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11-SEPTEMBER-2008 12:20:15 - Barbiturate Barbituric acid, the basic structure of all barbiturates Barbituric acid, the basic structure of all barbiturates Barbiturates are drugs that act as central nervous system depressants, and by virtue of this they produce a wide spectrum of effects, from mild sedation to anesthesia. They are also effective as anxiolytics and hypnotic and as anticonvulsants. They have addiction potential, both physical and psychological. Barbiturates have now largely been replaced by the benzodiazepines mainly due to benzodiazepines being significantly less dangerous in overdose. Barbiturates are derivatives of barbituric acid. Contents 1 History 2 Therapeutic uses 2.1 Other non-therapeutic uses 3 Mechanism of action 4 Tolerance, dependence and overdose 5 Recreational misuse and abuse 6 Legal status 7 Examples 8 See also 9 References 10 External links History Barbituric acid, was first synthesised on December 4, 1864, by German researcher Adolf von Baeyer. This was done by condensing urea an animal waste product with diethyl malonate an ester derived from the acid of apples. There are several stories about how the substance got its name. The most likely story is that von Baeyer and his colleagues went to celebrate their discovery in a tavern where the town's artillery garrison were also celebrating the day of Saint Barbara - the patron saint of artillerists. An artillery officer is said to have christened the new substance by amalgamating Barbara with urea.1 Barbituric acid itself does not have any effect on the CNS Central Nervous System, however to date chemists have derived over 2,500 compounds that do possess pharmacologically active qualities. The broad class of Barbiturates is broken down further and classified according to speed of onset and duration of action. Ultra-Short acting Barbiturates are commonly used for anesthesia because their extremely short duration of action allows for greater control. These properties allow doctors to rapidly put a patient under in emergency surgery situations. Doctors can also bring a patient out of anesthesia just as quickly should complications arise during surgery. The middle two classes of Barbiturates are often combined under the title Short-Intermediate acting. These Barbiturates are also employed for anesthetic purposes, and are also sometimes prescribed for anxiety or insomnia. This is not a common practice anymore however, due to the addiction liability associated with Barbiturates, they have been replaced by the Benzodiazepines for these purposes. The final class of Barbiturates are known as Long acting Barbiturates most notably phenobarbital, which has a half-life of roughly 92 hours. This class of Barbiturates is used almost exclusively as anticonvulsants, although on rare occasions they are sometimes prescribed for daytime sedation. Barbiturates in this class are not used for insomnia, because due to their extremely long half-life, patients would awake with a residual hang-over effect and feel groggy. No substance of medical value was discovered, however, until 1903 when two German chemists working at Bayer, Emil Fischer and Joseph von Mering, discovered that barbital was very effective in putting dogs to sleep. Barbital was then marketed by Bayer under the trade name Veronal. It is said that Von Mering proposed this name because the most peaceful place he knew was the Italian city of Verona.1 Barbiturates can in most cases be used as either the free acid or as salts of sodium, calcium, potassium, magnesium, lithium etc. Codeine- and Dionine-based salts of barbituric acid have been developed. In 1912, Bayer introduced another barbituric acid derivative, phenobarbital, under the trade name Luminal, as a sedative-hypnotic.2 Therapeutic uses Barbiturates like pentobarbital and phenobarbital were long used as anxiolytics and hypnotics. Today benzodiazepines have largely supplanted them for these purposes, because benzodiazepines have less potential for lethal overdoses.345 Barbiturates are classified as ultrashort-, short-, intermediate-, and long-acting, depending on how quickly they act and how long their effects last.6 Barbiturates are still widely used in surgical anesthesia, especially to induce anesthesia. Ultrashort barbiturates such as thiopental Pentothal produce unconsciousness within about a minute of intravenous IV injection. These drugs are used to prepare patients for surgery; other general anesthetics like nitrous oxide are then used to keep the patient from waking up before the surgery is complete. Because Pentothal and other ultrashort-acting barbiturates are typically used in hospital settings, they are not very likely to be abused, noted the DEA.7 Phenobarbital is used as an anticonvulsant for people suffering from seizure disorders such as febrile seizures, tonic-clonic seizures, status epilepticus, and eclampsia.8 Long-acting barbiturates such as phenobarbital Luminal and mephobarbital Mebaral are prescribed for two main reasons. When taken at bedtime, they help treat insomnia. When taken during the day, they have sedative effects that can aid in the treatment of tension and anxiety. These same effects have been found helpful in the treatment of convulsive conditions like epilepsy. Phenobarbital has also been used in the treatment of delirium tremens during alcohol detoxification, although benzodiazepines have a more favorable safety profile and are more often used.9 Long-acting barbiturates take effect within one to two hours and last 12 hours or longer.7 Other non-therapeutic uses Barbiturates in high doses are used for physician-assisted suicide PAS, and in combination with a muscle relaxant for euthanasia and for capital punishment by lethal injection.1011 Thiopental is an ultra-short acting barbiturate that is marketed under the name Sodium Pentothal is sometimes used as a truth serum. When dissolved in water, it can be swallowed or administered by intravenous injection. The drug does not itself force people to tell the truth, but is thought to decrease inhibitions, making subjects more likely to be caught off guard when questioned.12 Mechanism of action The principal mechanism of action of barbiturates is believed to be their affinity for the GABAA receptor Acts on GABA : BDZ receptor Cl- channel complex. GABA is the principal inhibitory neurotransmitter in the mammalian Central Nervous System CNS. Barbiturates bind to the GABAA receptor at the alpha subunit, which are binding sites distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Taken together, the findings that barbiturates potentiate inhibitory GABAA receptors and inhibit excitatory AMPA receptors can explain the CNS-depressant effects of these agents. At higher concentration they inhibit the Ca2+ dependent release of neurotransmitters.8 Barbiturates produce their pharmacological effects by increasing the length of time the chloride ion channel remains open at the GABAA receptor whereas benzodiazepines increase the opening frequency of the chloride ion channel at the GABAA receptor. The direct gating or opening of the chloride ion channel is the reason for the increased toxicity of barbiturates compared to benzodiazepines in overdose.1314 Tolerance, dependence and overdose With regular use tolerance to the effects of barbiturates develops. This in turn may lead to a need for increasing doses of the drug to get the original desired pharmacological or therapeutic effect.15 Barbiturate use can lead to both psychological and physical dependence and the drugs have a high abuse liability.16 Psychological addiction to barbiturates can develop quickly. The GABAA receptor, one of barbiturates' main sites of action, is thought to play a pivotal role in the development of tolerance to and dependence on barbiturates, as well as the euphoric high that results from their abuse.16 The mechanism by which barbiturate tolerance develops is believed to be different than that of ethanol or benzodiazepines, even though these drugs have been shown to exhibit cross-tolerance with each other.17 An overdose results when a person takes a larger-than-prescribed dose of a drug. Symptoms of an overdose typically include; sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, Staggering and in severe cases coma and death.18 The lethal dosage of barbiturates varies greatly with tolerance and from one individual to another. Even in inpatient settings, however, the development of tolerance is still a problem, as dangerous and unpleasant withdrawal symptoms can result when the drug is stopped after dependence has developed.15 Older adults and pregnant women should consider the risks associated with barbiturate use. When a person ages, the body becomes less able to rid itself of barbiturates. As a result, people over the age of sixty-five are at higher risk of experiencing the harmful effects of barbiturates, including drug dependence and accidental overdose.19 When barbiturates are taken during pregnancy, the drug passes through the mother's bloodstream to her fetus. After the baby is born, it may experience withdrawal symptoms and have trouble breathing. In addition, nursing mothers who take barbiturates may transmit the drug to their babies through breast milk.20 Recreational misuse and abuse Like ethanol, barbiturates are intoxicating and produce similar effects during intoxication. The symptoms of barbiturate intoxication include respiratory depression, lowered blood pressure, fatigue, fever, unusual excitement, irritability, dizziness, poor concentration, sedation, confusion, impaired coordination, impaired judgment, addiction, and respiratory arrest which may lead to death.21 Recreational users report that a barbiturate high gives them feelings of relaxed contentment and euphoria. The main risk of acute barbiturate abuse is respiratory depression. Physical and psychic dependence may also develop with repeated use.22 Other effects of barbiturate intoxication include drowsiness, lateral and vertical nystagmus, slurred speech and ataxia, decreased anxiety, a loss of inhibitions. Barbiturates are also misused to alleviate the adverse or withdrawal effects of illicit drug misuse.2324 Drug abusers tend to prefer short-acting and intermediate-acting barbiturates.25 The most commonly abused are amobarbital Amytal, pentobarbital Nembutal, and secobarbital Seconal. A combination of amobarbital and secobarbital called Tuinal is also highly abused. Short-acting and intermediate-acting barbiturates are usually prescribed as sedatives and sleeping pills. These pills begin acting fifteen to forty minutes after they are swallowed, and their effects last from five to six hours. Veterinarians use pentobarbital to anesthetise animals before surgery; in large doses, it can be used to euthanise animals.7 Slang terms for barbiturates include; barbs, bluebirds, blues, downers, goofballs, ludes though this term is more commonly used for Quaaludes, 714s, tooties and yellow jackets.26 Legal status In the 1950s and 1960s, increasing reports began to be published about barbiturate overdoses and dependence problems which eventually led to the scheduling of barbiturates as controlled drugs. In 1970 several barbiturates were designated in the United States as controlled substances with the passage of the American Controlled Substances Act of 1970. Pentobarbital, secobarbital and amobarbital were designated schedule II drugs, butabarbital schedule III, and barbital and phenobarbital schedule IV. In 1971 the Convention on Psychotropic Substances was signed in Vienna. Designed to regulate amphetamines, barbiturates, and other synthetics, the treaty today regulates secobarbital, amobarbital, butalbital, cyclobarbital, and pentobarbital as schedule III, and allobarbital, methylphenobarbital, phenobarbital, and vinylbital as schedule IV scheduled substances. Examples Barbiturates Short Name R5 R5 Full Name Allobarbital CH2CHCH2 CH2CHCH2 5,5-diallylbarbiturate Amobarbital CH2CH3 CH2CH2CHCH32 5-ethyl-5-isopentyl-barbiturate Aprobarbital CH2CHCH2 CHCH32 5-allyl-5-isopropyl-barbiturate Alphenal CH2CHCH2 C6H5 5-allyl-5-phenyl-barbiturate Barbital CH2CH3 CH2CH3 5,5-diethylbarbiturate Brallobarbital CH2CHCH2 CH2CBrCH2 5-allyl-5-2-bromo-allyl-barbiturate Phenobarbital CH2CH3 C6H5 5-phenyl-5-ethylbarbiturate See also Pharmacy and Pharmacology portal Benzodiazepines References ^ a b Barbiturates. Retrieved on 2007-10-31. ^ Sneader, Walter 2005-06-23. Drug Discovery. John Wiley and Sons, 369. ISBN 0-471-89979-8. ^ Whitlock FA 14. Suicide in Brisbane, 1956 to 1973: the drug-death epidemic. Med J Aust 1 24: 737-43. PMID 239307. ^ Johns MW 1975. Sleep and hypnotic drugs. Drugs 9 6: 448-78. doi:10.2165/00003495-197509060-00004. PMID 238826. ^ Jufe GS Jul-Aug 2007. New hypnotics: perspectives from sleep physiology. Vertex 18 74: 294-9. PMID 18265473. ^ Barbiturates: How Is It Taken?. azdrugs.org 2005-2007. Retrieved on 2007-10-31. ^ a b c DEA Brief on Barbiturates ^ a b Brunton, Laurence L.; Lazo, John S.; Parker, Keith L.; Goodman, Louis Sanford; Gilman, Alfred Goodman. Goodman Gilman's Pharmacological Basis of Therapeutics. McGraw-Hill. ISBN 0071422803. ^ Kosten TR, O'Connor PG. Management of drug and alcohol withdrawal. New England Journal of Medicine. 2003 May 1;34818:1786-95. PMID 12724485 ^ Administration and Compounding Of Euthanasic Agents. Retrieved on 15 Jul 2008. ^ Daniel Engber. Why do lethal injections have three drugs?. Slate Magazine. Retrieved on 15 Jul 2008. ^ Neuroscience for Kids - Barbiturates. Retrieved on 6-2-2008. ^ Neil Harrison; Wallace B Mendelson and Harriet de Wit 2000. Barbiturates. Neuropsychopharmacology. Retrieved on 15 Jul 2008. ^ Society for Neurochemistry, American; George J. Siegel M.D., Bernard W. Agranoff M.D., Stephen K. Fisher Ph.D., R. Wayne Albers Ph.D., Michael D. Uhler Ph.D. 1998 1999. Part 2 Chapter 16, Basic Neurochemistry - Molecular, Cellular and Medical Aspects, Sixth ion, Lippincott Williams and Wilkins. ISBN 0-397-51820-X. Retrieved on Jul 2008. ^ a b Zapantis A, Leung S September 2005. Tolerance and withdrawal issues with sedation. Crit Care Nurs Clin North Am 17 3: 211-23. doi:10.1016/j.ccell.2005.04.011. PMID 16115529. ^ a b Takehiko Ito, Toshihito Suzuki, Susan E. Wellman and Ing Kang Ho June 1996. Pharmacology of barbiturate tolerance/dependence: GABAa receptors and molecular aspects. Life Sciences 59 3: 169-95. doi:10.1016/0024-32059600199-3. ^ Allan AM, Zhang X, Baier LD August 1992. Barbiturate tolerance: effects on GABA-operated chloride channel function. Brain Res. 588 2: 255-60. PMID 1382810. ^ Barbiturate intoxication and overdose. MedLine Plus. Retrieved on 15 Jul 2008. ^ WebMD. Toxicity, Barbiturate. eMedicine. Retrieved on 15 Jul 2008. ^ Nau H; Kuhnz W, Egger HJ, Rating D, Helge H Nov-Dec 1982. Anticonvulsants during pregnancy and lactation. Transplacental, maternal and neonatal pharmacokinetics. Clin Pharmacokinet 7 6: 508-43. doi:10.2165/00003088-198207060-00003. PMID 6819105. ^ National Institute on Drug Abuse. Commonly Abused Drugs 1. Retrieved on 15 Jul 2008. ^ Schlatter J; Sitbon N, Saulnier JL 17. Drugs and drug abusers. Presse Med 30 6: 282-7. PMID 11252979. ^ Emedicine Health. Barbiturate Abuse 1. Retrieved on 15 Jul 2008. ^ Faulkner TP; Hayden JH, Mehta CM, Olson DA, Comstock EG 1979. Dose-response studies on tolerance to multiple doses of secobarbital and methaqualone in a polydrug abuse population. Clin Toxicol 15 1: 23-37. PMID 498734. ^ Coupey SM. Barbiturates. Pediatrics in Review. 1997 Aug;188:260-4. PMID 9255991 ^ Hamid H; El-Mallakh RS, Vandeveir K Mar 2005. Substance Abuse: Medical and Slang Terminology. South Med J 98 3: 350-362. Medscape. doi:10.1097/01.SMJ.0000153639.23135.6A. PMID 15813163. External links U.S. Drug Enforcement Administration Source for some public domain text used on this page. History of Barbiturates v d e Barbiturates N01AF, N03AA, N05CA Allobarbital Alphenal Amobarbital Aprobarbital Barbexaclone Barbital Brallobarbital Brophebarbital Bucolome Butabarbital Butalbital Butobarbital Butallylonal Crotylbarbital Cyclobarbital Cyclopal Enallylpropymal Ethallobarbital Febarbamate Heptabarbital Hexethal Hexobarbital Mephobarbital Metharbital Methohexital Methylphenobarbital Narcobarbital Nealbarbital Pentobarbital Phenobarbital Phetharbital Prazitone Probarbital Propallylonal Proxibarbal Proxibarbital Reposal Secbutabarbital Secobarbital Sigmodal Spirobarbital Talbutal Thialbarbital Thiamylal Thiobarbital Thiobutabarbital Thiopental Valofane Vinbarbital Vinylbital Retrieved from http://en..org/wiki/Barbiturate Categories: Barbiturates Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages ÄŒesky Dansk Deutsch Español Français Galego Hrvatski עברית LatvieÅ¡u Bahasa Melayu Nederlands 日本語 ‪Norsk bokmÃ¥l‬ ‪Norsk nynorsk‬ Polski Português РуÑ?Ñ?кий SlovenÅ¡Ä?ina СрпÑ?ки / Srpski Suomi Svenska УкраїнÑ?ька This page was last modified on 30 August 2008, at 10:00
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