pacira pharmaceuticals, inc. - Medication Listings

EXPAREL (bupivacaine liposome injectable suspension) is a sterile, non-pyrogenic white to off-white preservative-free aqueous suspension consisting of multivesicular liposomes containing bupivacaine. Bupivacaine is present at a concentration of 13.3 mg/mL. After injection of EXPAREL, bupivacaine is released from the multivesicular liposomes. EXPAREL is for infiltration or perineural use. Active Ingredient Bupivacaine is related chemically and pharmacologically to the amide-type local anesthetics. It is a homologue of mepivacaine and is related chemically to lidocaine. All three of these anesthetics contain an amide linkage between the aromatic nucleus and the amino, or piperidine group. They differ in this respect from the procaine-type local anesthetics, which have an ester linkage. Chemically, bupivacaine is 1-butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide with a molecular weight of 288.4. Bupivacaine has the following structural formula: Chemical Structure EXPAREL The median diameter of the liposome particles in EXPAREL ranges from 24 to 31 μm. The liposomes are suspended in a 0.9% Sodium Chloride Injection. Each vial contains bupivacaine at a nominal concentration of 13.3 mg/mL. Inactive ingredients and their nominal concentrations are: cholesterol, 4.7 mg/mL; 1, 2-dipalmitoyl-sn-glycero-3 phospho-rac-(1-glycerol) sodium salt (DPPG), 0.9 mg/mL; tricaprylin, 2.0 mg/mL; 1, 2-dierucoylphosphatidylcholine (DEPC), 8.2 mg/mL; phosphoric acid to adjust pH; and sodium chloride to adjust tonicity. The pH of EXPAREL is in the range of 5.8 to 7.4. Bupivacaine in EXPAREL has different functional properties relative to those of the unencapsulated or nonlipid-associated bupivacaine products. Bupivacaine that is released from EXPAREL has a different pharmacokinetic and systemic profile relative to other bupivacaine products. In addition, the nominal weight percent concentration of bupivacaine in EXPAREL is based on bupivacaine free base rather than bupivacaine HCl (100 mg of bupivacaine HCl contains 88.6 mg of bupivacaine free base) [see Dosage and Administration (2.1) ].

ZILRETTA (triamcinolone acetonide extended-release injectable suspension) is a microsphere formulation of triamcinolone acetonide, a corticosteroid, to be administered by intra-articular injection. ZILRETTA is formulated in 75:25 poly(lactic-co-glycolic acid) (PLGA) microspheres with a nominal drug load of 25% (w/w) and is provided as a sterile white to off-white powder. ZILRETTA is prepared with a supplied diluent containing an isotonic, sterile, aqueous solution of sodium chloride (NaCl; 0.9% w/w), sodium carboxymethylcellulose (CMC; 0.5% w/w), polysorbate-80 (0.1% w/w) and with sodium hydroxide (NaOH) and hydrochloric acid (HCl) as pH adjusters, as required to form a 5 mL sterile suspension intended for intra-articular injection. Active Ingredient The chemical name for triamcinolone acetonide is 9-fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene- 3,20-dione cyclic 16,17-acetal with acetone. Its structural formula is: MW 434.50 with a molecular formula of C 24 H 31 FO 6 Triamcinolone acetonide occurs as a white to almost white, crystalline powder having not more than a slight odor and is practically insoluble in water and very soluble in alcohol. Each vial of ZILRETTA powder contains 40 mg of triamcinolone acetonide in 160 mg of microspheres, resulting in 32 mg of deliverable triamcinolone acetonide when prepared according to the Instructions for Use. Chemical Structure