HIV drugs Flashcards
(37 cards)
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”
What group of HIV drugs should come to mind when you think about CYP issues?
PROTEASE INHIBITORS - the “-navirs”
Which of the protease inhibitors might you give if you’re trying to increase the concentration or prolong the effect of a drug in the bloodstream?
RITONAVIR
Suppose you begin taking a drug X (a cyp metabolized drug) for migraines and begin taking rifampin, what would you expect to happen?
• What HIV Drug might have the opposite effect?
- Headaches would come back, you would see a recurrence of symptoms due to induction of CYPs by rifampin
- RITONAVIR (protease inhibitor)
What the the ONLY HIV drug given subcutaneously?
ENFUVIRTIDE
Fusion and Integrase inhibitors
• Name them
• Administration?
MARAVIROC
ENFUVIRTIDE
RALTEGRAVIR (integrase inhibitor)
What is the point of giving Cobicistat?
• Orally active CYP3A4 inhibitor that can be given to increase the serum concentration of drugs like Ataznavire (a weak CYP inducer)
Besides Rifampin what other antimicrobials tend to have major effects on when given with HIV drugs, specifically RITONAVIR?
• What other HIV drugs is this drug contrainidcated with?
• Voriconazole - inhibits CYP2C9 (a little) and CYP3A4 (a lot)
- *ALL Protease Inhibitors Contraindicated
- *NNRTIs contratindicated
Activity of Rifampin vs. Rifabutin
RIfampin is a much intense inducer of CYP
What Black Box Warnings are associated with all of the NNRTIs?
• which has the most black box warnings?
• What raises your risk for experiencing these effects?
BBWs:
• Hepatic Disease
• Lactic Acidosis
• Neuropathy
ZIDOVUDINE - has the most, also causes Anemia, myopathy, and neutrapenia
RISK FACTORS:
• Being Obese
• Being a woman
