Flashcards in Antiretroviral Agents Deck (44)
This step of HIV replication involves binding of HIV to receptors on the surface of CD4 T cells.
This step in HIV replication involves the use of an enzyme to convert HIV RNA into DNA which then migrates to the host nucleus.
This step in HIV Replication involves the use of an enzyme to insert viral DNA into host DNA
INTEGRATION VIA INTEGRASE
This step in HIV replication involves creation of new viral rna
This step in HIV replication involves transformation into immature, noninfectious HIV particle or bud
This step in HIV replication involves cutting of the long HIV polyprotein chains into smaller functional HIV proteins to make mature infectious viral particle
BUDDING & MATURATION
This drug class blocks entry of CCR5-tropic viruses into the CD4 T cell. Give the only approved drug in this class.
Drugs in this class bind to envelope gp41 to prevent viral fusion to the CD4 T cell. Give the only approved drug of this class.
This drug class is known as the backbone of the ART regimens
NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
What is the MOA of NRTIs?
Undergoes intracellular phosphorylation
Active triphosphate bunds to reverse transcriptase
DNA elongation is terminated after incorporation of NRTI triphosphate
What 3 NRTIs should not be used as monotherapy for Hepatitis B? Why?
Risk of HBV resistance after prolonged use.
HBV flares after discontinuation
What are the 2 ADR of NRTIs?
Mitochondrial toxicity which may present as peripheral neuropathy, pancreatitis, lipoatrophy, and hepatic steatosis.
Lactic acidosis syndrome
NRTIs have drug to drug interactions with?
It decreases the concentration of Tenofovir
This NRTI is commonly combined with Emtricitabine.
If combined with Emtricitabine, considered as superior to other NRTI combi
Tenofivir Disoproxil Fumarate (TDF)
This NRTI combi is effective in decreasing HIV transmission when administered as pre-exposure prophylaxis to HIV-uninfected patients
Tenofovir Disoproxil Fumarate + Emtricitabine (TDF/FTC)
What are the main toxicities of Tenofovir Disoproxil Fumarate (TDF)?
Kidney Injury and Bone Loss
*do not give in px with GFR <60mL/min
What is the NRTI approved for use in patients with GFR of less than/equal ti 30mL/min
Tenofovir Alafenamide (TAF)
What are the 2 drugs that if combined with TAF, increases TAF levels?
Cobicistat or Ritonavir
How do Cobicistat and Ritonavir increase TAF bioavailability?
They inhibit intestinal P-glycoprotein
This NRTI in combination with Lamivudine is considered as first line NRTI combination for HIV
Abacavir-lamivudine combination has the greatest efficacy if combined with?
This NRTI is not given to patients with CAD because it increases risk for hyperlipidemia and vascular events
These NRTIs should not be used in combination because they will compete for intracellular phosphorylation
Lamivudine & Emtricitabine
What is the adr of lamivudine?
Pancreatitis. More severe in children
What is the adr of Emtricitabine?
Skin changes: hyperpigmentation of palms and soles
NNRTIs for tx-naive patients are?
Efavirens and Rilpivirine
NNRTI for drug-resistant px is?
What is the MOA of NNRTIs?
Prevents HIV-1 Reverse Transcriptase from adding new nucleotides to the growing DNA chain. Blocks cDNA elongation
True or False: NNRTIs are active against both HIV-1 and HIV-2.
False. Only vs HIV-1
What happens when an NNRTI-containing regimen is discontinued?
A period if functional NNRTI monotherapy may occur
What happens in a Functional NNRTI Monotherapy?
This happens when an NNRTI-containing regimen is discontinued.
NNRTI concentrations decline slower than other retrovirals. Therefor increasing the risk for NNRTI resistance
What is the remedy for the Functional NNRTI Monotherapy?
Once an NNRTI-containing regimen is stopped, the concomitant nucleoside backbone should be continued for 3-7 days after the NNRTI is discontinued
What are the adr of efavirenz and rilpivirine?
Neurologic and Psychologic
This NNRTI is given at a dose of 600mg OD. High-fat/high-caloric meals increase absorption.
Why shouldn't Efavirenz be initiated in women who are likely to become pregnant or are in the 1st 8 weeks of pregnancy?
Potential risk for NTDs, facial clefts, and anopthalmia. But it can be used later in gestation
What are the side effects of Efavirenz?
Cns toxicity, rash, hyperlipidemia, elevated hepatic transaminase
What are the advantages of efavirenz combined with TDF/FTC?
Low pill burden
This NNRTI may be used in tx-naive px with a baseline viral load <100,000 copies/mL and a CD4 count of morethan or equal to 200 cells/microL.
What are the side effects of Rilpivirine?
Rilpivirine must be administered with a meal and concimitant use of rilpivirine with ____________ & ___________ is contraindicated
Drug to drug interactions of rilpivirine
Rifampin, phenytoin, phenobarb, azoles, macrolides
This is the most commonly used NNRTI for px with drug-resistant virus
This drug class is an attractive option for px with either abn lipid profiles or risk factors for CAD since they have neutral effects on cholesterol & triglycerides