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Anti-HIV Agents: Reverse Transcriptase Inhibitors (NNRTI) – Antiviral Drugs

by Pravin Shukle, MD
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    Let's move on to the Non-Nucleoside Reverse Transcriptase Inhibitors. So these are a little bit different from the NRTIs. They bind on a different site. They do no require phosphorylation to be activated. And there is no cross resistance with the nucleoside reverse transcriptase inhibitors. We have use these agents as monotherapy. But if we do use as monotherapy, resistance develops quite quickly. So we try not to if possible used it as monotherapy. Now monotherapy occurs through a mutation in the pol gene. So this is something that does show up on the exams. It's worthwhile remembering that the pol gene codes for a mutation that can cause a resistance to the non-nucleoside reverse transcriptase inhibitors. Now one of the first agents that I'm going to talk about more for alphabetical reasons than usage reasons is delavirdine. It's got a lot of drug interactions because it's metabolised through cytochrome, sorry cytochrome P450. The 3A4 and the 2D6 isoenzymes. So there's a lot of drug interactions that we have be concerned about. These include the azoles and macrolides which can increase their blood levels. And they can also be decreased by things like antacids, by ddI, by phenytonin, rifampin. So there's all kinds of agents that will reduce their dosages as low as well. The other thing that is concerning with this patient on this medication is that if they are also on warfarin, it will effect the INR values. Toxicity with this agent, you can get a skin rash and up to one-fifth of all patients. So it is a significant level of skin rash. And of course we can't use this agent in pregnancy. EFV can be given once a day. It's metabolized by cytochrome as well. So there are going to be some drug interactions too. In...

    About the Lecture

    The lecture Anti-HIV Agents: Reverse Transcriptase Inhibitors (NNRTI) – Antiviral Drugs by Pravin Shukle, MD is from the course Antimicrobial Pharmacology.


    Author of lecture Anti-HIV Agents: Reverse Transcriptase Inhibitors (NNRTI) – Antiviral Drugs

     Pravin Shukle, MD

    Pravin Shukle, MD


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