Table 2 Main Characteristics of current available antivirals125,126,127,131,132,133,134,138,139,140,141,142,143,144,145,146.

From: Characteristics of human infection with avian influenza viruses and development of new antiviral agents

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*

  1. aNot identified;
  2. bData from independent research different from other neuraminidase inhibitor;
  3. *Mutations have been found to arise naturally drug-resistant in avian influenza;
  4. #Low resistance.