ASHP INJECTABLE DRUG INFORMATION PROCAINAMIDE HYDROCHLORIDE 1333 Procainamide Hydrochloride AHFS 24:04.04.04 Products Intact containers are packaged using nitrogen.3400 3401 Injection of air into the vial causes the solution to darken.40 Sulfites (e.g., Procainamide hydrochloride is available in 10-mL multidose vials sodium metabisulfite) are included in the formulation primarily providing 100 mg/mL or 2-mL multidose vials providing 500 mg/ 3400 to prevent discoloration that occurs as a result of oxidation of mL. Each mL of solution in the 10-mL vial also contains meth- p-aminobenzoic acid, a degradation product of procainamide ylparaben 1 mg and sodium metabisulfite 0.8 mg in water for 1916 3400 hydrochloride. The injection solution is initially colorless, injection. Each mL of solution in the 2-mL vial also contains but may turn slightly yellow over time.3400 3401 Solutions that methylparaben 1 mg and sodium metabisulfite 1.8 mg in water 3400 appear darker than a light amber color or are otherwise discol- for injection. In both vial sizes, the solution also may contain ored should not be used.3400 3401 hydrochloric acid and/or sodium hydroxide to adjust the pH.3400 Procainamide hydrochloride forms α- and β-glucosylamine Procainamide hydrochloride also is available in single-dose, 1896 3401 compounds with dextrose. The reaction proceeds rapidly, prefilled 10-mL syringes providing 100 mg/mL. Prefilled with about 10% procainamide loss in dextrose 5% occurring syringes are intended only for use in the preparation of intra- 1896 3401 in about 5 hours and 30% loss in 24 hours at 25°C. Equilib- venous infusion solutions. Each mL of solution also contains rium is achieved with about 62% of the procainamide present benzyl alcohol 9 mg and sodium bisulfite 0.9 mg in water for 1896 3401 as glucosylamines. The bioavailability, activity, and meta- injection. The solution also may contain hydrochloric acid 546 1896 3401 bolic fate of these compounds is not known. The α- and and/or sodium hydroxide to adjust the pH. β-glucosylamine compounds that form are reversible,1422 1896 pH although the extent of reversibility in plasma has been ques- 2051 Procainamide hydrochloride injection solution has a pH adjusted tioned. The rate and extent of complex formation are depen- to 5 (ranges from 4 to 6).3400 3401 dent on the dextrose concentration and the solution pH but are independent of the procainamide hydrochloride concen- Administration tration.1422 In dextrose concentrations ranging from 1 to 5%, the extent of procainamide complex formation ranged from Procainamide hydrochloride may be administered by intramus- 6% in 2 days in dextrose 1% up to 351422 to 60%1896 in dextrose 3400 cular or direct intravenous injection or intravenous infusion. 5%. Lowering the pH from the normal 4.5 to 1.4 with 0.01 N 3401 Manufacturers recommend that procainamide hydrochlo- hydrochloric acid completely prevented complex formation.1422 ride injection solution be diluted to a final volume with dextrose Similarly, increasing the solution pH to 8 is reported to block 5% prior to intravenous use in order to facilitate control of the complexation.1423 Maximum complex formation occurred at pH 3400 3401 administration rate. 3 to 51423 or 4 to 5.2,1358 the natural pH of procainamide hydro- If procainamide hydrochloride is administered as a direct chloride admixtures in dextrose 5%. The clinical importance of injection into a vein or into the tubing of an established intra- this complexation, if any, is uncertain. venous line, the drug should be administered slowly, and the Procainamide hydrochloride (Sandoz) 100 mg/mL repack- 3400 3401 rate of administration should not exceed 50 mg/min. aged in clear glass vials exhibited less than 10% loss in 193 days 3400 3401 Alternatively, a loading infusion may be administered. To stored at 23°C when exposed to light and 5°C when protected prepare a 20-mg/mL initial loading infusion, 1 g of procainamide from light.3402 All solutions of procainamide hydrochloride hydrochloride should be diluted to 50 mL with dextrose 5% for stored at 23°C exposed to light exhibited an increase or dark- intravenous administration at a rate of 1 mL/min for 25 to 30 ening of yellow color; however, the 100-mg/mL solution stored 3400 3401 minutes. in glass vials exhibited a more intense color as compared with Maintenance infusions of 2 mg/mL or 4 mg/mL (for fluid-re- 3-mg/mL solutions diluted in sodium chloride 0.9% stored in stricted patients) should be prepared by diluting 1 g of procain- polyvinyl chloride (PVC) bags.3402 Solutions stored in either amide hydrochloride to 500 or 250 mL, respectively, with container at 5°C and protected from light did not exhibit such dextrose 5%.3400 3401 Intravenous infusions with a final concen- color changes.3402 tration of 2 mg/mL may be administered at a rate of 1 to 3 mL/ min; infusions with a final concentration of 4 mg/mL may be Sorption administered at a rate of 0.5 to 1.5 mL/min.3400 3401 Procainamide hydrochloride was shown not to exhibit sorption to PVC bags and tubing, polyethylene tubing, Silastic tubing, Stability and polypropylene syringes.536 606 Intact vials and prefilled syringes of procainamide hydrochlo- ride should be stored at controlled room temperature.3400 3401 DOI: 10.37573/9781585286850.325 1334 PROCAINAMIDE HYDROCHLORIDE ASHP INJECTABLE DRUG INFORMATION Compatibility Information Solution Compatibility Procainamide HCl Test Soln Name Mfr Mfr Conc/L or % Remarks Ref C/I Dextrose 5% in sodium MGa b SQ 4 g 17% loss at room temperature and 5% loss at 4°C in 24 hr 522 I chloride 0.9% Dextrose 5% HOS, IMS 2, 4, and 20 g Manufacturer-recommended solution 3400, 3401 C Dextrose 5%c BAb ASC 4 and 8 g 10% or less loss in 24 hr at room temperature and under 1327 C refrigeration Dextrose 5% TRa SQ 1 g No loss in 8 hr but 12% loss in 24 hr at room temperature 545 I Dextrose 5% BAb ASC 4 and 8 g 12 to 14% loss in 12 hr at room temperature. 6 to 10% loss in 1327 I 24 hr under refrigeration Dextrose 5% TR ES 4 g 24% loss in 24 hr at room temperature in light 1358 I Dextrose 5% LY 4 and 10 g Physically compatible with 14 to 15% loss in 4 hr at 22°C 1419 I Dextrose 5% AB SQ 2 g 10% loss in 5 hr and 30% loss in 24 hr at 25°C due to reaction 1896 I with dextrose Sodium chloride 0.45% LY 4 and 10 g Physically compatible with no loss in 4 hr at 22°C 1419 C Sodium chloride 0.9% TRa SQ 1 g No decomposition in 24 hr at room temperature 545 C Sodium chloride 0.9% BAb SZ 3 g Less than 10% loss in 193 days at 23°C exposed to light. 3402 C Slightly increased concentration, likely due to evaporation, after 28 days, and increase in yellow color Sodium chloride 0.9% BAb SZ 3 g Less than 10% loss in 193 days at 5°C protected from light 3402 C a Tested in glass containers. b Tested in PVC containers. c Adjusted to approximately pH 7.5 with sodium bicarbonate 8.4%. Additive Compatibility Procainamide HCl Test Drug Mfr Conc/L or % Mfr Conc/L or % Test Solution Remarks Ref C/I Amiodarone HCl LZ 1.8 g SQ 4 g D5W, NSa Physically compatible. 5% or less amiodarone loss 1031 C in 24 hr at 24°C in light Atracurium BW 500 mg 4 g D5W Physically compatible and atracurium stable for 1694 C besylate 24 hr at 5 and 30°C Dobutamine HCl LI 1 g SQ 1 g D5W, NS Physically compatible with no color change in 24 789 C hr at 25°C Dobutamine HCl LI 1 g AHP 4 and 50 g D5W, NS Physically compatible for 24 hr at 21°C 812 C Esmolol HCl DU 6 g ES 4 g D5W 43% procainamide loss in 24 hr at room tempera- 1358 I ture under fluorescent light Ethacrynate MSD 50 mg SQ 1 g NS Altered UV spectra at room temperature 16 I sodium Flumazenil RC 20 mg ES 4 g D5Wb Visually compatible. No flumazenil loss in 24 hr at 1710 C 23°C in fluorescent light. Procainamide not tested Lidocaine HCl AST 2 g SQ 1 g D5W, LR, NS Physically compatible for 24 hr at 25°C 775 C.