Barbituric acid was first synthesized November 27, 1864, by German chemist Adolf von Baeyer. In 1912, Bayer introduced another barbituric acid derivative, phenobarbital, under the trade name Luminal, as a sedative-hypnotic. It was not until the 1950s that the behavioral disturbances and physical dependence potential of barbiturates became widely recognized, although some cases were noted as far back as the late 1930s in the UK and USA.
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, hypnotics, and anticonvulsants. Barbiturates also have analgesic effects; however, these effects are somewhat weak, preventing barbiturates from being used in surgery in the presence of other analgesics (opioids or volatile anesthetics such as halothane). In mice, barbiturates are hyperalgesic, increasing the sensitivity to pain. 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They have largely been replaced by benzodiazepines in routine medical practice, particularly in the treatment of anxiety and insomnia, due to the significant decrease in risk of overdose and the lack of an antidote for barbiturate overdose. Despite this, barbiturates are still in use for various purposes: in general anesthesia, epilepsy, treatment of acute migraines or cluster headaches, euthanasia, capital punishment, and assisted suicide. Barbiturates are derivatives of barbituric acid. Barbiturates such as phenobarbital were long used as anxiolytics and hypnotics, but today have been largely replaced by benzodiazepines for these purposes because of less potential for lethal overdoses. However, barbiturates are still used as anticonvulsants, as para-operative sedatives (e.g., sodium thiopental), and analgesics for cluster headaches and migraines.
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. Barbiturates are frequently employed as euthanizing agents in small-animal veterinary medicine.
Tolerance and dependence
With regular use, tolerance to the effects of barbiturates develops. As with all GABAergic drugs barbiturate withdrawal produces potentially fatal effects such as seizures in a manner reminiscent of delerium tremens and benzodiazepine withdrawal although its more direct mechanism of GABA agonism makes barbiturate withdrawal more severe than that of alcohol or benzodiazepines (subsequently making it one of the most dangerous withdrawals of any known addictive substance). 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.e. Valium), followed by slowly tapering off the benzodiazepine. Mental cravings for barbiturates can last for months or years in some cases and counselling/support groups are highly encouraged by addiction specialists. 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.
The unintended high it caused
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. 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 use, in a manner similar to long-acting benzodiazepines such as diazepam and clonazepam.
Barbiturates are also commonly used in suicide attempts.
The "1970 Barbiturates crisis"
These drugs were popular throughout the 1960’s and 1970’s in the UK, Ireland, France, the Netherlands, Sweden, Australia, Switzerland, France, W. Germany, Austria, Canada and the USA, but now are not often used by medical professionals due to the addiction and abuse issues. Major recreational abuse occurred in the USA since the mid 1960s and the UK in the late 1960s until the late 1970s, but some still occur in places.
The youth lead counter-culture of the 1960s spilled over into the following decade, colliding with the popular use of barbs and benzos by doctors. blow and acid were also popular amongst street users and Hippies at the time.
The British "1970 Barbiturates crisis" was a UK wide ~1968-78 crisis that had it's worst spell in 1970 and 1971. It involved users crawling in to secluded places like derelict basements and close tube stations to get high and begin later found dead amongst a pile of pills, usually barbiturates. The death toll was in it's thousands.
This lead to a crack down on their use, a short public education campaign, new legal classifications, GPs getting more reluctant to issue them and extended police powers.
A similar sort of crisis also hit several cities in the USA at abut the same time.
The 1971 Vienna Convention on Psychotropic Substances
In 1971, the Convention on Psychotropic Substances was signed in Vienna. Designed to regulate amphetamines, barbiturates, and other synthetics, the 34th version of the treaty, as of 25 January 2014, 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". The combination medication Fioricet, consisting of butalbital, caffeine, and paracetamol (acetaminophen), however, is specifically exempted from controlled substance status, while its sibling Fiorinal, which contains aspirin instead of paracetamol and may contain codeine phosphate, remains a schedule III drug.
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