Respiratory effects and tolerability of Mr 2264 Cl. A new opiate partial agonist in comparison with morphine and placebo.
In this double-blind, randomised, placebo-controlled cross-over study the respiratory effects of M(r) 2264 Cl 2 x 5 mg i.v., a new partial opiate receptor agonist, were investigated and compared with the respiratory effects of morphine 2 x 10 mg i.v. and placebo. As primary end-points, the slope of the rebreathing curve (dV'/dPCO2ET) and V55 (ventilation at PCO2ET = 55 mm Hg) were determined by Read's rebreathing method. The incidence of adverse events was also documented and compared. The respiratory depression after the intravenous administration of 5 mg and 10 mg M(r) 2264 Cl was comparable to the decreased sensitivity of the respiratory centre after the 20 mg morphine i.v. In contrast to morphine, a ceiling effect of M(r) 2264 Cl was found. The tolerability of M(r) 2264 Cl was comparable to that of morphine.
Zentrum der Anaesthesiologie und Wiederbelebung, Klinikum der Johann Wolfgang Goethe-Universität, Frankfurt, Germany.
M
M
Behne
D
D
Bremerich
J
J
Heinrich
H
H
Schumacher
M
M
Scherer
D000328:Adult; D018592:Cross-Over Studies; D004311:Double-Blind Method; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D009020:Morphine / Q000008:administration & dosage / Q000494:pharmacology*; D010111:Oxymorphone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D011957:Receptors, Opioid / Q000819:agonists*; D017473:Receptors, Opioid, kappa / Q000819:agonists; D017450:Receptors, Opioid, mu / Q000819:agonists; D012119:Respiration / Q000187:drug effects; D012125:Respiratory Center / Q000187:drug effects*
D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; C090192:Mr 2264; D009020:Morphine; D010111:Oxymorphone