Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1985 May;85(1):263–269. doi: 10.1111/j.1476-5381.1985.tb08855.x

The potencies and selectivities of four calcium antagonists as inhibitors of uterine contractions in the rat in vivo.

M H Abel, M Hollingsworth
PMCID: PMC1916779  PMID: 4027469

Abstract

The potencies of four calcium antagonists (nifedipine, gallopamil, verapamil and diltiazem) at inhibiting uterine contractions in vivo have been assessed in the conscious ovariectomized, post-partum rat. Their selectivities for this action, relative to their effects on blood pressure and heart rate, have been compared with salbutamol. All compounds produced a dose-dependent inhibition of intra-uterine pressure cycles. The rank order of potency was salbutamol greater than nifedipine greater than diltiazem = gallopamil greater than verapamil. All compounds produced a dose-dependent fall of mean blood pressure. The rank order of potency was salbutamol greater than nifedipine greater than gallopamil greater than verapamil greater than diltiazem. Salbutamol and nifedipine produced a tachycardia, which was very marked with salbutamol. Gallopamil, verapamil and diltiazem induced a moderate tachycardia at low doses but temporary cessation of heart beat occurred at high doses. Nifedipine and diltiazem, like salbutamol, exhibited some selectivity for inhibition of uterine contractions relative to their cardiovascular actions. Gallopamil and verapamil showed no selectivity for the uterus.

Full text

PDF
263

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bolton T. B. Mechanisms of action of transmitters and other substances on smooth muscle. Physiol Rev. 1979 Jul;59(3):606–718. doi: 10.1152/physrev.1979.59.3.606. [DOI] [PubMed] [Google Scholar]
  2. Csapo A. I., Puri C. P., Tarro S., Henzl M. R. Deactivation of the uterus during normal and premature labor by the calcium antagonist nicardipine. Am J Obstet Gynecol. 1982 Mar 1;142(5):483–491. doi: 10.1016/0002-9378(82)90749-9. [DOI] [PubMed] [Google Scholar]
  3. Downing S. J., Porter D. G. Oestrogen-induced myometrial quiescence in the post-partum rat is not mediated by adrenaline or by alpha- or beta-adrenoceptor activation. J Endocrinol. 1980 Jun;85(3):405–413. doi: 10.1677/joe.0.0850405. [DOI] [PubMed] [Google Scholar]
  4. EDMAN K. A., SCHILD H. O. The need for calcium in the contractile responses induced by acetylcholine and potassium in the rat uterus. J Physiol. 1962 May;161:424–441. doi: 10.1113/jphysiol.1962.sp006897. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Forman A., Andersson K. E., Ulmsten U. Inhibition of myometrial activity by calcium antagonists. Semin Perinatol. 1981 Jul;5(3):288–294. [PubMed] [Google Scholar]
  6. Granger S. E., Hollingsworth M., Weston A. H. A comparison of several calcium antagonists on uterine, vascular and cardiac muscles from the rat. Br J Pharmacol. 1985 May;85(1):255–262. doi: 10.1111/j.1476-5381.1985.tb08854.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Hahn D. W., McGuire J. L., Vanderhoof M., Ericson E., Pasquale S. A. Evaluation of drugs for arrest of premature labor in a new animal model. Am J Obstet Gynecol. 1984 Mar 15;148(6):775–778. doi: 10.1016/0002-9378(84)90565-9. [DOI] [PubMed] [Google Scholar]
  8. Hardy R. N., Lowe K. C., McNaughton D. C. Acute responses during blood substitution in the conscious rat. J Physiol. 1983 May;338:451–461. doi: 10.1113/jphysiol.1983.sp014683. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Hollingsworth M., Schnieden H. Letter: Salbutamol and inhibition of uterine contractions. J Pharm Pharmacol. 1973 Dec;25(12):996–998. doi: 10.1111/j.2042-7158.1973.tb09992.x. [DOI] [PubMed] [Google Scholar]
  10. Liggins G. C., Vaughan G. S. Intravenous infusion of salbutamol in the management of premature labour. J Obstet Gynaecol Br Commonw. 1973 Jan;80(1):29–32. doi: 10.1111/j.1471-0528.1973.tb02126.x. [DOI] [PubMed] [Google Scholar]
  11. Narimatsu A., Taira N. Effects of atrio-ventricular conduction of calcium-antagonistic coronary vasodilators, local anaesthetics and quinidine injected into the posterior and the anterior septal artery of the atrio-ventricular node preparation of the dog. Naunyn Schmiedebergs Arch Pharmacol. 1976 Aug;294(2):169–177. doi: 10.1007/BF00507850. [DOI] [PubMed] [Google Scholar]
  12. Nayler W. G., Horowitz J. D. Calcium antagonists: a new class of drugs. Pharmacol Ther. 1983;20(2):203–262. doi: 10.1016/0163-7258(83)90040-2. [DOI] [PubMed] [Google Scholar]
  13. Spedding M. Assessment of "Ca2+ -antagonist" effects of drugs in K+ -depolarized smooth muscle. Differentiation of antagonist subgroups. Naunyn Schmiedebergs Arch Pharmacol. 1982 Feb;318(3):234–240. doi: 10.1007/BF00500485. [DOI] [PubMed] [Google Scholar]
  14. Spedding M. Changing surface charge with salicylate differentiates between subgroups of calcium-antagonists. Br J Pharmacol. 1984 Sep;83(1):211–220. doi: 10.1111/j.1476-5381.1984.tb10137.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Spedding M. Differences between the effects of calcium antagonists in the pithed rat preparation. J Cardiovasc Pharmacol. 1982 Nov-Dec;4(6):973–979. doi: 10.1097/00005344-198211000-00015. [DOI] [PubMed] [Google Scholar]
  16. Weeks J. R., Collins R. J. Factors affecting voluntary morphine intake in self-maintained addicted rats. Psychopharmacologia. 1964 Oct 14;6(4):267–279. doi: 10.1007/BF00413156. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES