Scopolamine
Clinical data | |
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Trade names | Transdermscop, Kwells, others |
Other names | Hyoscine[1] |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682509 |
License data |
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intramuscular | |
Drug class |
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ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Metabolism | Liver |
Elimination half-life | 4.5 hours[6] |
Excretion | Kidney |
Identifiers | |
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JSmol) | |
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Scopolamine, also known as hyoscine,[7] or Devil's Breath,[8] is a natural or synthetically produced tropane alkaloid and anticholinergic drug that is used as a medication to treat motion sickness[9] and postoperative nausea and vomiting.[10][1] It is also sometimes used before surgery to decrease saliva.[1] When used by injection, effects begin after about 20 minutes and last for up to 8 hours.[1] It may also be used orally and as a transdermal patch since it has been long known to have transdermal bioavailability.[1][11]
Scopolamine is in the
Medical uses
Scopolamine has a number of formal uses in modern medicine where it is used in its isolated form and in low doses to treat:[20][21]
- Postoperative nausea and vomiting.
- Gastrointestinal spasms
- Renal or biliaryspasms
- Aid in gastrointestinal radiology and endoscopy
- Irritable bowel syndrome
- Clozapine-induced drooling
- Bowel colic
- Eye inflammation[26]
It is sometimes used as a
Breastfeeding
Scopolamine enters breast milk by secretion. Although no human studies exist to document the safety of scopolamine while nursing, the manufacturer recommends that caution be taken if scopolamine is administered to a breastfeeding woman.[27]
Elderly
The likelihood of experiencing adverse effects from scopolamine is increased in the elderly, relative to younger people. This phenomenon is especially true for older people who are also on several other medications. Scopolamine use should be avoided in this age group because of these potent anticholinergic adverse effects, which have also been linked to an increased risk for dementia.[28][29]
Adverse effects
Adverse effect incidence:[5][30][31][32]
Uncommon (0.1–1% incidence) adverse effects include:
- Dry mouth
- Anhidrosis (reduced ability to sweat to cool off)
- Tachycardia (usually occurs at higher doses and is succeeded by bradycardia)
- Bradycardia
- Urticaria(hives)
- Pruritus(itching)
Rare (<0.1% incidence) adverse effects include:
- Constipation
- Urinary retention
- Hallucinations
- Agitation
- Confusion
- Restlessness
- Seizures
Unknown frequency adverse effects include:
- reactions
- Dyspnea(shortness of breath)
- Rash
- Erythema
- Other hypersensitivity reactions
- Blurred vision
- Mydriasis (dilated pupils)
- Drowsiness
- Dizziness
- Somnolence
- Death
Overdose
- Tachycardia
- Arrhythmia
- Blurred vision
- Photophobia
- Urinary retention
- hallucinations
- Cheyne-Stokesrespiration
- Dry mouth
- Skin reddening
- Inhibition of gastrointestinal motility
Interactions
Due to interactions with metabolism of other drugs, scopolamine can cause significant unwanted side effects or unpredictable
Route of administration
Scopolamine can be taken
Pharmacokinetic
Scopolamine undergoes first-pass metabolism and about 2.6% is excreted unchanged in urine. Grapefruit juice decreases metabolism of scopolamine, consequently increasing plasma concentration.[35]
Pharmacodynamics
The pharmacological effects of scopolamine are mediated through the drug's competitive antagonism of the peripheral and central muscarinic acetylcholine receptors. Scopolamine acts as a nonspecific muscarinic antagonist at all four (M1, M2, M3, and M4) receptor sites.[36][37]
In doses higher than intended for medicinal use; the hallucinogenic
Although often broadly referred to as simply being 'anticholinergic',
Biosynthesis in plants
Scopolamine is among the
The
A
Subsequently,
History
Plants naturally containing scopolamine such as
In 1899, a Dr. Schneiderlin recommended the use of scopolamine and morphine for surgical anaesthesia, and it started to be used sporadically for that purpose.[12][47] The use of this combination in obstetric anesthesiology (childbirth) was first proposed by Richard von Steinbuchel in 1902 and was picked up and further developed by Carl Gauss in Freiburg, Germany, starting in 1903.[48] The method, which was based on a drug synergy between both scopolamine and morphine came to be known as Dämmerschlaf ("twilight sleep") or the "Freiburg method".[47][48] It spread rather slowly, and different clinics experimented with different dosages and ingredients; in 1915, the Canadian Medical Association Journal reported, "the method [was] really still in a state of development".[47] It remained widely used in the US until the 1960s, when growing chemophobia and a desire for more natural childbirth led to its abandonment.[49]
Society and culture
Names
Hyoscine hydrobromide is the international nonproprietary name, and scopolamine hydrobromide is the United States Adopted Name. Other names include levo-duboisine, devil's breath, and burundanga.[15][50]
Australian bush medicine
A
Recreational and religious use
While it has been occasionally used recreationally for its hallucinogenic properties, the experiences are often unpleasant, mentally and physically. It is also physically dangerous and officially classified as a
Historically, the various plants that produce scopolamine have been used psychoactively for
In the Bible, there are multiple mentions of Mandrake, a psychoactive and hallucinogenic plant root that contains scopolamine. It was associated with fertility and (sexual) desire where it was yearned for by Rachel, who apparently was "barren" (infertile) but trying to conceive.[61][62]
Interrogation
The effects of scopolamine were studied for use as a truth serum in interrogations in the early 20th century,[63] but because of the side effects, investigations were dropped.[64] In 2009, the Czechoslovak state security secret police were proven to have used scopolamine at least three times to obtain confessions from alleged antistate dissidents.[65]
Use in crime
Scopolamine can render a victim unconscious for 24 hours or more. In large doses, it can cause respiratory failure and death. The most common seems to be recorded in Colombia, where unofficial estimates put the number of annual scopolamine incidents at approximately 50,000. A travel advisory published by the U.S. Overseas Security Advisory Council (OSAC) in 2012 stated:
One common and particularly dangerous method that criminals use in order to rob a victim is through the use of drugs. Scopolamine is most often administered in liquid or powder form in foods and beverages. The majority of these incidents occur in night clubs and bars, and usually men, perceived to be wealthy, are targeted by young, attractive women. It is recommended that, to avoid becoming a victim of scopolamine, a person should never accept food or beverages offered by strangers or new acquaintances, nor leave food or beverages unattended in their presence. Victims of scopolamine or other drugs should seek immediate medical attention.[66]
Between 1998 and 2004, 13% of emergency-room admissions for "poisoning with criminal intentions" in a clinic of Bogotá have been attributed to scopolamine, and 44% to benzodiazepines.[15] Most commonly, the person has been poisoned by a robber who gave the victim a scopolamine-laced beverage, in the hope that the victim would become unconscious or unable to effectively resist the robbery.[15]
Beside robberies, it is also allegedly involved in
Research
Scopolamine is used as a research tool to study memory encoding. Initially, in human trials, relatively low doses of the muscarinic receptor antagonist scopolamine were found to induce temporary cognitive defects.
Scopolamine produces detrimental effects on short-term memory, memory acquisition, learning, visual recognition memory,
Scopolamine has been identified as a psychoplastogen, which refers to a compound capable of promoting rapid and sustained neuroplasticity in a single dose.[92] It has been, and continues to be investigated as a rapid-onset antidepressant, with a number of small studies finding positive results, particularly in female subjects.[93][94][95][96]
NASA agreed to develop a nasal administration method. With a precise dosage, the NASA spray formulation has been shown to work faster and more reliably than the oral form to treat motion sickness.[97]
Although a fair amount of research has been applied to scopolamine in the field of medicine, its
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External links
- Media related to Scopolamine at Wikimedia Commons
- "Scopolamine". Drug Information Portal. U.S. National Library of Medicine.