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Virology > Antivirals > Flashcards

Antivirals Flashcards

1
Q

What is a mM?

A

millimolar

10^-3

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2
Q

What is a um?

A

micromolar

10^-6

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3
Q

What is a nm?

A

nanomolar

10^-9

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4
Q

What are the 4 properties of a good antiviral?

A
  • good selective index
  • specificity and potency in vitro
  • good therapeutic index
  • good oral bioavailability
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5
Q

What are 4 things pharmacokinetics are affected by?

A

Absorption - how well does the drug get into circulation
Distribution - does it go to the right tissues?
Metabolism - how quickly is it broken down?
Excretion - how quickly is it excreted from the body?

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6
Q

How are new compounds discovered?

A
  • high throughput screening
  • molecular modelling
  • structure/activity relationships
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7
Q

Describe Phase I clinical trials

A

Small no of healthy volunteers (10-50)
Single small dose increasing to higher multiple doses
Looking for adverse effects and pharmacokinetics

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8
Q

Describe Phase II clinical trials

A

Small no of patients (50-100)
IIa - confirm metabolism is the same as healthy volunteers.
IIb - campre with placebo for efficacy. Usually double blinded

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9
Q

Describe Phase III clinical trials

A

Large nos of patients (1000s)
Randomised double-blind trial vs placebo and existing treatments.
Spectrum of therapeutic benefit:risk

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10
Q

Describe Phase IV clinical trials

A

After approval for marketing
Large scaler, broader patient pop
Monitored for long term effectiveness/side effects
Further studies may test the drug in new age groups of patient types and in new formulations.

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11
Q

What are the 4 types of herpesviruses?

A

HSV - cold sores, genital herpes
VZV - chicken pox, shingles
EBV - glandular fever
CMV - asymptomatic in adults but life-threatening to ICs and infants

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12
Q

What did the first antivirals target?

A

DNA replication in herpesvirus

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13
Q

Name 2 nucleoside analogues

A

Thymidine

Idoxuridine

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14
Q

What is an issue with idoxuridine?

A

Idoxuridine triphosphate can also be incorporated into DNA by host cell DNA Pol
Cannot be used as systemic antivirals

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15
Q

What was the first systemic antiviral?

A

Adenosine.

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16
Q

What is an issue with adenosine

A

Lower toxicity

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17
Q

Name 3 guanosine analogues

A

Aciclovir
Ganciclovir
Penciclovir

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18
Q

What are 2 pros of aciclovir?

A

Highly selective

Low toxicity

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19
Q

What is aciclovir effective against?

A

HSV, VZV, EBV but not CMV

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20
Q

What is ganciclovir used to treat?

A

CMV

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21
Q

What is a pro and a con of penciclovir?

A

Less selective than aciclovir/ganciclovir because it can be converted into its triphosphate form by cellular enzymes to.
More stable than aciclovir so persists int he body for longer

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22
Q

Describe the bioavailability of the guanosine analogues

A

Poor by oral uptake (10-20%)

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23
Q

How can the bioavailability of guanosine analogues be improved

A

Given as a valine ester e.g. valaciclovir or a diacetyl ester e.g. famciclovir.

24
Q

What is a prodrug

A

Metabolised in vivo to the active form e.g. valaciclovir or famciclovir

25
Q

What is foscarnet

A

PPi analogue.

26
Q

What is foscarnet active against

A

HSV, VZV, CMV.

Poxviruses, HBV, HIV

27
Q

What is sorivudine

A

Bromide modified uracil

Fatal interaction with anti-cancer drug 5-fluorouracil

28
Q

What is fialuridine

A

Fluorine modified idoxuridine

Phase II trails - delayed toxicity but not toxicity in animal models

29
Q

When can therapy be applied for influenza?

A

Prophylactically

Immediately on onset on symptoms

30
Q

What are the 2 classes of influenza drugs?

A

Adamantines - flu A only

Neuroaminidase inhibitors - flu A and B

31
Q

Give 2 examples of neuroaminidase inhibitors

A

Zanamivir and Oseltamivir

32
Q

What is ribavirin

A

Broad spectrum anti-RNA virus compound
Ribose neucleoside analogue
Used against children with RSV, viral haemorrhagic fevers, flaviviruses

33
Q

What are type I IFNs used to treat?

A

HBV and HCV with ribavirin

34
Q

What was the first anti HIV drug?

A

Zidovudine (AZT)

NRTI

35
Q

Name a next generation NRTI

A

Lamivudine

36
Q

Name a NNRT

A

Nevirapine

37
Q

Where is the HIV protease cleavage site?

A

Between the Phe-Pro.

38
Q

What is the first protease inhibitor?

A

Saquinovir

39
Q

Name 2 protease inhibitors

A

Saquinovir

Ritonavir

40
Q

What is the first integrase inhinitor

A

Raltegravir

41
Q

What is the first entry inhibitor?

A

Enfuvirtide

42
Q

What is a con of Enfuvirtide

A

Very expensive
Difficult regimen, self infection
98% skin reactions

43
Q

Name a fusion/cell entry inhibitor

A

Maraviroc - blocks CCR5

44
Q

Name a maturation inhibitor

A

Bevirimat

45
Q

What is HAART

A

Highly active antiretroviral therapy
2NRTIs + 1NNRTI
2NRTIs + 1PI

46
Q

What does therapy depend on?

A 
Country
Age
T cell count
Viral RNA level
Side effects
47
Q

What are ribozymes?

A

RNA enzymes, designed to bind and cleave viral RNA targets

48
Q

What do ribozymes target in HIV?

A

Tat, Rev, U5 region of HIV RNA

49
Q

What do Antisense RNAs in HIV?

A

Env mRNA, U5 region of HIV RNA

50
Q

What does RNAi target?

A

Tat, Rev, U5 region

51
Q

What do RNA decoys target?

A

TAR and RRE sequester Tat and Rev

52
Q

How can we combat resistance caused by RNA drugs?

A

Knock down levels of cellular proteins - CCR5

Use combination RNA therapy e.g. anti-CCR5 ribozyme, TAR decoy, shRNA against Tat and Rev mRNA

53
Q

Which modified viral proteins can we use to combat HIV?

A

RevM10 - mutant version of Rev that binds RRE in the viral RNA but unable export

54
Q

Which modified cellular proteins can we use to combat HIV?

A

TRIM5a - 1 aa change to this cellular protein prevent HIV infecting the cell.

55
Q

What are ZFNs used against?

A

CCR5 gene

Virology (6 decks)

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