Pharmacokinetics of a F(ab′) 2 scorpion antivenom in healthy human volunteers

Abstract

This paper presents the first study of F(ab′) 2 scorpion antivenom pharmacokinetics in humans. We have studied the pharmacokinetics of an antiscorpion venom preparation (Alacramyn™) in eight human healthy volunteers. The fabotherapic was administered as a 47.5 mg i.v. bolus. Blood samples were drawn at 0, 5, 15, 30, 45, 60, 90, 120, 180 and 360 min after antivenom administration. Subsequently, the volunteers made seven visits to the hospital. Four of them at 24 h intervals, one at day 10, and one at day 21. We measured antivenom plasmatic concentrations using a specific high sensitivity ELISA method for F(ab′) 2. The time course of F(ab′) 2 in serum of seven subjects was well described by a lineal combination of three exponential components; a four exponential component model was necessary to fit the eighth subject. The most significant antivenom pharmacokinetic parameters determined were: AUC ∞ =596.9 (369.3, 891.2) mg h l −1; V c =3.1 (2.3, 4.3) l; V ss=15.4 (12.8, 39.9) l; MRT=250.0 (218.8, 310.2) h; CL=96.6 (58.0, 139.2) ml h −1; t 1 / 2 , τ 1 (also called t 1/2, α )=0.25 (0.13, 0.37) h; t 1 / 2 , τ z (corresponding to the slowest component)=161.3 (141.0, 212.0) h.