Etravirine

Etravirine Uses, Dosage, Side Effects, Food Interaction and all others data.

Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor(NNRTI). Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection.On January 18, 2007, the FDA granted accelerated approved for the use of etravirine 100mg tablets in the treatment of adult HIV-1 infection documented to be resistant to therapy with other NNRTIs and antiretroviral agents. On March 26, 2012, approval was extended for use in treatment-experienced pediatric patients 6 to 18 years of age, weighing at least 16 kg. Etravarine must always be used in combination with other antiretroviral drugs.

Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1), and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.

Common side effects of use include mild to moderate rash within the first 6 weeks of therapy, nausea, diarrhea and peripheral neuropathy. Patients are advised to immediately contact their healthcare provider if a rash develops.

Etravirine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Etravirine
Availability	Prescription only
Generic	Etravirine
Etravirine Other Names	Etravirina, Etravirine
Related Drugs	Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild
Weight	100mg, 200mg, 25mg
Type	Oral tablet
Formula	C₂₀H₁₅BrN₆O
Weight	Average: 435.277 Monoisotopic: 434.049071779
Protein binding	Plasma protein binding is about 99.9% in vitro. In vitro, 99.6% is bound to albumin, and 97.66% - 99.02% is bound to 1-alpha glycoprotein.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV-1 infections in combination with other antiretroviral agents.

Indicated as an adjunct therapy in the treatment of adult HIV-1 infections resistant to therapy with other NNRTIs and antiretroviral agents.

Etravirine is also used to associated treatment for these conditions: Non-nucleoside reverse transcriptase inhibitor resistant HIV-1 infection

How Etravirine works

Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.

Food Interaction

Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of etravirine, which may increase its serum concentration.
Avoid St. John's Wort. This herb induces the CYP3A metabolism of etravirine and may reduce its serum concentration.
Take after a meal. Take after meals. This increases the bioavailability of etravirine.

[Moderate] ADJUST DOSING INTERVAL: Coadministration with food increases the oral bioavailability of etravirine.

The mechanism is unknown.

Compared to administration following a meal, the systemic exposure (AUC) to etravirine was decreased by about 50% when the drug was administered under fasting conditions.

The types of meal studied (ranging from 345 kilocalories containing 17 grams fat to 1160 kilocalories containing 70 grams fat) did not appear to make a difference with respect to impact on etravirine bioavailability.

MANAGEMENT: Etravirine should always be administered following a meal.

Etravirine Drug Interaction

Major: ritonavir, dolutegravirModerate: zolpidem, sulfamethoxazole / trimethoprim, warfarin, cobicistat / darunavir, pantoprazole, sulfamethoxazole / trimethoprimMinor: raltegravir, darunavir, emtricitabine / tenofovirUnknown: aspirin, pregabalin, gabapentin, acetaminophen, ropinirole, albuterol, cholecalciferol, bupropion, sertraline

Etravirine Disease Interaction

Moderate: liver dysfunction

Volume of Distribution

Distribution of etravirine into compartments other than plasma has not been evaluated in humans.

Elimination Route

Maximum oral absorption is achieved in 2.5-4 hours.

Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity.

Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal.

Half Life

Half life of 9.05-41 hours.

Clearance

Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment.

Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments.

Elimination Route

After a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed.

Etravirine is dialyzable (hemodialysis).