Anti-Retroviral Drugs Flashcards
Name the NRTIs.
Abacavir Lamivudine Tenofovir Emtricitabine Zidovudine Didanosine Stavudine
Name the NNRTIs.
Nevirapine
Efavirenz
Name the protease inhibitors.
any drug that ends in "-navir": Atazanavir Ritonavir Darunavir Fosamprenavir Indinavir Lopinavir Saquinavir
Name the fusion inhibitors.
Enfuvirtide
Maraviroc
Name the integrase inhibitor.
Raltegravir
Describe the route, metabolism, and elimination of the NRTIs.
Route: oral 1-2x/day
Metabolism: minimal/no CYPs, some are glucuronide metabolites
Elimination: in urine as drug and metabolite
Describe the route, metabolism, and elimination of the NNRTIs.
Route: oral 1-2x/day
Metabolism: CYP interaction
Elimination: urine/stool as metabolites
What is the metabolism of Delavirdine?
3A4/2D6 substrate.
Inhibits 3A4, 2D6, 2C9, 2C10
What is the metabolism of Efavirenz?
Induces 3A4/2B6
What is the metabolism of Nevirapine?
Induces 3A4/2B6
Describe the route, metabolism, and elimination of the protease inhibitors.
Route: oral 1-2x/day
Metabolism: serious CYP interaction
Elimination: stool mostly as metabolites
What is the metabolism of Atazanavir?
Inhibits 3A4/UGT
What is the metabolism of Saquinavir?
Inhibits 3A4/UGT
What is the metabolism of Indinavir?
Inhibits 3A4; substrate of 3A4/P-gp
What is the metabolism of Fosamprenavir?
Inhibits 3A4; substrate of 3A4/2D6/2C9/P-gp
What is the metabolism of Ritonavir?
Inhibits 3A4/2D6/P-gp/UGT
What is the metabolism of Lopinavir?
substrate for 3A4
What is the metabolism of Darunavir?
substrate for 3A4
What is the special HAART drug that is NOT given orally, and how is it given?
Enfuvirtide - given subcutaneously
Describe the route, metabolism, and elimination of the integrase/fusion inhibitors.
Route: orally 1-2x/day (except enfuvirtide)
Metabolism: different, only Maraviroc has CYP interactions
Elimination: stool/urine as drug and metabolites (except enfuvirtide)
What is the metabolism of Enfuvirtide?
catabolized to amino acids
What is the metabolism of Maraviroc?
3A4/P-gp substrate
What is the metabolism of Raltegravir?
glucuronide metabolite
What is cobicistat and what is it used for?
it’s an orally active 3A4 inhibitor and it’s used as a pharmacokinetic enhancer to increase the serum concentration of CYP3A substrates, such as the protease inhibitors atazanavir and darunavir
What is Atripla?
a once daily pill that constitutes a complete ART drug regimen; includes tenofovir, emtricitabine, and efavirenz
What are the contraindications/BBW of Abacavir?
contra: hypersensitivity and hepatic disease
BBW: lactic acidosis
What are the BBW of Didanosine?
hepatic disease, lactic acidosis, neuropathy, pancreatitis
What are the BBW of Emtricitabine?
hepatic disease, lactic acidosis, neuropathy
What are the BBW of Lamivudine?
hepatic disease, lactic acidosis, neuropathy
What are the BBW of Stavudine?
hepatic disease, lactic acidosis, neuropathy (MOST), pancreatitis
What are the BBW of Tenofovir?
hepatic disease, lactic acidosis, neuropathy, pancreatitis
What are the BBW of Zidovudine?
anemia, myopathy, neutropenia
What NNRTI has the most BBWs and what are they?
Nevirapine - hepatic disease (X), hypersensitivity (X), hepatitis, serious rash, females
Rash and hepatotoxicity are common to all members of what class?
NNRTIs
Efavirenz carries what weird toxicities?
CNS toxicities and vivid dreams
What 2 HAART drugs are contraindicated in pregnancy?
Delavirdine and Efavirenz
What are the major side effects of protease inhibitors?
GI intolerance, lipodystrophy, hyperglycemia/DM, dyslipidemia, nephrolithiasis (most common with indinavir), severe rash including SJS
Describe the role of peripheral neuropathy in HIV and HAART.
its a consequence of HIV infection of macrophages in the DRG and neuronal injury related to gp120; toxic peripheral neuropathy is a long term side effect of HAART (NNRTIs, NRTIs, and some PIs)
What are the recommended agents to prevent pneumo jiroveci?
Trimethoprim-Sulfamethoxazole
What are the recommended agents to prevent m. TB?
Isoniazid and Pyridoxine
What are the recommended agents to prevent toxoplasmosis?
Trimethoprim-Sulfamethoxazole
What are the recommended agents to prevent CMV?
val/gangciclovir
What are the recommended agents to prevent fungal infections?
Fluconazole
What drugs are used against CMV?
valganciclovir (PO), ganciclovir, foscarnet, cidofovir (last 3 = IV)
What are side effects of valganciclovir?
leukopenia, neutropenia, renal toxicity
What is the MOA and major toxicity of foscarnet?
viral DNA polymerase inhibitor; nephrotoxicity (hydrate patient before administration)
What is vidarabine and what is it used to treat?
nucleoside analog; treats EBV infection, applied to eye as ointment
What drug is given to treat KSHV?
Cidofovir, IV
also other anti-virals: ganciclovir, valganciclovir,
