Efavirenz

EFAVIRENZ- efavirenz tablet, film coated
Cipla USA Inc.

1 INDICATIONS AND USAGE

Efavirenz in combination with other antiretroviral agents is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and in pediatric patients weighing at least 3 months old and weighing at least 3.5 kg.

2 DOSAGE AND ADMINISTRATION

2.1 Hepatic Function

Monitor hepatic function prior to and during treatment with efavirenz tablets [see Warnings and Precautions (5.9) ].

Efavirenz tablets are not recommended in patients with moderate or severe hepatic impairment (Child Pugh B or C) [see Warnings and Precautions (5.9) and Use in Specific Populations (8.6)].

2.2 Adults

The recommended dosage of 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 efavirenz be taken on an empty stomach, preferably at bedtime. The increased efavirenz concentrations observed following administration of efavirenz 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 (5.6) , Adverse Reactions (6.1) , and Patient Counseling Information (17) ]. Efavirenz tablets should be swallowed intact with liquid.

Concomitant Antiretroviral Therapy

Efavirenz must be given in combination with other antiretroviral medications [see Indications and Usage (1) , Warnings and Precautions (5.3) , Drug Interactions (7.1) , and Clinical Pharmacology (12.3) ].

Dosage Adjustment

If efavirenz is coadministered with voriconazole, the voriconazole maintenance dose should be increased to 400 mg every 12 hours and the efavirenz dose should be decreased to 300 mg once daily using the capsule formulation. Efavirenz tablets must not be broken [see Drug Interactions (7.1, Table 5) and Clinical Pharmacology (12.3, Tables 7 and 8)].

If efavirenz is coadministered with rifampin to patients weighing 50 kg or more, an increase in the dose of efavirenz to 800 mg once daily is recommended [see Drug Interactions (7.1, Table 5) and Clinical Pharmacology (12.3, Table 8)].

2.3 Pediatric Patients

It is recommended that efavirenz be taken on an empty stomach, preferably at bedtime. Table 1 describes the recommended dose of efavirenz for pediatric patients weighing at least 40 kg [see Clinical Pharmacology (12.3) ]. The recommended dosage of efavirenz for pediatric patients weighing 40 kg or greater is 600 mg once daily.

Table 1: Efavirenz Dosing in Pediatric Patients

b Tablets must not be crushed.

Patient Body Weight Efavirenz Daily Dose Number of Tabletsb and Strength to Administer
at least 40 kg 600 mg one 600 mg tablet

3 DOSAGE FORMS AND STRENGTHS

  • Tablets

600-mg tablets are yellow coloured, capsule-shaped, biconvex, film coated tablets debossed with ‘301’ on one side and ‘CL’ on other side.

4 CONTRAINDICATIONS

  • Efavirenz 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.
  • Coadministration of efavirenz with elbasvir and grazoprevir is contraindicated [see Warnings and Precautions (5.1) and Drug Interactions (7.1) ].

5 WARNINGS AND PRECAUTIONS

5.1 Drug Interactions

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. The most prominent effect of efavirenz at steady-state is induction of CYP3A and CYP2B6 [see Dosage and Administration (2.2) and Drug Interactions (7.1)].

5.2 QTc Prolongation

QTc prolongation has been observed with the use of efavirenz [see Drug Interactions (7.3, 7.4) and Clinical Pharmacology (12.2)]. Consider alternatives to efavirenz when coadministered with a drug with a known risk of Torsade de Pointes or when administered to patients at higher risk of Torsade de Pointes.

5.3 Resistance

Efavirenz must not be used as a single agent to treat HIV-1 infection or added on as a sole agent to a failing regimen. Resistant virus emerges rapidly when efavirenz is administered as monotherapy. The choice of new antiretroviral agents to be used in combination with efavirenz should take into consideration the potential for viral cross-resistance.

5.4 Coadministration with Related Products

Coadministration of efavirenz with ATRIPLA (efavirenz 600 mg/emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg) is not recommended unless needed for dose adjustment (eg, with rifampin), since efavirenz is one of its active ingredients.

5.5 Psychiatric Symptoms

Serious psychiatric adverse experiences have been reported in patients treated with efavirenz. In controlled trials of 1008 patients treated with regimens containing efavirenz for a mean of 2.1 years and 635 patients treated with control regimens for a mean of 1.5 years, the frequency (regardless of causality) of specific serious psychiatric events among patients who received efavirenz or control regimens, respectively, were severe depression (2.4%, 0.9%), suicidal ideation (0.7%, 0.3%), nonfatal suicide attempts (0.5%, 0), aggressive behavior (0.4%, 0.5%), paranoid reactions (0.4%, 0.3%), and manic reactions (0.2%, 0.3%). When psychiatric symptoms similar to those noted above were combined and evaluated as a group in a multifactorial analysis of data from Study 006, treatment with efavirenz was associated with an increase in the occurrence of these selected psychiatric symptoms. Other factors associated with an increase in the occurrence of these psychiatric symptoms were history of injection drug use, psychiatric history, and receipt of psychiatric medication at study entry; similar associations were observed in both the efavirenz and control treatment groups. In Study 006, onset of new serious psychiatric symptoms occurred throughout the study for both efavirenz-treated and control-treated patients. One percent of efavirenz-treated patients discontinued or interrupted treatment because of one or more of these selected psychiatric symptoms. There have also been occasional postmarketing reports of death by suicide, delusions, and psychosis-like behavior although a causal relationship to the use of efavirenz cannot be determined from these reports. Postmarketing cases of catatonia have also been reported and may be associated with increased efavirenz exposure. Patients with serious psychiatric adverse experiences should seek immediate medical evaluation to assess the possibility that the symptoms may be related to the use of efavirenz, and if so, to determine whether the risks of continued therapy outweigh the benefits [see Adverse Reactions (6.1) ].

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