Scribd
Upload
4 views1 page

Non-Nucleoside RT Inhibitors Overview

Non-nucleoside reverse transcriptase inhibitors (Nevirapine, Delavirdine, Efavirenz, and Etravirine) are direct inhibitors of HIV-1 reverse transcriptase that work by inducing a conformational change in the enzyme's catalytic site, unlike nucleoside inhibitors which require intracellular phosphorylation. They are used in combination with other antiretroviral drugs to treat HIV infections, and are metabolized by P450 enzymes, causing numerous drug interactions. Potential adverse effects include fatal hepatotoxicity, psychiatric issues, and severe skin rashes.

Uploaded by

Falaq2
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOC, PDF, TXT or read online on Scribd
4 views1 page

Non-Nucleoside RT Inhibitors Overview

Non-nucleoside reverse transcriptase inhibitors (Nevirapine, Delavirdine, Efavirenz, and Etravirine) are direct inhibitors of HIV-1 reverse transcriptase that work by inducing a conformational change in the enzyme's catalytic site, unlike nucleoside inhibitors which require intracellular phosphorylation. They are used in combination with other antiretroviral drugs to treat HIV infections, and are metabolized by P450 enzymes, causing numerous drug interactions. Potential adverse effects include fatal hepatotoxicity, psychiatric issues, and severe skin rashes.

Uploaded by

Falaq2
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOC, PDF, TXT or read online on Scribd

Non-Nucleoside Reverse Transcriptase

Inhibitors
Nevirapine, Delavirdine, Efavirenz,
and Etravirine
Mechanism of action
These drugs are direct noncompetitive inhibitors of HIV-1
reverse transcriptase. Non-nucleoside reverse transcriptase
inhibitors block RNA-dependent and DNA-dependent polymerase
activities by inducing a conformational change that
disrupts the enzymes catalytic site. Unlike the nucleoside
reverse transcriptase inhibitors, these drugs do not require intracellular
phosphorylation for their actions. These drugs potentiate
the actions of other antiretroviral drugs.
Clinical use
Non-nucleoside reverse transcriptase inhibitors are used in
combination with other antiretroviral agents to treat HIV
infections.
Pharmacokinetics
These drugs are metabolized by the P450 enzymes and are
susceptible to numerous drug interactions by drugs that
induce or inhibit the hepatic P450 microsomal enzymes.
Adverse effects
This drug class has been associated with potentially fatal
hepatotoxicity, although etravirine appears to be the safest
in this regard. Efavirenz has been associated with adverse psychiatric
effects. Severe, life-threatening skin rashes, including
Stevens-Johnson syndrome and toxic epidermal necrosis, may
also occur.

You might also like