Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Infectious Disease > Antiretroviral Therapies > Flashcards

Antiretroviral Therapies Flashcards

1
Q

Maraviroc (MVC)

A

Adverse Effects:
“* Fever, URI, rash
* Hepatoxicity
* Can cause IgE mediated HS rxn”
Considerations:
“* Salvage therapy
* tropism testing (R5 tropic only)
* CYP3A4 (neither inducer or inhibitor)”
MOA:
CCR5 inhibitor; prevents HIV from binding this coreceptor
Class Effects:

Entry inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Efuviritide (T20)

A

Adverse Effects:
* Painful nodules can form at inj site
Considerations:
“* VERY expensive
* No significant DDIs
* Requires q12h subq inj
* Salvage therapy”
MOA:
Binds gp41 of HIV envelope preventing conformational change required for viral fusion & entry into cell
Class Effects:

Fusion inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

“Abacavir
(guanosine)” (ABC)

A

Adverse Effects:
HS rxn with HLA-B5701 that can cause fever, rash, multi-organ involvement, fatal (never re-challenge)
Considerations:
“* HLA-B5701 testing before starting
* Less effective if VL > 100,000 (not worrisome as long with other robust drugs)
* Metabolized by ADH (can cause pt to get drunk faster/longer)”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“ Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Emtricitabine (cytosine) (FTC)

A

Adverse Effects:
* Rare hyperpigmentation
Considerations:
“* Active against HBV
* HIV PREP (Truvada)
Should NOT be used w Lamivudine”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“ Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Lamivudine (cytosine) (3TC)

A

Adverse Effects:

Considerations:
“*Active against HBV
Should NOT be used w Emtricitabine”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“ Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Tenofovir DF (adenosine) (TDF)

A

Adverse Effects:
“* Renal toxicity
Decreased bone density”
Considerations:
“ Active against HBV
* HIV PREP (Truvada)
Requires less phosphorylation to become activated”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“ Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Tenofovir alafenamide (TAF)

A

Adverse Effects:
Less renal toxicity & bone effects than DF
Considerations:
“ Tenofovir (TFV) prodrug
More stable in plasma than TDF (less needed to produce same effect)
* Hydrolyzed to TFV (active form) intracellularly where you want it to act”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“ Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

“Zidovudine
(thymidine)” (AZT, ZDV)

A

Adverse Effects:
* Macrocytic anemia
Considerations:
“* First IV ART drug
* Used to prevent vertical transmission (first drug studied for this use)”
MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“* Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Didanosine (ddl)
Stavudine (d4T)

A

Adverse Effects:
“* Irreversible peripheral neuropathy
*Pancreatitis
* Lactic acidosis”
Considerations:

MOA:
Nucleotide analogs that competes for incorporation into growing viral DNA & inhibits further elongation by RT due to lack of 3’-OH group
Class Effects:
“* Drugs require intracellular phosphorylation to become activated (makes it difficult to check drug plasma levels)
* Renal elimination (few DDIs)
* Older drugs caused lactic acidosis long-term from mitochondrial toxicity “

NRTI (nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

“Efavirenz
(1st gen)” (EFV)

A

Adverse Effects:
“* Neuropsychiatric (dizzy, drowsy, dreams)
* Hyperlipidemia
* Rash (diffuse maculopapular lesions & blisters)”
Considerations:
“* Risk of NTD in pregnancy
* Rapid development of resistance w non-adherence”
MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

“Etravirine
(2nd gen)” (ETR)

A

Adverse Effects:
Nausea, rash
Considerations:
*BID dosing
MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

“Doravirine
(2nd gen)” (DOR)

A

Adverse Effects:
Nausea, headache, fatigue, diarrhea, dreams
Considerations:
“* NO food/acid effects
* Can be used w high VL”
MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

“Rilpivirine
(2nd gen)” (RPV)

A

Adverse Effects:
Nausea, rash
Considerations:
“* Must be taken w 400 cal mean & acid for absorption (cannot be taken with acid suppressive agent)
* Not recommended with baseline VL > 100,000 or CD4 < 200”
MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

“Delaviridine
(1st gen)” (DLV)

A

Adverse Effects:

Considerations:

MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

“Nevirapine
(1st gen)” (NVP)

A

Adverse Effects:
“* Hepatotoxic (greater risk w higher CD4 count)
* Rash “
Considerations:
“*Used internationally, not in US
* Rapid development of resistance w non-adherence”
MOA:
Non-competitive inhibitors that bind hydrophobic pocket on RT, inhibiting its ability to synthesize viral DNA
Class Effects:
*CYP3A4 inducers (decrease conc of other drugs)
* Cross-resistance within generations (not usually between)
* Rash (1st gen more often)

NNRTI (non-nucleoside)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Bictegravir (BIC)

A

Adverse Effects:
*Increases SCr
Considerations:
* ONLY available in single tablet (most used)
MOA:
Inhibits HIV integrase from integrating viral DNA into CD4’s DNA
Class Effects:
*Eliminated by glucuronidation (few DDIs; elvitegravir IS metabolized by CYP3A4 & requires boosting)
*Neutral effect on lipids
* Generally well tolerated but Aes include: headache, Cr Kinase elevation, myopathy, binds cations (separate dose from vitamins)

Integrase inhibitors

17
Q

Dolutegravir (DTG)

A

Adverse Effects:
*Increases SCr
Considerations:
* Can be crushed

MOA:
Inhibits HIV integrase from integrating viral DNA into CD4’s DNA
Class Effects:
*Eliminated by glucuronidation (few DDIs; elvitegravir IS metabolized by CYP3A4 & requires boosting)
*Neutral effect on lipids
* Generally well tolerated but Aes include: headache, Cr Kinase elevation, myopathy, binds cations (separate dose from vitamins)

Integrase inhibitors

18
Q

Elvitegravir (EVG)

A

Adverse Effects:
*Increases SCr (due to cobicistat booster)
Considerations:
*Requires booster due to CYP3A4 metabolism
MOA:
Inhibits HIV integrase from integrating viral DNA into CD4’s DNA
Class Effects:
*Eliminated by glucuronidation (few DDIs; elvitegravir IS metabolized by CYP3A4 & requires boosting)
*Neutral effect on lipids
* Generally well tolerated but Aes include: headache, Cr Kinase elevation, myopathy, binds cations (separate dose from vitamins)

Integrase inhibitors

19
Q

Raltegravir (RAL)

A

Adverse Effects:
“* Myopathy & rhabdomyolysis
* Increased bili & LFTs”

Considerations:
* BID dosing or new high dose but still requires lots of pills daily

MOA:
Inhibits HIV integrase from integrating viral DNA into CD4’s DNA
Class Effects:
*Eliminated by glucuronidation (few DDIs; elvitegravir IS metabolized by CYP3A4 & requires boosting)
*Neutral effect on lipids
* Generally well tolerated but Aes include: headache, Cr Kinase elevation, myopathy, binds cations (separate dose from vitamins)

Integrase inhibitors

20
Q

Atazanavir (ATZ)

A

Adverse Effects:
“* Hyperbilirubinemia/jaundice (asymptomatic)
* Nephrolithiasis
* Low association w lipodystrophy
* Lipid neutral”

Considerations:
* Requires acid for abs

MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“*CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

21
Q

Darunavir (DRV)

A

Adverse Effects:
“* Lipid friendly
* Low association w lipodystrophy
* Rash”
Considerations:
“* Highest barrier to resistance
* Contains sulfa moiety (low rxns with sulfa allergies)
MUST be boosted or it will not reach adequate drug levels”
MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

22
Q

Ritonavir (booster) (RTV)

A

Adverse Effects:
“*GI (nausea, vomiting, diarrhea)
* Loss of appetite
* Dyslipidemia
Paresthesias”
Considerations:
“ NOT used as single PI (large doses poorly tolerated)
Booster that inhibits CYP3A4 metabolism to increase PI conc”
MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

23
Q

Fosamprenavir (FPV)

A

Adverse Effects:
“*Rash
* GI effects
Paresthesias”
Considerations:
“ Used internationally
Prodrug of amprenavir (not available)
* Sulfa moiety
* daily-BID dosing”
MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

24
Q

“Cobicistat
(booster)”

A

Adverse Effects:
“* Increase SCr (NOT indicative of kidney dysfunction)
* Less GI than Ritonavir”

Considerations:
“* Booster (oral) that inhibits CYP3A4 & 2D6 to increase PI conc
* Non-inferior to Ritonavir
* No antiviral activity”

MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“*CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

25
Q

Lopinavir

A

Adverse Effects:
“* GI intolerance common
*Asthenia/pancreatitis”

Considerations:
“* Coformulated with ritonavir
* BID dosing”

MOA:
Inhibits viral protease from cleaving HIV precursor proteins into active proteins (viral particles produced are not infectious)
Class Effects:
“*CYP3A4 inhibitors (increase conc of other drugs)
* Common metabolic AEs (hyperlipidemia, insulin resistance/ diabetes, lipodystrophy, elevated LFTs, GI)”

Protease inhibitors (all require a booster)

Infectious Disease (8 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions