How does pentobarbital work? What are the potential adverse effects of pentobarbital therapy? What are the contraindications to using pentobarbital?

Pentobarbital: Mechanism of Action

Pentobarbital is a medication within the barbiturate class that primarily acts on the central nervous system. Its mechanism of action involves binding to the gamma-aminobutyric acid (GABA) A subtype receptors, leading to changes in the chloride transport receptor. This results in an increased duration of the chloride channels remaining open, thereby potentiating the depressant effects of GABA on the CNS. Pentobarbital also works by inhibiting glutamate, which is responsible for nerve depolarization and voltage-activated calcium currents, further contributing to its central nervous system depressant effects.

Indications for Pentobarbital

Pentobarbital has several approved indications, including the management of seizures, control of intracranial pressure in patients with severe brain injuries or cerebral ischemia, treatment of insomnia, and as a pre-anesthetic medication for surgical procedures. It is often compared to another barbiturate, phenobarbital, and studies have found that pentobarbital is superior in the treatment of refractory status epilepticus due to its faster brain penetration and shorter half-life.

Adverse Effects of Pentobarbital

The main adverse reactions associated with pentobarbital use are central nervous system effects, such as altered mental status, agitation, confusion, drowsiness, respiratory depression, bradycardia, hypotension, cardiovascular collapse, and syncope. Other significant side effects include hallucinations, headache, insomnia, nausea, vomiting, hepatoxicity, megaloblastic anemia, angioedema, local injection site reactions, laryngospasm, bronchospasm, apnea, and hyperkinesia.

Contraindications and Precautions for Pentobarbital

Contraindications to pentobarbital use include any prior hypersensitivity reactions to the drug or the barbiturate class, patients with depressed respiratory function, and those with porphyria. Caution is advised when using pentobarbital in the elderly, those with renal or hepatic impairment, and individuals with a history of drug use. Additionally, pentobarbital is a pregnancy category D drug, meaning it can cause fetal harm, and it is essential to monitor maternal blood levels for fetal safety in pregnant women.

Administration of Pentobarbital

Pentobarbital can be administered through three routes: intramuscular, intravenous, or oral. For intramuscular administration, it is advised to inject no more than 5 ml and only into a large muscle to avoid tissue irritation or necrosis. Intravenous administration should not exceed 50 mg/minute and should be given as a slow IV injection in the undiluted form, as rapid IV injection can result in adverse effects such as respiratory depression, hypotension, and bronchospasm. In pediatric populations, oral administration is easier by mixing the drug with flavored syrup to improve the taste.

Monitoring and Interprofessional Care

Careful monitoring is essential when using pentobarbital to ensure the safety and well-being of the patient. This includes monitoring for adverse effects, such as altered mental status, respiratory depression, and cardiovascular changes. An interprofessional team approach, involving physicians, nurses, pharmacists, and other healthcare professionals, is crucial in coordinating care, communicating effectively, and advancing the appropriate use of pentobarbital to improve patient outcomes.

Conclusion

Pentobarbital is a versatile medication used in the management of various medical conditions, including seizures, intracranial pressure control, insomnia, and as a pre-anesthetic. Understanding its mechanism of action, indications, adverse effects, and contraindications is essential for healthcare professionals to ensure the safe and effective use of this drug in the clinical setting. A collaborative, interprofessional approach to patient care is crucial in optimizing the outcomes for patients receiving pentobarbital therapy.

Pentobarbital – StatPearls – NCBI Bookshelf

Continuing Education Activity

Pentobarbital is a medication used to manage and treat several medical conditions, including seizures, intracranial pressure control, insomnia, and as a pre-anesthetic in the operating room. This activity reviews the indications, mechanism of action, administration, adverse effects, and contraindications of pentobarbital therapy in the clinical setting. It is intended to relate the essential points needed by members of an interprofessional team managing the care of patients undergoing treatment with pentobarbital and its related conditions and sequelae.

Objectives:

• Identify the mechanism of action of pentobarbital.

• Describe the potential adverse effects of pentobarbital.

• Review the appropriate monitoring for the toxicity of pentobarbital.

• Explain interprofessional team strategies for improving care coordination and communication to advance the use of pentobarbital and improve outcomes.

Access free multiple choice questions on this topic.

Indications

Pentobarbital is a drug within the barbiturate class that works primarily on the central nervous system. At low doses, indications include short-term sedatives to treat insomnia and as a pre-anesthetic for surgery.[1] At higher doses, pentobarbital serves as an anticonvulsant for emergent seizure control and medically induced comas. Pentobarbital is often subject to comparison with phenobarbital, another barbiturate, in the use of refractory status epilepticus. Studies have found that pentobarbital is superior in that it has faster brain penetration and a shorter half-life, making it the treatment of choice.

Common off-label uses are for control of intracranial pressure in patients with severe brain injuries, cerebral ischemia, and those receiving treatment for Reye syndrome.[2] Some US states use it for capital punishment, but this remains a widely controversial topic, and some manufacturers do not allow its sale to prisons. More commonly, it is used by veterinarians for euthanasia and anesthesia.[3] 

Mechanism of Action

Pentobarbital works in the central nervous system by binding to gamma-aminobutyric acid (GABA) A subtype receptors. This action induces a change in the chloride transport receptor, leading to an increase in the duration that the chloride channels remain open, hence potentiating GABA effects. GABA is responsible for producing CNS depression and thus prolonging the time the channels remain open and intensifying the depressant effects on the CNS.[4] Pentobarbital also works by inhibiting glutamate, which is responsible for nerve depolarization in the voltage-activated calcium currents.[5] This activity is an additive effect on CNS depression. It undergoes first-pass metabolism in the liver.

Administration

Pentobarbital administration can be through three routes: intramuscular, intravenous, or oral. For intramuscular administration, it is advised to inject no more than 5 ml and only into a large muscle to avoid tissue irritation or necrosis. Intravenous administration is not to exceed 50 mg/minute and should only be given by slow IV injection in the undiluted form.[6] It is essential to avoid tissue extravasation in this process as it has been known to cause tissue necrosis. Clinicians should avoid rapid IV injection as it can result in respiratory depression, hypotension, and bronchospasm, among other adverse effects. In pediatric populations, oral administration is easier by mixing the drug with flavored syrup to improve the taste.[7]

Adverse Effects

The main adverse reactions surrounding pentobarbital use are central nervous system effects, including altered mental status, agitation, confusion, drowsiness, respiratory depression, bradycardia, hypotension, cardiovascular collapse, and syncope. Other significant side effects to be aware of include hallucinations, headache, insomnia, nausea, vomiting, hepatoxicity, megaloblastic anemia, angioedema, local injection site reactions, laryngospasm, bronchospasm, apnea, and hyperkinesia. [1]

Contraindications

Contraindications to pentobarbital use include any prior hypersensitivity reactions to previous drug use or barbiturate class use. Other contraindications include patients with depressed respiratory function and porphyria. Avoid abrupt drug withdrawal in those on long-term therapy. It is advised to exercise caution using this drug in the elderly, those with renal impairment, hepatic impairment, and those with drug use history.[8]   

Barbiturates have been shown to cause fetal damage if used in pregnant women and are pregnancy category D drugs. This class of drugs can cross the placental barrier and distribute throughout the fetal tissue with the highest concentrations in the liver, brain, and placenta. It is essential to monitor maternal blood levels for fetal safety in any pregnant female taking these drugs. There is documentation of withdrawal in infants born to mothers who took barbiturates during pregnancy. Newborns should be closely monitored for seizures and hyperirritability as this may indicate a need for withdrawal treatment. Symptoms can be delayed for up to two weeks and require prompt treatment if indicated.[9]

Monitoring

Toxic doses of pentobarbital occur at approximately 1 gram in most adults, with death occurring at 2 to 10 grams. The therapeutic values for pentobarbital depend on the intended therapeutic effect. For sedation, it is 1 to 5 mcg/mL. For intracranial pressure therapy, it is 30 to 40 mcg/mL, and for therapeutic coma, it is 20 to 50 mcg/mL. Toxic values for sedation are greater than 10 mcg/mL. The time to steady-state in adults is 3 to 6 days. Monitoring parameters include EEG and serum drug levels. Other things to consider when assessing for toxicity are a complete blood count (CBC),  liver function tests (LFTs), and a blood urea nitrogen (BUN) to creatinine ratio if on continuous treatment. Clinicians need to be aware that pentobarbital is often confused with phenobarbital, a different drug with varying dosage differences.

Pentobarbital is a high-risk habit-forming drug categorized by the Federal Controlled Substances Act under DEA schedule II. Tolerance, physical dependence, and psychological effects can occur in patients with long-term use. Estimates are that beyond 400 mg daily for greater than 90 days is the threshold for developing a dependence. Doses of 600 to 800 mg daily for greater than 35 days correlate with withdrawal seizures. Symptoms of acute intoxication include gait and speech alterations and neurological manifestations. Chronic intoxication demonstrates confusion, agitation, insomnia, and generalized myalgias. Minor withdrawal is seen within 8 to 12 hours and major withdrawal within 16 hours, lasting for up to one week following cessation of the drug. Treatment of dependence includes close monitoring and gradual withdrawal of the drug by small dosage decreases over many weeks—infants with physical dependence commonly present with hyperactivity, sleep disturbances, and hyperreflexia. Treatment of withdrawal in this population usually spans over two weeks.[10]

Toxicity

Treatment of pentobarbital toxicity involves supportive care, as there is no antidote. Overdose can lead to airway compromise, cardiovascular collapse, coma, and death. Treatment often requires intubation, hemodynamic support with vasopressors, and maintaining body temperature with warmers, commonly in an ICU setting. In mild or early cases of toxicity, activated charcoal and alkaline diuresis have been added but show minimal benefits. Always contact poison control if poisoning or overdose is suspected.

Special care is necessary for those with renal and hepatic impairment. The manufacturer does not provide dosage adjustment recommendations for renal impairment, but it is essential to monitor kidney function if using high doses or before undergoing prolonged treatment. Similar effects occur in those with hepatic impairment, and recommendations are for close patient monitoring.

Pentobarbital interacts with several major classes of drugs and requires close monitoring to ensure therapeutic drug levels are maintained. As a class, barbiturates induce hepatic microsomal enzymes, which increase the rate of metabolism of other drugs metabolized by these hepatic enzymes. In particular, anticoagulants can be affected, and patients taking these drugs, predominantly Warfarin, may require dosage adjustments. Other drug interactions to be aware of include levothyroxine, corticosteroids, doxycycline, phenytoin, valproic acid, alcohol, monoamine oxidase inhibitors (MAOI’s), and some hormones such as estradiol, estrone, and progesterone, to name a few.[11]

Enhancing Healthcare Team Outcomes

Pentobarbital is not used widely in clinical medicine because of its poor safety, habituation, and lack of an antidote. All clinicians who prescribe should be aware of its toxicity and side effect profile.

Withdrawal from pentobarbital can be life-threatening. Managing pentobarbital withdrawal requires a well-trained interprofessional team of healthcare professionals, including nurses, pharmacists, and several physicians from different specialties. Without proper management, the morbidity and mortality from unrecognized pentobarbital withdrawal are high. Properly treating pentobarbital withdrawal begins the moment a health care provider recognizes the patient is either susceptible to or suffering from withdrawal. The moment that withdrawal is suspected, the interprofessional team must coordinate the care for the patient, including:

• Obtaining a thorough history and physical

• Ordering drug levels in the blood and or urine, appropriate labs, imaging in the emergency department

• Monitor the patient for signs and symptoms of respiratory depression, cardiovascular collapse, central nervous system dysfunction, renal or hepatic toxicity 

• Preparing to provide airway protection and vasopressor support if indicated

• Consult with the pharmacist about possible drug interactions if the patient is taking other medications

• Consult with a toxicologist

• Consult with the intensivist about ICU care and monitoring while in the hospital

• Consider long-term management with social work to provide outpatient follow-up.

To avoid the high potential for morbidity and mortality associated with pentobarbital, the pharmacist should recommend prescribing clinicians safer alternative agents. Nursing should monitor the patient at subsequent visits, verifying medication compliance and treatment effectiveness. With an interprofessional team approach, the morbidity of pentobarbital is reducible and clinical success optimized. [Level 5]

Review Questions

• Access free multiple choice questions on this topic.

• Comment on this article.

References

1.

Abou Khaled KJ, Hirsch LJ. Updates in the management of seizures and status epilepticus in critically ill patients. Neurol Clin. 2008 May;26(2):385-408, viii. [PubMed: 18514819]

2.

Adelson PD, Bratton SL, Carney NA, Chesnut RM, du Coudray HE, Goldstein B, Kochanek PM, Miller HC, Partington MD, Selden NR, Warden CR, Wright DW., American Association for Surgery of Trauma. Child Neurology Society. International Society for Pediatric Neurosurgery. International Trauma Anesthesia and Critical Care Society. Society of Critical Care Medicine. World Federation of Pediatric Intensive and Critical Care Societies. Guidelines for the acute medical management of severe traumatic brain injury in infants, children, and adolescents. Chapter 13. The use of barbiturates in the control of intracranial hypertension in severe pediatric traumatic brain injury. Pediatr Crit Care Med. 2003 Jul;4(3 Suppl):S49-52. [PubMed: 12847349]

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Holtkamp M, Masuhr F, Harms L, Einhäupl KM, Meierkord H, Buchheim K. The management of refractory generalised convulsive and complex partial status epilepticus in three European countries: a survey among epileptologists and critical care neurologists. J Neurol Neurosurg Psychiatry. 2003 Aug;74(8):1095-9. [PMC free article: PMC1738579] [PubMed: 12876241]

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Walker SE, Iazzetta J. Compatibility and stability of pentobarbital ininfusions. Anesthesiology. 1981 Oct;55(4):487-9. [PubMed: 7294399]

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Wermeling DP, Blouin RA, Porter WH, Rapp RP, Tibbs PA. Pentobarbital pharmacokinetics in patients with severe head injury. Drug Intell Clin Pharm. 1987 May;21(5):459-63. [PubMed: 3582175]

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Knodell RG, Spector MH, Brooks DA, Keller FX, Kyner WT. Alterations in pentobarbital pharmacokinetics in response to parenteral and enteral alimentation in the rat. Gastroenterology. 1980 Dec;79(6):1211-6. [PubMed: 6777235]

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Ehrnebo M. Pharmacokinetics and distribution properties of pentobarbital in humans following oral and intravenous administration. J Pharm Sci. 1974 Jul;63(7):1114-8. [PubMed: 4853598]

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By the 2019 American Geriatrics Society Beers Criteria® Update Expert Panel. American Geriatrics Society 2019 Updated AGS Beers Criteria® for Potentially Inappropriate Medication Use in Older Adults. J Am Geriatr Soc. 2019 Apr;67(4):674-694. [PubMed: 30693946]

9.

Ashtarinezhad A, Panahyab A, Shaterzadeh-Oskouei S, Khoshniat H, Mohamadzadehasl B, Shirazi FH. Teratogenic study of phenobarbital and levamisole on mouse fetus liver tissue using biospectroscopy. J Pharm Biomed Anal. 2016 Sep 05;128:174-183. [PubMed: 27262993]

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Preuss CV, Kalava A, King KC. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Sep 21, 2022. Prescription of Controlled Substances: Benefits and Risks. [PubMed: 30726003]

11.

Singh V. Survival after fatal pentobarbital ingestion. Indian J Anaesth. 2014 Jan;58(1):85-6. [PMC free article: PMC3968666] [PubMed: 24700912]

Disclosure: Anna Johnson declares no relevant financial relationships with ineligible companies.

Disclosure: Nazia Sadiq declares no relevant financial relationships with ineligible companies.

DOJ to Use Pentobarbital in Executions. Here’s Why That’s Controversial

U. S. Attorney General William Barr’s surprise announcement that the federal government would resume executions after more than 15 years included one detail in particular that is troubling many anti-death penalty advocates.

Barr announced last Thursday that the Justice Department will start executing federal death-row inmates for the first time since 2003, bringing back the practice that has been highly criticized and removed from certain states. Seven states have abandoned the death penalty since 2003.

“Congress has expressly authorized the death penalty through legislation adopted by the people’s representatives in both houses of Congress and signed by the President,” Attorney General Barr said in a statement. “The Justice Department upholds the rule of law—and we owe it to the victims and their families to carry forward the sentence imposed by our justice system.”

As opposed to prior executions, which used multiple drugs for lethal injection, federal executions will only use one drug: pentobarbital. Some states have already used the chemical for executions including Texas, Missouri and Georgia.

States started using it for executions in 2011, due to a shortage of sodium thiopental, which was previously used in executions––along with pancuronium bromide and potassium chloride.

Barr’s announcement comes five years after the botched execution of Clayton Lockett in Oklahoma. In 2014, Lockett was injected with a combination of midazolam, vecuronium bromide and potassium chloride. It was an untested blend of chemicals. Appearing to be unconscious, Lockett woke up and thrashed around before dying of a heart attack 43 minutes later. The case brought national attention to the drugs used in lethal injections.

Then-President Barack Obama responded to the public outrage on the incident by calling on Attorney General Eric Holder to review how the death penalty is applied.

Concerns over the effectiveness of multi-drug lethal injections also encouraged states to turn to pentobarbital, according to experts.

“Since 2010, 14 states have used pentobarbital in over 200 executions and federal courts, including the Supreme Court, have repeatedly upheld the use of pentobarbital in executions as consistent with the Eighth Amendment,” the Department of Justice said in a statement announcing the resumption of federal executions.

The first execution dates for the new procedure are set for December for five convicted murderers. There are currently 65 federal prisoners on death row.

Here’s what to know about pentobarbital and why it’s controversial.

What is pentobarbital?

Pentobarbital is a sedative that slows the activity of the brain and nervous system. The drug is commonly used to euthanize pets.

There have been 143 executions that were carried out only with pentobarbital, but it’s unclear where the federal government will get it from and how they will administer it.

“Nobody knows if the pentobarbital that the government has obtained will address the serious risks that individuals across the country are facing of being tortured to death through lethal injection,” Sam Spital, the Director of Litigation for the NAACP Legal Defense and Educational Fund tells TIME.

Capital punishment opponents say this is problematic because a bad batch of the drug, or improper use could lead to botched executions that cause pain before death.

Ruth Friedman, the director of the Federal Capital Habeas Project, says the Justice Department was deliberate in not giving details on where they’re getting the drug from or how it will be administered.

“We have no idea if it’s imported, we have no idea if it’s compounded or manufactured. There’s no way to know,” Freidman tells TIME. “That was a calculated decision.”

Freidman believes it is meant to avoid getting pushback from anti-death penalty groups.

In 2014, Oklahoma used a combination of pentobarbital, potassium chloride and vecuronium bromide to execute convicted murderer Michael Lee Wilson. As the drugs were administered Wilson said, “I feel my whole body burning” before he died.

The new federal guidelines state that only pentobarbital will be used and, according to the DOJ statement, the Supreme Court has upheld the use of this drug in executions.

In April, the Texas Supreme Court allowed the state to protect the identity of their pentobarbital supplier. The Supreme Court in Missouri upheld the use of pentobarbital for death row inmate Russell Bucklew. He is scheduled to be executed on Oct. 1.

Many pharmaceutical companies have stopped supplying drugs to the government for executions, but death penalty opponents say there are ways for the government to find workarounds.

Compounding pharmacies, which are companies that produce mixtures of drugs, are not as heavily regulated as drug manufacturers, and anti-death penalty advocates say that state governments are already using them to get access to drugs for lethal injections.

The DOJ would not comment on where the pentobarbital it plans to use in executions will come from, or how it will be administered.

In Texas, the Woodlands Compounding Pharmacy made the state return pentobarbital that had been purchased for executions after the company’s identity was publicly leaked. Missouri also paid cash for pentobarbital from a compounding pharmacy so there would be no paper trail.

Did the Justice Department go through the correct legal process?

Death penalty opponents are also concerned that Barr’s decision to use pentobarbital in executions did not go through the Administrative Procedures Act (APA), which governs the process of rule making for federal agencies.

“Congress and the public have a right to know what this is about,” Freidman says.

Megan McCracken, a lawyer at the University of California-Berkley School of Law’s Death Penalty Clinic, tells TIME that skipping the APA process makes this new death penalty procedure invalid and therefore open to legal challenges.

“That is an act that brings transparency and accountability to the rule making process for an agency and here they skipped that process all together,” McCracken says.

Normally, when a federal agency develops or makes changes to regulations, it must go through the APA which allows the public to comment on proposed changes before they are put into place.

There is also a lawsuit pending against the federal government on behalf of some death row inmates that argues the use of lethal injection exposes the inmates to a considerable risk of pain.

While the lawsuit is still under review in the federal D.C. District Court, the five men set to be executed in December were not a part of that lawsuit, so the Justice Department was able to avoid addressing the suit with its announcement.

How will this decision affect the state level?

Right now, there are 21 states that don’t have the death penalty and another four that have moratoriums on executions. Federal death row inmates make up a small proportion of the 2,673 inmates on death row in the states that don’t ban executions. According to experts, it’s unclear how the new federal decision will impact those states.

“I continue to believe that the country as a whole is moving away from the death penalty and I don’t believe this one decision will change that,” Spital says. “On the other hand, the federal government does lead by example and to have the federal government so sharply going this way is deeply troubling.”

Support for the death penalty was at a record low in 2016, but has increased slightly since then according to the Pew Research Center. A 2018 survey by Pew found that only 39% of Americans were against the death penalty while 54% were in support of it.

Nationwide, executions slowed down as states struggled to find the drugs for lethal injections. However, they have begun picking up again in some states. Texas has executed three people this year. Last year the state executed 13. Tennessee had three executions in 2018. Florida and Georgia both had two executions in 2018.

“There are many states that have been carrying out executions while the feds have been doing nothing so there’s no direct reason why this should affect any given state for any reason.” McCraken says.

However she also acknowledges that because it’s the federal government, that they could have an “atmospheric affect” on what the states decide to do.

“In so many states the death penalty is a broken system and it is just as broken in the federal government. So you have problems of race and innocence and the most vulnerable people ending up on death row,” McCraken says. “It shouldn’t be a situation where the feds are held up as leaders.”

Write to Josiah Bates at [email protected].

What are barbiturates and what preparations are they? ”, a practicing psychiatrist, psychiatrist-narcologist and psychotherapist Vladislav Sipovich.

What are barbiturates and what is the history of their discovery?

Barbiturates are a large group of medicines that have a depressant effect on the central nervous system (CNS). Moreover, the degree of inhibition depends on the dosage of the drug and varies from a mild sedative and hypnotic effect to the state of anesthesia.

Until recently, barbiturates have been prescribed as a sedative, sleep aid, and sleep enhancer. Now their use is significantly limited due to the narrowness of the therapeutic range, which can easily lead to overdose and intoxication, as well as due to the emergence of addiction and even the formation of persistent dependence.

Quite interesting and unusual is the history of discovery and getting the name of barbituric acid. She was born in 1864 in the laboratory of a chemist from Munich, Adolf Bayer, and this date coincided with the feast of St. Barbara, in German urate Barbar – hence the name barbiturates. Another version suggests that Bayer named the new substance after his then-girlfriend Barbara.

Since then, more than 2,500 barbiturates have been synthesized, of which 50 have been produced for commercial sale. Now there are a little more than 10 of them. According to the WHO recommendation, the root barb and the suffix al are often used to designate hypnotic barbiturates, for example, barbital, allobarbital, phenobarbital, etc. In addition, the prefix before the root indicates the features of the chemical formula: thio – the presence of a sulfur atom, cyclo – the cyclic (closed) spatial structure of the formula, vinyl – the presence of a vinyl group, phenyl – a phenyl group (benzene radical), etc.

As I said, all barbiturates are derivatives of barbituric acid. Their synthesis occurs as a result of the condensation of urea with dialkylmalonic acids at reflux in absolute ethanol with the addition of sodium ethoxide. This is a classic variant of the synthesis of barbiturates, although there are others, for example, by replacing acids with esters, and ethanol with methanol. But let’s not delve too deeply into these issues. Much more interesting are the mechanisms of the physiological action of barbiturates on the central nervous system.

How do barbiturates affect the nervous system and how is their effect manifested?

Barbiturates are able to interact with the perceiving barbiturate-benzodiazepine receptors of the neurotransmitter system GABA (gamma-aminobutyric acid), which is accompanied by a change in the work of sodium-chlorine channels and, ultimately, a slowdown in the passage of nerve impulses and a decrease in the excitability of nerve cells.

The difference in effects between the various derivatives of barbituric acid lies mainly in their duration and magnitude. This is the basis for the classification of barbitures into the following groups:
• Ultra short but strong action. For example, secobarbital and pentobarbital act for about 30 minutes; when administered intravenously, they cause drug-induced sleep for 1 minute.
• Short to medium duration effect, beginning to act after 15-40 minutes and remaining effective for 6-8 hours. For example, amobarbital, secobarbital, butabaobital, etc.
• With a long and delayed effect. An example is phenobarbital with a duration of action of 8-10 hours. They are mainly used in the treatment of epilepsy.

At the present stage, barbiturates are mainly used for premedication (preoperative preparation before general anesthesia) and as an anticonvulsant. Anxiety reduction and normal sleep before surgery are achieved with the use of high doses of barbiturates. In moderate dosage, they cause a state resembling alcohol intoxication with euphoria, impaired coordination of movements, clarity of consciousness and intelligibility of speech. With a systematic intake, a person loses the ability to learn, concentrate, and his memory suffers. In addition, by stimulating the vagus nerve, barbiturates can cause severe bronchospasm, which can sometimes be fatal. This is especially true in cases of intravenous administration of sodium thiopental, which is used for premedication.
The main clinical manifestations caused by drugs of this group are reduced to the following physiological effects:
• Sedative.
• Sleeping pills.
• Muscle-relaxing.
• Anticonvulsant.
• Narcotic.
• Antiphobic (anxiolytic, anti-anxiety).
• Amnestic (the ability to induce amnesia).

By the way, the first barbiturate used for medicinal purposes is barbital, known under the market name Veronal and introduced into medical practice in 1903 year. After 10 years, he was replaced by a stronger Phenobarbital.

How has the use of barbiturates in medicine evolved?

Veronal, already mentioned by me, was used as a sedative and the first sleeping pill.
Barbiturates were first introduced into medical practice in 1903, when barbital received the market name “veronal”. Until 1960, the popularity of barbiturates as anti-anxiety and sleeping pills grew, but then there was a decline in their demand. This was due to the development of addiction and the formation of drug dependence during their long-term use. Therefore, preference began to be given to safer benzodiazepines of the same therapeutic effect. Learn more about nootropics.

By the way, the problem of barbiturate addiction has been hushed up for a long time, although doctors have been paying attention to it since the 1930s. At the same time, barbiturate addicts prefer short or medium-acting barbiturates such as Seconal, Amital or Nembutal, figuratively calling them “red devils” or “green dragons” in the international drug jargon.
In veterinary medicine pentobarbital barbiturate is used for pain relief and euthanasia.

Barbiturate addiction – what is it and how is it treated?

Barbiturate addiction (barbiturate addiction) is much more dangerous than opiate addiction. It develops at the physiological level and is based on a change in the mechanism of action, which, at low and medium doses, normally reduces to such effects as:
• Blocking of the acetylcholinergic system.
• Strengthening the inhibitory role of GABA.
• Violation of the transmission of neurotransmitters through the lipid membranes of neurons.

When dependence occurs and the dosage is increased, everything happens exactly the opposite. Instead of a calming and relaxing effect, excitement, loss of self-control and aggression come, sometimes hallucinations join them. The danger of barbiturate addiction is primarily associated with a possible overdose and severe intoxication in case of poisoning with barbiturates.
There are 4 stages of barbiturate poisoning, characterized by the following symptoms:
• Apathy, drowsiness, inhibition of reactions.
• Difficulty in swallowing and breathing, retraction of the tongue, hyperthermia (fever), superficial coma with loss of consciousness.
• Deep coma with drop in temperature, respiratory paralysis and failure of vital organs.
• Postcomatous state of restoration of basic vital functions.

Drug addicts with an experience of more than 0.5 years may experience withdrawal syndrome, which develops when trying to reduce the dosage or completely abandon barbiturates. Learn more about obsessive compulsive disorder.

There is no specific antidote for barbiturate poisoning, so it is treated like any other intoxication – with accelerated elimination and symptomatic therapy. If no more than 8 hours have passed from taking the barbiturate, then gastric lavage with a 2% soda solution, taking sorbents and laxatives will be effective.

In case of violation of the respiratory function, 1 ml of Lobelin is injected subcutaneously, inhalation therapy with an oxygen-carbon mixture is carried out. To withdraw from a coma, barbiturate antagonists are used – cordiamine, caffeine, strychnine.

By the way, even prolonged use of seemingly harmless Corvalol leads to the appearance of barbiturates in the urine. You can quickly remove them with the help of drinking plenty of water and taking diuretics.

Based on what has been said, the question: barbiturate – what is it, a drug or a drug, can be answered unambiguously. With a single use or in compliance with the recommendations of a doctor, this is a medicine that helps to calm down, fall asleep, relieve anxiety and concern. When the dosage is exceeded and uncontrolled constant intake, any barbiturate is a drug, and people who regularly take barbiturates for euphoria are pharmacy addicts, or barbiturists. It must be said that even cores who constantly take drugs containing barbiturates run the risk of becoming a victim of addiction to them and will not be able to stop using them on their own. To achieve the effect, they will need an increasing dosage and it can end with all that drug addiction, and sometimes even lead to acute poisoning. Having a cumulative effect, barbiturates are able to accumulate in the body, which is fraught with an overdose even when taking a completely harmless next dose of the drug. It is not known when just one tablet can lead to acute poisoning.

How to get rid of barbiturate addiction? First of all, contact the specialists of a private or state drug treatment center. Treatment includes detoxification measures, complete elimination of barbiturates from the body, drug or psychological coding, a rehabilitation period, and periodic consultations with a treating psychiatrist-narcologist.

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Sodium pentobarbital – risk of overdose – Healthy Youth Center

Sodium pentobarbital (trade name Nembutal) is a common drug in the rapid-acting barbiturate class. According to the instructions for use, its main action is sleeping pills. The effect occurs after 20-30 minutes after ingestion. The main danger of this drug is overdose, which can lead to death. In case of an overdose, respiratory arrest occurs and almost instantaneous death of a person. In addition, pentobarbital, if used inappropriately, can cause dependence.

Interesting facts

In America, this drug was used as a death sentence, but the pharmaceutical company that produced this drug refused to supply it to prisons, which led to its replacement with analogues. Today, pentobarbital is used in countries where euthanasia (voluntary death) is allowed, as well as for the “euthanasia” of animals in veterinary medicine.

It was Nembutal who used the love of his life and Mayakovsky’s muse, Lilya Brik, for a successful suicide attempt at the age of 87.

In our country, sodium pentobarbital is included in List II of narcotic drugs, psychotropic substances and their precursors, and its circulation is strictly monitored by the responsible authorities. This substance is used by drug addicts for recreational purposes (for drug intoxication), as well as by people who attempt suicide.

Do not confuse pentobarbital with phenobarbital, which is an antiepileptic but also a barbiturate.

Composition and action

Dosage form of the substance – tablets, injection solution, capsules. The powder is highly soluble in water.

Sodium pentobarbital depresses the central nervous system. The drug acts on the nerve endings and blocks the ability to receive and transmit signals. In addition, the active substance acts on the enhancement of GABA receptors (inhibitory neurotransmitter). The medicine can cause drowsiness, lethargy, lethargy, as it negatively affects the cerebral cortex.

Medical effect of pentobarbital

If Etaminal-sodium is taken in therapeutic doses, not exceeding the daily dosage recommended by the doctor (usually 0.1 g), no side effects will occur.

How does dependence on barbiturates develop?

Addiction and drug addiction develop quite quickly. In just a few weeks of systematic use, there is not only a physical, but also a mental craving for the drug. However, addiction to the standard dose soon sets in. A person without another pill becomes nervous and irritable, emotionally unstable, aggressive, he is tormented by insomnia, which at times increases intoxication and the risk of serious health complications, including death.

If the next dose is missing, the addict begins to withdraw. The withdrawal syndrome is very difficult for the addict both mentally and physically. He cannot fully sleep, he is tormented by nightmares, depression, suicidal thoughts. The treatment of sodium pentobarbital addiction takes quite a long time, often recovery lasts 6-12 months.

It is not uncommon for people to come to the Center for Healthy Youth with poisoning from this drug and similar barbiturates. Mortality from overdose is about 3%.

Danger of the drug

Among the risk factors for overdose are:

• combination of tablets with alcohol intake;
• over-the-counter and uncontrolled use of the drug.

People with alcohol addiction, mental disorders, deep personal experiences and unstable psycho-emotional background are at risk of developing addiction and overdose. With regular intake, tolerance to the usual dose occurs, which leads to its increase, and with this an increase in the risk of poisoning.

Symptoms of an overdose of pentobarbital sodium

The danger of taking this substance is that often an overdose can be overlooked. The addict simply falls asleep, and then stops responding to external stimuli, neither pain nor a loud sound can wake him up. To determine that there is intoxication and a health hazard, it is necessary to monitor the reaction of the pupil to light. A healthy person has a narrow pupil in the light, and a wide one in the dark.

If you touch the cornea, the eyelids normally close instantly. If the addict does not have these reflexes, it is worth calling a narcologist to the house. Emergency drug treatment services in Moscow and throughout Russia are provided by the Center for Healthy Youth.

In case of a critical overdose of pentobarbital, the addict’s respiratory center is depressed, he begins to breathe less frequently, his pulse slows down and his blood pressure drops.

There are 4 phases of intoxication:

1. Falling asleep. The victim does not respond to stimuli, is drowsy and indifferent to everything.
2. Superficial coma. The person is unconscious, swallowing is difficult, tongue retraction is possible, airway is blocked.
3. Deep coma. Complete absence of reflexes. Violation of the work of internal organs, breathing.
4. Post-coma. Consciousness returns to the person, he can behave irritably, nervously, excitedly, have problems with sleep, feel overwhelmed, lethargic.

If the poisoning is mild, two intermediate phases are missing. If an addict has a deep coma, he may not get out of it without the provision of drug treatment. Death is not uncommon in drug abuse.

Consequences of use

Regular use of this sleeping pill can lead to significant health complications. Among them: neurological disorders, depression, mental disorders, disruption of the internal organs, kidneys, heart, coma. In 30% of addicts, after providing emergency care and resuscitation and detoxification, problems with the respiratory system, as well as trophic ulcers, dermatitis, bedsores, develop.

The causes of death of drug addicts are: cardiac arrest, respiratory arrest, liver dysfunction.

Emergency care

Even a minor overdose is a serious reason to call an ambulance doctor at home. It is important to make a call in time, as the condition of the victim may worsen. The primary task of doctors in case of intoxication is to remove toxins from the human body as soon as possible. If the victim is conscious, the stomach is cleansed, it is necessary to give him as much water as possible, adsorbents and induce vomiting so that toxic substances are no longer absorbed into the blood through the gastrointestinal tract. If there is paralysis of the respiratory system, it is worth giving the addict artificial respiration before the doctor arrives.

It is worth entrusting all other rehabilitation and medication measures to doctors. Specialists examine the patient and, based on express diagnostics, will be able to select symptomatic drugs, in particular, diuretics.

Inpatient treatment

Pharmacy drug poisoning is a condition that only experienced drug specialists can help. At home, it is very difficult to identify the entire clinical picture. It is possible to fully examine, examine, take tests from a patient only in the conditions of a hospital of a narcological center. Specialists measure vital signs, then study the state of internal organs, the consequences of poisoning, existing diseases, and draw up a complete drug treatment plan, including detoxification procedures.

Measures taken to cleanse and restore the patient’s body in the hospital:

• gastric probing;
• mechanical ventilation;
• infusion-drip therapy.

Droppers are installed to quickly remove toxins from the blood and cleanse the body, as well as normalize the water-salt, electrolyte and acid-base balance. In addition to infusions, hemodialysis and hemosorption are used, these are hardware methods of blood purification.