Advertisement

Cardiovascular Drugs and Therapy

, Volume 1, Issue 1, pp 45–50 | Cite as

Onset of action of captopril, enalapril, enalaprilic acid and lisinopril in normal man

  • P. F. Semple
  • A. M. M. Cumming
  • P. A. Meredith
  • J. J. Morton
Focussed Section: ACE Inhibitors

Summary

The effects of orally administered captopril, enalapril and lisinopril on plasma concentrations of angiotensin converting enzyme (ACE), angiotensin II (ANGII) and renin (PRC) were studied over a period of 6 hours in 6 normal subjects. A further 4 subjects received intravenous enalapril and enalaprilic acid (enalaprilat). Captopril (25 mg) by mouth caused a fall in pANGII that reached a nadir 30 to 40 minutes after administration but an effect was hardly apparent after 6 hours. Enalapril (10 mg) by mouth had less marked effects on pACE and pANGII with a decline in levels first apparent 1 hour after administration and the lowest levels reached between 3 and 6 hours. Lisinopril (10 mg) produced a progressive fall in pACE and pANGII from 1 hour to reach the lowest values 6 hours after treatment. Intravenous enalaprilat (5 mg) produced an immediate sustained fall in both pACE and pANGII but intravenous enalapril (7 mg) had a biphasic inhibitory effect.

Key words

ACE inhibitors captopril enalapril enalaprilic acid lisinopril angiotensin II 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Ader R, Chatterjee IC, Ports T, et al. Immediate and sustained bemodynamic and clinical improvement in chronic heart failure by an oral and converting enzyme inhibitor.Circulation 1980; 61:931–937.Google Scholar
  2. 2.
    Hodsman GP, Isles CG, Murray GD, et al. Factors related to the first dose hypotensive effect of captopril: prediction and treatment.Br Med J 1983; 286:832–834.Google Scholar
  3. 3.
    Cleland J, Semple PF, Hodsman P, et al. Angiotensin II levels, hemodynamics and sympathoadrenal function after low-dose captopril in heart failure.Am J Med 1984; 77:880–886.Google Scholar
  4. 4.
    Biollaz JM, Schelling JL, Jacot des Combes B, et al. Enalapril maleate and a lysine analogue (MK-521) in normal volunteers: relationship between plasma drug levels and the renin-angiotensin system.Br J Clin Pharmac 1982; 14:363–368.Google Scholar
  5. 5.
    Millar JA, Derkx FHM, McLean K, Reid JL. Pharmacodynamics of converting enzyme inhibition: the cardiovascular endocrine and autonomic effects of MK-421 (enalapril) and MK521.Br J Clin Pharmac 1982; 14:347–355.Google Scholar
  6. 6.
    Patchett AA, Harris E, Tristam EW, et al. A new class of angiotensin-converting enzyme inhibitors.Nature 1980; 288:280–283.Google Scholar
  7. 7.
    Packer M, Lee WH, Yushak M, Medina N. Comparison of captopril and enalapril in patients with severe chronic heart failure.New Engl J Med 1986; 315:847–853.Google Scholar
  8. 8.
    Millar JA, Leckie BJ, Morton JJ, et al. (1980). A microassay for active and total renin concentration in human plasma based on antibody trapping.Clin Chim Acta 1980; 101:5–15.Google Scholar
  9. 9.
    Morton JJ, Webb DJ. Measurement of plasma angiotensin II.Clin Sci 1985; 68:483–484.Google Scholar
  10. 10.
    Lieberman J. Elevation of serum angiotensin-converting enzyme (ACE) level in sarcoidosis.Am J Med 1975; 59:365–372.Google Scholar
  11. 11.
    Cushman DW, Cheung HS. Spectrophotometric assay and properties of the angiotensin-converting enzyme of rabbit lung.Biochem Pharmac 1971; 20:1637.Google Scholar
  12. 12.
    Tocco DJ, Deluna FA, Duncan AEW, et al. The physiological disposition and metabolism of enalapril maleate in laboratory animals.Drug Metab Dispos 1982; 10:15–19.Google Scholar
  13. 13.
    Roulston JE, Macgregor GA. The measurement of angiotensin converting enzyme in subjects receiving captopril.New Engl J Med 1980; 303:379.Google Scholar
  14. 14.
    Macgregor GA, Markandu ND, Rouston JE, et al. Maintenance of blood pressure by the renin-apgiotensin system in normal man.Nature 1981; 291:329–331.Google Scholar
  15. 15.
    Jarrott B, Drummer D, Hooper R, et al. Pharmacokinetic properties of captopril after acute and chronic administration to hypertensive subjects.Am J Cardiol 1982; 49:1547–1549.Google Scholar
  16. 16.
    Abrams WB, Davies RD, Gomez HJ. Clinical pharmacology of enalapril.J Hypertension (Suppl 2) 1984; 21:31–36.Google Scholar
  17. 17.
    Park CS, Malvin RL, Murray RD, Cho KW. Renin secretion as a function of renal renin content in dogs.Am J Physiol 1978; 234:F506-F509.Google Scholar
  18. 18.
    Niarchos AP, Pickering TG, Laragh JM. Cardiovascular response to isometric exercise and standing in normotensive subjects during converting enzyme inhibition with teprotide.Hypertension 1982; 4:538–544.Google Scholar

Copyright information

© Martinus Nijhoff Publishing 1987

Authors and Affiliations

  • P. F. Semple
    • 1
  • A. M. M. Cumming
    • 1
  • P. A. Meredith
    • 1
    • 2
  • J. J. Morton
    • 1
  1. 1.MRC Blood Pressure UnitWestern InfirmaryGlasgow
  2. 2.University Department of Materia MedicaStobhill HospitalGlasgow

Personalised recommendations