HIV therapy Flashcards
What kind of drugs are drugs ending in NAVIR?
Protease inhibitors
What is the mechanism of protease inhibitors? Which gene is their product on?
HIV-1 protease (on pol gene) cleaves polypeptide products into functional parts. Protease inhibitors prevent maturation of new virus.
What distinguishes Ritonavir from other protease inhibitors?
Boosts other drug concentrations by inhibiting cytochrome P-450
What drug is contraindicated with protease inhibitors?
Rifampin (CYP/UGT inducer) decreases protease inhibitor concentration
What is the toxicity of protease inhibitors?
Hyperglycemia, GI intolerance (n/d), lipodystrophy
Nephropathy/hematuria (indinavir)
What is the mechanism of NRTIs?
Competitively inhibit nucleotide binding to
reverse transcriptase and terminate the DNA
chain (lack a 3′ OH group). Tenofovir is a
nucleoTide; the others are nucleosides and
need to be phosphorylated to be active.
What is zidovudine used for?
General ppx, during pregnancy to decrease risk of fetal transmission
What are the NRTIs?
when UDINE, EAT D food. -udine (stav,lamiv, zido) Emtricitabine Abacavir Tenofovir Didanosine.
What are the toxicities of the NRTIs?
Bone marrow suppression (give G-CSF + EPO) Peripheral neuropathy Lactic acidosis (nucleosides) Anemia (ZDV) Pancreatitis (didanosine)
What kind of drug is raltegravir?
Integrase inhibitor. Inhibits HIV genome integration in host cell chromosome by irreversibly inhibiting HIV integrase.
What is the toxicity associated with raltegravir?
Inc creatine kinase
What are the NNRTIs?
Delavirdine, Efavirenz, Nevirapine
What is the mechanism of NNRTIs?
Bind to reverse transcriptase at site different
from NRTIs. Do not require phosphorylation
to be active or compete with nucleotides.
What is the toxicity associated with NNRTIs?
Rash and hepatotoxicity are common to all
NNRTIs. Vivid dreams and CNS symptoms
are common with efavirenz. Delavirdine and
efavirenz are contraindicated in pregnancy.
What are the fusion inhibitors?
Enfuvirtide, Maraviroc
