Barbiturates

Barbiturates

Barbiturates

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You could also do it yourself at any point in time. Would you like Wikipedia to always look as professional and up-to-date? We have created a browser extension. It will enhance any encyclopedic page you visit with the magic of the WIKI 2 technology. They are also effective as anxiolytics , hypnotics , and anticonvulsants. Barbiturates have addiction potential, both physical and psychological. They have largely been replaced by benzodiazepines in routine medical practice, particularly in the treatment of anxiety and insomnia, due to the significant lower risk of overdose and the lack of an antidote for barbiturate overdose. Despite this, barbiturates are still in use for various purposes: Barbiturates such as phenobarbital were long used as anxiolytics and hypnotics , but today have been largely replaced by benzodiazepines for these purposes because the latter are less toxic in overdose. 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 and slow creative thinking, making subjects more likely to be caught off guard when questioned, and increasing the possibility of the subject revealing information through emotional outbursts. This practice is no longer considered legally admissible in court due to findings that subjects undergoing such interrogations may form false memories, putting the reliability of all information obtained through such methods into question. Nonetheless, it is still employed in certain circumstances by defense and law enforcement agencies as a 'humane' alternative to torture interrogation when the subject is believed to have information critical to the security of the state or agency employing the tactic. There are special risks to consider for older adults, women who are pregnant, and babies. 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. 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. With regular use, tolerance to the effects of barbiturates develops. Similar to benzodiazepines the longer acting barbiturates produce a less severe withdrawal syndrome than short acting and ultra short acting barbiturates. Withdrawal symptoms are dose-dependent with heavier users being affected worse than lower-dose addicts. The pharmacological treatment of barbiturate withdrawal is an extended process often consisting of converting the patient to a long acting benzodiazepine i. Valium , followed by slowly tapering off the benzodiazepine. Patients should never try to tackle the task of discontinuing barbiturates without consulting a doctor due to the high lethality and relatively sudden onset of the withdrawal, attempting to quit 'cold turkey' may result in serious neurological damage, severe physical injuries received during convulsions, and even death via glutamatergic excitotoxicity. Some symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgement, drowsiness, shallow breathing, staggering, and, in severe cases, coma or death. 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. Tolerance to the anxiolytic and sedative effects of barbiturates tends to develop faster than tolerance to their effects on smooth muscle, respiration, and heart rate, making them generally unsuitable for a long time psychiatric use. Tolerance to the anticonvulsant effects tends to correlate more with tolerance to physiological effects, however, meaning that they are still a viable option for long-term epilepsy treatment. Barbiturates in overdose with other CNS central nervous system depressants e. In the case of benzodiazepines, not only do they have additive effects, barbiturates also increase the binding affinity of the benzodiazepine binding site, leading to exaggerated benzodiazepine effects. The longest-acting barbiturates have half-lives of a day or more, and subsequently result in bioaccumulation of the drug in the system. Users who consume alcohol or other sedatives after the drugs effects have worn but before it has cleared the system may experience a greatly exaggerated effect from the other sedatives which can be incapacitating or even fatal. This can result in fatal overdoses from drugs such as codeine , tramadol , and carisoprodol , which become considerably more potent after being metabolized by CYP enzymes. Although all known members of the class possess relevant enzyme induction capabilities the degree of inhibition overall as well as the impact on each specific enzyme span a broad range with phenobarbital and secobarbital being the most potent enzyme inducers and butalbital and talbutal being among the weakest enzyme inducers in the class. Barbiturates bind to the GABA A receptor at multiple homologous transmembrane pockets located at subunit interfaces, \\\\\\\\\\\\\\\[16\\\\\\\\\\\\\\\] 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. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. 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. Further, barbiturates are relatively non-selective compounds that bind to an entire superfamily of ligand-gated ion channels, of which the GABA A receptor channel is only one of several representatives. However, while GABA A 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. There are several stories about how the substance got its name. An artillery officer is said to have christened the new substance by amalgamating Barbara with urea. It is said that Mering proposed this name because the most peaceful place he knew was the Italian city of Verona. It was not until the s that the behavioural disturbances and physical dependence potential of barbiturates became recognized. 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. 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 , Bayer introduced another barbituric acid derivative, phenobarbital , under the trade name Luminal, as a sedative - hypnotic. Goofballs were distributed to reduce the demand on the respiratory system, as well as maintaining blood pressure, to combat the extreme conditions. Many soldiers returned with addictions that required several months of rehabilitation before discharge. This led to growing dependency problems, often exacerbated by indifferent doctors prescribing high doses to unknowing patients through the s and s. In the late s and s, increasing published reports of barbiturate overdoses and dependence problems led physicians to cut back their prescription, particularly for spurious requests. This eventually led to the scheduling of barbiturates as controlled drugs. There is a small group of List II drugs for which doctors have to write the prescriptions according to the same, tougher guidelines as those for List I drugs writing the prescription in full in letters, listing the patients name, and have to contain the name and initials, address, city and telephone number of the licensed prescriber issuing the prescriptions, as well as the name and initials, address and city of the person the prescription is issued to. Among that group of drugs are the barbiturates amobarbital , butalbital , cyclobarbital , and pentobarbital. Under the original CSA, no barbiturates were placed in schedule I, II, or V, \\\\\\\\\\\\\\\[27\\\\\\\\\\\\\\\] however amobarbital, pentobarbital, and secobarbital are schedule II controlled substances unless they are in a suppository dosage form. Designed to regulate amphetamines , barbiturates, and other synthetics, the 34th version of the treaty , as of 25 January \\\\\\\\\\\\\\\[update\\\\\\\\\\\\\\\] , regulates secobarbital as schedule II, amobarbital, butalbital, cyclobarbital, and pentobarbital as schedule III, and allobarbital , barbital , butobarbital , mephobarbital , phenobarbital , butabarbital , and vinylbital as schedule IV on its 'Green List'. Recreational users report that a barbiturate high gives them feelings of relaxed contentment and euphoria. Physical and psychological dependence may also develop with repeated use. Barbiturates are also used to alleviate the adverse or withdrawal effects of illicit drug use, in a manner similar to long-acting benzodiazepines such as diazepam and clonazepam. Drug users tend to prefer short-acting and intermediate-acting barbiturates. A combination of amobarbital and secobarbital called Tuinal is also highly used. 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. Sodium barbital and barbital have also been used as pH buffers for biological research, e. To install click the Add extension button. Try it — you can delete it anytime. Every page goes through several hundred of perfecting techniques; in live mode. Quite the same Wikipedia. Barbiturates were ranked 5th in dependence, 3rd in physical harm, and 4th in social harm. Generic structure of a barbiturate, including numbering scheme. Harvard University Linguistics Department. Archived from the original on 21 July Yakatan 21 Sep Journal of Pharmaceutical Sciences. Vertex Buenos Aires, Argentina in Spanish. Archived from the original on 7 June Retrieved 15 July Archived from the original on 25 July Archived from the original on 16 June Archived from the original on 20 July Transplacental, maternal and neonatal pharmacokinetics'. Journal of Biological Chemistry. Barbiturates therefore promote entry of GABA-activated channels into a long-lived open state, whereas \\\\\\\\\\\\\\\[benzodiazepines\\\\\\\\\\\\\\\] increase only the frequency of channel opening into the initial open state. These mechanistic studies reveal interesting details of the changes in channel gating caused by barbiturates but as yet have yielded no insights into the molecular sites of action. An additional interesting effect of barbiturates is direct gating of the channels, i. This usually occurs at significantly higher concentrations than those that potentiate the actions of GABA; these concentrations also are generally higher than those required for clinically effective anesthesia. Wayne Albers; Michael D. Lippincott Williams and Wilkins. Check date values in: Archived from the original on 7 November United States of America: American Psychiatric Publishing Inc. John Wiley and Sons. International Narcotics Control Board. Retrieved 19 December Archived from the original on 2 August Synthesis of an artificial receptor for barbiturates employing six hydrogen bonds'. Journal of the American Chemical Society. Retrieved 28 July Retrieved 21 December Ethotoin Fosphenytoin Mephenytoin Phenytoin ; Ureides: Lacosamide Lamotrigine Rufinamide Topiramate Zonisamide. Ethadione Paramethadione Trimethadione ; Succinimides: Ethosuximide Mesuximide Phensuximide ; Gabapentinoids: Gabapentin Pregabalin ; Others: Imepitoin Lamotrigine Topiramate Zonisamide. Acetazolamide Ethoxzolamide Sultiame Topiramate Zonisamide. Agomelatine Bupropion Tianeptine Vilazodone Vortioxetine. Glutethimide Methyprylon Pyrithyldione Piperidione. Agomelatine Melatonin Ramelteon Tasimelteon. Eszopiclone Zaleplon Zolpidem Zopiclone ; Others: Glutethimide Methyprylon Piperidione Pyrithyldione. Ranolazine Antiarrhythmics class I: Conotoxins Neosaxitoxin Saxitoxin Tetrodotoxin Others: Atracotoxins Robustoxin , Versutoxin Ciguatoxins Poneratoxin. Neomycin Spermidine Spermine ; Other positive allosteric modulators: This page was last edited on 31 October , at Basis of this page is in Wikipedia. Non-text media are available under their specified licenses. Main page Contents Featured content. Look up barbiturate in Wiktionary, the free dictionary. Blockers K ATP -specific: Blockers BK Ca -specific: Blockers Amiloride Benzamil Triamterene. Blockers Glibenclamide Lonidamine Piretanide. TRPs See here instead.

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