indivior inc. - Medication Listings

SUBLOCADE (buprenorphine extended-release) injection is a clear, viscous, colorless to yellow to amber, sterile solution for subcutaneous injection only . It is designed to deliver buprenorphine at a controlled rate over a one month period. The active ingredient in SUBLOCADE is buprenorphine free base, a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist. Buprenorphine is dissolved in the ATRIGEL ® delivery system at 18% by weight. The ATRIGEL ® delivery system is a biodegradable 50:50 poly(DL-lactide-co-glycolide) polymer and a biocompatible solvent, N -methyl-2-pyrrolidone (NMP). SUBLOCADE is provided in dosage strengths of 100 mg and 300 mg. Table 6 presents the delivered amounts of the raw materials and the approximate delivered volume for the two dosage strengths. Table 6 Amounts of Raw Materials and Delivered Volume for the Dosage Strengths Raw Materials in SUBLOCADE 100 mg Dosage 300 mg Dosage Buprenorphine 100 mg 300 mg Poly(DL-lactide-co-glycolide) 178 mg 533 mg N -methyl-2-pyrrolidone 278 mg 833 mg Approximate Delivered Volume 0.5 mL 1.5 mL The molecular weight of buprenorphine free base is 467.6, and its molecular formula is C 29 H 41 NO 4 . Chemically, buprenorphine is (2S)-2-[17-(Cyclopropylmethyl)-4,5α-epoxy-3-hydroxy-6-methoxy-6α,14-ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol. The structural formula is: Structural Formula

SUBOXONE® (buprenorphine and naloxone) sublingual film is an orange film, imprinted with a logo identifying the product and strength in white ink. It contains buprenorphine HCl, a mu-opioid receptor partial agonist, and a kappa- opioid receptor antagonist, and naloxone HCl dihydrate, an opioid antagonist, at a ratio of 4:1 (ratio of free bases). It is intended for sublingual or buccal administration and is available in four dosage strengths, 2 mg buprenorphine with 0.5 mg naloxone, 4 mg buprenorphine with 1 mg naloxone, 8 mg buprenorphine with 2 mg naloxone and 12 mg buprenorphine with 3 mg naloxone. Each film also contains polyethylene oxide, hydroxypropyl methylcellulose, maltitol, acesulfame potassium, lime flavor, citric acid, sodium citrate, FD&C yellow #6, and white ink. Chemically, buprenorphine HCl is (2S)-2-[17-Cyclopropylmethyl-4,5α-epoxy-3-hydroxy-6-methoxy-6α,14- ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol hydrochloride. It has the following chemical structure: Buprenorphine HCl has the molecular formula C 29 H 41 NO 4 • HCl and the molecular weight is 504.10. It is a white or off-white crystalline powder, sparingly soluble in water, freely soluble in methanol, soluble in alcohol, and practically insoluble in cyclohexane. Chemically, naloxone HCl dihydrate is 17-Allyl-4,5 α -epoxy-3, 14-dihydroxymorphinan-6-one hydrochloride dihydrate. It has the following chemical structure: Naloxone hydrochloride dihydrate has the molecular formula C 19 H 21 NO 4 • HCl • 2H 2 O and the molecular weight is 399.87. It is a white to slightly off-white powder and is freely soluble in water, soluble in alcohol, and practically insoluble in toluene and ether. Figure Figure

OPVEE (nalmefene) nasal spray is a pre-filled, unit-dose intranasal spray. Nalmefene, an opioid antagonist, is a 6-methylene analogue of naltrexone. The molecular structure of nalmefene is presented below: Molecular Formula: C 21 H 25 NO 3 ∙HCl Molecular Weight: 375.9, CAS # 58895-64-0 Chemical Name: 17-(Cyclopropylmethyl)-4,5α-epoxy-6-methylenemorphinan-3,14-diol, hydrochloride salt. Nalmefene is a white to off-white crystalline powder which is freely soluble in methanol and water, with a pK of 7.63. Each OPVEE nasal spray unit delivers 2.7 mg nalmefene (equivalent to 3mg nalmefene hydrochloride) in 0.1 mL solution. Inactive ingredients include benzalkonium chloride, disodium ethylenediaminetetraacetate, dodecylmaltoside, sodium chloride, and purified water. The pH range is 4.1 to 4.9. Chemical Structure

PERSERIS contains risperidone, an atypical antipsychotic. Risperidone belongs to the chemical class of benzisoxazole derivatives. The chemical designation 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl) piperidin-1-yl] ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a] pyrimidin-4-one. Its molecular formula is C 23 H 27 FN 4 O 2 and its molecular weight is 410.5 g/mol. The structural formula is: Risperidone is a white to off-white powder. It is practically insoluble in water and soluble in methanol and 0.1 N HCl. PERSERIS is available as a sterile two-syringe mixing system: a liquid syringe prefilled with the delivery system (colorless to yellow solution), and a powder syringe prefilled with risperidone (white to yellow). PERSERIS for extended release injectable suspension, for subcutaneous use, is available in 90 mg and 120 mg risperidone strengths. The quantitative composition is provided below ( Table 6 ). Table 6 PERSERIS Constituted Product Delivered Mass *PLGH poly D,L(lactide co-glycolide); 80:20 molar ratio of lactide to glycolide Component PERSERIS 90 mg PERSERIS 120 mg Risperidone 90 mg 120 mg PLGH* 228 mg 304 mg N -methyl-pyrrolidine 282 mg 376 mg Total mass 600 mg 800 mg Total volume 0.6 mL 0.8 mL Structural Formula