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B&L: Antiviral Drugs by Mind Map: B&L: Antiviral Drugs
0.0 stars - reviews range from 0 to 5

B&L: Antiviral Drugs

Herpes viruses: HSV, zoster, CMV

Most drugs are nucleoside analogs (metabolite is TP)

TP competitively inhibs viral DNA polymerase

Express highly selective toxicity, Initial conversion occurs via VIRAL kinase


MOA, acyclic guanosine analogs, Phosphorylated by viral thymidine kinase, produces TP, which inhibits viral DNA synthesis

Use, HSV-1, HSV-2, VZV, HSV encephalitis (type I herpes), DOC: serious HSV infections!!!, Famici-/valacyclovir: oral forms used to Tx genital herpes and shingles

Side effects, Well tolerated po, IV, Acute renal failure, Nuerotox


MOA, Acyclic guanoside analog

Use, Prv and Tx of CMV, Prv of CMV reactivation in transplant pts

Side effects, Greater tox than Acy- d/t less selectivity, BMD, Additive effect with AZT, Use foscarnet instead!!!, CNS: Headache, behavioral changes, convulsions, coma


MOA, NOT a nucleoside analog (i.e. does not require activation by kinases, Pyrophosphate analog, Blocks pyrophos binding site & inhib cleavage of pyrophos from dNTPs, Inhib viral DNA polymerase

Use, Serious HSV and CMV infections

SE, Renal insufficiency, Hyopcalcemia, Cardiac arrythmias d/t electrolyte imbalance

PK, IV only, Must titrate dose to Cr clearance

Resp. Virus Infections

Neuraminidase inhibitors

Zanamivir & Oseltamivir, Use, Influenza A & B, MOA, Competitive inhibitors of Flu A&B neuraminidases, Prevents the release of progeny from the host cell, Effective against Avain and Swine flu (Flu A H5N1 and H1N1, resp), Zanamivir, PK, Inhalation, Use, Tx only!!!, SE, Bronchospasm, Osetlamivir, PK, Oral prodrug, "O" is for "oral", Use, Prv & Tx!!!, SE, NV, Neuropsychiatric in kids!!!

Viral uncoating inhibitors: Amantadine & Rimantadine

Use, Influenza A, Not effective against Avian and Swine flu, Pre-exposure prophylaxis, Like in a nursing home epidemic

MOA, Prevents uncoating of viral RNA, Inhib viral proton channel M2

PK, Amantadine crosses BBB!!!, Used in Parkinsonism

SE, GI, nausea, anorexia, CNS, nervousness, ADD, insomnia, Elderly more susceptible, Worse with Amantadine

Resp. Syncytial Virus (RSV): Ribavirin

Use, Severe RSV in infants and kids, Hep C, In combo w/ IF-alpha

MOA, Guanosine analog

SE, Inhalation: reversible decline in pulm fn, Oral: Anemia


Hepatic Virus Infections



MOA, Turns on gene expression of proteins w/ antiviral effects

SE, BMD, Flu-like Sx, CNS: depression and suicidal behavior

Use, Hep B (in combo w/ Ribavirin), Hep C

Nucleoside analogs




Always used in combination Tx!!!

Triple combo = 2 nukes + 1 other class

Need to prevent resistance

Compliance is a major issue

Nucleoside analogs ("nukes")

MOA:, Triphophate inhibits HIV reverse transcriptase, selective for virus, Also causes chain termination

Side effects, Lactic acidosis, Hepatic steatosis

PK, Good bioavailability, Renally cleared (mostly)

Lamivudine, Good for pregnancy

Zidovudine (AZT), SE, BMD, anemia, neutropenia, Good for pregnancy, Single dose at birth used to reduce MTCT



NNRTs ("non-nukes")

MOA, Bind directly to HIV-RT

PK, Both undergo hepatic metabolism (CYP3A4), Potent CYP3A4 inducers!, MAJOR D-D interaxns!!!

Efavirenz, Advantages, Potent antiviral activity, Low pill burden, SE, Neuropsychiatric (dl), Teratogenic, PK, Metabolized by p450 - mixed inducer/inhibitor

Nevirapine, Advantage, Safe for pregnancy, SE, Rash, including rare hypersensitivity rxn, Hepatitis, PK, Metabolized by p450 - 3A inducer

Protease Inhibitors

MOA, Competative inhibition of viral protease, Sits in the virus's active site, Prevents immature virions from becoming mature, infections viruses

PK, Eliminated by hepatic metab (CYP3A4), D-D interaxn potential

SE, GI - NVD, Hepatotox, Metabolic, Body fat redistribution, Fat accumulation: abdominal and Buffalo hump, Lipatrophy: face, arms, legs, Hyperlipidemia, Insulin resistance

Ritonavir, use, Mostly used for PI boosting, Causes serious NV at high dose, At low dose (50mg) just inhib CYP3A4 to improve bioavailability of other PI in combo





Fusion inhibitor


Entry inhibitor: CCR5 co-receptor antag


Integrase inhib