SUSTIVA — efavirenz tablet, film coated
Physicians Total Care, Inc.
SUSTIVA® (efavirenz) in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. This indication is based on two clinical trials of at least one year duration that demonstrated prolonged suppression of HIV RNA [see Clinical Studies (14) ].
The recommended dosage of SUSTIVA (efavirenz) is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs). It is recommended that SUSTIVA be taken on an empty stomach, preferably at bedtime. The increased efavirenz concentrations observed following administration of SUSTIVA with food may lead to an increase in frequency of adverse reactions [see Clinical Pharmacology (12.3) ]. Dosing at bedtime may improve the tolerability of nervous system symptoms [see Warnings and Precautions (5.5), Adverse Reactions (6.1), and Patient Counseling Information (17.4) ].
Concomitant Antiretroviral Therapy
If SUSTIVA is coadministered with voriconazole, the voriconazole maintenance dose should be increased to 400 mg every 12 hours and the SUSTIVA dose should be decreased to 300 mg once daily using the capsule formulation (one 200-mg and two 50-mg capsules or six 50-mg capsules). SUSTIVA tablets should not be broken. See Drug Interactions (7.1, Table 7) and Clinical Pharmacology (12.3, Tables 8 and 9).
If SUSTIVA is coadministered with rifampin to patients weighing 50 kg or more, an increase in the dose of SUSTIVA to 800 mg once daily is recommended [see Drug Interactions (7.1, Table 7) and Clinical Pharmacology (12.3, Table 9)].
It is recommended that SUSTIVA be taken on an empty stomach, preferably at bedtime. Table 1 describes the recommended dose of SUSTIVA for pediatric patients 3 years of age or older and weighing between 10 and 40 kg [see Use in Specific Populations (8.4) ]. The recommended dosage of SUSTIVA for pediatric patients weighing greater than 40 kg is 600 mg once daily.
|Body Weight||SUSTIVA Dose (mg)|
|10 to less than 15||22 to less than 33||200|
|15 to less than 20||33 to less than 44||250|
|20 to less than 25||44 to less than 55||300|
|25 to less than 32.5||55 to less than 71.5||350|
|32.5 to less than 40||71.5 to less than 88||400|
|at least 40||at least 88||600|
200-mg capsules are gold color, reverse printed with “SUSTIVA” on the body and imprinted “200 mg” on the cap.
50-mg capsules are gold color and white, printed with “SUSTIVA” on the gold color cap and reverse printed “50 mg” on the white body.
600-mg tablets are yellow, capsular-shaped, film-coated tablets, with “SUSTIVA” printed on both sides.
SUSTIVA is contraindicated in patients with previously demonstrated clinically significant hypersensitivity (eg, Stevens-Johnson syndrome, erythema multiforme, or toxic skin eruptions) to any of the components of this product.
For some drugs, competition for CYP3A by efavirenz could result in inhibition of their metabolism and create the potential for serious and/or life-threatening adverse reactions (eg, cardiac arrhythmias, prolonged sedation, or respiratory depression). Drugs that are contraindicated with SUSTIVA are listed in Table 2.
|Drug Class: Drug Name||Clinical Comment|
|Antimigraine: ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine)||Potential for serious and/or life-threatening reactions such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.|
|Benzodiazepines: midazolam, triazolam||Potential for serious and/or life-threatening reactions such as prolonged or increased sedation or respiratory depression.|
|Calcium channel blocker: bepridil||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|GI motility agent: cisapride||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|Neuroleptic: pimozide||Potential for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|St. John’s wort (Hypericum perforatum)||May lead to loss of virologic response and possible resistance to efavirenz or to the class of non-nucleoside reverse transcriptase inhibitors (NNRTIs).|
Efavirenz plasma concentrations may be altered by substrates, inhibitors, or inducers of CYP3A. Likewise, efavirenz may alter plasma concentrations of drugs metabolized by CYP3A or CYP2B6 [see Contraindications (4.2) and Drug Interactions (7.1) ].
All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.