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Block 3 Pharm > AIDS drugs > Flashcards

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
Q

NNRTIz are all

A

active as given and don’t need to be P’d to be activated

26
Q

Five covered NRTIs

A 
Zidovudine
Abacavir
Lamivudine
Tenofovir
Emtricitabine
27
Q

Mech of Efavirenz

A

non-nucleoside inhibitor of reverse transcriptase; does not require phosphorylation for activity

28
Q

Efavirenz

A

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
Q

Sides of Efavirenz

A

rash and CNS~~ have nightmares

30
Q

1 HIV drug in US

A

Efavirenz

31
Q

Key protease inhibitors for HIV

A

Lopinavir and Ritonavir

32
Q

Use of Apartic protease inhibitos

A

In combo with RT inihbitors for HIV 1 and 2 to decrease viral load

33
Q

what can be used with RT inhibitors for HIV 1 and 2 to decrease viral load

A

Protease inhibitors like Lopinavir and Ritonavir

34
Q

Which protease inhibitor is used more as a PI booster and not as a PI itself

A

Ritonavir

35
Q

Which protease inhibitor is used specifically as protease inhibitor

A

Lopinavir

36
Q

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.

A

Protease inhibitors

bahahaha… HIV has giant gagpol and these guys stop it from being split up into function virions!!

37
Q

Common toxicities of lopinavir

A

nasty combo of Cushings and weird fat stuff
: diabetes
:alters lipid metabolism
fat redistribution
:alters metab of other drugs by inhibiting CYP3A4

38
Q

Diabetes, alters lipid metabolism, fat redistribution, alters met of other drugs (CYP3A)

A

Toxicity caused by Lopinavir

39
Q

Used a protease inhibitor to stop breakdown of gag-pol to infectious virions

A

Lopinavir

got a LOW chance of making those virions!

40
Q

Boosts lopinavir levels by blocking the metabolism of lopinavir by CYP3A

A

Ritonavir

41
Q

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

A

Enfuvirtide

42
Q

Enfuvirtide mech

A

stops fusion of HIV-1 and cellular CD4+ membranes

“Enfusionvirtide” no fusion!

43
Q

How does Enfuvirtide prevent fusion of HIV and CD4+

A

binds to gp41 subunit of HIV glycoprotein, blocking conformational changes
required for membrane fusion

44
Q

which class is Enfuvirtide effective against

A

HIV-1

45
Q

Side effects of Enfuvirtide

A

local injection site rxns, diarrhea and nausea… mainly used for pts that have failed other regimens

46
Q

used for pts that have failed early regimens

A

Enfuvirtide

47
Q

Maraviroc is used to tx

A

CCR5-tropic HIV-1 but NOT NOT for CXCR4 strains and strains resistant to other drugs

48
Q

When do CCR5 strains tend to predominate

A

early in infection… use Maraviroc

Maraviroc

49
Q

Mech of Maraviroc

A

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
Q

chemokine co-receptor (CCR5) antagonist (noncompetitive, allosteric)
- blocks entry of HIV into cells

A

Maraviroc

51
Q

Side effects of Marairoc

A

Hepatotoxic and possble CV events

–CYP3A4 substrate

52
Q

Raltegrivir class:

A

integrase inhibitor

53
Q

Raltegrivir uses:

A

treatment of HIV-1 in new and treatment-experienced patients works on virus that is resistant to other drugs

54
Q

inhibits HIV-1 integrase activity, preventing integration of HIV-1 DNA into the
genome

A

Raltegrivir

55
Q

Mech of Raltegrivir

A

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
Q

Importance of Drug Combinations

A
  • use 3 (or more) drugs per patient (2 or more drug classes)

* keep replication at zero to prevent resistance

57
Q

Importance of viral load

where do we want to keep viral load under

A
  • 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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