granisetron

gra-NI-se-tron

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

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).
Transdermal: Prevention of nausea and vomiting due to moderately/highly emetogenic chemotherapy.

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.

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.

(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

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).

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).

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

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.

(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;

Assess patient for nausea, vomiting, abdominal distention, and bowel sounds prior to and following administration.
Assess for extrapyramidal symptoms (involuntary movements, facial grimacing, rigidity, shuffling walk, trembling of hands) during therapy. This occurs rarely and is usually associated with concurrent use of other drugs known to cause this effect.
Monitor ECG in patients with HF, bradycardia, underlying heart disease, renal impairment, and elderly patients.
Monitor for signs and symptoms of serotonin syndrome (mental status changes [agitation, hallucinations, delirium, and coma], autonomic instability [tachycardia, labile BP, dizziness, diaphoresis, flushing, hyperthermia], neuromuscular symptoms [tremor, rigidity, myoclonus, hyperreflexia, incoordination], seizures, with or without gastrointestinal symptoms [nausea, vomiting, diarrhea]). If symptoms occur discontinue granisetron and treat symptomatically.
Transdermal: Monitor application site. If allergic, erythematous, macular, or papular rash or pruritus occurs, remove patch.

Lab Test Considerations:

May cause ↑ AST and ALT levels.

Correct hypokalemia and hypomagnesemia before administering.
For chemotherapy or radiation, granisetron is administered only on the day(s) chemotherapy or radiation is given. Continued treatment when not on chemotherapy or radiation therapy has not been found to be useful.
PO: Administer 1st dose up to 1 hr before chemotherapy or radiation therapy and 2nd dose 12 hr after the first.
SC: Use kit and components provided by manufacturer. Injection should be administered by health care professional. Remove kit from refrigerator and allow to warm to room temperature for 60 min. Activate one syringe warming pouch, and wrap syringe in warming pouch for 5 to 6 min to warm to body temperature. Do not inject solutions that contain particulate matter. Inject in back of upper arm or in skin of abdomen at least 1 inch away from umbilicus. Avoid injecting in areas where skin is burned, hardened, inflamed, or swollen. Topical anesthesia may be used at injection site prior to injection. Solution is viscous and requires a slow, sustained injection over 20 to 30 sec. Pressing the plunger harder will NOT expel medication faster.

IV Administration:

IV Push:
Rate: Administer undiluted granisetron over 30 sec or as a diluted solution over 5 min.
Y-Site Compatibility:
- acetaminophen
- alemtuzumab
- allopurinol
- amifostine
- amikacin
- aminocaproic acid
- aminophylline
- amiodarone
- amphotericin B lipid complex
- amphotericin B liposomal
- ampicillin
- ampicillin/sulbactam
- anidulafungin
- argatroban
- arsenic trioxide
- atracurium
- azithromycin
- aztreonam
- bivalirudin
- bleomycin
- bumetanide
- buprenorphine
- busulfan
- butorphanol
- calcium acetate
- calcium chloride
- calcium gluconate
- carboplatin
- carmustine
- caspofungin
- cefazolin
- cefepime
- cefotaxime
- cefotetan
- cefoxitin
- ceftaroline
- ceftazidime
- ceftriaxone
- cefuroxime
- chloramphenicol
- chlorpromazine
- ciprofloxacin
- cisatracurium
- cisplatin
- cladribine
- clindamycin
- cyclophosphamide
- cyclosporine
- cytarabine
- dacarbazine
- dactinomycin
- daptomycin
- daunorubicin hydrochloride
- dexamethasone
- dexmedetomidine
- dexrazoxane
- digoxin
- diltiazem
- diphenhydramine
- dobutamine
- docetaxel
- dopamine
- doxorubicin hydrochloride
- doxorubicin liposomal
- doxycycline
- droperidol
- enalaprilat
- ephedrine
- epinephrine
- epirubicin
- eptifibatide
- ertapenem
- erythromycin
- esmolol
- etoposide
- etoposide phosphate
- famotidine
- fentanyl
- filgrastim
- floxuridine
- fluconazole
- fludarabine
- fluorouracil
- fosaprepitant
- foscarnet
- fosphenytoin
- furosemide
- ganciclovir
- gemcitabine
- gentamicin
- glycopyrrolate
- haloperidol
- heparin
- hetastarch
- hydralazine
- hydrocortisone
- hydromorphone
- idarubicin
- ifosfamide
- imipenem/cilastatin
- insulin, regular
- irinotecan
- isoproterenol
- ketorolac
- labetalol
- leucovorin calcium
- levofloxacin
- lidocaine
- linezolid
- lorazepam
- magnesium sulfate
- mannitol
- melphalan
- meperidine
- meropenem
- mesna
- methotrexate
- methylprednisolone
- metoclopramide
- metoprolol
- metronidazole
- midazolam
- milrinone
- mitomycin
- mitoxantrone
- morphine
- moxifloxacin
- mycophenolate
- nafcillin
- nalbuphine
- naloxone
- nicardipine
- nitroglycerin
- nitroprusside
- norepinephrine
- octreotide
- oxaliplatin
- oxytocin
- paclitaxel
- pamidronate
- pantoprazole
- pemetrexed
- pentamidine
- pentobarbital
- phenobarbital
- phentolamine
- phenylephrine
- piperacillin/tazobactam
- potassium acetate
- potassium chloride
- potassium phosphate
- procainamide
- prochlorperazine
- promethazine
- propofol
- propranolol
- remifentanil
- rituximab
- rocuronium
- sargramostim
- sodium acetate
- sodium bicarbonate
- sodium phosphate
- succinylcholine
- sufentanil
- tacrolimus
- theophylline
- thiopental
- thiotepa
- tigecycline
- tirofiban
- tobramycin
- topotecan
- trastuzumab
- trimethoprim/sulfamethoxazole
- vancomycin
- vasopressin
- vecuronium
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voriconazole
- zidovudine
- zoledronic acid
Y-Site Incompatibility:
- amphotericin B deoxycholate
- dantrolene
- diazepam
- gemtuzumab ozogamicin
- phenytoin
Transdermal: Apply system to clear, dry, intact healthy skin on upper outer arm 24–48 hr before chemotherapy. Do not use creams, lotions, or oils that may keep patch from sticking. Do not apply to skin that is red, irritated, or damaged. Apply immediately after removing from package. Do not cut patch into pieces. Remove liner from adhesive layer and press firmly in place with palm of hand for 30 sec, especially around the edges, to make sure contact is complete. Patch should be worn throughout chemotherapy. If patch does not stick, bandages or medical adhesive tape may be applied on edges of patch; do not cover patch with tape or bandages or wrap completely around arm. Patient may shower and wash normally while wearing patch; avoid swimming, strenuous exercise, sauna, or whirlpool during patch use. Remove patch gently at least 24 hr after completion of chemotherapy; may be worn for up to 7 days. Fold so that adhesive edges are together. Throw away in garbage out of reach of children and pets. Do not reuse patch. Use soap and water to remove remaining adhesive; do not use alcohol or acetone.

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.
Transdermal: 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.

Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy or radiation therapy.
Prevention and treatment of postoperative nausea and vomiting.

~~Kytril~~, Sustol

granisetron (Transdermal): Sancuso

NDC Code^*

0054- West-Ward Pharmaceuticals Corp.
0054-0143- Granisetron Hydrochloride 0054-0143-07- 20 TABLET in 1 BOTTLE (0054-0143-07)

0054- West-Ward Pharmaceuticals Corp.
0054-0143- Granisetron Hydrochloride 0054-0143-08- 10 BLISTER PACK in 1 CARTON (0054-0143-08) > 2 TABLET in 1 BLISTER PACK

0054- West-Ward Pharmaceuticals Corp.
0054-0143- Granisetron Hydrochloride 0054-0143-87- 2 TABLET in 1 BOTTLE (0054-0143-87)

0143- West-Ward Pharmaceuticals Corp
0143-9744- Granisetron Hydrochloride 0143-9744-10- 10 VIAL, SINGLE-USE in 1 PACKAGE (0143-9744-10) > 1 mL in 1 VIAL, SINGLE-USE (0143-9744-01)

0143- West-Ward Pharmaceuticals Corp
0143-9745- Granisetron Hydrochloride 0143-9745-05- 5 VIAL, MULTI-DOSE in 1 CARTON (0143-9745-05) > 4 mL in 1 VIAL, MULTI-DOSE (0143-9745-01)

0143- West-Ward Pharmaceuticals Corp
0143-9745- Granisetron Hydrochloride 0143-9745-10- 10 VIAL, MULTI-DOSE in 1 CARTON (0143-9745-10) > 4 mL in 1 VIAL, MULTI-DOSE (0143-9745-01)

16714- Northstar Rx LLC
16714-221- Granisetron Hydrochloride 16714-221-01- 20 TABLET, FILM COATED in 1 BOTTLE (16714-221-01)

16714- Northstar Rx LLC
16714-221- Granisetron Hydrochloride 16714-221-30- 2 BLISTER PACK in 1 CARTON (16714-221-30) > 1 TABLET, FILM COATED in 1 BLISTER PACK (16714-221-10)

16714- Northstar Rx LLC
16714-221- Granisetron Hydrochloride 16714-221-32- 2 BLISTER PACK in 1 CARTON (16714-221-32) > 10 TABLET, FILM COATED in 1 BLISTER PACK (16714-221-12)

17478- Akorn, Inc.
17478-546- Granisetron Hydrochloride 17478-546-02- 1 VIAL, SINGLE-DOSE in 1 CARTON (17478-546-02) > 1 mL in 1 VIAL, SINGLE-DOSE

17478- Akorn, Inc.
17478-546- Granisetron Hydrochloride 17478-546-05- 1 VIAL, MULTI-DOSE in 1 CARTON (17478-546-05) > 4 mL in 1 VIAL, MULTI-DOSE

17478- Akorn, Inc.
17478-547- Granisetron Hydrochloride 17478-547-01- 10 VIAL, SINGLE-DOSE in 1 CARTON (17478-547-01) > 1 mL in 1 VIAL, SINGLE-DOSE

42043- OrchidPharma Inc
42043-390- Granisetron Hydrochloride 42043-390-02- 2 BLISTER PACK in 1 CARTON (42043-390-02) > 1 TABLET, FILM COATED in 1 BLISTER PACK (42043-390-00)

42043- OrchidPharma Inc
42043-390- Granisetron Hydrochloride 42043-390-20- 20 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (42043-390-20)

42043- OrchidPharma Inc
42043-390- Granisetron Hydrochloride 42043-390-21- 2 BLISTER PACK in 1 CARTON (42043-390-21) > 10 TABLET, FILM COATED in 1 BLISTER PACK (42043-390-40)

42747- Kyowa Kirin, Inc.
42747-726- Sancuso 42747-726-01- 1 POUCH in 1 CARTON (42747-726-01) > 1 PATCH in 1 POUCH > 168 h in 1 PATCH

47426- Heron Therapeutics
47426-101- SUSTOL 47426-101-06- 6 KIT in 1 CARTON (47426-101-06) > 1 SYRINGE, GLASS in 1 KIT >.4 mL in 1 SYRINGE, GLASS

51672- Taro Pharmaceuticals U.S.A., Inc.
51672-4138- Granisetron Hydrochloride 51672-4138-0- 100 BLISTER PACK in 1 CARTON (51672-4138-0) > 1 TABLET, FILM COATED in 1 BLISTER PACK

51672- Taro Pharmaceuticals U.S.A., Inc.
51672-4138- Granisetron Hydrochloride 51672-4138-1- 100 TABLET, FILM COATED in 1 BOTTLE (51672-4138-1)

51672- Taro Pharmaceuticals U.S.A., Inc.
51672-4138- Granisetron Hydrochloride 51672-4138-6- 20 TABLET, FILM COATED in 1 BOTTLE (51672-4138-6)

51991- Breckenridge Pharmaceutical, Inc.
51991-735- Granisetron Hydrochloride 51991-735-20- 2 BLISTER PACK in 1 CARTON (51991-735-20) > 10 TABLET in 1 BLISTER PACK

51991- Breckenridge Pharmaceutical, Inc.
51991-735- Granisetron Hydrochloride 51991-735-32- 1 BLISTER PACK in 1 CARTON (51991-735-32) > 2 TABLET in 1 BLISTER PACK

55150- AuroMedics Pharma LLC
55150-175- Granisetron Hydrochloride 55150-175-01- 1 VIAL, SINGLE-USE in 1 CARTON (55150-175-01) > 1 mL in 1 VIAL, SINGLE-USE

55150- AuroMedics Pharma LLC
55150-176- Granisetron Hydrochloride 55150-176-04- 1 VIAL, MULTI-DOSE in 1 CARTON (55150-176-04) > 4 mL in 1 VIAL, MULTI-DOSE

63323- Fresenius Kabi USA, LLC
63323-318- Granisetron 63323-318-01- 1 VIAL, SINGLE-USE in 1 BOX (63323-318-01) > 1 mL in 1 VIAL, SINGLE-USE

63323- Fresenius Kabi USA, LLC
63323-319- Granisetron 63323-319-04- 1 VIAL in 1 BOX (63323-319-04) > 4 mL in 1 VIAL

63850- Natco Pharma Limited
63850-0005- Granisetron hydrochloride 63850-0005-1- 10 TABLET, FILM COATED in 1 BLISTER PACK (63850-0005-1)

63850- Natco Pharma Limited
63850-0005- Granisetron hydrochloride 63850-0005-2- 2 TABLET, FILM COATED in 1 BLISTER PACK (63850-0005-2)

64679- Wockhardt USA LLC.
64679-661- GRANISETRON HYDROCHLORIDE 64679-661-02- 1 VIAL, MULTI-DOSE in 1 CARTON (64679-661-02) > 4 mL in 1 VIAL, MULTI-DOSE

64679- Wockhardt USA LLC.
64679-661- GRANISETRON HYDROCHLORIDE 64679-661-01- 5 VIAL, SINGLE-USE in 1 CARTON (64679-661-01) > 1 mL in 1 VIAL, SINGLE-USE (64679-661-04)

64679- Wockhardt USA LLC.
64679-661- GRANISETRON HYDROCHLORIDE 64679-661-03- 1 VIAL, SINGLE-USE in 1 CARTON (64679-661-03) > 1 mL in 1 VIAL, SINGLE-USE (64679-661-04)

64679- Wockhardt USA LLC.
64679-662- GRANISETRON HYDROCHLORIDE 64679-662-01- 5 VIAL, SINGLE-USE in 1 CARTON (64679-662-01) > 1 mL in 1 VIAL, SINGLE-USE (64679-662-03)

64679- Wockhardt USA LLC.
64679-662- GRANISETRON HYDROCHLORIDE 64679-662-02- 1 VIAL, SINGLE-USE in 1 CARTON (64679-662-02) > 1 mL in 1 VIAL, SINGLE-USE (64679-662-03)

66758- Sandoz Inc.
66758-035- Granisetron 66758-035-01- 1 VIAL, SINGLE-USE in 1 CARTON (66758-035-01) > 1 mL in 1 VIAL, SINGLE-USE

66758- Sandoz Inc.
66758-036- Granisetron 66758-036-01- 1 VIAL, MULTI-DOSE in 1 CARTON (66758-036-01) > 4 mL in 1 VIAL, MULTI-DOSE

67457- Mylan Institutional LLC
67457-863- Granisetron Hydrochloride 67457-863-01- 1 VIAL in 1 CARTON (67457-863-01) > 1 mL in 1 VIAL

67457- Mylan Institutional LLC
67457-864- Granisetron Hydrochloride 67457-864-04- 1 VIAL in 1 CARTON (67457-864-04) > 1 mL in 1 VIAL

69097- Cipla USA Inc.
69097-195- GRANISETRON HYDROCHLORIDE 69097-195-67- 1 mL in 1 VIAL, SINGLE-DOSE (69097-195-67)

69097- Cipla USA Inc.
69097-195- GRANISETRON HYDROCHLORIDE 69097-195-68- 5 VIAL in 1 CARTON (69097-195-68) > 1 mL in 1 VIAL

69097- Cipla USA Inc.
69097-196- GRANISETRON HYDROCHLORIDE 69097-196-67- 1 mL in 1 VIAL, SINGLE-USE (69097-196-67)

69097- Cipla USA Inc.
69097-197- GRANISETRON HYDROCHLORIDE 69097-197-67- 4 mL in 1 VIAL, MULTI-DOSE (69097-197-67)

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