Lisinopril pharmacokinetics in chronic renal failure

Br J Clin Pharmacol. 1988 Jun;25(6):719-24. doi: 10.1111/j.1365-2125.1988.tb05258.x.

Abstract

1. Lisinopril, a new orally active angiotensin converting enzyme inhibitor, was given to eight patients with stable chronic renal failure, in a dose of 5 mg 24 h-1 for 1 week. Creatinine clearance of the subjects ranged from 0.22 to 1.11 ml s-1. Lisinopril pharmacokinetics were studied over 8 days. 2. There was a close correlation between creatinine clearance and total 'area under the curve' over the 8 days of study (r = -0.88, P less than 0.05), and plateau lisinopril concentration and creatinine clearance (r = -0.77, P less than 0.05). 3. Serum angiotensin converting enzyme activity was inhibited in proportion to log serum lisinopril concentration (r = -0.99, P less than 0.001). Calculated IC50 was 47 ng lisinopril ml-1. from pooled data, with individual patients IC50 ranging from 20 to 70 ng lisinopril ml-1. 4. Creatinine clearance was unaltered by treatment. Serum potassium rose to over 5 mmol 1-1 in four patients, without adverse clinical effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Angiotensin-Converting Enzyme Inhibitors / pharmacokinetics*
  • Angiotensin-Converting Enzyme Inhibitors / therapeutic use
  • Blood Pressure / drug effects
  • Creatine / blood
  • Enalapril / analogs & derivatives*
  • Enalapril / blood
  • Enalapril / pharmacokinetics
  • Enalapril / therapeutic use
  • Female
  • Humans
  • Kidney Failure, Chronic / drug therapy
  • Kidney Failure, Chronic / metabolism*
  • Lisinopril
  • Male
  • Middle Aged
  • Peptidyl-Dipeptidase A / metabolism
  • Proteinuria / urine
  • Pulse / drug effects

Substances

  • Angiotensin-Converting Enzyme Inhibitors
  • Enalapril
  • Lisinopril
  • Peptidyl-Dipeptidase A
  • Creatine