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Christopher Evans
Christopher Evans


Barbiturates are drugs that cause relaxation and sleepiness. A barbiturate overdose occurs when someone takes more than the normal or recommended amount of this medicine. This can be by accident or on purpose. An overdose is life threatening.



Barbiturates are addictive. People who use them become physically dependent on them. Stopping them (withdrawal) can be life-threatening. Tolerance to the mood-altering effects of barbiturates develops rapidly with repeated use. But, tolerance to the lethal effects develops more slowly, and the risk of severe poisoning increases with continued use.

Barbiturates carry a risk of psychological and physical addiction. The risk of a fatal overdose is higher with barbiturates than other drugs as the difference between a safe dose and a deadly one is small.

A class of drugs known as benzodiazepines has largely replaced barbiturates for both medical and recreational use, although benzodiazepines also carry a high risk of physical dependence and other adverse effects. Examples include Valium and Ativan.

The first barbiturates were made in the 1860s by the Bayer laboratories in Germany. Barbiturates increase the activity of a chemical in the brain that helps transmit signals. This chemical is known as gamma amino butyric acid (GABA).

How quickly barbiturates act and how long their effects last can vary. They can be classified as ultra short-, short-, intermediate-, and long-acting. When people take barbiturates by mouth, their effects begin within 30 minutes of swallowing and last from 4 to 16 hours.

In the late 1950s and 1960s, there was an increase in reports of barbiturate overdoses and dependence problems, and physicians stopped prescribing them. Eventually, barbiturates were scheduled as controlled drugs.

Presently, barbiturates are nearly nonexistent on the black market. However, although illegal barbiturate use is rare, it remains an extremely dangerous drug to abuse because of the high risk of fatal overdose.

As a person uses barbiturates more, the difference between a dose that causes the desired effect and that of a fatal overdose becomes narrower. This makes overdoses more common in long-term use such as for more than 2 weeks.

Barbiturate withdrawal can also be fatal. Up to 75 percent of individuals withdrawing from a barbiturate may have one or more seizures, along with confusion and elevated body temperature. Up to 66 percent of people may experience delirium for several days.

Although widely used in the middle of the 20th century, present-day barbiturate use is uncommon. Some barbiturates are still made and sometimes prescribed for certain medical conditions. However, most barbiturate use has been replaced by the development of newer, safer, alternative drugs.

Barbiturates (except for the less-soluble phenobarbital) are mainly metabolized by the liver into inactive, water-soluble compounds by oxidation and then are renally excreted or conjugated to glucuronic acid and excreted in bile. The most significant aspect of the metabolism of barbiturates (e.g., phenobarbital, thiopental, methohexital) is their effect on the hepatic microsomal enzyme system (cytochrome P450 (CYP) enzymes). These effects are dependent on the duration of exposure to the barbiturate.Acutely, barbiturates interact with various CYPs and inhibit the biotransformation of other CYP substrates; likewise, other substrates (e.g., other drugs or endogenous substrates) can inhibit the barbiturate metabolism.Chronic use of barbiturates will cause upregulation, or induction, of the microsomal enzymes (CYPs 1A2, 2C9, 2C19, and 3A4), increasing the metabolism of drugs metabolized by these enzymes. This can lead to patients requiring larger dosages of medication to achieve therapeutic effect and/or increased clearance. This enzyme induction also causes barbiturate tolerance due increased barbiturate metabolism.In addition, barbiturates induce other enzymes, notably δ-aminolevulinic acid (ALA) synthetase. ALA synthetase is involved in the porphyrin production pathway, and therefore barbiturates are contraindicated in patients with acute intermittent porphyria (AIP) or variegate porphyria because they may precipitate an attack, manifested by severe abdominal pain, nausea, vomiting, psychiatric disorders, and neurologic abnormalities.

The primary mechanism of action of barbiturates is inhibition of the central nervous system. It causes central nervous system depression. This is brought about by stimulating the inhibitory neurotransmitter system in the brain called the [gamma]-aminobutyric acid (GABA) system.

The GABA channel is a Chloride channel that has five cells at its gate. When barbiturates bind to the GABA channel they lead to prolonged opening of the channel letting in Chloride ions into the cells in the brain. This leads to increased negative charge and alters the voltage in the brain cells.

Effective January 1, 2014, Medicare will cover barbiturates for any medically accepted indication. Therefore, effective January 1, 2014, the Medicaid program will no longer cover barbiturates prescribed for any condition when billed for full benefit Medicare/Medicaid dual eligibles. These drugs will be billed directly to the beneficiary's Part D plan or, when applicable, to Medicare Part B.

Barbiturates are classified as Schedule II substances, meaning they have definite potential for physical and psychological dependence and abuse. Barbiturates may be habit-forming. Tolerance, psychological dependence, and physical dependence may occur especially following prolonged use of high doses of barbiturates.

Barbiturates have a very narrow therapeutic index, meaning small differences in dose can result in big differences in the effects of the drug and patients can easily develop side effects. Combining barbiturates with other drugs such as opioids, benzodiazepines, antidepressants, or over-the-counter (OTC) medications with antihistamines could be fatal.

This medication contains barbiturates. Do not take barbiturates if you are allergic to amobarbital (Amytal), secobarbital (Seconal), butabarbital (Butisol), pentobarbital (Nembutal), belladonna and phenobarbital (Donnatal), butalbital/acetaminophen/caffeine (Esgic, Fioricet), and butalbital/aspirin/caffeine (Fiorinal Ascomp, Fortabs) or any ingredients contained in these drugs.

Barbiturates work by increasing the amount of gamma-aminobutyric acid (GABA) in the brain. GABA is an inhibitory neurotransmitter, so increasing its levels reduces nerve transmission. Because of this action, barbiturates can induce sleep, prevent seizures, reduce anxiety, and relieve muscle spasms.

Different types of barbiturates stay in the body for different lengths of time. Short-acting barbiturates have a shorter half-life and are eliminated faster. Longer-acting ones have a longer half-life and stay in the body longer. On drug tests, barbiturates can be detected in blood for 72 hours, in saliva for three days, in urine for up to six weeks, and in hair follicles for up to three months.

Other drugs that can interact with barbiturates include alcohol, anticoagulant medications, corticosteroids, sedatives, hypnotics, CNS depressants, and monoamine oxidase inhibitors (MAOIs). Always tell your doctor about any medications, substances, or supplements you are taking before taking barbiturates or any other medications.

Barbiturates are sedative-hypnotic drugs that were once commonly used as sedatives or anti-anxiety medications. A physician must prescribe barbiturates; otherwise, their use is considered illicit. Among their limited uses, barbiturates are used to manage some seizure disorders, as well as for pre-procedural sedation. In rarer instances, they are prescribed for the treatment of headaches, anxiety, and insomnia. However, their use in most areas of medicine has largely been supplanted by that of other, safer medications.

Phenobarbital has a relatively narrow therapeutic range, which means that the dose needs to be just right for it to be safe and effective. Those who take phenobarbital to control seizures are regularly tested to see if the drug concentration in their bodies is within the right range. For those abusing barbiturates like phenobarbital, their likelihood of visiting a doctor to test their drug levels is extremely low. These users are at high risk of quickly boosting the concentration of the drug in their bodies to toxic levels if they regularly misuse it.

Even in the short term, the effects of barbiturates, if taken in excess, can quickly reach dangerous and potentially deadly levels. Also, because barbiturates are often taken with other drugs such as alcohol, narcotic painkillers, and even stimulants, the risk is even higher.

Some people abuse these drugs because they desire the pleasant psychoactive effects of barbiturates, which are similar to those of alcohol. These effects include making the user feel happy, relaxed, more talkative, and less inhibited.

A person who is abusing barbiturates will exhibit signs that are similar in presentation to those of someone who is intoxicated by alcohol. Barbiturate side effects include, but certainly are not limited to the following:1,2,3

Prior to the 1970s, barbiturates were the drug of choice for the treatment of anxiety disorders and anxiety-related issues and for many types of seizure disorders. However, due to their potential for abuse, the federal government restricted access to barbiturates in 1970.2,6,7 Benzodiazepines (e.g. Xanax, Valium, Ativan, etc.) have largely assumed the role that barbiturates once played in treating anxiety. However, barbiturates are sometimes prescribed for certain patients, such as those with seizures disorders.

Since the restrictions on access to barbiturates were implemented, the number of individuals abusing these drugs has declined dramatically. Because of relatively scant data, the actual figures regarding the abuse of barbiturates are less reliable. However, we do know that: 041b061a72


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