Treprostinil

After subcutaneous infusion, treprostinil is completely absorbed, with a bioavailability of about 100%, and it reaches steady-state concentrations in approximately 10 hours.^L41860 The pharmacokinetics of treprostinil follow a two-compartment model and are linear between 2.5 and 125 ng/kg/min.^L41860 Subcutaneous and intravenous doses of treprostinil are bioequivalent at 10 ng/kg/min. Compared to healthy subjects, patients with mild and moderate hepatic insufficiency had a corresponding C_max 2- and 4-times higher and an AUC_0-? 3- and 5-times higher when given a subcutaneous treprostinil dose of 10 ng/kg/min for 150 min.^L41860 When given orally at doses between 0.5 and 15 mg twice a day, treprostinil follows a dose-proportional pharmacokinetic profile.^L41865 The oral bioavailability of treprostinil is 17%, and drug concentration reaches its highest level between 4 and 6 hours after oral administration.^L41865 The oral absorption of treprostinil is affected by food. The AUC and C_max of oral treprostinil increase 49% and 13%, respectively, when this drug is administered with a high-fat, high-calorie meal.^L41865 The AUC and C_max of inhaled treprostinil were proportional to the doses administered (18 to 90 ?g).^L41855 The bioavailability of inhaled treprostinil was 64% in patients receiving 2 doses of 18 ?g, and 72% in patients receiving two doses of 36 ?g.^L41855 Two separate studies that evaluated the pharmacokinetics of inhaled treprostinil at a maintenance dose of 54 ?g found that the mean C_max was 0.91 and 1.32 ng/mL, respectively, with a corresponding T_max of 0.25 and 0.12 hr and a mean AUC of 0.81 and 0.97 hr?ng/mL.^L41855