Pharmacology HIV Tx Flashcards
There are __ antiretroviral medications from _ major classes currently available for the management of HIV-infected patients.
25
6
The use _ nucleoside reverse transcriptase inhibitor (NRTI) agents plus a ___ active drug from a different class, is most effective in suppressing HIV RNA, minimizing drug toxicity, and/or reducing HIV-related morbidity and mortality.
2
3rd
Classes of antiretroviral drugs most commonly used in initial regimens include:
Nucleoside (and nucleotide) reverse transcriptase inhibitors (NRTIs)
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
Protease inhibitors (PIs)
Integrase strand transfer inhibitors (INSTIs)
Treatment for patients w/o cormid conditions?
dolutegravir
plus either
tenofovir-emtricitabine or abacavir-lamivudine
What is HLA-B
major histocompatibility complex, class I, B) is a human gene that provides instructions for making a protein that plays a critical role in the immune system
An adverse effect from abacavir is a ___________________, which can be severe and potentially life-threatening.
treatment-limiting hypersensitivity reaction
Why do you want to test HLA-B*5701 testing?
A test to predict who will develop a severe allergic reaction to the anti-HIV drug abacavir
____________________ has been associated with the presence of the major histocompatibility complex class I allele HLA-B*5701.
Abacavir-induced hypersensitivity reaction
A screening test for the HLA-B*5701 allele can assist clinicians to identify patients who are at risk of developing a hypersensitivity reaction to ________.
abacavir.
When is Abacavir contraindicated?
Abacavir is contraindicated in patients who are positive for HLA-B*5701.
_________ is generally avoided in individuals with reduced kidney function. Thus, regimens that do not use a first-line nucleoside combination should be considered
Tenofovir
tenofovir-emtricitabine recomended
We administer a regimen using tenofovir-emtricitabine as the nucleoside combination in patients who have what two things?
chronic hepatitis B virus (HBV) infection and normal kidney function.
Prefer a regimen using _________________ as the nucleoside combination in patients who have a history of, or who are at high risk for, ______ _______.
tenofovir-emtricitabine
heart disease.
_______ may have a modest effect on lowering ______.
Tenofovir
lipids
Osteoporosis patients on Abacavir-lamivudine have a great risk of what?
greater loss of bone density unless HLA-B*5701 positive
Prefer a regimen that uses tenofovir-emtricitabine
Patients who are being treated for __ with a rifampin-containing regimen, we prefer _________.
TB
efavirenz
_______________ enable decreased pill burdens which can improve patient adherence
Coformulations
Truvada is?
Tenofovir-emtricitabine (Truvada)
Epzicom is ?
Abacavir-lamivudine (Epzicom)
Combivir is?
Zidovudine-lamivudine (Combivir)
____________ genes help the immune system recognize and respond to foreign substances
Human leukocyte antigen (HLA)
HLA-B*57:01 allele has been associated with hypersensitivity to ___________?
abacavir ( NNRTI)
Patient with symptoms suggestive of a hypersensitivity reaction to abacavir confirmed by _______________ had a positive HLA-B*5701 test
skin-patch testing
Abacavir hypersensitivity reaction that occurs in between ___________ of patients treated with the drug due to the positive HLA-B 5701
5% - 8%
Fusion inhibitors examples?
Enfuvirtide (Fuzeon
Aplaviroc
Vicriviroc
Maraviroc (CCR% and gp120 inhibitors,
Injection site pain, allergic reactions
Entry inhibitors examples?
CCR5 antagonist) (Maraviroc
hepatitis, rash
NRTIs examples?
Tenefovir / Emtricitabine
Abacavir / Lamivudine
NNRTIs examples?
Efavirenz
Integrase inhibitors examples?
Dolutegravir, Raltegravir, Elvitegravir
hepatitis, rash
Protease inhibitors examples?
Darunavir
primary therapy
Fusion Inhibitor class?
CCR5 antagonist class
Fusion Inhibitors block the _________ site?
Blocks gp120 site
The antiviral effect of _____ and ______ is essentially the same
NRTIs and NNRTIs
______ act on viral DNA synthesis where the process is halted, known as chain termination
NRTI’s
________ block reverse transcriptase by binding directly to the enzyme
NNRTI’s
NRTIs and NNRTIs both act in similar sites within the ____ cell
CD4 cell
Integrase inhibíos work where?
nucleus
Integrase Inhibitors MOA?
block the action of integrase enzyme
Integrase Inhibitors : Less integration of provirus = ?
less CD4 damage
Protease Inhibitors ?
Viral budding at envelope as exits from CD4 cell ( exit point?)
NRTI-sparing?
PI + NNRTI
Tenefovir / Emtricitabine / Dolutegravir?
(NRTI) + (Integrase Inhibitor)
Tenefovir / Emtricitabine / Raltegravir?
(NRTI) + (Integrase Inhibitor)
Tenefovir / Emtricitabine / Darunavir / Ritonavir ?
(NRTI) + (Protease inhibitor + booster)
*blocks the metabolizing enzyme in the liver - Ritonavir**
Tenefovir / Emtricitabine / Elvitegravir /cobicistat (inhibits liver enzymes) ?
(NRTI) + (Integrase Inhibitor / booster)
Abacavir / Lamivudine / Dolutegravir ?
(NRTI) + (Integrase Inhibitor)
Truvada ?
Tenefovir / Emtricitabine
Epzicom ?
Abacavir / Lamivudine
Stribild ?
Tenefovir / Emtricitabine / Cobicistat / Elvitegravir
Triumeq ?
Abacavir / Lamivudine / Dolutegravir
HIV primary medications generally prefer tenofovir - emtricitabine over ______-_______
abacavir-lamivudine
There is a greater body of evidence supporting the safety and tolerability of _________________
tenofovir-emtricitabine
HIV Drugs core?
NRTI’s
Baseline NRTI Strategies?
tenofovir-emtricitabine (Truvada)
abacavir-lamivudine (Epzicom)
zidovudine-lamivudine (Combivir)
NNRTI based Naive tx?
Efavirenz / tenofovir / emtricitabine
Rilpivirine / tenofovir / emtricitabine
Protease Inhibitor Based Biave tx?
Atazanavir + (cobicistat or ritonavir) + tenofvir / emtricitabine
Darunavir + cobicistat or ritonavir) + abacavir / lamivudine
Darunavir / cobicistat + tenofovir / emtricitabine
HIV: who to treat?
Recommend antiretroviral therapy (ART) be offered to HIV-infected patients, including asymptomatic individuals, regardless of their immune status.
Newer medications have fewer side effects and more safe
Stratigies for pregnancy, diabetics, HBV, HIVAN, high risk of transmitting virus to others
When to start HIV tx?
ART should be offered to those at risk of transmitting to:
- heterosexual partner
- other transmission risk groups
Patients with HIV starting ART should be willing and able to commit to tx and should understand the ________/_____ of therapy and importance of adherence
benefits / risks
Benefits of early HIV tx?
- Maintaining higher CD4 count to prevent damage to the immune system
- Decrease risk of HIV associated complications: Opportunistic infections, underlying inflammation
Decrease risk of transmission