The appropriate esters 1-3 were synthesized by the alkylation of unsubstituted pyrimidin-8-on[2,1-f]theophylline I with ethyl-chloroacetate, ethyl-acrylate and ethyl-4-bromobutyrate. The acids 4-6 were obtained by hydrolysis of the esters 1-3, and transformed into Na salts 4a-6a. Amidation of the ester 1 with 25% ammonia and hydroxylamine led to amide 7 and N-hydroxyamide 8. The bromination of ...

bachground: to induce anesthesia in cesarean, thiopental is often used, and propofol may be used as an alternative. considering different effects and contradictions deriving from previous studies, this study aimed to investigate the effects of thiopental and propofol on apgar score. methods: a double blind clinical trial study was designed on pregnant women scheduled for elective cesarean. pati...

Laryngeal mask is a supraglothic instrument for ventilation of patients who are under anesthesia. Insertion of laryngeal mask requires maintaining sufficient depth of anesthesia to avoid airway reflex (gagging, coughing and spasms). The present study investigated two techniques of anesthesia with propofol-atracurium and thiopental-atracurium to facilitate insertion of the laryngeal mask, term o...

Currently available models of thiopental disposition kinetics using only plasma concentration-time data neglect the influence of intratissue diffusion and provide no direct information on tissue partitioning in individual subjects. Our approach was based on a lumped-organ recirculatory model that has recently been applied to unbound compounds. The goal was to find the simplest model that accoun...

The cerebral metabolic effects of a massive dose of thiopental (177 mg/kg) were investigated in seven dogs. The systemic circulation was supported with an extracorporeal circuit. At an infusion rate of 2 mg/kg/min, cerebral oxygen consumption (CMR(O(2))) decreased progressively until cerebral electrical silence was produced. This occurred after a mean dose of 72 mg/kg, which caused a mean decre...

OBJECTIVE To evaluate effects of medetomidine on anesthetic dose requirements, cardiorespiratory variables, plasma cortisol concentrations, and behavioral pain scores in dogs undergoing ovariohysterectomy. DESIGN Randomized, prospective study. ANIMALS 12 healthy Walker-type hound dogs. PROCEDURE Dogs received medetomidine (40 micrograms/kg [18.2 micrograms/lb] of body weight, i.m.; n = 6)...

We have compared the effect of clinical doses of propofol with thiopental on epileptiform activity in the electrocorticograms (ECoG) of 20 epileptic patients undergoing temporal lobe resection. After baseline ECoG had been obtained, with inspired concentrations of 0.5-1% isoflurane and 70% nitrous oxide to provide background anaesthesia, subjects were allocated randomly to receive boluses of ei...

In this study, we compared the effects of Type I benzodiazepine receptor-selective agonists (zolpidem, quazepam) and Type I/II non-selective agonists (zopiclone, triazolam, nitrazepam) with either an ultra-short action (zolpidem, zopiclone, triazolam) or long action (quazepam, nitrazepam) on motor coordination (rota-rod test) and muscle relaxation (traction test) following the recovery from thi...

The effect of intravenous administration of two sedatives, diazepam (0.3 mg/kg) and thiopental (6.0 mg/kg), on the vestibulo-ocular reflex (VOR) in man was investigated on 9 volunteers. The VOR was evoked with a velocity step rotation test and gain and time constant of prerotatory and postrotatory nystagmus were measured. Both drugs reduced VOR gain. Diazepam-induced reduction lasted 8 h and th...

Although it is known that there are some pharmacological differences between the structurally similar barbiturates, the underlying mechanism of action remains unclear. We have compared the effects of thiopental, thiamylal and phenobarbital on both voltage-gated calcium channels (VGCC) and N-methyl-D-aspartate (NMDA) receptors in rat hippocampal slices by determining changes in intracellular cal...