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

by Pravin Shukle, MD

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    00:00 Let's move on to the Strand Transfer Inhibitors.

    00:04 Now what is a strand transfer inhibitor? So this is part of the nucleic acid synthesis part.

    00:11 And you have to be able to transfer information from one strand of mRNA or RNA to the DNA of the host cell.

    00:19 Remember that virus are interesting little beings in that they actually change the DNA of the host cell.

    00:27 What makes HIV a bit unique is that which cells it's effecting.

    00:32 Because HIV will effect the very cells that are the soldiers of the body, the white blood cells.

    00:37 But other cells as well will effect your host DNA.

    00:42 So it's important to recognize that the nucleic acid synthesis part of it, it's going to be huge in terms of our targeting.

    00:49 Now the integrase strand transfer inhibitors are a fairly large group of drugs.

    00:56 And it's important for you to know the group as a whole, not necessarily the names of individual drugs for the USMLE Step 1 or the MCCQE.

    01:05 Now we're often using these agents on treatment-naive patients.

    01:09 They are not metaobolized by cytochrome P450 but they do undergo glucoronidation.

    01:15 If you've forgotten what glucoronidation is, go back to the pharmacology lectures on pharmacokinetics and how we change medications to make them more amenable to activity in the body.

    01:28 We sometimes use this agent with rifampin.

    01:32 Now remember that rifampin doesn't just induce the cytochrome system but it also induces UDP-glucuronosyltransferase.

    01:40 So we sometimes have to double the dose, when we administer it in combination with rifampin.

    01:47 Now this, these drugs they bind with integrase.

    01:50 Integrase is common to and essential to both HIV-1 and HIV-2 viruses.

    01:57 It inhibits the strand transfer and the integration of the rDNA into host cells is inhibited through this process.

    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. Treatment naïve patients
    2. Pregnant patients
    3. Children
    4. Patients with renal dysfunction
    5. Patients with hepatic dysfunction
    1. Glucuronidation
    2. Cytochrome P450 system
    3. Acetylation
    4. Glutathione conjugation
    5. Methylation

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

     Pravin Shukle, MD

    Pravin Shukle, MD

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