Summary
Nalorphine (150 μg/kg) and levallorphan (20 μg/kg), when administered to lightly anaesthetized subjects who had not received a narcotic, caused significant depression of respiratory rate and minute volume. In contrast, 5 and 10 μg/kg naloxone caused no respiratory depression. These doses of nalorphine, levallorphan, and naloxone caused a moderate decrease of pulse rate and systolic blood pressure. Naloxone 5 and 10 μg/kg offered significantly greater protection against the respiratory depressant effects of 20 μg/kg oxymorphone administered five minutes later than 150 μg/kg nalorphine or 20 μg/kg levallorphan. None of the three narcotic antagonists affected the oxymorphone-induced decrease of pulse rate, and all had about the same protective effect against the fall of systolic blood pressure caused by this compound. Since doses of naloxone, which provide significantly better protection against narcotic-induced respiratory depression than the conventional doses of nalorphine and levallorphan, cause no respiratory depression in themselves, it should be considered the narcotic antagonist of choice for clinical use.
FrRésumé
La nalorphine (150 μ/kg) et la levallorphan (20 μg/kg), administrés à des sujets sous anesthésie légère et qui n’avaient pas reçu de narcotique, ont produit une dépression marquée du rythme respiratoire et du volume minute. Par contre, 5 et 10 μg/kg de naloxone n’ont pas causé de dépression respiratoire. Ces doses de nalorphine, de levallorphan et de naloxone ont produit une diminution modérée de la fréquence cardiaque et de la pression sanguine systolique. Cinq et dix μg/kg de naloxone ont donné une bien meilleure protection contre la dépression respiratoire produite par 20 μg/kg d’oxymorphone, administrés cinq minutes après, que 150μg/kg de nalorphine ou 20 μg/kg de levallorphan. Aucun de ces trois antagonistes des narcotiques n’a modifié le ralentissement du pouls provoqué par l’oxymorphone et tous ont exercé a peu près le même effet protecteur contre la chute de pression systolique produite par ce médicament.
Puisque des doses de naloxone, qui produisent une protection réellement meilleure contre la dépression respiratoire consécutive aux narcotiques que ne le font les doses ordinaires de nalorphine et de levallorphan, ne produisent par ellesmêmes aucune dépression respiratoire, il faudrait considérer ce produit (naloxone) comme 1’antagoniste de choix des narcotiques pour usage clinique.
Article PDF
Similar content being viewed by others
Avoid common mistakes on your manuscript.
References
Eckenhoff, J. E.;Elder, J. D., Jr.; &King, B. D. N-allyl-normorphine in the Treatment of Morphine or Demerol Narcosis. Am. J. Med. Sc.223: 191 (1952).
Eckenhoff, J. E. &Oech, S. R. Effects of Narcotics and Antagonists upon Respiration and Circulation in Man. Clin. Pharmacol. Therap.1: 483 (1960).
Fraser, H. F.;Van Horn, C. D.; &Isbell, H. Studies on N-allyl-normorphine in Man: Antagonism to Morphine Sulfate and Heroin and Effects of Mixtures of N-allyl-normorphine and Morphine. Am. J. Med. Sc.231: 1 (1956).
Huggins, R. A.;Spencer, W. A.;Geddes, L. A.;Deavers, S.; &Moyer, J. H. Respiration Functions in Man Following Intravenous Administration of Morphine, N-allyl-normorphine, and N-allyl-morphine after Morphine. Arch. Intemat. Pharmacodyn.111: 275 (1957).
Lasagna, L. &Beecher, H. K. Analgesic Effectiveness of Nalorphine-morphine Combinations in Man. J. Pharmacol. Exper. Therap.112: 356 (1954).
Salomon, A.;Marcus, P. S.;Herschfus, J. A.; &Segals, M. S. N-allyl-normorphine (Nalline) Action on Narcotized and Non-narcotized Subjects. Am. J. Med.17: 214 (1954).
Tenney, S. M. &Mithoefer, J. C. The Respiratory Depressant Action of N-allyl-normorphine in the Normal Subject and in Patients with Respiratory Acidosis Secondary to Pulmonary Emphysema. New England J. Med.249: 886 (1953).
Schwab, M.;Becker, H. M.;Koppen, E.;Podworny, M.; &Wagner, P. H. Der Einfluss des Morphin-Antagonisten (-)-N-Allyl-3-hydroxymorphinan auf die normale und die durch (-)-N-Methyl-3-hydroxymorphinan und morphin gehemmte Atmung des gesunden Menschen. Arzneimittel-Forsch.7: 283 (1957).
Swerdlow, M. Levallorphan: Effects of Large Doses. Anaesthesia.13: 318 (1958).
Thomas, D. V. &Tenney, S. M. Effect of Levorphan and Levallorphan on the Respiratory Mechanism of Normal Man. J. Pharmacol. Exper. Therap.113: 250 (1955).
Foldes, F. F.;Shapira, M.;Torda, T. A. G.;Duncalf, D.; &Shiffman, H. P. Studies on the Specificity of Narcotic Antagonists. Anesthesiology.26: 320 (1965).
Foldes, F. F. &Torda, T. A. G. Comparative Studies with Narcotics and Narcotic Antagonists in Man. Acta Anaesth. Scandinav.9: 121 (1965).
Jasinski, D. R.;Martin, W. R.; &Haertzen, C. A. The Human Pharmacology and Abuse Potential of N-allyl-noroxymorphone (Naloxone). J. Pharmacol. Exper. Therap.157: 420 (1967).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Foldes, F.F., Duncalf, D. & Kuwabara, S. The respiratory, circulatory, and narcotic antagonistic effects of nalorphine, levallorphan, and naloxone in anaesthetized subjects. Can. Anaes. Soc. J. 16, 151–161 (1969). https://doi.org/10.1007/BF03005795
Issue Date:
DOI: https://doi.org/10.1007/BF03005795