Scpharmaceuticals

FUROSCIX

furosemide injection 80 mg/ 10 ml

Peak

SUBCUTANEOUS · SOLUTION

12.1 Mechanism of Action Furosemide primarily inhibits the reabsorption of sodium and chloride in the proximal and distal tubules and in the loop of Henle. The high degree of diuresis is largely due to the unique site of action. The action on the distal tubule is independent of any inhibitory effect on carbonic anhydrase and aldosterone. 12.2 Pharmacodynamics In adult patients with NYHA Class II and Class III heart failure, subcutaneous administration of FUROSCIX (30 mg furosemide over the first hour followed by 12.5 mg per hour for the subsequent 4 hours, total 80mg furosemide) produced similar diuresis and natriuresis to intravenous administration (two 40 mg bolus doses separated by 120 minutes) at 8 and 24 hour post-dose. The duration of diuretic effect with FUROSCIX is up to 8 hours after initiation of dosing. 12.3 Pharmacokinetics Absorption In adult patients with NYHA Class II-III congestive heart failure, subcutaneous infusion of FUROSCIX (30 mg furosemide over the first hour followed by 12.5 mg per hour for the subsequent 4 hours, 80 mg furosemide total), the bioavailability was 99.6% (90% CI: 94.8, 104.8) with a median T max of 4 hours relative to 80 mg intravenous furosemide (two 40-mg bolus doses separated by 120 minutes). The pharmacokinetic parameters of FUROSCIX are presented in Table 1 below: Table 1: Pharmacokinetic Data of FUROSCIX Following Subcutaneous Infusion (n = 15) Dose C max (ng/mL) AUC t (ng×hr/mL) T 1/2 (hr) AUC ∞ (ng×hr/mL) FUROSCIX: 30 mg subcutaneously infused over the first hour followed by 12.5 mg per hour for the subsequent 4 hours (total dose: 80 mg furosemide) 2040 ± 449 13000 ± 4000 3.2 ± 0.9 13100 ± 4010 Furosemide administered as 2 x 40 mg bolus doses intravenously, separated by 120 minutes (total dose: 80 mg furosemide) 8580 ± 2540 13000 ± 4050 2.6 ± 0.3 13200 ± 4170 The impact of subcutaneous edema at the administration site of FUROSCIX on drug absorption is unknown. Distribution Furosemide is extensively bound to plasma proteins, mainly to albumin. Plasma concentrations ranging from 1 mcg per mL to 400 mcg per mL are 91% to 99% bound in healthy individuals. The unbound fraction averages 2.3% to 4.1% at therapeutic concentrations. Elimination The terminal half-life of furosemide is approximately 2 hours. Metabolism Furosemide glucuronide is the only or at least the major biotransformation product of furosemide in humans. Excretion Significantly more furosemide is excreted in urine following the intravenous injection than after the tablet or oral solution. Specific Populations Pediatric Patients FUROSCIX was not evaluated in a pediatric clinical study. Based on population pharmacokinetic modeling and simulation, pediatric patients aged 6 to <17 years and weighing 43 kg and above are predicted to have comparable exposures to adult patients following FUROSCIX administration. Geriatric Patients Furosemide binding to albumin may be reduced in elderly patients. Furosemide is predominantly excreted unchanged in th

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