anti HIV Flashcards
Need tropism assay
Maraviroc
NRTI with hypersensitivity
Abacavir: due to genetic disposition
NRTI with highest side effect of lactic acidosis and hepatic steatosis due to mitochondrial toxicity? Lowest?
highest: stavudine
lowest: lamivudine, emtricitabine
Two NRTIs that are antagonistic of each other
stavudine, zidovudine
lamivudine, emtricitabine
main toxicity of NNRTI
rash on trunk and extremities
What can tenofovir be combined with to create increased effects against HIV? What is the significance?
Combined with emtricitabine (Truvada)
Used as initial HIV therapy, extending time to virologic failure and first adverse event.
**1st effective antiretroviral chemoprophylaxis before exposure (infection prevention!)
major toxicity of Nevirapine
hepatoptoxicity: increased liver enzymes
severe and life-threatening
2 major toxicities of efavirenz
neuropsychiatric
teratogenic (Category D)
HIV-1 specific
raltegravir
NNRTIs
maraviroc
What inhibits the UGT? What anti-HIV does this affect?
atazanavir inhibits
raltegravir is metabolized by UGT
What is the most effective ART available?
protease inhibitors
What two PIs are used in conjunction to increase effects up to 100x?
Ritonavir increases Lopinavir’s effects 100x
Do NRTIs have to be phosphorylated?
yes, by cellular kinases
Do NNRTIs have to be phosphorylated?
no!
First line of NRTI in HAART
tenofovir+emtricitabine OR zidovudine+lamivudine
**emtri/lam can be used in place of each other
anti-HIV BM suppressor
zidovudine
anti-HIV: peripheral neuropathy
didanosine, stavudine
anti- HIV: pancreatitis
didanosine (dose limiting), stavudine, lamivudine (kids), ritonavir
anti-HIV: nephrotoxicity
indinavir
anti-HIV: hepatotoxicity
NNRTIs, NRTIs, PIs
*life-threatening in nevirapine
anti-HIV: rash
abacavir, NNRTIs
anti-HIV: diarrhea
didanosine, nelfinavir, ritonavir, lopinavir/ritonavir
anti-HIV: ocular effects
didanosine
What is needed for ARV regimen?
3 drugs from at least 2 classes
What is different about NRTIs from their analogs that makes them effective?
3’ hydroxyl end is replaced by azido, hydrogen, etc. which terminates the synthesis of the chain
What type of anti-HIV are used as secondary therapy when resistance occurs?
intgrase inhibitors (raltegravir)
What is used in conjuction with HAART to increase effectiveness?
Fusion inhibitors (enfuvirtide, maraviroc)
What type of cells do NRTIs have the greatest effect on?
Those that have not yet been infected, but are susceptible
What anti-herpesvirus drug interacts with didanosine? What is the end effect?
Ganciclovir increases didanosine plasma concentration x2
First line of NNRTI in HAART
efavirenz
*avoid in prego
First line of PI in HAART
atazanavir + ritonavir, fosamprenavir + ritonavir (BID), OR lopinavir/ritonavir (BID)
What are NNRTIs excreted as?
glucuronide conjugates
What drug can cause anemia? How can it be alleviated?
Zidovudine can cause anemia in children. Offset by EPO administration