Pharmacokinetic study of alpha1-antitrypsin infusion in alpha1-antitrypsin deficiency

Chest. 1997 Sep;112(3):607-13. doi: 10.1378/chest.112.3.607.

Abstract

Objectives: To ascertain how long 120 mg/kg alpha1-antitrypsin concentrate (alpha1-AT-C), administered I.V. every 2 weeks, can maintain alpha1-antitrypsin (alpha1-AT) serum levels above 70 to 80 mg/dL. Secondary objectives were to summarize the nature, severity, and relationship of a plasma-derived alpha1-AT-C infusion to any side effects.

Methods: This was an open-label uncontrolled pharmacokinetic study. Alpha1-AT-C was administered I.V. every 2 weeks for 10 infusions in 23 patients with PIZ alpha1-AT deficiency. Serum alpha1-AT levels and neutralizing elastase activity were measured preinfusion, postinfusion, and at nadir. During two infusion periods, daily serum alpha1-AT and neutralizing elastase activities were measured on the seventh to 14th days. Five patients received BAL assays for alpha1-AT and neutralizing elastase activity. Adverse events were recorded in a patient diary and by a nurse at each infusion visit.

Results: The 120-mg/kg dose of alpha1-AT-C could not maintain nadir serum protective levels above 70 or 80 mg/dL for the entire 14-day dosing interval in most patients. None of the patients had alpha1-AT levels above 80 mg/dL for all 14 days. The serum alpha1-AT and neutralizing elastase levels correlated suggesting functional activity. The BAL alpha1-AT and neutralizing elastase activities were low and did not correlate with serum levels.

Conclusion: Alpha1-AT-C at 120 mg/kg administered every 2 weeks did not maintain nadir serum alpha1-AT levels above 70 to 80 mg/dL for a 14-day dosing interval. Higher doses every 2 weeks or decreased interval between infusions may be required.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Bronchoalveolar Lavage Fluid / chemistry
  • Cough / chemically induced
  • Drug Administration Schedule
  • Dyspnea / chemically induced
  • Fatigue / chemically induced
  • Female
  • Forced Expiratory Volume / drug effects
  • Headache / chemically induced
  • Humans
  • Infusions, Intravenous
  • Male
  • Medical Records
  • Middle Aged
  • Pancreatic Elastase / blood
  • Rhinitis / chemically induced
  • Serine Proteinase Inhibitors / administration & dosage
  • Serine Proteinase Inhibitors / adverse effects
  • Serine Proteinase Inhibitors / blood
  • Serine Proteinase Inhibitors / deficiency
  • Serine Proteinase Inhibitors / pharmacokinetics*
  • Treatment Outcome
  • Trypsin Inhibitors / administration & dosage
  • Trypsin Inhibitors / adverse effects
  • Trypsin Inhibitors / blood
  • Trypsin Inhibitors / deficiency
  • Trypsin Inhibitors / pharmacokinetics*
  • Vital Capacity / drug effects
  • alpha 1-Antitrypsin / administration & dosage
  • alpha 1-Antitrypsin / adverse effects
  • alpha 1-Antitrypsin / analysis
  • alpha 1-Antitrypsin / pharmacokinetics*

Substances

  • Serine Proteinase Inhibitors
  • Trypsin Inhibitors
  • alpha 1-Antitrypsin
  • Pancreatic Elastase