purdue pharma lp - Medication Listings

BUTRANS is a transdermal system providing systemic delivery of buprenorphine, a mu opioid partial agonist analgesic, continuously for 7 days. The chemical name of buprenorphine is 6,14-ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)- α-(1,1-dimethylethyl)-4, 5-epoxy-18, 19-dihydro-3-hydroxy-6-methoxy-α-methyl-, [5α, 7α, (S)]. The structural formula is: The molecular weight of buprenorphine is 467.6; the empirical formula is C 29 H 41 NO 4 . Buprenorphine occurs as a white or almost white powder and is very slightly soluble in water, freely soluble in acetone, soluble in methanol and ether, and slightly soluble in cyclohexane. The pKa is 8.5 and the melting point is about 217°C. System Components and Structure Five different strengths of BUTRANS are available: 5, 7.5, 10, 15, and 20 mcg/hour (Table 6). The proportion of buprenorphine mixed in the adhesive matrix is the same in each of the five strengths. The amount of buprenorphine released from each system per hour is proportional to the active surface area of the system. The skin is the limiting barrier to diffusion from the system into the bloodstream. Table 6: BUTRANS Product Specifications Buprenorphine Delivery Rate (mcg/hour) Active Surface Area (cm 2 ) Total Buprenorphine Content (mg) BUTRANS 5 6.25 5 BUTRANS 7.5 9.375 7.5 BUTRANS 10 12.5 10 BUTRANS 15 18.75 15 BUTRANS 20 25 20 BUTRANS is a rectangular or square, beige-colored system consisting of a protective liner and functional layers. Proceeding from the outer surface toward the surface adhering to the skin, the layers are (1) a beige-colored web backing layer; (2) an adhesive rim without buprenorphine; (3) a separating layer over the buprenorphine-containing adhesive matrix; (4) the buprenorphine-containing adhesive matrix; and (5) a peel-off release liner. Before use, the release liner covering the adhesive layer is removed and discarded. Figure 1: Cross-Section Diagram of BUTRANS (not to scale). The active ingredient in BUTRANS is buprenorphine. The inactive ingredients in each system are: levulinic acid, oleyl oleate, povidone, and polyacrylate cross-linked with aluminum. Chemical Structure Fig 1

HYSINGLA ER (hydrocodone bitartrate) extended-release tablets are supplied in 20 mg, 30 mg, 40 mg, 60 mg, 80 mg, 100 mg and 120 mg film-coated tablets for oral administration. The tablet strengths describe the amount of hydrocodone per tablet as the bitartrate salt. Hydrocodone bitartrate is an opioid agonist. Its chemical name is 4,5α-epoxy-3-methoxy-17-methylmorphinan-6-one tartrate (1:1) hydrate (2:5). Its structural formula is: Empirical formula: C 18 H 21 NO 3 ∙ C 4 H 6 O 6 ∙ 2½H 2 O; Molecular weight: 494.49. Hydrocodone bitartrate exists as fine white crystals or a crystalline powder. It is affected by light. It is soluble in water, slightly soluble in alcohol, and insoluble in ether and chloroform. The 20 mg, 30 mg, 40 mg, 60 mg, 80 mg, 100 mg and 120 mg tablets contain the following inactive ingredients: Butylated Hydroxytoluene (BHT, an additive in Polyethylene Oxide), Hydroxypropyl Cellulose, Macrogol/PEG 3350, Magnesium Stearate, Microcrystalline Cellulose, Polyethylene Oxide, Polysorbate 80, Polyvinyl Alcohol, Talc, Titanium Dioxide, and Black Ink. The 20 mg tablets also contain Iron Oxide Yellow and FD&C Blue #2 Aluminum Lake/Indigo Carmine Aluminum Lake. The 30 mg tablets also contain Iron Oxide Yellow. The 40 mg tablets also contain Iron Oxide Yellow, Iron Oxide Red, and Iron Oxide Black. The 60 mg tablets also contain Iron Oxide Yellow and Iron Oxide Red. The 80 mg tablets also contain Iron Oxide Red. The 100 mg tablets also contain FD&C Blue #2 Aluminum Lake. Black Ink Contains: Shellac Glaze (in Ethanol), Isopropyl Alcohol, Iron Oxide Black, N-Butyl Alcohol, Propylene Glycol and Ammonium Hydroxide. Chemical Structure

Nalmefene hydrochloride injection, an opioid antagonist, is a 6-methylene analogue of naltrexone. The chemical structure is shown below: Molecular Formula: C 21 H 25 NO 3 ∙HCl Molecular Weight: 375.9, CAS # 58895-64-0 Chemical Name: 17-(Cyclopropylmethyl)-4,5 a -epoxy-6-methylenemorphinan-3,14-diol, hydrochloride salt. Nalmefene hydrochloride is a white to off-white crystalline powder which is freely soluble in water up to 130 mg/mL and slightly soluble in chloroform up to 0.13 mg/mL, with a pK a of 7.6. Nalmefene hydrochloride injection is available as a sterile solution for intravenous, intramuscular, and subcutaneous administration in concentration of 1 mg of nalmefene free base per mL. The 1 mg/mL concentration contains 1.108 mg of nalmefene hydrochloride per mL, 9.0 mg of sodium chloride per mL, and the pH is adjusted to 3.9 with hydrochloric acid. Concentration and dosage of nalmefene hydrochloride injection are expressed as the free base equivalent of nalmefene. Chemical Structure

OXYCONTIN ® (oxycodone hydrochloride) extended-release tablets is an opioid agonist supplied in 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, and 80 mg tablets for oral administration. The tablet strengths describe the amount of oxycodone per tablet as the hydrochloride salt. The structural formula for oxycodone hydrochloride is as follows: C 18 H 21 NO 4 ∙ HCl MW 351.83 The chemical name is 4, 5α-epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one hydrochloride. Oxycodone is a white, odorless crystalline powder derived from the opium alkaloid, thebaine. Oxycodone hydrochloride dissolves in water (1 g in 6 to 7 mL). It is slightly soluble in alcohol (octanol water partition coefficient 0.7). The 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg and 80 mg tablets contain the following inactive ingredients: butylated hydroxytoluene (BHT), hypromellose, polyethylene glycol 400, polyethylene oxide, magnesium stearate, titanium dioxide. The 10 mg tablets also contain hydroxypropyl cellulose. The 15 mg tablets also contain black iron oxide, yellow iron oxide, and red iron oxide. The 20 mg tablets also contain polysorbate 80 and red iron oxide. The 30 mg tablets also contain polysorbate 80, red iron oxide, yellow iron oxide, and black iron oxide. The 40 mg tablets also contain polysorbate 80 and yellow iron oxide. The 60 mg tablets also contain polysorbate 80, red iron oxide and black iron oxide. The 80 mg tablets also contain hydroxypropyl cellulose, yellow iron oxide and FD&C Blue #2/Indigo Carmine Aluminum Lake. Chemical Structure

ZURNAI™ (nalmefene injection) is a sterile, pre-filled, single-dose auto-injector designed to deliver a dose of 1.5 mg nalmefene (provided as nalmefene hydrochloride) in 0.5 mL. Nalmefene hydrochloride, 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 water up to 130 mg/mL and slightly soluble in chloroform up to 0.13 mg/mL, with a pKa of 7.63. Each ZURNAI auto-injector delivers 1.5 mg nalmefene (equivalent to 1.7 mg nalmefene hydrochloride) in 0.5 mL solution. The pH range is 3.5 to 4.5. The inactive ingredients in ZURNAI nalmefene injection include: hydrochloric acid to adjust pH; magnesium chloride, 4.7 mg; and water for injection. Chemical Structure