View source for Talk:Amobarbital

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'''Amobarbital''' (formerly known as '''amylobarbitone''' or '''sodium amytal''' as the soluble sodium salt) is a drug that is a barbiturate derivative. It has sedative-hypnotic properties. It is a white crystalline powder with no odor and a slightly bitter taste. It was first synthesized in Germany in 1923. It is considered a short to intermediate acting barbiturate.<sup>[''citation needed'']</sup> If amobarbital is taken for extended periods of time, physiological and psychological dependence can develop. 

Amobarbital withdrawal mimics delirium tremens and may be life-threatening. Amobarbital was manufactured by Eli Lilly and Company in the US under the brand name Amytal in bright blue bullet shaped capsules (known as Pulvules) or pink tablets (known as Diskets) containing 50, 100, or 200 milligrams of the drug. The drug was also manufactured generically. Amobarbital was widely misused, known as '''Blue Heavens''' on the street. Amytal, as well as Tuinal, a combination drug containing equal quantities of secobarbital and amobarbital, were both manufactured by Eli Lilly until the late-1990s. However, as the popularity of benzodiazepines increased, prescriptions for these medications became increasingly rare beginning in the mid to late-1980s.

==Chemistry==
Amobarbital (5-ethyl-5-isoamylbarbituric acid), like all barbiturates, is synthesized by reacting malonic acid derivatives with urea derivatives. In particular, in order to make amobarbital, α-ethyl-α-isoamylmalonic ester is reacted with urea (in the presence of sodium ethoxide).

==Pharmacology==
In an in vitro study in fat thalamic slices amobarbital worked by activating GABAA receptors, which decreased input resistance, depressed burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increased both the amplitude and decay time of inhibitory postsynaptic currents.[2]

Amobarbital has been used in a study to inhibit mitochondrial electron transport in the rat heart in an attempt to preserve mitochondrial function following reperfusion.[3]

A 1988 study found that amobarbital increases benzodiazepine receptor binding in vivo with less potency than secobarbital and pentobarbital (in descending order), but greater than phenobarbital and barbital (in descending order).[4] (Secobarbital > pentobarbital > amobarbital > phenobarbital > barbital)

It has an LD50 in mice of 212 mg/kg s.c.

==Subjective effects==
{{Preamble/SubjectiveEffects}}                                                                        
{{effects/base
|{{effects/physical|
*'''[[Effect::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.
*'''[[Effect::Motor control loss]]''' 
*'''[[Effect::Muscle relaxation]]
*'''[[Effect::Dizziness]]'''
*'''[[Effect::Decreased blood pressure]]''' - Barbiturates may decrease blood pressure in some individuals and have occasionally been used to reduce intracranial pressure.<ref>Barbiturates for acute traumatic brain injury | http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD000033.pub2/abstract</ref>
*'''[[Effect::Respiratory depression]] 
*'''[[Effect::Seizure suppression]]'''
*'''[[Effect::Physical euphoria]]''' - The physical euphoria with Amobarbital is very strong and similar to short-acting barbiturates such as [[pentobarbital]] and [[secobarbital]].
*'''[[Effect::Decreased libido]]'''

}}

{{effects/visual|
*'''[[Effect::Acuity suppression]]''' - Like many [[depressant |depressants]], high doses of amobarbital may cause blurred vision.
}}

|{{effects/cognitive|
*'''[[Effect::Anxiety suppression]]'''
*'''[[Effect::Cognitive euphoria]]''' - This effect is strong and similar to [[pentobarbital]] and [[secobarbital]]. The feeling itself can be described as an extremely strong feeling of relaxed contentment.
*'''[[Effect::Thought deceleration]]'''
*'''[[Effect::Analysis suppression]]'''
*'''[[Effect::Disinhibition]]'''
*'''[[Effect::Amnesia]]'''
*'''[[Effect::Language suppression]]''' - At higher doses, amobarbital is known to cause slurred speech.
*'''[[Effect::Compulsive redosing]]'''
*'''[[Effect::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 [[antipsychotic]]s.
*'''[[Effect::Delusions|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:

*[https://erowid.org/experiences/subs/exp_Barbiturates_Amobarbital.shtml Erowid Experience Vaults: Amobarbital]


==Toxicity and harm potential==
[[File:harmchart.png|thumb|right|300px|Radar plot showing relative physical harm, social harm, and dependence of barbiturates in comparison to other drugs.<ref>Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644</ref>]]
Amobarbital likely has [[Toxicity::moderate toxicity]] relative to dose. However, amobarbital is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[alcohol]] or [[opioids]]]]. Phenobarbital has a higher risk of death or serious adverse effects associated with concurrent [[depressant]] use than other drugs such as benzodiazepines. 

It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug.

===Lethal dosage===
It has an LD50 in mice of 212 mg/kg s.c.

===Tolerance and addiction potential===
Amobarbital is [[Addiction potential::extremely physically and psychologically addictive]]. Barbiturate withdrawal is medically serious and can potentially cause a life-threatening withdrawal syndrome that can cause [[seizure |seizures]], [[psychosis]], and death. Drugs which lower the seizure threshold such as [[tramadol]] and [[amphetamine]] should be avoided during withdrawal. 

Tolerance will develop to the sedative-hypnotic effects of amobarbital after prolonged use. It is unknown exactly how long it takes for tolerance to reach baseline. Amobarbital 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. [https://www.google.com/ 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.
*'''[[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 [[stimulant]]s due to the risk of excessive intoxication. Stimulants decrease the [[sedation|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 [[benzodiazepine |benzodiazepines]] and [[alcohol]] since they work in a similar fashion, but bind to distinct allosteric sites on the GABA<sub>A</sub> receptor, thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA<sub>A</sub> 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<ref>Barbiturates and benzodiazepine effects | https://www.ncbi.nlm.nih.gov/pubmed/2471436</ref>. 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]], [[language suppression |slurred speech]], [[confusion]], [[delusions]], [[respiratory depression]], coma or death<ref>Barbiturate Overdose | https://medlineplus.gov/ency/article/000951.htm</ref>.

==Legal status==
Internationally, amobarbital is listed in Schedule IV of the UN Convention on Psychotropic Substances.<ref>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</ref>

==See also==
*[[Depressant |Depressants]]
*[[Benzodiazepine |Benzodiazepines]]
*[[GABA]]

==External links==
*[https://en.wikipedia.org/wiki/Amobarbital Amobarbital (Wikipedia)]
http://isomerdesign.com/PiHKAL/search.php?domain=pk&id=3973&name=Amobarbital

==Literature==

*APA formatted reference

Please see the [[citation formatting guide]] if you need assistance properly formatting citations.

==References==
<references />

[[Category:Psychoactive substance]]
[[Category:Depressant]]
[[Category:Anxiolytics]]
[[Category:Barbiturate]]
[[Category:Phenethylamine]]