General

Pronunciation
e-TRA-veer-een

Trade Name(s)

• Intelence

Pregnancy Category
Category B

Ther. class.
antiretrovirals

Pharm. class.
non nucleoside reverse transcriptase inhibitors

Indications

HIV infection (with other antiretrovirals)

Action

Binds to the enzyme reverse transcriptase which results in disrupted viral DNA synthesis

Therapeutic Effect(s):
Evidence of decreased viral replication and reduced viral load with slowed progression of HIV and its sequelae

Pharmacokinetics

Absorption: Well absorbed following oral administration. Food enhances absorption

Distribution: Unknown

Protein Binding: 99.9%

Metabolism and Excretion: Mostly metabolized by the liver (CYP3A4, CYP2C9 and CYP2C19 enzyme systems); minimal renal excretion; mostly eliminated in feces as unchanged drug and metabolites

Half-life: 41 hr

TIME/ACTION PROFILE (blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2.5–4 hr	12 hr

Contraindication/Precautions

Contraindicated in:
Concurrent use with other non-nucleoside reverse transcriptase inhibitors (NNRTIs), rifampin, rifapentine, St. John's wort.

Use Cautiously in:

• Concurrent use of antiarrhythmics, anticonvulsants, antifungals, clarithyromycin, rifabutin, diazepam, dexamethasone, HMG Co-A reductase inhibitors (statins), immunusuppressants

• Geri: Consider age-related decrease in organ function and body mass, concurrent disease states and medications

• Pedi: OB: Lactation: Pregnancy, lactation and children (safety not established, breast-feeding not recommended in HIV-infected women)

Adverse Reactions/Side Effects

CNS: SEIZURES, anxiety, confusion, fatigue, headache, insomnia, sleep disorders.

EENT: blurred vision, vertigo.

CV: MYOCARDIAL INFARCTION, angina pectoris, atrial fibrillation, hypertension.

GI: nausea, abdominal pain, anorexia, dry mouth, hepatitis, stomatitis, vomiting.

GU: renal failure.

Endo: gynecomastia, hyperglycemia, hyperlipidemia.

Hemat: anemia, hemolytic anemia.

Derm: rash.

Metabolic: fat redistribution.

Neuro: peripheral neuropathy.

Misc: allergic reactions including STEVENS-JOHNSON SYNDROME, IMMUNE RECONSTITUTION SYNDROME.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

• Etravirine is a substrate of the CYP3A4, CYP2C9, and CYP2C19 enzyme systems; other medications the induce or inhibit these systems may be expected to alter the response to etravirine. Etravirine is an inducer of CYP3A4 and an inhibitor of CYP2C9 and CYP2C19. The effects of medications that are substrates of these enzyme systems may be altered by concurrent use.

• Concurrent use with other NNRTIs including efavirenz, nevirapine, and delavirdine may lead to effectiveness and should be avoided.

• Concurrent use with protease inhibitors (PIs) including atazanavir, fosamprenavir, nelfinavir, and indinavir may lead to altered plasma levels and should be untertaken with concurrent low dose ritonavir.

• Concurrent use with higher dose ritonavir, combination tipranavir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir alter levels and effectiveness of etravirine and should be avoided.

• Concurrent use of the combination saquinavir/ritonavir should be undertake cautiously.

• blood levels and effectiveness of antiarrhythmics including amiodarone, bepridil, disopyramide, flecainide, lidocaine, mexiletine, quinidine, propafenone, and quinidine; blood level monitoring recommended.

• Blood levels and effects may be by anticonvulsants including carbamazepine, phenobarbital, and phenytoin.

• Concurrent use with voriconazole may levels of both drugs; levels of itraconazole and ketoconazole (dose adjustments may be necessary)

• May alter levels and response to clarithromycin; other agents should be considered

• Rifampin and rifapentine blood levels and effectiveness and should be avoided; rifabutin should only be used without a protease inhibitor/ritonavir combination.

• May blood levels and sedation from diazepam, monitor for effects.

• Levels and effectiveness may be by dexamethasone use cautiously and consider alternatives.

• May alter blood levels and effects of fluvastatin, lovastatin, and simvastatin (dose adjustments may be necessary.

• May alter blood levels and effects of cyclosporine, sirolimus, and tacrolimus; careful monitoring required.

Drug-Natural Products
St. John's wort may blood levels and effectiveness; avoid concurrent use

Route/Dosage

• PO (Adults): 200 mg twice daily.

Availability

• Tablets: 100 mg

Assessment

• Assess for change in severity of HIV symptoms and for symptoms of opportunistic infections during therapy

• Assess patient for rash (mild to moderate rash usually occurs in the 2nd wk of therapy and resolves within 1–2 wks of continued therapy. If rash is severe (extensive erythematous or maculopapular rash with moist desquamation or angioedema) or accompanied by systemic symptoms (serum sickness-like reaction, Stevens—Johnson syndrome, toxic epidermal necrolysis), therapy must be discontinued immediately.

Lab Test Considerations

• Monitor viral load and CD4 cell count regularly during therapy

» Monitor liver function tests periodically during therapy. May cause serum AST, ALT concentrations

» May cause pancreatic amylase and lipase

» May cause in total cholesterol, low density lipoprotein, serum triglyceride, and glucose levels

» May cause serum creatinine

» May cause neutrophils, platelet count, anemia and hemolytic anemia

Potential Nursing Diagnoses

• Risk for infection (Indications)

• Noncompliance (Patient/Family Teaching)

Implementation

PO: Administer 2 tablets twice daily following a meal; type of food does not matter. Swallow tablet whole, do not crush, break, or chew. If patient has difficulty swallowing, may disperse tablet in a glass of water. Once dispersed, patient should stir well and drink immediately; rinse glass with water and drink several times to ensure entire dose is consumed

Patient/Family Teaching

• Emphasize the importance of taking etravirine as directed, at the same time each day. It must always be used in combination with other antiretroviral drugs. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses following a meal if remembered within 6 hrs of the time its usually taken, then return to regular schedule. If more than 6 hrs from time dose is usually taken, omit dose and resume dosing schedule; do not double doses

• Instruct patient that etravirine should not be shared with others

• Inform patient that etravirine does not cure AIDS or prevent associated or opportunistic infections. Etravirine does not reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of etravirine are unknown at this time

• May cause dizziness, impaired concentration, or drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known

• Instruct patient to notify health care professional immediately if rash or signs of Immune Reconstitution Syndrome (signs and symptoms of an infection) occur.

• Advise patient to avoid taking other Rx, OTC, vitamins, or herbal products, especially St. John's Wort, without consulting health care professional

• Inform patient that changes in body fat (increased fat in upper back and neck, breast, and around back, chest, and stomach area, loss of fat from legs, arms, and face) may occur

• Advise patients taking oral contraceptives to use a nonhormonal method of birth control during etravirine therapy and to notify health care professional if they become pregnant or plan to breastfeed while taking etravirine

• Emphasize the importance of regular follow-up exams and blood counts to determine progress and monitor for side effects

Evaluation/Desired Outcomes

• Delayed progression of AIDS and decreased opportunistic infections in patients with HIV

• Decrease in viral load and increase in CD4 cell counts

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