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PubMed1977

[Effects of minor tranquilizers and neuroleptics on open-field behavior in rats (author's transl)].

Minor tranquilizers (diazepam, nitrazepam, oxazepam, bromazepam, medazepam, fludiazepam, meprobamate) at low doses increased ambulation score to 145 approximately 288% of control rats. Nitrazepam, diazepam and bromazepam which are potent, clinically prescribed minor tranquilizers increased the ambulation at lower doses than was seen with the other drugs. Fludiazepam and nitrazepam showed a maximum increase in ambulation at the same dose. Fludiazepam, nitrazepam and diazepam proved to have potent inhibitory effects on defecation. Trifluperidol, haloperidol and ID-4708 (a new butyrophenone derivative) and chlorpromazine when given at low doses reduced ambulation, while at higher doses defecation was inhibited. These four drugs reduced ambulation and elicited a recover in rates of defecation in methamphetamine treated rats. Clozapine, thioridazine and floropipamide inhibited defecation at nearly the same doses which reduced ambulation in rats not given the methamphetamine tratment. These three durugs reduced ambulation, but did not produce a recovery in the defecation rates in methamphetamine-treated rats. These results indicate that neuroleptics such as clozapine which rarely induce extrapyramidal side-effects when clinically prescribed, inhibit defecation at nearly the same doses which reduce ambulation. In methamphetamine-treated rats, haloperidol was 31 times more potent than chlorpromazine in inhibiting activity noted with ambulation. This ratio in open-field test was close to the ratio of potency of these drugs as antipsychotic clinically prescribed agents.

Animals↗
PubMed1979

[Decrease of ACh response in isolated duodenum from SART stressed (repeated cold stressed) mice (author's transl)].

ACh response in the isolated duodenum from SART stressed (repeated cold stressed) mice was remarkably decreased in comparison to normal mice 5 days after onset of loading SART stress, and maximal contraction in SART stress mice duodenum was about 37% of that in non-stressed mice. Pilocarpine and KCl responses were also considerably decreased, but BaCl2 response was much the same as in the controls. Thus, the contraction system of the muscle is apparently not damaged by SART stress. Though body weights decreased, the daily intake of food incressed in SART stressed mice. Length of small intestine from SART stressed mice was much the same as in controls, but wet weights of small intestines were larger than in controls. Autonomic agonists, antagonists, tranquilizers and other drugs were given intraperitoneally to mice once daily during SART stress, and the ACh responses in the isolated duodenum were investigated. Pretreatment with adrenergic and anticholinergic drugs inhibited the decrease of ACh response, but antiadrenergic and cholinergic drugs had no effects. Pretreatment with tranquilizers such as reserpine, chlorpromazine, carpipramine and imipramine inhibited the decrease of ACh response in the isolated duodenum, but diazepam, meprobamate and benadryl had no influence. Pretreatment of neurotropin, a neurosedative had good inhibitory effects. Our results suggest that SART stressed mice may be in a state of unbalance regarding sympathetic and parasympathetic nerves, particularly with regard to abnormal tension in the parasympathetic nervous system, in part of duodenum. Pretreatment with most of the above drugs had no influence on loss of body weight in SART stressed mice while pretreatment with neurotropin inhibited body weight to a considerable extent.

Acetylcholine↗
PubMed1982

Effect of doxapram on the action of other drugs and the hepatic drug-metabolizing system in mice.

Effects of doxapram, a respiratory stimulant, on the action of other drugs and the activity of the hepatic drug-metabolizing enzyme were studied in mice. The hypothermic effect induced by aminopyrine and the muscle relaxant effect induced by meprobamate were potentiated by the pretreatment with doxapram 60 min before. Furthermore, doxapram significantly enhanced the lethalities of picrotoxin and strychnine and the analgesic actions of aminopyrine and morphine. The plasma concentration of aminopyrine or pentobarbital in doxapram-treated mice was higher than those in untreated mice, and the plasma concentration of normustard related to an active metabolite of cyclophosphamide after the administration of cyclophosphamide was lower in doxapram-treated mice. On the other hand, doxapram (50 mg/kg, i.p.) reduced remarkably the activities of aminopyrine N-demethylase and aniline hydroxylase in the hepatic 9,000xg supernatant fraction, and also reduced the cytochrome P-450 contents in hepatic microsomes. However, no significant alteration by doxapram was observed on the activities of NADH-ferricyanide reductase and NADPH-cytochrome c reductase and cytochrome b5 contents. It seems likely that the mechanisms of the interaction between doxapram and combined drugs involved the depression of the hepatic drug-metabolizing system in microsomes and a subsequent variation of drug level in the plasma.

Aminopyrine↗
PubMed1983

Cross-physical dependence liability of psychotropic drugs in rats dependent on barbiturates.

Rats were rendered physically dependent on phenobarbital by phenobarbital-admixed foods. Barbital, phenobarbital, ethanol, diazepam, nitrazepam, meprobamate, methaqualone, chlorpromazine, diphenylhydantoin, mephenesin, reserpine and clonidine were cross-administered to evaluate the mode of suppression of withdrawal signs and cross-physical dependence liability. The drugs were administered several times during the period from 17-18 hr (when withdrawal signs began to appear) to about 48 hr after the withdrawal of phenobarbital. From the mode of suppression and severity of relapsed withdrawal signs, these drugs were classified into the following 3 types: Type 1: drugs suppressing withdrawal signs of phenobarbital (WSP) almost completely and followed by the relapse of severe WSP. Type II-a: drugs suppressing WSP partially and followed by the relapse of moderate WSP. Type II-b: drugs suppressing WSP partially and followed by the relapse of only mild or practically no signs. Type III (III-a and -b): drugs practically failing to suppress or rather aggravate WSP. Consequently, we found that it was possible to evaluate precisely the cross-physical dependence on sedative-hypnotics by means of investigation for the method of suppression of WSP and the relapse of such signs upon their withdrawal.

Animals↗
PubMed1989

Behavioral analysis of zopiclone on the basis of their discriminative stimulus properties in the rat.

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.

Animals↗
PubMed2004

Carisoprodol withdrawal syndrome.

A 43-year-old man with chronic back and shoulder pain was treated with hydrocodone. He began taking excessive amounts of the drug, so his physicians stopped prescribing it. The patient then obtained the muscle relaxant carisoprodol on his own from several sources. He was consuming up to 30 or more tablets/day (> or =10,500 mg/day) for several weeks, then abruptly stopped taking the drug. Within 48 hours he developed anxiety, tremors, muscle twitching, insomnia, auditory and visual hallucinations, and bizarre behavior. The symptoms intensified and peaked on the fourth day after carisoprodol cessation. The patient required brief treatment with olanzapine and tapering dosages of lorazepam while the symptoms gradually resolved. To our knowledge, this is the first documented case of a withdrawal syndrome with carisoprodol. The symptoms most likely resulted because of accumulation of meprobamate, the active metabolite of carisoprodol in humans. Clinicians prescribing carisoprodol should be aware of the possibility for abuse or addiction. Further, we recommend that carisoprodol be designated a controlled substance at the federal level.

Adult↗
PubMed1964

ADJUSTING FIXED-RATIO SCHEDULES IN THE SQUIRREL MONKEY.

On an adjusting schedule of reinforcement, a parameter of the schedule is varied as a function of some characteristic of the animal's performance. In Experiment I, the fixed-ratio response requirement was varied as a function of the time that elapsed before the animal started responding in each fixed-ratio (initial pause). When initial pauses were shorter than a specified duration, the response requirement was increased; when they were longer than the specified duration, the response requirement was decreased. Specified durations of 1, 2, 4, 8, and 15 min were studied. The average response requirement maintained by each monkey was directly related to the length of the specified duration of initial pause. In Experiment II, the fixed-ratio response requirement was constant, but reinforcement occurred only when the initial pause was longer than a specified duration. The average durations of initial pauses were directly related to the length of the specified duration and to the response requirement. Meprobamate consistently decreased the average durations of initial pauses.

Adaptation, Psychological↗
PubMedDate not supplied

Tiapride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in geriatric agitation.

Tiapride is a substituted benzamide derivative with selective dopamine D2-receptor antagonist properties which appears to have preferential affinity for extrastriatal dopamine receptors. Animal and clinical studies show that tiapride has anxiolytic properties but the mechanism of action is uncertain. Results from limited studies indicate that the clinical efficacy of tiapride in the treatment of agitation, aggressiveness, anxiety and sleep disorders in the elderly appears superior to that of placebo, chlorpromazine, lorazepam and meprobamate. Tiapride also exerts a beneficial effect on vigilance and alertness in elderly patients and causes less sedation than chlorpromazine. Tiapride is well tolerated at the dosages recommended for elderly patients. Further well designed comparative studies with newer drugs are needed to determine the relative place of tiapride in the treatment of geriatric agitation, and such studies should also address the quality-of-life benefits for the patient. Additional clinical experience to determine the efficacy of tiapride in elderly patients with more than one disease condition, receiving concomitant medications, and/or with renal impairment is also required. However, despite these current limitations, tiapride may have potentially important applications in this difficult area of clinical medicine.

Aged↗
PubMed1989

Recent developments in the study of the effects of cigarette smoking on clinical pharmacokinetics and clinical pharmacodynamics.

With the ever-increasing population of cigarette smokers, the potential for cigarette smoke to affect drug therapy both pharmacokinetically and pharmacodynamically is significant. The overriding pharmacokinetic effect is increased drug metabolism through the induction of liver enzymes. The constituents of tobacco smoke, primarily nicotine, have their own pharmacological effects which may potentiate or antagonise the desired pharmacological effect of a particular drug, thereby affecting its efficacy. Furthermore, end-organ responsiveness may also be altered by tobacco. These latter 2 aspects constitute altered clinical pharmacodynamics. Approximately 30 drugs have been evaluated in terms of cigarette smoking. Induction of liver enzymes has been shown to increase the metabolism of imipramine, meprobamate, oestrogens, pentazocine, phenylbutazone, theophylline and warfarin. Nicotine has been shown to inhibit diuresis, alter ulcer healing, impair subcutaneous absorption, affect protein binding and stimulate catecholamine release; these effects have been evaluated in terms of therapy with frusemide (furosemide), histamine H2-antagonists, insulin, lignocaine (lidocaine) and beta-blockers, respectively. The interactions have not been correlated with clinical significance in all cases. Diminished end-organ responsiveness may account for reduced drowsiness in smokers receiving chlorpromazine and benzodiazepines, compared with non-smokers. Smoking has been associated with diminished pain tolerance, requiring increased dosages of morphine, pethidine (meperidine) and propoxyphene. Enzyme-inducers such as carbamazepine, phenytoin and phenobarbitone appear to be minimally affected by cigarette smoke, perhaps because hepatic enzymes are already maximally stimulated. Codeine, corticosteroids and nortriptyline do not appear to be affected by cigarette smoke. The bioavailability of glutethimide is higher in smokers, but this has not been associated with greater efficacy. The effect of smoking on paracetamol (acetaminophen) has been variable, depending on the extent of smoking, and does not appear to be of clinical significance.

Animals↗
PubMed1981

Biological evaluation of hemoperfusion in acute poisoning.

The efficiency of hemoperfusion in acute poisoning cannot be clinically estimated, because: (a) concomittant intestinal absorption, hepatic metabolism, and urinary excretion must be taken into account. (b) With supportive treatment alone, spontaneous recovery usually occurs in 98% of the intoxications in Intensive Care Units. The efficiency of hemoperfusion can only be estimated biologically. Measuring the blood level at the beginning and the end of hemoperfusion as well as measuring the clearances of the drug is misleading. A better method is to measure the amount of extracted drug, either indirectly by calculation (from hourly differences of arterio-venous measures of drug concentration multiplied by the blood flow) or directly by elution of the cartridge. In a practical way, if the blood level of drug is readily available after the patient is hospitalized, the optimum efficiency of hemoperfusion can be estimated beforehand, so that the decision to carry out the hemoperfusion can be maintained, postponed, or abandoned. For the most part, the experience of toxicologists has shown hemoperfusion to be ineffective for drugs with weak extracellular distribution (such as Digoxine, tricyclic drugs, heavy metals, Colchicine). Its effectiveness for certain drugs with poor in-vitro dialysance (such as Paracetamol) or with a small percentage of intestinal absorption (such as Paraquat) is still debatable. In the case of intoxications by hypnotic drugs, one hemoperfusion allows an average of 4-12% of the ingested medium and short barbiturates, and 7-17% of the ingested Meprobamate. Whether these results can be judged satisfactory, life-saving, or insignificant is largely a matter of personal standards.

Acute Disease↗
PubMed1978

Carisoprodol dependence: a case report.

Although known to have central nervous system effects comparable to those of meprobamate, carisoprodol has not previously been reported to be a dependence-producing drug. This case report is of a woman, previously addicted to other drugs, who became dependent on carisoprodol.

Adult↗
PubMed1982

Publication trends in the drug dependence literature.

Publications dealing with psychotropic drug use and dependence were analyzed for the years 1960-1980 using the numbers of articles cited in each yearly edition of Cumulated Index Medicus. The following headings were reviewed: drug abuse, drug dependence, alcoholism, smoking, heroin addiction, cannabis, cannabinoids, cocaine, phencyclidine, lysergic acid diethylamide, diazepam, and meprobamate. The number of citations for a given year was used to calculate the percentage of the literature for that year which fell under each of those headings. In general, it appears that the growth of the scientific literature included under many of these headings has been more rapid than the overall growth of the literature.

Humans↗
PubMed1998

Carisoprodol-induced myoclonic encephalopathy.

CASE REPORT: A 39-year-old man ingested 35 g carisoprodol. He developed agitation, tachycardia, myoclonus, and coma. The blood carisoprodol was 71 micrograms/mL; the meprobamate was 26 micrograms/mL. DISCUSSION: Carisoprodol overdose is thought to induce simple central nervous system depression. This case demonstrates a severe overdose with symptoms more consistent with myoclonic encephalopathy. A review of cases presenting to the San Francisco Division of the California Poison Control System during 1997 suggests that carisoprodol is more commonly associated with agitation and bizarre movement disorders than the current literature suggests. The pharmacology and potential mechanisms of toxicity are discussed. CONCLUSION: Agitation, hypertonia, and a myoclonic encephalopathy may be seen with significant carisoprodol intoxication.

Adult↗
PubMed1999

Fatal ingestion of sodium hypochlorite bleach with associated hypernatremia and hyperchloremic metabolic acidosis.

Ingestion of sodium hypochlorite bleach is usually benign, leading most poison centers to advocate conservative, home management. We report a rare, fatal case of household bleach ingestion. A 66-y-old female ingested an unknown quantity of regular CLOROX bleach (5.25% sodium hypochlorite, pH = 11.4). Upon discovery, she was vomiting spontaneously, and had slurred speech and oral mucosal discoloration. On hospital arrival the patient became unresponsive with shallow respirations. Laboratory studies revealed hypernatremia (169 mEq Na/L), hyperchloremia (143 mEq Cl/L), and metabolic acidosis (5 mmol total CO2/L). Radiographic evaluation showed bilateral pneumothoraces and pneumoperitoneum. The patient was intubated and ventilated, hypotension was treated with fluid resuscitation, and metabolic acidosis corrected with sodium bicarbonate. Naloxone and flumazenil were given without effect, and thoracostomy tubes were placed. Rapid deterioration of vital signs and mental status ensued, with cardiorespiratory arrest from which she was resuscitated. A second cardiac arrest resulted in death. Autopsy revealed esophageal and gastric mucosal erosions, perforation at the gastroesophageal junction, and extensive necrosis of adjacent soft tissue. Stomach contents contained sodium hypochlorite, and pleural and peritoneal fluid had the aroma of bleach. Postmortem vitreous humor Na was 187 mEq/L and Cl was 169 mEq/L. Toxicologic analysis revealed meprobamate metabolites in the urine, and lidocaine in the blood. The literature regarding fatal bleach ingestion is reviewed.

Acidosis↗
PubMed2000

[Centrally acting muscle relaxants and traffic hazards].

BACKGROUND: An increasing number of the centrally acting muscle relaxants were withdrawn from the Norwegian market during the 1988-98 period. The only drug in this group now marketed in Norway is carisoprodol. The National Institute of Forensic Toxicology in Norway analyses all blood samples from suspected drugged drivers. In later years there has been a marked increase in the number of blood samples testing positive for carisoprodol or meprobamate (the major metabolite). MATERIAL AND METHODS: 480 cases testing positive for central muscle relaxants in the years 1984-1998 were further studied. RESULTS: Compared with blood samples positive primarily for benzodiazepines, there were more women in the group (39% vs. 15%), and fewer drugs and less alcohol were detected. INTERPRETATION: The positive samples may indicate misuse or abuse due to the fact that high drug concentrations and concomitant use of benzodiazepines were frequent. This knowledge should have implications for doctors prescribing centrally acting muscle relaxants.

Accidents, Traffic↗
PubMed1975

Pharmacological actions of some simple analogues of reserpine. I. Analgesic effects.

In view of the fact that reserpine treatment lowers pain threshold, structural analogues of reserpine molecule were tested against thermal and visceral pain. Some compounds belonging to piperidino- and morpholino derivatives of acetanilide showed promising analgesic activity. These compounds in earlier studies had shown tranquillizing effect. Combination studies with meperidene, phenylbutazone, phenazone and meprobamate did not significantly change the analgesic activity in thermal methods but the test-compounds were potentiated by phenylbutazone and phenazone in writhing test.

Acetates↗
PubMed2002

[Acute toxicological cases during a ten-year period in our clinic].

INTRODUCTION: There's a fact, that Hungary has held the first places in suicidal statstics. METHODS: The authors studied toxicological cases between 1989 and 1998 at the 1st Department of Medicine of the Medical and Health Science Centre, at the University of Debrecen, paying special attention to suicidal poisoning cases. RESULTS: 2% of the patient turnover accounted for acute poisoning cases, the number of which increased during the 10 years in question. 70% of the cases were of suicidal intentions, 20% were unintentional, these poisonings were not committed on purpose, while the proportion of iatrogenic intoxication cases was 10%. Amongst the failed suicide cases there was a higher proportion of women, whereas a higher percentage of men accounted for "successful" suicide cases. When examining auto-intoxication cases it turned out that the medicine most frequently used was meprobamate, besides benzodiazepines. Mortality rate was highest in the glutethimide intoxication cases. Most poisonings with suicidal intentions took place in the 2nd quarter of the year. Most completed suicides were committed on Wednesdays and Thursdays. 81% of the iatrogenic intoxication cases happened to be with digitalis and coumarin overdose. Nearly 50% of the cases turned out to be combined intoxications. 40% of the men took alcoholic drinks during the auto-intoxications. In the case of 135 patients extracorporeal detoxification therapy was applied, which consisted mostly of hemoperfusion. Three quarters of the patients needed psychiatric care and every fourth patient was admitted to the Department of Psychiatry. 6.9% of the poisonings were fatal. CONCLUSIONS: The growing number of toxicological cases--amongst these suicidal poisonings--compels us to pay more attention to the setting up of interdisciplinary based prevention as well as running effective toxicological centres. All physicians have a responsibility to recommend psychiatric care for people suffering from mental problems or depression and for the unsuccessful or potential suicide seeking help for the first time. Family doctors in primary medical care and who meet patients first have an important role in this job.

Adolescent↗
PubMed2003

Somatic dysfunction during carisoprodol cessation: evidence for a carisoprodol withdrawal syndrome.

Carisoprodol is a commonly used skeletal muscle relaxant with potential for abuse because of its active metabolite, meprobamate, and several reports have suggested that patients abruptly stopping intake of carisoprodol may have a withdrawal syndrome. The authors studied changes in the occurrence of somatic dysfunctions in five patients during an 8-day period following discontinuation from large doses of carisoprodol. Results showed that the number of somatic dysfunctions changed significantly during the withdrawal period. Each patient had an increase in the number of somatic dysfunctions during the first 3 days after cessation of carisoprodol with return to at or near baseline by the eighth day. This was reflected statistically in a significant-within-subjects effect for time. Results of supplemental analyses revealed a significant component of the effect and a trend for the quadratic component to be significant. Increases in the number of somatic dysfunctions during carisoprodol discontinuation support the existence of a carisoprodol withdrawal syndrome.

Adult↗