Anti-Retroviral Pharm Flashcards
What drugs are in the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTIs) class?
Delavirdine, Efavirenz, Nevirapine, Etravirine, Rilpivirine
What is the MOA of NNRTIs?
Bind HIV reverse transcriptase causing inhibition of RNA/DNA-dependent DNA polymerase
How is resistance created to NNRTIs?
Point mutations that alter NNRTI binding
What is the main SE of Delavirdine?
Skin rash
What are the SE’s of Efavirenz?
CNS issues
Skin rash
Hypercholesterolemia
What are the SE’s of Nevirapine?
Rash
Liver toxicity
What are the SE’s of Etravirine*?
Rash
Nausea
Diarrhea
What are the SE’s of Rilpivirine*?
Rash Depression HA Insomnia Increased aminotransferases
Which NNRTI can be used to prevent transmission from mother to newborn?
Nevirapine
Which NNRTI can be used after the first 8 weeks of gestation?
Efavirenz
Which NNRTI can be used during all of pregnancy?
Rilpivirine
What is the suffix of the drugs in the Protease Inhibitor (PI) class?
-navir
What is the MOA of the PIs?
Block HIV proteases –> prevention of maturation of proteins that make up virion core
Which PIs can be used during pregnancy?
Atazanavir/Darunavir (if boosted)
Lopinavir
What are the SE’s of Atazanavir?
Diarrhea, nausea, skin rash, jaundice
What are the SE’s of Darunavir?
Rash, sulfa hypersensativity
What are the SE’s of Fosamprenavir?
HA, nausea, diarrhea, depression, sulfa hypersensitivity
What are the SE’s of Indinavir?
Hyperbilirubinemia (jaundice), nephrolithiasis
What must the pt do to avoid stone formation when taking Indinavir?
Drink lots of water
How is Darunavir given?
Co-administered with Ritonavir or Cobicistat
What are the SE’s of Lopinavir?
None
What are the SE’s of Nelfinavir, Ritonavir, and Saquinavir?
GI issues
What are the SE’s of Tipranavir?
GI issues, maculopapular rash, sulfa hypersensitivity
Which PIs should not be given to pts with sulfa allergies?
Darunavir, Fosamprenavir, Tipranavir
Which PI is used mainly as a booster because it is a potent CYP450 inhibitor?
Ritonavir
Which PI is used for Tx of Tx-experienced pts who have resistant HIV strains?
Tipranavir
Which drug is in the Fusion Inhibitor class?
Enfuvirtide
What is the MOA of Enfuvirtide?
Binds gp41 preventing fusion of viral envelope to host cell membrane
How is resistance created to Enfuvirtide?
Mutations in gp41
When is Enfuvirtide used?
As salvage Tx
How is Enfuvirtide administered?
SubQ injection 2x daily
What drug is in the Entry Inhibitor class?
Maraviroc
What is the MOA of Maraviroc?
Binds CCR5 preventing viral entry into the host cell
How is resistance created to Maraviroc?
Mutations in V3 loop of gp120
What are the SE’s of Maraviroc?
Possible hepatotoxicity
What is the suffix for the drugs in the Integrase Strand Transfer Inhibitor (INSTI) class?
-tegravir
What is the MOA of INSTIs?
Inhibit integration of reverse-transcriptase HIV DNA into host DNA
Which INSTI has some SE and what is the SE?
Dolutegravir;
Hypersensitivity rxn
Which INSTI can be used during pregnancy?
Raltegravir
Which INSTI is used for Tx of Tx-naive pts with HIV?
Dolutegravir
Which INSTI requires a booster with Cobicistat?
Elvitegravir
