Etravirine

Mechanism :

As a non-nucleoside reverse transcriptase inhibitor, etravirine has activity against HIV-1 by binding to reverse transcriptase.

Indication :

HIV-1 infection with documented non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance

Contraindications :

Hypersensitivity to etravirine or any component of the formulation; concomitant use with the hepatitis C combination regimen of ombitasvir, paritaprevir, ritonavir and with drugs containing dasabuvir.

Dosing :

Oral: Children 2 to <18 years of age:

≥10 kg to <20 kg:

100 mg twice daily.

≥20 kg to <25 kg:

125 mg twice daily.

≥25 kg to <30 kg:

150 mg twice daily.

≥30 kg:

200 mg twice daily.

Adverse Effect :

Rash, nausea, increased LDL, GI disorders, fatigue, peripheral neuropathy, increased creatinine, diarrhea, Stevens-Johnson syndrome, erythema multiforme, angina, angioedema, TEN.

Interaction :

CYP2C19 Inducers: May increase the metabolism of CYP2C19 Substrates.
CYP3A4 Inducers: May increase the metabolism of CYP3A4 Substrates.
CYP3A4 Substrates: CYP3A4 Inducers may decrease the serum concentration of CYP3A4 Substrates.
Efavirenz: Reverse Transcriptase Inhibitors (Non-Nucleoside) may increase the serum concentration of Efavirenz.
HMG-CoA Reductase Inhibitors (Statins): Etravirine may decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins).
Phosphodiesterase 5 Inhibitors: Etravirine may decrease the serum concentration of Phosphodiesterase 5 Inhibitors.
Protease Inhibitors: May decrease the serum concentration of Etravirine. This effect is anticipated with darunavir, saquinavir, and lopinavir (with low-dose ritonavir).

Hepatic Dose :

Mild and moderate hepatic impairment: No dosage adjustment needed.
Severe hepatic impairment: Use is not recommended as pharmacokinetics in severe hepatic impairment has not been studied.