Professional Documents
Culture Documents
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
Pharmacokinetics
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
Ganciclovir
1. Needs Viral Thymidine Kinase for its bioactivation with HSV or Needs Phosphotransferase for its bioactivation with CMV 2. Inhibits Viral DNA Polymerase
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
Foscarnet
1. Does not require phosphorylation for anti-viral activity 2. Inhibits Viral DNA Polymerase 3. Inhibits the Viral RNA Polymerase & HIV Reverse Transcriptase
Vidarabine
Fomivirsen
Anti-sense oligonucleotide binds to mRNA of CMV inhibits protein synthesis Mechanism of Action Mechanism of Resistance Pharmacokinetics
Drug
Use
Zidovudine (AZT)
Undergoes glucuronidation
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
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
Zanamivir Oseltamivir
Inhibitors of Neurominidase, produced by influenza virus, the enzyme required for preventing the clumping of virions
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
*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
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
~GI irritation ~Induces CYP 1A2 ~Inhibits CYP3A4 & 2D6 ~Kidney stones ~Diarrhea ~Hyperbilirubinemia