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Anti-HIV Agents: Integrase Strand Transfer Inhibitors – Antiviral Drugs

by Pravin Shukle, MD

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    00:01 Now the next category of drugs is a fairly large one.

    00:05 It’s the integrase inhibitors.

    00:07 If you go back to our original slide looking at the entry of the virus into the cell, the integrase helps viral DNA get integrated into host DNA, so it’s an important part of the replication cycle.

    00:22 There's a lot of drugs in this category.

    00:24 You can see them here, I'm not going to go through them individually but there's just a very, very long list.

    00:31 We use these agents in treatment-naïve patients.

    00:35 What that means is that a patient who comes into the HIV clinic as a new patient and has never been put on anti-HIV medications this is one of the medications we’ll often use.

    00:47 It is not metabolized through the cytochrome system but it does undergo glucuronidation.

    00:53 Go back to the original pharmacology lectures to see what that means.

    00:58 If it’s used with rifampin and remember, that rifampin isn't just an inducer of cytochrome, it also induces UDP glucuronyl transferase, doses should be doubled.

    01:10 It binds with integrase that is both common and essential to HIV-1 and HIV-2 virus particles so it works in both categories. It inhibits the transfer of genetic material and it interferes with the integration of rDNA into the host cells.

    01:30 Now, when I talk about the medications working on both HIV-1 and HIV-2, if you think about it, that’s one of the reasons why we like to use this in treatment-naïve patients because sometimes we may not have all of the information.

    01:45 Generally, in most HIV clinics we do but there are going to be situations where you don’t know what type of HIV they have.


    About the Lecture

    The lecture Anti-HIV Agents: Integrase Strand Transfer Inhibitors – Antiviral Drugs by Pravin Shukle, MD is from the course Antimicrobial Pharmacology.


    Included Quiz Questions

    1. It induces the metabolism of raltegravir via increased activity of UDP glucuronosyltransferase.
    2. It induces the metabolism through reduction of glucoronidation.
    3. It reduces the metabolism through induction of glucoronidation.
    4. It reduces the metabolism through reduction of glucoronidation.
    5. It does not affect raltegravir metabolism as raltegravir is not metabolized through CYP450.

    Author of lecture Anti-HIV Agents: Integrase Strand Transfer Inhibitors – Antiviral Drugs

     Pravin Shukle, MD

    Pravin Shukle, MD


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