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Barbiturates

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CONTENTS

Barbiturates are central nervous system depressants that are used as anticonvulsants, sedative-hypnotics, and anesthetics. Barbiturates are classified as controlled drugs in the United States which means that they have significant potential for abuse and addiction and should be used as prescribed by the doctor. Barbiturates are extremely dangerous due to a narrow window of safe use and this puts these drugs at an increased risk of an overdose which can be life-threatening.

Barbiturates belong to the class of sedative-hypnotic drugs that were introduced in the late 19^th century by the Bayer laboratories in Germany and they became popular as sleeping pills. Barbiturates are derivatives of barbituric acid and these drugs are used to treat anxiety, insomnia, headache, and seizures. Barbiturates may also be used for induction of anesthesia in a pre-operative setting. However, in the 1960s and 1970s barbiturates were immensely used as recreational drugs that lead to their abuse and increased the risk of overdose.

Barbiturates Intoxication and Overdose

Barbiturates are quite dangerous because they a have narrow therapeutic index. The therapeutic index is the ratio of the dose of the drug that is toxic to the dose of the drug that is therapeutic. This means that there is very little difference in the dose of barbiturates that causes sedation as for medical purposes and the one that causes death therefore they are not routinely prescribed nowadays.

Barbiturates are classified as Schedule II, III, and IV controlled substances in the United States depending on the type of drug and the form of the drug in which it is used since these drugs carry increased risk of physical and psychological dependence which eventually leads to addiction and abuse. However, barbiturates have largely been replaced by a newer class of drugs called benzodiazepines due to their safer drug profile, albeit they too possess the potential for addiction and abuse.

Barbiturates are central nervous system depressants and they bring about their action by interfering with the prime inhibitory neurotransmitter GABA; stimulating its inhibitory effect by impeding the nerve conduction and reducing the activity of the brain.

This action of barbiturates results in a calming effect on the entire body identical to that produced by alcohol and causes muscle relaxation with reduced heart rate, low blood pressure, and shallow breathing. Barbiturates also exert their effect on the respiratory centers in the brain along with simultaneously influencing the cardiovascular system. Moreover, it also numbs the sensation of pain providing analgesia, and also causes loss of consciousness by impairing the activity of the central nervous system.

Barbiturates are classified based on their duration of action. Following is the classification of barbiturates:

Ultra-Short-Acting Barbiturates: These drugs have an immediate onset of action that beings within minutes and their effect lasts for a very short duration. These types of barbiturates are used for inducing anesthesia in a hospital setting. This category includes Thiopental (Pentothal), Thiamylal (Surital), and Methohexital (Brevital).

Short-Acting Barbiturates: These drugs have a rapid onset of action that begins in 10 to 15 minutes and the effect lasts for 3 to 4 hours. These types of barbiturates are used as sedatives.
Intermediate-Acting Barbiturate: Their onset of action begins in 45 to 60 minutes and the effect lasts for 6 to 8 hours. These types of barbiturates are used for imparting sleep.

Short-acting and intermediate-acting benzodiazepine include Phenobarbital (Nembutal) and Secobarbital (Amytal). These drugs are classified as Schedule II drugs. Other short and intermediate-acting barbiturates that are Schedule III drugs include Butalbital (Fiorinal), Butabarbital (Butisol), and Aprobarbital (Alurate).

Long-Acting Barbiturates: These drugs have a slower onset of action that begins in 30 to 60 minutes but their effect lasts longer for 10 to 16 hours. These types of barbiturates are used to treat seizures. It includes Phenobarbital (Luminal) and Mephobarbital (Mebaral). These drugs are classified as Schedule IV drugs.

Phenobarbital is approved by the WHO as the first-line treatment of epilepsy in the pediatrics age group and adults. Phenobarbital is also the most widely used barbiturate. Barbiturates are available as capsules, tablets, injectable, and suppositories.

Barbiturates are known by a variety of street names owing to their popularity among drug abusers for being highly addictive and for their availability in the black market. The street names for barbiturates are as follows:

Downers
Barbs
Blue heavens
Blues
Pinks
Rainbows
Christmas trees
Goofballs
Reds
Red devils
Blockbusters
Sleepers
Sekkies
Double trouble
Yellow jackets

Yes, barbiturates are associated with increased potential for addiction hence they should only be used for legitimate medical purposes as prescribed by your doctor.

Since barbiturates are psychoactive substances, they alter brain chemistry by increasing the levels of GABA neurotransmitters. The brain becomes dependent on the stimulating effect of barbiturates that lead to the release of this inhibitory neurotransmitter. Barbiturates produce an inhibitory and sedating effect accompanied by relaxation, drowsiness, and euphoria and individuals often misuse these drugs to attain these pleasurable effects for recreational purposes.

Addiction to barbiturates can even develop when the drug is taken as prescribed due to which individuals who are taking barbiturates are strictly monitored. Tolerance to barbiturates develops in as little as two weeks. During this phase, an individual requires more of the drug to achieve the same effect whether therapeutic or recreational. Once tolerance develops, individuals start taking increased doses of barbiturates which leads to the development of physical and psychological dependence since the brain finds it difficult to work in the absence of the stimulus as mentioned earlier. During this phase, discontinuation of the drug results in withdrawal symptoms that are quite painful and unpleasant for the individual to bear.

Eventually, addiction to barbiturates results, and the individual starts taking increased doses of the drug despite the negative consequences that ensue after its misuse. During barbiturate addiction, individuals feel compelled to use the drug regardless of the adverse events that result. Injecting, snorting, or smoking barbiturates increases the odds of developing an addiction since drugs reach the bloodstream faster through these routes as compared to when someone is ingesting the drug in the form of a tablet or capsule.

Moreover, the addictive potential of barbiturates depends on their duration of action since drugs that are short-acting produce the effects faster and the feelings of high also fade sooner due to which individual has to keep consuming increased doses of the drug leading to a vicious cycle of abuse. Amobarbital (Amytal) has the highest risk of addiction since it is a short-acting barbiturate with a fast onset of action as mentioned above.

Developing an addiction to barbiturates is influenced by various factors. These include:

Genetics: The genetic makeup of an individual plays a primary role in the development of addiction. It has been proven through scientific grounds that individuals who have a first-degree relative with a history of addiction are more likely to develop an addiction to drugs such as barbiturates.
Environmental: Individuals living in an environment with increased levels of stress, or those who have not been restricted about using abusive drugs and those who have been consuming drugs since an early age are more likely to develop an addiction to barbiturates.
Psychological: Individuals with a history of mental illness frequently misuse barbiturates. Moreover, individuals doing suicide attempts also use barbiturates to aid themselves in this process.

Prescription drug abuse is quite common among individuals since they presume that a drug prescribed for legitimate medical reasons cannot cause them harm when misused. However, this belief has no scientific grounds since drugs like barbiturates that are scheduled as controlled substances have significant potential for addiction and abuse when used outside medical purposes. According to statistics, 2% of Americans older than 12 years of age have used a prescription drug for non-medical reasons.

Barbiturates are often abused due to their highly addictive nature as it makes this drug class quite popular among drug abusers. It has been reported in a survey that 9% of high school students have taken barbiturates for non-medical reasons at least once in their lifetime. However, barbiturate abuse has declined since these drugs are replaced by other drug types such as benzodiazepines but still the risk associated with barbiturate addiction and overdose is quite prevalent.

According to statistics, more than 3000 deaths are reported each year due to barbiturate overdose in the United States. Of these 42% are due to suicide attempts, and the remaining is due to accidental mixing of barbiturate with other drugs such as alcohol which leads to overdose.

Barbiturates have effects similar to alcohol and individuals abusing barbiturates often feel disinhibited, intoxicated, and drowsy. Since barbiturate and alcohol both are central nervous system depressants they produce similar signs and symptoms when abused. Barbiturates are also used by drug abusers to counteract the effect of stimulant drugs such as cocaine and methamphetamine and therefore they are referred to as ‘downers’.

When the pattern of barbiturate abuse was studied it was found that there are two age groups in which barbiturate abuse is prevalent. According to research, the first group consists of females older than 45 years of age since they are taking barbiturate treatment for a certain medical condition such as epilepsy or anxiety and they become psychologically or physically dependent on barbiturates during their treatment.

The second group in which barbiturate abuse was prevalent consists of young males who are poly-drug abusers and who do not use barbiturates as the first choice of drug to abuse rather as an alternative to a drug that is not available, or to induce sleep after the stimulant effect of methamphetamine.

Barbiturate abuse through the intravenous route is the most dangerous because apart from the fact that barbiturates are highly addictive through this route, there is an increased risk of morbidity and mortality linked with acquiring infection such as hepatitis, septicemia, and endocarditis due to the use of unsterilized injection.

There are certain tell-tale signs that signal toward barbiturate addiction and one should not ignore them since paying heed at the beginning of addiction can prevent serious complications associated with barbiturate overdose.

Following are the symptoms of barbiturate addiction:

Impaired motor coordination
Slurred speech
Shallow breathing
Mood swings
Agitation
Irritability
Sedation
Decreased anxiety
Inability to make decisions
Forgetfulness
Confusion
Disorientation
Sleepiness
Change in vocalization

Some behavioral and social symptoms of barbiturate addiction are as follows:

Loss of interest in activities that earlier used to excite them
Withdrawing themselves from social interactions
Poor hygiene
Behavior that disrupts relationships
Financial struggles because of inability to meet workplace requirements

If you find any of these symptoms in your loved ones, you must provide them with the treatment for barbiturate addiction.

As with all other medications, barbiturates also have a multitude of side effects that are associated with their use.

Common side effects of barbiturates are as follows:

Confusion
Diarrhea
Nausea
Vomiting
Drowsiness
Dizziness
Headache
Irritability
Vertigo
Skin rash

There are certain psychological effects associated with barbiturates. They are as follows:

Severe anxiety
Insomnia
Mood disorder
Hallucinations
Depression
Suicidal ideations

Physical effects of barbiturates

When barbiturates are given intravenously as anesthetics they cause a drop in blood pressure with increased heart rate. Respiratory depression and apnea are common side effects of barbiturates. Barbiturates cause their effect on all body tissues. Following is the list of physical effects of barbiturates:

Respiratory distress
Cardiac arrest
Drowsiness
Disorientation
Increased sensitivity to sound
increased sensitivity to pain
Increased risk of pneumonia and bronchitis
Confusion
Headache
Unconsciousness
Coma

Short term effects of barbiturates

Apart from the calming and relaxing effect associated with barbiturate use, some short-term effects of barbiturates are agitation, irritation, emotional instability, headache, vomiting, slurred speech, and confusion.

Long-term effects of barbiturates

Long-term effects of barbiturates are linked with the use of the drug for a prolonged period and they consist of change in coordination, impaired judgment, hampered memory, paranoia, and suicidal thoughts. It can also result in coma and death.

FAQs

Is barbiturate a stimulant?

No, barbiturate is not a stimulant. Barbiturate is a central nervous system depressant. It impairs the signal transmission across neurons and depresses the activity of the brain thus producing a relaxed and calming effect.

What are barbiturates used for?

Barbiturates although less commonly used now, are prescribed for the treatment of epilepsy or seizure disorders, insomnia, neonatal withdrawal, and for inducing anesthesia in pre-operative settings.

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