Measurements of brain amobarbital concentrations in rats anesthetized and overdosed by amobarbital and treated centrally with dibutyryl cyclic AMP.
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Salivary excretion of amobarbital in man.
The concentrations of amobarbital in saliva and serum were determined in 5 normal adults following ingestion of 120 mg of sodium amobarbital. There was excellent linear relationship between amobarbital concentrations in saliva and serum (r = 0.993); salivary levels were 36.1% of serum levels. Since the pH of saliva was generally lower than that of blood in man, the degree of ionization of amobarbital in serum and saliva had to be taken into consideration. Estimation of the protein binding of amobarbital in serum from concentrations of amobarbital in saliva and serum was in good agreement with the in vitro data of equilibrium dialysis.
Adult↗
Multiple effects of amobarbital on Ehrlich ascites tumor cells. Inhibition of pyruvate dehydrogenase.
The inhibition of the proliferation of hyperdiploid Ehrlich ascites tumor cells in suspension cultures by amobarbital is coupled to an increased glycolytic activity as shown by lactic acid production and glucose consumption; higher concentrations of amobarbital than 1 mM enhance the ATP/ADP ratio of the total cell. The actual activity of pyruvate dehydrogenase of intact cells is completely inhibited in the presence of 2 mM amobarbital as was shown by the 14CO2 evolution from [114C]pyruvate or the incorporation of 14CO2 into the total lipid fraction of the cells from [U-14C]lactate. The pyruvate dehydrogenase complex from Ehrlich ascites tumor cells is completely inhibited by 1 mM amobarbital in vitro. The activity of alpha-oxoglutarate dehydrogenase is inhibited by amobarbital, too, as well as shown by measuring the 14CO2 evolution from [1-14C]glutamate with intact cells. It is suggested that the inhibition of pyruvate dehydrogenase in the presence of amobarbital is the result of a direct action on the enzyme as well as the consequence of a change in the cellular redox state or its energy charge.
Adenosine Diphosphate↗
Enzyme induction following a single dose of amobarbital in dogs.
The elimination of amobarbital in dogs was investigated by injecting various doses of amobarbital into a given animal. At low doses (3 mg/kg) serum levels declined in a first-order fashion. Superficially, at high doses (20 mg/kg) the relationship between serum concentration and time could be quantitatively characterized by simple one-compartment saturable kinetics. Indeed, qualitatively, saturation of the amobarbital-metabolizing enzymes was indicated by a shallower initial slope of the semilogarithmic concentration--time profile at the high than at the low dose. However, in addition, an acute enzyme induction phenomenon was observed which was indicated by a shorter terminal half-life of amobarbital at the high dose than after the low dose and also by a shortening in antipyrine half-life.
Amobarbital↗
The amobarbital interview.
In two apparently disoriented patients, the emergency physician's use of amobarbital quickly eliminated diagnoses of an organic etiology. Although thousands of amobarbital interviews have had no complications, the use of amobarbital should follow a thorough evaluation. The amobarbital interview is a safe and simple technique to discriminate functional from organic illness, thus avoiding unnecessary medical and surgical treatment, neglected illness, and inappropriate disposition.
Adult↗
Effect of human growth hormone on amobarbital metabolism in children.
Drug metabolism changes during the course of growth and development. Hormones mediate somatic growth and may mediate other developmental changes. To determine the effect of human growth hormone (hGH) on human drug metabolism, 6 hGH-deficient children were given single oral doses of amobarbital before and 6 wk after beginning hGH replacement therapy. Amobarbital was selected as a marker of hepatic microsomal oxidation. Half-lives rose from 13.89 +/- 2.78 hr to 22.75 +/- 3.97 hr, volume of distribution was unchanged, and clearance fell from 62.2 +/- 15.2 ml/kg/hr to 31.2 +/- 11.4 ml/kg/hr. Results indicate that hGH slows the metabolism of amobarbital, probably through an effect on the hepatic microsomal drug-oxidizing system.
Adolescent↗
Distinctive patterns of amobarbital metabolites.
This paper establishes that the relative proportion of amobarbital metabolites in urine is highly variable from person to person and that observations of plasma half-life give no indication of this variability, but it shows that a valid estimate of a given person's metabolite pattern can be obtained by studying a single urine specimen in the postdistributive phase. The two metabolites which were measured in urine accounted on the average of 9 subjects for 80% +/- 3% of the dose with a range from 66% to 94%. The two metabolites were the well known 3'-hydroxyamobarbital (COH) as a product of side chain hydroxylation and N-beta-D-glucopyranosyl amobarbital (N-glu), a glucose conjugate which at some earlier time had been mistaken for an N-hydroxylation product. Among 129 volunteer subjects, the metabolite ratio N-glu/COH showed a median value of about 0.5 with a range from 0 to 2.8. A virtual absence of N-glu was observed in one of the 129 subjects and confirmed by a second administration of amobarbital 3 mo later. Of the 14 subjects with predominant N-glu excretion 4 were of Chinese origin, while there were 6 Chinese among the 115 other subjects (p less than 0.02).
Amobarbital↗
A method for studying drug metabolism in populations: racial differences in amobarbital metabolism.
The two main metabolites of amobarbital excreted in urine are 3'-hydroxyamobarbital (C-OH) and 1-(beta-D-glucopyranosyl) amobarbital (N-glu). When testing the metabolite ratio in small single samples of urine, it was found that the urine in a Caucasian population contained about one-third glucose conjugation and two-thirds hydroxylation product, while an Oriental population excreted both metabolites in equal proportion. Attempts to learn the causes for the different metabolite ratios led to an investigation of metabolite concentrations in urine. The sums of the average urinary concentration of C-OH was greater in Caucasians than in Orientals, no matter how the data were expressed; the reverse was true for the N-glu metabolite. C-OH data was scattered more widely among Orientals than Caucasians; this might indicate bimodality of the distribution curves. There also was a trend toward more N-glu metabolite in urine of females than of males. Measuring the metabolite/creatinine ratios narrowed the distribution range of the data, particularly after correction for sex difference in creatinine, but population differences were not changed. Expected relationships between metabolite content of urine, sampling times, and plasma half-life (t1/2) were established by calculation. A Caucasian female with no capacity for N-glucosidation was found during the first part of this population survey. An Oriental male with only trace capacity for amobarbital hydroxylation was found in the second part.
Amobarbital↗
The effect of diazepam, chlorpromazine and amobarbital on the contingent negative variation.
The effects of diazepam (5 mg), chlorpromazine (CPZ, 12.5 mg) and amobarbital (100 mg) on the contingent negative variation (CNV) at Cz and Oz were studied in groups of 10 subjects each. Amobarbital and placebo were given by the double-blind crossover method. Two kinds of experimental paradigms were used: Click (warning stimulus, S1)--flashes (imperative stimulus, S2)--and click--electrical stimulation--motor response. The results obtained were as follows; 1) CNV amplitudes were decreased significantly by administration of diazepam only at Cz when S2 was flashes and at both Cz and Oz when S2 was electrical stimulation. 2) CPZ-induced effects were of either augmentation or decrement in CNV amplitudes depending on the subject and on the modality of S2. Involvement of dose-dependent factor was suggested. 3) Amobarbital and placebo did not give any significant changes to the CNV. 4) Significant correlations between CNV amplitudes at Cz and Oz were found before drug administration and even after taking drugs exclusive of diazepam. Its decremental ratio from Cz to Oz was approximately 0.6 to 0.8. The correlation coefficient became to be insignificant after taking diazepam only when S2 was flashes.
Adult↗
Amobarbital treatment of multiple personality. Use of structured video tape interviews as a basis for intensive psychotherapy.
The case of a 30-year-old woman with five distinct personalities is presented. The patient was treated, using a system of structured video taped sodium amobarbital interviews, in which areas to be explored were developed in psychotherapy. Tapes were played for the patient after each session. The taped material was used as the basis for psychotherapeutic investigation. The patient evidenced many of the features previously reported in cases of multiple personality, specifically: being the product of an unwanted pregnancy in a repressively rigid family; emotional distancing by one parent; strong sibling rivalry with an adopted sib; family history of mental illness; a traumatic first sexual experience (rape); a marriage to a maladjusted individual in an attempt to escape the parental home; a high internalized standard of performance and an inability to display anger or negative feelings toward the parents. In the course of treatment, the patient's personalties fused and she was able to accept each component as part of herself. No further fragmentation has occurred during the year following discharge. The therapy technique minimized dependency, and the possiblity of addiction to amobarbital interviews permitted more active patient therapy involvement, and set clear-cut goals and expectations for improvement before further amobarbital interviews could be conducted.
Adult↗
Clinical usefulness of sodium amobarbital interviewing.
We report a double-blind, randomized, placebo-controlled study utilizing a within-subjects design on 20 hospitalized, psychiatric patients who participated in sodium amobarbital interviews to determine if the drug has a specific effect in eliciting clinically useful information. The patients selected had difficulty communicating with their primary therapists during the postadmission, diagnostic interviews. Two raters completed a Hamilton Depression Scale, a New Haven Schizophrenia Index, and a Brief Psychiatric Rating Scale after each interview. Although both the amobarbital and saline interviews were moderately useful in obtaining new information, we found no significant difference in the primary therapists' assessments of clinical usefulness. In addition, the drug interview did not uncover material that would aid in the differential diagnosis between depression and schizophrenia. There was, however, a significant negative correlation between the assessment of general usefulness and the time interval between admission and interviewing. We report our only exception, a case of catatonic schizophrenia, in which the patient responded specifically to the drug.
Adult↗
UV spectrophotometric determination of aminophylline, amobarbital, and ephedrine hydrochloride in an antiasthma capsule preparation.
A simple and rapid procedure for the determination of aminophylline, amobarbital, and ephedrine hydrochloride in a capsule preparation is described. Aminophylline and amobarbital are determined simultaneously using differential UV spectrophotometry; ephedrine hydrochloride is determined separately after elution from an alginic acid column with 0.1 N hydrochloric acid.
Aminophylline↗
Influence of the suspension of continued treatment with flurazepam and amobarbital on two discrimination learning schedules.
The authors have studied the effect of the suspension of chronic treatment with flurazepam and amobarbital on the operant behavior of rats that for the first time were in the presence of two fixed-interval discrimination schedules. With the sound discrimination schedule, the responses emitted by the treated animals had charactistics similar to those of control animals. With the temporal discrimination schedule, though it is not possible to distinguish between learning rates, modifications in the intensity of the effect (increases in lever pressing) indicate that, considering the doses, the action of flurazepam is slight and that of amobarbital clear and statistically significant.
Acoustic Stimulation↗
Age-dependent disposition of amobarbital: analog computer evaluation.
Previously published observations on 4-hour and 24-hour amobarbital blood levels in two groups of subjects (ages 20--40 and over-65) were analyzed with use of an analog computer and literature data for the rate constants of absorption, distribution and metabolism. It was found that the volume of distribution did not change with age, and the increase in biologic half-life from 22.8 hours in the young subjects to 86.62 in the elderly subjects was due to a decreased rate of metabolism. When the one-point method is used, the size of the nightly dose of amobarbital should be reduced in elderly subjects from 200 mg to 50 mg in order to maintain the same steady-state blood levels found in younger subjects.
Adult↗
N-hydroxyamobarbital: the second major metabolite of amobarbital in man.
After oral administration of 14C-labeled amobarbital to healthy subjects, most of the radioactivity was recovered in urine and only 4-5% in feces over a period of 6 days. No unchanged amobarbital was excreted. Two major metabolites were found and isolated. One was 3'-hydroxyamobarbital, which has been previously identified by Maynert. The second could be identified as N-hydroxyamobarbital on the basis of its spectral and chemical properties.
Amobarbital↗
Single alternation with water reward:effects of sodium amobarbital on two strains of rats selectively bred for high and low emotionality.
The action of sodium amobarbital is studied during the patterning effect in rats selectively bred for low and high emotionality. The drug disrupts patterned running in the goal section of the alley in Maudsley non-reactive but not in Maudsley reactive rats for the last five trial-pairs. Sodium amobarbital also affects the behavior of these strains in a differential manner, in start and run sections, during the first trial-pair. The results show that a function-related physiological change has taken place in the Maudsley strains of rats.
Amobarbital↗
Amobarbital metabolism in man: N-glucoside formation.
N-Hydroxyamobarbital, the compound previously proposed as the second major metabolite of amobarbital was synthesized. The metabolite was shown not to be N-hydroxyamobarbital. NMR and MS analyses on the metabolite suggested it could be a derivative of N-beta-D-glucopyranoside. This proposed structure was confirmed by comparison with the spectral data of synthetic amobarbital-N-methyl-N-2,3,4,6-tetraacetyl-beta-D-glucopyranoside.
Amobarbital↗
A case of deficiency of N-hydroxylation of amobarbital.
It has been shown recently that the overall metabolism of amobarbital in man is essentially under genetic control. The drug normally undergoes two hydroxylation reactions, leading to 3'-hydroxyamobarbital (C-OH) and N-hydroxyamobarbital (N-OH). This paper describes a sibship in which two mothers who are identical twins show a gross deficiency on N-OH elimination in urine. The whole set of sibship data suggests that this deficiency represents a recessive trait controlled by a single pair of allelic autosomal genes which regulate N-OH formation. Several methodical approaches to assess an individual's capacity for N-OH formation are illustrated. There was no evidence of compensatory or concordant regulation of the two hydroxylation reactions. The case of this family illustrates that the functional lack of a biotransformation reaction is almost certain to be overlooked if one measures only the disappearance of a multimetabolized drug and not the appearance of metabolites.
Adolescent↗