Theoretic significance of pH dependence of narcotics and narcotic antagonists in clinical anesthesia

Determination of the effect of pH and temperature on pKa partition, and drug distribution coefficients in a series of common narcotics and their antagonists has shown that within the range of blood pH (7.1 to 7.7) encountered in the practice of anesthesiology, marked differences of distribution of the drugs between a model lipid (octanol) and water can occur. When these data are considered in the light of clinical experience with narcotics used in patients undergoing or recovering from surgical procedures, a correlation between the depth and duration of narcosis or the efficacy of narcotic antidotes and ventilatory status is seen. This correlation can be explained in part if the influence of blood pH on the probable CNS/blood distribution of a given drug is taken into consideration. Support is given to this proposal by representative studies in the literature. The very different drug distribution coefficients of two closely related narcotic antagonists, naloxone and naltrexone, correctly predicted the faster onset and shorter duration of the former, which was confirmed by reported clinical observations.

Medienart:

Artikel

Erscheinungsjahr:

1976

Erschienen:

1976

Enthalten in:

Zur Gesamtaufnahme - volume:55

Enthalten in:

Anesthesia and analgesia - 55(1976), 2 vom: 16. März, Seite 253-6

Sprache:

Englisch

Beteiligte Personen:

Benson, D W [VerfasserIn]
Kaufman, J J [VerfasserIn]
Koski, W S [VerfasserIn]

Themen:

059QF0KO0R
36B82AMQ7N
Journal Article
Naloxone
Narcotic Antagonists
Narcotics
Octanols
Pentazocine
RP4A60D26L
Research Support, U.S. Gov't, Non-P.H.S.
Water

Anmerkungen:

Date Completed 02.06.1976

Date Revised 03.07.2019

published: Print

Citation Status MEDLINE

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM000046388