CONTRAVE Extended-release tablet Ref.[50756] Active ingredients: Bupropion Naltrexone

CONTRAVE extended-release tablets contain naltrexone hydrochloride (HCl) and bupropion HCl.

Naltrexone HCl, USP, an opioid antagonist, is a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone differs in structure from oxymorphone in that the methyl group on the nitrogen atom is replaced by a cyclopropylmethyl group. Naltrexone HCl is also related to the potent opioid antagonist, naloxone, or n-allylnoroxymorphone.

Naltrexone HCl has the chemical name of morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, hydrochloride, (5α)-. The empirical formula is C₂₀H₂₃NO₄•HCl and the molecular weight is 377.86.

The structural formula is:

Naltrexone HCl is a white to yellowish, crystalline compound. It is soluble in water to the extent of about 100 mg/mL.

Bupropion HCl is an antidepressant of the aminoketone class. Bupropion HCl closely resembles the structure of diethylpropion. It is designated as (±)1(3 chlorophenyl)2[(1,1-dimethylethyl)amino]-1-propranone hydrochloride. It is related to phenylethylamines. The empirical formula is C₁₃H₁₈ClNO•HCl and the molecular weight is 276.2.

The structural formula is:

Bupropion HCl powder is white, crystalline, and highly soluble in water.

CONTRAVE is available for oral administration as a round, bi-convex, film-coated, extended-release tablet. Each tablet has a trilayer core composed of two drug layers, containing the drug and excipients, separated by a more rapidly dissolving inert layer. Each tablet contains 8 mg of naltrexone HCl and 90 mg of bupropion HCl. Tablets are blue and are debossed with NB-890 on one side. Each tablet contains the following inactive ingredients: microcrystalline cellulose, hydroxypropyl cellulose, lactose anhydrous, L-cysteine hydrochloride, crospovidone, magnesium stearate, hypromellose, edetate disodium, lactose monohydrate, colloidal silicon dioxide, Opadry II Blue and FD&C Blue #2 aluminum lake.