ABSTRACT
Benzyloxyphenethylpiperazines are a new class of high affinity NK1 receptor antagonists. Oral bioavailability and selectivity can be fine tuned by the nature of the substituents on the basic nitrogen atom. Addition of substituents with a carboxylic acid group led to very selective and orally active NK1 antagonists free of interaction with L-type calcium channels.
Subject(s)
Neurokinin-1 Receptor Antagonists , Piperazines/chemical synthesis , Piperazines/pharmacology , Acylation , Alkylation , Animals , Biological Availability , CHO Cells , Carboxylic Acids/chemistry , Carboxylic Acids/pharmacology , Chemical Phenomena , Chemistry, Physical , Cricetinae , Crystallography, X-Ray , Guinea Pigs , Humans , Indicators and Reagents , Models, Molecular , Molecular Conformation , Nitrogen , Pulmonary Edema/chemically induced , Pulmonary Edema/prevention & control , Structure-Activity RelationshipABSTRACT
Twenty patients with major abdominal hernia were treated by prosthesis interposed in pre or intraperitoneal position by medial incision. This surgery can produce healthy respiratory morbidity. Indeed, these patients are commonly obeses and smokers. The reintegration of the viscera in the abdominal cavity increases the pressure in this cavity and pertubs the diaphragmatic motility. The association of peridural technique and propofol perfusion gives an excellent awakening combined to a good postoperative analgesia. So this association permits to obtain from patient a helpful collaboration which limits dramatically the postoperative complications.
Subject(s)
Anesthesia, Epidural/methods , Hernia, Ventral/surgery , Propofol/administration & dosage , Respiratory Tract Diseases/etiology , Aged , Blood Pressure , Female , Heart Rate , Humans , Male , Middle Aged , Physical Therapy Modalities , Postoperative Complications/prevention & control , Preanesthetic Medication , Respiratory Tract Diseases/physiopathology , Surgical MeshABSTRACT
Two hundred current surgical procedures were done in adult patients using neuroleptanalgesia with either methohexital (1 mg/kg) or etomidate induction (0.3 mg/kg) in half of the cases. The cardiovascular function was less altered with etomidate (less occurrence of tachycardia, blood pressure drops or systolo-diastolic pinching). The etomidate dosage chosen more often gave an immediate satisfactory sleep. However, with methohexital induction, less signs of awakening were observed during the surgical procedure. The frequent postoperative somnolence also points, although indirectly, to a longer residual effect of the barbiturate. Both drugs sometimes gave erythema. The injection of etomidate was more frequently painful in the arm. On the other hand, hiccups occurred with methohexital induction only. Etomidate induced myoclonia in one-third of the cases premedicated with diazepam and after preliminary injection of a minimal amount of fentanyl. Without these precautions, myoclonia can occur in two-thirds of the patients. However, these myoclonia are bothersome and of prolonged duration in rare instances and would be of real annoyance only when this drug would be used alone for surgical procedures of short duration where perfect patient immobility is required. We therefore conclude and confirm that etomidate is a good induction agent for neuroleptanalgesia anesthesia procedures.
