Oseltamivir
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Oseltamivir
Tamiflu
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Summary
Common uses
Influenza A and B treatment (within 48 hours of symptom onset)0, Post-exposure influenza prophylaxis0, Outbreak control in long-term care facilities0
Pharmacy
Starting dose
Treatment: 75 mg PO BID × 5 days (adult); pediatric weight-based; prophylaxis: 75 mg PO once daily × 7-10 days
Preparations
30, 45, 75 mg capsules; 6 mg/mL oral suspension
US FDA Max
150 mg/d (treatment)
Pharmacology
Routes
Oral
Onset
Symptom shortening detectable within 24-48 hours of starting (small absolute benefit; ~1 day reduction in symptom duration)
Duration
12 hours
Half-life
~6-10 hours (oseltamivir carboxylate, the active metabolite)[1]
Bioavailability
~75% (oral, as the active carboxylate after hepatic esterase activation)[1]
Pregnancy
Generally used when influenza treatment is indicated; pregnancy is a recognized risk factor for severe influenza.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Oseltamivir is an ester prodrug activated by hepatic carboxylesterase to oseltamivir carboxylate, a competitive inhibitor of influenza A and B neuraminidase; blocking neuraminidase prevents sialic acid cleavage from host glycoproteins, trapping newly assembled virions on the cell surface and limiting spread to neighboring cells.0 Modest clinical benefit (~1 day faster symptom resolution in healthy adults treated within 48 hours); larger absolute benefit in hospitalized, high-risk, and severely ill patients. Neuropsychiatric events (delirium, abnormal behavior, especially in children) are FDA-labeled adverse effects of uncertain causal contribution[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Tamiflu (oseltamivir phosphate), Genentech, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021087s066lbl.pdf