palonosetron

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

REMS

Prevention of acute and delayed nausea and vomiting caused by initial or repeat courses of moderately or highly emetogenic chemotherapy (moderately emetogenic chemotherapy for adults only).
Prevention of postoperative nausea and vomiting for up to 24 hr after surgery.

Blocks the effects of serotonin at receptor sites (selective antagonist) located in vagal nerve terminals and in the chemoreceptor trigger zones in the CNS.

Therapeutic effects:

Decreased incidence and severity of nausea and vomiting following emetogenic chemotherapy or surgery.

Absorption: IV administration results in complete bioavailability.

Distribution: Well distributed to tissues.

Metabolism/Excretion: 50% metabolized by the liver via the CYP1A2, CYP2D6, and CYP3A4 isoenzymes to inactive metabolites; 40% excreted unchanged in urine.

Half-Life: 40 hr.

ROUTE	ONSET	PEAK	DURATION
IV	within 30 min	unknown	7 days

Contraindicated in:

Hypersensitivity; cross sensitivity with other 5-HT₃ antagonists may occur.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Neonates <1 mo (safety and effectiveness not established).

Drug-drug:

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 Chemotherapy-Induced Nausea/Vomiting

IV (Adults ): 0.25 mg given 30 min before start of chemotherapy.
IV (Children 1 mo–<17 yr): 20 mcg/kg (max dose = 1.5 mg) given 30 min before start of chemotherapy.

Prevention of Postoperative Nausea/Vomiting

IV (Adults ): 0.075 mg given immediately before induction of anesthesia.

(Generic available)

Solution for injection: 0.05 mg/mL
In combination with: fosnetupitant (Akynzeo); netupitant (Akynzeo); see Appendix [not included in this PDA edition].

Assess patient for nausea, vomiting, abdominal distention, and bowel sounds prior to and following administration.

Lab Test Considerations:

May cause transient ↑ in serum bilirubin, AST, and ALT levels.

1st dose is administered prior to emetogenic event.
- Repeated dose within a 7-day period is not recommended.

IV Administration:

IV Push: Administer dose undiluted 30 min prior to chemotherapy or immediately prior to the induction of anesthesia. Flush line prior to and after administration with 0.9% NaCl. Do not administer solutions that are discolored or contain particulate matter.
Concentration: 0.05 mg/mL.
Rate: Administer over 30 sec in adults and 15 sec in children 30 min before starting chemotherapy and over 10 sec for postoperative nausea and vomiting.
Y-Site Compatibility:
- alemtuzumab
- amifostine
- amikacin
- aminocaproic acid
- aminophylline
- amiodarone
- amphotericin B liposomal
- ampicillin
- ampicillin/sulbactam
- anidulafungin
- argatroban
- atropine
- azithromycin
- aztreonam
- bivalirudin
- bleomycin
- bumetanide
- buprenorphine
- busulfan
- butorphanol
- calcium acetate
- calcium chloride
- calcium gluconate
- carboplatin
- carmustine
- caspofungin
- cefazolin
- cefepime
- cefotaxime
- cefotetan
- cefoxitin
- ceftazidime
- ceftriaxone
- cefuroxime
- chloramphenicol
- chlorpromazine
- ciprofloxacin
- cisatracurium
- cisplatin
- clindamycin
- cyclophosphamide
- cyclosporine
- cytarabine
- dacarbazine
- dactinomycin
- dantrolene
- daptomycin
- daunorubicin hydrochloride
- dexamethasone
- dexmedetomidine
- dexrazoxane
- digoxin
- diltiazem
- diphenhydramine
- dobutamine
- docetaxel
- dopamine
- doxorubicin hydrochloride
- droperidol
- enalaprilat
- ephedrine
- epinephrine
- epirubicin
- eptifibatide
- erythromycin
- esmolol
- etoposide
- etoposide phosphate
- famotidine
- fentanyl
- fluconazole
- fludarabine
- fluorouracil
- fosaprepitant
- foscarnet
- fosphenytoin
- furosemide
- gemcitabine
- gentamicin
- glycopyrrolate
- haloperidol
- heparin
- hetastarch
- hydralazine
- hydrocortisone
- hydromorphone
- idarubicin
- ifosfamide
- insulin regular
- irinotecan
- isoproterenol
- ketorolac
- labetalol
- LR
- leucovorin calcium
- levofloxacin
- lidocaine
- linezolid
- lorazepam
- magnesium sulfate
- mannitol
- melphalan
- meperidine
- meropenem
- mesna
- methadone
- methotrexate
- metoclopramide
- metoprolol
- metronidazole
- midazolam
- milrinone
- mitomycin
- mitoxantrone
- morphine
- moxifloxacin
- nalbuphine
- naloxone
- neostigmine
- nicardipine
- nitroglycerin
- nitroprusside
- norepinephrine
- octreotide
- oxaliplatin
- oxytocin
- paclitaxel
- paclitaxel protein bound
- pamidronate
- phenobarbital
- phentolamine
- phenylephrine
- piperacillin/tazobactam
- potassium acetate
- potassium chloride
- potassium phosphate
- procainamide
- prochlorperazine
- promethazine
- propofol
- propranolol
- remifentanil
- rocuronium
- sodium acetate
- sodium bicarbonate
- sodium phosphate
- succinylcholine
- sufentanil
- tacrolimus
- theophylline
- thiotepa
- tigecycline
- tirofiban
- tobramycin
- topotecan
- trimethoprim/sulfamethoxazole
- vancomycin
- vasopressin
- vecuronium
- verapamil
- vinblastine
- vincristine
- vinorelbine
- zidovudine
Y-Site Incompatibility:
- acyclovir
- allopurinol
- amphotericin B deoxycholate
- diazepam
- doxycycline
- ganciclovir
- gemtuzumab ozogamicin
- imipenem/cilastatin
- methylprednisolone
- minocycline
- nafcillin
- pantoprazole
- pentamidine
- pentobarbital
- phenytoin
- thiopental

Inform patient of purpose of medication.
Advise patient to notify health care professional if nausea or vomiting occur.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy or surgery.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆