Drug Acyclovir

Mechanism of Action 1. Needs Viral Thymidine Kinase for its bioactivation 2. Inhibits Viral DNA Polymerase

Mechanism of Resistance 1. Lack of Viral Thymidine Kinase 2. Changes in the Viral DNA Polymerase


Use *Herpes Simplex (HSV) *Varicella Zoster *Genital herpes *Herpes simplex keratitis *Herpes simplex encephalitis (IV) *Chickenpox *CMV *HSV *VZV *Prophylaxis & treatment of CMV infections (Retinitis) in AIDs patients and transplant recipients


1. Needs Viral Thymidine Kinase for its bioactivation with HSV or Needs Phosphotransferase for its bioactivation with CMV 2. Inhibits Viral DNA Polymerase

Famciclovir Cidofovir Anti-Herpes

1. Its phosphorylation to active form inside the cell is independent of viral enzymes 2. Inhibits Viral DNA Polymerase

*Inhibits HSV, CMV, Adenovirus, Papilloma virus *CMV retinitis *Genital warts


1. Does not require phosphorylation for anti-viral activity 2. Inhibits Viral DNA Polymerase 3. Inhibits the Viral RNA Polymerase & HIV Reverse Transcriptase

*CMV retinitis *Acyclovir resistant strains of HSV



Anti-sense oligonucleotide binds to mRNA of CMV inhibits protein synthesis Mechanism of Action Mechanism of Resistance Pharmacokinetics

Injected intravitreally in CMV retinitis

Category Anti-Retroviral (HIV)



Zidovudine (AZT)

Inhibits Reverse Transciptase

Interrupts DNA chain elongation

Undergoes glucuronidation

*Prophylaxis following needlestick injury *Used to prevent vertical transmission

Stavudine (D4T) Nucleoside Reverse Transciptase Inhibitors (NRTI) Common to all: ~Lactic acidosis Didanosine (ddl)

Lamivudine Zalcitabine (ddC) Non-Nucleoside Nevirapine Delaviridine Reverse Efavirenz Transciptase Inhibitors (NNRTI) Common to all: ~Not myelosuppreant Protease Inhibitors Saquinavir Ritonavir

Directly binds to site on HIV-1 reverse transcriptase and inhibits it

*Used synergistically with NRTI and/or PI in HAART *Prevents vertical transmission

Common to all: ~CYP inhibitors Indinavir ~Hyperglycemia due to insulin resistance ~Hyperlipidemia ~Lipodystrophy

~Protease inhibitors ~Inhibit HIV Protease results in the production of immature, non-infectious viral particles

Specific point mutation in Pol gene (Pol gene, normally is responsible for viral assembly)

due to insulin resistance Nelfinavir ~Hyperlipidemia ~Lipodystrophy Fusion Inhibitor Enfuvirtide Binds to gp41 and inhibits the fusion of viral and cellular membranes Mechanism of Action Inhibits the 1st step in replication of Influenza A ex. Viral uncoating Mechanism of Resistance Pharmacokinetics Use in combination with other anti-virals on patients failing treatment Use ~Influenza A ONLY! ~Parkinson's Disease

Category Anti-Influenza

Drug Amantadine Rimantadine

Zanamivir Oseltamivir

Inhibitors of Neurominidase, produced by influenza virus, the enzyme required for preventing the clumping of virions

~Both Influenza A & B

Anti-Hepatitis B Interferon alpha Activate a host cell ribonuclease which preferentially degrades viral mRNA *Hepatitis B (alone or with Lamivudine ) *Hepatitis C (with Ribavarin ) *Kaposi's Sarcoma *Papilomatosis *Genital warts

Adefovir Lamivudine Ribavarin

Triphosphate form inhibits viral RNA polymerase

*Respiratory Synctitial Virus infections *Influenza A & B *Lassa virus *Chronic Hepatitis C

Adverse Effects

~Bone marrow suppression ~Hematoxicity - Leukopenia, Thrombocytopenia ~Mucositis ~Crystalluria ~Seizures in overdose


~Nephrotoxicity ~Acute tubular necrosis ~Electrolyte imbalance ~Hypocalcemia

Adverse Effects

~Bone marrow suppresion anemia, leukopenia, thrombocytopenia ~Myopathy ~Peripheral neuropathy ~Peripheral neuropathy ~Avoid Stavudine + Zidovudine because they both compete for the same kinases ~Pancreatitis ~Peripheral neuropathy ~Avoid Didanosine + Zalcitabine because of additive toxicity

~Stevens Johnson Syndrome ~CNS dysfunction

~GI irritation ~Induces CYP 1A2 ~Inhibits CYP3A4 & 2D6 ~Kidney stones ~Diarrhea ~Hyperbilirubinemia

~Diarrhea ~Both CYP inducer and inhibitor

Adverse Effects *Atropine like peripheral side effects *Livedo reticularis

~GI irritation ~Flu like syndrome

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