|Summary sheet: Pentobarbital|
|Common names||Pentobarbital, pentobarbitone, Nembutal|
|Routes of Administration|
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. Pentobarbital drastically enhances the effects of other depressants such as alcohol, and concurrent use may lead to respiratory depression and possibly death.
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.
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.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- 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
- Respiratory depression
- Decreased blood pressure - Barbiturates may decrease blood pressure in some individuals and have occasionally been used to reduce intracranial pressure.
- Seizure suppression
- Physical euphoria
- Decreased libido
- Pain relief - Compared to other agents such as opioids, this effect is generally considered to be quite weak.
- 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
- 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.
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 .
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.
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.
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. 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.
- International: Internationally, pentobarbital is a Psychotropic Schedule III under the UN Convention on Psychotropic Substances.
- United States: In the United States, pentobarbital is a Schedule II Controlled Substance.
- United Kingdom: In the United Kingdom, pentobarbital is a Class B drug.
- Australia: In Australia, pentobarbital is an S8 Controlled Drug.
- Germany: In Germany, pentobarbital is an Anlage III Prescription Only drug.
- Canada: In Canada, pentobarbital is a Schedule IV drug.
- Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
- Barbiturate withdrawal effects | https://www.ncbi.nlm.nih.gov/pubmed/10349206
- Barbiturates for acute traumatic brain injury | http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD000033.pub2/abstract
- Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
- Barbiturates and lung cancer | http://ije.oxfordjournals.org/content/28/3/375.long
- Barbiturates and benzodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436
- Barbiturate Overdose | https://medlineplus.gov/ency/article/000951.htm
- 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
- DEA Schedule II Drugs | https://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_12.htm
- Drug Penalties | https://www.gov.uk/penalties-drug-possession-dealing
- S8 Controlled Drugs | http://www.health.nsw.gov.au/pharmaceutical/Documents/drugsofaddiction-sch8.pdf
- Anlage III Drugs | http://www.drogen-wissen.de/DRUGS/DW_GE/btmg_a3_text.shtml
- Canada Schedule IV Drugs | http://laws-lois.justice.gc.ca/eng/acts/c-38.8/page-15.html#h-31