Medical Pharmacology: Antiviral Drug Practice Questions

Medical Pharmacology: Antiviral Drug Practice Questions

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Etravirine (Intelence):
1. Activity against HIV-1 and HIV-2.
2. Classified as a nonnucleoside reverse transcriptase inhibitor (NNRTI)
Etravirine (Intelence): exhibits uniqueness in that it may inhibit reverse transcriptase otherwise resistant to other members of this drug class (NNRTIs).
1. True
2. False
Etravirine combining with the NNRTI-binding domain results in inhibition of HIV-1 reverse transcriptase, even in the presence of frequently observed NNRTI resistance mutations.
1. True
2. False
Etravirine and efficacy for resistant HIV-1 strains.
1. The resistance which etravirine overcomes is associated with first-generation NNRTIs involving HIV strains with particular mutations (K103N and Y181C).
2. Etravirine resistance, however, does occur and appears similar to resistance seen with nevirapine and efavirenz.
3. Both
4. Neither
Etravirine pharmacokinetics:
1. Etravirine should not be taken with food as doing so reduces systemic exposure.
2. Primary route of administration is through hepatic metabolism.
3. Both
4. Neither
Etravirine metabolites (methyl-and dimethyl-hydroxylated derivatives):
1. Formation of these metabolites are catalyzed by particular cytochrome P450 drug metabolizing isoforms including CYP3A4, CYP2C9, and CYP2C19.
2. This process utilizing the cytochrome P450 drug metabolizing system and these isoforms in particular are responsible for etravirine elimination.
3. Both
4. Neither
The most notable side effect associated with etravirine (Intelence) administration is rash.
1. True
2. False
Etravirine administration increases the concentration of both CYP3A4 and glucuronosyl transferases. In addition etravirine inhibits the action of CYP2C9 and CYP2C19. A consequence of these interactions is the occurrence of drug-drug interactions.
1. True
2. False
Etravirine can be added to these anti-HIV retroviral agents without dose adjustments:
1. Darunavir/ritonovir
2. Lopinavir/ritonovir
3. Saquinavir/ritonovir
4. All of the above
Coadministration of etravirine with statin agents probably should be avoided.
1. True
2. False

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Source Material:

Acosta EP Chapter 62 Antiviral Agents (Nonretroviral) in Goodman & Gilman's: The Pharmcological Basis of Therapeutics, 14e, (Brunton LL Knollmann BC eds) McGraw-Hill Education, 2023.

Safrin S Chapter 49 Antiviral Agents in Basic & Clinical Pharmacology (Katzung BG, Editor; Vanderah TW, Associate editor) 15e McGraw Hill 2021.

Li JZ Coen DM Chapter 38 Pharmacology of Viral Infections in Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy 4e (Golan DE Armstong EJ Armstrong AW, eds) Wolters Kluwer 2017.

Waller DB Sampson AP Section 11 Chemotherapy in Medical Pharmacology & Therapeutics Elsevier 2018.

Burchum JR Rosenthal LD Chapter 97 Antiviral Agents I: Drugs for Non-HIV Viral Infections in Lehne's Pharmacology for Nursing Care Elsevier 2022.

Waller DB Sampson AP Section 11: Chapter 51 Chemotherapy of infections in Medical Pharmacology & Therapeutics Elsevier 2018.

Benavides S Bahal O'Mara N Nahata MC Chapter 79 Viral Infections in Applied Therapeutics: The Clinical Use of Drugs (Zeind C, Carvalho MG Cheng JW Zaiken K Lapointe T, eds) Wolters Kluwer, 2024.

Davanathan AS Symonds AE Adams JL Cottrell ML Chapter 76 Pharmacotherapy of Human Immunodeficiency Virus Infection in Applied Therapeutics: The Clinical Use of Drugs (Zeind C, Carvalho MG Cheng JW Zaiken K Lapointe T, eds) Wolters Kluwer, 2024.

Flexner CW Chapter 64 Antiretroviral Agents and Treatment of HIV Infection in Goodman & Gilman's: The Pharmcological Basis of Therapeutics, 14e, (Brunton LL Knollmann BC eds) McGraw-Hill Education, 2023.

Burchum JR Rosenthal LD Chapter 98 Antiviral Agents II: Drugs for HIV Infection and Related Opportunistic Infections in Lehne's Pharmacology for Nursing Care Elsevier 2022.

Woster PM Chapter 30 Drugs Used to Treat Viral Infections in Foye's Principles of Medicinal Chemistry 8e (Roche VF Zito SW Lemke TL Williams DA, eds) Wolters Kluwer 2020.