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PubMed1998

Supercritical fluid extraction and negative ion electrospray liquid chromatography tandem mass spectrometry analysis of phenobarbital, butalbital, pentobarbital and thiopental in human serum.

Four commonly used barbiturates (phenobarbital, butalbital, pentobarbital and thiopental) were analyzed in human serum using supercritical fluid extraction (SFE) and negative ionization LC/ESI-MS/MS. Barbital was used as the internal standard. Carbon dioxide SFE was performed at 40 degrees C and 500 atm, with a total extraction time of 35 min. The analytes were collected off-line in a liquid trap containing absolute methanol. Samples were then concentrated by vacuum centrifugation. The high performance liquid chromatography separation utilized gradient elution with a total analysis time of 21 min. The precursor and major product ions for the four barbiturates were monitored on a triple quadrupole mass spectrometer with negative ion electrospray ionization (ESI) in the multiple reaction monitoring mode as follows: (1) thiopental (m/z 241.20-->58.00), (2) phenobarbital (m/z 231.10-->188.0), (3) pentobarbital (m/z 225.10-->181.90) and (4) butalbital (m/z 222.80-->179.90). In the case of phenobarbital, pentobarbital and butalbital, the most abundant product ion arises from the loss of 43 u (HCNO loss). However, in the case of thiopental, the most abundant product ion was observed at m/z 58.0 (the [M-183]-ion, or NCS-). Mechanisms for the formation of the collision induced dissociation reaction products of these barbiturates are proposed.

Barbiturates↗
PubMedDate not supplied

Interrelation between plasma protein binding, rate of injection and the anaesthetic effect of thiopental.

1. Following thiopental injection to rabbits in doses of 5 mg kg-1 intravenously (i.v.) the sleeping time lasted longer after injection by bolus than after administration made more slowly over 30 or 60s, respectively. 2. Peak concentration in the blood of the animals after bolus injection was about four time higher than after slow injection. 3. The determination of protein binding showed that the unbound fraction of thiopental at the high concentration following bolus injection is almost doubled compared with the unbound concentration following the slow injections. Therefore it is concluded that this contributes to an increased concentration of thiopental in the brain during the initial phase of distribution thus extending the sleeping time. 4. The results from experiments using a distribution model give additional evidence supporting this conception.

Anesthesia, Intravenous↗
PubMed1989

Thiopental infusion in the treatment of intracranial hypertension complicating fulminant hepatic failure.

Intracranial hypertension complicating fulminant hepatic failure has a mortality in excess of 90% in the presence of renal failure if not rapidly responsive to mannitol and ultrafiltration. Based on data which suggest that barbiturates can be of value in controlling the intracranial hypertension of head injury, intravenous thiopental was assessed in 13 patients with fulminant hepatic failure. All had developed acute renal failure complicated by intracranial hypertension unresponsive to other modes of therapy and were likely by all published criteria to have little chance of survival. The dosage of thiopental was adjusted incrementally until intracranial pressure, measured by extradural transducers, fell to within normal limits or adverse hemodynamic changes occurred. The intracranial pressure was reduced, in each case, by 185 to 500 mg (median: 250 mg) thiopental given over 15 min, and in eight cases continuing infusion achieved stable normal intracranial pressure and cerebral perfusion pressure. Five of the patients made a complete recovery and there were only three deaths from intracranial hypertension. Side effects were few and included minor hypotension controlled by dose reduction. The response of otherwise intractable intracranial hypertension and the 38% survival rate was remarkable for a group of patients with such a poor prognosis.

Adult↗
PubMedDate not supplied

Abnormal embryogenesis induced by thiopental.

The effects of thiopental on chick embryos were analyzed in the present study. Thiopental was dissolved in saline and injected into embryonating chicken eggs at doses ranging from 0.2 to 4.0 mg per egg. The injections were made into the air sacs of eggs after two to four days of incubation. Control eggs were injected with an equivalent volume of saline (0.1 ml per egg). In all 1080 chicken eggs were used for this study. All embryos were examined on day 7. The LD50 for eggs injected on days 2, 3 and 4 was 2.1, 1.9, and 4.1 mg per egg, respectively. The principal malformations observed were exencephaly, anencephaly, twisted limbs, twisted neck, microphthalmia, everted viscera, and hemorrhage above the left eye and in both cerebral hemispheres. The results of the present study indicate that thiopental has a tendency to cause malformations in the chick embryos tested.

Abnormalities, Drug-Induced↗
PubMed2002

Acute effects of pentobarbital, thiopental and urethane on lung oedema induced by alpha-naphthythiourea (ANTU).

This study was designed to investigate the possible participation of urethane, pentobarbital sodium and thiopental sodium anaesthesia in the lung oedema induced by alpha-naphthylthiourea (ANTU), which is a well known noxious chemical agent in the lung. ANTU when injected intraperitoneally (i.p.) into rats (10 mg x kg (-1) i.p.) produced lung oedema as indicated by an increase in lung weight/body weight (LW/BW) ratio and pleural effusion (PE) reaching a maximum within 4 h. Administration of urethane prior to ANTU, at doses of 100 and 200mg(100g)(-1), elicited a significant and dose-dependent inhibition in LW/BW ratio and PE. Thiopental sodium at doses of 25, 50 mg x kg (-1), also produced a significant and dose-dependent inhibition of both parameters. Prior i.p. injection of pentobarbital sodium at a dose of 40 mg x kg (-1) elicited a significant inhibition in both parameters. These results suggest that i.p. urethane, thiopental sodium and pentobarbital sodium pretreatment have a prophylactic effect on ANTU-induced lung injury in rats. The possible role of the anaesthetics in lung oedema induced by ANTU and the possible underlying mechanisms are discussed.

Animals↗
PubMed1995

Pharmacokinetics of thiopental after single and multiple intravenous doses in critical care patients.

Thiopental was administered to neurosurgical patients for cerebral protection and its pharmacokinetic parameters were determined after a single bolus of 540, 1000 or 1500 mg (3 subjects) or after multiple doses of 250 mg (5 subjects) and 500 mg (2 subjects) every two hours for up to 7 days. The data were analysed by a two- or three-compartment model and linear kinetics. After a single iv bolus, the mean initial volume of distribution (V1) was 0.481 l.kg-1, and the steady-state volume of distribution (Vss) was 2.16 l.kg-1. The distribution (t1/2 alpha) and elimination (t1/2 beta) half-lives were 0.590 and 5.89 h, respectively, and the mean residence time (MRT) was 7.44 h. The clearance was 5.41 ml.min-1.kg-1. With repeated injections, the pharmacokinetic parameters for each patient were estimated taking into account all administered doses and blood samples, which were taken whenever possible daily at steady state and after the last dose. The variability observed in the pharmacokinetic parameters of thiopental reflected by the coefficient of variation (CV%) was wide but was of similar magnitude within patients (CVintra) as it was between patients (CVinter). The steady-state trough plasma concentration (Cmin obs) ranged from 4.8 to 30 mg.l-1 (mean 16.0 mg.l-1 and median 14.3 mg.l-1). Peak concentrations (Cmax obs) ranged from 8.35 to 45 mg.l-1 (25.4 mg.l-1, and median 23.3 mg.l-1). The values of V1 and Vss were similar to those obtained after a single dose. For V1, the mean was 0.333 l.kg-1. The mean Vss was 2.68 l.kg-1, with a CVintra of 12.6 to 56% and a CVinter of 13.2%. A shorter distribution half-life t1/2 alpha was noted on multiple dosing; the mean value was 0.122 h. The elimination half-life t1/2 beta and the mean residence time became longer due to a decrease in clearance. For t1/2 beta the mean value was 16.3 h. The mean MRT was 21.9 h, CVintra 9.19 to 48.5%, and the CVinter 35.3%. The mean clearance was 2.16 ml.min-1.kg-1, CVintra 7.28 to 25.5%, and the CVinter 20.4%. This value is 50% lower than after a single dose. Identification of the kinetic parameters of thiopental allows simulation of the effects of doses on subsequent plasma levels and will permit a priori prediction of day to day adjustment of drug dosage.

Adolescent↗
PubMed1993

Effects of thiopental on middle cerebral artery blood velocities: a transcranial Doppler study in children.

The effect of an intravenous injection of thiopental on middle cerebral artery blood velocities was assessed by transcranial pulsed Doppler monitoring in 20 children: ten head-injured patients and ten control subjects. Thiopental induced a moderate but immediate decrease of middle cerebral artery blood velocities in both groups; this variation was significant (P < 0.01) and more prolonged in the head-injured than in control patients. Transcranial Doppler ultrasonography thus appears to be suitable for monitoring children in intensive care units and could help to avoid the use of thiopental in patients with low cerebral artery blood flow velocity.

Adolescent↗
PubMed1975

The effects of increased glucose supply and thiopental anesthesia on energy metabolism of the isolated perfused rat brain.

The effects of glucose concentrations in the perfusion medium ranging from 5 to 15 mM and thiopental, on cerebral energy metabolism were studied using the isolated perfused rat brain. After a perfusion time of 30 min brain levels of the following substrates and metabolites were determined: P-creatine, ATP, ADP, AMP, glycogen, glucose, glucose-6P, fructose-6-P, pyruvate, lactate, alpha-ketoglutarate, glutamate, ammonia. In control experiments increasing the glucose concentration in the perfusion medium produced an increase of intracellular brain glucose concentration only, revealing a linear relationship between glucose content in brain and blood. Neither high-energy phosphates nor glycolytic intermediates were markedly affected by the changes in blood glucose. With an anesthetic dose of thiopental (0.15 mM) in the perfusion medium identical metabolic alterations occured in all experiments: P-creatine and glucose were significantly increased whereas ADP, AMP, lactate and pyruvate were diminished. Also with thiopental brain glucose was linearly related with the glucose concentration in the perfusion medium. The calculated regression line was apparently parallel with that from control experiments; that means thipental always caused an elevation of brain glucose by the same amount of 0.9 mumoles/g--irrespective of the initial cerebral glucose content. The results yield further evidence that glucose transport is not the rate-limiting step in glycolysis. The action of thiopetal on glycolytic pathway is discussed.

Adenine Nucleotides↗
PubMed1981

Comparison of the placental transfer of thiopental and diazepam in caesarean section.

Drug concentrations were measured in whole blood obtained from mother and child after induction of general anaesthesia with thiopental or diazepam and delivery by Caesarean section. In 27 cases given thiopental 3 mg/kg intravenously the 5-min child/mother concentration ratio rose with increasing injection-delivery (I-D) interval up to 8-10 min. The concentration in the newborn at 2 h showed a similar trend. In 30 cases given diazepam 0.3 mg/kg for sleep induction, there were some low values in cases delivered within 4 min after the injection. However, higher neonatal concentrations and child/mother ratios were observed when the operation lasted 4-5 min, and there was no further increase in cases with longer I-D intervals. There is evidence to suggest that net transfer to the fetus proceeds at a slower rate with thiopental than with diazepam. However, in the present series of low risk elective Caesarean sections, there was no appreciable difference between the induction agents with regard to their effect on the newborn infant.

Adult↗
PubMed2005

Propofol is superior to thiopental for intubation without muscle relaxants.

PURPOSE: To compare intubating conditions and cardiovascular changes following induction of anesthesia and tracheal intubation in patients receiving either lidocaine-remifentanil-propofol or lidocaine-remifentanil-thiopental prior to induction. METHODS: In a randomized, double-blind study 76 healthy adult patients were assigned to one of two groups: lidocaine 1.5 mg.kg(-1), remifentanil 2 mug.kg(-1) and propofol 2 mg.kg(-1) (Group P) or lidocaine 1.5 mg.kg(-1), remifentanil 2 mug.kg(-1) and thiopental 5 mg.kg(-1) (Group T). Ninety seconds after the administration of the hypnotic agent, laryngoscopy and tracheal intubation were attempted. Intubating conditions were assessed as excellent, good or poor on the basis of ease of ventilation, jaw relaxation, position of the vocal cords, and patient's response to intubation and slow inflation of the tracheal cuff. The mean arterial pressure (MAP) and heart rate (HR) were measured 45 sec after hypnotic agent administration, immediately after tracheal intubation, two and five minutes after intubation. RESULTS: Excellent intubating conditions were obtained in 84% of Group P patients and 50% of Group T patients (P < 0.05). The percentage decrease from baseline MAP was significantly higher in Group P than in Group T postinduction (27.4% +/- 11.6 vs 21.8% +/- 10.0) and immediately postintubation (19.0% +/- 16.7 vs 11.2% +/- 14.9). The percentage change from baseline HR was significantly higher in Group P than in Group T postinduction (13.8% +/- 9.7 vs 0.5% +/- 12.4), immediately postintubation (8.7% +/- 13.7 vs 2.1% +/- 13.1), and two minutes postintubation (7.04% +/- 14.3 vs 3.5% +/- 14.3). CONCLUSION: Lidocaine-remifentanil-propofol is superior to lidocaine-remifentanil-thiopental for tracheal intubation without muscle relaxants. However, it induces more hypotension and bradycardia.

Adolescent↗
PubMed1999

Thiopental and midazolam do not seem to impede metabolism of glutamate in brain-injured patients.

Increased extracellular glutamate levels are related to glial and neuronal damage. Glutamate-mediated toxicity is limited by glial uptake and metabolic transformation of glutamate to glutamine and the energetic compounds alanine and lactate which are utilized by surrounding neurons. Under in vitro conditions, barbiturates have been shown to reduce glutamate uptake and its further metabolism, possibly impeding metabolic coupling between astrocytes and neurons. The aims were to investigate if under clinical conditions, the barbiturate thiopental reduces important detoxification of glutamate, resulting in lower CSF glutamine, alanine and lactate levels as opposed to patients receiving midazolam. During long-term administration of thiopental and midazolam, pathologically elevated ventricular CSF glutamate levels were associated with significantly increased glutamine and alanine levels up to 14 days after trauma. CSF lactate, however, remained normal. These data suggest that long-term administration of thiopental and midazolam under clinical conditions does not impede enzymatic activities responsible for detoxification and metabolism of glutamate.

Adolescent↗
PubMed2000

Attenuation of brain high frequency electrocortical response after thiopental in early stages of Alzheimer's dementia.

RATIONALE: Pathological brain regions generate proportionately less high-frequency (beta) activity than non-pathological regions, a phenomenon accentuated by barbiturate administration. OBJECTIVES: Previously, we reported a loss of high-frequency brain electrical response to thiopental in dementia of the Alzheimer's type (DAT). The current study examines whether this phenomenon may be detected in early stages of the illness. METHODS: Using quantitative electroencephalography, we examined power in the 20-28 Hz band in patients with early DAT (n=7, age 71.0+/-3.2 years, Folstein Mini Mental State Score, MMSE 26.2+/-0.8), normal controls (n=8, age 74.3+/-3.2 years, MMSE 29.0+/-0.3) and subjects with moderately severe DAT (n=6, age 76.6+/-3.0 years, MMSE=12.5+/-3.7) at baseline and following an intravenous bolus of thiopental (0.5 mg/kg). RESULTS: No significant group differences in beta power were detectable at baseline. In response to thiopental, early DAT subjects compared to controls showed a significantly smaller beta power response in the frontal region at 1-3 min postinjection. Losses were smaller than those of subjects with moderately severe DAT and demonstrated a non-linear correlation with decreases in cognitive function as assessed by the MMSE score (r2=0.75). CONCLUSION: In early stages of DAT, a barbiturate challenge may unmask abnormalities in brain electrical activity not seen at baseline. Such changes may reflect underlying cortical deafferentation.

Aged↗
PubMed1995

Effects of thiopental, halothane and isoflurane on the calcium-dependent and -independent release of GABA from striatal synaptosomes in the rat.

The effects of the anesthetic agents thiopental, halothane and isoflurane on the release of GABA induced by depolarization and/or reversal of the GABA carrier were investigated in a synaptosomal preparation obtained from the rat striatum. Veratridine (1 microM) and KCl (9 mM) elicited a significant, Ca(2+)-dependent release of [3H]GABA. The KCl-evoked release was not significantly modified in the presence of nipecotic acid (10(-5) M), a selective blocker of the neuronal GABA carrier. The [3H]GABA release was significantly decreased by omega-conotoxin (10(-7) M, a blocker of the N voltage-dependent Ca2+ channels, but was affected by neither nifedipine (10(-4) M) nor omega-Aga-IVA (10(-7) M which block the L and P Ca2+ channels, respectively. Thiopental application (10(-5) to 10(-3) M) was followed by a dose-related, significant, decrease in both the veratridine and KCl-induced releases, whether nipecotic acid was present or not. In contrast, halothane and isoflurane (1-3%) failed to alter [3H]GABA release. Altogether, these results suggest that reduction of the depolarization-evoked GABA release might contribute to thiopental anesthesia, but this seems unlikely for volatile anesthetics.

Anesthetics↗
PubMed1986

Visual versus computer evaluation of thiopental-induced EEG changes in temporal lobe epilepsy.

Thiopental-induced EEG beta activity was analyzed both visually and by computer in 33 patients with complex partial epilepsy. Studies were done in 16 patients with depth electrodes in limbic structures and 17 patients with scalp and sphenoidal electrodes. The percentage of drug-induced change in beta activity was quantified by computer using spectral analysis. The statistical significance of asymmetries between homologous sites in the amount of change was determined. The spatial distribution of significant asymmetries was used for localization and compared with the results of independent visual analysis of the thiopental EEG. Concordance between computer and visual evaluation occurred in 10 of 17 scalp/sphenoidal and 10 of 16 depth electrode tests. The accuracy of visual and computer localization was determined by comparing them with locus of itcal EEG onset, interictal spikes, and positron emission tomography. In scalp/sphenoidal studies, computer analysis indicating asymmetry appeared more likely to correlate with independent clinical criteria than visual analysis. In depth studies the reverse appeared to be true. Scalp/sphenoidal tests yielded positive results in 25-30% of patients whereas depth electrode tests were positive in 50-70% of patients. The results indicate that computer analysis of surface thiopental tests is an accurate and useful supplement to visual evaluation of these tests.

Brain↗
PubMed1984

Amino acid neurotransmitters in the CNS: effect of thiopental.

Thiopental, a thiobarbiturate which partitions prefentially into the hydrophobic environment, inhibited transport of amino acid neurotransmitters, GABA, aspartate and glutamate, and of biogenic amine, dopamine, across the synaptosomal membrane. At a given protein and thiopental concentration GABA transport was more sensitive to the barbiturate than were the movements of aspartate and glutamate although the uptake of each amino acid was inhibited essentially to the same extent as was its K+-stimulated release. By contrast, inhibition of dopamine uptake was larger than that of its release. Thiopental also inhibited the release of amino acid neurotransmitters caused by anaerobiosis. It is suggested that the barbiturate modifies the properties of the synaptosomal lipids and/or hydrophobic segments of proteins and thereby, simultaneously and independently, affects various membrane functions. The equal inhibition of uptake and release of amino acid neurotransmitters is consistent with the postulate that their transport occurs through the reversible membrane carriers which function efficiently in both the inward and outward directions.

Amino Acids↗
PubMed1991

Determination of thiopental in human serum and plasma by high-performance capillary electrophoresis-micellar electrokinetic chromatography.

The quantitation of thiopental in human serum and plasma was investigated using high-performance capillary electrophoresis (HPCE) in a micellar configuration and the results were compared with reversed-phase high-performance liquid chromatography (HPLC). Thiopental and an internal standard (carbamazepine for HPCE and thiamylal for HPLC) were extracted from serum or plasma using pentane and a phosphate buffer (pH 6.4). HPCE analysis took place in a phosphate-borate buffer with 50 mM sodium dodecyl sulphate using an automated instrument and HPLC was performed with a C8 column and a mobile phase of phosphate buffer-acetonitrile (65:35, v/v). HPCE and HPLC data from 66 patient samples compared well based on linear regression analysis. However, estimates obtained with the inclusion of the internal standard were lower than those based on the sample peak only. This example allows the elucidation of the advantages of using HPCE as an assay methodology for the therapeutic monitoring of thiopental and other drugs.

Chromatography↗
PubMed1985

Interference of pentobarbital and thiopental with the vascular contraction and noradrenaline release in human cerebral arteries.

Thiopental and pentobarbital induced dose-dependent vasodilations in human cerebral arteries previously contracted with noradrenaline (NA), serotonin (5-HT) and KCl. Preincubation with both barbiturates decreased the contractions evoked by the three agents. Pentobarbital and thiopental reduced the Ca2+-induced contractile effects in K+-depolarized arteries and 5-HT-Ca2+ and NA-Ca2+ contractions dose-dependently. The tritium release evoked by K+ from these vessels prelabelled with [3H]NA was significantly reduced by both barbiturates at 10(-3) M and by Ca2+ removal. These results indicate that pentobarbital and thiopental essentially produce a similar interference with Ca2+ influx inhibiting the contractile responses induced by the three vasoactive agents and the exocytotic NA release evoked by K+.

Cerebral Arteries↗
PubMed1986

Effect of thiopental sodium and barbitone sodium on the total acetylcholine content and acetylcholinesterase activity in the brain tissue of Arvicanthis niloticus.

The total ACh content and AChE activity were determined 1 hr after the i.p. injection of different doses of thiopental sodium (5, 10 and 20 mg/ml/100 g body wt) and barbitone sodium (20, 40 and 80 mg/ml/100 g body wt). The effect of different time intervals (1 min, 10 min, 30 min, 1 hr, 2.5 hr, 5 hr, 8 hr, 12 hr, 24 hr and 48 hr) on the total ACh content and AChE activity was investigated after i.p. injection of 10 mg thiopental sodium and 40 mg barbitone sodium/ml/100 g body wt. Both thiopental sodium and barbitone sodium increased the total ACh content in the brain tissue of Arvicanthis niloticus. Both drugs inhibited the brain AChE activity. It is thought that the increase in the total ACh content in the brain tissue of Arvicanthis niloticus may be due to a decrease in the release of ACh from the neuronal tissue and a decrease in AChE activity.

Acetylcholine↗