HIV Drugs Flashcards
(36 cards)
What’s the goal of therapy in HIV?
maximally inhibit viral replication and reduce viral RNA to undetectable levels
After therapy is initiated, an increase in viral load may indicate what?
drug resistance
What’s the general strategy in terms of drug combo in adults who have never been treated for HIV before?
one of these: NNRTI, protease inhibitor, or integrase inhibitor
plus a dual combo of NRTIs
What are the four nucleoside reverse transcriptase inhibitors we know?
zidovudine (AZT)
lamivudine
emtricitabine
abacavir
What’s the mechanism of the NRTIs?
they competitively inhibit reverse transcritase and can be incoporated into viral DNA chain and cause termination
What do the NRTIs need in order to become active?
they need to be phosphorylated by cellular enzymes to the trphosphate form in order to be active
What are the general adverse affects of the NRTIs?
you can get a potentially fatal syndrome of lactic acidosis with hepatis steatosis
this is likely due to mitochodnrial toxicity
they’re also associated with fat redistribution and thus, hyperlipidemia
What are th emore specific side effects for zidovudine?
granulocytopenia and anemia - in up to 45% of patient!
also CNS disturbances: severe headache, insomnia, malaise
nausea
What’s the specific side effect for abacavir?
hypersensitivity reactions
What’s the one NUCLEOTIDE reverse transcriptase inhibitor
tenofovir
What’s the mechanism of action for tenofovir?
same as the nucleosides - chain terminator
What’s the adverse effects of tenofovir?
nausea, vomiting, diarrhea and potential for renal failure
fatal lactic acidosis has been reported
WHat are the two non nucleoside reverse transcriptase inhibitors?
efavirenz and etravirine
What’s the mechanism for efavirenz and etravirine?
they bind directly to the reverse transcriptase enzyme at a distinct side and render it unable to produce viral DNA
True or false: the non nucleoside reverse transcriptase inhibitors do not require phosphorylation like the nucleoside RT inhibitors do.
true
Are the NNRTIs more effective against HIV1 or 2?
HIV-1
What are the general adverse effects of the NNRTIs?
severe rashes
metabolized by cyp450 - drug interactions
Which NNRTI has the specific side effect of vivid dreams, nightmares and hallucinations?
efavirenz
What are the more specific side effects for etravirine?
rash, nausea, peripheral neuropathy
What are the three protease inhibitors?
atazanavir
ritonavir
darunavir
What’s the mechanism of the protease inhibitors?
they ihibit protease, so the pre-proteins don’t get cleaves to the necessary proteins for the virus
this means the virus is no longer infectious because new viral particles cannot mature
What are the adverse effects of the protease inhibitors?
GI disturbances hepatotoxicity hyperglycemia insulin resistance hyperlipidemia peripheral lipoatrophy and central fat accumulation metabolized by/inhibit CYP3A4
Which protease inhibitor is poorly tolerated at high doses, so it’s given to increase the serum concentrations of other protease inhibitors, thus decreaseing their dosage frequency?
ritonavir
HOW does ritonavir increase the serum concentrations of the other protease inhibitors?
it’s a potent inhibitor of CYP3a4, which metabolizes the other proteases to decrease their effectiveness
