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PubMed1998

Pharmacodynamics and pharmacokinetics of thiopental.

Thiopental is an ultra short-acting barbiturate which remains the standard against which other induction agents are judged; it is also indicated for the therapy of brain hypoxic-ischaemia injuries and status epilepticus. Aspects of drug distribution that govern the onset and end of drug effect have been intensively studied to determine which parameters (in patient characteristics, diseases and administration modalities) influence effective dose and concentrations in individual patients. Thiopental has been used as a reference for pharmacokinetic and/or pharmacodynamic models in the study of rapid and short acting effect drugs. In anaesthesiology the pharmacokinetics of thiopental are described as linear; when doses and duration of treatment increase, nonlinear pharmacokinetics occur because of the saturation and/or the induction of the metabolism.

Adult↗
PubMed1979

Effect of althesin anesthesia on blood loss during therapeutic abortion. A comparison with local and thiopental anesthesia.

During recent years, the use of steroid anesthesia has rapidly increased. In our hospital, a number of surgical procedures have been performed under Althesin anesthesia, and in some cases the peroperative bleeding seemed to be rather profuse. Blood loss was studied in 90 healthy women in the first trimester of pregnancy undergoing therapeutic abortion using different types of anesthesia. The patients were divided into three equal groups according to the duration of pregnancy. In each group, 10 patients underwent operation under local anesthesia, 10 under thiopental anesthesia and 10 under Althesin. In all three groups, blood loss was the smallest when local anesthesia was used (Fig 1). Amounting to only one third to one half of that occurring under thiopental anesthesia. Under thiopental anesthesia the blood loss gradually increased with increasing gestational age with moderate variations. Alternatively, in this investigation, Althesin anesthesia was characterized by pronounced blood loss, particularly in the ninth and tenth weeks of pregnancy, and in some cases by rather profuse bleeding. We find that Althesin anesthesia should be used for gynecological surgery only in departments which are equipped to control profuse bleeding and possible cardiovascular complications.

Abortion, Therapeutic↗
PubMed1989

Effects of intravenous diazepam and thiopental on the vestibulo-ocular reflex in man.

The effects of i.v. injection of diazepam 0.3 mg/kg and thiopental 6.0 mg/kg on vestibulo-ocular reflex (VOR) were studied in 9 healthy volunteers. One hour after injection of both diazepam and thiopental VOR gain was reduced and time constant shortened. Four hours after intravenous injection of diazepam the VOR gain was still significantly reduced and had not yet returned to control 8 h after injection. Although both drugs were detected in blood still 8 h after the injection, there were no longer significant effects on VOR. Moreover, individual values of VOR gain and time constant did not correlate with the blood concentrations of the drugs. Decrease of VOR gain and shortening of time constant after i.v. given diazepam and thiopental in man are interpreted as resulting from both specific effects on VOR and non-specific reduction of alertness.

Adult↗
PubMed1985

Comparative adipose tissue kinetics of thiopental, DDE and 2,4,5,2',4',5'-hexachlorobiphenyl in the rat.

A comparative study on the fate of thiopental, DDE, and 2,4,5,2',4',5'-hexachlorobiphenyl (6-CB) with emphasis on adipose tissue kinetics was carried out after single i.v. doses to adult male rats. The time course of the concn. in blood, adipose and other tissues were determined for the three compounds for periods up to 40 h, 14 and 28 d, respectively, allowing for mass balances and for calculation of pharmacokinetic parameters. Appreciable amounts of thiopental, DDE and 6-CB appeared in adipose tissues, but the kinetics were profoundly different, the adipose tissue concn. peaking after one hour, 17 h, and five to six weeks, respectively. Thus, although DDE and 6-CB are much more lipophilic than thiopental, they were very much slower in entering adipose tissue. The results indicate that adipose tissue storage of drugs and other xenobiotics cannot be explained as a simple partition phenomenon. Rather, disposition in adipose tissue may be determined by initial binding in other tissues.

Adipose Tissue↗
PubMedDate not supplied

A comparison of thiopental, propofol, and diazepam-ketamine anesthesia for evaluation of laryngeal function in dogs premedicated with butorphanol-glycopyrrolate.

Thiopental, propofol, and diazepam-ketamine were compared for evaluation of laryngeal function in dogs. There was no significant difference among the three protocols in time to observation of normal function after drug administration or in the occurrence of swallowing, laryngospasm, or breathing. Jaw tone was significantly greater with diazepam-ketamine. Exposure of the larynx was excellent in five dogs and moderate in three dogs, each receiving thiopental or propofol. Exposure was excellent in one dog, moderate in six dogs, and poor in one dog receiving diazepam-ketamine. Exposure of the larynx for laryngeal function evaluation is more readily accomplished with thiopental or propofol than with diazepam-ketamine.

Anesthesia↗
PubMedDate not supplied

[Effect of etomidate and thiopental on the onset of rocuronium action].

HYPOTHESIS: Differences in the hemodynamic effects of induction agents may cause them to affect the onset of action of rocuronium differently. OBJECTIVES: To compare the onset of action of rocuronium after induction with etomidate and thiopental. PATIENTS AND METHODS: Forty adult ASA I patients received 3 micrograms.kg-1. Three minutes later anesthesia was induced randomly with either 5 mg.kg-1 of thiopental (group I, n = 20) or 0.3 mg.kg-1 of etomidate (group II, n = 20). Rocuronium 0.6 mg.kg-1 was administered over 5 s. Baseline blood pressure and heart rate were measured just before delivery of rocuronium and just before intubation. Onset of action was defined as the time from injection of rocuronium until achievement of a blockade > or = 95% of the first electromyographic response in a trian-of-four stimulus of the short adductor of the thumb. We also studied intubation conditions. RESULTS: Etomidate was associated with a smaller decrease in systolic arterial pressure than was thiopental. Onset of action was 81 +/- 29 s in group I versus 72 +/- 23 s in group II (NS). Similar intubation conditions were observed in both groups. CONCLUSIONS: These results suggest that the induction drug does not affect rocuronium's onset of action.

Adult↗
PubMed2000

Effects of induction anesthetic agents on outcome of assisted reproductive technology: a comparison of propofol and thiopental sodium.

BACKGROUND: The use of propofol, as compared to barbiturates (e.g. thiopental), for short surgical procedures has been associated with more rapid recovery from the procedure. Propofol, an intravenous anesthetic drug, is frequently used as an adjunct to transvaginal oocyte retrieval but little is known about its effects upon fertilization, embryo development, and pregnancy rate when used drug the for induction of general anesthesia. This study was conducted to compare the outcome of assisted reproductive technology (ART) with the use of propofol versus thiopental sodium for the induction of general anesthesia during oocyte retrieval. METHODS: In this retrospective study, 92 cases of infertile patients who underwent oocyte retrieval under the induction of general anesthesia with, respectively, either propofol (Group I, 72 cases) or thiopental sodium (Group II, 20 cases) were compared for fertilization rate, cleavage rate, and pregnancy rate. RESULTS: The fertilization rate was 68.9% for Group I and 66.7% for group II (p = 0.614). The cleavage rate was 96.5% for Group I and 94.8% for Group II (p = 0.294). The rate of good embryo grading and poor embryo grading was, respectively, 85.1% and 14.9% for Group I, versus 85.7% and 14.3% for Group II (p = 0.887). The pregnancy rate was 30.5% for Group I and 20.0% for Group II (p = 0.354). The implantation rate and abortion rate was, respectively, 9.1% and 18.2% for Group I versus 7.2% and 25.0% for Group II (implantation rate, p = 0.590; abortion rate, p = 0.600). CONCLUSION: There were no significant differences between these two groups for fertilization rate, cleavage rate, pregnancy rate, implantation rate and abortion rate. We suggest cautious use of propofol for the procedure of oocyte retrieval despite its associated more rapid post-operative recovery including less nausea/vomiting.

Anesthetics, Intravenous↗
PubMed1975

[Fluorohistochmical studies on localization of 5-hydroxytryptamine neurons in the rat brain following administration of thiopental sodium].

The localization of 5-hydroxytryptamine (5-HT) neurons in the rat brain was studied by the fluorescence histochemical method of Falck and Hillarp. A model experiment and tissue experiment were used to measure the characteristics of wave length of 5-HT fluorophor and we decided 420 mmu for excitation maxima and 520 mmu for emission maxima. The 5-HT neurons both in frontal and sagittal sections of the brain from reserpine-nialamide-treated rats were observed fluorohistochemically. The brain was divided into 5 portions; medulla oblonga, pons, midbrain, diencephalon and telencephalon. In frontal sections, from B1 to B8 cell groups were localized in raphe nuclei, in the region of 200 mu width on both sides from the central plane, excluding most of B2 cells and cells of B9 group which were situated on both side apart from the central plane. Microphotographs taken from about 34 areas of a sagittal section were composed to determine the interrelationship between B cell groups of 5-HT neurons. The frontal sections untreated with reserpine-nialamide showed a faint fluorescence of 5-HT neurons, however, after the administration of thiopental sodium 80 mg/kg i.p. the fluorescence of 5-HT neurons was increased in intensity and the observable cells were increased in number, especially in the B7 cell group. The yellow fluorescence of 5-HT nerve terminals in nuc suprachiasmaticus in the sagittal section was increased in intensity and varicosities of the terminals were readily observed. These results verified the increase of 5-HT in 5-HT neurons after the administration of thiopental and suggest that the 5-HT neuron may play a role in the mechanism of the central action of a thiopental.

Animals↗
PubMed2003

Comparison of the effects of propofol versus thiopental induction on postoperative outcomes following surgical procedures longer than 2 hours.

The use of propofol as an induction agent for surgeries lasting less than 2 hours has been shown to result in a faster emergence from anesthesia. Our study was performed to analyze the impact of propofol on surgical procedures lasting longer than 2 hours. A convenience sample of 84 men and women undergoing nonemergency laparoscopic procedures scheduled for longer than 2 hours were enrolled in this prospective study and randomly assigned to receive a standardized induction with thiopental or propofol. Nausea and pain were measured using a 0 to 10 verbal numeric rating scale. Recovery from anesthesia was measured using a modified Newman Bender Motor Gestalt Test. Statistical analysis was used to analyze all ordinal and interval data. A P value of less than, 05 was considered significant. No differences were found between the propofol and thiopental groups in demographics, total surgical time, anesthesia time, recovery times, postoperative analgesic and emetic requirements, satisfaction scores, or incidence of nausea and vomiting. Discharge times from the postanesthesia care unit and to home were similar between groups. Based on the results, we concluded that propofol offered no advantages over thiopental in postoperative outcomes in laparoscopic surgical procedures longer than 2 hours.

Adult↗
PubMed1977

Pulmonary metastases, a potential biologic consequence of anesthetic-induced immunosuppression by thiopental.

This set of experiments was devised to determine the effects of the commonly employed anesthetic induction agent, thiopental, on the incidence of pulmonary metastases in a murine fibrosarcoma system. A correlation was made with cell-mediated immune responses in vivo and in vitro. In two separate experiments, thiopental-treated mice had a significantly increased incidence of pulmonary metastases. This was correlated with an impaired delayed hypersensitivity reaction to the de novo antigen. 2,4-dinitrochlorobenzene (DNCB) and a suppressed mixed leukocyte culture (MLC) reaction. However, if animals were sensitized with DNCB 5 days prior to receiving pentothal, no impairment of DNCB reactivity was noted. This suggests strongly that the observed defect is in the afferent arm of the immune response. Thiopental suppresses cell-mediated immune responses in this system, and the observed biologic consequence is an increase in pulmonary metastases.

Anesthetics↗
PubMed1992

A comparative study of propofol and thiopental as induction agents for elective caesarean section.

Twenty women for elective caesarean section received either propofol 2.3 mg/kgr or thiopental 4.4 mg/kgr for induction of general anaesthesia. Maintainance was similar for both groups. Mean arterial pressure and heart rate were recorded non-invasively before anaesthesia, during intubation, one and five minutes after intubation. There were no significant differences in haemodynamic response between the two groups. During intubation heart rate rose in both groups, but remained increased five minutes after tracheal intubation only in the thiopental treated women (p less than 0.05). There was no significant neonatal depression as assessed by Apgar Scores and blood gas analyses. Propofol appears to be a suitable alternative to thiopental as an induction agent for obstetric anaesthesia.

Anesthesia, General↗
PubMedDate not supplied

[Comparison of the effects of midazolam and thiopental on the neuromuscular response of vecuronium, atracurium, and pancuronium].

To assess the possible interactions of midazolam and thiopental with the muscular relaxants vecuronium (0.08 mg/kg), atracurium (0.5 mg/kg), and pancuronium (0.1 mg/kg), a comparative analysis was undertaken in two groups of 18 and 32 patients treated respectively with midazolam (0.3 mg/kg) and thiopental (5 mg/kg). The beginning of the effect, maximal blockade, duration of the clinical response, and the spontaneous recovery index were measured on electromyographic recordings of action potentials evoked by train of four supramaximal stimuli delivered every 20 sec on the ulnar nerve. Conditions for intubation were assessed 2 minutes after administration of muscular relaxant. There were no significant differences in neuromuscular parameters in either of the two groups of patients treated with midazolam or with thiopental independently of the relaxant drug administered.

Adult↗
PubMed2006

Intravenous propofol precipitates the hypotension induced by inadvertent epidural thiopental injection.

Administration of improper drugs into epidural space is occasionally present in anesthetic practice. In most instances it would not contribute to significant neurological complications. There had not been severe hypotension reported in the literature in consequence of inadvertent epidural thiopental administration. Here we describe our experience in a case of inadvertent epidural administration of thiopental coinciding with induction of anesthesia with propofol, as a consequence of which profound hypotension was induced, necessitating aggressive inotropic and vasopressive agents to maintain blood pressure. Rapid vascular uptake of thiopental in the epidural space and synergistic action of propofol jointly contributed to the development of the hypotension. Attempts to forestall neurological sequela after the inadvertence seem unnecessary unless apparent symptoms or signs of neurological injury have come upon.

Aged↗
PubMedDate not supplied

[Effects of thiopental and propofol on suppressor T lymphocyte activity and noradrenaline release].

The effects of thiopental and propofol on lymphocyte suppressor T activity were studied in the basal state and after 20 min, 24 hours, and 4 days of anesthesia induction in 20 patients undergoing gynaecologic surgery. Both drugs induced a decrease in lymphocyte suppressive T activity which recovered after 4 days and tended to be larger, although not significantly, with thiopental. Serum noradrenaline concentration significantly increased after two hours of propofol anesthesia and after 20 min and 2 hours of thiopental administration. These results demonstrate that the relationship between lymphocyte suppressive T activity and noradrenaline corresponds theoretically to anesthesia deepness.

Female↗
PubMedDate not supplied

[Comparison of anesthesia with thiopental or etomidate in short duration operations].

Forty ASA I-II women who were scheduled for uterine curettage were randomly allotted to two groups of 20 patients each. Both groups were age- and weight- matched. They were pre-treated with atropine (0.01 mg/kg) and diazepam (0.1 mg/kg). Anesthesia was induced with 2.5% thiopental (5 mg/kg) or 0.1% etomidate (0.3 mg/kg) and was maintained with N2/O2 at 50% and isoflurane at 1% adding supplementation doses of inducer (20% of initial dose) when required. Quality of induction and maintenance of anesthesia, cardiovascular effects, secondary effects and quality and rapidity of awakening were evaluated. Etomidate patients presented a higher number of secondary effects and pain on injection of the drug (p less than 0.05) and occurrence of excitatory motions (p less than 0.01) attained statistical significance. Evaluation of anesthesia quality was significantly higher with thiopental (p less than 0.05). There were no differences with respect to the remaining studied variables. We conclude that etomidate when used as unique agent in anesthesia induction has no advantages over thiopental in healthy patients undergoing short duration operations.

Adult↗
PubMed1990

[Recovery, amnesia and affective state following propofol in comparison with thiopental].

Numerous reports have described a definite sense of well-being after anesthesia with propofol (Disoprivan). The present study was designed to assess postoperative mood as recorded with a quantitative self-rating method. Postoperative recovery and amnesia were also investigated. Thirty unpremedicated female patients aged 20-60 (ASA grade 1 or 2) who were scheduled for minor gynecological operations were enrolled in the study after informed consent. The patients were randomly allocated to three study groups: group A, induction with propofol 2 mg/kg and maintenance with propofol 0.15 mg/kg per min together with N2O/O2; group B, induction with propofol 2 mg/kg and maintenance with enfluran and N2O/O2; group C, induction with thiopental until loss of the eye lash reflex and maintenance with enfluran and N2O/O2. Postoperative amnesia was assessed by showing five picture cards at 5-min intervals, starting when the patients were able to state the correct date of birth. A test of recovery (p-deletion) was carried out after 30 and again after 60 min. The postoperative mood state was evaluated with the adjective checklist of Janke and Debus 5 h after waking. In good agreement with published reports, propofol patients recovered more rapidly than thiopental patients. A significant but irrelevant amnesia occurred after 5 min in group B. However, in some cases amnesia lasting up to 20 min was observed. The global mood status showed a significantly higher score for positive items and a lower score for negative items after propofol administered by either technique than after thiopental (P = 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1985

Reversal of thiopental-induced anesthesia by 4-aminopyridine, yohimbine, and doxapram in dogs pretreated with xylazine or acepromazine.

Groups of atropinized dogs (6 dogs/group) were sedated, using xylazine HCl (2.2 mg/kg of body weight, IM) or acepromazine maleate (0.25 mg/kg, IM), and were anesthetized to loss of pedal reflexes, using thiopental, IV. The dogs were given 1 of the following test antagonists, IV: saline solution (2 ml; control group), 4-aminopyridine (4-AP; 0.5 mg/kg), yohimbine (0.4 mg/kg), doxapram (5.0 mg/kg), or dual combinations of the latter 3 substances in the same doses as used for each agent. In xylazine-treated dogs, the mean dosage of thiopental required to induce anesthesia was 4.8 mg/kg. Control mean arousal time (MAT) and walk time (MWT) were 37.1 minutes and 53.8 minutes, respectively. These values were decreased to less than 2 minutes and less than 3 minutes, respectively, by yohimbine, 4-AP + yohimbine, and doxapram + yohimbine. With doxapram and with 4-AP + doxapram, MAT was less than 2 minutes and MWT was less than 8 minutes. In acepromazine-treated dogs, the mean dosage of thiopental required for anesthesia was 15.0 mg/kg. Control MAT and MWT were 20.7 minutes and 36.5 minutes, respectively. These values were decreased to 8.1 minutes and 18.1 minutes, respectively, by doxapram, and to 3.5 minutes and 19.9 minutes, respectively, by doxapram + yohimbine. Doxapram, 4-AP + doxapram, and doxapram + yohimbine caused periodic extensor rigidity before and during arousal. This rigidity was accompanied by opisthotonos in 2 dogs of the doxapram + yohimbine group and may have been mild tonic seizures.(ABSTRACT TRUNCATED AT 250 WORDS)

4-Aminopyridine↗
PubMed1989

A randomized comparison between midazolam and thiopental for elective cesarean section anesthesia: II. Neonates.

In a randomized blind trial, the general condition of 40 neonates was assessed following midazolam- or thiopental-based general anesthesia for elective cesarean section. Among 19 neonatal neurobehavioral observations and tests, statistically significant differences between the midazolam and the thiopental groups were rare. However, a statistically significant interaction with regard to body temperature, general body tone, and arm recoil was observed where results were inferior for midazolam, although only within the first 2 hours. It was concluded that midazolam is as safe as thiopental for the induction and maintenance of elective cesarean section anesthesia in neonates.

Anesthesia, Obstetrical↗