Scopolamine
Scopolamine is a naturally occurring tropane alkaloid found in plants of the Solanaceae family, including Datura species, where it serves as the primary psychoactive compound. Structurally related to atropine and hyoscyamine, it acts as a muscarinic acetylcholine receptor antagonist. While medically approved for the prevention of motion sickness and postoperative nausea1, recreational doses produce intense deliriant hallucinations. Medium to high doses carry significant adverse effects, and extreme caution is strongly advised.
Contents
Dosage & Duration
Dosage
Absorption observations included 0.5 mg administrations, but dose-tier ranges were not available.
Subjective Effects
Effects vary widely by individual, dose, and context.
Physical
The physical effects of datura are usually described as extremely uncomfortable. They can be broken down into several components all of which progressively intensify proportional to dosage. These are described below and generally include:
Cognitive
The cognitive effects of datura are described by many as generally negative and dysphoric throughout the trip, primarily consisting of extreme paranoia and feelings of impending doom. It is largely confusing and disorienting often leading to a complete inability to communicate or understand normal language. It contains unique cognitive effects found almost exclusively in the deliriant class. The most prominent of these effects include:
Visual
Distortions
As for visual distortions and alterations, effects experienced are detailed below:
Hallucinatory States
The effects of Datura are extremely efficient at inducing delirious hallucinations which can be broken into the two categories described below:
Suppressions
Datura does not enhance visual stimuli in the way that psychedelics do; instead they tend to degrade and decrease visual aptitude both increasing hallucination and degrading vision. These components are detailed below:
Auditory
The auditory effects of Datura are common in their occurrence and exhibit a range of effects which commonly includes:
Reagent Testing
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Pharmacology
Pharmacodynamics
Scopolamine acts as a non-selective competitive antagonist at muscarinic acetylcholine receptors2 (M1 through M5), with relatively weaker inhibition at the M5 subtype. Through this broad antimuscarinic activity, it disrupts parasympathetic signaling in both the central and peripheral nervous systems.2 The hallucinogenic and deliriant properties associated with higher doses are specifically linked to antagonism of postsynaptic M1 receptors; no other muscarinic subtypes have been implicated in these effects.3 Scopolamine has also been reported to interact with neuronal nicotinic acetylcholine receptor subunits (alpha-4 and beta-2), though these interactions remain poorly characterized.
Pharmacokinetics
Scopolamine is primarily metabolized in the liver, though its metabolic pathway in humans remains incompletely characterized. CYP3A4 is implicated in oxidative demethylation, as supported by in vitro studies and altered pharmacokinetics observed with grapefruit juice coadministration. The primary metabolites are various glucuronide and sulfide conjugates. Oral bioavailability is low due to substantial first-pass metabolism2, with estimates ranging from roughly 13% to 20-40%, while intranasal administration achieves considerably higher bioavailability at approximately 83%. Reported elimination half-life values for oral administration vary between roughly 1 hour and an average of 5 hours (range 2-10 hours); intravenous and intramuscular routes show half-lives of approximately 69 minutes. About 2.6% of an oral dose is recovered unchanged in urine.2
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Tolerance
Other anticholinergic/antimuscarinic agents
Harm Potential
Addiction & Dependence
Psychological
Extremely LowPsychological addiction potential is minimal due to the typically unpleasant nature of the experience. Recreational use is rare as effects are often described as mentally and physically distressing rather than rewarding.
Physical
ModeratePhysical dependence can develop with chronic therapeutic use. Withdrawal symptoms include nausea, dizziness, vomiting, gastrointestinal disturbances, sweating, headaches, bradycardia, hypotension, and various neuropsychiatric manifestations.1 Severe symptoms may require medical attention.
Toxicity
CNS depression ranging from drowsiness to coma can occur with overdose;1 cognitive impairment and impaired ability to operate machinery are documented effects at therapeutic and higher doses.
Gastrointestinal effects including decreased bowel sounds and constipation can occur;1 these effects are typically associated with the anticholinergic mechanism rather than direct toxicity.
Urinary retention can occur as an anticholinergic effect, particularly at higher doses or in susceptible individuals.1
Psychosis Risk
Scopolamine is formally classified as a deliriant and can exacerbate psychosis and cause psychiatric reactions including hallucinations, confusion, agitation, and restlessness.1 Mass hospitalizations for psychosis have occurred following ingestion of scopolamine-containing substances; more than 20 people were hospitalized with psychosis in Norway in 2008 after ingesting counterfeit tablets containing scopolamine.5
Seizure Risk
Seizures and seizure-like activity are documented neuropsychiatric effects but are rare, occurring in less than 0.1% of patients at therapeutic doses.4 Convulsions have been reported in overdose cases.1
History & Culture
Traditional and Spiritual Use
Plants naturally containing scopolamine, including Atropa belladonna (deadly nightshade), Brugmansia (angel's trumpet), Datura (jimsonweed), Hyoscyamus niger, Mandragora officinarum, Scopolia carniolica, Latua, and Duboisia myoporoides, have been recognized and utilized for various purposes in both…
Legality
By Country
References
Source Pages
Citations
- (2024-03-14). TRANSDERM SCOP- scopolamine patch, extended release. DailyMed. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b877a694-a1d0-4280-937a-a06820b12a88123456789101112
- Renner UD, Oertel R, & Kirch W. (2005). Pharmacokinetics and pharmacodynamics in clinical use of scopolamine. Therapeutic Drug Monitoring, 27(5), 655-665. https://doi.org/10.1097/01.ftd.0000168293.48226.571234
- Dawson AH, & Buckley NA. (2016). Pharmacological management of anticholinergic delirium - theory, evidence and practice. British Journal of Clinical Pharmacology, 81(3), 516-524. https://doi.org/10.1111/bcp.128391
- (18 September 2017). Hyoscine 400 micrograms/ml Solution for Injection. (emc). https://www.medicines.org.uk/emc/product/3581/smpc123
- Vallersnes OM, Lund C, Duns AK, Netland H, & Rasmussen IA. (2009). Epidemic of poisoning caused by scopolamine disguised as Rohypnol tablets. Clinical Toxicology, 47(9), 889-893. https://doi.org/10.3109/155636509033338041
- (n.d.). Genesis 30:14–16 (King James Version). Bible Gateway. http://www.biblegateway.com/passage/?search=Genesis%2030:14-16&version=KJV1
- (2019). The Use of Morphine and Scopolamine to Induce Twilight Sleep. https://embryo.asu.edu/pages/use-morphine-and-scopolamine-induce-twilight-sleep12
- (7 June 2019). Visitors to Art of Healing exhibition told how Australian Indigenous bush medicine was given to every allied soldier landing at Normandy on D-Day. kcl.ac.uk. https://www.kcl.ac.uk/news/australian-indigenous-bush-medicine-was-given-to-allied-soldiers-on-d-day123
- (n.d.). TRANSDERM SCOP - scopolamine patch, extended release (DailyMed label setid b877a694). DailyMed / NLM. https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=b877a694-a1d0-4280-937a-a06820b12a881
- (2015). Transdermal patches: history, development and pharmacology. https://pmc.ncbi.nlm.nih.gov/articles/PMC4403087/1
- (n.d.). Hyoscine hydrobromide (scopolamine) - WHO Electronic Essential Medicines List. World Health Organization. https://list.essentialmeds.org/medicines/2811
- (2014). Childbirth, Scopolamine and the History of Truth Serum. Nature's Poisons. https://naturespoisons.com/2014/03/06/childbirth-scopolamine-and-the-history-of-truth-serum/1
- (n.d.). Scopolamine: The Realities of Devil's Breath in Colombia. Medellin Guru. https://medellinguru.com/scopolamine/1
- (2008). Scopolamine Hydrobromide Injection - Product Information (DIN 02242811). Health Canada Drug Product Database. https://health-products.canada.ca/dpd-bdpp/info?lang=eng&code=666361
Further Reading
Automated synthesisInformation aggregated and synthesized using an autonomous workflow built by Josie Kins.
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