ANTIVIRAL DRUGS

Class Drug PK MOA Clinical Uses

Nucleoside Acyclovir • synthetic guanosine (nucleoside) • Inhibition of viral genome • HSV-1 and 2, varicella zoster
Analogue Gancyclovir analogues replication (DNA/RNA polymerase virus, CMV
Valacyclovir • Acy inhibitor • Acy - Labialis & Genital
Penciclovir • oral (poor availability), IV if • Undergo intracellular phosphorylation Herpes, Herpes zoster
Famciclovir required, topical to the active triphosphate moiety and (shingles)
Cidovir • Gan inhibit viral DNA polymerase by • Gan – CMV infections,
• i.v. admin , (oral is poor), newer competing with endogenous retinitis
slow release formulation can be nucleotides (dGTP, dCTP)
inserted in vitreous humour • All interfere with DNA replication
• Useful in immuno-compromised after incorporation into elongating
patients chain terminating nucleotide chain
S/E
• Acy - quite safe, temporary
kidney dysfunction at high doses
• Gan - neutropenia

Ribavirin • Guanosine analogue • blocks synthesis of dGTP, inhibits Treatment of viral respiratory
Trivabirin S/E viral RNA polymerase i.e. interferes infections
• Contraindicated in pregnancy with viral mRNA synthesis • Effective against a broad
(teratogenic) spectrum of viruses (DNA &
• Anaemia RNA)
• Especially useful for
respiratory syncytial virus
(RSV) infection in children
• Influenza A & B, hepatitis C
(with interferon)
• Effective orally and also used
as an aerosol
Tricylic Amantadine • Resistance: mutation in M2 • Inhibitor of viral uncoating Treatment of viral respiratory
Amines Rimantadine transmembrane protein • blocks viral H+ ion-channel (M2 infections
• Well absorbed orally transmembrane protein) • Influenza A & B –
S/E • prevents acidification of virus (vaccination is preferable)
• Amantadine - can enter CNS containing vesicles • Virtually all H1N1 strains are
(dose-dependent) - dizziness, • prevents uncoating resistant
insomnia, tremors. Possibly • Effective for treatment, if
teratogenic? (avoid in started within 48h of infection,
pregnancy) and for
• prevention in unvaccinated
individuals
Prodrug Oseltamivir • prodrug – requires activation in • Inhibitor of viral release Treatment of viral respiratory