Pharmacology of Antiviral Drugs Flashcards
What are the viral cell attachment inhibitors?
Palivizumab
Maraviroc
Enfuvirtide
Docosanol
What are the viral Penetration inhibitors?
Interferons
What are the viral nucleic acid uncoating inhibitors?
Amantadine
Rimantadine
What are the 3 groups of transcription inhibitors?
Nucleoside/nucleotide reverse transcriptase inhibitors
Non-nucleotide/nucleoside reverse transcriptase inhibitors
Viral DNA polymerase inhibitors
What are the nucleoside/nucleotide reverse transcriptase inhibitors?
Zidovudine
What are the non-nucleoside/nucleotide reverse transcriptase inhibitors?
Efavirenz
What are the viral DNA polymerase inhibitors?
Ganciclovir
Acyclovir
What are the protease inhibitors?
Saquinavir
What are the viral release inhibitors?
Oseltamivir
Zanamivir
What is Enfuvirtide specific for?
HIV-1
How is Enfuvirtide metabolized?
Proteolytic hydrolysis
What is Enfuvirtide saved for?
Salvage therapy in HIV-1
How does Enfuvirtide work?
Inhibits HIV binding to CD4 cells
What is Maraviroc used to treat?
HIV
How does Maraviroc work?
Specifically binds host cell cytokine receptor (CCR5) needed for HIV entry into the cell
How is Maraviroc metabolized?
P450 CYP3A4 metabolism and renal excretion
How is Maraviroc transported out of the GI tract?
G glycoprotein substrate
What is Docosanol used to treat?
Herpes simplex
What type of compound is Docosanol?
A 22 carbon aliphatic alcohol
How does Docosanol work?
Inhibits fusion between plasma membrane and herpes simplex virus envelope preventing viral entrance into the cell
Maraviroc main adverse effects?
Cough, upper respiratory infections, muscle-joint pain
What is Palivizumab used to treat?
Respiratory syncytial virus
How does Palivizumab work?
Monoclonal antibody directed against a surface protein antigen on RSV
Adverse effects of Palivizumab?
Elevated liver transaminases
What is Palivizumab really?
A monoclonal antibody injected prophylactically
What population would you use Palivizumab?
Premature babies and infants at high risk
What are the three chemically different forms of interferons produced by human cells?
Type I
Type II
Interferon receptors
What cells produce type I interferons?
Leukocytes
Fibroblasts
What cells produce type II interferons?
T cells
NK cells
What are type I interferons produced in response to?
Viral stimulation
What are type II interferons produced in response to?
Immune stimuli and associated cytokines
What family are interferon receptors a part of?
JAK-STAT group of tyrosine kinase receptors
Mechanism of interferon action?
Binds to IFN type I receptor
Initiating JAK-STAT phosphorylation
STAT goes to nucleus host DNA reducing mRNA transcription needed for viral replication complex
What are the interferon alpha drugs?
Interferon alfa-2a
Interferon alfa-2b
What are the interferon beta drugs?
Interferon beta-1a
Interferon beta-1b
What are the type I interferons?
Alpha Beta Delta Epsilon Kappa Tau Omega
What are the type II interferons?
Gamma
What do viral uncoating inhibitors affect?
Influenza A viral RNA in hosts cells
How is Rimantadine metabolized?
Cleared by hydroxylation and conjugation
How is Amantadine metabolized?
Glomerular filtration
What is the net effect of transcription inhibitors?
Reduced viral replication
DNA polymerase inhibitors metabolism?
Renal clearance GFR dependent
Effect of non-nucleoside reverse transcription inhibitors on metabolism?
P450 inducers or inhibitors
What do protease inhibitors do?
Prevent post-translational cleavage of precursors inhibiting formation of the mature virus
Adverse affects of protease inhibitors?
CYP3A4 metabolism major drug interactions
Buffalo hump
Shrunken face
Pot belly
What do viral release inhibitors inhibit?
Neuraminidase
Mechanism of viral release inhibitors?
Particles cling to sialic acid receptors of active neuraminidase enzyme sites
What do viral release inhibitors cause by clinging to sialic acid receptors?
Failure to cleave sialic acid residues leaves completed virus clinging to the host cell or each other
What are neuraminidase inhibitors good for use against?
Influenza A
Influenza B
How are neuraminidase inhibitors excreted?
Active metabolites found in urine so reduce does in renal failure
What does neuramidase do?
Cleaves sialic acid receptors from the virus allowing the virus to go free