Barbiturates insomnia

Pharmacological Profiles of Anxiolytics and Sedative—Hypnotics. Historically, chemotherapy of anxiety and sleep disorders rehed on a wide variety of natural products such as opiates, alcohol, cannabis, and kawa pyrones. Use of various bromides and chloral derivatives ia these medical iadications enjoyed considerable popularity early ia the twentieth century. Upon the discovery of barbiturates, numerous synthetic compounds rapidly became available for the treatment of anxiety and insomnia. As of this writing barbiturates are ia use primarily as iajectable general anesthetics (qv) and as antiepileptics. These agents have been largely replaced as treatment for anxiety and sleep disorders. 

The short-acting clomethia2ole [533-45-9] (1), sometimes used as therapy for sleep disorders ia older patients, shares with barbiturates a risk of overdose and dependence. Antihistamines, such as hydroxy2iae [68-88-2] (2), are also sometimes used as mild sedatives (see HiSTAMlNES AND HISTAMINE antagonists). Antidepressants and antipsychotics which have sedative effects are used to treat insomnia when the sleep disorder is a symptom of some underlyiag psychiatric disorder. 

Pentobarbital, marketed under the name Nembutal, is a barbiturate used i treating insomnia. It is synthesized in three steps from diethyl maionatt Show how you would synthesize the dialkylated intermediate, and then pre pose a mechanism for the reaction of that intermediate with urea to giv pentobarbital. 

No health hazards are known with the proper use of kava (Gruenwald et al. 1998). Kava has been approved by the German Commission E for treatment of anxiety and insomnia. In clinical studies of kava for anxiety, adverse effects were uncommon and did not differ across placebo and kava groups. There do not appear to be any studies published on the effects of acute overdosage with kava. Given its CNS depressant effects, it should not be taken with other similar drugs, including benzodiazepines, barbiturates. 

Nonbarbiturates. After the introduction of the barbiturates, there was little progress in the medical treatment of anxiety until meprobamate (Equanil, Miltown) was introduced in 1950. Soon after its introduction, a series of similar medicines entered the market, including carisoprodol (Soma), glutethimide (Doriden), methaqualone (Qaalude, Sopor), methyprylon (Noludar), and ethchlorvynol (Placidyl). These medications have all been used to treat anxiety, insomnia, and muscle spasms. 

Barbiturates. The first barbiturate, barbital, was introduced at the turn of the 20th century. Hundreds of others, including phenobarbital and pentobarbital, were later developed. The barbiturates were a highly successful class of medications as it became clear that they treated not only alcohol withdrawal but seizure disorders, anxiety, and insomnia as well. By the 1960s, however, the barbiturates were largely surpassed by the benzodiazepines. The newer benzodiazepines act in a similar fashion and provide much the same therapeutic benefit but are significantly safer and easier to tolerate. 

Ethinamate is a hypnotic, which does not have, however, a considerable advantage over barbiturates and benzodiazepines, and is used much less in treating insomnia. Synonyms for this drug are valamide, ivalmad, valamin, and others. 

As with all of the examined drugs in this chapter, methyprylon is intended for treating insomnia. The pharmacological effects of methyprylon are similar to those of barbiturates. However, barbiturates are beginning to give way, thanks to the introduction of benzodiazepines into medical practice. Synonyms for this drug are noctar, noludar, and others. 

Hypnotic Short-term treatment of insomnia, because barbiturates appear to lose their effectiveness in sleep induction and maintenance after 2 weeks. If insomnia persists, seek alternative therapy (including nondrug) for chronic insomnia. Preanesthetic Used as preanesthetic sedatives. 

Pentobarbital (Nembutal, Others) [C-ll] [Anticonvulsant, Sedative/ Hypnotic/Barbiturate] Uses Insomnia, convulsions, induce coma following severe head injury Action Barbiturate Dose Adults. Sedative ... 

A significant advantage of the benzodiazepines over other central nervous system depressants (e.g., the barbiturates) is that they possess a much greater separation between the dose that produces sleep and the dose that produces death. This increased margin of safety has been one of the major reasons benzodiazepines have largely replaced the barbiturates and other types of sedative-hypnotics in the treatment of anxiety and insomnia. In addition, benzodiazepine aclministration is associated with few side effects. 

Before the introduction of the benzodiazepines, a number of drugs from different chemical and pharmacological classes were used in the treatment of anxiety and insomnia. However, these drugs are more toxic and produce more serious side effects than do the benzodiazepines. Many also have signihcant abuse potential. Consequently, most of these compounds are no longer widely used. These drugs include the barbiturates (e.g., pentobarbital, amobarbital), carbamates (e.g., meprobamate), piperidinediones (e.g., glutethimide), and alcohols (e.g., ethchlorvynol). 

Barbiturates are usually taken orally, sometimes with alcohol to increase the intoxicating effect, or by injection. The ultrashort-acting barbiturate Pentothal produces surgical anesthesia within about one minute after intravenous administration. The onset of action of the short- and intermediateacting barbiturates taken orally for insomnia is from 10 to 60 minutes, and the effects last up to six hours. Barbiturates distribute to body fat and are found in breast milk. They may cause drowsiness, slow heartbeat, and shortness of breath in babies of nursing mothers who are taking these drugs. 

Phenobarbital, mephobarbital and metarbital are the only oral anticonvulsants which are effective at sub-hypnotic levels. Many barbiturates are classified as Schedule II, III, or IV due to their high potential for overdose and dependence. Abrupt withdrawal may cause seizures, restlessness, trembling, and insomnia and may be fatal. Phenobarbital is used as an anticonvulsant for the treatment of epilepsy and in some combination medications for the relief of irritable bowel syndrome. 

Valerian Valeriana officinalis) The roots of this plant are dried to produce a potent extract that induces sleepiness and helps treat insomnia. Like lavender, it depresses the activity of the central nervous system in a fashion similar to stronger prescription tranquilizers such as benzodiazepines and barbiturates, but without the dulling or hangover effects the next day or impairing the ability to drive a car. 

Compared to barbiturates, benzodiazepines are relatively safe medications that produce little tolerance and suppression of REM sleep, and benzodiazepine overdoses are much less common. However, benzodiazepines are not without unwanted side effects. As mentioned above, longer-acting benzodiazepines can produce residual drowsiness, grogginess, and weakness the next day (benzodiazepines are also muscle relaxants). Benzodiazepines can produce rebound insomnia, in which the person experiences significant insomnia after he or she stops taking the medication. This is particularly true with benzodiazepines that have short half-lives. To avoid this, the patient should never stop cold turkey rather, the dosage should be slowly tapered off over several days to a week. 

The depressant effect of barbiturates is often sought by persons who are self-medicating for amdety-related problems or insomnia. Drugs of the benzodiazepine family (Librium, Valium, and Xanax) are also legitimately prescribed for the treatment of anxiety as well as muscle spasms or convulsions. However, doctors and patients must be careful because prolonged or excessive use can lead to dependence. Illegal use often involves forged prescriptions or the cooperation of illicit doctors. 

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