Table 2. Main Characteristics of current available antivirals125,126,127,131,132,133,134,138,139,140,141,142,143,144,145,146.
Characteristics | Amantadine | Rimantadine | Oseltamivir | Zanamivir | Laninamivir | Peramivir |
---|---|---|---|---|---|---|
Molecular weight | 187.7 | 215.8 | 312.4 (free base) | 332.3 | 472.53 | 328.4 |
Prophylaxis dosing (Adult) | 100 mg bid | 100 mg bid | 75 mg qd | 10 mg qd | –a | –a |
Treatment dosing (Adult) | 100 mg bid | 100 mg bid | 75 mg bid for 5 d | 10 mg bid for 5 d | 40 mg single dose | 600 mg qd for 5–10 d |
Route | Oral | Oral | Oral | Inhaled | Inhaled | Parenteral |
Half-life (h) | 12–18 | 24–36 | 6–10 | 4.14–5.05 | >240 | 12–25 |
Use status and major adverse reactions | Pregnancy class C drugs, neuropsychiatric reactions | Pregnancy class C drugs, neuropsychiatric reactions | Few major adverse effect, nausea, vomiting and transient neuropsychiatric reactions | Few major adverse effect, nausea, cough, and fatal bronchospasm (patients with underlying pulmonary disease) | Few major adverse effect, nausea, vomiting, and dizziness | Few major adverse effect, diarrhea, nausea, vomiting and decreased neutrophil count |
Inhibitory activity on Avian influenza | EC50 to AIV: H5N3: 0.1 μmol/L H7N2: 0.1 μmol/L H9N2: 0.5 μmol/L (plaque assay) | IC50s of NA activity (N1–N9): 1.4–3.6 nmol/L; EC50 to AIV (N1–N9): 1.0–42.0 μmol/L (ELISA); 0.1–0.9 nmol/L (plaque assay) | IC50s of NA activity (N1–N9): 1.4–11.5 nmol/L; EC50 to AIV (N1–N9): 4.0–58.3 μmol/L (ELISA); 0.6–3.6 nmol/L (plaque assay) | IC50s of NA activity (N1–N9): 1.8–27.9 nmol/L; EC50 to AIV (N1–N9): 0.3–2.5 nmol/L (plaque assay) | IC50s of NA activity (N1–N9): 0.9–4.3 nmol/L; EC50 to AIV (N1–N9): 0.5–11.8 μmol/L (ELISA) | |
Reported mutations confer to drug resistance | M2: L26F, V27A*, V27D*, V27T, V27S, I27T*, I27S*, I27A*, A30E*, A30T, A30P*, A30V, A30G, S31N*, G34E*, W41A; HA: G23C | H275Y*, N295S*,#; N2 NA: E119V*, D151E#, R224K, E276D#, R292K*, N294S*,#, R371K; N9 NA: H274Y, R292K | N1 NA: I223R*; N2 NA: E119A, E119D, R224K, R292K*,#, R371K, E276D, N9 NA: E119G | N1 NA: N295S | N1 NA: H275Y*, N295S*; N2 NA: E119V, R292K* |
aNot identified;
bData from independent research different from other neuraminidase inhibitor;
*Mutations have been found to arise naturally drug-resistant in avian influenza;
#Low resistance.