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Leslie Clark Fact Sheet: Sedative Hypnotics Definition/Description of Sedative Hypnotics The definition of Sedative is a central nervous system depressants used to relieve anxiety, fear and apprehension. Along with this definition comes the definition of Hypnotics which is a central nervous system depressant used to induce drowsiness and encourage sleep. In terms of drugs, sedative refers to a substance that moderates activity and excitement while inducing a calming effect, while hypnotic refers to a substance that causes drowsiness and facilitates the onset and maintenance of natural sleep. Due to their pharmacodynamic actions, especially the sedative effects, many of the sedative-hypnotics are considered potential drugs of abuse, and are therefore regulated as controlled substances. Along these lines, several sedative-hypnotic drugs have developed an interesting and alarming niche in the group of “club drugs” that have become popular in the past decade. Types of Sedative Hypnotics The sedative-hypnotics may be divided into three major groups: (1) benzodiazepines, (2) barbiturates, and (3) other drugs that do not fall into either of the first two groups. Benzodiazepines are the most popular and safest Central Nervous System depressants in use today. Barbiturates are potent central nervous system depressants usually not referred because of the narrow margin of safety. Names of Sedative Hypnotics Benzodiazepines Alprazolam (Xanax) Amobarbital (Amytal) Butabarbital (Butisol) Mephobarbital (Mebaral) Pentobarbital (Nembutal) Phenobarbital (Luminol) Secobarbital (Seconal) Barbiturates Chlordiazepoxide (Librium) Clonazepam (Klonopin) Leslie Clark Clorazepate (Tranxene) Diazepam (Valium) Estazolam (Prosom) Flurazepam (Dalmane) Lorazepam (Ativan) Midazolam (Versed) Oxazepam (Serax) Quazepam (Doral Temazepam (Restoril Triazolam (Halcion) Selected Other Sedative-Hypnotics Buspirone (Buspar) Chloral Hydrate (Somnote) Eszoplicone (Lunesta) Ramelteon (Rozerem) Zaleplon (Sonata) Zolpidem (Ambien) Therapeutic Uses of sedative hypnotics In clinical therapeutics, sedative-hypnotics are useful for treatment of a variety of diseases related to the central nervous system, such as acute and chronic anxiety, anesthesia, seizure control, and insomnia. Sedative-hypnotic drugs have a sedative, calming, and anxiolytic effect on patients, especially those who are acutely anxious. However, this calming effect is generally accompanied by some psychomotor and cognitive effects as well. At high enough doses, all of these drugs will induce sleep (hypnosis). However, some are better than others for use as an aid for inducing sleep. While most of these drugs decrease the time it takes to fall asleep, they also unfortunately decrease the amount of time spent in REM sleep (zaleplon is an exception, as it does not change the time spent in REM sleep). The decrease in the time it takes to fall asleep makes many of these drugs useful as a sleep aid; however, the effect of the decrease in REM sleep induced by most of these drugs is currently unclear, and may explain some of the negative effects of these drugs. Sedative-hypnotics is anesthesia. Some these drugs are very useful as anesthetic agents (e.g., barbiturates), while others are not useful at all. The usefulness of these drugs in anesthesia is largely dependent on their onset of action and their duration of action. Hypnotics are used for the treatment of insomnia which is characterized by difficulties with falling asleep or maintaining sleep. (Some hypnotics may have other uses. For example, zolpidem (Ambien, Ambien CR) also is used for promoting improvement in motor symptoms associated with Parkinson's disease although this use is not FDA-approved indication.) work, in general, by increasing the activity of gamma-aminobutyric acid (GABA), a neurotransmitter in the brain. Neurotransmitters are chemicals made and released by nerves that attach to other nerves, and serve as a means of communicating with other nerves. Increases in GABA activity in the brain produce drowsiness and facilitate/maintain sleep. Leslie Clark Therapeutic Uses of sedative hypnotics `In clinical therapeutics, sedative-hypnotics are useful for treatment of a variety of diseases related to the central nervous system, such as acute and chronic anxiety, anesthesia, seizure control, and insomnia. Sedative-hypnotic drugs have a sedative, calming, and anxiolytic effect on patients, especially those who are acutely anxious. However, this calming effect is generally accompanied by some psychomotor and cognitive effects as well. At high enough doses, all of these drugs will induce sleep (hypnosis). However, some are better than others for use as an aid for inducing sleep. While most of these drugs decrease the time it takes to fall asleep, they also unfortunately decrease the amount of time spent in REM sleep (zaleplon is an exception, as it does not change the time spent in REM sleep). The decrease in the time it takes to fall asleep makes many of these drugs useful as a sleep aid; however, the effect of the decrease in REM sleep induced by most of these drugs is currently unclear, and may explain some of the negative effects of these drugs. Sedative-hypnotics is anesthesia. Some these drugs are very useful as anesthetic agents (e.g., barbiturates), while others are not useful at all. The usefulness of these drugs in anesthesia is largely dependent on their onset of action and their duration of action. Hypnotics are used for the treatment of insomnia which is characterized by difficulties with falling asleep or maintaining sleep. (Some hypnotics may have other uses. For example, zolpidem (Ambien, Ambien CR) also is used for promoting improvement in motor symptoms associated with Parkinson's disease although this use is not FDA-approved indication.) work, in general, by increasing the activity of gamma-aminobutyric acid (GABA), a neurotransmitter in the brain. Neurotransmitters are chemicals made and released by nerves that attach to other nerves, and serve as a means of communicating with other nerves. Increases in GABA activity in the brain produce drowsiness and facilitate/maintain sleep. Physiological effects from the abuse of sedative hypnotics Side effects of hypnotics include: headache , nervousness, talkativeness, apprehension, irritability; confusion, euphoria, relaxed feeling, weakness, tremor, lack of concentration, disorders of coordination, depression, dreaming/nightmares, insomnia, palpitations, chest pains, and rapid heart rate. Leslie Clark Side effects involving the stomach and intestines include: heartburn, nausea, vomiting, diarrhea, constipation, abdominal pain, loss of appetite, alterations in taste, dry mouth, and excessive salivation (rare). Detrimental effects of the abuse of Sedative Hypnotics Benzodiazepines are commonly used as a secondary drug of abuse and combined with illicit drugs. Another combination is the use of benzodiazepines with stimulants such as cocaine. Addicts claim that this combination enhances the pleasant effects of the stimulant and reduces the “crashing” that occurs after using high doses. Those that abuse sedative hypnotics are treated for persistent insomnia or anxiety with daily exposures to a CNS depressant. The patient becomes agitated, unable to sleep and severely anxious a state of panic may be experience when deprived of the drug. References Gbemudu, A. (n.d.). Sleep Disorder Drugs (Hypnpotics/Sedatives). In The internet Drug Index. Retrieved March 13, 2011, from http://www.rxlist.com/script/main/art.asp?articlekey=94755#overview Hason, G. R., Venturelli, P. J., & Fleckenstein, A. E. (2009). Drugs and Society (10th ed.). Sudbury: Jones and Bartlett. Nelson, M. H. (2006). Sedative Hypnotic Drugs. Retrieved March 13, 2011, from http://pharmacy.wingate.edu/faculty/mnelson/PDF/Sedative_Hypnotics.pdf