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Antivirals Flashcards

(55 cards)

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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

Study These Flashcards
A

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

24
Q

What is a prodrug

Study These Flashcards
A

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

25
What is foscarnet
PPi analogue.
26
What is foscarnet active against
HSV, VZV, CMV. | Poxviruses, HBV, HIV
27
What is sorivudine
Bromide modified uracil | Fatal interaction with anti-cancer drug 5-fluorouracil
28
What is fialuridine
Fluorine modified idoxuridine | Phase II trails - delayed toxicity but not toxicity in animal models
29
When can therapy be applied for influenza?
Prophylactically | Immediately on onset on symptoms
30
What are the 2 classes of influenza drugs?
Adamantines - flu A only | Neuroaminidase inhibitors - flu A and B
31
Give 2 examples of neuroaminidase inhibitors
Zanamivir and Oseltamivir
32
What is ribavirin
Broad spectrum anti-RNA virus compound Ribose neucleoside analogue Used against children with RSV, viral haemorrhagic fevers, flaviviruses
33
What are type I IFNs used to treat?
HBV and HCV with ribavirin
34
What was the first anti HIV drug?
Zidovudine (AZT) | NRTI
35
Name a next generation NRTI
Lamivudine
36
Name a NNRT
Nevirapine
37
Where is the HIV protease cleavage site?
Between the Phe-Pro.
38
What is the first protease inhibitor?
Saquinovir
39
Name 2 protease inhibitors
Saquinovir | Ritonavir
40
What is the first integrase inhinitor
Raltegravir
41
What is the first entry inhibitor?
Enfuvirtide
42
What is a con of Enfuvirtide
Very expensive Difficult regimen, self infection 98% skin reactions
43
Name a fusion/cell entry inhibitor
Maraviroc - blocks CCR5
44
Name a maturation inhibitor
Bevirimat
45
What is HAART
Highly active antiretroviral therapy 2NRTIs + 1NNRTI 2NRTIs + 1PI
46
What does therapy depend on?
``` Country Age T cell count Viral RNA level Side effects ```
47
What are ribozymes?
RNA enzymes, designed to bind and cleave viral RNA targets
48
What do ribozymes target in HIV?
Tat, Rev, U5 region of HIV RNA
49
What do Antisense RNAs in HIV?
Env mRNA, U5 region of HIV RNA
50
What does RNAi target?
Tat, Rev, U5 region
51
What do RNA decoys target?
TAR and RRE sequester Tat and Rev
52
How can we combat resistance caused by RNA drugs?
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
Which modified viral proteins can we use to combat HIV?
RevM10 - mutant version of Rev that binds RRE in the viral RNA but unable export
54
Which modified cellular proteins can we use to combat HIV?
TRIM5a - 1 aa change to this cellular protein prevent HIV infecting the cell.
55
What are ZFNs used against?
CCR5 gene

Virology (6 decks)

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