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Antiviral Drugs
See title
22
Medical
Professional
01/22/2012

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Cards

Term
Maraviroc
Definition
Prevents binding to CCR5, a host membrane protein

Attachment/Early Inhibition (anti-HIV)
Term
Enfurvitide
Definition
Similar to viral protein gp41, prevents fusion. Exact mechanism unknown.

Attachment/Early Inhibition (anti-HIV)
Term
Amantadine
Definition
1st generation, also blocks host ion channels, leading to unwanted side effects. Also used as a treatment for Parkinson’s.

Uncoating Inhibition (Anti-influenza A)
Adamantanes – M2 ion channel inhibitors. Resistance to both is common and develops rapidly
Term
Rimantadine
Definition
Newer, fewer side effects, can be used prophylactically

Uncoating Inhibition (Anti-influenza A)
Adamantanes – M2 ion channel inhibitors. Resistance to both is common and develops rapidly
Term
Acycolovir
Definition
Used against HSV and VZV. Guanine base attached to broken sugar ring. Inhibits at two viral enzymes – thymidine kinase and herpesvirus DNA pol. Slight toxicity (human cells can also phosphorylate). Valcyclovir is prodrug form.

Viral Replication Inhibition
Term
Penciclovir
Definition
Similar to Acyclovir, but a better inhibitor of TK and worse inhibitor of DNA pol. Famciclovir is oral form.

Viral Replication Inhibition
Term
Ganciclovir
Definition
Used against CMV. Very toxic, only use for serious infections. Similar to acyclovir, but TK does not phosphorylate (carried out by a different viral enzyme unique to CMV). Valganciclovir is oral prodrug.

Viral Replication Inhibition
Term
Herpesviruses [includes herpes simplex virus 1 (HSV), cytomegalovirus (CMV), and varicella zoster virus (VZV)]

These are latent viruses - antiviral works on actively replicating virus, not in latency.
Definition
Term
Cidofovir
Definition
Does not require phosphorylation; effective against kinase-deficient mutants. dCTP analogue. Toxic, used in CMV retinf itis.

NucleoTide analogues
Term
Zidovudine (AZT)

Nucleoside/nucleotide analogue (used in combination therapy for HIV)
Definition
Thymine analogue, obligatory chain terminator. Requires phosphorylation for activation, which is carried out by human kinase. Accumulation of phosphorylated form accounts for toxicity (bone marrow suppression). Inhibits viral RT.
Term
Lamivudine (3TC)

Nucleoside/nucleotide analogue (used in combination therapy for HIV)
Definition
Similar to AZT, but less toxic due to increased specificity. Also effective against HBV (targets HBV pol). Emtricitabine (FTC) similar.
Term
Foscarnet (PFA)




Nonnucleoside DNA polymerase inhibitors
Definition
Does not require phosphorylation, inhibits DNA pol directly. Also effective against HSV and CMV (second-line). Poor oral bioavailability.
Term
Efavirnez, Nevirapine, Delavirdine, Etravine

Nonnucleoside Reverse Transcriptase Inhibitors
Definition
Directly inhibit viral RT. Good oral bioavailability but resistance develops rapidly.
Term
Raltegravir


Integrase Inhibitors
Definition
inhibits integration of HIV into host genome. Only for use in combination therapy.
Term
Inhibition of Viral Maturation
Definition
HIV Protease Inhibitors – Ritonavir most common (long list, see book). Contains Phe-Pro analogue (mimics active site of HIV protease, not a target of human enzymes) and is a suicide inhibitor. Results in viral particles that bud from the cell, but do not mature and are non-infectious. Major side effects are changes in fat distribution and metabolic abnormalities.
Term
Inhibition of Viral Release
Definition
Block influenza (A and B) neuraminidase. Reduce duration of symptoms – use controversial for seasonal flu but good effectiveness against H5N1 (avian flu).
Zanamivir – inhalational route, resistance develops rapidly
Oseltamivir – Good oral bioavailability
Term
Fomivirsen
Definition
Anti-CMV. Antisense oligonucleotide designed to irreversibly bind to mRNA of viral IE2 regulatory protein.
Term
Docosanol
Definition
22-carbon saturated alcohol, effective against enveloped viruses (particularly HSV). Topical (cold sore treatment).
Term
Ribavirin
Definition
“Broad spectrum antiviral” but only approved for inhalation in RSV treatment and with interferon for hepatitis C virus (HCV). Quasi-nucleoside analogue (sugar attached to non-natural base). Lowering of cellular GTP levels thought to be main mechanism of action, but viral RNA pol inhibition also possible.
Term
Vaccination



(Immune system modulation)
Definition
Active and Passive. Rabies vaccine used therapeutically.
Term
Interferon-α


(Immune System Modulation)
Definition
Used to treat HCV, HBV, HPV infection, Kaposi Sarcoma virus (KSV, HHV8) lesions
Term
Imiquimod


(Immune System Modulation)
Definition
Interacts with TLR7 and TLR8 to boost innate immunity. Used to treat HPV-related disease.
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