The Info List - Sedative

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A sedative or tranquilliser[1] is a substance that induces sedation by reducing irritability[2] or excitement.[3] They are central nervous depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA), which are brain chemicals performing communication between brain cells. In spite of the fact that each sedative acts in its own way, they produce beneficial relaxing effect by increasing GABA activity.[4] At higher doses it may result in slurred speech, staggering gait, poor judgment, and slow, uncertain reflexes. Doses of sedatives such as benzodiazepines, when used as a hypnotic to induce sleep, tend to be higher than amounts used to relieve anxiety, whereas only low doses are needed to provide a peaceful effect.[5] Sedatives can be misused to produce an overly-calming effect (alcohol being the classic and most common sedating drug). In the event of an overdose or if combined with another sedative, many of these drugs can cause unconsciousness (see hypnotic) and even death.


1 Terminology

1.1 The term "chemical cosh" 1.2 Types of sedatives

2 Therapeutic use 3 Risks

3.1 Sedative dependence 3.2 Misuse 3.3 Dangers of combining sedatives and alcohol 3.4 Worsening of Psychiatric Symptoms 3.5 Amnesia 3.6 Disinhibition and crime

4 See also 5 References 6 Further reading

Terminology[edit] There is some overlap between the terms "sedative" and "hypnotic". Advances in pharmacology have permitted more specific targeting of receptors, and greater selectivity of agents, which necessitates greater precision when describing these agents and their effects:

Anxiolytic refers specifically to the effect upon anxiety. (However, some benzodiazepines can be all three: sedatives, hypnotics, and anxiolytics). Tranquilizer can refer to anxiolytics or antipsychotics. Soporific
and sleeping pill are near-synonyms for hypnotics.

The term "chemical cosh"[edit] The term "chemical cosh" (a club) is sometimes used popularly for a strong sedative, particularly for:

widespread dispensation of antipsychotic drugs in residential care to make people with dementia easier to manage.[6] use of ritalin to calm children with attention deficit hyperactivity disorder, though paradoxically this drug is known to be a stimulant.

See also Antipsychotic

Types of sedatives[edit]

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Benzylbutylbarbiturate Butalbital Amobarbital Pentobarbital Secobarbital Sodium thiopental Phenobarbital


Clonazepam Diazepam Estazolam Flunitrazepam Lorazepam Midazolam Nitrazepam Oxazepam Triazolam Temazepam Chlordiazepoxide Alprazolam Clobazam Clorazepate Etizolam


Eszopiclone Zaleplon Zolpidem Zopiclone

Orexin antagonists


First generation Antihistamines

Diphenhydramine Dimenhydrinate Doxylamine Promethazine Hydroxyzine Brompheniramine Chlorpheniramine

General Anesthetics

Nitrous oxide Sevoflurane Halothane Xenon Enflurane Chloroform Isoflurane Methoxyflurane Desflurane Ethyl chloride Cyclopropane Chloral hydrate Ketamine Esketamine Etomidate Propofol Chlorobutanol

Herbal sedatives

Duboisia hopwoodii Chamomile Prostanthera
striatiflora catnip Kava
(Piper methysticum) valerian cannabis Passiflora
spp.(passiflora incarnata) Physochlaina
- notably P. infundibularis Validol

and analogues

Afloqualone Cloroqualone Diproqualone Etaqualone Methaqualone Methylmethaqualone Mebroqualone Mecloqualone Nitromethaqualone

Skeletal Muscle

Baclofen Meprobamate Carisoprodol Cyclobenzaprine Metaxalone Methocarbamol Tizanidine Chlorzoxazone Orphenadrine Gabapentin Pregabalin


Tramadol Tapentadol Morphine Hydromorphone Oxymorphone Oxycodone Hydrocodone Methadone Propoxyphene Meperidine Fentanyl Codeine Carfentanil Remifentanil Alfentanil Sufentanil Opium


Amitriptyline Trazodone Mirtazapine Doxepin Desipramine Imipramine Clomipramine Amoxapine Trimipramine Nortriptyline Nefazodone


Olanzapine Clozapine Thiothixene Haloperidol Fluphenazine Prochlorperazine Trifluoperazine Loxapine Quetiapine Asenapine


(2M2B) Ethanol Glutethimide GHB Dextromethorphan

Therapeutic use[edit] Doctors often administer sedatives to patients in order to dull the patient's anxiety related to painful or anxiety-provoking procedures. Although sedatives do not relieve pain in themselves, they can be a useful adjunct to analgesics in preparing patients for surgery, and are commonly given to patients before they are anaesthetized, or before other highly uncomfortable and invasive procedures like cardiac catheterization, colonoscopy or MRI. They increase tractability and compliance of children or troublesome or demanding patients. Risks[edit] Sedative dependence[edit] Some sedatives can cause psychological and physical dependence when taken regularly over a period of time, even at therapeutic doses.[7][8][9][10] Dependent users may get withdrawal symptoms ranging from restlessness and insomnia to convulsions and death. When users become psychologically dependent, they feel as if they need the drug to function, although physical dependence does not necessarily occur, particularly with a short course of use. In both types of dependences, finding and using the sedative becomes the focus in life. Both physical and psychological dependence can be treated with therapy. Misuse[edit] Main article: Drug overdose Further information: Combined drug intoxication See also: Benzodiazepine
overdose and Barbiturate
overdose Many sedatives can be misused, but barbiturates and benzodiazepines are responsible for most of the problems with sedative use due to their widespread recreational or non-medical use. People who have difficulty dealing with stress, anxiety or sleeplessness may overuse or become dependent on sedatives. Some heroin users may take them either to supplement their drug or to substitute for it. Stimulant users may take sedatives to calm excessive jitteriness. Others take sedatives recreationally to relax and forget their worries. Barbiturate
overdose is a factor in nearly one-third of all reported drug-related deaths. These include suicides and accidental drug poisonings. Accidental deaths sometimes occur when a drowsy, confused user repeats doses, or when sedatives are taken with alcohol. A study from the United States found that in 2011, sedatives and hypnotics were a leading source of adverse drug events (ADEs) seen in the hospital setting: Approximately 2.8% of all ADEs present on admission and 4.4% of ADEs that originated during a hospital stay were caused by a sedative or hypnotic drug.[11] A second study noted that a total of 70,982 sedative exposures were reported to U.S. poison control centers in 1998, of which 2310 (3.2%) resulted in major toxicity and 89 (0.1%) resulted in death. About half of all the people admitted to emergency rooms in the U.S. as a result of nonmedical use of sedatives have a legitimate prescription for the drug, but have taken an excessive dose or combined it with alcohol or other drugs.[12] There are also serious paradoxical reactions that may occur in conjunction with the use of sedatives that lead to unexpected results in some individuals. Malcolm Lader at the Institute of Psychiatry in London estimates the incidence of these adverse reactions at about 5%, even in short-term use of the drugs. The paradoxical reactions may consist of depression, with or without suicidal tendencies, phobias, aggressiveness, violent behavior and symptoms sometimes misdiagnosed as psychosis.[13] Dangers of combining sedatives and alcohol[edit] Further information: Combined Drug Intoxication Sedatives and alcohol are sometimes combined recreationally or carelessly. Since alcohol is a strong depressant that slows brain function and depresses respiration, the two substances compound each other's actions and this combination can prove fatal. Worsening of Psychiatric Symptoms[edit] The long-term use of benzodiazepines may have a similar effect on the brain as alcohol, and are also implicated in depression, anxiety, posttraumatic stress disorder (PTSD), mania, psychosis, sleep disorders, sexual dysfunction, delirium, and neurocognitive disorders (including benzodiazepine-induced persisting dementia which persists even after the medications are stopped).[14] As with alcohol, the effects of benzodiazepine on neurochemistry, such as decreased levels of serotonin and norepinephrine, are believed to be responsible for their effects on mood and anxiety.[15][16][17][18][19][20] Additionally, benzodiazepines can indirectly cause or worsen other psychiatric symptoms (e.g., mood, anxiety, psychosis, irritability) by worsening sleep (i.e., benzodiazepine-induced sleep disorder). Like alcohol, benzodiazepines are commonly used to treat insomnia in the short-term (both prescribed and self-medicated), but worsen sleep in the long-term. While benzodiazepines can put people to sleep but, while asleep, the drugs disrupt sleep architecture: decreasing sleep time, delaying time to REM sleep, and decreasing deep slow-wave sleep (the most restorative part of sleep for both energy and mood).[21][22][23] Amnesia[edit] Sedatives can sometimes leave the patient with long-term or short-term amnesia. Lorazepam
is one such pharmacological agent that can cause anterograde amnesia. Intensive care unit
Intensive care unit
patients who receive higher doses over longer periods, typically via IV drip, are more likely to experience such side effects. Disinhibition and crime[edit] Sedatives — most commonly alcohol[24] but also GHB, Flunitrazepam (Rohypnol), and to a lesser extent, temazepam (Restoril), and midazolam (Versed)[25] — have been reported for their use as date rape drugs (also called a Mickey) and being administered to unsuspecting patrons in bars or guests at parties to reduce the intended victims' defenses. These drugs are also used for robbing people. Statistical overviews suggest that the use of sedative-spiked drinks for robbing people is actually much more common than their use for rape.[26] Cases of criminals taking rohypnol themselves before they commit crimes have also been reported[citation needed], as the loss of inhibitions from the drug may increase their confidence to commit the offence, and the amnesia produced by the drug makes it difficult for police to interrogate them if they are caught. See also[edit]

Hypnotic Antidepressants Benzodiazepine
withdrawal syndrome Tranquilizer Tranquilizer gun Diphenhydramine


^ Also spelled tranquillizer (Oxford spelling) and tranquilizer (US spelling); see spelling differences ^ "Johns Hopkins Colon Cancer Center - Glossary S".  ^ "sedative" at Dorland's Medical Dictionary ^ "Sedatives Psychology Today". Psychology Today. Retrieved 2017-11-20.  ^ Montenegro M, Veiga H, Deslandes A, et al. (June 2005). "[Neuromodulatory effects of caffeine and bromazepam on visual event-related potential (P300): a comparative study.]". Arq Neuropsiquiatr. 63 (2B): 410–5. doi:10.1590/S0004-282X2005000300009. PMID 16059590.  ^ "'Chemical cosh' will be cut for dementia sufferers". Telegraph.co.uk. 25 October 2010. Retrieved 12 September 2015.  ^ Yi PL; Tsai CH; Chen YC; Chang FC (March 2007). "Gamma-aminobutyric acid (GABA) receptor mediates suanzaorentang, a traditional Chinese herb remedy, -induced sleep alteration". J Biomed Sci. 14 (2): 285–97. doi:10.1007/s11373-006-9137-z. PMID 17151826.  ^ Ebert B; Wafford KA; Deacon S (December 2006). "Treating insomnia: Current and investigational pharmacological approaches". Pharmacol Ther. 112 (3): 612–29. doi:10.1016/j.pharmthera.2005.04.014. PMID 16876255.  ^ Sarrecchia C, Sordillo P, Conte G, Rocchi G (1998). "[Barbiturate withdrawal syndrome: a case associated with the abuse of a headache medication]". Ann. Ital. Med. Int. (in Italian). 13 (4): 237–9. PMID 10349206.  ^ Proudfoot H, Teesson M, Australian National Survey of Mental Health and Wellbeing (October 2002). "Who seeks treatment for alcohol dependence? Findings from the Australian National Survey of Mental Health and Wellbeing". Soc Psychiatry Psychiatr Epidemiol. 37 (10): 451–6. doi:10.1007/s00127-002-0576-1. PMID 12242622.  ^ Weiss AJ, Elixhauser A. Origin of Adverse Drug Events in U.S. Hospitals, 2011. HCUP Statistical Brief #158. Agency for Healthcare Research and Quality, Rockville, MD. July 2013. [1] ^ Professor Jeffrey S Cooper (10 December 2007). "Toxicity, Sedatives". USA: eemedicine. Retrieved 18 December 2008.  ^ "benzo.org.uk - Benzodiazepines: Paradoxical Reactions and Long-Term Side-Effects". Retrieved 12 September 2015.  ^ American Psychiatric Association (2013). Diagnostic and statistical manual of mental disorders, fifth edition. Arlington, VA: American Psychiatric Association.  ^ Collier, Judith; Longmore, Murray (2003). "4". In Scally, Peter. Oxford Handbook of Clinical Specialties (6 ed.). Oxford University Press. p. 366. ISBN 978-0-19-852518-9.  ^ Professor Heather Ashton (2002). "Benzodiazepines: How They Work and How to Withdraw".  ^ Lydiard RB, Laraia MT, Ballenger JC, Howell EF (May 1987). "Emergence of depressive symptoms in patients receiving alprazolam for panic disorder". Am J Psychiatry. 144 (5): 664–5. doi:10.1176/ajp.144.5.664. PMID 3578580.  ^ Nathan RG, Robinson D, Cherek DR, Davison S, Sebastian S, Hack M (1 January 1985). "Long-term benzodiazepine use and depression". Am J Psychiatry. American Journal of Psychiatry. 142 (1): 144–5. PMID 2857068.  ^ Longo, L. P.; Johnson, B. (2000-04-01). "Addiction: Part I. Benzodiazepines--side effects, abuse risk and alternatives". American Family Physician. 61 (7): 2121–2128. ISSN 0002-838X. PMID 10779253.  ^ Tasman A, Kay J, Lieberman JA (2008). Psychiatry, third edition. Chichester, England: John Wiley & Sons. pp. 2603–2615.  ^ Ashton, Heather (2005-05-01). "The diagnosis and management of benzodiazepine dependence". Current Opinion in Psychiatry. 18 (3): 249–255. doi:10.1097/01.yco.0000165594.60434.84. ISSN 0951-7367. PMID 16639148.  ^ Morin, Charles M.; Bélanger, Lynda; Bastien, Célyne; Vallières, Annie (2005-01-01). "Long-term outcome after discontinuation of benzodiazepines for insomnia: a survival analysis of relapse". Behaviour Research and Therapy. 43 (1): 1–14. doi:10.1016/j.brat.2003.12.002. ISSN 0005-7967. PMID 15531349.  ^ Poyares, Dalva; Guilleminault, Christian; Ohayon, Maurice M.; Tufik, Sergio (2004-06-01). "Chronic benzodiazepine usage and withdrawal in insomnia patients". Journal of Psychiatric Research. 38 (3): 327–334. doi:10.1016/j.jpsychires.2003.10.003. ISSN 0022-3956. PMID 15003439.  ^ Weir E. (July 10, 2001). "Drug-facilitated date rape". Canadian Medical Association Journal. 165 (1): 80. PMC 81265 . PMID 11468961.  ^ Negrusz A; Gaensslen RE. (August 2003). "Analytical developments in toxicological investigation of drug-facilitated sexual assault". Analytical and Bioanalytical Chemistry. 376 (8): 1192–7. doi:10.1007/s00216-003-1896-z. PMID 12682705.  ^ Thompson, Tony (19 December 2004). "'Rape drug' used to rob thousands". The Observer. Retrieved 2008-05-08. 

Further reading[edit]

Tone, Andrea. The Age of Anxiety: A History of America's Turbulent Affair with Tranquilizers (Basic Books, 2009) 288 pp.; ISBN 978-0-465-08658-0 excerpty and text search

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2M2B Chloralodol Ethanol
(alcohol) Ethchlorvynol Methylpentynol Trichloroethanol


Allobarbital Amobarbital Aprobarbital Barbital Butabarbital Butobarbital Cyclobarbital Ethallobarbital Heptabarb Hexobarbital Mephobarbital Methohexital Narcobarbital Pentobarbital Phenallymal Phenobarbital Propylbarbital Proxibarbal Reposal Secobarbital Talbutal Thiamylal Thiopental Thiotetrabarbital Vinbarbital Vinylbital


Brotizolam Cinolazepam Climazolam Doxefazepam Estazolam Flunitrazepam Flurazepam Flutoprazepam Lorazepam Loprazolam Lormetazepam Midazolam Nimetazepam Nitrazepam Phenazepam Quazepam Temazepam Triazolam


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Etomidate Metomidate Propoxate


Acecarbromal Apronal
(apronalide) Bromisoval Capuride Carbromal Ectylurea

Neuroactive steroids

Acebrochol Allopregnanolone Alphadolone Alphaxolone Eltanolone Hydroxydione Minaxolone Progesterone


Eszopiclone Indiplon Lirequinil Necopidem Pazinaclone Saripidem Suproclone Suriclone Zaleplon Zolpidem Zopiclone




Glutethimide Methyprylon Pyrithyldione Piperidione


Afloqualone Cloroqualone Diproqualone Etaqualone Mebroqualone Mecloqualone Methaqualone Methylmethaqualone Nitromethaqualone


Acetophenone Acetylglycinamide chloral hydrate Bromide compounds

Lithium bromide Potassium bromide Sodium bromide

Centalun Chloral betaine Chloral hydrate Chloralose Clomethiazole Dichloralphenazone Gaboxadol Kavalactones Loreclezole Paraldehyde Petrichloral Sulfonylalkanes

(sulfonal) Tetronal Trional

Triclofos Sesquiterpene

Isovaleramide Isovaleric acid Valerenic acid


1,4-Butanediol 4-Fluorophenibut Aceburic acid Baclofen GABOB GHB (sodium oxybate) GBL GVL Phenibut Tolibut



Captodiame Cyproheptadine Diphenhydramine Doxylamine Hydroxyzine Methapyrilene Perlapine Pheniramine Promethazine Propiomazine


antagonists and reuptake inhibitors

Etoperidone Nefazodone Trazodone

Tricyclic antidepressants

Amitriptyline Doxepin Trimipramine, etc.

Tetracyclic antidepressants

Mianserin Mirtazapine, etc.


Typical antipsychotics

Chlorpromazine Thioridazine, etc.

Atypical antipsychotics

Olanzapine Quetiapine Risperidone, etc.


Clonidine Detomidine Dexmedetomidine Lofexidine Medetomidine Romifidine Tizanidine Xylazine



Trazodone Tricyclic antidepressants

Amitriptyline Doxepin Trimipramine, etc.

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Mianserin Mirtazapine, etc.


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Chlorpromazine Thioridazine, etc.

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Olanzapine Quetiapine Risperidone, etc.




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