Indications
HIV infection (with other antiretrovirals).
Action
Binds to the enzyme reverse transcriptase which results in disrupted
viral DNA synthesis.
Therapeutic Effects: 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 |
Contraindications/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.
Metab:
fat redistribution.
Neuro:
peripheral
neuropathy.
Misc:
allergic reactions including
STEVENS-JOHNSON SYNDROME,
IMMUNE RECONSTITUTION SYNDROME.
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: St. John's wort may ↓ blood levels and effectiveness; avoid concurrent use.
Route/Dosage
PO (Adults): 200 mg twice daily.
Availability
Tablets: 100 mg.