• Toxicological Research
• /
• v.7 no.1
• /
• pp.29-35
• /
• 1991

Barbiturates are commonly abused tranquilizer and a rapid method to determine these drugs in biological samples is needed. In this study, was screened barbiturates in urine specimens by the fluorescence polarization immunoassay method(FPIA) and the positive samples were confirmed and identified by the more definitive GC/MS method. Fifteen positive smples which have barbiturate values higher than 0.5 ng/ml were analyzed by the GC/MS method. Eight samples were identified as phenobarbital and five samples were identified as crotilbarbitone.

• YAKHAK HOEJI
• /
• v.25 no.4
• /
• pp.167-173
• /
• 1981

Spectroscopic investigation has been carried out to know the binding mechanism of riboflavin with barbiturates, such as phenobarbital and amobarbital in chloroform solution by using infrared and nuclear magnetic resonance spectra. Phenobarbital and isoalloxazine form a 1:1 cyclic hydrogen bonded dimer through the 3-N imino and the 2-C carbonyl groups of the isoalloxazine ring of the latter, and the 1-N (or 3-N) imino and the 2-C carbonyl groups of the pyrimidine ring of the former. Amobarbital and riboflavin form a 1:1 cyclic hydrogen bonded dimer by the same mode of phenobarbital.

• BMB Reports
• /
• v.33 no.3
• /
• pp.221-227
• /
• 2000

The distribution of barbiturates in the model membranes of total lipids (SPMVTL) and total phospholipids (SPMVPL) extracted from synaptosomal plasma membrane vesicles was determined by employing a fluorescent probe technique. The two fluorescent probes 2-(9-anthroyl)stearic acid and 12-(9-anthroyl)stearic acid were utilized as probes for the surface and the hydrocarbon interior of the outer monolayer of the SPMVTL and SPMVPL, respectively. The Stern-Volmer equation of fluorescent quenching was modified to calculate the relative distribution. The analysis of preferential quenching of these probes by barbiturates indicates that pentobarbital, hexobarbital, amobarbital and phenobarbital are predominantly distributed on the surface area, while thiopental sodium has an accessibility to the hydrocarbon interior of the outer monolayer of the SPMVTL and SPMVPL. From these results, it is strongly suggested that the more effective penetration into the hydrocarbon interior of the outer monolayer of the membrane lipid bilayer could result in a higher general anesthetic activity.

• Journal of Veterinary Clinics
• /
• v.16 no.2
• /
• pp.352-362
• /
• 1999

Thiopental sodium is known as ultrashort-acting barbiturates and can be employed advantageously for numerous conditions. But thiopental has the side effects of cardiovascular and respiratory systems which has barbiturates and are depend on the dose of thiopental. The side effects are reduced when the thiopental is preceded by a tranquilizer and sedative. In these drugs, benzodiazepines have the minimal effects of cardiovascular and respiratory systems. In this study, the effects of midazolam preanesthetic administration, followed by thiopental anesthetic induction, on cardiovascular system and thiopental induction requirement were studied in 14 mixed breed dogs. Cardiovascular data were recorded baseline, after premedication of saline 0.45 ml/kg or midazolam 0.1, 0.2, 0.4, 0.8 mg/kg, intubation, and 5, 10, 15, 20, 30 minutes after intubation. Extubation, head-up, sternal recombency, standing, and walking recovery times were recorded. The results were summarized as follows; (1) The 0.1, 0.2, 0.4, and 0.8 mg/kg dosages of midazolam insignificantly decreased thiopental dose requirement necessary to accomplish intubation by 6, 20, 21 and 28%. (2) The 0.1, 0.2, 0.4, and 0.8 mg/kg dosages of midazolam insignificantly reduced the times of extubation, head-up, sternal recumbency, standing, and walking recovery. (3) Midazolam was effective in reducing the frequency and duration of arrhythmia after intubation. (4) Heart rates of preanestheic midazolam administraion groups increased after thiopental injection which insignificantly changed smaller than those of control group. (5) Arterial blood pressures did not vary significantly among groups.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.spc8
• /
• pp.2883-2884
• /
• 2011

• Archives of Pharmacal Research
• /
• v.15 no.2
• /
• pp.184-186
• /
• 1992

Malonic acid amides were synthesized using different amino acids and their esters. THe synthesized compounds were evaluated for their sedative activity on rats. Potentiating effect of all the compounds on pentobarbitone induced sleep on rats was observed. Plasma protein binding studies were also carried out and it was observed that the synthesized compounds have low plasma protein binding as compared to barbiturates.

• The Korean Journal of Physiology and Pharmacology
• /
• v.2 no.3
• /
• pp.287-295
• /
• 1998

Diazepam is known to have cardiovascular depressive effects through a combined action on benzodiazepinergic receptor and the GABA receptor-chloride ion channel complex. Moreover, it is known that barbiturates also have some cardiovascular regulatory effects mediated by the central GABAergic system. Therefore, this study was undertaken to delineate the regulatory actions and interactions of these systems by measuring the responses of the cardiovascular system and renal nerve activity to muscimol, diazepam and pentobarbital, administered intracerebroventricularly in rabbits. When muscimol $(0.03{\sim}0.3\;{\mu}\;g/kg)$, diazepam $(10{\sim}100\;{\mu}\;g/kg)$ and pentobarbital $(1{\sim}10\;{\mu}\;g/kg)$ were injected into the lateral ventricle of the rabbit brain, there were similar dose-dependent decreases in blood pressure (BP) and renal nerve activity (RNA). The relative potency of the three drugs in decreasing BP and RNA was muscimol ＞ pentobarbital ＞ diazepam. Muscimol and pentobarbital also decreased the heart rate in a dose-dependent manner; however, diazepam produced a trivial, dose-independent decrease in heart rate. Diazepam $(30\;{\mu}g/kg)$ augmented the effect of muscimol $(0.1\;{\mu}g/kg)$ in decreasing blood pressure and renal nerve activity, but pentobarbital $(3\;{\mu}g/kg)$ did not. Bicuculline $(0.5\;{\mu}g/kg)$, a GABAergic receptor blocker, significantly attenuated the effect of muscimol in decreasing BP and RNA, either alone or with diazepam, and that of pentobarbital in decreasing BP and RNA, either alone or with muscimol. We inferred that the central benzodiazepinergic and barbiturate systems help regulate peripheral cardiovascular function by modulating the GABAergic system, which adjusts the output of the vasomotor center and hence controls peripheral sympathetic tone. Benzodiazepines more readily modulate the GABAergic system than barbiturates.

• Journal of Pharmaceutical Investigation
• /
• v.9 no.4
• /
• pp.1-7
• /
• 1979

The analytical method of phenobarbital and mephobarbital in the pharmaceutical preparation were investigated by the partition chromatographic method. The influence of 13 kinds of excipients and various kinds of ingredients such as 8 kinds of antipyretics and 5 kinds of antacids on the partition chromatographic analysis of phenobarbital and mephobarbital in the preparation were investigated. The results were not affected by materials with the exception of caffeine, aspirin and sulpyrin.

• Korean Journal of Veterinary Research
• /
• v.14 no.1
• /
• pp.41-44
• /
• 1974

The effect of Panax ginseng on the sleeping time of chicken anesthetized with pentobarbital sodium were observed to elucidate the influence of ginseng on the duration of action of barbiturates. The results were as follows: 1. By the oral administration of ginseng powder(0.1~0.6 g/day/head for a week) shortened the sleeping time of very young chicken anesthetized with pentobarbital sodium.

• Biomolecules & Therapeutics
• /
• v.4 no.3
• /
• pp.232-238
• /
• 1996

The physical dependence potency of DA-5018, a non-narcotic analgesic agent, was tested in mice dosed with 0.5 and 4 mg/kg/day for 2 months and daily increasing doses of 1, 2, 4, 6, 8 and 10 mg/kg over 10 days. Physical dependence was assessed taking natural withdrawal induced morphine-type abstinence (jumping, falling, biting or backward locomotion, rearing etc.) as well as barbiturates-type abstinence (body weight reduction, convulsion, ataxia etc.) into consideration. The results were compared with those after the same daily increasing doses of morphine. DA-5018 did not show evidence of physical dependence liability or abuse potential as measured by morphine-type or barbiturate-type abstinence signs following daily increasing or 2-month repeated administration. On the other hand, daily increasing doses of morphine produced physical dependence and the dependent state disappeared about 6 hours after the start of withdrawal signs. In the single dose suppression test, a single dose of morphine completely suppressed natural withdrawal signs that appeared in morphine-dependent animals. Therefore, these results indicate that DA-5018 does not have abuse potential and physical dependence liability.