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Terms in this set (104)
CD4 cell counts less than _________ are associated with development of opportunistic infections
What is virologic suppression?
-sustained reduction in HIV RNA level below the assay limit of detection (50 copies/mL)
What are indications to begin ARV therapy?
1) History of AIDS defining Illness
2) CD4 count <500 cells/mm^3
4) HIV associated neuropathy/nephropathy
5) HBV coinfection when HBV treatment is indicated
What are examples of Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI)s?
What is the MOA of NRTI?
Nucleoside or nucleotide analogs that lack 3'-hydroxyl group enter the cells, are phosphorylated and form synthetic substrates for viral reverse transcriptase. These molecules terminate proviral DNA when incorporated in the viral genome
Which NRTI has food restrictions?
What is the major adverse effect of NRTIs?
Lactic Acidosis Hepatic Steatosis Syndrome
didanosine>stavudine>zidovudine (alphabetical order)
-inhibit DNA polymerase gamma and block mtDNA
-inhibit oxidative phosphorylation complexes promoting production of cytosolic lactate
What are other AE of NRTIs?
-Lactic acidosis-hepatic steatosis syndrome
Discontinuation of NRTIs can cause what AE?
-discontinuation of agents that have an anti-HBV activity is associated with increase in HBV titer
LET your doctor know if you have HBV
What is the clinical indication of Abacavir?
combination therapy component for HIV-1 experienced patients
What is the major AE of Abacavir?
Hypersensitivity in patients with HLA-B 5071
What is the clinical indication of Zidovudine?
combination therapy component of HIV-1 and HIV-2
children, adults, pregnancy
What are the major AE of Zidovudine?
anemia and neutropenia
What are the contraindications of Zidovudine?
Stavudine antagonist, do not coadminister
What are the drug interactions of Zidovudine?
-Gancliclovir (BM toxicity)
Which NRTIs are preferred for naive patients?
What are the AE of Didanosine?
What are the contraindications of Didanosine?
Do not administer with Ztavudine or Zalcitabine
What are the drug interactions of Didanosine?
What are the AE of Emtracitabine?
What are the Contraindications of Emtracitabine?
do not coadminister with Lamivudine or in resistant patients
What are the AE of Lamivudine?
What are the contraindications of Lamivudine?
Do not coadminister with emtracitabine or in resistant patients
What are the drug interactions of Lamivudine?
What are the AE of stavudine?
What are the contraindications of Stavudine?
What are the drug interactions of Stavudine?
What are the AE of Tenofovir?
What are the contraindications of Tenofovir?
What are the drug interactions of Tenofovir?
What are the AE of Zidovudine?
anemia and neutropenia
What are the contraindications of Zidovudine?
What are examples of Nonnucleotide Reverse Transcriptase Inhibitors (NNRTI)s?
What is the MOA of NNRTIs?
noncompetitive inhibitors bind to RT and induce a conformational change that greatly reduces enzyme activity
NNRTIs inhibit HIV___ but not HIV____ RT
inhibit HIV-1, not HIV-2
What is the advantage of using NNRTIs?
use of PIs can be reserved for later, reducing exposure to common PI adverse effects
What are the disadvantages of NNRTIs?
1) prevalence of NNRTI- resistant virus
2) low genetic barrier of NNRTIs to resistance
What are the major AE of NNRTIs?
influence CYP450 enzyme activity
-many drug interactions
what are the indications of Efavirenz?
preferred as part of initial ARV therapy HIV-1, only once daily NNRTI
What are the major AE of Efavirenz?
Transient CNS effects
What are drug interactions of Efavirenz?
-lowers exposure to PIs and methadone
What is the clinical indication of Nevirapine?
combination component for HIV-1, recommended as alternative to Efavirenz in treatment of naive women with pretreatment CD4<250 cells/mm and men with CD4<400 cells/mm
What is the major AE of Nevirapine?
What is the contraindication of Nevirapine?
Women with pretreatment CD4> 250 cells/mm and men with CD4 > 400 cells/mm
What are drug interactions with Nevirapine?
-lowers exposure to PIs and methadone
What are examples of Protease Inhibitors?
What is the MOA of Protease Inhibitors?
inhibit HIV aspartyl protease, block processing of viral proteins required to produce mature viral particle
How is the bioavailability of PI's enhanced?
high fat meals
What is the major AE of PIs?
-CYP substrates and inhibitors (drug interactions)
Which drugs should not be coadministered with PIs due to CYP dependent metabolism?
7) St. John's Wart
What are the clinical indications of Ritonavir?
active against HIV-1 and HIV-2
-Boosting of PIs (potent CYP3A4 inhibitor and so low dose administration will enhance exposure of other PIs)
What are the major AE of Ritonavir?
paresthesias, not well tolerated
What are contraindications of Ritonavir?
co-administration with rifampins
What is PI-induced metabolic syndrome?
a cluster of metabolic risk factors that tend to occur together that inc. risk of developing heart disease, stroke, diabetes
-insulin resistance, hyperinsulinemia
-lipodystrophy, central obesity, facial and limb lipoatrophy
-inc. macrophage CD36 leading to inc. cholesterol uptake and atherosclerosis
Which Statins should be used in patients undergoing ARV therapy?
Which statins should be avoided in patients undergoing ARV therapy?
What is the MOA of Raltegravir?
Viral integrase Inhibitor
-blocks insertion of reverse-transcribed viral DNA into the host DNA by binding the Mg cofactors required for the strand transfer
-mutations that alter orientation of Mg ions can be resistant to INTIs
What are the indications of Raltegravir?
-combination therapy for naive and experienced patients
What are the AE of Raltegravir?
What are examples of Integrase Inhibitors?
What is the MOA of Enfuvirtide?
-binds to HIV surface glycpoprotein gp41 to block confirmation required for membrane fusion with host cell
What are the indications of Enfuvirtide?
combination therapy in experienced patients with viral suppression failure
-injected 2x daily
What is the AE of Enfuvirtide?
injection site reaction/inflammation
What is the MOA of Maraviroc?
-small molecule reversible antagonist of the CCR5 interaction with gp120
-blocks CCR5-trophic HIV-1 entry
What are the clinical indications of Maraviroc?
combination therapy for experienced patients with viral suppression failure following a tropism test
What are resistance mechanisms to consider in Maraviroc use?
1) mutation of CCR5- binding amino acid sequence in HIV gp120
2) emergence of CXCR4 trophic viruses
What are the AE of Maraviroc?
What are drug interactions with Maraviroc?
-altered by rifampins or ritonavir
Can Rifampin be used in the treatment of TB in HIV-infected patients?
No, dramatically reduces exposure to all PI's and multiple NNRTIs
What is the only HIV-drug that Rifampin can be co-administered with?
What is the preferred alternative to treatment in HIV-infected patients with TB?
-also requires monitoring and dose adjustment of ARV
What is the recommended ARV starting regimen for naive patients?
1) 1NNRT1 + 2NRTI
2) 1PI (boosted with RTV) + 2 NRTI
What is the recommended NNRTI option in ARV therapy regimens?
-not for pregnant patients or patients who could become pregnant
What is the alternate NNRTI option in ARV therapy regimens?
- not for patients with moderate or severe hepatic impairment
- not for women with pre ARV CD4 > 250 or men wtih CD4 > 400
What are the Preferred PI options in ARV therapy regimens? (4)
1) Atazanavir + ritonavir (not for patients who require high dose PPIs)
2) Darunavir + ritonavir
3) Fosamprenavir + Ritonavir (2x daily)
4) Lopinavir + Ritonavir (not for pregnant women )
What are the Alternative PI options in ARV therapy regimens? (3)
1) Atazanavir (not in combo with tenofvir or didansine/lamivudine)
2) Fosamprevanir +/- Ritonavir (1x daily)
3) Saquinavir + Ritonavir
What are the preferred dual NRTI options in ARV therapy regimens?
Tenofovir + Emtricitabine
(do not use with uboosted atazanavir)
-use with caution in pts. with renal insufficiency or pts taking nevirapine
What are the alternative dual NRTI options in ARV therapy regimens? (3)
1) Abacavir + lamivudine (not for HLA-B 5701 or high viral load or high risk CVD)
2) Didanosine + Lamivudine or etricitabine (not with unboosted atazanavir or pts with hx or pancreatitis or peripheral neuropathy)
3) Zidovudine + Lamivudine (caution in pts with anemia or neutropenia)
What is virologic suppression failure?
Inability to achieve or maintain suppression of viral replication to levels below the limit of detection (<50 copies/mL)
What is immunologic failure?
inability to achieve and maintain and adequate CD4 T-cell response despite virologic suppression
What is important to consider when changing drug regimens due to treatment failure?
-drug resistance is usually cumulative, consider all previous treatment history and test results
-drug resistance test
Which treatment regimens should you never use? (3)
1) Monotherapy with NRTI
2) Dual NRTI regimens
3) Triple NRTI regiments
(can use Abacavir/zidovudine/lamivudine or tenofovir/zidovudine/lamivudine in pts who have no better options)
Why should Atazanavir and indinavir never been used together?
Why should Didanosine and Stavudine never be used together?
high incidence of toxicity and serious lactic acidosis
Why should double NNRTI combos never be used?
EFV +NVP has more adverse effects than separate, both reduce ETV
Why should EFV never be used in 1st trimester of pregnancy?
Why should EMtcicitabine and Lamivudine never be used together?
similar resistance prolie
Why should Etravirine and unboosted PI never be used together
Induced PI metabolism
Why should Etravirine and boosted ATV, FPV, or TPV never be used together?
induced PI metabolism
Why should Nevirapine in naive women with CD4 > 250 or men wtih CD4 >400 not be used?
high incidence of hepatotoxicity
Why should stavudine and Zidovudine never be used together?
Why should unboosted darunavir, saquinivir or tipranavir not be used?
which NNRTI is preferred for naive patients?
Which PIs are preferred for naive patients?
What is an AE of Atazanavir?
contraindicated in hepatic insufficiency
What is an AE of fosamprenavir?
What is an AE of indinavir?
What is an AE of lopinavir?
Liemia, GI, lipodystrophy
What is an AE of nelfinavir?
what is an AE of ritonavir?
What is an AE of saquinavir?
lipodystrophy, rash, anemia
What is an AE of darunavir?
What is an AE of tipranavir?
inc. lipids, glucose
Which PIs are contraindicated in pts with sulfa allegies
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