RAPIVAB
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RAPIVAB (RAPIVAB).
Neuraminidase inhibitor; inhibits influenza virus neuraminidase, preventing viral replication and release from infected cells.
| Metabolism | Peramivir is not significantly metabolized; predominantly eliminated unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Primarily renal as unchanged drug via glomerular filtration and tubular secretion; ~70% excreted unchanged in urine over 24 hours, with ~30% undergoing hepatic metabolism via glucuronidation followed by biliary excretion. |
| Half-life | Terminal elimination half-life is approximately 24-30 hours in healthy adults; prolonged in renal impairment (up to 40-60 hours in severe cases), supporting once-daily dosing. |
| Protein binding | ~3% bound to plasma proteins, primarily albumin; extensive free fraction contributes to high tissue penetration. |
| Volume of Distribution | Vd approximately 0.7 L/kg, suggesting distribution into total body water; high volume indicates extensive extravascular tissue penetration including respiratory tract. |
| Bioavailability | Not applicable for IV route; oral bioavailability is <5% due to extensive first-pass metabolism and low oral absorption; administered exclusively as IV infusion. |
| Onset of Action | Intravenous infusion: inhibition of viral neuraminidase activity detectable within 1 hour; peak plasma concentrations achieved at end of infusion. |
| Duration of Action | Duration of antiviral effect extends over dosing interval (~24 hours) due to sufficient plasma concentrations; clinical symptomatic improvement typically observed within 24-48 hours of treatment initiation. |
200 mg IV as a single dose infused over 30 minutes.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for any degree of renal impairment. |
| Liver impairment | No dose adjustment required for any degree of hepatic impairment. |
| Pediatric use | For patients 2 to <12 years: single weight-based IV dose of 12 mg/kg (maximum 200 mg) infused over 30 minutes. For patients ≥12 years: same as adult (200 mg IV single dose). |
| Geriatric use | No specific dose adjustment recommended; safety and efficacy based on limited data, but no age-related pharmacokinetic differences observed. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAPIVAB (RAPIVAB).
| Breastfeeding | Unknown if peramivir is excreted in human breast milk. M/P ratio not available. Caution advised. Consider risk-benefit ratio of influenza treatment versus potential infant exposure. |
| Teratogenic Risk | Pregnancy Category C. In animal studies, no evidence of fetal harm at doses up to 10 times the human exposure. No adequate and well-controlled studies in pregnant women. Should be used during pregnancy only if potential benefit justifies potential risk to fetus. First trimester: limited data, no known teratogenicity. Second and third trimesters: risk of maternal and fetal complications from influenza outweighs theoretical drug risks. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to peramivir or any component of the formulation","Severe renal impairment (CrCl <10 mL/min) or end-stage renal disease requiring hemodialysis (unless benefit outweighs risk)"]
| Precautions | ["Severe skin/hypersensitivity reactions (e.g., Stevens-Johnson syndrome, erythema multiforme) reported","Neuropsychiatric events (delirium, abnormal behavior) reported primarily in pediatric patients, risk of injury; monitor for signs of abnormal behavior","Renal impairment requires dose adjustment; contraindicated in patients with creatinine clearance <10 mL/min or on hemodialysis unless benefit outweighs risk","Bacterial infection may occur with influenza; use only after confirmed influenza or during community outbreak","Efficacy not established in serious illness requiring hospitalization or in immunocompromised patients"] |
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| Fetal Monitoring | Monitor for maternal adverse effects: nausea, vomiting, diarrhea, neutropenia, and hypersensitivity reactions. Fetal monitoring: standard prenatal care; consider ultrasound if maternal influenza severe. |
| Fertility Effects | No data on fertility in humans. Animal studies: no effects on fertility or reproductive performance at doses up to 10 times human exposure. |