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efavirenz

Detailed Prescribing Information

May 2011

 

 

Efavirenz = Sustiva
Forms Available 50 mg, 100mg, 200 mg capsules; 600 mg tablets
Dosing 3x200 mg or 600 mg daily

Usually taken at bedtime but if too much stimulation or dreaming, dosing can be done in the AM

Meal dependence High fat meals elevate Cmax of capsule by 40% and tablets by 80% which may result in increased CNS stimulation and adverse events.
Consider initiating therapy on an empty stomach and if tolerated administer with low fat and then regular feeds.
Contraindication Pregnancy or desire to become pregnant or inadequate birth control precautions

Do not use with saquinavir as the sole protease inhibitor

Midazolam, triazolam, and ergot derivatives are not to be used with Sustiva.

St. John's Wort may decrease Sustiva levels and is therefore not to be used.

Voriconazole should not be used with efavirenz.

Adverse Effects

50% CNS stimulation including sleeplessness, confusion, nightmares: this may be debilitating over short-term or long-term

5% incidence of rash, usually mild and NONPROGRESSIVE with continued treatment

Hepatitis which may be severe

Interactions

Efavirenz decreases PI levels (compensate by increasing PI dosage 25-33%)

Increase indinavir to 1000 mg po q8h

Increase lopinavir/ritonavir to 4 x 133mg/33mg caps twice a day

Increase amprenavir to 8x150 twice a day or use ritonavir 100 mg twice a day

Decreases oral contraceptive pill efficacy

Decreases methadone, fentanyl, imidazole antifungal drug levels

Decreases warfarin efficacy

Decreases voriconazole levels to subtherapeutic

Suggested lab follow-up  Liver profile at 30 days and every 2-3 months and as indicated
Warning Low barrier to one-step mutation.  Use only with other potent agents.
Sudden discontinuation of efavirenz-containing antiretroviral regimens without substitution of other potent antiretroviral or antiretroviral combination may result in prolonged subtherapeutic serum levels of nevirapine.  These subtherapeutic drug levels may result in the development of mutational resistance and loss of activity for efavirenz and the NNRTI class as it exists currently (May 2004)  See Usage Suggestions below for further information.
Administration
Protocol
Initiation of efavirenz:

Initiate therapy during a period that is noncritical for CNS function in the patient's life (eg on a work weekend).  Dosing may be suggested either immediately before bedtime or in the AM, whichever is better tolerated by the patient.  Tolerance to these CNS effects (sleeplessness, nightmares, alteration of mentation, stimulation) may improve over the first two weeks of therapy.

Observe dosing interactions with protease inhibitors carefully (see above)

Discontinuation of efavirenz:
It is recommended that when antiretrovirals are discontinued that include nevirapine and
efavirenz, a potent and active protease inhibitor should be substituted first for the NNRTI.  This PI substitution therapy should then be continued for 2 weeks.  At that point when NNRTI serum and/or intracellular levels are essentially zero, the PI-based substitute antiretroviral therapy may be stopped.  Alternatively stop the efavirenz for 5 days prior to stopping the NRTI backbone.
Complete prescribing information http://www.sustiva.com

 

 

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Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI)
efavirenz  |  nevirapine  |  delavirdine  |  etravirine  |  rilpivirine
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Fusion Inhibitors
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Quick Menu / Table of Contents
Introduction Principles Management NRTI Info NNRTI Info
PI Info Fusion Inhibitors Drug Summary Investigational Adherence
Lab Evaluation Resistance Tests PEP Antiretroviral Tables OI Prevention
Vaccinations TB Therapy Hepatitis Therapy OI Diagnosis OI Therapy
Bibliography Links Palliative Therapy

 

Updated 5.22.2011