-
British Journal of Pharmacology Aug 19701. When administered to intact white mice, the central depressants-diphenhydramine, promethazine, chlorpromazine, gammahydroxybutyrate, gammabutyrolactone, hyoscine, and...
1. When administered to intact white mice, the central depressants-diphenhydramine, promethazine, chlorpromazine, gammahydroxybutyrate, gammabutyrolactone, hyoscine, and pethidine-produced sedation in small doses, but excitement and convulsions in higher doses. When given to mice pretreated with subanaesthetic doses of phenobarbitone these drugs abolished the righting reflex both in convulsant doses (hyoscine excepted) and in non-convulsant doses. These effects are similar to the effects previously observed with local anaesthetics.2. Meprobamate, diazepam and chlorpromazine produced a loss of righting reflex both when given alone and following phenobarbitone. When given alone in higher doses, chlorpromazine induced convulsions.3. The central stimulants bemegride and picrotoxin antagonized the loss of righting reflex produced by phenobarbitone, but nikethamide, caffeine and strychnine did not alter the depressant effects of phenobarbitone.4. On the basis of these and previous studies with intact white mice a tentative classification of drugs having generalized depressant and stimulant effects on the central nervous system was proposed and discussed.
Topics: Adjuvants, Anesthesia; Aminobutyrates; Animals; Bemegride; Caffeine; Central Nervous System; Central Nervous System Stimulants; Chlorpromazine; Diazepam; Diphenhydramine; Female; Glutamates; Hydroxybutyrates; Lactones; Meperidine; Meprobamate; Mice; Motor Activity; Nikethamide; Phenobarbital; Picrotoxin; Promethazine; Reflex; Scopolamine; Seizures; Strychnine; Tranquilizing Agents
PubMed: 4394969
DOI: 10.1111/j.1476-5381.1970.tb09895.x -
Acta Poloniae Pharmaceutica 2005The dried extracts of aerial parts of Celesia coromandeliane Vahl. (Scrophulariaceae) were evaluated for CNS activities in mice. The methanol extract of aerial part of...
The dried extracts of aerial parts of Celesia coromandeliane Vahl. (Scrophulariaceae) were evaluated for CNS activities in mice. The methanol extract of aerial part of Celesia coromandeliane (MECC) was found to cause significant depression in general as well as exploratory behavioral profiles in mice. MECC showed reduction in muscle relaxant activity by 30 degrees inclined screen test, as well as potential remarkably the pentobarbitone sodium-, diazepam- and meprobamate-induced sleeping time of mice. The petroleum ether extract of aerial parts of Celesia coromandeliane (PECC) showed significant analgesic properties as evidenced by the significant reduction in the number of writhes and stretches induced in mice by 1.2% acetic acid solution. Pretreatment with PECC caused significant protection against strychnine- and leptazol-induced convulsions. All these results were compared with respective controls for the evaluation of significance. The presence of steroids in PECC and saponins in MECC might be responsible for respective CNS activities in mice.
Topics: Analgesics; Animals; Anticonvulsants; Behavior, Animal; Central Nervous System Agents; Ethers; Exploratory Behavior; Female; Lethal Dose 50; Male; Medicine, Traditional; Methanol; Mice; Muscle Relaxants, Central; Plant Extracts; Scrophulariaceae; Sleep; Solvents
PubMed: 16459484
DOI: No ID Found -
Basic & Clinical Pharmacology &... Mar 2014Deliberate drug poisoning leads to 1% of emergency department (ED) admissions. Even if most patients do not exhibit any significant complication, 5% need to be referred...
Deliberate drug poisoning leads to 1% of emergency department (ED) admissions. Even if most patients do not exhibit any significant complication, 5% need to be referred to an intensive care unit (ICU). Emergency physicians should distinguish between low- and high-acuity poisoned patients at an early stage to avoid excess morbidity. Our aim was to identify ICU transfer factors in deliberately self-poisoned patients without life-threatening symptoms on admission. We performed a 3-year retrospective observational study in a university hospital. Patients over 18 years of age with a diagnosis of deliberate drug poisoning were included. Clinical and toxicological data were analysed with univariate tests between groups (ED stay versus ICU transfer). Factors associated with ICU admission were then included in a logistic regression analysis. Two thousand five hundred and sixty-five patients were included. 63.2% were women, and median age was 40 (28-49). 142 patients (5.5%) were transferred to ICU. Cardiac drugs [adjusted OR (aOR) = 19.81; 95% confidence interval (95% CI): 7.93-49.50], neuroleptics (aOR = 2.78; 95% CI: 1.55-4.97) and meprobamate (aOR = 2.71; 95% CI: 1.27-5.81) ingestions were significantly linked to ICU admission. A presumed toxic dose ingestion (aOR = 2.27; 95% CI: 1.28-4.02), number of ingested tablets (aOR = 1.01; 95% CI: 1.01-1.02 for each tablet) and delay between ingestion and ED arrival <2 hr (aOR = 2.85; 95%CI: 1.62-5.03) were also factors for ICU referral. The Glasgow Coma Scale was the only clinical feature associated with ICU admission (aOR = 1.57; 95% CI: 1.44-1.70 for each point loss). These results suggest that emergency physicians should pay particular attention to toxicological data on ED admission to distinguish between low- and high-acuity self-poisoned patients.
Topics: Adult; Emergency Service, Hospital; Female; Glasgow Coma Scale; Hospitals, University; Humans; Intensive Care Units; Male; Middle Aged; Patient Transfer; Poisoning; Referral and Consultation; Retrospective Studies; Self-Injurious Behavior
PubMed: 23998644
DOI: 10.1111/bcpt.12132 -
Japanese Journal of Pharmacology Nov 1989Zopiclone is a new cyclopyrrolone derivative which exerts pharmacological activities similar to those of benzodiazepines in behavioral and biochemical studies. In order...
Zopiclone is a new cyclopyrrolone derivative which exerts pharmacological activities similar to those of benzodiazepines in behavioral and biochemical studies. In order to clarify the discriminative stimulus properties of zopiclone, 8 rats were trained to discriminate the interoceptive stimulus induced by zopiclone (3.2 mg/kg, i.p.) from those of saline. Following discrimination acquisition, administration of zopiclone resulted in drug-appropriate responding with an ED50 of 1.3 (1.0-1.8) mg/kg. The zopiclone discriminative stimulus generalized to the benzodiazepines diazepam (1.8 mg/kg), nitrazepam (10 mg/kg) and alprazolam (10 mg/kg). A non-benzodiazepine, suriclone, at 3.2 mg/kg, generalized to the zopiclone stimulus in 5 out of 7 rats, but meprobamate, hydroxyzine, tracazolate and muscimol did not. The benzodiazepine antagonist Ro 15-1788 (1 mg/kg) completely blocked zopiclone stimulus. In contrast, however, bicuculline and pentetrazol failed to antagonize it. The serotonin antagonist cinanserin and ritanserin neither generalized to the zopiclone stimulus nor did they exhibit antagonism. These results suggest that the zopiclone discriminative stimulus is mediated by binding to benzodiazepine receptors and appears not to be related to GABAergic or serotonergic system.
Topics: Animals; Anti-Anxiety Agents; Azabicyclo Compounds; Behavior, Animal; Benzodiazepines; Bicuculline; Discrimination Learning; Dose-Response Relationship, Drug; Flumazenil; Hypnotics and Sedatives; Male; Muscimol; Naphthyridines; Pentylenetetrazole; Piperazines; Piperidines; Rats; Rats, Inbred WKY; Ritanserin; Serotonin Antagonists; Sulfur Compounds
PubMed: 2576082
DOI: 10.1254/jjp.51.337 -
Basic & Clinical Pharmacology &... Nov 2009The centrally acting muscle relaxant carisoprodol has previously been shown to cause psychomotor impairment and to have a narrow therapeutic range. In Norway,...
The centrally acting muscle relaxant carisoprodol has previously been shown to cause psychomotor impairment and to have a narrow therapeutic range. In Norway, carisoprodol was therefore reclassified to the highest scheduling level from 1 August 2007 and withdrawn from the market on 1 May 2008. The aim of this study was to examine to what extent this action resulted in reduced numbers of driving under the influence (DUI) cases and forensic autopsies concerning carisoprodol, as well as reduced numbers of contacts to the National Poisons Information Centre (NPIC) in Norway regarding carisoprodol. From 2004 to 2008, carisoprodol (and/or its metabolite meprobamate) was detected in a total of 1261 DUI cases, decreasing from 312 in 2004 to 47 in 2008. During the same period, carisoprodol was detected in 194 forensic autopsies, also here decreasing, from 53 cases in 2004 to 11 cases in 2008. The NPIC received 1180 contacts primarily concerning carisoprodol over this period, decreasing from 267 contacts in 2004 to 87 contacts in 2008. During the same period, the sales figures for carisoprodol decreased dramatically, and we observed a relation between the numbers of DUI cases, forensic autopsies and contacts to the NPIC concerning carisoprodol and the sales figures for the drug. This study showed that the rescheduling and withdrawal of carisoprodol from the Norwegian market had a positive effect on the prevalence of carisoprodol in impaired driving, deaths and contacts regarding intoxications. This, together with previous publications, indicates that the population reflected in our data uses regularly prescribed carisoprodol and, to a lesser degree, drug from an illegal street market.
Topics: Accidents, Traffic; Automobile Driving; Carisoprodol; Forensic Toxicology; Humans; Meprobamate; Muscle Relaxants, Central; Norway; Poison Control Centers; Poisoning; Prevalence; Risk Factors; Safety-Based Drug Withdrawals; Substance Abuse Detection
PubMed: 19663822
DOI: 10.1111/j.1742-7843.2009.00459.x -
Canadian Medical Association Journal Jun 1956
Topics: Anticonvulsants; Anxiety; Anxiety Disorders; Mental Disorders; Meprobamate; Muscle Relaxants, Central
PubMed: 13316683
DOI: No ID Found -
Annals of the Rheumatic Diseases Nov 1963
Topics: Aminopyrine; Antirheumatic Agents; Aspirin; Blood Platelets; Chloroquine; Colchicine; Complement Fixation Tests; Drug Hypersensitivity; Gold; Humans; Hydroxychloroquine; Meprobamate; Phenacetin; Phenylbutazone; Probenecid; Purpura; Purpura, Thrombocytopenic; Quinacrine; Rheumatic Diseases; Splenectomy; Toxicology
PubMed: 14087256
DOI: 10.1136/ard.22.6.440 -
British Journal of Pharmacology Aug 19701. In the neuronally isolated cortex of the cat, local application of diphenhydramine, promethazine, gammahydroxybutyrate, gammabutyrolactone, gamma aminobutyric acid,...
1. In the neuronally isolated cortex of the cat, local application of diphenhydramine, promethazine, gammahydroxybutyrate, gammabutyrolactone, gamma aminobutyric acid, hyoscine and pethidine, and the intravenous injection of diazepam and meprobamate depressed or abolished the surface negative and surface positive response to direct stimulation and raised the stimulus threshold of the positive burst response. These effects were the same as previously demonstrated for general and local anaesthetics on the same preparation.2. Chlorpromazine produced a similar depression in small concentrations but caused spontaneous activity in higher concentrations.3. In contrast to local application, pethidine when given by intravenous injection in a high dose produced convulsant activity in the isolated cortical slab. The possibility was suggested that the convulsant activity was produced by a metabolite of pethidine.4. The results of this investigation suggest that the central depression produced by a number of structurally unrelated drugs is indicative of an anaesthetic-like property of these drugs.
Topics: Action Potentials; Aminobutyrates; Anesthesia, General; Anesthesia, Local; Animals; Cats; Cerebral Cortex; Chlorpromazine; Depression, Chemical; Diazepam; Diphenhydramine; Electric Stimulation; Female; Hydroxybutyrates; In Vitro Techniques; Lactones; Male; Meperidine; Meprobamate; Promethazine; Scopolamine; Seizures; Tranquilizing Agents
PubMed: 5485146
DOI: 10.1111/j.1476-5381.1970.tb09896.x -
British Journal of Clinical Pharmacology Jul 2009
Topics: Adolescent; Adult; Aged; Anti-Anxiety Agents; Drug Overdose; Female; Glasgow Coma Scale; Humans; Male; Meprobamate; Middle Aged; Young Adult
PubMed: 19660012
DOI: 10.1111/j.1365-2125.2009.03406.x -
California Medicine Aug 1957Emotional disturbances in children may be due to an anxiety state, to obsessive-compulsive neurosis, to schizophrenia or to a brain injury causing a behavior disorder....
Emotional disturbances in children may be due to an anxiety state, to obsessive-compulsive neurosis, to schizophrenia or to a brain injury causing a behavior disorder. Children in an anxiety state have difficulty in school because anxiety interferes with concentration, impairs memory and makes decisions difficult. Consequently, these children often fear school and express their anxiety by behavior disturbances which alienate them from parents and teachers. There are a number of chemotherapeutic agents physicians can use as a part of the treatment of emotionally disturbed children. Phenobarbital is valuable for short-term therapy for the anxious child. Meprobamate also may be prescribed for anxiety reactions. It is of limited value for the hyperkinetic and obsessive-compulsive child and of no value in the schizophrenic child. Atarax (hydroxyzine dihydrochloride) is beneficial for the neurotic and hyperkinetic brain-injured child. Children with severe anxiety reactions and schizophrenic disorders respond best to chlorpromazine or reserpine.It must be emphasized that drug therapy is a part of the total therapeutic attack on the emotional problems of children.
Topics: Anxiety; Anxiety Disorders; Attention Deficit Disorder with Hyperactivity; Attention Deficit and Disruptive Behavior Disorders; Child; Child Behavior Disorders; Chlorpromazine; Emotions; Humans; Mental Disorders; Meprobamate; Obsessive-Compulsive Disorder; Parents; Reserpine; Schizophrenia; Tranquilizing Agents
PubMed: 13446749
DOI: No ID Found