Author: Charles Frank

Barbiturates: Usage, Effects, and Signs of Barbiturate Overdose

A key reason why healthcare providers don’t prescribe barbiturates as often now is the risk of misusing them. Because of that risk, you should keep these medications under lock and key in a secure place in your home. Keeping them out of the hands of children and teenagers is essential. Acting cautiously can help avoid accidental poisoning or recreational misuse of these medications, both of which can have deadly consequences. While barbiturates are useful for the above listed, some of these uses are less common in certain countries. For example, barbiturates are less common for pre-anesthesia in the United States because many newer drugs are more effective and have fewer side effects.

Barbiturates became known as “goofballs” about the time of World War II, when they were used to help soldiers cope with combat conditions. Between the 1940s and ’70s, however, the abuse of barbiturate drugs became highly prevalent in Western societies. In North America barbiturates were widely used by youth gangs and deviant subcultures as depressants and attracted notoriety because they were often taken in combination with other substances (e.g., stimulants such as amphetamines). Alcohol greatly intensifies the depressant effect of barbiturates, and in the 1950s and ’60s, barbiturates taken with alcohol became a common agent in suicide cases. The use and availability of barbiturates in the United States declined steeply following the federal Comprehensive Drug Abuse Prevention and Control Act of 1970. As a street drug, barbiturates were largely replaced by other substances during the 1970s, especially by PCP.

However, barbiturates are still proven medications for treating many conditions. They also combine well with other medications like acetaminophen (Tylenol® or Paracetamol®) to treat certain conditions. Today, barbiturates are generally only used to treat extreme and serious cases of insomnia. They are also used to help control seizures in epilepsy, as well as an adjunct to anesthesia in some cases. If you suspect that someone has overdosed on barbiturates, seek medical attention immediately. Barbiturates became popular during the 1960s and 1970s in treating seizures, sleep problems, and anxiety.

1. 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.
2. Ingeborg Bachmann may have died of the consequences of barbiturate withdrawal (she was hospitalized with burns, the doctors treating her not being aware of her barbiturate addiction).
3. This Cys-loop receptor superfamily of ion channels includes the neuronal nACh receptor channel, the 5-HT3 receptor channel, and the glycine receptor channel.
4. The use of barbiturates declined after the introduction of benzodiazepines.
5. It has also been used to treat anxiety, drug withdrawal (particularly from other barbiturates), and sleep aid.
6. Barbiturates induce a number of hepatic CYP enzymes (most notably CYP2C9, CYP2C19, and CYP3A4),[22] leading to exaggerated effects from many prodrugs and decreased effects from drugs which are metabolized by these enzymes to inactive metabolites.

The Misuse of Drugs Act classifies barbiturates as class B drugs, which means that these drugs can be bought in accordance with a doctor’s prescription; however, any other form of possession or supply of barbiturates is considered an offense. The maximum penalty that a person can receive for any unauthorized possession of barbiturates is 5 years in prison and a fine for possession. Low doses of barbiturates can lower anxiety levels and relieve tension. Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation. All barbiturates affect gamma-aminobutyric acid (GABA), a neurotransmitter (chemical) that nerves use to communicate with one another.

(ex. If a benzodiazepine increases the frequency of channel opening by 300%, and a barbiturate increases the duration of their opening by 300%, then the combined effects of the drugs increases the channels’ overall function by 900%, not 600%). To this end, tolerance occurs when larger doses than the original dose are required to produce the same effects. This can increase the risk of overdose, signs of which include shallow breathing, rapid and weak pulse, dilated pupils, clammy skin, coma, and even death as a result of the severe depression of both the CNS and respiratory system.

This barbiturate was used to treat seizures in young children due to its effectiveness as an anticonvulsant. It has also been used to treat anxiety, drug withdrawal (particularly from other barbiturates), and sleep aid. The use of barbiturates declined after the introduction of benzodiazepines.

Thiopental is relatively short-acting and is used to induce anesthesia before general anesthetics are given. The prolonged use of barbiturates—especially secobarbital and pentobarbital—may cause the development of a tolerance to them and require amounts much larger than the original therapeutic dose. Denial of a barbiturate to the habitual user may precipitate a withdrawal syndrome that is indicative of physiological dependence on the drug. An overdose of barbiturates can result in coma and even death due to severe depression of the central nervous and respiratory systems.

Classification

Some barbiturates are also used to relieve tension or anxiety prior to surgery. Barbiturates also easily produce tolerance, meaning it takes more of the drug to produce the same effects. Signs of a barbiturate overdose include clammy skin, dilated pupils, shallow respiration, rapid and weak pulse, and coma. These drugs are sometimes prescribed to help reduce anxiety and induce sleep, but they can also be dangerous and habit-forming.

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 and Z-drug such as zolpidem, zaleplon and eszopiclone for sleep. 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. Research shows tolerance can develop with even one administration of a barbiturate.

When should I see my healthcare provider?

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. The lethal dose is highly variable among different members of the class, with superpotent barbiturates such as pentobarbital being potentially fatal in considerably lower doses than the low-potency barbiturates such as butalbital. Even in inpatient settings, 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, such as phenobarbital, were long used as anxiolytics and hypnotics. Intermediate-acting barbiturates reduce time to fall asleep, increase total sleep time, and reduce REM sleep time. People who use substances tend to prefer short-acting and intermediate-acting barbiturates.[43] The most commonly used are amobarbital (Amytal), pentobarbital (Nembutal), and secobarbital (Seconal). A combination of amobarbital and secobarbital (called Tuinal) is also highly used.

Used as an anesthetic in animals, this drug formerly used to treat seizures and convulsions has the dubious distinction of being one of the preferred drugs used for state executions in the U.S. This short-acting barbiturate is frequently used to treat migraine headaches, often combined with acetaminophen, aspirin, and caffeine. You are encouraged to report negative side effects of prescription drugs to the FDA. The theory was that someone asked a question while under the influence of amobarbital would be less likely to be able to think of a false answer, which requires more focus than simply telling the truth. Benzodiazepines have largely replaced barbiturates in most medical uses.

For more information on drug interactions, visit the RxList Drug Interaction Checker. Barbiturates are medications used for treating headaches, insomnia, and seizures. Barbiturates have some risks, but these risks should be minimal if you take your medication exactly as prescribed. You also shouldn’t have a problem with barbiturate dependence if you take your medication as your healthcare provider instructs.

Sleep Disorders: Insomnia, Sleep Apnea, and More

Barbiturates of intermediate duration of action, such as amobarbital and butabarbital sodium, act for 6 to 12 hours and are used to relieve insomnia. Short-acting barbiturates, such as pentobarbital and secobarbital, are used to overcome difficulty in falling asleep. Ultrashort-acting barbiturates, such as thiopental sodium and thiamylal, are used intravenously to induce unconsciousness smoothly and rapidly in patients about to undergo surgery, after which gaseous anesthetics are used to maintain the unconscious state.

The most common uses are for anesthesia reasons, treating epilepsy and nonepileptic seizures, insomnia and other conditions. Barbiturates are sedative-hypnotic medications, meaning they cause you to feel relaxed or sleepy. For over a century, they’ve treated many conditions, including seizures, migraines, insomnia and more. They’re less common today because of the risk of misuse and certain side effects.

How Many Types of Insomnia Are There?

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. Barbiturates are synthetic drugs used in medicine to depress the central nervous system (CNS). The effects of barbiturates range from mild sedation to coma, with their indications ranging from sedatives, hypnotics, or as part of anesthesia.