Creator: Dr. Osheen Kour
Published: 2022-12-29T17:52:47

Barbiturate drug intoxication acts as a central nervous system depressant causing sleepiness and relaxation. Read this article to know more.

Written by

Dr. Osheen Kour

Medically reviewed by

Dr. Kaushal Bhavsar

December 29, 2022

March 17, 2023

Introduction

Barbiturates belong to a sedative-hypnotics group of drugs. These addictive drugs cause physical dependency and life-threatening withdrawal symptoms. In addition, people consume Barbiturates on purpose or accidentally, which leads to drug overdose and fatal consequences. Barbiturates were mainly used to treat seizures, insomnia, headaches, and pre-operative sedatives. But these drugs are replaced with Benzodiazepines because of the side effects and overdose caused by Barbiturates. Therefore, Barbiturates can cause both physical and psychological addiction and dependency.

What Are the Common Names for Barbiturate Drugs?

Red devil.
Christmas tree.
Pinks.
Barbs.
Yellow jacket.
Goof balls.

What Is the History of Barbiturate Drug Abuse?

Barbiturates became popular for insomnia, seizure, and anxiety in the 1960s and 1970s. The drug was later used for recreational purposes to treat anxiety and other side effects.
After the 1970s, a new group of sedative-hypnotics called Benzodiazepines was. These new medications were extensively used as a replacement for Barbiturates in the medical profession except in some specific conditions.
This gradual decrease in the use of Barbiturates also reduced the substance abuse of the drug, thus minimizing its addiction.

What Are the Symptoms Caused by Barbiturate Toxicity?

The symptoms caused by Barbiturate toxicity are as follows:

Headache.
Confusion.
Gastrointestinal problem.
Ataxia (lack of coordination).
Drowsiness.
Sedation.
Respiratory depression.
Memory and motor skill impairment.

What Are the Side Effects Caused by Barbiturates?

The risk factors caused by Barbiturate toxicity are as follows:

Lightheadedness or dizziness.
Constipation.
Anxiety.
Irritability.
Nausea and vomiting.
Hangover effects.
Chest pain.
Fever.
Breathing difficulties.
Fainting sensation.

What Are the Different Types of Barbiturates?

Barbiturates are mainly of four types.

These include:

Ultra-Short Acting Barbiturates: Thiopental, Methohexital, and Thiamylal. These are usually taken intravenously and can cause anesthesia effects within a few minutes.
Short-Acting Barbiturates: Secobarbital and Pentobarbital. These are taken orally to induce sleep and sedation and produce effects within 15 to 30 minutes, lasting up to five to six hours.
Long-Acting Barbiturates: Mephobarbital and Phenobarbital. These are also taken orally to treat anxiety and seizures. They produce effects within an hour and last up to 12 hours.

What Are the Uses of Barbiturates Drugs?

Barbiturates are used for the following purposes:

Methohexital- This is mainly used as anesthesia for minor surgical and diagnostic procedures.
Phenobarbital- This Barbiturate medication is used to stop and treat seizures whenever they occur.
Pentobarbital- It is used as a pre-anesthesia and is also helpful to treat seizures.
Amobarbital is a short-acting medication for insomnia and is also used in some neurological tests for brain function.
Butalbital- It is a combination medication mainly consisting of Acetaminophen, Aspirin, Codeine, and Caffeine. The drug can treat migraines and headaches with these different combinations.
Secobarbital- This medication is usually ineffective against insomnia, and doctors also avoid prescribing it.
Primidone- The medication can treat seizures as it can prevent convulsions.

What Is the Mechanism of Action of Barbiturate Drugs?

Barbiturates work by inhibiting the GABA (gamma-aminobutyric acid) system leading to central nervous system depression. The GABA system consists of a chloride channel, and when Barbiturate interacts with GABA, these chloride ions enter the brain's cells for a prolonged period. Barbiturates alter the nerve impulses of the brain cells, thus causing depression of the nerve impulses and central nervous system.

The complications related to Barbiturate toxicity are as follows.

Barbiturates can reduce blood pressure and heart rate and may also cause cessation of breathing which can be fatal and life-threatening.
The drug can also affect the liver, thus altering the other drug effects and making them less effective.
Barbiturates increase the medical tolerance of the drugs at higher doses. However, it can cause drug dependency, which can be fatal if the drug is not taken longer.
Barbiturates lead to drug addiction on prolonged use despite having hazardous health effects and consequences.
The drugs affect fetal growth and development and cause harm to breastfeeding newborns.

How Is Barbiturate Toxicity Diagnosed?

Medical professionals can diagnose Barbiturate toxicity in the following ways:

Urine and blood test.
Chest x-rays.
ECG (electrocardiogram).
CT scan (computed tomography).

What Are the Treatment Options for Barbiturate Toxicity?

Barbiturate toxicity does not have any antidote treatment available.
First-line treatment for Barbiturate toxicity is mainly supportive in managing airway obstruction and circulation.
Intubation and mechanical ventilation support are provided if a person shows respiratory depression and sedation symptoms.
Activated charcoal therapy is done via a nasogastric tube to remove toxic substances from the stomach.
Severe cases of Barbiturates may also need hemodialysis and alkaline diuresis.
During the recovery phase, a person must be given counseling about Barbiturate misuse and overuse.

What Are the Contraindications of Barbiturates?

Barbiturates should not be taken with alcohol or other central nervous system depressants such as sleep medications, antihistamines, narcotics, muscle relaxants, or medicines for seizures. Multiple CNS depressants can lead to unconsciousness and death.
Barbiturates can produce side effects in children causing unusual excitement.
These drugs can also cause depression and confusion in older people.
Barbiturates have the potential to alter medical test results.
People with a history of drug abuse, mental depression, and suicidal tendencies should be administered Barbiturates carefully and cautiously.
Barbiturates are contraindicated in pregnancy because they can cause harm to the fetus and also produces withdrawal symptoms in newborn babies if a mother consumes Barbiturates in the last trimester of the pregnancy.
Breastfeeding mothers should also avoid Barbiturates as they can be present in breast milk, causing harm to newborns.

What Is the Differential Diagnosis for Barbiturate Toxicity?

Alcohol toxicity.
Benzodiazepine toxicity.
Hypoglycemia.
Myxedema coma.

What Are the Barbiturate Withdrawal Symptoms?

A person using Barbiturates for drug abuse should never stop consuming the drug instantly. It can be fatal, leading to the death of a person. The withdrawal symptoms include:

Stomach pain.
Seizures.
Nausea and vomiting.
Disorientation.
Hallucinations.
Hyperthermia (increased body temperature).
Restlessness.

Conclusion

Barbiturates are sedative medications that can relax the body. However, the drugs can cause severe health hazards and dependency with small doses. Barbiturates have a small therapeutic window which means even a tiny extra amount can cause a drug overdose. Although the drug is not commonly used these days due to alternative medications available. Cases of acute poisoning with Barbiturates are still experienced in many developing countries. Barbiturate toxicity can cause fatal health consequences and prolonged medical care; quitting the drug can enhance recovery from an overdose.

Frequently Asked Questions

1. What Is the Remedy for Toxicity Caused by Barbiturates?

The remedy for toxicity caused by barbiturates is typically focused on supportive care and addressing the symptoms. It involves maintaining vital functions, ensuring proper hydration, and providing necessary respiratory support. In severe cases, activated charcoal may be administered to limit absorption, and medical professionals may consider employing specific antidotes, such as Flumazenil, in cases of overdose or excessive sedation. Prompt medical attention and close monitoring are crucial in managing barbiturate toxicity.

2. What Are the Typical Adverse Effects of Barbiturates?

The typical adverse effects of barbiturates can vary depending on the specific drug and individual response. Common side effects may include drowsiness, sedation, dizziness, impaired coordination, confusion, and respiratory depression. Barbiturates can also lead to paradoxical reactions, such as excitability or agitation. Long-term use can result in tolerance, dependence, and potential withdrawal symptoms upon discontinuation. It is essential to monitor for these adverse effects and adjust the dosage or discontinue the medication as needed under medical supervision.

3. In What Situations Is Barbiturate Poisoning Employed?

Barbiturate poisoning is employed in specific situations, such as deliberate self-harm attempts, drug overdoses, or accidental ingestion. In emergency settings, it may be necessary to remove the barbiturates from the body through techniques like gastric lavage or administration of activated charcoal to limit absorption. Medical professionals may also administer supportive care, including airway management, ventilation, and intravenous fluids, to stabilize the individual and prevent further complications. Prompt medical attention is crucial to manage barbiturate poisoning effectively and minimize potential harm.

4. What Is the Mechanism Behind the Toxicity of Barbiturates?

The mechanism behind the toxicity of barbiturates is primarily related to their ability to enhance the inhibitory effects of the neurotransmitter Gamma-Aminobutyric Acid (GABA) in the central nervous system. Barbiturates bind to specific GABA receptors, leading to increased chloride ion influx into neurons, resulting in neuronal hyperpolarization and suppression of neuronal activity. However, excessive or prolonged use of barbiturates can disrupt the balance of neuronal activity, leading to adverse effects such as respiratory depression, sedation, and overdose. The exact mechanisms of barbiturate toxicity can also involve other pathways, including direct effects on ion channels and neurotransmitter release.

5. What Are the Examples of Barbiturates?

Three examples of barbiturates are Phenobarbital, Pentobarbital, and Secobarbital. Phenobarbital is commonly used as an anticonvulsant and sedative, while pentobarbital is primarily used for anesthesia induction and euthanasia in veterinary medicine. Secobarbital, also known as Seconal, is a short-acting barbiturate previously used as a sedative-hypnotic. These examples highlight the diverse range of barbiturates and their various medical applications.

6. What Classification of Drug Do Barbiturates Belong to?

Barbiturates belong to the classification of drugs known as central nervous system depressants. They act as sedatives, hypnotics, and anticonvulsants by depressing the activity of the central nervous system. Barbiturates work by enhancing the inhibitory effects of the neurotransmitter Gamma-Aminobutyric Acid (GABA), resulting in a decrease in neuronal activity and inducing sedation and relaxation. Due to their potential for abuse, barbiturates are classified as controlled substances and should be used cautiously under medical supervision.

7. What Is the Mode of Action of Barbiturates?

The action of barbiturates is primarily centered on enhancing the neurotransmitter Gamma-Aminobutyric Acid (GABA) activity in the brain. Barbiturates bind to specific GABA receptors, increasing chloride ion influx into neurons, resulting in neuronal hyperpolarization and decreased excitability. Depending on the therapeutic use, this leads to sedation, relaxation, and reduced anxiety or seizures. The action of barbiturates on GABAergic neurotransmission helps to promote calming and inhibitory effects in the central nervous system.

8. Which Diuretic Is Utilized in Cases of Barbiturate Poisoning?

There is no specific diuretic used in cases of barbiturate poisoning. Diuretics are not the primary treatment for barbiturate overdose or toxicity. The main focus of management involves supportive care, ensuring vital functions, and addressing symptoms. Activated charcoal may be administered to limit absorption, and specific antidotes like Flumazenil may be considered in cases of overdose or excessive sedation. The use of diuretics in barbiturate poisoning is not a recommended or standard approach.

9. What Is the Primary Impact of Barbiturates?

The major effect of barbiturates is depression of the Central Nervous System (CNS). Barbiturates act as potent sedatives and hypnotics, inducing a state of sedation, relaxation, and sleep. They can also produce varying levels of anesthesia, depending on the dosage and specific barbiturate used. Barbiturates have a depressant effect on neuronal activity, resulting in decreased brain function, reduced anxiety, and muscle relaxation. It is important to note that barbiturates should be used cautiously due to their potential for respiratory depression, overdose, and addiction.

10. Which Substance Was the First Barbiturate?

The first barbiturate is considered to be barbital, also known as Veronal. It was synthesized in 1903 by German chemist Emil Fischer and his colleagues. Barbital was the first compound in the barbiturate class to be discovered and introduced for medical use. It was initially used as a sedative and sleep aid. Still, its medical applications have since been largely replaced by other drugs due to safety concerns and the development of newer medications with improved efficacy and safety profiles.

11. How Do Barbiturates Influence the Neurotransmitter GABA?

Barbiturates enhance the activity of the neurotransmitter gamma-aminobutyric acid (GABA) in the brain. They bind to GABA receptors and increase the duration of GABA-mediated chloride ion channel opening, leading to increased inhibitory effects. This results in an overall decrease in neuronal excitability and a sedative effect. By enhancing GABAergic neurotransmission, barbiturates promote relaxation, reduce anxiety, induce sleep, and have anticonvulsant properties. The specific effects on GABAergic neurotransmission contribute to the therapeutic actions and potential side effects of barbiturates.

12. What Is the Most Common Purpose for Administering Barbiturates?

The most common use of barbiturates is sedatives or hypnotics to induce sleep or reduce anxiety. They are often prescribed for short-term management of insomnia or as pre-anesthetic medications before surgical procedures. Barbiturates can also be used as anticonvulsants to control seizures. However, their use in this context has diminished over time due to safety concerns and the availability of alternative medications with better risk profiles. It's important to note that using barbiturates for these purposes should be carefully monitored and limited due to the potential for dependence, tolerance, and adverse effects.

13. Which Barbiturate Is Used in Anesthesia?

Thiopental, also known as sodium thiopental, is the barbiturate commonly used in anesthesia. It is a short-acting barbiturate with a rapid onset of action, making it suitable for induction of anesthesia. Thiopental produces a state of deep sedation and hypnosis, allowing for the initiation of general anesthesia before administering other anesthetic agents. However, its use has declined recently, with many medical professionals opting for newer, safer anesthesia induction agents.

14. Is Serotonin Classified as a Barbiturate?

No, serotonin is not classified as a barbiturate. Serotonin is a neurotransmitter, a chemical messenger that transmits signals between nerve cells in the brain. Barbiturates, on the other hand, are a class of drugs that act as central nervous system depressants and have sedative, hypnotic, and anticonvulsant properties. While both serotonin and barbiturates can affect brain function and mood, they operate through different mechanisms and have distinct classifications in pharmacology.

15. Who Is Considered the Founding Figure of Barbiturates?

The discovery and development of barbiturates are attributed to Adolf von Baeyer, a German chemist often referred to as the father of barbiturates. Baeyer and his team synthesized barbituric acid in 1864, which served as the foundational compound for the subsequent development of barbiturates. Baeyer's work laid the groundwork for understanding the chemical structure and properties of barbiturates, leading to their later application as sedatives, hypnotics, and anticonvulsants in medicine. His contributions to the field of organic chemistry, including the discovery of barbiturates, earned him the Nobel Prize in Chemistry in 1905.

16. What Is the Origin of the Term Barbiturates?

Barbiturates are derived from barbituric acid, the initial compound discovered by Adolf von Baeyer. The term "barbiturate" combines "barbituric," referring to the chemical compound, and the suffix "-ate," is commonly used in chemistry to denote a salt or ester. This naming convention was adopted to categorize and identify this class of drugs, which share a similar chemical structure and pharmacological properties. The term "barbiturates" has since become synonymous with this specific group of compounds with sedative, hypnotic, and anticonvulsant effects.

17. How Do Barbiturates Affect the Functioning of the Liver?

Barbiturates can have various effects on the liver. Prolonged or excessive use of barbiturates can lead to liver damage or toxicity. The liver metabolizes barbiturates, and their breakdown products can strain liver function. Hepatotoxicity, characterized by liver inflammation and damage, is a potential side effect of long-term barbiturate use. Furthermore, barbiturates can induce hepatic enzymes, which can affect the metabolism of other medications, leading to potential drug interactions. Close monitoring of liver function is essential when using barbiturates, and their use should be avoided or carefully managed in individuals with pre-existing liver disease.

18. What Is the Mechanism of Action of Barbiturates in the Brain?

Barbiturates work in the brain by enhancing the neurotransmitter gamma-aminobutyric acid (GABA) activity. They bind to GABA receptors and facilitate the opening of chloride ion channels, leading to increased brain inhibitory signaling. This inhibitory effect results in a decrease in neuronal excitability and overall CNS depression. Barbiturates also modulate other neurotransmitter systems, such as glutamate and serotonin, further contributing to their sedative and hypnotic effects. By altering neurotransmitter balance and neuronal activity, barbiturates induce sedation, sleep and can have anticonvulsant properties.