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AIDS drugs Flashcards

1
Q

Zidovudine is what type of drug

A

NRTI

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2
Q

Zidovudine mechanism

A

thymidine nucleoside analogue that is phosp by cellular kinase to active form ( tri-Ps)
inhibits reverse transcriptase
early terminator for DNA

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3
Q

Side effects of Zidovudine

A

Bone marrow suppression
avoid drugs that inhibit glycuronyl transferase
myopathy

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4
Q

thymidine nucleoside analogue that is phosp by cellular kinase to active form ( tri-Ps)
inhibits reverse transcriptase
early terminator for DNA

A

Zidovudine

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5
Q

Drugs that inhibit glucuronidation of AZT will increase:

A

hematologic toxicity of AZT~~ more drugs head down path that creates toxic amines leading to bone marrow suppresion

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6
Q

Mech of Lamivudine

A

Nucleoside analog inhibitor of reverse transcriptase; must be phosphorylated

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7
Q

Use of Lamivudine

A

synergistic with AZT of Zidovudine

Lambs are docile adn get along well with others

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8
Q

Side effect of Lamivudine

A

nauseua and diarhhea

you ate Lamb and it gave you these but IG this is a dociel nice drug and works well with others

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9
Q

General mech of NRTIs

A

Nucleoside analogues that need to be phosphrotyalted to be active
competitive inhibitors of RT
Cause DNA chain termination when incorporated into DNA

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10
Q

Tenofovir is a

A

NRTI, WELL tolerated

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11
Q

Tenofovir is like AZT because

A

inhibits RT by competing with dATP for incorporation into DNA, resulting in chain termination

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12
Q

Tenofovir unlike AZT because

A

nucleotide prodrug that is hydrolyzed to tenofovir phosphonate; further phosphorylated

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13
Q

NRTI prodrug

A

Tenofovir

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14
Q

fluorinated analog of 3TC that inhibits RT by competing for dCTP incorporation
into DNA, resulting in chain termination

A

Emtricitabine

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15
Q

Emtricitabine

A

flourinated analog of 3TC (lamivudine)

inhibits RT by competing dCTP incorporation~ early chain termination

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16
Q

Emtricitabine inhibts RT by competing _____ incorporation

A

dCTP

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17
Q

Tenofovir inhibits RT by competing with _______ for incorporation into DNA

A

dATP

“a Ten out of Ten gets an ‘A” for dATP”

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18
Q

Emtricitabine has simular mechanism and resistance as 3TC but a ______ 1/2 life

A

longer

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19
Q

This NRTI has some activity against Hep B

A 
EMtricitabine
EM was FLOORED when she TRIed to get rid of Hep B but couldn't so she got a "C"
(for dCTP)
(FLOORED for flourinated of 3TC)
EM and TRied for emtricitabine
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20
Q

Emtricitabine uses:

A

NRTI combo therapy drug

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21
Q

Abacavir

A

NRTI: nucleoside analog inhibitor of RT and phosphorylated by cell enZ to active drug

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22
Q

Adverse effect of Abacavir (NRTI)

A

Hypersensitity in those with 5701 HLA-B allele

you’re BAC’s A itching

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23
Q

Other sides associtaed with NRTIs

A

Lactic acidosis and hepatic steatosis

24
Q

NNRTIs are

A

non-nucleoside inhibitors of RT:

Efavirenz

25
NNRTIz are all
active as given and don't need to be P'd to be activated
26
Five covered NRTIs
``` Zidovudine Abacavir Lamivudine Tenofovir Emtricitabine ```
27
Mech of Efavirenz
non-nucleoside inhibitor of reverse transcriptase; does not require phosphorylation for activity
28
Efavirenz
F this virion; bad ass, doesn't need phosphorylation for activity to inhibit RT...it a non-nucleoside inhibitor because it doesn't want to be liek the other NRTIs
29
Sides of Efavirenz
rash and CNS~~ have nightmares
30
#1 HIV drug in US
Efavirenz
31
Key protease inhibitors for HIV
Lopinavir and Ritonavir
32
Use of Apartic protease inhibitos
In combo with RT inihbitors for HIV 1 and 2 to decrease viral load
33
what can be used with RT inhibitors for HIV 1 and 2 to decrease viral load
Protease inhibitors like Lopinavir and Ritonavir
34
Which protease inhibitor is used more as a PI booster and not as a PI itself
Ritonavir
35
Which protease inhibitor is used specifically as protease inhibitor
Lopinavir
36
Prevents viral protease from cleaving Gag-pol polypeptide into separate functional proteins. Fits into protease active site and acts as competitive inhibitor. - Results in non-infectious viral particles.
Protease inhibitors | bahahaha... HIV has giant gagpol and these guys stop it from being split up into function virions!!
37
Common toxicities of lopinavir
nasty combo of Cushings and weird fat stuff : diabetes :alters lipid metabolism fat redistribution :alters metab of other drugs by inhibiting CYP3A4
38
Diabetes, alters lipid metabolism, fat redistribution, alters met of other drugs (CYP3A)
Toxicity caused by Lopinavir
39
Used a protease inhibitor to stop breakdown of gag-pol to infectious virions
Lopinavir | got a LOW chance of making those virions!
40
Boosts lopinavir levels by blocking the metabolism of lopinavir by CYP3A
Ritonavir
41
inhibits the fusion of viral (HIV-1) and cellular (CD4+) membranes - binds to gp41 subunit of HIV glycoprotein, blocking conformational changes required for membrane fusion
Enfuvirtide
42
Enfuvirtide mech
stops fusion of HIV-1 and cellular CD4+ membranes | "Enfusionvirtide" no fusion!
43
How does Enfuvirtide prevent fusion of HIV and CD4+
binds to gp41 subunit of HIV glycoprotein, blocking conformational changes required for membrane fusion
44
which class is Enfuvirtide effective against
HIV-1
45
Side effects of Enfuvirtide
local injection site rxns, diarrhea and nausea... mainly used for pts that have failed other regimens
46
used for pts that have failed early regimens
Enfuvirtide
47
Maraviroc is used to tx
CCR5-tropic HIV-1 but NOT NOT for CXCR4 strains and strains resistant to other drugs
48
When do CCR5 strains tend to predominate
early in infection... use Maraviroc | Maraviroc
49
Mech of Maraviroc
chemokine co-receptor (CCR5) antagonist (noncompetitive, allosteric) - blocks entry of HIV into cells Mara rocks...shes only 5 and doesn't let bad people in!
50
chemokine co-receptor (CCR5) antagonist (noncompetitive, allosteric) - blocks entry of HIV into cells
Maraviroc
51
Side effects of Marairoc
Hepatotoxic and possble CV events | --CYP3A4 substrate
52
Raltegrivir class:
integrase inhibitor
53
Raltegrivir uses:
treatment of HIV-1 in new and treatment-experienced patients works on virus that is resistant to other drugs
54
inhibits HIV-1 integrase activity, preventing integration of HIV-1 DNA into the genome
Raltegrivir
55
Mech of Raltegrivir
stops HIV-1 integrase activty HIV-1 can't get it's genome into DNA More like "Ral INTEGRA-vir" because keeps the integrity our OUR genome by stoping HIV INTEgrase
56
Importance of Drug Combinations
* use 3 (or more) drugs per patient (2 or more drug classes) | * keep replication at zero to prevent resistance
57
Importance of viral load | where do we want to keep viral load under
* viral load monitors drug effectiveness | * initiate treatment if CD4 count is <350, or if other factors so warrant

Block 3 Pharm (19 decks)

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