
[BARBITUR(IC ACID) + -ATE2.]
USAGE NOTE When this class of drugs was introduced in the early part of this century, barbiturate had its main stress on the penultimate syllable, a pronunciation that is still used in the medical profession. As the word passed into the general vocabulary the stress shifted to the antepenultimate syllable, bringing the stress pattern more in line with words like acculturate, accurate, and saturate. Either pronunciation is considered correct now. Since at least the 1960s the pronunciation (bär-bĭch'ə-wĭt), without the second r, has been considered nonstandard despite the fact that it is quite common. In a recent survey 62 percent of the Usage Panel still disapprove of this pronunciation, while 38 percent approve of it, suggesting that the usage is becoming less stigmatized. One reason for this may be that the pronunciation without the second r is simply easier to say, since the combination (-ər-ĭt) occurs relatively infrequently in English. In addition, the presence of the first r may influence the dropping out of the second r by the phonological process of dissimilation.
For more information on barbiturate, visit Britannica.com.
A group of drugs widely used for the suppression of anxiety, the induction of sleep, and the control of seizures. Some of them, when injected intravenously, produce a general anesthesia. See also Anesthesia.
Barbituric acid, from which the various barbiturate congeners come, is a malonyl urea. Following the synthesis of this compound, a dozen or more closely related compounds were synthesized by adding or substituting various radicals to the general formula. The names of many of them have become familiar; examples are Phenobarbital, Meberal, Seconal, Nembutal, Amytal, and Pentothal.
These drugs act by suppressing the excitability of all tissues; but all tissues are not equally sensitive. Low dosages induce drowsiness, and high dosages coma and death. The spread between the therapeutic and fatal doses varies with the different barbiturates.
The prolonged use of these drugs results in habituation; and insomnia, agitation, confusional psychosis, and seizures may occur within 24 to 36 hours of withdrawal. Overdose is one of the commonest means of suicide in Western countries, and life can be saved only by admission to a hospital where respiration can be maintained and cerebral anoxia prevented.
Barbiturates are a group of drugs derived from barbituric acid. Barbiturates act as depressants of the central nervous system and have powerful sedative and anxiety-reducing properties. They have been commonly used in sleeping pills and to help people to relax. One of their side-effects is to interfere with the ability to perform complex skills. Barbiturates are habit-forming and prolonged use may lead to addiction.
| bambuterol hydrochloride, balsalazide sodium, balanced salt solution | |
| barrier preparations, basiliximab, becaplermin |
Drugs derived from barbituric acid. Barbiturates are depressants of the central nervous system, and have powerful anxiolytic and sedative properties. They have been commonly used in sleeping pills. Their effects are likely to disrupt the performance of complex motor skills. Habitual use of barbiturates can result in a true addiction.
The drugs differ widely in the duration of their action, which depends on the rapidity with which they are distributed in body tissues, degraded, and excreted. Ultrashort-acting barbiturates such as thiopental sodium (Pentothal) are often used as general anesthetics. Secobarbital (Seconal) and pentobarbital sodium (Nembutal) are short-acting barbiturates, amobarbital (Amytal) is intermediate in duration of action, and phenobarbital (Luminal) is a long-acting derivative.
Barbiturates are used to relax patients before surgery, as anticonvulsants, and as sleeping pills. They also are commonly abused. Taken regularly, barbiturates can be psychologically and physically addictive (see drug addiction and drug abuse). Barbiturate addicts must be withdrawn from the drug gradually to avoid severe withdrawal symptoms such as convulsions. Overdose can cause coma or death. In the United States the manufacture and distribution of barbiturates were brought under federal control by the 1965 Drug Abuse and Control Act, and they are legally available only by prescription.
Bibliography
See publications of the Drugs & Crime Data Center and Clearinghouse, the Bureau of Justice Statistics Clearinghouse, and the National Clearinghouse for Alcohol and Drug Information.
Substances derived from an organic compound that are used as sedatives and sleep inducers. Barbiturates, which work by depressing the activity of the central nervous system, are sometimes used in the treatment of illnesses such as epilepsy.
| barbital, bar, banding density | |
| barn, barnase, barometer |
Any of a group of organic compounds derived from barbituric acid. There are a number of barbiturates. They all depress the nervous system and are used to induce apathy and sleep, and in high doses, as anesthetics. They vary in their sedative effects, in the duration of their effectiveness and in their toxicity. Those that are used in veterinary medicine are: (1) pentobarbital sodium (Nembutal); largely superseded, but still sometimes used for intravenous anesthesia in companion animals; (2) thiopental sodium, which has a short period of effectiveness, an advantage in many veterinary situations, e.g. examination of a pharynx; (3) thialbarbital sodium, a medium length compound; (4) thiamylal sodium, a compound with ultrashort action.
A derivative of barbituric acid that acts as a sedative or hypnotic. Barbiturates are controlled substances that have addictive potentials.

Barbiturates are drugs that act as central nervous system depressants, and can therefore produce a wide spectrum of effects, from mild sedation to total anesthesia. They are also effective as anxiolytics, as hypnotics, and as anticonvulsants. Barbiturates also have analgesic effects, however these effects are somewhat weak, preventing barbiturates from being used in surgery in the absence of other analgesics. They have addiction potential, both physical and psychological. Barbiturates have now largely been replaced by benzodiazepines in routine medical practice - for example, in the treatment of anxiety and insomnia – mainly because benzodiazepines are significantly less dangerous in overdose. However, barbiturates are still used in general anesthesia, for epilepsy, and assisted suicide.[1] Barbiturates are derivatives of barbituric acid.[2]
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Barbituric acid was first synthesized December 6, 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 feast of Saint Barbara—the patron saint of artillerists. An artillery officer is said to have christened the new substance by amalgamating Barbara with urea.[3] Another story holds that Von Baeyer synthesized the substance from the collected urine of a Munich waitress named Barbara.[4] No substance of medical value was discovered, however, until 1903 when two German scientists 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.[3]
It was not until the 1950s that the behavioural disturbances and physical dependence potential of barbiturates became recognized.[5]
While barbituric acid itself does not have any direct effect on the central nervous system, chemists have derived over 2,500 compounds from it that possess pharmacologically active qualities. The broad class of barbiturates is further broken down and classified according to speed of onset and duration of action. Ultrashort-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, owing to the dangers of long-term use of barbiturates; they have been replaced by the benzodiazepines for these purposes. The final class of barbiturates are known as long-acting barbiturates (the most notable one being 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 prescribed for daytime sedation. Barbiturates in this class are not used for insomnia, because, owing to their extremely long half-life, patients would awake with a residual "hang-over" effect and feel groggy.
Barbiturates can in most cases be used either as 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.[6]
Barbiturates such as 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.[7][8][9]
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.[10][11] Thiopental is an ultra-short acting barbiturate that is marketed under the name sodium pentothal. It is often mistaken for "truth serum" or sodium amytal, an intermediate-acting barbiturate that is used for sedation and to treat insomnia, but was also used in so-called sodium amytal "interviews" where the person being questioned would be much more likely to provide the truth whilst under the influence of this drug. When dissolved in water, sodium amytal can be swallowed, or it can be 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]
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 beta 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.[13] Barbiturates produce their pharmacological effects by increasing the duration of chloride ion channel opening at the GABAA receptor (pharmacodynamics: This increases the efficacy of GABA), whereas benzodiazepines increase the frequency of the chloride ion channel opening at the GABAA receptor (pharmacodynamics: This increases the potency of GABA). The direct gating or opening of the chloride ion channel is the reason for the increased toxicity of barbiturates compared to benzodiazepines in overdose.[14][15]
Further, barbiturates are relatively non-selective compounds that bind to an entire superfamily of ligand-gated ion channels, of which the GABAA receptor channel is only one of several representatives. This superfamily of ion channels includes the neuronal nAChR channel, the 5HT3R channel, the GlyR channel and others. However, while GABAA receptor currents are increased by barbiturates (and other general anaesthetics), ligand-gated ion channels that are predominantly permeable for cationic ions are blocked by these compounds. For example, neuronal nAChR channels are blocked by clinically relevant anaesthetic concentrations of both thiopental and pentobarbital.[16] Such findings implicate (non-GABA-ergic) ligand-gated ion channels, e.g. the neuronal nAChR channel, in mediating some of the (side) effects of barbiturates.[17]
Older adults and pregnant women and babies 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.[18] 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.[19]
With regular use, tolerance to the effects of barbiturates develops.
Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness, shallow breathing, staggering, and in severe cases coma and death. The lethal dosage of barbiturates varies greatly with tolerance and from one individual to another. The amount of 1 g in dose orally can be highly poisonous with dosages from 2g to 10 g being generally fatal depending on the person tolerance level. 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. Barbiturates in overdose with other CNS (central nervous system) depressants for example, alcohol, opiates or benzodiazepines is even more dangerous due to additive CNS and respiratory depressant effects. In the case of benzodiazepines not only do they have additive effects, barbiturates also increase the binding affinity of the benzodiazepine binding site thus leading to an exaggerated effect of benzodiazepines.
Marilyn Monroe and Judy Garland both died of barbiturate overdose.
A rare adverse reaction to barbiturates is Stevens–Johnson syndrome, which primarily affects the mucous membranes.
Barbiturates produce effects similar to ethanol 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.[20]
Recreational users[who?] 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 psychological dependence may also develop with repeated use.[21] Other effects of barbiturate intoxication include drowsiness, lateral and vertical nystagmus, slurred speech and ataxia, decreased anxiety, a loss of inhibitions. Barbiturates are also used to alleviate the adverse or withdrawal effects of illicit drug misuse.[22][23]
Drug users tend to prefer short-acting and intermediate-acting barbiturates.[24] 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.[25]
Slang terms for barbiturates include barbs, bluebirds, dolls, downers, goofballs, sleepers and tooties.[26]
In the 1940s, military personnel were given "Goofballs" during WWII in the South Pacific region to allow soldiers to tolerate the heat and humidity of daily working conditions. Goofballs were distributed to lower the respiratory system and blood pressure to combat the extreme conditions. Many soldiers returned with addictions that required several months of rehabilitation before discharge. This led to addiction problems through the 1950s and 1960s.
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.
In 1988, the synthesis and binding studies of an artificial receptor binding barbiturates by 6 complementary hydrogen bonds was published.[27] Since this first article, different kind of receptors were designed, as well as different barbiturates and cyanurates, not for their efficiencies as drugs but for applications in supramolecular chemistry, in the conception of materials and molecular devices.
| Short Name | R1 | R2 | IUPAC Name |
|---|---|---|---|
| Allobarbital | CH2CHCH2 | CH2CHCH2 | 5,5-diallylbarbiturate |
| Amobarbital | CH2CH3 | CH2CH2CH(CH3)2 | 5-ethyl-5-isopentyl-barbiturate |
| Aprobarbital | CH2CHCH2 | CH(CH3)2 | 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-ethyl-5-phenylbarbiturate |
| Look up barbiturate in Wiktionary, the free dictionary. |
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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
Dansk (Danish)
n. - barbiturat
Nederlands (Dutch)
slaappil, barbituraat
Français (French)
n. - barbiturique
Deutsch (German)
n. - Schlaftablette, Barbiturat
Ελληνική (Greek)
n. - βαρβιτουρικό
Italiano (Italian)
barbiturico
Português (Portuguese)
n. - barbiturato (m) (Quím.)
Español (Spanish)
n. - barbitúrico
Svenska (Swedish)
n. - barbiturat, sömntablett
中文(简体)(Chinese (Simplified))
巴比妥酸盐
中文(繁體)(Chinese (Traditional))
n. - 巴比妥酸鹽
한국어 (Korean)
n. - 바르비투르산염 유도제[진정제, 수면제]
日本語 (Japanese)
n. - バルビツール酸塩, バルビツール剤
العربيه (Arabic)
(الاسم) نوع من المخدرات
עברית (Hebrew)
n. - תרופת הרגעה
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