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Scopolamine, also known as hyoscine, is a tropane alkaloid drug with muscarinic antagonist effects.
It is obtained from plants of the family Solanaceae (nightshades), such as henbane or jimson weed (Datura species). It is among the secondary metabolites of these plants.
The drug can be highly toxic and should be used in minute doses. As an example, in the treatment of motion sickness, the dose, gradually released from a transdermal patch, is only 0.33 milligram of scopolamine per day. An overdose can cause delirium, delusions, paralysis, stupor and death.
Additional recommended knowledge
Scopolamine is named after the plant genus Scopolia. The name "hyoscine" is from the scientific name for henbane, Hyoscyamus niger.
Scopolamine acts as a competitive antagonist at specific muscarinic acetylcholine receptors, specifically M1 receptors; it is thus classified as an anticholinergic, or, more specifically, as an anti-muscarinic drug. (See the article on the parasympathetic nervous system for details of this physiology.)
In medicine scopolamine has 3 primary uses: treatment of nausea and motion sickness, treatment of intestinal cramping, and for ophthalmic purposes. Use as a general depressant and adjunct to narcotic painkillers is also common. The drug is less commonly used as a preanesthetic agent and uncommonly for some forms of Parkinsonism. Scopolamine is also used as an adjunct to narcotic analgesia, such as the product Twilight Sleep which contained morphine and scopolamine, some of the original formulations of Percodan and some European brands of methadone injection, as well as use of tablets or patches to combat nausea as well as enhance the pain-killing ability of various opioids. Scopolamine can be used as an occasional sleep aid and was available in some over the counter products in the United States for this purpose until November 1990.
Routes of administration
Scopolamine can be administered by transdermal patches, oral, ophthalmic and intravenous. The transdermal patch for prevention of nausea and motion sickness employs scopolamine base. The oral, ophthalmic and intravenous forms are usually scopolamine hydrobromide (for example in Donnatal).
Its use in the form of a transdermal patch to prevent post-operative nausea is perhaps its greatest current use in the US.
The drug is used in eye drops to induce mydriasis (pupillary dilation) and cycloplegia (paralysis of the eye focusing muscle), primarily in the treatment of eye disorders that benefit from its prolonged effect, e.g. uveitis, iritis, iridocyclitis, etc.
Scopolamine, in common with the large percentage of anticholinergics which cross the blood-brain barrier such as diphenhydramine, dicyclomine, trihexyphenidyl and related drugs, is said to produce euphoria at and around therapeutic doses as well as to potentiate this and other effects of morphine, methadone, hydromorphone, oxycodone and other opioids. It is therefore occasionally seen as a recreational drug. The use of medical scopolamine (most often in the form of tablets) for euphoria is uncommon but does exist and can be seen in conjunction with opioid use. The euphoria is the result of changes in dopamine and acetylcholine levels and ratios and appears to be related to some part of the chemical structure of the drug and other factors known or unknown -- even closely related drugs like atropine and hyoscyamine do not produce euphoria whilst the others listed above certainly appear to.
Another separate group of users prefer dangerously high doses, especially in the form of datura or belladonna preparations, for the deliriant and hallucinogenic effects. The hallucinations produced by scopolamine, in common with other potent anticholinergics, are especially real-seeming and create a perception of a new world filled with frenzied, violent energy. The difference in realism of hallucinations caused by anticholinergics such as scopolamine and other hallucinogens such as the phenethylamines or dissociatives like PCP is quite large. Additionally, an overdose of scopolamine can quite often be fatal, unlike other more commonly used hallucinogens. For these reasons, naturally occurring anticholinergics are rarely used for recreational purposes.
The use of scopolamine as a truth drug was investigated in the 1950s by various intelligence agencies, including the CIA as part of Project MKULTRA. Nazi doctor Josef Mengele experimented on scopolamine as an interrogation drug.
In Colombia a plant admixture containing scopolamine called Burundanga has been used shamanically for decades. In recent years the criminal use of scopolamine has become an epidemic. Approximately fifty percent of emergency room admissions for poisoning in Bogotá have been attributed to scopolamine.
Also in Caracas, Venezuela, crime related to burundanga techniques has multiplied in the last years. Targets are easily approached and just with physical contact they administer the drug to the victim. Reports of techniques of administration include wafting the powder to the victim with a puff of air, drugged chewing gum, or even craftily dropping the powder into the collar of a shirt or the front of a woman's low-cut dress.
Victims of this crime are often admitted to a hospital in police custody, under the assumption that the patient is experiencing a psychotic episode. A telltale sign is a fever accompanied by a lack of sweat.
Scopolamine is used criminally as a date rape drug and as an aid to robbery, the most common act being the clandestine drugging of a victim's drink. It is preferred because it induces retrograde amnesia, or an inability to recall events prior to its administration or during the time of intoxication.
Scopolamine is being investigated for its possible usefulness alone or in conjunction with other drugs in assisting people in breaking the nicotine habit. The mechanism by which it mitigates withdrawal symptoms appears to be at least partially different from that of clonidine meaning that the two drugs can be used together without duplicating or cancelling out the effects of each other.
Scopolamine (hyoscine) causes memory impairments to a similar degree as diazepam.
The common side effects are related to the anticholinergic effect on parasympathetic postsynaptic receptors: dry mouth, throat and nasal passages, thirst, blurred vision and sensitivity to light, constipation, difficulty urinating and tachycardia. Other effects include flushing and fever, as well as excitement, restlessness, hallucinations, or delirium, especially with higher doses. These side effects are commonly observed with oral or parenteral uses of the drug and generally not with topical ophthalmic use. An extreme adverse reaction to ultra-high doses of drugs and other preparations containing scopolamine is temporary blindness which can last up to 72 hours.
Sometimes side effects of scopolamine can be mistaken for symptoms of cancer because of the nausea and anisocoria associated with brain tumors. However, scopolamine induced anisocoria clears up usually within 3 days.
Use in scuba diving has led to the discovery of another side effect. In deep water, below 50–60 feet, some divers have reported pain in the eyes, but the pain subsides quickly if the diver ascends to a depth of 40 feet or less. Mydriatics can precipitate an attack of glaucoma in susceptible patients, so the medication should be used with extra caution among divers who intend to go below 50 feet.
When combined with morphine, it produces amnesia and a tranquilized state known as twilight sleep. Although originally used in obstetrics, it is now considered dangerous for that purpose for both mother and baby.
Scopolamine was one of the active ingredients in Asthmador, an over the counter smoking preparation marketed in the 1950's and 60's claiming to combat asthma and bronchitis.
Scopolamine was used in the 1940s through the 1960s that put mothers in labor into a kind of "twilight sleep" that didn’t stop pain, but merely eliminated the memory of pain by attacking the brain functions responsible for self-awareness and self-control. Often, this resulted in a kind of psychosis, followed by post-traumatic stress-like memories in thousands of new mothers.
Scopolamine was an ingredient used in some over-the-counter sleep aids prior to November 1990 in the United States, when the FDA forced several hundred ingredients allegedly not known to be effective off the market. Scopolamine shared a small segment of this market with diphenhydramine, phenyltoloxamine, pyrilamine, doxylamine and other first generation antihistamines, many of which are still used for this purpose in drugs like Sominex, Tylenol PM, NyQuil and so on.
"I had been shot full of dope to keep me quiet. Perhaps scopolamine too, to make me talk." (quote by Marlowe in Farewell, My Lovely)
"There's a drug called scopolamine, truth serum, that sometimes makes people talk without their knowing it. It's not sure fire, any more than hypnotism is. But it sometimes works." (quote by Marlowe in "Farewell, My Lovely")
Back in the forties Scopolamine showed promise, and still does today, to some degree, as a "truth serum" although its drawbacks are too many for it to be a surefire "cure" against lying.
Categories: Natural tropane alkaloids | Deliriants | Muscarinic antagonists | Alkaloids | Plant toxins
|This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Scopolamine". A list of authors is available in Wikipedia.|