Anti-Viral Agents pt. 2 Flashcards
Drugs act as Reverse Transcriptase Inhibitors (8)
Zidovudine, Didanosine, Zalcitabine,Stavudine, Abacavir, Tenofovir disoproxil, lamivudine, emtricitabine
A prodrug analog with Abacavir and synergistic with RT inhibitors for HIV adult patients.
Tenofovir disoproxil
Orally active nucleoside reverse-transcriptase inhibitor
Emtricitabine
The triphosphate form of this drug is a nucleoside reverse transcriptase inhibitor in combination therapy for HIV and AIDS.
Abacavir
This drug has antiretroviral activity against HIV and low toxicity.
Lamivudine
Lamivudine together with Azidothymidine increases CD4 count.
T or F
True
Close congener of AZT, thymidine nucleoside analog
Stavudine
What is the dose-limiting effect of Stavudine
peripheral neuropathy
MOA of Stavudine
Triphosphate form competitively inhibits incorporation of thymidine triphosphate into retroviral DNA
Known as the former Azidothymidine and used against HIV 1 and 2
Zidovudine
MOA of Zidovudine
Triphosphate form competitively inhibits reverse transcriptase, causes DNA chain termination – yielding incomplete proviral DNA
RTI that is active against HIV 1, 2, and AZT resistant forms.
Zalcitabine
Zalcitabine works by the inhibition of the enzyme __________ caused by ____________ which causes termination of viral DNA chain elongation.
Reverse transcriptase
Dideoxycytidine triphosphate (ddCTP)
A purine nucleoside analog and is 10-100 fold less potent that Azidothymidine but less myelosupression.
Didanosine
Didanosine is also used as a treatment for AIDS patients with intolerance to AZT.
T or F
True
Didanosine and Zalcitabine inhibits the both enzymes.
T or F
True
Drug acts as Miscellaneous Nucleoside Antimetabolites
Ribavirin
Ribavirin is known to inhibit RNA and DNA viruses replication.
T or F
True
Drugs known as Non-Nucleoside Reverse Transcriptase Inhibitors
Nevirapine
Delavirdine
Efavirenz
- Non-Nucleoside Reverse Transcriptase Inhibitors have specific activity against HSV-1.
- The rapid emergence of resistance prohibits multitherapy with any of the NNRTIs and the NRTIs or the protease inhibitors.
a. First statement is correct.
b. Second statement is correct.
c. Both of the statements are correct.
d. Both of the statements are incorrect.
a. First statement is correct.
1. Non-Nucleoside Reverse Transcriptase Inhibitors have specific activity against HSV-1.
2. The rapid emergence of resistance prohibits MONOTHERAPY with any of the NNRTIs and the NRTIs or the protease inhibitors.
Delavirdine binds directly to a site on the viral reverse transcriptase that is near to but distinct from the binding site of the NRTIs (Allosteric Site)
T or F
True
Drugs that inhibit non-nucleoside reverse transcriptase compete with nucleoside triphosphate but require phosphorylation to be active.
T or F
False
These drugs neither compete with nucleoside triphosphate nor require phosphorylation to be active
Arrests replication of the virus at the maturation step to prevent spread of cellular infection.
HIV Protease Inhibitory Drugs
Drugs that inhibit HIV Protease
Tipranavir Fosamprenavir Atazanavir Indinavir Lopinavir Nelfinavir Amprenavir Ritonavir Saquinavir
Used against HSV-1 and HSV-2 and against varicella-zoster virus, Epstein-Barr Virus and Cytomegalovirus
Acyclovir
Approved for combination w/ Ritonavir
Lopinavir