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PubMed1979

Self-poisoning treated in the ICU.

This retrospective study compares number and type of self-poisonings admitted to the intensive care units (ICU) at Sahlgren's Hospital, Gothenburg, during 1972 and 1976. The total number of patients requiring intensive care was unchanged, but a change in the pattern of self-poisoning was seen. In 1976 the number of patients requiring intensive care following acute alcohol intoxication had increased, whereas the number of barbiturate and methaqualone poisonings decreased. Tricyclic antidepressants formed the largest group in both years. Fewer patients needed endotracheal intubation and IPPV in 1976 than in 1972. Also, fewer complications were seen, and the death rate among ICU-treated patients decreased. In the Gothenburg area barbiturates accounted for one half of all deaths due to self-poisoning and tricyclic antidepressants for one fifth. Any expected decrease in intensive care as a result of fewer barbiturate and methaqualone poisonings was obscured by an increase in severe alcohol intoxication.

Alcoholic Intoxication↗
PubMed1979

Anomie and drug use in high school students.

The use of alcohol, tobacco, and drugs as it relates to anomie was studied in 11th grade students. A questionnaire was administered to 1,314 11th grade students which included Srole's Anomie Scale as well as items pertaining to the usage of alcohol, tobacco, marijuana, cocaine, LSD, heroin, amphetamines, barbiturates, and methaqualone. The name of each drug was given along with the colloquial terms typically used to identify each drug. Substance users showed significantly higher anomie scores than nonusers on alcohol, tobacco, marijuana, LSD, amphetamines, and barbiturates. Although the results were not statistically significant for cocaine, heroin, or methaqualone, the differences between substance users and nonusers were all in the predicted direction.

Adolescent↗
PubMed1989

[Observation on the efficacy and experimental study of compound suanzaoren ansen capsules in insomnia].

374 patients suffering from insomnia were divided into three groups by random: 202 cases in group I were treated with compound Suanzaoren Ansen capsules (SAC); 85 cases in group II were treated with Zhusha Ansen pills (ZAP) as control; 87 cases in group III were treated with Methaqualone (Hyminal) also as control. The therapeutic results were as follows: Groups I, II and III showed significant effective rates of 49.50%, 18.82% and 32.18% respectively; moderate effective rates of 34.65%, 48.24% and 49.43% respectively; and total rates of effectiveness of 84.15, 67.06% and 81.61% respectively. The authors found significant statistical difference between group I and II (P less than 0.005) and of no statistical difference between group I and III (P greater than 0.05). The results showed that the effects of compound SAC were better than ZAP, and similar to that of methaqualone. EEG analysis carried out while sleeping confirmed the effects mentioned above. Low toxicity (LD50 10.7 g/kg) of compound SAC was found through animal experimentations. No towards reactions were revealed in clinical trials except nausea in 3 cases. Heart rate and blood pressure changed lightly in a few cases.

Adolescent↗
PubMed1981

[Detoxication by hemoperfusion].

In 13 patients (2 males, 11 females, 15-70 years of age) on account of severe intoxications with hypnotics sedatives, psychopharmaca, in most cases mixed intoxications, with propranolol and halogenized hydrocarbons a 4--8-hour haemoperfusion treatment with amberlite XAD-4-Resin was performed. 11 patients survived, 1 patient died in irreversible cardiogenic shock of a propranolol intoxication, another patient of the sequels of a crotylbarbital and methaqualone intoxication. The curves of the course of the blood concentration of the individual substances showed a good elimination for phenobarbital and crotylbarbital, methaqualone, meprobamat and didropyridine as well as trichlorethylene, a less good elimination for nitrazepam, propranolol and tetrachlorethylene, Altogether the effectiveness of the detoxication clearly higher in the time unit, compared with the dialysis.

Adolescent↗
PubMed1980

Hemodynamic failure induced by narcotic and toxic doses of 12 CNS depressants in intact and pithed rats.

UNLABELLED: Heart rate (HR), cardiac output (CO), stroke volume (SV), arterial blood pressure (BP), and peripheral resistance (PR) were assessed in awake rats and in rats anesthetized with hexobarbital, pentobarbital, secobarbital, secbutabarbital, methaqualone, chloral hydrate, urethane, ethanol, guaiphenesine, meprobamate, diazepam and chlorpromazine (respired artificially). Anesthesia mostly was accompanied by an increase of HR and PR and a decrease of CO and SV, whereas BP remained unchanged or somewhat declined. Infusion of further amounts of the CNS depressants caused a dose-dependent decrease of HR, CO and BP but did not influence SV whereas PR declined but did not fall considerably beyond the values in awake rats. A strong decline of CO, SV and BP but no change of HR and PR occurred after pithing in rats. Anesthetic doses of hexobarbital, pentobarbital, secobarbital, secbutabarbital, methaqualone, and guaiphenesine produced no hemodynamic effects in pithed rats. Chloral hydrate, urethane, ethanol, meprobamate, diazepam, and chlorpromazine, on the other hand, in anesthetic doses depressed the CO and BP of pithed rats without influencing PR. In toxic doses, the CNS depressants caused comparable hemodynamic changes in pithed as in anesthetized rats. CONCLUSION: Hemodynamic failure induced by narcotic doses of CNS depressants is mainly due to a depression of the vasomotor center(s) and an impairment of cardiovascular reflex control, that after toxic doses is mainly caused by the direct cardiovascular-depressive actions of these drugs.

Animals↗
PubMed1975

Experimental drug intoxication: treatment with charcoal haemoperfusion.

Dogs were given large doses of barbiturates, glutethimide, ethanol, methaqualone, ethchlorvynol, meprobamate, chloral hydrate, paracetamol and aspirin. These were treated by haemoperfusion using a column packed with charcoal coated with an acrylic hydrogel. Clearances for most drugs were significantly higher than those reported for haemodialysis. Minimal clearances of common biochemical entities were observed and although leucocyte and platelet counts were diminished, no deleterious effects attributable to this were encountered. Careful histological examination of tissues derived from perfused dogs revealed no evidence of charcoal emboli.

Acetaminophen↗
PubMed1978

Determination of monoureides in biological fluids by high-pressure-liquid-chromatography.

A sensitive and specific method for the simultaneous determination of bromisoval, carbromal, and methaqualone is described. The drugs are adsorbed from serum onto charcoal at pH 11 and eluted from it with organic solvent. The eluate is separated by high-pressure liquid-chromatography on reverse phase (RP 18) column using acetonitrile: water (26 : 74 by volume) as mobile phase. The eluted drugs are detected by uv-absorption at 210 nm. The method is sensitive, specific, precise, and accurate.

Bromisovalum↗
PubMedDate not supplied

Learned taste aversions induced by hypnotic drugs.

Taste aversions reflect the association of drug-produced noxious interoceptive stimuli with distinctive tastes. In the present experiments, taste aversions to sweetened condensed milk were induced in rats by a wide range of doses of the hypnotic drugs, hexobarbital, amobarbital, chloral hydrate, flurazepam and methaqualone and by anesthetization with ethyl ether. Observation of changes in motor behavior following drug administration could not be used to predict the development of taste aversions. Despite the fact that hypnotic drugs have punishing properties, which these paradox is discussed in terms of procedural differences between taste aversion and self-administration experiments.

Animals↗
PubMed1993

Quantification of dimethindene in plasma by gas chromatography-mass fragmentography using ammonia chemical ionization.

A gas chromatographic-mass fragmentographic method using ammonia chemical ionization for the determination of dimethindene in human plasma is described. The drug was isolated from plasma by liquid-liquid extraction with hexane-2-methylbutanol. Plasma components were separated on a capillary column coated with chemically bonded methyl silicone. For detection of dimethindene, its quasi-molecular ion (M + H+) was mass fragmentographically monitored after chemical ionization with ammonia as reagent gas. Dimethindene was quantified using methaqualone as the internal standard: the quantification limit in plasma was 0.2 ng/ml, the within-run precision was 8.0% and the inter-run precision 5.6%. The plasma concentration-time profile was established after a single dose of 4 mg of dimethindene with an average maximum concentration of 5.5 ng/ml, detectable up to 48 h post application.

Ammonia↗
PubMedDate not supplied

One man's poison.

In an unrandomised uncontrolled study on boats and trains, capsules of flurazepam (30 mg) and temazepam (20 mg), when chewed, but not when swallowed whole (even with the ends pricked), gave a better night's sleep than 'Mandrax' (methaqualone 250 mg/diphenhydramine 50 mg) and a better night's sleep than nitrazepam 7.5 mg.

Capsules↗
PubMed1997

Shift of the high-performance liquid chromatographic retention times of metabolites in relation to the original drug on an RP8 column with acidic mobile phase.

The effect of the structural change in the metabolization of drugs on the HPLC retention time with an RP8 column with an acetonitrile-phosphate buffer (pH 2.3) as the mobile phase was investigated at model compound pairs of 29 functionalization reactions. A more or less typical region for T(M)=log(k'M/k'D) was found for each of these reactions (with k'M and k'D being the capacity factors of the metabolite and the drug, respectively), which can be explained by an increase or a decrease of the hydrophilic properties caused by the structural change. This effect is superimposed by an essential influence of the unchanged part of the molecule and in some cases by special intramolecular interactions like the hydrogen bond. Despite the more complicated structure of real drugs the results obtained at the model compound pairs were confirmed for most of the 55 metabolite/drug pairs. The practical use of the T(M) values as a support to distinguish between different metabolites in the HPLC-DAD analysis of intoxications is demonstrated with cases of poisoning with diphenhydramine, propafenone and methaqualone.

Chromatography, High Pressure Liquid↗
PubMed1990

Synthesis and anticonvulsant activity of some new 2-substituted 3-aryl-4(3H)-quinazolinones.

A series of 4(3H)-quinazolinones structurally related to 2-methyl-3-o-tolyl-4(3H)-quinazolinone (methaqualone, 3) were synthesized and evaluated for anticonvulsant activity. Preliminary screening of these compounds revealed that 2-[2-oxo-2-(4-pyridyl)ethyl]-3-aryl-4(3H)-quinazolinones 6l and 8i, 8k, and 8p-r having a single ortho substituent on the 3-aryl group had the most promising anticonvulsant activity. Compounds 6l and 8i possessing 3-o-tolyl and 3-o-chlorophenyl groups, respectively, showed good protection against MES- and scMet-induced seizures, combined with relatively low neurotoxicity after intraperitoneal administration in mice. They also exhibited low toxicity in tests for determining the mean hypnotic dose (HD50) and the median lethal dose (LD50). Although these compounds were markedly more potent as anticonvulsants when administered orally in mice and rats, they were also more neurotoxic. This neurotoxicity was particularly acute in oral tests with rats, which resulted in marginal protective indices. In drug differentiation tests, compound 6l was ineffective against seizures induced by bicuculline, picrotoxin, and strychnine, while 8i showed some protection against picrotoxin-induced seizures.

Animals↗
PubMed1976

[Treatment of severe hypnotic poisoning with extracorporeal haemoperfusion (author's transl)].

Four patients with severe hypnotic intoxication, twice after suicidal intake of barbital, once of barbital, methaqualone and carbromal, and once of carbromal, were treated with six activated charcoal haemoperfusions. Three patients showed rapid improvement in the level of consciousness followed by complete recovery. One female patient died in cerebral coma due to complete acute cerebromalacia following hypoxia. Serious complications due to the haemoperfusion did not occur. Correct use of activated charcoal haemoperfusion enriches the therapeutic spectrum of severe exogenous intoxications.

Adult↗
PubMedDate not supplied

Solid-phase extraction and GC/MS confirmation of barbiturates from human urine.

A highly selective and sensitive procedure has been developed for isolating and identifying barbiturates in human urine. With a new disposable bonded silica gel solid-phase extraction (SPE) column and hexobarbital as an internal standard (IS), amobarbital, butabarbital, pentobarbital, phenobarbital, secobarbital, and methaqualone were selectively isolated from endogenous urine components. Capillary gas chromatography/ion trap mass spectrometry (GC/MS) analysis of the extracts generated a full mass spectrum for the detection, identification, and quantitation of barbiturates. Linear quantitative response curves for the drugs have been generated over a concentration range of 20-500 ng/mL. Overall extraction efficiencies for drugs averaged greater than 90%, and the quantitative response curves exhibited correlation coefficients of 0.996 to 0.999.

Amobarbital↗
PubMed1996

A case of lethal intoxication after ingestion of toquilone compositum.

A case of acute intoxication of both methaqualone and diphenhydramine is reported. The analysis of these compounds was performed by liquid-liquid extraction (Toxi-Lab DPC procedure) followed by gas chromatography/mass spectrometry determination; both substances are contained in the pharmaceutical formulation called Toquilone Compositum (Medichemie, Switzerland).

Bile↗
PubMed1983

Students and drug abuse, 1974 and 1980.

The paper presents a secondary analysis of students treated in hospital emergency rooms. The comparison of data provided in 1974 and 1980 data reveals a significant increase in the abuse of alcohol with drugs, methaqualone and marijuana. Fifty percent of these students ingested drugs to commit suicide or as a suicide gesture. These data suggest that school health professionals and counselors be alerted to student drug overdoses to assist students confronted with suicidal ideation.

Adolescent↗
PubMed1973

Changes in plasma -glutamyl transpeptidase activity associated with alterations in drug metabolism in man.

A significant rise in plasma gamma-glutamyl transpeptidase activity (GGT) was observed on 13 out of 14 occasions on which patients on long-term treatment with the oral anticoagulant warfarin were given amylobarbitone, quinalbarbitone, or phenazone (antipyrine) for 30 days. In 13 of these 14 studies there was evidence that drug administration had stimulated the rate of warfarin metabolism. One patient showed no increase in plasma GGT activity, yet a significantly increased rate of warfarin metabolism, and another patient showed an increase in plasma GGT activity without a change in warfarin metabolism. When alterations in both plasma GGT activity and plasma warfarin concentration occurred together in response to drug administration the changes followed a similar time course, occurring after about one week of drug administration with maximal changes at about 10 or 15 days. Administration of chlordiazepoxide, diazepam, nitrazepam, and methaqualone did not stimulate the rate of warfarin metabolism in four patients studied, but plasma GGT activity increased significantly in two of these four instances. The implications of these observations in the interpretation of plasma GGT activities are discussed.

Acyltransferases↗