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SBL > HIV Pharm Crossword > Flashcards

HIV Pharm Crossword Flashcards

1
Q

HIV integrase strand inhibitor with ~ 14 hr half-life (i.e. suitable for once per day dosing); widely recommended for initial ART because-while resistance can develop due to integrase mutations- there is a high genetic barrier to this resistance

A

dolutegravir

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2
Q

newer INSTI, only available in 1x/day oral combination, well absorbed in comparison to other INSTI, high genetic barrier to development of resistance like dolutegravir, and very well tolerated

A

bictegravir

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3
Q

cytochrome P450 isozyme that is inhibited, induced, etc. by a wide range of drugs including several antiretroviral drugs (e.g. PI and NNRTI), which leads to numerous potentially troublesome drug interactions (e.g. oral contraceptives)

A

CYP3A4

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4
Q

current concern of HIV ART given that there are multiple effective drugs, can assist with adherence

A

convenience

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5
Q

adenosine analog that is the only NRTI nucleoTIDE (ie has a phosphate already attached, so only needs 2 more to be active), an NNRTI of choice due to its relative safety, long half-life and co-formulation in once/day pills

A

tenofovir

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6
Q

newest/arguably best NNRTI with unique resistance mechanisms such that it works if resistance to efavirenz or rilpivirine; less significant drug-drug interactions and lower incidence of typical side effects

A

doravirine

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7
Q

can occur rapidly with HIV monotherapy to confer resistance, typically 4-5 are required for HIV to develop resistance to protease inhibitors which is reason resistance is slow to develop and seldom a cause for treatment failure with PI

A

mutations

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8
Q

type of reverse transcriptase inhibition by NNRTI

A

didanosine

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9
Q

HIV infected people for whom ART is recommended ASAP

A

all

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10
Q

preventing this is a goal of HIV therapy, counseling is important at all ages

A

transmission

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11
Q

emergence of this tropism in HIV renders it resistant to maraviroc

A

CXCR4

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12
Q

pre-exposure ____ is available for HIV-negative sexual partners of those with HIV infection as is post-exposure ____ for those who likely were exposed to HIV

A

prophylaxis

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13
Q

if plasma levels of this are sustained at <200 copies/ml, sexual transmission of HIV to partners is prevented

A

HIV RNA

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14
Q

interesting/newer pro-drug formulation of tenofovir that has higher intracellular concentrations and less renal and bone toxicity due to lower plasma levels

A

alafenamide

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15
Q

among the toxicities associated with some NRTI that is thought to be due to inhibition of DNA polymerase gamma

A

myopathy

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16
Q

1st generation integrase inhibitor, now largely replaced by newer drugs since their longer half-lives permit once daily dosing

A

raltegravir

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17
Q

the combination of dolutegravir and lamivudine is the only recommended ____-agent treatment naive ART regimen provided < 500,000 HIV copies per ml and no HBV at start

A

dual

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18
Q

virus (abbr.) sensitive to some HIV drugs such as tenofovir (recommended for continuation) and emtricitabine and lamivudine (in combo with tenofovir); discontinuation of these inhibiting drugs can cause a disease flare-up; importantly abacavir, has no impact on this

A

HBV

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19
Q

characterizes ART when HIV copy number persists at >200/ml despite treatment

A

failure

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20
Q

generally in either treatment-experienced or treatment-naïve groups, both groups can have some unique struggles needing experts skilled with motivation, transitioning, etc.

A

young

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21
Q

cytidine-like NRTI that can be used as part of approved dual agent ART; HIV can develop resistance to it relatively quickly when used as monotherapy but doing so increases reverse transcriptase fidelity, slows replication, and thereby helps to increase long-term effectiveness of other agents

A

lamivudine

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22
Q

ending of generic drug name that strongly suggests the drug is an integrase strand transfer inhibitor

A

gravir

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23
Q

weaker HIV protease inhibitor discovered to be a very potent inhibitor of CYP3A4, and “boosting” other more effective drugs is the sole reason for its use

A

ritonavir

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24
Q

not a contraindication for ART

A

substance use disorder

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25
Q

new INSTI available in combo with rilpivirine as a once every 4 weeks IM injection

A

cabotegravir

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26
Q

recommended every 6 months for HIV patients using TDF because of potential adverse effects on kidney function

A

urinalysis

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27
Q

efavirenz was initially thought to be one but no more, some concern that dolutegravir is one

A

teratogen

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28
Q

because it is this type of drug, darunavir has a higher risk for rash and hypersensitivity reactions than drugs not in this category

A

sulfa

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29
Q

HIV integrase strand inhibitor suitable for once per day dosing when boosted, use will likely decline with availability of bictegravir from same company

A

elvitegravir

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30
Q

aka fatty liver, potential adverse effect of HIV therapies such as zidovudine

A

hepatic steatosis

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31
Q

blockade of DNA polymerase here is thought to be responsible for many of the adverse effects associated with some NRTI, especially early NRTI

A

mitochondria

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32
Q

stands for highly active antiretroviral therapy, may still see this used but now obsolete

A

HAART

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33
Q

intracellular site where typically a single copy of HIV DNA is located in infected cells

A

host genome

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34
Q

symptoms of this appear when HIV RNA copy numbers are high in plasma and CD4+ lymphocyte numbers are low

A

AIDS

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35
Q

1st prodrug formulation of tenofovir, a phosphorylated adenosine analog, to overcome its otherwise poor bioavailability

A

disoproxil fumarate

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36
Q

1st HIV protease inhibitor, its short half-life caused a troublesome pill burden and it is among the agents well-known for promoting irreversible lipodystrophy with long-term use

A

saquinavir

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37
Q

effective use of ART means it can hopefully exit its HIV-infected host without becoming infected

A

newborn

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38
Q

current position of NNRTI in +1 hierarchy for addition to NRTI backbone in ART

A

third

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39
Q

person to contact whenever ART fails

A

expert

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40
Q

drug class that is the typical second choice for +1 drug in ART, block a virus aspartyl protease enzyme (abbr.)

A

PI

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41
Q

early HIV target since mammalian cells lack this

A

reverse transcriptase

42
Q

thymidine analog and the 1st antiretroviral drug discovered, this NRTI is still in widespread use in resource-poor settings due to its well-known tolerability, toxicity, and efficacy profiles

A

zidovudine

43
Q

syndrome refers to chronic inflammation and/or reactivation of autoimmune disease in HIV patients as lymphocyte levels increase during ART

A

immune reconstitution

44
Q

intrinsically resistant to NNRTI, but rarely seen in US

A

HIV-2

45
Q

syndrome seen in patients with reduced GFR due to tenofovir toxicity in the proximal tubules, occurs less with tenofovir alafenamide

A

Fanconi

46
Q

while some ART drugs inhibit CYP3A4, NNRTI tend to do this

A

induce

47
Q

along with enfuviritide and maraviroc, new drugs ibalizumab and fostemsavir inhibit this step of viral infection in multi-drug resistant HIV patients

A

entry

48
Q

ending of generic drug name that suggests the drug is an HIV protease inhibitor

A

navir

49
Q

not possible for cells infected with HIV by using current therapies

A

eradication

50
Q

for HIV, this equates to non-transmissible

A

undetectable

51
Q

early protease inhibitor requiring 3x/day dosing, no longer used but remains test fodder for its unique ability to cause crystalluria/renal stones

A

indinavir

52
Q

measured regularly during antiretroviral therapy to help ensure that it is and/or remains effective

A

CD4 count

53
Q

enzyme responsible for insertion of retroviral DNA into the human genome, and an excellent drug target since mammalian genomes lack enzymes with this capability

A

integrase

54
Q

form of testing that must be done before prescribing abacavir

A

genetic

55
Q

population of HIV-infected people that can be especially hard to treat, in part due to polypharmacy

A

elderly

56
Q

portion of generic drug name indicating that the drug is an HIV integrase inhibitor

A

tegravir

57
Q

early NRTI adenosine analog noteworthy for its adverse effects due to mitochondrial toxicity

A

didanosine

58
Q

CYP3A4 inhibitor co-administered with some ART drugs metabolized for elimination by this enzyme

A

cobicistat

59
Q

prescribing 1x/day of these for ART has increased treatment adherence

A

combination pills

60
Q

a 2-drug combo from this antiretroviral drug therapy class typically provides the “backbone” for current HIV treatment strategies, each agent should target a different DNA base

A

NRTI

61
Q

reason for a thorough evaluation of patient history and contemplation of new strategy rather than adding a single new drug to an HIV treatment regimen or stopping treatment altogether

A

treatment failure

62
Q

class of drugs that selectively inhibits only HIV-1 reverse transcriptase; binds to a distant hydrophobic pocket in a manner that causes a conformational change to abolish its activity

A

NNRTI

63
Q

the HIV drug class (abbr.) that is now the primary +1 addition to an NRTI backbone because of relative safety

A

INSTI

64
Q

drugs eliminated from the body like this tend to have few drug-drug interactions

A

unchanged

65
Q

serious NRTI toxicity associated with early agents such as stavudine

A

peripheral neuropathy

66
Q

the only NRTI that is a guanosine analog, relatively safe in most but can cause a unique and potentially fatal hypersensitivity syndrome in those with the HLA-B*5701 locus

A

abacavir

67
Q

unconjugated _____ not associated with hepatitis is a toxicity associated with atazanavir

A

hyperbilirubinemia

68
Q

NNRTI approved for use in treatment-experienced people infected with HIV since it still works after HIV mutations that cause resistance to nevirapine and efavirenz

A

etravirine

69
Q

reason to avoid some antiretroviral drugs such as indinavir and tenofovir and/or decrease the dosages/use with caution

A

renal insufficiency

70
Q

irreversible disfiguring re-distribution of body fat associated with HIV and its treatment, much less common now but was strongly associated with zidovudine and especially stavudine use in years past

A

lipodystrophy

71
Q

highly effective but less than ideal means of preventing the spread of sexually transmittable diseases

A

abstinence

72
Q

type of potentially fatal adverse effect strongly associated with abacavir use in patients with HLA*B5701, but also a rare adverse effect of other HIV drugs as well including some INSTI drugs

A

hypersensitivity

73
Q

can see a typically self-limiting decrease in this with use of tenofovir

A

bone density

74
Q

can happen with prolonged use of emtricitabine, especially to the palms and soles of African Americans

A

hyperpigmentation

75
Q

develops to all ART drugs when used as monotherapy, reason for testing when ART therapy fails, NNRTI were historically most susceptible to its rapid appearance

A

resistance

76
Q

HIV protease inhibitor only available as a boosted combo often used in recent past (e.g. works after failure of another PI-containing regimen) but has now been supplanted by darunavir and atazanavir

A

lopinavir

77
Q

the combo of tenofovir and emtricitabine is often this for treatment-naïve HIV patients due to its safety, potentially superior efficacy, and also due to the convenience of a once/daily co-formulation

A

preferred NRTI backbone

78
Q

increasing the duration and quality of this is an HIV treatment goal for something that was initially far more deadly

A

survival

79
Q

if a protease inhibitor is selected for a treatment-naïve HIV patient, this boosted is a 1st choice due to its long half-life and reduced side effects, but can cause sulfa drug hypersensitivity reactions

A

darunavir

80
Q

an NNRTI, early studies with it demonstrated the importance of combo therapy in treating HIV after the virus in ~1/3 of patients developed resistance to it after a single monotherapy exposure

A

nevirapine

81
Q

important consideration of HIV ART for promoting adherence given that there are now multiple treatment options

A

tolerance

82
Q

NRTI do this during reverse transcriptase mediated synthesis of proviral DNA

A

terminate elongation

83
Q

treatment for HIV infection does not protect against this (abbr.)

A

STI

84
Q

adverse effect of INSTI class, especially for non-white women, appears to be worst for dolutegravir and negligible for cabotegravir

A

weight gain

85
Q

term means that a CYP3A4 inhibitor was administered along with the active drug that is metabolized by CYP3A4

A

boosted

86
Q

required of NRTI for them to be active

A

phosphorylation

87
Q

possible and perhaps severe for HBV when HIV drugs with activity against HBV are discontinued

A

rebound viremia

88
Q

syndrome that is focus of black box warnings on NRTI, of much greater concern for early HIV drugs that inhibited mitochondrial DNA polymerase

A

lactic acidosis

89
Q

phase II metabolic process for antiretroviral drug elimination that tends to result in fewer drug-drug interactions

A

glucuronidation

90
Q

NNRTI recommended for treatment-naïve patients, susceptible to resistance mutations but not he one that quickly inactivated nevirapine and efavirenz meaning they will still work; recently available in combo with cabotegravir for 1x/4 weeks IM injection

A

rilpivirine

91
Q

common side effect of efavirenz, but typically subsides and rarely leads to discontinuation of the drug

A

CNS toxicity

92
Q

will block HIV entry if an expensive test with a long turnaround time shows that the virion requires the CCR5 co-receptor

A

maraviroc

93
Q

cytidine analog, one of the least toxic antiretroviral drugs and an NRTI of 1st choice to its long half-life and excellent performance when co-formulated with tenofovir

A

emtricitabine

94
Q

a 36 aa peptide that inhibits formation of a 6-helix bundle critical for HIV fusion with the host cell membrane, drug is a last resort for ART since expensive and must be administered subQ 2x/day

A

enfuvirtide

95
Q

1st generation NNRTI, has some typically self-limiting CNS side effects that seldom require drug discontinuation

A

efavirenz

96
Q

HIV enzyme that cleaves at the N-terminal side of Pro residues in the long polypeptides (e.g. gag, pol) packaged into newly budded virions to release the enzymes and capsid structural components required for their metamorphosis into a mature virus capable of causing infection

A

protease

97
Q

always look for this before initiating ART, reason for avoiding use of dolutegravir in a sub-population of HIV infected people

A

pregnancy

98
Q

when boosted, an initial option if a protease inhibitor is used for treatment-naïve HIV patients due to its long half-life and reduced side effects

A

atazanavir

99
Q

among early thymidine NRTI, notable for significant toxicities now associated with the drug class including CNS toxicity, fat wasting/lipodystrophy, and the ability to cause lactic acidosis and hepatic steatosis

A

stavudine

100
Q

generic abbr. for drugs used in combo to treat HIV infections

A

ART

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