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PubMed1979

Discriminative stimulus properties of pentylenetetrazol and bemegride: some generalization and antagonism tests.

In an operant procedure of lever pressing on a FR 10 schedule of food reinforcement, male hooded rats were trained to respond with a lever on one side of a food cup following a drug injection, and to respond with a lever on the alternate side following a 1 ml/kg saline injection. All of 14 subjects learned to discriminate reliably between the effects of 20 mg/kg pentylenetetrazol (PTZ) and saline. Seven of eight rats learned to discriminate between the effects of bemegride (5 mg/kg) and saline. None of 14 rats learned to discriminate between 5mg/kg PTZ and saline. The bemegride discriminative stimulus generalized to PTZ (20mg/kg) and was antagonized by chlordiazepoxide (10 mg/kg). Chlordiazepoxide, diazepam, flurazepam, clobazam, and meprobamate were all effective antagonist of PTZ in a dose-dependent manner. Bemegride and cocaine generalized to the PTZ discriminative stimulus in a dose-dependent manner, but d-amphetamine, methylphenidate, and nicotine did not. Since bemegride and PTZ are convulsants at higher doses, the discriminative stimulus properties of these drugs might be based on a subtle convulsive brain state. The anxiolytic properties of benzodiazepines and meprobamate suggest that the discriminative stimulus produced by these convulsants is related to an "anxiety-inducing" action.

Animals↗
PubMed1978

The action of CNS drugs on an isolated sympathetic nerve preparation of rabbit.

The effect of some centrally active drugs on the transmission of nerve impulses through the isolated cervical sympathetic nerve and superior cervical ganglion of the rabbit has been studied by recording both preganglionic and ganglionic responses to single square wave stimuli. Chlorpromazine, trifluoperazine and haloperidol have a greater axonal depressant action than the known local anaesthetics procaine and xylocaine. Chlordiazepoxide and diazepam are similar in local anaesthetic potency to procaine while meprobamate and sodium pentobarbitone possess only slight axonal depressant properties. Meprobamate, sodium pentobarbitone and possibly diazepam have ganglion blocking properties while procaine, chlorpromazine, trifluoperazine, haloperidol and chlordiazepoxide reduce the ganglion potential by virtue of their preganglionic action.

Action Potentials↗
PubMed1988

Conditioned defensive burying as a model for identifying anxiolytics.

Rats exposed to a presumably aversive stimulus such as electric shock respond by heaping litter on the source, a behavior known as conditioned defensive burying (CDB). Because some anxiolytics suppress this behavior, CDB has been proposed as a screening method for anxiolytics. We tested the effects of the conventional anxiolytics chlordiazepoxide (4-32 mg/kg) and meprobamate (75-125 mg/kg), the novel anxiolytic buspirone (8-64 mg/kg), the antidepressant imipramine (4-16 mg/kg), the opiate analgesic morphine (2-8 mg/kg), and the antipsychotic chlorpromazine (1-16 mg/kg) on CDB. Chlordiazepoxide, meprobamate, imipramine, and morphine significantly suppressed CDB, but chlordiazepoxide did so only at a dose that reduced general activity. Buspirone and chlorpromazine did not suppress CDB at doses that reduced activity. There were some methodological differences from previous studies. We conclude that the test as constituted in this study lacks drug-class specificity. The necessity of distinguishing between specific reduction of burying and general reduction of activity is emphasized.

Animals↗
PubMed1997

Patterns of analgesic prescribing in a South African primary care setting.

The primary aim of this study was to assess patterns of prescribing of analgesic medications in a primary care setting in South Africa. Medication records of 47,103 patients for the year 1995 were retrospectively reviewed. Analgesic agents represented 12.3% of the total number and 14.2% of the total cost of all the products prescribed. Analgesic products were prescribed to nearly three times as many females as males. Most analgesic prescriptions were for non-opioid analgesics (93.8%). More than half (56.8%) of all the prescriptions for analgesics were available without a prescription from a medical practitioner. Analgesic prescription diminished as age increased. The high prescribing rate of analgesics to children younger than 10 years was a cause for concern. Furthermore, meprobamate-containing analgesics accounted for 12.2% of central nervous system drugs and 28.1% of the non-opioid analgesics that were prescribed. This finding was also a cause for concern due to the dependence-producing properties of meprobamate. It was concluded that the pharmacist has an important role to fulfil in the counselling of patients with respect to the use of analgesic products.

Adolescent↗
PubMed2005

Carisoprodol intoxications and serotonergic features.

The symptoms and signs of carisoprodol intoxications do not resemble those caused by its metabolite meprobamate. Meprobamate most probably produces its effects through the GABAergic neurotransmitter system. The signs and symptoms of carisoprodol intoxications, however, are not easily explained by interaction with this neurotransmitter system. In the present study, four cases of carisoprodol intoxications are presented with emphasis on the presence of serotonergic signs and symptoms. All four cases fulfilled three different sets of criteria for the diagnosis of serotonin syndrome. These findings could indicate that an increased serotonin level in the central nervous system could explain some of the symptoms and signs of carisoprodol intoxications. This may have implications for the clinical evaluation and treatment of such intoxications. Since few laboratories routinely screen for carisoprodol it is important to keep this drug in mind when encountering intoxications displaying serotonergic symptoms.

Adult↗
PubMed1980

Avoidance enhancement and discriminative response control by anxiolytics with drugs acting on the GABA system.

Two types of conditioned behaviors were investigated for the purpose of evaluating anxiolytic drugs. A conditioning procedure used was an active avoidance in poorly-performing mice. Chlordiazepoxide, diazepam, chlorazepate and meprobamate increased the avoidance rate, while chlorpromazine, haloperidol and nortriptyline did not produce such an effect. The effect of diazepam was potentiated by gamma-aminobutyric acid (GABA) and aminoxyacetic acid (AOAA) and antagonized by picrotoxin and thiosemicarbazide, but was influenced little by spiroperidol, alpha-methyltyrosine, phenoxybenzamine and levallorphan. In addition, the effect of other anxiolytics was potentiated by AOAA and antagonized by picrotoxin. Biperiden, methamphetamine, caffeine and morphine also induced an avoidance enhancement, which was not influenced by AOAA. A drug discrimination experiment was also performed using a milk-reinforced two-lever operant method. In the rats trained to discriminate phenobarbital from saline, diazepam produced a dose-related phenobarbital-lever selection, which was potentiated by AOAA and antagonized by picrotoxin. Chlordiazepoxide, chlorazepate and meprobamate also elicited responses on the phenobarbital-lever. On the other hand, haloperidol, nortriptyline, biperiden, methamphetamine, caffeine and morphine produced a saline-lever selection, at the doses tested. These results suggest that, among several drugs tested, the avoidance enhancement and discriminative response control by anxiolytics may be closely linked with the GABA system.

Aminooxyacetic Acid↗
PubMed1999

Carisoprodol (soma): abuse potential and physician unawareness.

Carisoprodol is a noncontrolled skeletal muscle relaxant whose active metabolite is meprobamate, a Schedule IV controlled substance. Although several case reports have shown that carisoprodol has abuse potential, it continues to be widely prescribed. The usage patterns of 40 patients who had taken carisoprodol for three or more months (20 of whom had no history of substance abuse and 20 of whom carried a diagnosis of substance abuse or dependence) were reviewed and compared and a survey was conducted to assess physician awareness of the abuse potential of the drug. Findings showed that some patients using carisoprodol for over three months may abuse the medication, especially those individuals with a history of substance abuse. A significant percentage of the physician population is unaware of the potential of carisoprodol for abuse and of its metabolism to meprobamate, a controlled substance. Physicians should exercise caution when prescribing carisoprodol, especially if the patient has a history of substance abuse.

Adult↗
PubMed1997

Carisoprodol: a drug of continuing abuse.

Carisoprodol (Soma) is a noncontrolled, skeletal-muscle relaxant whose active metabolite is meprobamate. Despite previous indications that the drug may be abused, it continues to be widely prescribed for musculoskeletal conditions involving muscle spasm. Presented here are three cases demonstrating patterns of carisoprodol abuse not previously reported. Carisoprodol usage should be limited to short-term treatment. Patients for whom carisoprodol is prescribed are at risk for meprobamate dependence.

Adult↗
PubMed1991

Discriminative stimulus effects of the novel anxiolytic buspirone.

Separate groups of Long-Evans rats were trained to discriminate either 0.56 or 1.0mg/kg buspirone i.p. in a two-lever, drug vs no-drug discrimination procedure. Training took twice as long for the lower versus the higher training-dose group. Generalization tests were conducted with buspirone (0.1-1.8mg/kg, i.p., 0.32-10mg/kg, p.o.), pentylenetetrazole (1-18mg/kg, i.p.), meprobamate (3.2-180mg/kg, p.o.), haloperidol (0.01-0.32mg/kg, i.p.), and 8-OH-DPAT (0.01-0.32mg/kg, i.p.). Buspirone p.o. was 0.5-1.0 log(10) units less potent than buspirone i.p. in producing dose-dependent generalization (i.e. > 80% buspirone-lever responding). Dose-effect functions for the 1.0 training-dose group were to the right of those for the 0.56 group. Partial generalization to meprobamate occurred in both groups, representing the first report of overlap of the buspirone discriminative stimulus with that of another anxiolytic. Complete generalization to 8-OH-DPAT occurred, consistent with buspirone's prominent 5HT(1A)-receptor activity and replicating findings in the pigeon. Partial generalization to haloperidol was concluded: every rat generalized to haloperidol, but the gradients did not increase monotonically and drug-lever responding at a given dose was inconsistent within and across rats. The haloperidol results suggest a stronger influence of the dopaminergic component in the buspirone discriminative stimulus in rats than was found with pigeons. Although a previous study found generalization to buspirone from pentylenetetrazole in baboons, there was no generalization to pentylenetetrazole from buspirone in the present study.

Journal Article↗
PubMed1976

[The effect of neurotropic substances on the self-stimulation reaction at the thalamic level].

The effect of d-amphetamine, cocaine, caffeine, morphine, imipramine, phenobarbital, LSD-25, benactyzine, meprobamate, diazepam, chloridiazepoxide on the lateral hypothalamic self-stimulation of rats was investigated. D-amphetamine, cocaine, caffeine, morphine, imipramine decreased the threshold of selfstimulation. Meprobamate, diazepam, chlordiazepoxide failed to influence this index, but increase the intensity of self-stimulation during the threshold, the optimum and more than the optimum cirrent intensity. Benactyzine, LSD-25, phenobarbital decreased the threshold and increased the frequency of self-stimulation during all the current intensities. A comparative study of the above results showed the agents of the first group to exert a direct stimulating action on the positive reinforcement system. Tranquillizers activated this system due to their depressive action on the negative reinforcement system. Benactyzine, LSD-25, phenobarbital activated the system and depressed the system of negative reinforcement.

Animals↗
PubMedDate not supplied

[Effect of various neurotropic drugs on chronic hyperreflexia in rats after cordotomy].

Substances modulating calcium permeability of cell membrane (verapamil imidazol, 4-aminopyridine), decreasing motor activity (meprobamate) and blocking adrenoreceptors (clophelin, propranolol, droperidol, aminazine++ have been studied for their action on the monosynaptic discharge of the ventral roots (MD VR) reinforced due to chronic cutting of the spinal cord. It is found that verapamil and meprobamate depress more strongly MD VR of rats with chronic cutting of the spinal cord than of those with the acute one. Imidazol and 4-aminopyridine reinforcing MD VR of rats with acute cutting of the spinal cord have no influence on the analogous index of rats with chronic cutting of the spinal cord. Adrenoblockers do not change the amplitude of MD VR in both groups of the animals.

Adrenergic beta-Antagonists↗
PubMed1992

The treatment of sleep disorders.

Narcolepsy is clinically associated with cataplexy, sleep paralysis and hypnagogic hallucinations. It is treated by reassurance (that there is no physical disease) and by stimulants such as ephedrine and amphetamine on an intermittent basis. The special tricyclic antidepressant clomipramine is also used, and mono-amine oxidase inhibitors (MAOIs) are useful in theory. Obstructive sleep apnoea is an important and often unrecognised cause of daytime somnolence. It is treated by weight reduction (pickwickian syndrome), hormones, or recently, with continuous positive pressure apparatus. Night terrors (pavor nocturnus) and sleepwalking typically occur during deep sleep (stage 3 and 4 throughout the episode) in children. In a night terror the child sits up with a scream, with eyes open, but inaccessible. He eventually falls asleep calmly. Sleepwalking, too, shows the features of inaccessibility and subsequent amnesia for the episode. Both conditions are normally treated with reassurance (to the parents) but may occasionally warrant benzodiazepines. Enuresis usually occurs in non-rapid eye movement (NREM) sleep, especially stages 3 and 4. The reason for the efficacy of tricyclic antidepressants is not precisely known. Delirium tremens (DT) is treated as a rebound excess of REM sleep, with benzodiazepines and other drugs. It is the withdrawal syndrome (with or without major seizures) to the barbiturate-alcohol group of drugs, which includes alcohol, chloral, paraldehyde, glutethimide, methylprylone, ethchlorvynol, meprobamate and meprobamate-diphenhydramine. Insomnia may be treated by the above drugs, by analgesics, antidepressants, major tranquillisers (neuroleptics) and miscellaneous other compounds. For the majority of patients, however, the most suitable group seems to be the benzodiazepines. The benzodiazepines are much safer than their predecessors, in both acute and chronic usage.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1985

Behavioral effects of nonbenzodiazepine anxiolytic drugs: a comparison of CGS 9896 and zopiclone with chlordiazepoxide.

Zopiclone and CGS 9896 are two nonbenzodiazepine compounds which have been shown to displace benzodiazepines from their binding sites. The present study compared the behavioral effects of these two compounds in rats with those of chlordiazepoxide. The three drugs produced dose-related increases in punished drinking as did pentobarbital and meprobamate but not PK 9084, which also acts at benzodiazepine binding sites, or buspirone. Rates of lever pressing suppressed by punishment were also increased by chlordiazepoxide and zopiclone. CGS 9896 exerted a similar although less marked effect. Lever pressing maintained by a differential reinforcement of low rate 18-sec schedule of milk presentation was increased by low doses of chlordiazepoxide and zopiclone and decreased by higher doses leading to dose-related reductions in numbers of reinforcers obtained. CGS 9896 also reduced number of reinforcers but without affecting rate of responding. In rats trained to discriminate a dose of chlordiazepoxide from saline, chlordiazepoxide, zopiclone, pentobarbital and meprobamate produced chlordiazepoxide-appropriate responding. CGS 9896 also produced chlordiazepoxide-appropriate responding at a wide range of doses although the stimulus properties of this compound appeared to be weaker than those of the other active drugs. Chlordiazepoxide and zopiclone produced dose-related increases in food intake in food-deprived rats. CGS 9896 had similar effects at low doses but its effects were less consistent at higher doses. Thus, zopiclone has a behavioral profile very similar to that of chlordiazepoxide. Although many of the effects of CGS 9896 were similar to those of chlordiazepoxide, a number of differences were also observed.

Animals↗
PubMed1977

Some aspects of the neuropharmacology of phenylurea.

The neuropharmacology of phenylurea was studied. The compound is a potent sedative hypnotic agent with a fairly good margin of safety. It produced significant motor incoordination and behavioral changes in sub-sedative doses, thus suggesting that it acts on the areas of the brain which control motor coordination (neurological deficit) and spontaneous motor movements (awareness of environment). The activity pattern of phenylurea as measured on the rotarod treadmill was identical with that of an ataractic drug, meprobamate, and different from that of the sedative drug, 2-ethylcrotonylurea (ectylurea). It exhibited significant meprobamate-like antistrychnine (myorelaxant) activity, and at high doses only, anticonvulsant activity (pentetrazole antagonism). Phenylurea also protected mice against tremorine-induced tremors. A sub-sedative dose of phenylurea significantly prolonged pentobarbital sleeping time.

Animals↗
PubMed1981

[Midazolam in preoperative sleep].

In order to determine the hypnotic effects of midazolam administered per os, the drug was compared with meprobamate and a placebo in patients about to undergo surgery. The study involved 83 patients, 57 female and 26 male: 67 cases of maxillofacial surgery and 16 cases of gynaecological surgery. The study was carried out using the technique of comparison in parallel series of single doses of midazolam (15 mg) with meprobamate (250 mg) and a placebo according to the double placebo technique. The patients were aged between 18 and 60 years, male and female, and were included without any particular attention being paid to sufferers from sleep disturbances or not. The variables selected for the study were 29 in number concerning the assessment of the patient of sleep and awakening, surveillance of the time taken to fall asleep, the duration and quality of sleep and the state after awakening.

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↗
PubMed1996

An investigation into the prescribing of analgesics.

OBJECTIVE: To investigate the prescribing of analgesic agents in a defined South African patient population. DESIGN: Retrospective drug utilisation study. SETTING: Prescribing behaviour of a sample of 50 dispensing doctors in Port Elizabeth. Data were obtained from a medical aid which used a formulary system. MAIN OUTCOME MEASURES: Percentage of central nervous system drugs that analgesics comprised; proportion of patients using combination analgesics; cost of analgesics. RESULTS: On average, 83.3% of all central nervous system drugs dispensed were analgesic agents. These agents represented 70.9% of the total cost of central nervous system drugs. A high percentage (82.2%) of the analgesic agents dispensed were combination or polycomponent analgesics. The combination analgesic tablet, consisting of paracetamol, meprobamate, caffeine and codeine phosphate, was the most frequently prescribed central nervous system drug. This product accounted on average for 40.4% of all analgesics dispensed. Nearly half (46.0%) of all the analgesics dispensed by the sample of doctors were available without a prescription. CONCLUSION: The high prescribing rate of combination analgesic prescription was a cause for concern, given the dependence-producing potential of some of the ingredients, e.g. meprobamate. The prescribing and use of analgesics should be carefully monitored by further drug utilisation studies in light of the serious adverse effects, such as analgesic nephropathy, associated with the longterm use of these agents.

Analgesics↗
PubMed1963

STRESS MODIFICATION OF DRUG RESPONSE.

Rats stressed by unilateral hind-leg ligation show a significantly decreased pharmacological response to the effects of hexobarbital, meprobamate, and pentobarbital. This effect is dependent upon an intact pituitaryadrenal axis, since it is absent in both hypophysectomized and adrenalectomized animals. It can be simulated by intravenous administration of adrenocorticotrophic hormone or corticosterone. The effect of stress on drug response is not noted with barbital, a compound which is not metabolized; this effect is inhibited by treatment of the animal with a drug metabolism inhibitor such as SKF 525-A (diethylaminoethyl 2,2-diphenylpentanoate). Compounds which can stimulate adrenocorticotrophic hormone secretion or act directly on the adrenals to produce corticosteroids should thus be able to stimulate their own metabolism or that of other drugs.

Adrenal Glands↗