 mg given at least 30 min prior to chemotherapy (with dexamethasone) on Day 1 of chemotherapy; do not administer more frequently than every 7 days.

Renal Impairment

SC (Adults ): CCr 30–59 mL/min: Do not administer more frequently than every 14 days.

US Brand Names ⬆ ⬇

granisetron: ~~Kytril,~~ Sustol,

granisetron (transdermal): Sancuso

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.

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)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	60 min	24 hr
IV	1–3 min	30 min	up to 24 hr
TD	unknown	48 hr	unknown
SUBQ	unknown	12 hr	7 days

Patient/Family Teaching ⬆ ⬇

Instruct patient to take granisetron as directed.
Advise patient to notify health care professional immediately if involuntary movement of eyes, face, or limbs occurs.
May cause dizziness and drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional if symptoms of abnormal heart rate or rhythm (racing heartbeat, shortness of breath, dizziness, fainting) or serotonin syndrome occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Instruct patient on correct application, removal, and disposal of patch. Advise patient to read Patient Information sheet prior to using and with each Rx refill in case of new information. Inform patient that additional granisetron should not be taken during patch application unless directed by health care professional.
Advise patient referred for MRI test to discuss patch with referring health care professional and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
Advise patient to avoid using a heating pad near or over patch and to cover patch application site with clothing to avoid exposure to sunlight, sunlamp, or tanning beds during and for 10 days following removal of patch.
Instruct patient to notify health care professional if pain or swelling in the abdomen occurs or if redness at patch removal site remains for more than 3 days.

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Indications ⬇