Names and pronunciation
(e-tra′veer-een) Intelence
Source page 533
Loading InternPractice…
Individual generic drug information
Extracted information for etravirine only.
(e-tra′veer-een) Intelence
Source page 533
Func. class.: Antiretroviral
Source page 533
Chem. class.: Nonnucleoside reverse transcriptase inhibitor (NNRTI)
Source page 533
ACTION: Binds directly to reverse transcriptase, thus blocking the RNA- and DNA-dependent DNA polymerase action and causing a disruption of the enzyme’s catalytic site
Source page 533
USES: In combination with other anti- retroviral agents for HIV infection in treatment-experienced patients with evi- dence of HIV replication despite ongoing antiretroviral therapy
Source page 533
Extracted information for etravirine only.
CONTRAINDICATIONS: Breast- feeding, hypersensitivity Precautions: Pregnancy, children, geri- atric patients, impaired hepatic function, antimicrobial resistance, hepatitis, hypercholesterolemia, hypertriglycer- ides, immune reconstitution syndrome
Source page 533
SIDE EFFECTS CNS: Headache, insomnia, amnesia, anxiety, confusion, fatigue, nightmares, peripheral neuropathy, seizures, stroke, tremor CV: Atrial fibrillation, hypertension, MI EENT: Blurred vision GI: Nausea, vomiting, diarrhea, anorexia, abdominal pain, increased AST/ALT, constipation, flatulence, gastri- tis, GERD, hematemesis, hepatitis, hepa- tomegaly, pancreatitis GU: Renal failure HEMA: Hemolytic anemia, neutropenia, thrombocytopenia, anemia INTEG: Rash, erythema multiforme, angioedema, Stevens-Johnson syndrome MS: Rhabdomyolysis OTHER: Diabetes mellitus, gynecomastia, hyperamylasemia, hypercholesterolemia, hyperglycemia, hyperlipidemia RESP: Dyspnea, bronchospasm SYST: DRESS
Source page 533
INTERACTIONS • Do not use concurrently with atazanavir, carBAMazepine, delavirdine, fosamprena- vir, fosphenytoin, phenytoin, PHENobarbi- tal, rifapentine, rifAMPin, tipranavir, rilpivirine • Altered effect of cycloSPORINE, tacro- limus, sirolimus Increase: myopathy, rhabdomyolysis— HMG-CoA reductase inhibitors Increase: etravirine levels—CYP3A4 inhibitors (fluconazole, itraconazole, ketoconazole, lopinavir, posaconazole, ritonavir, voriconazole) Increase: withdrawal symptoms— methadone Increase: levels of diazePAM, rifAMPin, voriconazole, warfarin Decrease: levels of CYP3A4 inducers (amiodarone, atazanavir, clarithromycin, flecainide, fosamprenavir, lidocaine, mexiletine, propafenone, quiNIDine, sildenafil, tadalafil, vardenafil) Decrease: etravirine levels—darunavir, dexamethasone, disopyramide, efavirenz, nevirapine, ritonavir, saquinavir, tipranavir Drug/Herb Decrease: etravirine—St. John’s wort
Source page 534
Extracted information for etravirine only.
DOSAGE AND ROUTES E • Adult/child/adolescent ≥6 yr, ≥30 kg: PO 200 mg bid • Child/adolescent ≥6 yr, 25 to 29 kg: PO 150 mg bid • Child/adolescent ≥6 yr, 20 to 24 kg: PO 125 mg bid • Child/adolescent ≥6 yr, 16 to 19 kg: PO 100 mg bid
Source page 533
Available forms: Tablets 25, 100, 200 mg
Source page 533
Administer: In combination with other antiretrovirals with food or after a meal • Tablets may be dispersed in ≥5 mL of water; once dispersed, stir well, give immediately, rinse glass, have patient drink to ensure all medication taken • Store in cool environment; protect from light
Source page 533
Extracted information for etravirine only.
Assess: • Symptoms of HIV, possible infec- tions: increased temperature • HIV: monitor viral load, CD4 counts, plasma HIV RNA during treatment; watch for decreasing granulocytes, Hb; if low, therapy may have to be discontinued and restarted after hematologic recovery; blood transfusions may be required; cho- lesterol/lipid profile • Fatal hypersensitivity reactions: fe- ver, rash, nausea, vomiting, fatigue, cough, dyspnea, diarrhea, abdominal discomfort; treatment should be discontinued and not restarted; incidence of rash may be worse in women • Blood dyscrasias (anemia, granulo- cytopenia): bruising, fatigue, bleeding, poor healing • Renal failure: BUN, serum uric acid, CCr prior to, during therapy; may be ele- vated throughout treatment • Hepatitis/pancreatitis: hepatic studies prior to and during therapy: bili- rubin, AST, ALT, amylase, alkaline phos- phatase, creatine phosphokinase, cre- atinine, monthly • Pregnancy/breastfeeding: use only if benefits outweigh risk; enroll pregnant pa- tients in the Antretroviral Pregnancy Regis- try (800-258-4263); do not breastfeed
Source page 534
Evaluate: • Therapeutic response: increased CD4 count, decreased viral load
Source page 534
CLINICAL CONSIDERATIONS
Source page 534
Patient and caregiver information: • That product is not a cure but will control symptoms; that patient is still infective, may pass AIDS virus to others • To notify prescriber of sore throat, swol- len lymph nodes, malaise, fever; other infections may occur; to stop product and notify prescriber immediately if skin rash, fever, cough, SOB, GI symptoms occur; to advise all health care providers that allergic reaction has occurred with etravirine • That follow-up visits must be contin- ued, since serious toxicity may occur; blood counts must be performed • To use contraception during treat- ment; that patient is still able to trans- mit disease • About information on medication guide and warning card; discuss points on guide • That other products may be necessary to prevent other infections • To take medication after a meal HIGH ALERT
Source page 534
Extracted information for etravirine only.
PHARMACOKINETICS 99.9% plasma protein binding; metabo- lized by CYP3A4, 2C9, 2C19; half-life 21-61 hr; excreted in feces
Source page 534
Filter the extracted dose blocks for this individual drug.
E
• Adult/child/adolescent ≥6 yr, ≥30 kg: PO 200 mg bid
Candidate age grouping · source page 533
E
• Child/adolescent ≥6 yr, 25 to 29 kg: PO 150 mg bid
Candidate age grouping · source page 533
E
• Child/adolescent ≥6 yr, 20 to 24 kg: PO 125 mg bid
Candidate age grouping · source page 533
E
• Child/adolescent ≥6 yr, 16 to 19 kg: PO 100 mg bid
Candidate age grouping · source page 533