baloxavir

REMS

Treatment of acute uncomplicated influenza in patients who have been symptomatic for ≤48 hr and who are otherwise healthy or at high risk of developing influenza-related complications.
Postexposure prophylaxis of influenza following contact with an individual who has influenza.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Children <5 yr (↑ risk of treatment-emergent resistance).

Adv. Reactions/Side Effects ⬆ ⬇

EENT: nasopharyngitis

GI: diarrhea, nausea

Neuro: headache

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Medications containing divalent or trivalent cations, including calcium, iron, magnesium, selenium, or zinc, may ↓ absorption of baloxavir; avoid concurrent use.
May ↓ the therapeutic effect of the live-attenuated influenza vaccine.

Drug-Food:

Calcium in foods or dairy products may ↓ absorption of baloxavir; avoid concurrent administration.

Availability ⬆ ⬇

Oral suspensionstrawberry flavor: 2 mg/mL
Tablets: 40 mg; 80 mg

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥5 yr and ≥80 kg): 80 mg as a single dose (as tablets or oral suspension).
PO (Adults and Children ≥5 yr and 20–<80 kg): 40 mg as a single dose (as tablets or oral suspension).
PO (Adults and Children ≥5 yr and <20 kg): 2 mg/kg as a single dose (as oral suspension).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits the endonuclease activity of the polymerase acidic protein in the viral RNA polymerase complex that is required for viral gene transcription, thereby resulting in inhibition of influenza virus replication.

Therapeutic effects:

Reduced duration of flu-related symptoms.

Classifications ⬆ ⬇

Therapeutic Classification: antivirals

Pharmacologic Classification: endonuclease inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Administered as a prodrug (baloxavir marboxil), which is rapidly absorbed from the GI tract and converted by the liver to the active form, baloxavir.

Distribution: Extensively distributed to tissues.

Protein Binding: 93–94%.

Metabolism/Excretion: Rapidly metabolized by the liver by UGT1A3 to baloxavir, the active metabolite. Primarily excreted in feces (80%); 15% excreted in urine (3% as active metabolite).

Half-Life: 79 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	4 hr	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take baloxavir as directed. Advise patient to read Patient Information before taking baloxavir.
Advise patient to notify health care professional immediately if signs and symptoms of hypersensitivity reactions (rash; hives; difficulty breathing; swelling of lips, face, and throat) occur.
Advise patient to consult health care professional before receiving a live-attenuated influenza vaccine after taking baloxavir.
Advise patient that baloxavir is not a substitute for a flu shot. Patients should receive annual flu shot according to immunization guidelines.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any new medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Pregnant women are at higher risk of severe complications from influenza, which may lead to adverse pregnancy and/or fetal outcomes, including maternal death, stillbirth, birth defects, preterm delivery, low birth weight, and small for gestational age.

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Indications ⬇