efavirenz


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efavirenz

 [ef´ah-vi″renz]
a non-nucleoside reverse transcriptase inhibitor, used as an antiretroviral in treatment of human immunodeficiency virus infection; administered orally.

efavirenz

Sustiva

Pharmacologic class: Nonnucleoside reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category D

Action

Inhibits human immunodeficiency virus (HIV) reverse transcriptase (required for transcription of HIV-1 RNA to DNA), leading to viral cell death

Availability

Capsules: 50 mg, 200 mg

Tablets: 600 mg

Indications and dosages

HIV infection (given with one or more additional antiretrovirals)

Adults and children older than age 3 and weighing more than 40 kg (88 lb): 600 mg P.O. once daily

Children weighing 32.5 to 40 kg (71.5 to 88 lb): 400 mg P.O. once daily

Children weighing 25 to 32.5 kg (55 to 71.5 lb): 350 mg P.O. once daily

Children weighing 20 to 25 kg (44 to 55 lb): 300 mg P.O. once daily

Children weighing 15 to 20 kg (33 to 44 lb): 250 mg P.O. once daily

Children weighing 10 to 15 kg (22 to 33 lb): 200 mg P.O. once daily

Dosage adjustment

• Concurrent use of rifampin or voriconazole

Contraindications

• Hypersensitivity to drug
• Concurrent use of astemizole, cisapride, midazolam, triazolam, ergot derivatives, voriconazole, or bepridil

Precautions

Use cautiously in:
• hypercholesterolemia, hepatic impairment, concurrent use of hepatotoxic drugs, mental illness, or substance abuse
• concurrent use of St. John's wort (use not recommended)
• pregnant or breastfeeding patients
• children.

Administration

• Give on empty stomach.
• Know that drug is given with other antiretrovirals.

Adverse reactions

CNS: dizziness, drowsiness, fatigue, insomnia, abnormal dreams, hypoesthesia, depression, headache, poor concentration, nervousness, anxiety, CNS depression, suicidal ideation

CV: arrhythmias

GI: nausea, diarrhea, flatulence, abdominal pain, dyspepsia

GU: hematuria, renal calculi

Hepatic: hepatotoxicity

Respiratory: respiratory depression

Skin: rash, diaphoresis, pruritus,erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: increased appetite

Interactions

Drug-drug.Azole antifungals (ketoconazole, voriconazole): decreased antifungal plasma concentration, increased efavirenz plasma concentration

Calcium channel blockers: possible decreased calcium channel blocker concentration

Clarithromycin, indinavir: reduced blood levels of these drugs

CNS depressants (including antidepressants, antihistamines, opioids): increased CNS depression

CYP450 inducers (including phenobarbital, rifabutin, rifampin): increased clearance and decreased blood level of efavirenz

CYP450 inhibitors, ergot alkaloids, estrogen, midazolam, ritonavir, triazolam: increased blood levels of these drugs, greater risk of serious adverse reactions (including arrhythmias, CNS and respiratory depression, and hepatotoxicity)

HMG-CoA reductase inhibitors: decreased plasma concentration of atorvastatin, pravastatin, and simvastatin

Hormonal contraceptives: increased ethinyl estradiol blood level

Protease inhibitors: decreased plasma level and efficacy of these drugs

Saquinavir: decreased saquinavir blood level

Warfarin: increased or decreased warfarin effects

Drug-diagnostic tests.Alanine aminotransferase, aspartate aminotransferase, gamma-glutamyltransferase, total cholesterol, triglycerides: increased levels

Urine cannabinoid test: false-positive result

Drug-food.High-fat meal: increased drug absorption

Drug-herbs.St. John's wort: decreased efavirenz blood level and efficacy, drug resistance

Drug-behaviors.Alcohol use: increased CNS depression

Patient monitoring

• Monitor dietary intake and hepatic and lipid profile.
• Closely monitor patients with hepatic failure.

Record mood changes and stay alert for suicidal ideation or behavior.
• Be aware that drug may cause hypercholesterolemia.
• Know that amount of HIV in blood may increase if patient stops drug therapy even briefly.

Patient teaching

• Instruct patient to take with full glass of water, preferably at bedtime to improve tolerance of CNS effects. Also tell him to avoid taking drug with high-fat meals.
• Inform patient that drug must be taken in combination with other antiretrovirals.
• Tell patient that drug doesn't cure HIV or AIDS and that he can still transmit virus to others.

Advise patient to report suicidal thoughts and other psychiatric symptoms.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

Tell female patient to immediately inform prescriber if she becomes pregnant.
• Advise female patient to use adequate contraceptive measures for 12 weeks after discontinuing drug.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

efavirenz

/ef·a·vi·renz/ (ef´ah-vi″renz) an antiretroviral, inhibiting reverse transcriptase; used in the treatment of HIV infection.

efavirenz

(ə-fä′vîr-ĕnz′)
n.
An antiviral drug, C14H9ClF3NO2, that is a non-nucleoside reverse transcriptase inhibitor and is used in combination with other drugs for the treatment of HIV infection.

efavirenz

an antiviral.
indications It is used to treat HIV-1 in combination with other antiretroviral agents.
contraindications Known hypersensitivity to this drug prohibits its use.
adverse effects Adverse effects include abdominal pain, headache, dizziness, fatigue, impaired concentration, insomnia, abnormal dreams, and depression. Common side effects include diarrhea, nausea, and rash.

efavirenz

Sustiva AIDS A reverse transcriptase inhibitor used with other antivirals–eg, zidovudine, lamivudine for HIV-1 infection Adverse effects N&V, maculopapular rash, fatigue, headache, dizziness. See Non-nucleoside reverse transcriptase inhibitor.

efavirenz

A non-nucleoside reverse transcriptase inhibitor used, in combination with other antiretroviral drugs, to treat HIV infections. The drug is on the WHO official list. A brand name is Sustiva.
References in periodicals archive ?
DRIVE-AHEAD is an ongoing Phase 3 multicenter, double-blind, randomized, active comparator-controlled clinical trial evaluating the safety and efficacy of a once-daily, single-tablet, fixed-dose combination containing doravirine 100 mg, lamivudine 300 mg and tenofovir disoproxil fumarate 300 mg versus a once-daily, single-tablet, fixed-dose combination containing efavirenz 600 mg, emtricitabine 200 mg, and tenofovir disoproxil fumarate 300 mg in treatment-naive HIV-1 infected adults.
The Kirby Institute's ENCORE1 trial1 showed that a reduced dose of 400 mg Efavirenz is non-inferior to a dose of 600 mg, when combined with Tenofovir and Emtricitabine during 48 weeks in ART-naive adults with HIV-1 infection.
The investigators next determined that the risk of suicidal behavior was significantly higher in the 3,516 START participants on efavirenz than in the 1,169 subjects on other ART drugs.
Though only 13 patients were under Tenofovir, Lamivudine and Efavirenz regimen, abnormalities in LFT, Lipid Profile and Serum Ca 2+ and PO4 levels were seen in more proportions in TLE regimen compared to 185 patients with Tenofovir, Lamivudine and Nevirapine regimen.
12,17,18] The 2010 Clinical Guidelines for the Management of HIV and AIDS in Adults and Adolescents in South Africa [19] stated that the recommended safety monitoring for the NPSEs of efavirenz is 'clinical'.
Association between efavirenz as initial therapy for HIV-1 infection and increased risk for suicidal ideation or attempted or completed suicide: An analysis of trial data.
Case definition of drug allergy to efavirenz included rash, skin eruption, urticaria, and/or erythema following exposure to efavirenz.
The researchers analysed samples of blood and cerebrospinal fluid from HIV-infected subjects who were taking efavirenz in the North Eastern AIDS Dementia study.
For the study led by Haughey, researchers obtained samples of blood and cerebrospinal fluid from HIV-infected subjects enrolled in the NorthEastern AIDS Dementia study who were taking efavirenz.
He started Kivexa and efavirenz, following full discussions on side effects and adherence with his doctor and the clinic pharmacist.
Efavirenz is an antiretroviral drug that belongs to the class of drugs called non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of highly active antiretroviral therapy (HAART) for the treatment of HIV type-1 (AHFS, 2007).
The only drug in the integrase inhibitor class approved for the treatment of HIV-1 infection as part of combination antiretroviral therapy raltegravir also appears to be better tolerated than efavirenz and has a more favorable metabolic profile, according to 4 years of follow-up data presented by Dr.