| Deliriant | |
|---|---|
| Drug class | |
 Chemical structure ofscopolamine, one of the most well-known deliriants. | |
| Class identifiers | |
| Synonyms | Antimuscarinic; Anticholinergic; Muscarinic antagonist; Muscarinic acetylcholine receptor antagonist |
| Use | Recreational,medical |
| Mechanism of action | Muscarinic acetylcholine receptorantagonism |
| Biological target | Muscarinic acetylcholine receptors |
| Chemical class | Various |
| Legal status | |
| Legal status |
|
| In Wikidata | |
Deliriants are a subclass ofhallucinogen. The term was coined in the early 1980s to distinguish these drugs frompsychedelics such asLSD anddissociatives such asketamine, due to their primary effect of causingdelirium, as opposed to the more lucid and less disturbed states produced by other types of hallucinogens, where rational thought is better preserved (including the ability to distinguish hallucinations from reality).[1] The term generally refers toanticholinergic drugs, which aresubstances that inhibit the function of theneurotransmitteracetylcholine.[1]
Common examples of deliriants include plants of the generaDatura andBrugmansia, both containingscopolamine, as well as higher than recommended dosages ofdiphenhydramine (Benadryl).[2][3] A number of plant deliriants such as that of theSolanaceae family, particularly in theAmericas, have been used by someindigenous cultures to reach delirious andaltered states of consciousness for traditions or rituals, such as rites of passage,divination orcommunicating with the ancestors.[4] Despite their long history of use, deliriants are the least-studied class of hallucinogens in terms of their behavioral and neurological effects.[5]
The term was introduced byDavid F. Duncan andRobert S. Gold due to a characteristic delirium-like effect which is known to manifest as a reoccurring symptom for anticholinergic hallucinogens.[1] The term deliriant originates from delirium (dēlīrĭum) which comes from the Latin verb delirare, which means 'to go off the furrow', 'to derail'. liria (furrow) - The earth thrown up between two furrows, a ridge. ex, e - out of, from. delirio - frenzy,madness, deranged.[5] It is said to be a figurative reference to going off or out of thefurrow whenploughing (agricultural) so as to be analogous to the mental aberration that is being in delirium.
The altered state of consciousness produced by common or 'classical' deliriant substances such asscopolamine,atropine anddiphenhydramine is mediated through the drug compounds' competitiveantagonism of the peripheral and centralmuscarinic acetylcholine receptors, especially theM1 muscarinic receptor. M1 receptors are located primarily in thecentral nervous system and are involved in perception, attention, and cognitive functioning.
Delirium is primarily associated with antagonism ofpostsynaptic M1 receptors.[6][7] However, antagonism of both the M1 receptor and theM2 receptor have been implicated as having negative effects onmemory andcognition, and theselective M2 receptor antagonisthyoscyamine has been reported to produce deliriant effects similarly to M1 receptor antagonists.[6][8] Conversely, theM3 receptor has not been implicated in cognition.[8]
The central nervous system actions of deliriants are complex, and other muscarinic acetylcholine receptors, including the M3,M4, andM5 receptors, may also be involved in the effects of the drugs.[9] As an example, the M1, M2, M4 and M5 receptors have all been implicated in regulatingdopamine release, with the M1, M2, and M4 receptors having inhibitory effects on dopamine release and the M5 receptor having stimulatory effects.[9]
Peripheral muscarinic receptors are part of theautonomic nervous system. M2 receptors are located in the brain and heart, M3 receptors are in salivary glands and M4 receptors are in the brain and lungs.[7] Scopolamine is a nonspecific muscarinic antagonist at all four (M1,M2,M3, andM4) receptor sites.[10][11] Due to these compounds' inhibition of various signal transduction pathways, the decrease inacetylcholine signaling is what leads to many of the cognitive deficits and mental impairments.[12]
It has also been said that common anticholinergic agents/hallucinogens should be more accurately referred to asantimuscarinics, as for instance these agents do not generally blocknicotinic receptors.[7]
Thehallucinogenic experience anddelirium produced, particularly by (M1 inhibiting) anticholinergics is characterized bystupor,agitation,confusion,confabulation,emotional bluntness,dysphoria,memory deficits, incoherency of thoughts,hypoactivityorhyperactivity (mixed delirium), lucid intervals,akathisia, realisticvisualhallucinations or illusions (as opposed to thepseudohallucinations experienced on other classes of hallucinogens) and regression to "phantom" behaviors such asdisrobing,plucking or interacting with imaginary objects or scenes.[13][7] The effects of these kinds of anticholinergic compounds have also been likened todelirious fevers,sleepwalking,fugue states orpsychotic episodes in that the subject has minimal control over their actions and may have little or norecollection of the experience afterwards. This is a notable departure from the effects ofserotonergicpsychedelics.[3][14]
Scopolamine has been shown to exert a greater impairment onepisodic memory,event-related potentials,memory retention andfree recall compared toDPH (an anticholinergic andantihistamine).[15] Some antihistamines may also act as deliriants in high doses.[citation needed] Due to scopolamine's prominent amnesiac and impairing effects, it has been used inColombia for criminal purposes such as 'drugging' individuals, usually perceived as wealthy, and robbing them due to scopolamine's discombobulating effects and enhancedsuggestibility.[16] It is usually done by putting the extracted and isolated powder form of the alkaloid in a victim's (alcoholic) drink, oftentimes directly by or with the help of attractive women to act as criminal accomplices to the robbers.[17][18][19]
In Colombia, isolated (powdered) scopolamine has become infamous and is referred to there by several monikers such asBurundanga and "Devil's Breath". It is usually extracted by criminals from theBorrachero Tree and may even occasionally be encountered as astreet drug there.[20]
Theantimuscarinic plant-based alkaloids scopolamine and atropine are also notorious for their characteristic hyperactive effects and ability to cause stark and dream-like hallucinations.[5][21] The hallucinations themselves are often described by users as disturbing, unpleasant or dark in nature.[22][2][23] Other commonly reported behaviors and experiences include holding conversations with imagined persons orentities, smoking nonexistent cigarettes (even with nonsmokers), visual hallucinations of spiders orshadow figures or being unable to recognize one'sown reflection in a mirror.[2] Deliriants in particular appear to be noted for their powerful effects on users' behavior.[5]
Ken Hedges, who was curator of archaeology at theSan DiegoMuseum of Man, and also studied hallucinogen-based Kumeyaayrock art recalled how when he was a student at San Diego's Mount Miguel High School in 1960, two teenage boys inOjai who sampleddatura were found on that town's main street at night; "in a state of mind that could only be called extremely deranged, they were walking from streetlight to streetlight, banging their heads on each pole until they were covered with blood." Hedge claimed that even amongNative Americans, "terrifying visions" were often the result for "those who submitted themselves to the plant's power."[24]Anthropological assessment of the sacredChumashDatura cult inSouthern California ascertained that within the tribe, frequent or repeat users ofdatura tended to gradually become more and more antisocial, often adopting behavior patterns that the rest of the tribe viewed as "capricious malevolence".[25]
During one of his workshops in Hawaii, psychonautTerence McKenna discussed the effects of the hallucinogenicSolanaceae plants compared to psychedelics, stating that:
"They (solanaceae deliriants) are psychoactive and interesting. I don't know how much is to be learned there. It seems to me it's a path of power, and it's also a path of danger. They're quite peculiar. It's hard to keep control. It's the drug where people invariably tear their clothes off and run into public. I mean, I don't know why they do that but just over and over again you hear stories of people taking their clothes off and then going into public… In Nepal, there isDatura metel, which is theconspecific species toDatura meteloides in North America, and we would grind it up and take the seeds and… it's freaky. It doesn't teach you about higher consciousness, it sort of leads you into a world oftwilight confusion and magical and somewhat demonic forces… A lot of sorcery goes on arounddatura, especially in Latin America. It's a strange world. A world of shadows and forces, and shifting boundaries."
During an on-camera interview, author ofThe God Molecule: 5-MeO-DMT and the Spiritual Path to the Divine Light, Gerardo Ruben Sandoval Isaac explained that in the Oaxaca "mushroom village" ofSan José del Pacifico, thepsilocybin mushrooms are regarded as being "related to light" and that (Brugmansia) is "related to the darkness" and that they (the tribes) "are aware of the polarity of this flower", further crediting the idea that the hallucinogenic experience produced by deliriants is typically of a "dark" and disturbing nature.[citation needed] Whendatura was first formally discovered in colonialJamestown,Virginia in 1676 by English soldiers duringBacon's Rebellion, they spent 11 days in altered mental states after using the leaves of the plant, which they did not know were psychoactive and poisonous, as part of a salad.[26]
HistorianRobert Beverley Jr. wrote of the observable effects seen during their intoxicated state; "They (the soldiers) turned natural fools upon it for several days: one would blow up a feather in the air; another would dart straws at it with much fury; and another, stark naked, was sitting up in a corner like a monkey, grinning and making mows (grimaces) at them; a fourth would fondly kiss and paw his companions, and sneer in their faces with a countenance more antic than any in a Dutch droll… They were not very cleanly; for they would have wallowed in their own excrements if they had not been prevented. A thousand such simple tricks they played, and after eleven days returned (to) themselves again, not remembering anything that had passed."[26]
Naturally-occurring anticholinergic deliriants are found in the plant speciesAtropa belladonna (deadly nightshade), variousBrugmansia species (Angel's Trumpets),Datura stramonium (Jimson weed),Hyoscyamus niger (henbane), andMandragora officinarum (mandrake) in the form of thetropane alkaloidsscopolamine,atropine, andhyoscyamine. Other, lesser known plant sources of scopolamine and related tropanes includeScopolia carniolicaendemic toEurope,Latua endemic to southernChile,Solandra endemic toMexico andDuboisia myoporoides, which is endemic toAustralia and contains bothscopolamine andnicotine.[27][21][28] Scopolamine has often been considered,pharmacologically andpsychonautically the premier and paradigmatic deliriant substance, to which all other deliriants and/or antimuscarinic hallucinogens are usually compared.[29][4]
Synthetic compounds such asdiphenhydramine (Benadryl),dimenhydrinate (Dramamine), andtropine benzilate are deliriants.Nutmeg, although purportedly not as strong or as unpleasant as diphenhydramine or scopolamine, is considered a deliriant, due to its propensity to cause anticholinergic-like symptoms when taken in large doses.[30] The effects caused bymyristicin andelemicin found innutmeg's essential oil can last up to several days, similarly to the tropane alkaloids found indatura.[31][32] The mushroom referred to asfly agaric with its active agentsibotenic acid andmuscimol may also be considered an 'atypical' deliriant, although fly agaric is probably more accurately described as ahypnotic.[33][34]
In rare cases, highly toxic plants from theAconitum (wolfsbane) genus have been used as "deliriants" by certain groups practicingEuropean witchcraft, theleft-hand path orasceticism due to the unpleasant but supposedaltered state of consciousness which can be a side effect of wolfsbane poisoning. Plants of the aconitum genus contain theneurotoxinaconitine and in the case ofAconitum ferox, an extremely toxic alkaloid calledpseudaconitine, which is in rare cases, taken as anordeal poison andentheogen on theIndian subcontinent by ascetic groups such as theAghori, where it may be mixed with other psychoactive plants or poisons such as datura andcannabis. Risk of death is considered very high when takingA. ferox and its use is restricted to only the most experiencedadepts of their particular school ofShivaism.[35][36][37]
Despite the fully legal status of several common deliriant plants andOTC medicines, deliriants are largely unpopular asrecreational drugs due to the severe dysphoria, uncomfortable and generally damaging cognitive and physical effects, as well as the unpleasant nature of the hallucinations.[23][22] Anticholinergics are said to be typically responsible for 15–20% of acute poisoning admissions, up to 40% of poisoning admission tointensive care units and 16% of poison centre calls. The anticholinergic syndrome may be accompanied by sedation,coma, seizures and/orcardiovascular toxicity not necessarily mediated by muscarinic antagonism but rather secondary to other drug effects on other receptors orion channels.[7] In theory, an idealantidote for theanticholinergic syndrome caused by these particular substances would be a selectiveM1receptor agonist. Some are in development but reportedly as of 2016, none are in clinical use.[7]
Ultimately, user reports of recreational deliriant usage on the drug resource websiteErowid also generally indicate a firm unwillingness to repeat the experience.[38] In addition to potentially dangerous mental/behavioral effects (accidents during deliriant experiences are common)[39] sometropane alkaloids, such as those found in plants of theDatura genus, are exceptionally toxic and can cause death due totachycardia-induced heart failure,hypoventilation andhyperthermia even in small doses.[40] Anticholinergics have been shown to increase the risk of developingdementia with long-term use, even at therapeutic doses, therefore they are presumed to carry an even greater risk when used at hallucinogenic dosages.[41][42] Scopolamine in particular has been implemented in scientific models used to study thecholinergic hypothesis for Alzheimer's disease and other related dementias.[43]
Despite these overtly negative effects both on the physical and mental health of the user, usage of deliriants for recreational purposes has still gone on for centuries and was said to be introduced inEurope and surrounding areas bythe Romani people, who would smoke or ingest plants such asdatura to experience hallucinations.[44] It has been said that certain groups who used deliriant plants, especially inhedgewitchery (wortcunning) practices, would traditionally mix in medicinal orneuroprotective plants either directly during theintoxications or later on to counter negative health consequences or symptoms such as dysphoria or senility.[45][46][47]
.jpg)
Deliriants such ashenbane, belladonna, mandrake,jimsonweed andfly agaric are associated with and featured in many stories and beliefs withinEuropean mythology.[48][49][50][47] In ancient Greek myth, wreaths of henbane leaves were used to crown the newly deceased to make them forget their former lives as they crossed or wandered near theRiver Styx in theunderworld.[14] Thebelladonna plant genus,Atropa is named after theGreek Fate,Atropos, who cut the thread of life.[50] In early medieval times, Mandrake was believed to have commonly grown undergallows wherebodily fluids dripped from the bodies of deceased murderers, with some sources stating blood and others claimingsemen or urine.[14][51][52]
Tropane-containing nightshades have played an integral role inOld Worldfolklore andEuropean witchcraft.[21][51][45] Henbane is reputed for having been used inGreco-Roman magic during ancient times as well as being associated withblack magic andmaleficium during theLate Middle Ages.[21] During this period in medieval Europe, the Central European speciesScopolia carniolica was also used as an admixture inlove potions.[53] Belladonna was purported to aid in the "flight of witches" where they reportedly would experience "bacchanaliancarousal" or hallucinatorydreaming.[45][54]
Mandrake (the root ofMandragora officinarum) is mentioned twice in theBible,[55][56] and was also frequently mentioned as a typical ingredient inflying ointment recipes since at least as far back as theEarly Modern Period.[48] During this time period, theNew World plantdatura stramonium (jimsonweed) was discovered inNorth America by colonialists and eventually lumped in with the other classic 'witches weeds' of the nightshade family that were endemic to Europe.[48][21] Datura has a long history of usage both inMexico and theSouthwestern United States by indigenous cultures using it forritualistic,sacred andmagical purposes.[57][58][4]
In modern times, bothDatura andBrugmansia are still used for sorcery, black magic, andshamanism inLatin America.[59][60] In certain South American countries, members of theBrugmansia genus have been known to be occasionally added toayahuasca brews by malevolent sorcerers (brujos) or bad shamans who wish to take advantage of unsuspecting tourists. Genuine shamans (curanderos) believe one of the purposes for this is to "steal one's energy and/or power", of which they believe every person has a limited amount.[60]
Since medieval times, extremelynoxious plants of theAconitum (wolfsbane) genus were also associated with folklore and magic and were used for similar purposes as the tropane-containing nightshades.[21] Despite being a highly poisonous and often deadly plant to work with, it was still often included in recipes for flying ointments and magical salves, likely as a way to help counteract both thecardiac andhyperthermic side effects of the scopolamine.[35][45] The aconitum genus (specificallyaconitum napellus) was firmly associated withsuperstition and witchcraft in Europe, particularly when it came to mythos surrounding werewolves andlycanthropy.[61][45] This is believed to have originated at least partially from wolfsbane's alleged tendency to causeparesthesia which supposedly can be reported to feel like one's body is covered in fur.[35] InGreek mythology, the goddessHecate is said to have invented aconitum whichAthena used to transformArachne into a spider.[62][63]
Anticholinergics[edit]
Disubstitutedglycolic acid esters: | Antihistamines[edit]
Other[edit]
|
Delirium is only associated with the antagonism of post‐synaptic M1 receptors and to date other receptor subtypes have not been implicated
Antagonism at M1 and M2 receptors have negative impact on memory and cognition [60]. [...] Atropine and scopolamine are non-selective competitive antagonist of muscarinic receptors. Atropine has the highest affinity for subtype M1, followed by M2 and M3 and weak affinity for M4 and M5 [71]. On the other hand, scopolamine has strong affinity for M1-M4 compared to M5 [72] while hyoscyamine binds to M2 only [73].
Media related toDeliriants at Wikimedia Commons
