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PubMed1991

Chlormethiazole: current status in the treatment of the acute ethanol withdrawal syndrome.

Comparative clinical studies of Chlormethiazole with a vast array of pharmacologically unrelated drugs like benzodiazepines, tiapride, bromocriptine, carbamazepine and phenothiazines over the years clearly established it as a useful, dependable and effective drug to treat patients with moderate to severe ethanol withdrawal syndrome, when used early in a flexible reducing regime tailed off over 7-10 days. It has been found to be highly effective in the treatment, and particularly in the prevention of DT's in high-risk patients, if given at an early stage. This paper critically reviews the important international clinical trial literature of various drugs currently used in the treatment of ethanol withdrawal syndrome, including DT's, it highlights the efficacy and superiority of Chlormethiazole over other drugs, and also discusses the probable mechanism of its actions in these conditions.

Alcohol Withdrawal Delirium↗
PubMed2000

Effect of starvation and chlormethiazole on cytochrome P450s of rat nasal mucosa.

Cytochrome P450 (CYP) enzymes of nasal tissue are relatively resistant to induction by classical inducers. In the present study, the effects of starvation on the expression of CYP1A, 2A, 2B, 2C, 2E, 2G, and 3A subfamilies in the nasal mucosa of rat were studied. Fasting for 72 hr caused an increase in 2E1-dependent p-nitrophenol hydroxylase and 1A-dependent ethoxy- (or methoxy) resorufin dealkylase activities, but did not affect either 2A-linked coumarin hydroxylase or the testosterone hydroxylase activity, the latter reaction being a marker of several CYPs including 2G1. Whereas increases in 2E1- and 1A- associated catalytic activities were accompanied by a concomitant increase in the corresponding apoproteins as determined by immunoblotting, immunoactive protein bands reactive with antibodies raised against rat 1A1, 2B1, 2C11, 3A1 or rabbit nasal 2A10/11 and 2G1 were not altered. Fasting also increased CYP2E1 and CYP1A2 on the mRNA level, but did not alter CYP1A1 mRNA as determined by hybridization with cDNA probes selective for these cytochromes. A reiterative administration of chlormethiazole, a specific inhibitor of 2E1 in liver, strongly inhibited many CYPs, including 2E1, 1A2, 2G1, and 2A in the nasal mucosa, but did not influence expression of 2B or 3A as determined by immunoblotting or catalytic activities. The chlormethiazole-mediated inhibition of 1A1 and 2E1 was demonstrated to be at the mRNA level. These results suggest that fasting induces the gene expression of 2E1 and 1A2 and that the mechanisms involved in the regulation of CYPs in the nasal mucosa are tissue-specific. The inducibility of the above-mentioned isoforms may have a significant role in the clearance of drugs and bioactivation of inhaled compounds.

Animals↗
PubMed1979

Dependence on chlormethiazole and effects of its withdrawal.

Five cases of physical dependence on chlormethiazole are reported. Because sudden withdrawal may precipitate an acute "organic psychosis", chlormethiazole should only be used in hospitals and, even then, only for a maximum of 9 days.

Acute Disease↗
PubMed2003

Diazepam and chlormethiazole attenuate the development of hyperthermia in an animal model of the serotonin syndrome.

The serotonin (5-HT) syndrome is the most serious toxic interaction of antidepressants, but no pharmacotherapy has yet been established. In the present study, we created an animal model of the 5-HT syndrome by intraperitoneally injecting rats with clorgyline (2 mg/kg) and 5-hydroxy-L-tryptophan (5-HTP) (100 mg/kg) and evaluated the effectiveness of potent 5-HT(2A) receptor antagonists and GABA-enhancing drugs, including diazepam and chlormethiazole. The rectal temperature of the rats was measured, and the noradrenaline (NA) and 5-HT levels in the anterior hypothalamus were measured by microdialysis. In the group pre-treated with saline, the rectal temperature increased to more than 40 degrees C, and all of the animals died within 90 min after administration. Pre-treatment with potent 5-HT(2A) receptor antagonists prevented the development of hyperthermia and death in the rats. Pre-treatment with diazepam, 10 and 20mg/kg, and chlormethiazole, 50 and 100mg/kg, attenuated the development of hyperthermia. Although neither of these drugs completely prevented the rats from dying, they prolonged their survival time. Regardless of the type of therapeutic agents, the concentration of 5-HT increased to about 1100-fold the pre-administration level. The NA levels in the saline group increased to about 16-fold the pre-administration levels, but the increase was significantly lower in the rats that survived as a result of drug therapy. These results suggest that GABA-mimetic drugs may be effective against the 5-HT syndrome, although they have a somewhat weaker effect than the potent 5-HT(2A) receptor blockers, and that not only is 5-HT activity increased in the brain in the 5-HT syndrome, but the NA system is also enhanced.

5-Hydroxytryptophan↗
PubMed1980

Simultaneous quantitation of chlormethiazole and two of its metabolites in blood and plasma by gas--liquid chromatography.

A simple and rapid gas chromatographic method for the quantitation of chlormethiazole and two of its pharmacologically active metabolites, 5-acetyl-4-methylthiazole and 5-(1-hydroxyethyl)-4-methylthiazole, in plasma and blood is described. The total analysis time is less than 20 min for a single sample. The method requires 50--500 microliter of plasma or 1 ml of blood. The compounds are detected with a nitrogen--phosphorus detector. An internal standard technique is used for the quantitation. Calibration data are linear over the range 32--2376 ng of chlormethiazole and a similar range of the metabolites in plasma. The method may be used for pharmacokinetic studies.

Adult↗
PubMed1987

Improved high-performance liquid chromatographic procedure for the determination of chlormethiazole levels following solid-phase extraction from plasma.

An improved high-performance liquid chromatographic method for the determination of chlormethiazole levels in plasma is described. The drug is extracted from plasma using commercially available reversed-phase extraction columns; recovery values obtained using Sep-Pak C18 and Bond Elut C1, C2, C4, C6, C8, C18 columns are compared. Separation was achieved by reversed-phase chromatography, using a mobile phase consisting of 0.025 M sodium acetate buffer, pH 4.5-acetonitrile (67:33) at a flow-rate of 1.6 ml/min in conjunction with a 15-cm Jones Chromatography Apex ODS column. The analytical column was protected by a Waters Assoc. Guard-Pak module containing a Guard-Pak CN insert. Using ultraviolet detection at 254 nm chlormethiazole levels in the region of 50 ng/ml can be measured with only 500 microliter of plasma.

Chlormethiazole↗
PubMed1980

Prolonged infusion of chlormethiazole in intensive care.

Chlormethiazole has proved useful for prolonged sedation in patients receiving artificial ventilation of the lungs during intensive care. In short-term infusions sedation and unconsciousness can be produced quickly and reversal is rapid on stopping the administration. After prolonged infusion, however, recovery is much slower because of accumulation of the drug. The pharmacokinetics of chlormethiazole in both short and prolonged infusions were studied in four patients. Following brief administrations the drug disappeared very quickly from the blood as a result of re-distribution and the patients wakened after a few minutes. Unconsciousness was associated with plasma concentrations in the range of 3--5 micrograms ml-1. After 48 h administration, recovery was much slower, the elimination half-life varying from 3.5 to 12.1 h.

Adolescent↗
PubMed1985

Cardiovascular effects of a chlormethiazole infusion in combination with extradural anaesthesia.

The cardiovascular effects of an infusion of chlormethiazole 30-40 ml min-1 were studied in six patients following an extradural injection of 2% lignocaine. There were small but statistically significant decreases in mean arterial pressure and left ventricular ejection time during the infusion. Increases in the pre-ejection period were noted, but there were no significant changes in cardiac output, stroke volume or heart rate. Patient acceptance was high. It is concluded that sedation with an infusion of chlormethiazole, during surgery carried out under extradural anaesthesia, has no clinically adverse cardiovascular effects.

Adult↗
PubMed1991

Basophil histamine release in atopic patients after in vitro provocation with thiopental, Diprivan and chlormethiazole.

The degree of histamine release induced by three different anesthetic drugs was studied in vitro using basophil leukocytes from atopic patients (n = 11) and controls (n = 14). In all, eight dilutions (1/2 to 10(-5)) of Diprivan and its solvent Intralipid, thiopental and chlormethiazole in aqueous solution, were used. Histamine was released in four controls with weak dilutions (1/2 to 10(-5)) of Diprivan (n = 2) and thiopental (n = 2). The reaction with thiopental was greater than that with Diprivan. Five of the atopic subjects released histamine with one or more drug: thiopental and Diprivan four times each, Intralipid twice, and chlormethiazole once. Histamine release was greater in these patients than in controls, and occurred with dilutions ranging from 1/2 to 10(-2), except for one case. It is concluded that atopic patients release histamine with hypnotic anesthetic drugs more easily than normal subjects. In the clinical setting, where blood concentration of the drugs studied is equivalent to a dilution of less than 10(-3), they do not release much histamine. They may be used in atopic patients if the drugs are injected slowly.

Basophils↗
PubMed1985

Chlormethiazole: an effective oral sedative for cranial CT scans in children.

Oral chlormethiazole was assessed as an alternative form of sedation for cranial computerized axial tomography in children aged 0-9 years. It was found to be highly effective with a rapid onset of action, brief period of action and no side effects. It was found to be preferable to intramuscular lytic cocktail, being particularly suitable for day cases. Chlormethiazole might lend itself to use in other non-painful procedures in childhood.

Administration, Oral↗
PubMed1986

Effect of chlormethiazole on the hepatic monooxygenase enzyme system.

Ethanol abuse has been shown to induce hepatic monooxygenase activity. In order to study the effect of chlormethiazole on the hepatic monooxygenase enzyme system, the O-deethylation of 7-ethoxycoumarin was studied. Chlormethiazole was found to inhibit ethanol-induced monooxygenase activity.

Adult↗
PubMed1986

Changes in psychophysiological and conditioning variables during chlormethiazole-medicated and unmedicated ethanol withdrawal: preliminary report.

Autonomic lability during ethanol withdrawal in chlormethiazole-medicated and unmedicated groups was investigated using electrodermal measures. Vulnerability to Pavlovian aversive conditioning was also assessed. Ethanol withdrawal was associated with increased autonomic arousal and aversive conditioning, suggesting an increased risk of phobia acquisition. Chlormethiazole administered during ethanol withdrawal may protect against such developments.

Adolescent↗
PubMed1986

Chlormethiazole as a sleep cover for regional anaesthesia.

Intravenous chlormethiazole has been used in conjunction with regional anaesthesia to induce sedation in several hundred patients. Advantages of using chlormethiazole include rapid induction and recovery. Disadvantages include nasal irritation.

Anesthesia, Conduction↗
PubMed1999

Apnea syndrome in a patient with Alzheimer dementia under chlormethiazole treatment: a clinical experience report.

Sleep apnea syndromes in conjunction with dementia have attracted considerable interest among geropsychiatrists in recent years. This clinical case report describes a demented and delirious elderly patient with a history of alcoholism who developed a sleep apnea syndrome under treatment with chlormethiazole. The risk of chlormethiazole treatment may be underestimated in vulnerable patients, e.g. those suffering from severe respiratory diseases or dementia. Alternative treatments for delirious states need to be evaluated instead.

Aged↗
PubMed1979

Chlormethiazole--no hangover effect but not an ideal hypnotic for the young.

The hangover effects of 768 mg chlormethiazole, an hypnotic with a half-life of approximately 4 hr, were compared with those of placebo in a double-blind cross-over study in 8 young subjects. Ten hours after dosing there were no differences between the preparations in the subjects' psychomotor performance, EEG sleep scores, or visual analogue ratings. Thus, an hypnotic which is rapidly removed from the body may confer considerable advantages. However, all 8 subjects had unpleasant nasal symptoms following chlormethiazole, and it is therefore not an ideal hypnotic for this age group.

Adult↗
PubMed1983

Chlormethiazole in the treatment of neonatal status epilepticus.

A pre-term neonate with status epilepticus resistant to conventional treatment but who responded to a chlormethiazole infusion is reported. Nineteen days of continuous infusion was required before treatment could be discontinued and oral phenytoin substituted. Chlormethiazole should be considered in the treatment of resistant convulsions in the newborn.

Chlormethiazole↗
PubMed1983

Comparison of chlormethiazole (Heminevrin) and chlordiazepoxide (Librium) in the treatment of acute alcohol withdrawal.

This study was carried out to compare the efficacy of chlormethiazole and chlordiazepoxide in the treatment of acute alcohol withdrawal syndrome in 40 patients. Repeated biochemical, clinical, and psychophysiological measurements were obtained in a randomized, double-blind design in which one group of patients received chlormethiazole and a second group received chlordiazepoxide over a period of 7 days. Analysis indicated both drugs to be of equivalent potency and were equally well tolerated by patients. The more severe aspects of withdrawal were brought under control within the first 4 days of treatment. However, even at 7 days, there still persisted some symptoms attributable to the withdrawal from alcohol.

Adult↗