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Flashcards in Antiviral Drugs Deck (72)
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1

The most severe constraint limiting the use of antiviral drugs?

not the lack of efficacy but the toxicity to the mammalian cell (poor selective toxicity)

2

Virus specific enzymes

proteases, mRNA capping enzyme, neuraminidases, ribonucleases, kinases, integrases and uncoating enzymes

3

In the case of antivirals, the therapeutic window is

the ratio of the minimum dose that is toxic to host cells over the minimum dose that is toxic to the virus

4

What is required to maintain the suppression of many viral infections

an intact immune system (because antiviral drugs available so far are virostatic)

5

Three subclasses of drugs that prevent viral entry into host cells

1. inhibitors of attachment that compete with a viral receptor
2. coreceptor antagonists
3. fusion inhibitors that prevent fusion with host cells

6

Maraviroc

CCR5 coreceptor antagonist - tested for AIDS treatment

7

what kind of patients should maraviroc be used in

CCR5-tropic patients (M-tropic)

8

When should maraviroc dose be adjusted

if used with drugs that inhibit or stimulate cytochrome P450 CYPA3 enzyme to adjust for changes in its metabolism

9

cenicriviroc

dual CCR5 and CCR2 antagonist

10

PRO 140

a CCR5 monoclonal antibody
for treatment experienced patients

11

Enfuvirtide (T-20)

fusion inhibitor
derived from the natural gp41 HR2 sequence
first HIV fusion inhibitor acting by specifically inhibiting the function of the gp41 transmembrane glycoprotein of HIV-1

12

Virus uncoating corresponds to

loss of viral protein coat (nucleocapsid proteins in nonenveloped viruses) or fusion of viral lipid memebranes (loss of lipid envelope in membrane containing viruses) with an endosome/lysosome

13

good target for therapy by interfering with pH?

endosome/lysosome compartment

14

Arildone

inhibits uncoating of picornaviruses that do not have a lipid membrane by blocking ion transport; drug inserts into a canyon in the VP1 viral proteins and blocks ion transport

15

What happens when you inhibit viral integrase?

prevent the insertion of the virus genetic code into the DNA of infected cells

16

Integrase inhibitors

Raltegravir (1st one)
elvitegravir, dolutegravir ect.

17

targets of drugs that act on the duplication of the viral genome

polymerases

18

nucleoside analog drugs

idoxuridine, cytarabine, vidarabine, ribavirin, acyclovir, ganciclovir, azidothimidine

19

Drugs that act on polyadenylation, methylation, capping, and splicing of viral RNA

ribavirin, interferon

20

Ribavirin inhibits

replication of DNA and RNA viruses including influenza A and B, RSV, hepatitis C, HIV

21

Ribozymes are

RNA molecules that induce specifically the cleavage of nucleic acids

22

Nonspecific drug that inhibits protein translation

interferon

23

What does neuraminidase or sialidase do?

helps spread the influenza virus from cell to cell by removing sialic acid from the surface of infected cells so that viral particles may escape

24

zanamivir is a potent inhibitor of

viral neuraminidase of type A and B influenza viruses

25

zanamivir acts as

a sialic acid analog inhibitor
highly specific for influenza viral neuraminidase and has little activity against mammalian/bacterial neuraminidases

26

Zanamivir requires

aerosol delivery to the respiratory tract

27

Oseltamivir

carbocyclic sialic acid analogue

28

Examples of drugs that interfere with the assembly of the molecular components into the whole virus

protease inhibitors

29

Examples of protease inhibitors

aquinavir, ritonavir, indinavir, nelfinavir, amprenavir, lopinavir, atazanavir, fosamprenavir, tipranavir, darunavir, asunaprevir

30

Amantadine inhibits

uncoating of the viral RNA of influenza A
may act on the maturation stage of the virus in the trans-golfi network
acts on the maturation of influenza HA glycoprotein