Sedative-hypnotic drugs ethanol

Buspirone causes less psychomotor impairment than benzodiazepines and does not affect driving skills. The drug does not potentiate effects of conventional sedative-hypnotic drugs, ethanol, or tricyclic antidepressants, and elderly patients do not appear to be more sensitive to its actions. Nonspecific chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, gastrointestinal distress, and paresthesias and a dose-dependent pupillary constriction may occur. Blood pressure may be significantly elevated in patients receiving MAO inhibitors. 

Barbiturates, which preceded benzodiazepines as the most commonly abused sedative hypnotics (after ethanol), are now rarely prescribed to outpatients and therefore constitute a less common prescription drug problem than they did in the past. Street sales of barbiturates, however, continue. Management of barbiturate withdrawal and addiction is similar to that of benzodiazepines. 

Overdosage with ethanol and sedative-hypnotic drugs (eg, benzodiazepines, barbiturates, 7-hydroxybutyrate [GHB], carisoprodol [Soma] see Chapters 22 and 23) occurs frequently because of their common availability and use. 

Overall the anthiistamines are relatively safe. However, their CNS depressant actions are enhanced by co-ingestion of ethanol, sedative-hypnotic drugs, and opioids their anticholinergic actions are potentiated by co-ingestion of tricyclic antidepressants and phenothiazines. Therefore the... 

Ethanol, a sedative-hypnotic drug, is the most important alcohol of pharmacologic interest. It has few medical applications, but its abuse as a recreational drug is responsible for major medical and socioeconomic problems. Other alcohols of toxicologic importance are methanol and ethylene glycol. 

Tolerance and dependence Tolerance occurs mainly as a result of CNS adaptation but may be partly caused by an increased rate of ethanol metabolism. There is cross-tolerance to other sedative-hypnotic drugs. Both psychologic and physical dependence are marked, the latter demonstrated by an abstinence syndrome that occurs if a chronic user abruptly discontinues ethanol intake. 

Withdrawal from ethanol or sedative-hypnotic drugs... 

II. Drugs utilized. Contrary to the popular belief that specific date rape drugs are involved In these crimes, a variety of drugs with amnestic or CNS depressant effects can be used to facilitate assault, including benzodiazepines, other sedative-hypnotic drugs, skeletal muscle relaxants, anticholinergics, hallucinogens, and of course, ethanol (Table 1-45). 

B. Management of withdrawal from ethanol and other sedative-hypnotic drugs. 

The sedative-hypnotic action of chloral hydrate should be explained by the formation of trichloroethanol, which is synthesized as a result of its reduction in tissues. Despite the fact that the precise mechanism of action of chloral hydrate is not known, it evidently acts analogous to ethanol on the CNS by inCTeasing membrane permeability, which leads to sedation or sleep. Chloral hydrate can be used for insomnia as an alternative to benzodiazepines. Synonyms for this drug are aquachloral, chloradorm, chloratol, noctec, and others. 

Tolerance—decreased responsiveness to a drug following repeated exposure—is a common feature of sedative-hypnotic use. It may result in the need for an increase in the dose required to maintain symptomatic improvement or to promote sleep. It is important to recognize that partial cross-tolerance occurs between the sedative-hypnotics described here and also with ethanol (see Chapter 23)—a feature of some clinical importance, as explained below. The mechanisms responsible for tolerance to sedative-hypnotics are not well understood. An increase in the rate of drug metabolism (metabolic tolerance) may be partly responsible in the case of chronic administration of barbiturates, but changes in responsiveness of the central nervous system (pharmacodynamic tolerance) are of greater importance for most sedative-hypnotics. In the case of benzodiazepines, the development of tolerance in animals has been associated with down-regulation of brain benzodiazepine receptors. Tolerance has been reported to occur with the extended use of zolpidem. Minimal tolerance was observed with the use of zaleplon over a 5-week period and eszopiclone over a 6-month period. 

Long-acting drugs such as chlordiazepoxide and diazepam and, to a lesser extent, phenobarbital are administered in progressively decreasing doses to patients during withdrawal from physiologic dependence on ethanol or other sedative-hypnotics. Parenteral lorazepam is used to suppress the symptoms of delirium tremens. 

A pharmacodynamic interaction involves either inhibition or enhancement of the clinical effects of the victim drug as a consequence of similar or identical end-organ actions. Examples are the increase or decrease of the sedative-hypnotic actions of benzodiazepine agonist drugs due to coadministration of ethanol or... 

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