Pentobarbital
Death may occur when barbiturates are combined with depressants such as opiates, benzodiazepines, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]
It is strongly discouraged to consume moderate to heavy dosages of these substances together.
| Summary sheet: Pentobarbital |
| Pentobarbital | |||||||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||||||
| Common names | Pentobarbital, pentobarbitone, Nembutal | ||||||||||||||||||||||||||||||
| Systematic name | 5-Ethyl-5-(1-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione | ||||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||||
| Psychoactive class | Depressant | ||||||||||||||||||||||||||||||
| Chemical class | Barbiturate | ||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||
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Pentobarbital, also known as pentobarbitone in British English and by the brand name Nembutal, is a short-acting psychoactive drug of the barbiturate class which produces powerful anxiolytic, hypnotic, muscle relaxant and amnesic effects. Pentobarbital is used medically as a hypnotic for the short-term treatment of insomnia and as an anticonvulsant in emergency situations. Pentobarbital is also used to put patients into medically induced comas. Pentobarbital works in a similar fashion to benzodiazepines, however barbiturates bind to a distinct allosteric site on the GABAA receptor.
Compared to other barbiturates such as phenobarbital, pentobarbital has a prompt onset of action, generally working within fifteen minutes of ingestion. Pentobarbital's anxiolytic effects may last for up to 36 hours after the primary effects have worn off.
Pentobarbital, like most short-acting barbiturates, is deemed to be extremely addictive. The abrupt discontinuation of pentobarbital in dependent individuals may be life-threatening and lead to seizures and even death[2]. Pentobarbital drastically enhances the effects of other depressants such as alcohol, and concurrent use may lead to respiratory depression and possibly death.
Chemistry
Pentobarbital is a drug of the barbiturate class. Barbiturate drugs contain the backbone of barbituric acid. Pentobarbital has a 5-ethyl, 5-methylbutyl substitution on the 5-position of the barbituric acid backbone which gives it its unique pharmacological effects. Pentobarbital's empirical formula is C11H18N2O3 and has a molar mass of 226.27 grams per mole.
Pharmacology
Barbiturates behave similarly to benzodiazepines. Pentobarbital binds to an allosteric site on the GABAA receptor and potentiates the effects of the endogenous ligand, gamma-aminobutyric acid. When barbiturates bind to the GABAA receptor, it causes the ion pore to open for extended periods of time, causing an increase of intracellular chlorine ion concentrations. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of barbiturates on the nervous system.
Pentobarbital has a bioavailability of 70-90%. 45-60% of pentobarbital will bind to proteins. Its biological half life is 15-48 hours. Pentobarbital is metabolized by the liver and excreted by the kidneys.
Subjective effects
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects 
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- Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
- Motor control loss
- Muscle relaxation
- Dizziness
- Respiratory depression
- Decreased blood pressure - Barbiturates may decrease blood pressure in some individuals and have occasionally been used to reduce intracranial pressure.[3]
- Seizure suppression
- Physical euphoria
- Decreased libido
- Pain relief - Compared to other agents such as opioids, this effect is generally considered to be quite weak.
Visual effects 
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- Acuity suppression - Like many depressants, high doses of pentobarbital may cause blurred vision.
Cognitive effects 
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- Anxiety suppression
- Cognitive euphoria - Compared to other GABAergic depressants, this effect is particularly strong. The feeling itself can be described as an extremely strong feeling of relaxed contentment.
- Thought deceleration
- Analysis suppression
- Disinhibition
- Amnesia
- Language suppression - At higher doses, pentobarbital is known cause slurred speech.
- Compulsive redosing
- Emotion suppression - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of antipsychotics.
- Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others. It most commonly occurs at heavy dosages.
Experience reports
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
Pentobarbital likely has moderate toxicity relative to dose. However, pentobarbital is potentially lethal when mixed with depressants like alcohol or opioids. Pentobarbital has a higher risk of death or serious adverse effects associated with concurrent depressant use than other drugs such as benzodiazepines. There have been studies linking the use of barbiturates, particularly phenobarbital, with the development of cancer [5].
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
Pentobarbital is extremely physically and psychologically addictive. Barbiturate withdrawal is medically serious and can potentially cause a life-threatening withdrawal syndrome that can cause seizures, psychosis, and death. Drugs which lower the seizure threshold such as tramadol and amphetamine should be avoided during withdrawal. If an individual is addicted to a short-acting barbiturate such as pentobarbital, switching to a longer acting drug such as phenobarbital may be of some benefit.
Tolerance will develop to the sedative-hypnotic effects of pentobarbital after prolonged use. It is unknown exactly how long it takes for tolerance to reach baseline. Pentobarbital presents cross-tolerance with all barbiturates, meaning that after its consumption all barbiturates will have a reduced effect.
Dangerous interactions
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be harmless in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.
- Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should try to fall asleep in the recovery position or have a friend move them into it. Pentobarbital is deemed to have an increased incidence of serious adverse effects when used concurrently with other depressants than other depressants.
- Dissociatives - This combination can lead to an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
- Stimulants - It is unsafe to combine barbiturates with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of barbiturates, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of barbiturates will be considerably increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of barbiturates per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.
Overdose
Barbiturate overdose may occur when a barbiturate is taken in extremely heavy quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as benzodiazepines and alcohol since they work in a similar fashion, but bind to distinct allosteric sites on the GABAA receptor, thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABAA receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer[6]. Barbiturate overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and properly. Barbiturate overdose has an increased frequency of serious adverse effects when compared to other depressants.
Symptoms of a barbiturate overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death[7].
Legal status
Internationally, pentobarbital is listed in Schedule III of the UN Convention on Psychotropic Substances.[8]
- Australia: Pentobarbital is a Schedule 8 controlled substance.[9]
- Canada: Pentobarbital is a Schedule IV controlled substance.[10]
- Germany: Pentobarbital is controlled under Anlage III BtMG (Narcotics Act, Schedule III)[11] It can only be prescribed on a narcotic prescription form.
- Russia: Pentobarbital is a Schedule II controlled substance.[12]
- Switzerland: Pentobarbital is a controlled substance specifically named under Verzeichnis B. Medicinal use is permitted.[13]
- United Kingdom: Pentobarbital is a Class B controlled substance.[14]
- United States: Pentobarbital is a Schedule II controlled substance.[15]
See also
External links
References
- ↑ Risks of Combining Depressants - TripSit
- ↑ Sarrecchia, C., Sordillo, P., Conte, G., Rocchi, G. (December 1998). "[Barbiturate withdrawal syndrome: a case associated with the abuse of a headache medication]". Annali Italiani Di Medicina Interna: Organo Ufficiale Della Societa Italiana Di Medicina Interna. 13 (4): 237–239. ISSN 0393-9340.
- ↑ Roberts, I., Sydenham, E. (12 December 2012). Cochrane Injuries Group, ed. "Barbiturates for acute traumatic brain injury". Cochrane Database of Systematic Reviews. doi:10.1002/14651858.CD000033.pub2. ISSN 1465-1858.
- ↑ Nutt, D., King, L. A., Saulsbury, W., Blakemore, C. (24 March 2007). "Development of a rational scale to assess the harm of drugs of potential misuse". The Lancet. 369 (9566): 1047–1053. doi:10.1016/S0140-6736(07)60464-4. ISSN 0140-6736.
- ↑ Friedman, G. D., Habel, L. A. (1 June 1999). "Barbiturates and lung cancer: a re-evaluation". International Journal of Epidemiology. 28 (3): 375–379. doi:10.1093/ije/28.3.375. ISSN 0300-5771.
- ↑ Twyman, R. E., Rogers, C. J., Macdonald, R. L. (March 1989). "Differential regulation of gamma-aminobutyric acid receptor channels by diazepam and phenobarbital". Annals of Neurology. 25 (3): 213–220. doi:10.1002/ana.410250302. ISSN 0364-5134.
- ↑ Barbiturate intoxication and overdose: MedlinePlus Medical Encyclopedia
- ↑ UN Convention on Psychotropic Substances | https://www.unodc.org/documents/commissions/CND/Int_Drug_Control_Conventions/1971_Schedules/Revision1_2015/ST_CND_1_ADD2_Rev1_e_V1600359.pdf
- ↑ S8 Controlled Drugs | http://www.health.nsw.gov.au/pharmaceutical/Documents/drugsofaddiction-sch8.pdf
- ↑ Branch, L. S. (2022), Consolidated federal laws of Canada, Controlled Drugs and Substances Act
- ↑ "Anlage III BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 26, 2019.
- ↑ Постановление Правительства РФ от 01.10.2012 N 1002 (ред. от 09.08.2019) “Об утверждении значительного, крупного и особо крупного размеров наркотических средств и психотропных веществ, а также значительного, крупного и особо крупного размеров для растений, содержащих наркотические средства или психотропные вещества, либо их частей, содержащих наркотические средства или психотропные вещества, для целей статей 228, 228.1, 229 и 229.1 Уголовного кодекса Российской Федерации” - КонсультантПлюс
- ↑ "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020.
- ↑ Drugs penalties
- ↑ DEA Schedule II Drugs | https://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_12.htm