morphinans and Wounds-and-Injuries

In a previous study concerning balanced anesthesia we realized that the adrenergic sympathetic reaction caused by intubation could not be suppressed by nalbuphine-HCl (NAL), a new narcotic agonist-antagonist in the same way as by fentanyl (FE). The aim of the study was to investigate whether the observed autonomic reaction could be overcome by: (a) varying the interval between injection of NAL and intubation or (b) increasing the induction-dose of NAL. MATERIALS and METHODS. After receiving institutional approval and the patients' written informed consent, a two-part randomized trial arrangement was made using two groups of 10 surgical patients each. During the first part the induction-dose of NAL was 1.5 mg/kg BW and that of FE was 0.005 mg/kg BW. Midazolam 0.15 mg/kg BW was the induction hypnotic. Orotracheal intubation was performed 15 min after NAL and 10 min after FE injection. During the second part, the NAL dosage was 2.5 mg/kg BW and intubation was carried out 10 min after opiate injection. Induction conditions in the FE group were unchanged. RESULTS. NAL causes adrenergic sympathetic hemodynamic and autonomic reactions immediately after injection (Figs. 1a + b, 2a + b). The rate-pressure product increase during intubation is significantly higher after NAL than after FE administration and cannot be suppressed by increasing the dosage or increasing the injection-intubation interval. In contrast, the postoperative period is characterized by long-lasting analgesia (114 min vs 82 min in the FE group) and sedation, especially after administration of 2.5 mg/kg BW NAL. CONCLUSION. These results may be explained by the agonist-antagonist activity of NAL at the opiate receptor sites.

Topics: Adult; Anesthesia, General; Anesthesia, Inhalation; Anesthesia, Intravenous; Blood Pressure; Clinical Trials as Topic; Dose-Response Relationship, Drug; Female; Fentanyl; Heart Rate; Humans; Male; Morphinans; Nalbuphine; Random Allocation; Respiration; Wounds and Injuries

One new morphinane alkaloid, sinomenine N-oxide (1), and one new natural occurring morphinane alkaloid, N-demethylsinomenine (2), together with six known alkaloids, 7,8-didehydro-4-hydroxy-3,7-dimethoxymorphinan-6-ol (3), sinomenine (4), sinoacutine (5), N-norsinoacutine, acutumine, and acutumidine, were isolated from the stems of Sinomenium acutum. Their structures were elucidated on the basis of spectroscopic analysis and chemical methods. Compounds 2, 3, and 5 have protective effects against hydrogen peroxide-induced cell injury.

Topics: Alkaloids; Animals; Drugs, Chinese Herbal; Hydrogen Peroxide; Molecular Structure; Morphinans; Nuclear Magnetic Resonance, Biomolecular; PC12 Cells; Plants, Medicinal; Rats; Sinomenium; Wounds and Injuries

Forty-six patients with moderate to severe pain caused by orthopedic injuries, burns, multiple trauma, or intraabdominal conditions were treated with intravenous (IV) nalbuphine hydrochloride (Nubain; DuPont Pharmaceuticals, Wilmington, DE) by paramedics before arrival at the hospital. Patients who weighed less than 60 kg received 15 mg nalbuphine, and patients weighing greater than 60 kg received 20 mg nalbuphine. Forty-one of 46 patients (89%) experienced pain relief from nalbuphine, with maximum relief occurring within 15 minutes after the administration of the drug. Two addicted patients received no pain relief. There were no untoward side effects following nalbuphine administration, and the patients' heart rates, mean arterial pressures, and respiratory rates remained constant and stable throughout the study period. Repeated assessment of the patient by paramedics in the field was not impaired by nalbuphine treatment. In summary, nalbuphine hydrochloride is a useful and safe analgesic drug for IV use by paramedics in the prehospital setting.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Emergencies; Emergency Medical Technicians; Female; Humans; Male; Middle Aged; Morphinans; Nalbuphine; Pain; Wounds and Injuries

Topics: Acepromazine; Analgesics; Animals; Castration; Cesarean Section; Cyclopropanes; Dog Diseases; Dogs; Drug Combinations; Evaluation Studies as Topic; Female; Male; Morphinans; Neoplasms; Neuroleptanalgesia; Pentanols; Pregnancy; Tooth Extraction; Wounds and Injuries