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PubMed1984

Effects of zoxazolamine and related centrally acting muscle relaxants on nigrostriatal dopaminergic neurons.

The effects of zoxazolamine (ZOX) and related centrally acting muscle relaxants on striatal dopamine (DA) metabolism and turnover, and substantia nigra zona compacta DA neuronal impulse flow were studied in rats. ZOX, chlorzoxazone and mephenesin, but not meprobamate, chloral hydrate, diazepam, pentobarbital, ethanol or dantrolene, decreased striatal DA metabolism without affecting striatal DA concentrations. More specifically, ZOX, as a representative muscle relaxant, was shown to decrease striatal DA turnover without directly affecting DA synthesis, catabolism, reuptake, or release. ZOX decreased nigral DA neuronal firing rates and dramatically decreased firing rate variability (normally many of the cells fire with bursting firing patterns but after ZOX the cells often fired with a very regular pacemaker-like firing pattern). ZOX and related centrally acting muscle relaxants appear to decrease striatal DA turnover by decreasing both neuronal firing rate and firing rate variability. The possible relationships between DA neuronal activity and muscle tone are discussed.

Animals↗
PubMed1987

Serum dopamine-beta-hydroxylase activity and alcohol withdrawal symptoms.

Fifty male alcoholics had serum dopamine-beta-hydroxylase (DBH) activity, and serum prolactin (PRL) levels measured on the day of withdrawal, and 22 of them also on days 7 and 28 after it. The obtained values were related to the development of withdrawal symptoms. Treatment was begun with meprobamate on the first day of withdrawal, and from day 7 it was completed with disulfiram (250 and 500 mg/day, respectively). Serum DBH activity decreased significantly by day 7, however a further fall of it occurred by day 28 only in patients receiving high doses (500 mg) of disulfiram. PRL levels rose over the period of withdrawal which reached significance level on day 28. No correlation was found between serum DBH activity and the severity of withdrawal symptoms. Serum DBH activity did not differ from that of the healthy controls at either point of time, while serum PRL level was significantly elevated throughout the period of the study.

Adult↗
PubMed1982

Drug immunotoxicological approaches with some selected medical products: cyclophosphamide, methylprednisolone, betamethasone, cefoxitine, minor tranquillizers.

Alterations of the normal immune response were estimated in C57B1/6 mice pretreated with cyclophosphamide, methylprednisolone sodium succinate, betamethasone sodium phosphate or cefoxitine as positive controls and three minor tranquillizers: dipotassium chlorazepate, diazepam and meprobamate. The specific immune response against sheep red blood cells (SRBC) was evaluated by numeration of the direct plaque-forming cells (PFC; humoral immunity) and by measurement of the footpad swelling (delayed-type hypersensitivity, DTH). In our experiments, the results with the positive controls were in the same order as those described by others, and at the dose levels used, these three minor tranquillizers did not really alter the specific humoral and cellular immune response against SRBC in the C57B1/6 mice.

Animals↗
PubMedDate not supplied

The human distribution of some barbiturate sedatives in combination with miscellaneous CNS-active drugs.

This paper presents 14 cases in which the distribution of barbiturates and the hydroxylated metabolites in combination with miscellaneous CNS-active drugs was studied. In 7 of these cases the other drug present was methadone, and in the remainder dihydrocodeine, morphine, propoxyphene, amitriptyline, meprobamate, cyclizine and dipipanone, diphenhydramine and methaqualine. Amitriptyline, methadone, cyclizine and dipipanone, methaqualone and diphenhydramine appeared to modify the distribution of amylorbarbitone and quinalbarbitone. Likewise, the barbituates seemed to alter the distribution of amitriptyline, propoxyphene and, in one instance, methadone.

Adult↗
PubMed1996

Acute overdose of zolpidem.

Zolpidem (Ambien) is an imidazopyridine hypnotic recently introduced in the USA. We report a case of a fatal overdose of Ambien. A 68-year-old female ingested at least 30 tablets of 10 mg Ambien (300 mg). She was found dead at home. Toxicological analyses revealed blood concentration of 4.1, 19.3 and 2.3 micrograms/ml of zolpidem, meprobamate and carisoprodol, respectively.

Aged↗
PubMed1991

History of benzodiazepine dependence.

The benzodiazepines were developed in the 1950s, some introduced in the 1960s, and many more since then. Pharmacologically, they are sedative/hypnotics akin to alcohol, chloral, the barbiturates, and meprobamate. All have been widely used both within and outside the licit medical context. Usage of benzodiazepines increased dramatically during the 1960s and early 1970s; tranquilizer but not hypnotic usage has since declined. Both abuse and misuse were documented early, but the incidence was deemed low in view of the widespread prescription. Normal-dose physical dependence was first suspected in the early 1970s but it was not until the early 1980s that scientific evidence was adduced to establish its reality and frequency. Further studies have revealed the complex nature of the withdrawal syndrome. A reaction has set in against these drugs, with attempts to limit them to short-term use.

Anti-Anxiety Agents↗
PubMed1994

Impact of regulation on benzodiazepine prescribing to a low income elderly population, New York State.

On 1 January 1989, in an effort to reduce diversion of benzodiazepines for illicit use and reduce inappropriate prescribing, a regulation was implemented requiring the reporting of all benzodiazepine prescriptions to the New York State Department of Health. To assess the impact of the regulation on prescribing practices to the elderly, we followed the number of benzodiazepines and other central nervous system medications prescribed to a cohort of participants in an elderly pharmaceutical insurance program. Benzodiazepines were prescribed for 4652 (22%) of the 20,944 patients studied. By the last quarter of 1989, benzodiazepines were prescribed for 3120 (15%) patients, a decrease of 33%. The number of prescriptions of benzodiazepines decreased by 5010 (45%), from 11,123 to 6113. Decreases in the number of prescriptions were similar across benzodiazepine brands (range 40-56%). Statistically significant (p < 0.05) decreases were seen in all sex, age, race and marital status groups. Increases in number (and percent increases) of prescriptions for miscellaneous anxiolytics (i.e. hydroxyzine (399, 69%), meprobamate (299, 149%), buspirone (263, 111%), chloral hydrate (138, 265%), antidepressants (658, 19%), barbiturates (150, 29%), and tranquilizers (198, 19%), some of which may be more toxic or less effective, were noted. New York State's reporting regulation was effective in reducing both the number of patients being prescribed benzodiazepines and the number of prescriptions given to those who remain on benzodiazepines in the elderly population studies.

Aged↗
PubMed2004

Validated semiquantitative/quantitative screening of 51 drugs in whole blood as silylated derivatives by gas chromatography-selected ion monitoring mass spectrometry and gas chromatography electron capture detection.

A comprehensively validated procedure is presented for simultaneous semiquantitative/quantitative screening of 51 drugs of abuse or drugs potentially hazardous for traffic safety in serum, plasma or whole blood. Benzodiazepines (12), cannabinoids (3), opioids (8), cocaine, antidepressants (13), antipsychotics (5) and antiepileptics (2) as well as zolpidem, zaleplon, zopiclone, meprobamate, carisoprodol, tizanidine and orphenadrine and internal standard flurazepam, were isolated by high-yield liquid-liquid extraction (LLE). The dried extracts were derivatized by two-step silylation and analyzed by the combination of two different gas chromatographic (GC) separations with both electron capture detection (ECD) and mass spectrometry (MS) operating in a selected ion-monitoring (SIM) mode. Quantitative or semiquantitative results were obtained for each substance based on four-point calibration. In the validation tests, accuracy, reproducibility, linearity, limit of detection (LOD) and limit of quantitation (LOQ), selectivity, as well as extraction efficiency and stability of standard stock solutions were tested, and derivatization was optimized in detail. Intra- and inter-day precisions were within 2.5-21.8 and 6.0-22.5%, and square of correlation coefficients of linearity ranged from 0.9896 to 0.9999. The limit of quantitation (LOQ) varied from 2 to 2000 ng/ml due to a variety of the relevant concentrations of the analyzed substances in blood. The method is feasible for highly sensitive, reliable and possibly routinely performed clinical and forensic toxicological analyses.

Gas Chromatography-Mass Spectrometry↗
PubMed2004

The chick separation stress paradigm: a validation study.

To expand the generalizability of the chick separation stress paradigm as a high-throughput anxiolytic screen, six positive drug probes (doses in mg/kg: meprobamate 15-120, pentobarbital 2.5-20.0, chlordiazepoxide 2.5-15.0, buspirone 2.5-10.0, imipramine 1-15, and clonidine 0.10-0.25) and five negative drug probes (amphetamine 0.5-4.0, scopolamine 0.2-1.6, caffeine 5-20, chlorpromazine 1-30, and haloperidol 0.03-1.00) were evaluated in the test. Seven-day-old chicks received intramuscular injections of either vehicle or drug probe 15 min prior to tests in either a mirror (low-stress) or a no-mirror (high-stress) condition for a 3-min observation period. The dependent measures were distress vocalizations to index separation stress and sleep onset latency to index sedation. All positive drug probes attenuated distress vocalizations in a dose-dependent manner, except buspirone. All positive drug probes affected sleep onset latency in a dose-dependent manner, except buspirone and imipramine. In all cases, the anxiolytic-like effect of positive drug probes was greater than its sedative effect. None of the negative drug probes affected either distress vocalizations or sleep onset latency, except for the highest dose of amphetamine, which caused pronounced stereotypy. These findings demonstrate that this anxiolytic screen is sensitive to a wide range of positive pharmacological probes and insensitive to a wide range of negative pharmacological probes.

Animals↗
PubMedDate not supplied

[Prescription of psychotropic drugs in paediatry: approved indications and therapeutic perspectives].

In France, psychotropic drugs may be classified in four categories according to their official data. The first category corresponds to psychotropic drugs with an approved indication available in paediatry. Theyare old agents (e.g. haloperidol, amitriptyline, benzodiazepines...) with the exception of methylphenidate (hyperactivity). The second one corresponds to pharmacological agents approved for some indications obtained with adults but not for a1l (i.e. restricted indication: e.g. sertraline approved in paediatry only for OCD but not for depression, risperidone approved only for the treatment of disruptive behaviors in children with subaverage IQs). For the third category, the psychotropic agent is either contraindicated or unadvised under the age of 15 or 18 years, by lack of data (e.g. most of SSRI or atypical antipsychotic drugs). For the last category, official data available in brief summaries offer no information on paediatric use and consequently their administration does not appear possible. Up to now, no approved use has been delivered to injection route (IM or IV) in France, except for an IM formulation of zuclopenthixol. Prescribing psychotropic drug has to respect good practices including close psychological and somatic monitoring that associates the young patient and his relative (psycho-education program). Particular key-points should be taken into consideration (i.e. pharmacokinetic and physiological specificities, risk of false passage under the age of 6 years with capsules or tablets, presence of alcohol in some oral solution or bitter aroma...). Beside these official data, many studies have been published but must be carefully interpreted according to their level of pertinence. Meta-analysis gather all randomised controlled trials published or not, analyse their specific pertinence and thus provide clinically relevant elements. Randomised controlled trials present clinical interest but key-points in study design must be checked (e.g. number of patients, inclusion and exclusion criteria, length of the study and clinical relevance of clinical scales...). Other studies like open trials or clinical cases do not offersufficient guarantees. Some randomised controlled trials of clinical relevance have been carried out in this population with new pharmacological classes (eg SSRI, atypical antipsychotic drugs) and may lead to extended indications in children and adolescents. According to bibliographic and official data, the main criteria in the prescribing choice may take into consideration the following sis stressing a poor benefit/risk ratio. SSRI may offer better prospects but their use has not been approved in this indication, until now. In OCD, sertraline shows great interest to enhance clinical response and represents the molecule of reference. No drug has been approved for mood disorders in children or adolescent, in France, contrary to USA where lithium can be administered over the age of 12 years. In addition, antiepileptic drugs like carbamazepine or divalproate have conducted to clinical improvement in some studies. Benzodiazepines, hydroxyzine and meprobamate use should be strictly restricted in case of anxiety symptoms but are the only agents approved in this indication despise promising results obtained with SSRI. Transitory insomnia may take advantage of alimemazine prescription (approved use over the age of 36 months). Some typical neuroleptics are indicated in tics or in behaviour disorders associated to autism or related syndromes but present clinical limitations and poor tolerability. Promising clinical trials (randomised or not) have been conducted with new atypical antipsychotic drugs like risperidone. In conclusion, present data available for paediatric use of psychotropic agents emphasizes that safety and effectiveness are not always well established in particular for the treatment of chronic disorders (long term tolerability assessment). Moreover, studies should be carried out to specify factors promoting adherence and quality of life for this young population in order to optimise clinical benefit of drug prescription.

Adolescent↗
PubMed1977

Routine analysis of barbiturates and some other hypnotic drugs in the blood plasma as an aid to the diagnosis of acute poisoning.

A gas-liquid chromatographic method has been devised whereby both the qualitative and the quantitative analysis of a number of hypnotic drugs in the blood may be accomplished simultaneously. Small (50-mul) plasma aliquots are required. The technique is rapid and will detect 2 mg/l concentrations of these compounds. The barbiturates glutethimide, methaqualone, and meprobamate are the principal drugs covered by the scheme. After overdose the concentrations that occur in man are at, or above, this minimum level of detection.

Barbiturates↗
PubMed1998

Pharmacological evaluation of a modified open-field test sensitive to anxiolytic drugs.

In a recent study it has been shown that benzodiazepine receptor agonists attenuate novelty-induced suppression of feeding and increase the percentage of animals feeding in the open field. Food-deprived rats were placed in one corner of the open field containing food in the center. The number of rats beginning to eat in the first 5 min was recorded. In the present study this test was validated pharmacologically using known "anxiolytic" or "nonanxiolytic" drugs. The following substances (effective doses, given IP) increased the number of rats feeding within 5 min in the center of the open field: meprobamate (30.0-300 mg/kg), 8-OH-DPAT (10 and 30 microg/kg), ipsapirone (1.0 and 2.0 mg/kg), ritanserin (0.125-0.5 mg/kg), tropisetron (0.1-10.0 microg/kg), ondansetron (0.3-3.0 microg/kg), lisuride (0.28-0.55 mg/kg), morphine (0.3 and 1.0 mg/kg), propranolol (0.3 and 1.0 mg/kg), clozapine (1.0 mg/kg). Drugs without "anxiolytic" effects in other animal models or in humans, including amphetamine, apomorphine, haloperidol, sulpiride, and mCPP did not increase the incidence of food intake in this test. Ethanol and hexobarbital, in nonsedative doses, had no effect in this paradigm. Drugs and doses effective in the modified open-field test caused no increase in food intake in an independent food consumption test using food-deprived rats staying in the familiar cages. The results suggest that the modified open-field test can detect "anxiolytic" drug properties and is valid for the assessment of "anxiolytic" effects from different classes of drugs.

Animals↗
PubMed1981

Value of toxicological investigation in the diagnosis of acute drug poisoning in children.

In the 2 years 1978 and 1979 specimens from 287 children aged between 10 days and 14 years were received for general toxicological investigations. Of the 95 (33%) cases of confirmed poisoning, the diagnosis was established as a direct result of the analyses in 48 patients. No diagnosis was made in at least 85 (30%) of the remaining cases. Benzodiazepines were the drugs most commonly encountered (33%), followed by barbiturates, glutethimide, and meprobamate (15%), salicylate and paracetamol (15%), tricyclic antidepressants (12%), and ethanol (11%). 36 patients were severely poisoned (grade 3 or 4 coma, or convulsions), although only 1 patent died. There was evidence that drug(s) had been administered without authorisation in at least 7 instances, and in 51 (54%) of the poisoned patients there was sufficient concern about the safety of the child or the mode of administration of the drug(s) to institute legal proceedings (8 cases), involve the social services (25 cases), or arrange further medical appointments (18 cases). Drugs are readily available in most households and offer a means of inflicting injury that is less easily detectable than physical assault. For this reason, comprehensive toxicological investigations should be considered in children not only when they may assist in management but also in the presence of unusual or unexplained symptoms which could be drug-induced.

Adolescent↗
PubMed1985

Ability of calcium bis acetyl homotaurine, a GABA agonist, to prevent relapse in weaned alcoholics.

After they had been weaned off alcohol in hospital 85 severe alcoholics (above 200 g alcohol/day) were included in a double-blind study of calcium bis acetyl homotaurine (Ca AOTA, 25 mg/kg/day), a new gamma-aminobutyric acid agonist, versus placebo. Patients were treated as outpatients during the 3-month study. The only other treatment that patients received was meprobamate, 800 to 1200 mg/day, in the first month. The criterion for success was abstinence at 3 months (with normal gamma-glutamyl transpeptidase being one of the criteria). Of the 70 patients who completed the study, 33 received Ca AOTA and 37 placebo. 20 patients on Ca AOTA did not relapse, compared with 12 on placebo (p less than 0.02 by X2 test). Side-effects were noted by 7 patients on Ca AOTA and 2 on placebo. The results suggest that Ca AOTA may be useful in helping severe alcoholics who have been weaned off alcohol not to relapse.

Acamprosate↗
PubMed1990

Identification and differentiation of barbiturates, other sedative-hypnotics and their metabolites in urine integrated in a general screening procedure using computerized gas chromatography-mass spectrometry.

A gas chromatographic-mass spectrometric procedure is described for the identification and differentiation of sedative-hypnotics and their metabolites in urine. The following 24 barbiturates and thirteen other hypnotics could be detected: acecarbromal, allobarbital, amobarbital, aprobarbital, barbital, brallobarbital, bromisoval, (sec)butabarbital, butalbital, butobarbital, carbromal, clomethiazole, crotylbarbital, cyclobarbital, cyclopentobarbital, diethylallylacetamide, dipropylbarbital, glutethimide, guaifenesin, ethinamate, heptabarbital, hexobarbital, meprobamate, methaqualone, metharbital, methohexital, methylphenobarbital, methyprylone, pentobarbital, phenobarbital, propallylonal, pyrithyldione, secobarbital, thiobutabarbital, thiopental, vinbarbital and vinylbital. The procedure presented is integrated in a general screening procedure (general unknown analysis) for several groups of drugs detecting over 300 drugs and over 1000 of their metabolites. It includes cleavage of conjugates by acid hydrolysis, isolation by liquid-liquid extraction, derivatization by acetylation, separation by capillary gas chromatography, and identification by computerized mass spectrometry. Using mass chromatography with the selected ions m/z 83, 117, 141, 167, 169, 207, 221 and 235, the presence of barbiturates, other hypnotics and/or their metabolites was indicated. The identity of positive signals in the reconstructed mass chromatograms was confirmed by a visual or computerized comparison of the stored full mass spectra with the reference spectra. The sample preparation, mass chromatograms, reference mass spectra and gas chromatographic retention indices are documented.

Acetylation↗
PubMed2000

Flumazenil reversal of carisoprodol (Soma) intoxication.

A 52-year-old woman presented with central nervous system depression and a Glasgow Coma Score of 9 secondary to ingestion of carisoprodol, a centrally acting muscle relaxant analgesic. After administration of i.v. flumazenil, the patient's neurologic status normalized and she required no further therapy. Carisoprodol and its active sedative-hypnotic metabolite, meprobamate, are gamma aminobutyric acid receptor indirect agonists with central nervous system chloride ion channel conduction effects similar to the benzodiazepines, thus making flumazenil a potentially useful antidote in toxic presentations.

Antidotes↗
PubMed2005

Fate of endocrine-disruptor, pharmaceutical, and personal care product chemicals during simulated drinking water treatment processes.

The potential occurrence of endocrine-disrupting compounds (EDCs) as well as pharmaceuticals and personal care products (PPCPs) in drinking water supplies raises concern over the removal of these compounds by common drinking water treatment processes. Three drinking water supplies were spiked with 10 to 250 ng/L of 62 different EDC/ PPCPs; one model water containing an NOM isolate was spiked with 49 different EDC/PPCPs. Compounds were detected by LC/MS/MS or GC/MS/MS. These test waters were subjected to bench-scale experimentation to simulate individual treatment processes in a water treatment plant (WTP). Aluminum sulfate and ferric chloride coagulants or chemical lime softening removed some polyaromatic hydrocarbons (PAHs) but removed <25% of most other EDC/ PPCPs. Addition of 5 mg/L of powder activated carbon (PAC) with a 4-h contact time removed 50% to >98% of GC/ MS/MS compounds (more volatile) and 10% to >95% of LC/ MS/MS compounds (more polar); higher PAC dosages improved EDC/PPCP removal. EDC/PPCP percentage removal was independent of the initial compound concentration. Octanol-water partition coefficients served as a reasonable indicator of compound removal under controlled PAC test conditions, except for EDC/PPCPs that were protonated or deprotonated at the test pH and some that contained heterocyclic or aromatic nitrogen. Separate chlorine or ozone experiments decreased the EDC/PPCP initial concentration by <10% to >90%; EDC/PPCPs were likely transformed to oxidation byproducts. Ozone oxidized steroids containing phenolic moieties (estradiol, ethynylestradiol, or estrone) more efficiently than those without aromatic or phenolic moieties (androstenedione, progesterone, and testosterone). EDC/PPCP reactivity with oxidants were separated into three general groups: (1) compounds easily oxidized (>80% reacted) by chlorine are always oxidized at least as efficiently by ozone; (2) 6 of the -60 compounds (TCEP, BHC, chlordane, dieldrin, heptachlor epoxide, musk ketone) were poorly oxidized (<20% reacted) by chlorine or ozone; (3) compounds (24 of 60) reacting preferentially (higher removals) with ozone rather than chlorine. Conventional treatment (coagulation plus chlorination) would have low removal of many EDC/PPCPs, while addition of PAC and/or ozone could substantially improve their removals. Existing strategies that predict relative removals of herbicides, pesticides, and other organic pollutants by activated carbon or oxidation can be directly applied for the removal of many EDC/PPCPs, but these strategies need to be modified to account for charged (protonated bases or deprotonated acids) and aliphatic species. Some compounds (e.g., DEET, ibuprofen, gemfibrozil) had low removals unless ozonation was used. Other compounds had low removals by all the WTP processes considered (atrazine, iopromide, meprobamate, TCEP), and removal processes capable of removing these types of compounds should be investigated.

Alum Compounds↗
PubMed1976

Solid-phase synthesis of drug glucuronides by immobilized glucuronosyltransferase.

Rabbit liver glucuronosyltransferase immobilized on beaded agarose has been used to synthesize glucuronic acid conjugates of meprobamate, diethylstibestrol, bilirubin, borneol, benzioc acid, and p-nitrothiophenol. The immobilized enzyme exhibited a high degree of specificity for UDPGA as cofactor when p-nitrophenol is used as substrate. Other cofactors tested were less effective, all producing less than 10% conjugation relative to UDPGA. The effects on agarose-bound enzyme activity of a variety of cosolvents and emulsifiers have been studied. Ethanol, dimethyl sulfoxide, propylene glycol, and bovine serum albumin are among the cosolvents and emulsifiers which can be used within limited concentration ranges to sulubilize lipophilic substrates for conjugation. Concentrations of calcium and magnesium cations between 1.5 and 10.0mM were found to enhance glucuronosyltransferase activity of the immobilized enzyme.

Calcium↗