Skip to main content
Log in

Nefedipine Serum Concentration; Effects upon blood pressure and heart rate in normotensive volunteers

  • Published:
European Journal of Drug Metabolism and Pharmacokinetics Aims and scope Submit manuscript

Summary

Nifedipine (10 mg) was administered orally to 8 normotensive volunteers. Various measurements such as concentration in serum, blood pressure, and heart rate, were made at 0, 20′, 40′, I, 2, 3, 4, 6, 8 and 24 h after administration.

The sample serum, internal standard (diethyl 2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate), HCl and NaN02 were allowed to react and GLC-ECD was carried out after extration with organic solvent. The retention time was 3 min for nifedipine and 4 min for internal standard.

Absorption curves were classified into 3 types: a rapid absorption rate (2 subjects) in which the maximum measured nifedipine concentration (70–80 ng/ml) was obtained, within 20–40 min after administration, a slower absorption rate (3 subjects) and an intermediate absorption rate (3 subjects) and an intermediate absorption rate (3 subjects). A decrease in systolic blood pressure was observed, but no significant difference in diastolic blood pressure and heart rate could be noted among the volunteers.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Bossert F. und Vater W., (1971): Dihydropyrine, eine neue Gruppe stark wirksamer Coronartherapeutika. Naturwissenshaften,58. 578.

    Article  CAS  Google Scholar 

  2. Vater W., Kroneberg G., Hoffmeister F. Kaller H., Meng K., Oberdorf A., Puis W., Schlolßmann K. and Stoepel K., (1972): Pharmacology of 4-(2′ -Ni trophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethylester (Nifedipine). Arzeim. Forsch.,22. 1–14.

    CAS  Google Scholar 

  3. Hashimoto K., Taira N., Ono H., Chiba S., Hashimoto K., Endoh M., Kokubun H., Iijima T., Kimura T., Kubota K. and Ogura K., Nifedipine (1975), Basis of its pharmacological effect. In 1st International Nifedipine (Adalat) Symposium. Hashimoto, Kimura and Kobayashi (Eds). pp 11–22, University of Tokyo Press, Tokyo.

    Google Scholar 

  4. Berson J. A. and Brown E., (1955): Studies on dihydropyridines. I, The preparation of unsymmetrical 4-aryll,4-dihydropyridines by the Hantzsch-Beyer synthesis. J. Am. Chern. Soc.,77. 444–447.

    Article  CAS  Google Scholar 

  5. Hantzsch A., (1882): Ueber die Synthese pyridinartiger Verbindungen aus Acetessigather und Aldehydammoniak. Justus Liebigi’s Annalen der Chemie,215. 1–82.

    Article  Google Scholar 

  6. Schlolßmann K., (1972): Fluorometrische bestimmung des 4-(2’ -nitrophenyl)-2,6-dimethyl-1,4-dihydropridin3,5-dicarbonsauredimethylester und seines hauptmetaboliten. Arzneim. Forsch.,22. 60–62. ßολιτεν Aρζνειμ Φορσωη.22. 60–62.

    Google Scholar 

  7. Pedersen O. L. and Mikkelsen E., (1971): Acute and chronic effects of nifedipine in arterial hypertension. Eur. J. Pharmacol.,14. 375–381.

    Google Scholar 

  8. Pedersen O. L., Christensen N. J. and Ramsch K., (1980): Comparison of acute effects of nifedipine in normotensive and hypertensive man. J. Cardiovasc. Pharmacol.,2, 357–366.

    Article  Google Scholar 

  9. Duhm B., Maul W., Medenwald H., Patzschke K. und Wegner L. A., (1972): Tierexperimentelle untersuchungen zur pharmakokinetik und biotransformation von radioaktive markiertem 4-(2′ -nitrophenyl)-2,6dimethyl-I,4-dihydropyridin-3,5-dicarbonsäuredimethylester. Arzneim. Forsch.,22. 42–52.

    CAS  Google Scholar 

  10. Medenwald H., SchloBmann K. und Wiinsche C., (1972): Strukturaufklaung der renalen ausscheidungsprodukte von 4-(2′ -nitrophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsauredimethylester. Armeim. Forsch.,22. 53–56.

    CAS  Google Scholar 

  11. Hoster F.A., Duhm B., Maul W., Mendenwald H., Patzschke K. und Wegner L. A., (1972): Klinische Untersuchungen zur Phamakokinetik von radioaktive markiertem 4-(2′ -ntophenyl)-2,6-dimethyl-1,4-dihydropyridin-3,5-dicarbonsauredimethylester. Arzneim. Forsch.,22. 330–334.

    Google Scholar 

  12. Higuchi S., Sasaki H. and Sado T., (1975): Determination of a new cerebral vasodilator 2,6-dimethyl-4-(3nitrophenyl)-I,4-dihydropyridine-3,5-dicarboxylic acid 3-2-(N-benzyl-N-methylamino)-ethyl ester 5-methyl ester hydrochloride (YC-93) in plasma by electron capture gas chromatography. J. Chromatogr.,110. 301–307.

    Article  CAS  PubMed  Google Scholar 

  13. Higuchi S. and Shiobara Y., (1978): Quantitative determination of nifedipine in human plasma by selected ion monitoring. Biomed. Mass Spectrom.,5. 220–223.

    Article  CAS  PubMed  Google Scholar 

  14. Jakobsen P., Pedersen O.L. and Mikkelsen E., (1979): Gas chromatographic determination of nifedipine and one of its metabolites using electron capture detection J. Chromatogr.,162. 81–87.

    Article  CAS  PubMed  Google Scholar 

  15. Kondo S., Kuchiki A., Yamamoto K., Akimoto K., Takanashi K., Awata N. and Sugimoto I., (1980): Identification of nifedipine metabolites and their determination by gas chromatography. Chern. Pharm. Bull. (Tokyo),28. 1–7.

    CAS  Google Scholar 

  16. Wagner J. G. and Nelson E., (1963): Per cent absorbed time plots derived from blood level and/or urinary excretion data. J. Pharm. Sci.,52. 1056–1062.

    Google Scholar 

  17. Olivari M.T., Bertorelli C., Polese A., Fiorentini C., Moruzzi P. and Guazzi M. D., (1979): Treatment of hypertention with nifedipine, a calcium antagonistic agent. Circulation59. 1056–1062.

    CAS  PubMed  Google Scholar 

  18. Thibonnier M., Bonnet F. and Corvol P., (1980): Antihypertensive effect of fractionated sublingual administration of nifedipine in moderate essential hypertension. Eur. J. Clin. Pharmacol.,17. 161–164.

    Article  CAS  PubMed  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Nakashima, T., Inoki, M. & Nakanishi, Y. Nefedipine Serum Concentration; Effects upon blood pressure and heart rate in normotensive volunteers. European Journal of Drug Metabolism and Pharmacokinetics 9, 73–78 (1984). https://doi.org/10.1007/BF03189607

Download citation

  • Received:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF03189607

Key-words

Navigation