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Nnrtis: Nonnucleoside Reverse Trancriptase Inhibitors

NNRTIs are non-nucleoside reverse transcriptase inhibitors that are used to treat HIV. Examples include efavirenz, nevirapine, delavirdine, and etravirine. NNRTIs work by binding to reverse transcriptase in a way that prevents viral DNA synthesis. They do not require phosphorylation to be active. Resistance can emerge rapidly via single mutations. NNRTIs have various pharmacokinetic properties and side effect profiles that are important to consider when selecting an appropriate regimen for patients.

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65 views12 pages

Nnrtis: Nonnucleoside Reverse Trancriptase Inhibitors

NNRTIs are non-nucleoside reverse transcriptase inhibitors that are used to treat HIV. Examples include efavirenz, nevirapine, delavirdine, and etravirine. NNRTIs work by binding to reverse transcriptase in a way that prevents viral DNA synthesis. They do not require phosphorylation to be active. Resistance can emerge rapidly via single mutations. NNRTIs have various pharmacokinetic properties and side effect profiles that are important to consider when selecting an appropriate regimen for patients.

Uploaded by

Malueth Angui
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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NNRTIs

NONNUCLEOSIDE REVERSE TRANCRIPTASE


INHIBITORS

BY

TOBIAS OMONDI
EXAMPLES
1. Efavirenz
2. Nevirapine
3. Delavirdine
4. Etravirine:
• Is the newest NNRTI approved for treatment of experienced
HIV patients
• May be effective against HIV strains resistant to other drugs in
this group
MODE OF ACTION
They inhibit HIV-reverse transcriptase by binding at a site
remote from the active site(this site is different from the
binding site of NRTIs)

They produce conformational change in the enzyme


that prevents substrate binding

NNRTIs do not require phosphorylation to be active


and do not compete with nucleoside triphosphates

There is no cross-resistance with NRTIs


RESISTANCE
 Resistance emerges rapidly by single point gene
mutations(mutations occur in the pol gene, and is rapid if these
agents are used as monotherapy)
PHARMACOKINETICS
EFAVIRENZ:
 Oral absorption is less good
 Fatty foods may enhance its oral bioavailability
 Can be given once daily because of its long half life of two days
 EFV is metabolized by hepatic cytochrome P450
Pharmacokinetics
NEVIRAPINE:
 Oral absorption is very good with good oral
bioavailability
 Penetrates most tissues including the CNS
 Has a half life of more than 24hours
 Metabolized by the hepatic cytochrome P450-
cyp3A4 isoform
 Used in combination regimens
 Is effective in prevention of vertical HIV
transmission when given as a single dose to
mothers at the onset of labour and to a neonate
Pharmacokinetics/dynamics
DELAVIRDINE:

 Metabolized by both cyp3A4 and cyp2D6

ETRAVIRINE:

 Its a substrate as well as an inducer of cyp3A4 and also inhibits


cyp2c9 and cyp2c19
SIDE EFFECTS
EFAVIRENZ:
i. Skin rash

ii. Elevation of plasma cholesterol

iii. CNS dysfunction-night mares,drowsiness,headache

iv. Avoid it in pregnancy particularly in first trimester-


its teratogenic

v. Nausea,vomiting,abdominal pain,diarrhea
Side effects
NEVIRAPINE:

Hypersensitivity reactions:

i. Rash-common in female(15-20%)

ii. Stevens Johnson syndrome

Hepatotoxicity-can lead to fulminant hepatitis

Nausea,vomiting,abdominal pain,diarrhea

Fatigeu,headache,drowsiness
Side effects
DELAVIRDINE:

i. Skin rash in up to 20% of patients

ii. Avoid it in pregnancy because of its

iii. Teratogenicity

ETRIVARINE:
i. Rash

ii. Nausea,diarrhea

iii. Elevation of serum cholesterol levels, triglycerides and transaminase


levels may occur
DRUG INTERACTIONS
 RIFAMPIN, an enzyme inducer will lower the
blood levels of NNRTIs & PIs and hence reduce
their effectiveness

 CIMETIDINE & MACROLIDES increase blood


levels of NEVIRAPIN

 ANTIACIDS,DDI,PHENYTOIN,RIFAMPIN,NIFEDIP
INE,PIs,QUINIDINE & WARFARIN decrease the
blood levels of DELAVIRDINE
REMEMBER
When treating TB and giving concurrent
ART,the ART regimen require adjustment

ART option with RIFAMPIN is EFV based


regimen

THANK YOU

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