Pharmacokinetics of dextropropoxyphene in acute poisoning. 1978

J Schou, and H Angelo, and W Dam, and K Jensen, and J M Christensen

Dextropropoxyphene (DP) is a commonly used medicament for suicide attempts in Denmark. Death may occur from respiratory depression or cardiac arrest. Mechanical hyperventilation which induces hypocapnia seems to reduce the occurrence of cardiac complications. In an attempt to relate the clinical events to the plasma concentrations of DP and the major metabolite norpropoxyphene (NP) we studied patients with acute poisoning treated either for 48 h with induced hypocapnia by hyperventilation or under a conservative regime. Hypocapnia was found to lead to a significant increase in the plasma half-life of DP. Under conservative treatment the plasma half-life was 17.9 +/- 6.7 (S.D.) h (n = 6), while under induced hypocapnia the mean of values from 5 patients was 30.5 +/- 6.9 (S.D.) h. Maximum serum levels of DP and NP were, however, significantly higher in the intensively treated patients (n = 7) than in those treated conservatively (n = 9), though less marked for NP compared to DP (DP: 4.9 +/- 2.1/2.4 +/- 1.0 mumol/l, NP: 6.3 +/- 2.4/4.1 +/- 1.7 mumol/l). A concentration dependent renal clearance of NP was not demonstrable. Possible explanations are the following: 1) A change in disposition pattern blood/tissue of DP during hypocapnia. 2) A reduced metabolism DP to NP during hypocapnia. 3) A reduction in other routes of elimination.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D011431 Dextropropoxyphene A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect. D-Propoxyphene,Darvon,Propoxyphene,Propoxyphene Hydrochloride,Propoxyphene Hydrochloride, (R*,R*)-(+-)-Isomer,Propoxyphene Hydrochloride, (R-(R*,R*))-Isomer,Propoxyphene Hydrochloride, (R-(R*,S*))-Isomer,Propoxyphene Hydrochloride, (S-(R*,R*))-Isomer,Propoxyphene Maleate, (+)-Isomer,Propoxyphene Phosphate, (S-(R*,S*))-Isomer,Propoxyphene Sulfate, (S-(R*,S*))-Isomer,D Propoxyphene,Hydrochloride, Propoxyphene
D012121 Respiration, Artificial Any method of artificial breathing that employs mechanical or non-mechanical means to force the air into and out of the lungs. Artificial respiration or ventilation is used in individuals who have stopped breathing or have RESPIRATORY INSUFFICIENCY to increase their intake of oxygen (O2) and excretion of carbon dioxide (CO2). Ventilation, Mechanical,Mechanical Ventilation,Artificial Respiration,Artificial Respirations,Mechanical Ventilations,Respirations, Artificial,Ventilations, Mechanical
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001711 Biotransformation The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.

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