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Pharm Block 12 > Antivirals > Flashcards

Antivirals Flashcards

(72 cards)

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1
Q

“Avir”

A

AIDS

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2
Q

“Ovir”

A

Herpes

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3
Q

“Ivir”

A

Influenza

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4
Q

Why a kind of virus is herpes

A

DNA

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5
Q

What kind of drugs treat DNA viruses?

A

“Ovir”

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6
Q

What kind of virus is influenza

A

RNA

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7
Q

What kind of drug treats an RNA virus

A

“Ivir”

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8
Q

What kind of virus if HIV

A

Retrovirus

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9
Q

What kind of drugs treat retroviruses

A

“Avir”

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10
Q

Clinical presentation of HIV

A

High viral load and persistent decrease in CD4 lymphocytes

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11
Q

Drugs used for HIV

A
  • reverse transcriptase inhibitors: NRTIs, NtRTIs, NNRTIs
  • protease inhibitors
  • fusion inhibitors
  • integrate inhibitors
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12
Q

What are the main enzymes involved in the HIV virus

A

Reverse transcriptase
Protease
Integrase

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13
Q

What kind of HIV drugs stop entry into the cell?

A

Fusion inhibitors

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14
Q

What do reverse transcriptase inhibitors do

A

Stop DNA

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15
Q

What do proteases do in HIV

A

Matures virus to infect other cells

-use protease inhibitors

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16
Q

What do protease inhibitors do in HIV treatment

A

Prevents virus from maturing and infecting other cells

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17
Q

What does integrase do in HIV

A

Integrates genetic material into host DNA

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18
Q

What do integrase inhibitors do in treating HIV

A

Prevent the virus from integrating genetic material into host DNA

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19
Q

Nucleoside

A

DNA + sugar

-not active, no phosphates

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20
Q

Nucleotides

A

DNA base + sugar +3 phosphates

-active

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21
Q

How can a nucleoside become active

A

Get 3 phosphates attached to it and become a nucleotide

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22
Q

What are the nucleoside reverse transcriptase inhibitors (NRTIs) used for HIV

A

Zidovudine
Lamivudine
Emtrictabine

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23
Q

MOA of NRTIs

A
  • host enzyme activates the drug by adding on 3 phosphates to the drug (host kinases)
  • 5’-triphosphate-DRUG terminates DNA elongation, competes with natural deoxynucleotides for reverse transcriptase
  • competitive inhibitor, looks like DNA but just inhibits it
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24
Q

How do NRTIs differ from thymidine

A

They lack the 3’ hydroxyl

  • cant elongate with this
  • chain termination of DNA
  • looks like nucleotide in body, but stops chain because no 3’ hydroxyl
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25
Adverse effects of NRTIs
Bone marrow suppression: AZT (zidovudine) - could make you sicker because more immunosuppression - lower risk today because of combination therapy allowing a lower dose of this drug
26
What are considered the least toxic NRTIs
Lamivudine and emtricitabine
27
How do you use NRTIs
Always in combination, use two at a time - cant do laivruline and emtrictabine together because Rhett both look like cystine and will compete with each other - have to use one of those with zidovudine
28
What is the nucleotide reverse transcriptase inhibitors used for HIV (NtRTI)
Tenofovir (TDF) | -there’s an O in there but it does not treat herpes!
29
MOA of NtRTIs (tenofovir (TDF))
Has a single phosphate on its sugar residue and must be further phosphorylated to the active form tenofovir triphosphate Drug with a single phosphate that needs two more Prodrugs
30
How is tenofovir Rxed
With emtricitabine
31
What are the non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Efavirenz
32
MOA of NNRTIs (efavirenz)
Bind to reverse transcriptase at a site below the catalytic site (allosteric inhibition) Does NOT require phosphorylation to become active
33
Which HIV drugs need phosphorylated?
NRTIs | NtRTIs
34
Which HIV drugs do not need phosphorylated
NNRTIs
35
Adverse effects of NNRTIs (efavirenz)
CNS effects (vivid dreams)
36
What is the protease inhibitor used to treat HIV
Ritonavir
37
MOA of ritonavir
Protease cleansed viral precursor proteins; critical for producing mature infectious visions, inhibits this
38
Adverse effects of protease inhibitors (ritonavir)
Central adiposity and insulin resistance | -hyperglycemia
39
Is ritonavir a P450 inhibitor or inducer
Inhibitor
40
Why is ritonavir (a P450 inhibitor) frequently given together with other PIs?
Because it boosts other PIs - give other PI at low dose because plasma levels will be increased due to ritonavir - used with lopinavir usually
41
Fusion inhibitors in HIV treatment (enfuvirtide)
- enfuvirtide | - blocks gp41 protein on T cell surface to prevent viral entry
42
What are the fusion inhibitors to treat HIV
Enfuvirtide | Maraviroc
43
Maraviroc, fusion inhibitor in HIV treatment
Blocks CCR5 protein on macrophage (or T cell) surface to prevent viral entry
44
Integrase inhibitor in treating HIV
Raltegravir -inhibits the HIV enzyme integrase; this enzyme integrates the viral genetic material into human chromosomes “Avir”=HIV “Teg”=integrase
45
What is the best way to treat HIV
``` Combination therapy -2 NRTIS with one of the following: —1-2 PIs —and NNRTI —raltegravir ```
46
How is post exposure prophylaxis treated in HIV
The same way as it regularly is
47
Evaluating therapeutic outcomes of HIV
Check CD4 Decreased CD4=risk of opportunistic infections
48
What is PrEP in HIV
Pre-exposure prophylaxis -used for people who do not have HIV but are high risk or exposure through sex or IV dirt use -combination of tenofovir and emtricitabine
49
HSV-1
Cold sores
50
HSV-2
Genital herpes
51
Herpes zoster
Shingles
52
What is herpes zoster (shingles) caused by
Herpesvirus varicella-zoster, same virus that causes chickenpox - reactivation of citrus causes shingles - pain in one dermatome
53
What are the anti herpes drugs we talk about
Acyclovir Cidofovir Ganciclovir Foscarnet
54
MOA of acyclovir
Prodrug - nucleoside that needs 3 phosphates - herpes donates a phosphate to it and then human enzymes donate two phosphates to it - competitive inhibitor of DNA polymerase
55
Adverse effects of acyclovir
Well tolerated, fe side effects
56
What enzyme puts a phosphate onto the acyclovir drug
Thymidine kinase | -this from the viral genome phosphorylated acyclovir over a hundred times faster than host cell enzyme
57
Resistance of acyclovir
Downregulate the enzyme TK
58
Why cant you use acyclovir on TK- strains of herpes
Because it needs TK to add a phosphate to it to activate it. If there isn’t any TK, it wont activate
59
Which herpes medication can be used in TK- strains and works by getting phosphorylated by host kinases
Cidofovir
60
Ganciclovir and herpes
Used like acyclovir but used for CMV retinitis; bone marrow suppression is major toxicity
61
What herpes medication can be used to CMV retinitis?
Ganciclovir
62
What is the side effect of ganciclovir
Bone marrow suppression | -“gangs” up on bone marrow
63
MOA of foscarnet
- Herpes - not prodrug - selectively inhibits the pyrophosphate binding site on virus-specific DNA polymerases and reverse transcriptase - works on TK- strains
64
What are the two herpes drugs that can work on TK- strains of herpes
Foscarnet and cidofovir
65
Spectrum of foscarnet
CMV retinitis
66
What drugs can treat CMV retinitis
Ganciclovir and foscarnet
67
Adverse effects of foscarnet
Nephrotoxicity
68
What two viruses cause influenza in humans
Influenza A and B | -hemagglutinin and neuraminidase on surface
69
Main types of influenza in the past 3 decades
H3N2 and H1N1
70
Drugs to treat influenza
Oseltamivir
71
MOA of oseltamivir
-block neuraminidases thereby inhibiting the budding and release of virus from the cells
72
Antiviral spectrum of oseltamivir
Influenza A and B prophyalxis and treatment

Pharm Block 12 (7 decks)

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