Clinical Information
Gen. Code and Des.
40657 efavirenz ORAL CAPSULE 200 MG
GCN and Des.
43303 efavirenz ORAL CAPSULE 200 MG
Strength
200MG
Dose Form
CAPSULE
Product Category
RX Pharmaceuticals
Fine Line Class
850085008510 All Rx Products
DEA Class
NC
OMP Family
AHFS Class
8180816 HIV NONNUCLEOSIDE REV.TRANSCRIP. INHIB.
Active Ingredients
7651 efavirenz 154598524
Inactive Ingredients
2432 lactose 64044515
2549 gelatin 9000708
SUSTIVA- efavirenz tablet, film coated
A-S Medication Solutions
1 INDICATIONS AND USAGE
SUSTIVA (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 at least 3 months old and weighing at least 3.5 kg. �
2 DOSAGE AND ADMINISTRATION
2.1 Adults
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 [ ]. Dosing at bedtime may improve the tolerability of nervous system symptoms [ and ]. SUSTIVA capsules or tablets should be swallowed intact with liquid. For patients who cannot swallow capsules or tablets, the capsule sprinkle method of administration is recommended [ ]. see Clinical Pharmacology (12.3) see , , Warnings and Precautions (5.5)Adverse Reactions (6.1)Patient Counseling Information (17)see Dosage and Administration (2.3)
Concomitant Antiretroviral Therapy
SUSTIVA must be given in combination with other antiretroviral medications [ and ]. see , , , Indications and Usage (1)Warnings and Precautions (5.2)Drug Interactions (7.1)Clinical Pharmacology (12.3)
DOSAGE FORMS AND STRENGTHS
� Capsules
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.
� Tablets
600 mg tablets are yellow, capsular-shaped, film-coated tablets, with "SUSTIVA" printed on both sides.
4 CONTRAINDICATIONS
4.1 Hypersensitivity
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.
DESCRIPTION
SUSTIVA (efavirenz) is an HIV-1 specific, non-nucleoside, reverse transcriptase inhibitor (NNRTI). Efavirenz is chemically described as (S)-6-chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Its empirical formula is C H ClF NO
Efavirenz is a white to slightly pink crystalline powder with a molecular mass of 315.68. It is practically insoluble in water (<10 microgram/mL).
SUSTIVA is available as capsules for oral administration containing either 50 mg or 200 mg of efavirenz and the following inactive ingredients: lactose monohydrate, magnesium stearate, sodium lauryl sulfate, and sodium starch glycolate. The capsule shell contains the following inactive ingredients and dyes: gelatin, sodium lauryl sulfate, titanium dioxide, and/or yellow iron oxide. The capsule shells may also contain silicon dioxide. The capsules are printed with ink containing carmine 40 blue, FD&C Blue No. 2, and titanium dioxide. Capsules:
SUSTIVA is available as film-coated tablets for oral administration containing 600 mg of efavirenz and the following inactive ingredients: croscarmellose sodium, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. The film coating contains Opadry Yellow and Opadry Clear. The tablets are polished with carnauba wax and printed with purple ink, Opacode WB. Tablets:
Microbiology
Mechanism of Action
Efavirenz is an NNRTI of HIV-1. Efavirenz activity is mediated predominantly by noncompetitive inhibition of HIV-1 reverse transcriptase. HIV-2 reverse transcriptase and human cellular DNA polymerases α, β, γ, and δ are not inhibited by efavirenz.
