Bind to a specific domain or region of the HIV-1 reverse transcriptase.
The binding site of the NSRIs is distinct from the catalytic or active site of reverse transcriptase.
Both
Neither
NNRTIs inhibit the enzyme by this mechanism:
Competitive
Noncompetitive
Uncompetitive
Non-nucleoside reverse-transcriptase inhibitors(NNRTIs) target and show activity against this/these viruses:
HIV-1
HIV-2
Both
Neither
All nonnucleoside reverse transcriptase inhibitors are eliminated principally by:
Renal excretion
Hepatic metabolism
Both
Neither
Example/example of NNRTIs described as "moderately potent" inducers of cytochrome P450 liver drug metabolizing enzymes:
Efavirenz (Sustiva)
Etravirine (Intelence)
Nevirapine (Viramune)
A & B
B & C
A & C
A, B & C
NNRTIs drugs may be used as monotherapy since their mechanism of action precludes development of resistance.
True
False
A single exposure, that is a single dose of the NNRTI drug nevirapine with no other antiretroviral drugs present, is sufficient to promote resistance mutations in as many as 33% of patients.
True
False
Etravirine and rilpivarine represent NNRTI agents relatively
unsusceptible to drug resistance due to single-amino-acid alterations at the NNRTI binding domain.
True
False
NNRTIs in combination with other antiretroviral agents are capable of extended viral replication suppression with increased CD4+ counts.
True
False
Rash represents a common side effect associated with nearly all NNRTIs agents, with the exception of doravirine.
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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.
