HIV drugs Flashcards
What is the advantage to using drugs from different classes?
- Synergy
* Decreased Resistance
What is the typical way that HAART therapy is prescribed, in terms of mechanism of action?
Give:
• 2 NRTI’s + (NNRTI or protease inhibitor or integrase inhibitor)
What should you do first if detect through western blot and elisa that a patient is relapsing despite HAART therapy?
- Ask if they are actually taking the therapy
2. Perform Resistance Testing
Before initiating therapy with miravoc what should you do?
• Make sure they are CCR5+, otherwise the drug is useless
NRTI’s and NNRTI’s act on what step in the HIV life cycle?
Reverse Transciption
• These are (Non) Nucleotide Reverse Transciption inhibitors
What drugs act as NRTI’s?
• are the competitive or non-competitive inhibitors?
• Do they work on HIV-1 and 2?
ABACAVIR LAMIVUDINE (3TC) TENOFOVIR (TDF) EMTRICIBINE ZIDOVUDINE (AZT)
Inhibition:
• Competitive
Tropism:
• Work on HIV 1 and 2
What drugs act as NNRTIs?
• are the competitive or non-competitive inhibitors?
• Do they work on HIV-1 and 2?
EFAVIRENZ
NEVIRAPINE
DELAVIRDINE
Inhibition:
• Non-competitive
Tropism:
• Work on HIV 1
What drugs act as protease inhibitors?
• are the competitive or non-competitive inhibitors?
• Do they work on HIV-1 and 2?
the -navirs
ATAZNAVIR
RITONAVIR
Inhibition:
• Competetive
Tropism:
• HIV 1 ONLY
What drugs act as Fusion inhibitors?
• are the competitive or non-competitive inhibitors?
• Do they work on HIV-1 and 2?
ENFUVIRTIDE - HIV-1 ONLY
MARAVOC - CCR5+ ONLY
What drugs act as integrase inhibitors?
RALTEGRAVIR
DOLUTEGRAVIR
NRTIs • Administration • Metabolism • Standouts??? • Drugs?
Administration:
• Oral
Metabolism:
• No Significant CYP interactions
Standouts:
• Abacavir - is metabolized by ALCOHOL DEHYDROGENASE (don’t drink with it)
ABACAVIR LAMIVUDINE (3TC) TENOFOVIR (TDF) EMTRICIBINE DIDANOSINE STAVUDINE ZIDOVUDINE (AZT
NNRTIs • Administration • Metabolism • Standouts??? • Drugs?
Administration:
• Oral
Metabolism:
• Delavirdine - weakly CYPS
• Efavirenz, Nevirapine - INDUCE CYPS
Which NNRTIs might cause unwanted pregnancy?
• why?
Efavirenz, Nevirapine
• They INDUCE CYP3A4 and CYP2B6 which can lead to ORAL CONTRACEPTIVE FAILURE
What happens to drug metabolism when you give a patient Rifamin and Rifabutin, what would you have to do to counteract this?
• is it okay to give NNTRI’s with this?
Rifampin and Rifabutin
• Known PAN-INDUCERS of CYP
Efavirenz OKAY to give with these but you need to UP THE DOSE
What class of drugs should you NEVER give rifampin with? • Why?
PROTEASE INHIBITORS - the “-navirs”