HIV Drugs Flashcards
Name the “entry inhibitors.”
Enfuviritide
Maraviroc
Enfuviritide MOA.
Peptide that binds to gp41 and prevents membrane fusion
Maraviroc MOA.
CCR5 antagonist
Name the nucleoside reverse transcriptase inhibitors: NRTIs.
Abacavir Lamivudine Tenofovir disoproxil Zidovudine (AZT) Emtriciatbine Didanosine Stavudine
MOA of NRTIs.
Prodrugs converted to triposphates that competitively inhibit binding of natural nucleotides to dNTP-binding site of reverse transcriptase AND act as chain terminators via insertion into growing strand.
Why do NRTIs stop growing DNA strand?
they lack 3’ hydroxyl group
Name the non-nucleoside reverse transcriptase inhibitors: NNRTIs.
Efavirenz
Nevirapine
MOA of NNRTIs.
bind to a site on reverse transcriptase different than NRTIs and do NOT compete with nucleoside triphosphates but simply inhibit it
List the HIV-1 protease inhibitors.
Atazanavir
Ritonzvir
Amprenavir
other “navir”s
MOA of HIV-1 protease inhibitors.
inhibit the viral protease processing of proteins to “mature them”
List the DNA strand transfer inhibitor.
Raltegravir
MOA of Raltegravir.
Binds to integrase and inhibits integration of viral dsDNA into host genome
What is the only anti-HIV drug that is NOT taken orally?
enfuviritide
What drugs have UGT conjugation?
abacavir
emtricitabine
atazanavir
raltegravir
What drug has metabolism by alcohol dehydrogenase?
abacavir
What drug has metabolism by oxidation?
emtricitabine
What drug is catabolized to amino acid?
enfuvirtide
What drugs are you worried about CYP interactions?
NNRTIs
PIs
Maraviroc
What drug is a P-gp substrate?
maraviroc
Why do you need to genotype HIV viruses?
There are different serotypes of the virus. You cannot assume that the viral infection your patient has is a naïve virus!
What antifungals do you need to avoid with CYP metabolized HIV drugs?
voriconazole is a CYP inhibitor
What antibiotics do you need to avoid with CYP metabolized HIV drugs?
rifampin/rifabutin is an inducer
may need to double the dose
What herb do you need to avoid with CYP metabolized HIV drugs?
St. John’s Wort (inducer of CYP)
What herb/food do you need to avoid with saquinavir?
garlic will have interaction with saquinavir
What 2 adverse effects are broadly seen with HAART therapy? Why?
ALMOST ALL HIV DRUGS LEAD TO PERIPHERAL NEUROPATHY (dysfunciton of mitochondrial oxidative metabolism)/LIPODYSTROPHY!!!
Why do you give ritonavir with low doses with other PIs?
Ritonavir used in low doses as a BOOSTER so you can give other PIs with it at lower doses/increase their effectiveness
What adverse effects are commonly seen with NRTIs?
May also cause lactic acidosis!! May also cause hepatic disease/pancreatitis! RASH.
Nevarapine is contraindicated with what?
NOT with hypersensitivity and hepatic disease.
Abacavir is contraindicated with what?
NEVER take abacavir with hypersensitivity and hepatic disease!!!
What drugs rely on an acidic environment to be absorbed?
ataznavir and raltegravir
When taking a protease inhibitor, what should you be concerned about?
THINK OF CARDIOTOXICITY!! (also hypokalemia and other lowered ions)
What drugs have carb/lipid metabolism effects and hepatotoxicity?
protease inhibitors
What NRTIs are recommended for pregnant women?
lamivudine, zidovudine
What NNRTIs are recommended for pregnant women?
nevirapine
What PIs are recommended for pregnant women?
Lopinavir
Ritonavir
Prophylaxis for pneumocystis jiroveci.
trimethoprim-sulfamethoxazole
Prophylaxis for M. tuberculosis
isoniazid + pyridoxine
Prophylaxis for Toxoplasmosis
trimethoprim-sulfamethoxazole
Prophylaxis for CMV
ganciclovir
Prophylaxis for fungal infections and yeast infections.
Fluconazole
