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Sublingual captopril — a pharmacokinetic and pharmacodynamic evaluation


In this study we compared the pharmacokinetics and pharmacodynamics of captopril after sublingual and peroral administration. Single 25 mg doses of captopril were administered sublingually and perorally on two different occasions in a randomised cross-over fashion to eight healthy volunteers aged 22–35 years. The kinetics of unchanged captopril, plasma renin activity (PRA), BP and heart rate were studied over three hours after both peroral and sublingual administration of captopril.

Mean pharmacokinetic parameters for unchanged captopril after sublingual administration were: Cmax, 234 ng·ml−1; tmax, 45 min; AUC (0–3 h), 15.1 μg·ml−1. min. Mean pharmacokinetic parameters for unchanged captopril after peroral administration were: Cmax, 228 ng·ml−1; tmax, 75 min; AUC (0–3 h), 17.0 μg·ml−1. min. tmax was significantly shorter when captopril was administered sublingually; all other pharmacokinetic parameters were equivalent.

The plasma captopril concentrations achieved post drug administration led to increases in PRA and reductions in BP. tmax for PRA was 86 min for sublingual captopril and 113 min for perorally administered drug. Peak PRA values were, however, not significantly different. BP, as expected, was not reduced dramatically in these healthy volunteer subjects, however, in systolic BP vs time profiles, BP was significantly lower after volunteers received sublingual captopril. Heart rate increased slightly after captopril administration; there were no differences between the two routes of administration. Administration of captopril sublingually, therefore led to a more rapid attainment of plasma captopril concentrations and had a more rapid onset of pharmacological effect when compared with peroral administration.

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  1. Al-Furaih T, Elborn JS, McElnay JC, Nicholls DP, Scott MG, Stanford CF (1988) Influence of pH on the buccal absorption of captopril. Br J Clin Pharmacol 26: 656–657

  2. Dessi-Fulgheri P, Bandiera F, Rubattu S, Cocco F, Madeddu P, Oppes M, Tonolo GC, Glorioso N, Rappelli A (1987) Comparison of sublingual and oral captopril in hypertension. Clin Exper Hypertension A9: 593–597

  3. Duchin KL, McKinstry DN, Cohen AI, Migdalof BH (1988) Pharmacokinetics of captopril in healthy subjects and in patients with cardiovascular diseases. Clin Pharmacokinet 14: 241–259

  4. Hauger-Klevene JH (1986a) Comparison of sublingual captopril and nifedipine. Lancet II: 219

  5. Hauger-Klevene JH (1986b) Effect of a single dose of sublingual captopril in hypertension patients. Eur J Clin Pharmacol 30: 379–380

  6. Martines Amenos A, Carratala J, Pinto X, Santalo M, Tamayo C, Pujol YM (1987) Hypertensive crisis: a comparative study of oral captopril, sublingual captopril and sublingual nifedipine. Medicina Clinica 89 (Suppl 2): 59–61

  7. McMurray JJ, Struthers AD (1988) Captopril in patients with ileus. Lancet II: 471

  8. Ohman KP, Kagedal B, Larsson R, Kalberg BE (1985) Pharmacokinetics of captopril and its effect on blood pressure during acute and chronic administration and in relation to food intake. J Cardiovasc Pharmacol 7: S20-S24

  9. Pereira CM, Tam YK, Collins-Nakai RL, Ng P (1988) Simplified determination of captopril in plasma by high performance liquid chromatography. J Chromatogr (Biomed Appl), 425: 208–213

  10. Tschollar W, Belz GG (1985) Sublingual captopril in hypertensive crises. Lancet II: 34–35

  11. Tschollar W, Belz GG, Essig J, Runge J, Wellstein A (1987) Fast and safe blood pressure reduction from sublingual captopril. J Am Coll Cardiol 9 [Suppl 2]: 226A

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Al-Furaih, T.A., McElnay, J.C., Elborn, J.S. et al. Sublingual captopril — a pharmacokinetic and pharmacodynamic evaluation. Eur J Clin Pharmacol 40, 393–398 (1991).

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Key words

  • Captopril
  • sublingual
  • pharmacokinetics
  • pharmacodynamics