HIV Pharm Crossword Flashcards by Ceara VanBuskirk

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

dolutegravir

How well did you know this?

Not at all

Perfectly

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

bictegravir

How well did you know this?

Not at all

Perfectly

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)

CYP3A4

How well did you know this?

Not at all

Perfectly

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

convenience

How well did you know this?

Not at all

Perfectly

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

tenofovir

How well did you know this?

Not at all

Perfectly

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

doravirine

How well did you know this?

Not at all

Perfectly

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

mutations

How well did you know this?

Not at all

Perfectly

type of reverse transcriptase inhibition by NNRTI

didanosine

How well did you know this?

Not at all

Perfectly

HIV infected people for whom ART is recommended ASAP

all

How well did you know this?

Not at all

Perfectly

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

transmission

How well did you know this?

Not at all

Perfectly

emergence of this tropism in HIV renders it resistant to maraviroc

CXCR4

How well did you know this?

Not at all

Perfectly

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

prophylaxis

How well did you know this?

Not at all

Perfectly

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

HIV RNA

How well did you know this?

Not at all

Perfectly

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

alafenamide

How well did you know this?

Not at all

Perfectly

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

myopathy

How well did you know this?

Not at all

Perfectly

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

raltegravir

How well did you know this?

Not at all

Perfectly

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

dual

How well did you know this?

Not at all

Perfectly

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

HBV

How well did you know this?

Not at all

Perfectly

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

failure

How well did you know this?

Not at all

Perfectly

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

young

How well did you know this?

Not at all

Perfectly

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

lamivudine

How well did you know this?

Not at all

Perfectly

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

gravir

How well did you know this?

Not at all

Perfectly

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

ritonavir

How well did you know this?

Not at all

Perfectly

not a contraindication for ART

substance use disorder

How well did you know this?

Not at all

Perfectly

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

cabotegravir

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

urinalysis

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

teratogen

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

sulfa

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

elvitegravir

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

hepatic steatosis

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

mitochondria

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

HAART

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

host genome

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

AIDS

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

disoproxil fumarate

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

saquinavir

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

newborn

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

third

person to contact whenever ART fails

expert

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

early HIV target since mammalian cells lack this

reverse transcriptase

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

zidovudine

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

immune reconstitution

intrinsically resistant to NNRTI, but rarely seen in US

HIV-2

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

Fanconi

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

induce

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

entry

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

navir

not possible for cells infected with HIV by using current therapies

eradication

for HIV, this equates to non-transmissible

undetectable

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

indinavir

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

CD4 count

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

integrase

form of testing that must be done before prescribing abacavir

genetic

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

elderly

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

tegravir

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

didanosine

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

cobicistat

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

combination pills

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

NRTI

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

treatment failure

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

NNRTI

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

INSTI

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

unchanged

serious NRTI toxicity associated with early agents such as stavudine

peripheral neuropathy

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

abacavir

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

hyperbilirubinemia

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

etravirine

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

renal insufficiency

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

lipodystrophy

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

abstinence

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

hypersensitivity

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

bone density

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

hyperpigmentation

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

resistance

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

lopinavir

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

preferred NRTI backbone

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

survival

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

darunavir

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

nevirapine

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

tolerance

NRTI do this during reverse transcriptase mediated synthesis of proviral DNA

terminate elongation

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

STI

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

weight gain

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

boosted

required of NRTI for them to be active

phosphorylation

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

rebound viremia

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

lactic acidosis

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

glucuronidation

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

rilpivirine

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

CNS toxicity

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

maraviroc

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

emtricitabine

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

enfuvirtide

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

efavirenz

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

protease

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

pregnancy

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

atazanavir

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

stavudine

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

ART

HIV Pharm Crossword Flashcards

(100 cards)