antibioticsbooks

Non-nucleoside Reverse
Transcriptase Inhibitors
(NNRTIs)
Agents: efavirenz (EFV), etravirine (ETR),
rilpivirine (RPV), nevirapine (NVP), delavirdine
(DLV)
Combinations: efavirenz/tenofovir/
emtricitabine (Atripla), rilpivirine/tenofovir/
emtricitabine (Complera)
The non-nucleoside reverse transcriptase inhibitors
(NNRTIs) inhibit the same enzyme as the
NRTIs but work through a different mechanism
and have greatly different pharmacologic properties.
That extra N makes a big difference: it’s very
important to keep the two drug classes straight.
Mechanism of Action
Instead of inhibiting the action of reverse transcriptase
by “pretending” to be regular nucleosides,
NNRTIs bind to a different part of the enzyme. The
binding of the NNRTI causes a change in the conformation
of the enzyme that interferes with its
ability to form the viral DNA chain.
Spectrum
Only current clinical use is for HIV.
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