palonosetron

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.

Contraind./Precautions ⬆ ⬇

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).

Adv. Reactions/Side Effects ⬆ ⬇

GI: constipation, diarrhea

Neuro: dizziness, headache

Interactions ⬆ ⬇

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

Availability ⬆ ⬇

(Generic available)

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

Route/Dosage ⬆ ⬇

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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.

Classifications ⬆ ⬇

Therapeutic Classification: antiemetics

Pharmacologic Classification: five ht3 antagonists

Pharmacokinetics ⬆ ⬇

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.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV	within 30 min	unknown	7 days

Patient/Family Teaching ⬆ ⬇

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.

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Indications ⬇