HIV Drugs Flashcards
What classes of drugs are selected in a HAART cocktail?
2 nucleoside reverse trascriptase inhibitors (NRTIs) \+ one of the following 1 non-NRTI 1 protease inhibitor 1 integrase inhibitor
NRTIs must be phosphorylated by kinases to form ________, which inhibit Reverse Transcriptase because they __________
- synthetic nucleotides
- lack a 3’ OH group, thus terminating the growing DNA chain
As with all nucleotide analogues, the primary side effect of NRTIs is __________
Bone marrow suppression
why? bone marrow, hair follicles, and epithelia are LABILE tissues that never enter G0 phase
Peripheral neuropathy also common
Mutations in what HIV gene will cause resistance to NRTIs?
pol gene
this gene contains RT, proteases, and integrases
Zidovudine (AZT, ZDV) is a ______ analogue
thymine
Didanosine (ddI) is a _____ analogue
Inosine (which is a purine precursor; A+G)
Stavudine (d4T) is a _______ analogue
thymine
Emtricitabine (FTC), Abacavir (ABC), and Lamivudine (3TC) are ________ analogues.
cytosine
How do NNRTIs differ from NRTIs in their mechanism of action.
Both attack RT, NNRTIs bind @ allosteric site
NNRTIs are non-nucleoside, so they do not cause myelosuppression!
What are some side effects of the NNRTI Nevirapine?
induces cyp450 (drug interactions) causes rash, minor elevation in liver enzymes
(big in reducing vertical transmission)
What are some side effects of the NNRTI Efavirenz?
causes insomnia and nightmares
Protease inhibitors work by inhibiting what specific enzyme on what HIV gene?
aspartate protease
pol gene
Protease inhibitors share what common ending?
-NAVIR
Ex: ritonavir, Indinavir, atazanivir
What are some common side effects with the protease inhibitors?
- cytochrome p450 inducers (drug interactions)
- dyslipidemia
- hyperglycemia/diabetes mellitus II
Integrase inhibitors such as ________ can cause side effects of ________
- Raltegravir
- hypercholesterolemia
ralTEGRAvir = inTEGRAse inhibitor
