HIV Pharm Flashcards by Jordan Trager

What are the main classes of HIV drugs?

NRTI, nucleoside reverse transcriptase inhibitors
NNRTI, non-nucleoside reverese transcriptase inhibitors
INSTI, integrase strand transfer inhibitors
protease inhibitors
fusion inhibitors
entry blockers

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What does a normal ART regimen look like?

What classes are first, second, and thrid line?

combination regimen of 3 drugs from at least 2 different classes

“2 +1”

First line:

“2” -> NRTI
“+1” -> INSTI

Second line:

-“+1” -> protease inhibitors

Thrid line:

-“+1” -> NNRTI

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What changes should be made when an HIV patient does not respond to their ART therapy?

2 or more of the drugs should be changed to prevent formation of drug resistance

new drugs should have a different mechanism of resistance from original drugs

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What are NRTIs?

Nucleoside reverse transcriptase inhibitors:

-mimic nucleotides but lack 3’ -OH, incorperated into HIV DNA during synthesis by reverse transcriptase -> chain termination

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What black box warning is associated with NRTIs and why?

-NRTIs are not recognized by human DNA polyerase, however, they are partially recognized by mitochondrial DNA polymerase -> mitochondrial toxicity

-lactic acidosis

peripheral neuropathy
anemia
myopathy

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What is a common suffix in NTRIs?

“-vudine”

not found in all NTRIs

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What is zidovudine (AZT)?

What if any toxicities are associated with it?

NRTI (“-vudine”)

-thymidine analog, needs phosphorylation

Toxicities:

myelosupression -> cytopenias
lipodystrophy (common to thymidine analogs)
mitochondrial toxicity (common to all NTRIs)

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What is stavudine (d4T)?

What if any toxicities are associated with it?

NRTI (“-vudine”)

-thymidine analog, needs phosphorylation

Toxicities:

peripheral neuropathy
lipodystrophy (*most prominent in stavuidne*)
mitochondrial toxicity (common to all NTRIs)

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What is emtricitabine (FTC)?

What if any toxicities are associated with it?

NRTI

-cytosine analog, needs phosphorylation

Toxicities:

hyperpigmentation of palms and soles (common in AAs)
one of the least toxic

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What is lamivudine (3TC)?

What if any toxicities are associated with it?

NRTI (“-vudine”)

-cytidine analog, needs phosphorylation

Toxicities:

peripheral neuropathy
one of the least toxic

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What is abacavir (ABC)?

What if any toxicities are associated with it?

NRTI

-guanosine analog (only one), needs phosphorylation

Toxicities:

-fatal hypersensitivity with HLA-B*5701 -> rash

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What is tenofovir disoproxil fumarate (TDF)?

What if any toxicities are associated with it?

NRTI

-adenosine analog, already phosphorylated

Toxicities:

-nephrotoxicity -> (Fanconi syndrome)

-decreased bone density

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What is tenofovir alafenamide (TAF)?

What if any toxicities are associated with it?

NRTI

-adenosine analog, already phosphorylated

Toxicities:

well tolerated
lower plasma concentrations that TDF -> less risk of renal and bone s/x

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What NRTI is most commonly used in children and pregnant women?

-zidovudine

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What NRTI(s) is also effective against HTLV?

-zidovudine

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What NRTI(s) is also effective against HBV?

emtricitabine (both C)
lamivudine (both C)
tenofovir

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What NRTIs are often co-formulated?

emtricitabine / lamivudine (cytosine)
tenofovir (adenosine)

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What are INSTIs?

Integrase strand transfer inhibitors:

-blocks integration of HIV DNA into cell DNA -> no viral DNA replication

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What is a common suffix in INSTIs?

Study These Flashcards

“-tegravir”

inteGRAse

What is raltegravir?

What if any toxicities are associated with it?

Study These Flashcards

INSTI (“-gravir”)

Toxicities:

generally well tolerated
immune reconstitution syndrome
rhabdomyolysis
hypersensitivity reaction

What is dolutegravir?

What if any toxicities are associated with it?

Study These Flashcards

INSTI (“-gravir”)

Toxicities:

-generally well tolerated

-possible neural tube defects w/ pregnancy

immune reconstitution syndrome
rhabdomyolysis
hypersensitivity reaction

What is bictegravir?

What if any toxicities are associated with it?

Study These Flashcards

INSTI (“-gravir”)

comes only in combination with other drugs

Toxicities:

-generally well tolerated

What makes INSTIs first line “+1” ART drugs?

Study These Flashcards

will often still be effective when other drugs are resisted (unique mechanism of resistance)
development of resistance is actually genetically resisted

-generally well tolerated

What are protease inhibitors?

Study These Flashcards

inhibit cleavage of HIV precursor proteins into active proteins

target:

homodimer asrpartyl protease (cleaves proline)
human aspartyl proteases are monomers and not affected

What is a **common suffix** in **protease inhibitors**?

"-navir"

What is **darunavir**? What is special about it?

**Protease inhibitor** ("-navir") **-current first choice PI** -sulfa drug -\> **possible hypersensitivity**

What is **atazanavir**? What is special about it?

**Protease inhibitor** ("-navir") -elevated unconjugated bilirubin w/o hepatitis

What is **lopinavir**? What is special about it?

Protease inhibitor -often works after failure of other PIs

What is **indinavir**? Whats special about it?

protease inhibitor ("-navir") -not used any more due to **crystaluria/renal stone**

What are **common toxicities** of **protease inhibitors**?

- dyslipidemia - immune reconstitution syndrome - GI symptoms

What drugs are almost always given along with protease inhibitors?

CYP3A4 inhibitors - ritonavir - cobicistat - most protease inhibitors are metabolized by CYP3A4 so inhibitors increase the concentration of PIs

What is **ritonavir**?

**CYP3A4 inhibitor**

What is **cobicistat**?

**CYP3A4 inhibitor** -used w/ **azatanavir** and **darunavir**

What are **NNRTIs**?

**_Non-nucleoside reverse transcriptase inhibitors_**: -non-competitive reverse transcriptase inhibitor

What is a common feature in the name of NNTRIs?

**"-vir-"** is in the **middle of the name**, not the end _{(Don't rely on this outside of HIV medications, its literally just something I found helpful. Enfuvirtide and maraviroc break this rule so I'm sure there are non-HIV antivirals that do as well)}

nevirapine

**NNTRI**

efavirenz

**NNTRI**

etravirine

**NNTRI**

rilpivrine

**NNTRI**

doravirine

**NNTRI**

What makes NNRSTIs third line "+1" ART drugs?

- **only effective against HIV-1;** HIV-2 naturally resistant - **easily develop resistance**

What are **fusion inhibitors**?

targets **gp41** which is involved in viral membrane fusion with host cell -\> **virus can't fuse, cells not infected**

What is **enfuvirtide**?

**Fu**sion inhibitor (en**fu**virtide) -**must be administered parenerally**

What are the **benefits/disadvantages** of **enfuvirtide**?

Benefits: -**unique mechanism**; remains active following resistance to other drugs Disadvantages: - **not effective against HIV-2** - VERY **expensive**

What are **entry blockers**?

**blocks GP120** (HIV molecule that recognizes CXCR4 and CCR5) from **binding CCR5**

What is **maraviroc**?

entry bl**oc**ker maravir**oc**

What are the **benefits/disadvantages** of **maraviroc**?

Benefits: -unique mechanism; remains active following resistance to other drugs Disadvantages: - only **effective against** HIV that is **tropic to CCR5 only**; ineffective against CXCR4 only tropic and mixed tropic - requires expensive testing to determine tropism

HIV Pharm Flashcards

(47 cards)