Micro 25 - HIV Drugs Flashcards
When should HAART start?
Initiation: everyone with HIV regardless of CD4 count; definitely in anyone with a CD4 count less than 200.
What are some protease inhibitors?
All end in “navir”
Saquinavir Ritonavir Indinavir Nelfinavir Fosamprinavir Lopinavir Tipranavir Atazanavir Darunavir
How do protease inhibitors work?
Protease takes polypeptides that were translated from the HIV mRNA and chops them into individual functioning proteins in order to allow new infectious virus to form. So these drugs prevent development of new viruses by halting the replicative process.
Which type of HIV Drug or class causes GI intolerance?
Protease inhibitors.
Which type of HIV Drug or class causes inhibit cytochrome P450?
Protease inhibitors, especially ritonavir. Used to increase the concentration of other HIV drugs.
Which type of HIV Drug or class causes hyperlipidemia/hypertryglyceridemia?
Protease Inhibitors
Which type of HIV Drug or class causes lipodystrophy?
Protease inhibitors.
Which type of HIV Drug or class causes pancreatitis?
Ritonavir
Which type of HIV Drug or class causes nephrolithiasis?
Indinavir, atazanavir.
Which type of HIV Drug or class causes increased bilirubin?
Atazanavir.
What is HAART?
Highly Active Antiretroviral Therapy: Combination of at least 3 different HIV medications to avoid resistance. Usually combines 2 nucleoside reverse transcriptase with 1 from a different class of med.
What are NRTIs.
Nucleoside Reverse Transcriptase Inhibitors: They inhibit HIV reverse transcriptase, preventing the virus from replicating. They are all nucleoside analogs (guanicine analogs or cytocine analogs): when the virus needs a guanicine or cytocine, it grabs a NRTI, binding right into the reverse transcriptase functional side (called competitive inhibition), shutting it down. So NRTIs are competitive inhibitors for reverse trancriptase and musr be phosphorylated or activated by thymidine kinase in order to work.
What are some NRTIs?
Zidovudine AZT Didanosine DDI Lamivudine 3TC Abacavir ABC Emtricitabine FTC Tenofovir TDF Zalcitabine DDC
What is AZT and what are its use recomendation?
It Zidovudine and it is a NRTIs. It is used mainly in newborns born to HIV (+) mother, given to the mother at the time of delivery if she hasn’t been following her anti HIV regiment; if she has, then does not need to take AZT.
What is the treatment of occupational exposure to AIDS?
A 3 drug regiment for 4 weeks.
Which NRTI causes Bone marrow suppression?
Most of them but especially Zidovudine.
Which NRTI causes pancreatitis and peripheral neuropathy?
Didanosine, Zalcitabine, stavudine.
Which NRTI causes hepatic steatosis?
Didanosine, stavudine.
Which NRTI causes hypersensitivity reaction?
Abacavir
What are some Non-nucleoside reverse transcriptase inhibitors (NNRTIs)?
Nevirapine Delavirdine Efavirenz Etravirine Rilpivirine
How do NNRTIs work?
Non-competitively inhibit reverse transcriptase. They do not require phosphorylation to be active (doesn’t required thymodine kinase).
What HIV/AIDS drug causes rash?
NNRTIs.
What HIV/AIDS causes Neuropsychiatric symptoms (nigthmares, vivid dreams, dizziness, worsening depression)?
Efavirenz.
What HIV/AIDS causes false-positive drug test to cannabinoids?
Efavirenz.
What HIV/AIDS causes teratogenic effects?
Efavirenz
What is Enfuvirtide and what does it do? And what is the catch of this drug?
A fusion inhibitor. Binds to gp41, inhibiting the virus from fusing to the host cell. Can only be given by injection and costs a lot, given in drug resistant AIDS.
What are Elvitegravir and Raltegravir and what does they do?
It is an integrase inhibitor in HIV. Raltegravir can cause nausea, rash and myopathy.
What does Maraviroc do and what is the catch?
CCR5 antagonist (macrophages have a lot of these receptors). It inhibits gp120 conformational change so virus cannot bind host cell effectively. Patients must go through a trophism test to see that the patient has an CCR5 virus and not an CXR4 virus: this drug can only be used in patients with all R5 virus.
What is Ritonavir?
Protease inhibitor.
What is Didanosine?
NRTI.
What is Delavirdine?
NNRTI.
What is Zidovudine?
NRTI.
What is Abacavir?
NRTI.
What is Lamivudine?
NRTI.
What is Nelfinavir?
Protease inhibitor.
What is Efavirenz?
NNRTI.
What drug interferes with gp41?
Enfuvirtide.
What drug interferes with gp120?
Maraviroc (only on CCR5 virus).
What HIV/AIDS drug causes lactic acidosis?
NRTIs.
What HIV/AIDS drug cause GI intolerance?
Protease inhibitors.
What HIV/AIDS drugs can cause pancreatitis?
Didanosine, ritonavir.
What HIV/AIDS drug can cause peripheral neuropathy?
Didanosime, stavudine, zalcitabine.
What HIV/AIDS drug can cause megaloblastic anemia?
Zidovudine.
What HIV/AIDS drug can cause rash?
NNRTIs.
What HIV/AIDS drug can cause hyperglycemia, DM, and lipid abnormalities?
Protease inhibitors.
What HIV/AIDS drug can cause bone marrow suppression?
Zidovudine.
Which class of HIV drugs causes redistribution of fat into a buffalo hump on the back of the neck?
Saquinavir and ritonavir.
