It is crucial to keep yourself and your loved ones safe during the COVID-19 outbreak. Yet addiction may pose even a higher danger than the virus.

Learn about recovery during the pandemic:

What Are Barbiturates Used For? Uses And MOA

Barbiturates mechanism of action

Important InformationThis information is for educational purposes only. We never invite or suggest the use, production or purchase of any these substances. Addiction Resource and it’s employees, officers, managers, agents, authors, editors, producers, and contributors shall have no direct or indirect liability, obligation, or responsibility to any person or entity for any loss, damage, or adverse consequences alleged to have happened as a consequence of material on this website. See full text of disclaimer.

Barbiturates are drugs which have depressing and calming effects on the body, and the barbiturate therapy includes sleep problems, migraines, anxiety, epilepsy, seizures, coma induction, and reducing high blood pressure among others. The barbiturates uses have almost the same effects to those of alcohol, varying from relaxation to the inability to feel pain and even loss of consciousness.

Learn more about Barbiturates

How Barbiturates Work

The drugs stimulate the Gamma-aminobutyric acid or GABA neurotransmitter in the brain inhibiting the central nervous system and therefore causing central nervous system depression.

The Barbiturates mechanism of action varies depending on the purpose of use. When used as a medication, the drug relieves anxiety, reduces muscle spasms, induces sleep, and prevents seizures. When used as a recreational drug, it reduces inhibition, induces euphoria, relaxation, slurred speech, impaired judgment, confusion, and loss of coordination. Recrearional use is illegal as it is considered as abuse.

The action and effects of barbiturate therapy vary depending on the type of drug used. The drugs have as ultra-short- (thiopental, methohexital), short- (secobarbital, pentobarbital), intermediate- (butabarbital, amobarbital), and long-acting effects (primidone, phenobarbital). Taken by mouth, the drug’s effects begin in about 30 minutes.barbiturate drug test can detect the drug in the blood for up to 72 hours.

Barbiturates Uses

These drugs are usually used or prescribed by doctors for epilepsy, severe trauma to the skull, to increase blood pressure in the head, injury, sleep disorder, jaundice, seizures, anxiety, migraines or as an anesthetic.

Barbiturates For Migraines

Barbiturates for headaches should be considered a last resort when the common migraine drugs show no results. Butalbital barbiturate is usually used together with acetaminophen and caffeine in the treatment of migraine.

In this situation, the barbiturate mechanism of action is helping the patient sleep off the pain by inducing sedation. Although this treatment does offer relief, it does not address the underlying problem, which is the dilation of blood vessels in the brain.

Using barbiturate for migraine for too long can lead to medication overuse headache (MOH) or even severe withdrawal symptoms if the treatment is stopped suddenly.

Patients using these drugs for a long time might need to be hospitalized to be able to stop the medication safely. Barbiturates are addictive and might cause withdrawal symptoms, increasing the migraine intensity and duration in the long run. Some specialists believe that this drug should not be used at all to treat migraines.

asian woman with migraine

Barbiturates For Anxiety

Not long ago, barbiturates were used to treat anxiety and agitation as they reduced the activity of nerves leading to muscle relaxation. But due to their risk of abuse, overdose, tolerance, and withdrawal, they were replaced with benzodiazepines. In comparing barbiturates vs benzodiazepines, the latter proves to be safer and more effective.

The drug can cause anxiety if the treatment is stopped suddenly. This drug’s withdrawal symptoms can occur suddenly and include agitation, restlessness, and anxiety, among others. So instead of treating the condition, this drug can cause it.

Barbiturates For Sleep

Being in the sedative-hypnotic class, this drug depresses the central nervous system causing sleepiness. Some doctors prescribe short or long-acting barbiturates as sleeping pills or sedatives.

A study made to determine the effectiveness of the drug on sleep showed that 200 mg of sodium amylobarbitone administered for five nights reduced the delay to sleep, depressed R.E.M. sleep, and increased the sleep period. After the 5th night, the REM sleep returned to typical values, which means the body started to develop tolerance. Withdrawal symptoms were also present when stopping the drug, even at such low doses.

Although this drug can prove to be useful for sleep, it can cause addiction, exaggerated REM sleep, and can even worsen sleep problems.

Barbiturates For Seizures And Epilepsy

Phenobarbitone or Phenobarbital has proved to be the most efficient anticonvulsant barbiturate in treating seizures and epilepsy.

Although new treatments are available, this treatment is still frequently prescribed for patients who have epilepsy, not because it would be more efficient, but because of the physicians’ discomfort with the newer AEDs.

Studies have shown that these drugs might significantly impair cognition and lead to withdrawal seizures. Specialists also noted the presence of severe behavioral and cognitive problems at high doses of Phenobarbital, as well as hyperactivity, depression, sleep disorders and even intolerable side-effects that led to reducing the drug dosage to a minimum.

Barbiturate Anesthesia

The ultrashort action drugs are used for anesthesia due to the short duration of action, allowing for greater control. This means that a doctor can rapidly anesthetize a patient in emergencies and wake the patient up just as quickly in case of complications during surgery.

The drug can also be used for deep anesthesia for mechanically ventilated patients, for those with elevated intracranial pressure and with closed-head injury, improving the survival rate.

woman under anesthesia

In this case, too, barbiturate drugs come with dangers such as increased heart rate, depressed breathing, and constricted blood vessels. That is why using these drugs as anesthetics is not common practice anymore, being replaced with benzodiazepines.

Barbiturates for Alcohol Poisoning And Withdrawal

Barbiturates have been successfully used to treat alcohol withdrawal syndrome, especially in the emergency department and the severe withdrawal in the intensive care unit. The drug enhances the GABA activity and also suppresses glutaminergic activity, a dual mechanism of action which works well in the pathophysiology of alcohol withdrawal.

Barbiturates for Jaundice

Phenobarbital has proved efficient in treating newborn jaundice, decreasing the level of bilirubin. In a study, jaundiced newborn infants were given low doses of Phenobarbital for five days, measuring their liver synthesized blood-clotting factors and bilirubin levels each day.

After only two days, the level of mean serum bilirubin was significantly lower, decreasing the need for blood transfusions and phototherapy.  The drug improved the liver function helping it clearing bilirubin.

Barbiturates To Reduce Blood Pressure

Some of these depressants can be used to reduce blood pressure because they are metabolized by the liver enzyme systems, which also break down the calcium-channel blockers and antibiotic erythromycin used to treat high blood pressure. This means that if barbiturates are used together with these drugs, the effects will last for a longer time than usual.

It should be noted that barbiturates mixed with other drugs to reduce blood pressure can result in a dangerous drop in the blood pressure levels.

On the other hand, the drugs proved efficient in reducing intracranial hypertension or ICP by decreasing the cerebral blood volume and metabolic demands. The risk is the decrease in blood pressure to the point of affecting cerebral perfusion pressure.

doctor checking blood pressure

Barbiturates For Coma Induction

Barbiturate coma therapy (BCT) or barbiturate induced coma has been used to control increased intracranial pressure (IICP). What the drug does is vasoconstricting standard brain areas and decreasing the need for metabolic oxygen and cerebral blood flow. It also stabilizes the lysosomal membrane, reducing intracellular calcium concentration, maintaining the membrane, and suppressing seizure.

Complications can arise, such as azotemia, hypotension, hepatic dysfunction, pulmonary edema, and electrolyte imbalance. Fortunately, most of these complications can be successfully handled in the intensive care unit setting.

BCT is also indicated during vascular neurosurgery such as arteriovenous malformation (AVM) surgery, carotid surgery, or after significant bleeding caused by subarachnoid hemorrhage (SAH) or AVMs.

Are Barbiturates Still Prescribed?

Until the 1950s, these drugs were effectively used as sleeping pills, hypnotics, and sedatives, but over the past decade, the use and abuse of the drug have declined dramatically. This happened due to the development of safer and newer alternatives.

Although efficient for various uses, the drug comes with the risk of physical and psychological addiction, as well as barbiturate overdose. The difference between a safe and a deadly dose is tiny. Although the drug is seldom used as tranquilizers and sedatives, they still play an essential part in neurology practice, in the treatment of epilepsy and as an anesthetic.

However, due to the high abuse potential, it is recommended to get a professional consultation before usage. Drug rehabilitation facilities offer their services for patients of all ages and financial situations. Call now to get a consultation regarding drug abuse treatment.

Sources
  1. Lader M. Antianxiety drugs: clinical pharmacology and therapeutic use. Drugs. 1976 Nov;12(5):362-73. https://www.ncbi.nlm.nih.gov/pubmed/10153
  2. J. I. Evans, S. A. Lewis, I. A. M. Gibb, and Mary Cheetham. Sleep and Barbiturates: some Experiments and Observations. Br Med J. 1968 Nov 2; 4(5626): 291–293. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1912258/
  3. Smith MC1, Riskin BJ. The clinical use of barbiturates in neurological disorders. Drugs. 1991 Sep;42(3):365-78. https://www.ncbi.nlm.nih.gov/pubmed/1720379
  4. Alvarez N. Barbiturates in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:16-23. https://www.ncbi.nlm.nih.gov/pubmed/10030427
  5. Martin K, Katz A. The Role of Barbiturates for Alcohol Withdrawal Syndrome. Psychosomatics. 2016 Jul-Aug;57(4):341-7. https://www.ncbi.nlm.nih.gov/pubmed/27207572
  6. D. Sinniah, L. K. Tay, and A. E. Dugdale. Phenobarbitone in neonatal jaundice. Arch Dis Child. 1971 Oct; 46(249): 712–715. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1647820/
  7. Roberts I1, Sydenham E. Barbiturates for acute traumatic brain injury. Cochrane Database Syst Rev. 2012. https://www.ncbi.nlm.nih.gov/pubmed/23235573
  8. Young-Il Kim, M.D., Seung-Won Park, M.D.,corresponding author Taek-Kyun Nam, M.D., Yong-Sook Park, M.D., Byung-Kook Min, M.D., and Sung-Nam Hwang, M.D. The Effect of Barbiturate Coma Therapy for the Patients with Severe Intracranial Hypertension: A 10-Year Experience. J Korean Neurosurg Soc. 2008 Sep; 44(3): 141–145. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2588298/
Medically Reviewed By Michael Espelin APRN
Sharon Levy

About Author

Sharon Levy, MD, MPH

After successful graduation from Boston University, MA, Sharon gained a Master’s degree in Public Health. Since then, Sharon devoted herself entirely to the medical niche. Sharon Levy is also a certified addiction recovery coach.

Comments

Leave a comment