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Hyoscine , also known as scopolamine , is a drug used to treat motion sickness and postoperative nausea and vomiting. Sometimes it is also used before surgery to reduce saliva. When used with injections, the effect begins after about 20 minutes and lasts up to 8 hours. It can also be used by mouth and as a dermal patch.

Common side effects include drowsiness, blurred vision, dilated pupils, and dry mouth. This is not recommended in people with glaucoma or intestinal obstruction. It is unclear whether the use during pregnancy is safe; However, it seems safe during breastfeeding. Hyoscine is in the family of antimuscarinic drugs and works by blocking some of the effects of acetylcholine in the nervous system.

Hyoscine was first written in 1881 and began to be used in 1947. It is the WHO Model Essential Medicines, the most effective and safe drugs needed in the health system. Hyoscine is produced from a nightshade family plant. The name "scopolamine" comes from one type of nightshade known as Scopolia while the name "hyoscine" comes from another type known as Hyoscyamus niger .


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Medical use

Hyoscine has a number of uses in medicine, where it is used to treat the following:

  • Postoperative nausea and vomiting and marine diseases, leading to their use by scuba divers
  • motion sickness (which is often used as a transdermal patch behind the ears)
  • Gastrointestinal spasms
  • Renal or biliary spasms
  • Assistance in gastrointestinal radiology and endoscopy
  • Irritated bowel syndrome
  • Clozapine-induced (drooling) induced hypersalivation
  • Colon colon
  • Inflammation of the eye

Sometimes used as premedication (primarily to reduce respiratory secretions) to surgery, mostly with injections.

Pregnancy

Hyoscine crosses the placenta and is the category of pregnancy C United States and drug Category B1 Australia, which means the risk to the fetus can not be ruled out. Adequate studies of women and animals are not available to exclude danger, but existing studies have not shown an increased risk. Drugs should be given only if potential benefits justify the potential risks to the fetus. This can cause respiratory depression and/or neonatal hemorrhage when used during pregnancy. Transdermal hyoscine has been used in addition to epidural anesthesia for cesarean delivery without adverse CNS effects on newborns. Unless used before a caesarean section, it should only be used during pregnancy if the benefits for the mother outweigh the potential risks to the fetus.

Breastfeeding

Hyoscine enters breast milk through secretions. Although there is no human study to document the safety of hiosin while breastfeeding, manufacturers recommend that caution be taken if hyoscines are given to women who breastfeed.

Elderly

The likelihood of experiencing side effects from hiosin increases in the elderly relative to younger people. This phenomenon is especially true for older people who also use some other drugs. It is recommended that the use of hiosin should be avoided in this age group due to strong anticholinergic side effects.

Maps Hyoscine



Adverse effects

Incident side effects:

Rarely (0.1-1% incident) side effects include:

  • Dry mouth
  • Dishidrosis (reducing the ability to sweat to cool)
  • Tachycardia (usually at higher doses and replaced by bradycardia)
  • Bradycardia
  • Urticaria (itching)
  • Pruritus (itching)

Rare side effects (& lt; 0.1%) include:

  • Constipation
  • Urine retention
  • Hallucinations
  • Agitation
  • Confusion
  • Restless
  • Seizures

Unknown frequency side effects include:

  • anaphylactic shock
  • Anaphylactic reactions
  • Dispnea (shortness of breath)
  • Rash
  • Eritema
  • Other hypersensitivity reactions
  • Blurred vision
  • Mydriasis (dilated pupil)
  • Drowsy
  • Dizzy
  • Somnolen

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Overdose

Physostigmine is a cholinergic drug ready to cross the blood-brain barrier, and has been used as an antidote to treat depressive central nervous system overdose of sharks. In addition to these supportive care, gastric lavage and induced emesis (vomiting) are usually recommended as treatment for oral overdoses. Overdose symptoms include:

  • Tachycardia
  • Arrhythmia
  • Blurred vision
  • Photophobia
  • Urine retention
  • Drowsy reaction or paradox that can appear with hallucinations
  • Cheyne-Stokes respiration
  • Dry mouth
  • Reddened skin
  • Inhibits gastrointestinal motility

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Interactions

Because of interactions with other drug metabolism, hiosin can cause significant undesirable side effects when taken with other drugs. Particular attention should be paid to other drugs in the same class of pharmacology as hyoscine, also known as anticholinergic. The following medications have the potential to interact with the metabolism of hiosin: analgesic/pain medications, ethanol, zolpidem, thiazid diuretics, buprenorphine, anticholinergic drugs such as thiotropium, etc.

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Administrative route

Hyoscine can be drunk, subcutaneously, intravenously, and through a transdermal patch. Transdermal patch ( for example, Transderm Sc? P) for the prevention of nausea and intoxication using a hiosin base, and effective up to three days. Oral, ophthalmic, and intravenous forms have shorter half-lives and are usually found in the form of hyoscine hydrobromide (eg in Scopace, soluble or Donnatal tablets).

NASA is currently developing a nasal administration method. With the right dose, NASA's spray formulation has proven to work faster and more reliably than oral form.

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Action mechanism

Although commonly referred to as nonspecific antimuscarinic, there is indirect evidence for the specificity of m1-receptor subtypes.

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Biosynthesis in plants

Hyoscine is one of the plant secondary metabolites of the Solanaceae plant family (nightshade), such as plants, jimson weed ( Datura ), angel trumpets ( Brugmansia ), and corkwood ( Duboisia ).

Hyoscine biosynthesis begins with L-ornithine decarboxylation to putrescine by ornithine decarboxylase. Putrescine is methylated to N-methylputrescine by putrescine N-methyltransferase.

A putrescine oxidase that specifically recognizes the methacylated putrein catalyzes the deamination of this compound into 4-methyaminamobutane, which then undergoes spontaneous ring formation of the N-methyl-pyrolysis cation. In the next step, the pyrrolium cation condenses with acetoacetic acid to produce hygrine. No enzymatic activity can be shown to catalyze this reaction. Hygrine further reorganized into tropinone.

Furthermore, tropinone reductase I converts tropinone into a trophic that condenses with phenylalanine phenylactine derived into littorine. A cytochrome P450 is classified as Cyp80F1 oxidizing and rearranging littorine into hyoscyamine aldehyde. In the final step, hyoscyamine undergoes epoxidation catalyzed by 6beta-hydroxyhyoscyamine epoxidase which produces hyoscine.

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History

One of the earlier alkaloids was isolated from plant sources, hyoscine has been used in a purified form (such as various salts, including hydrochlorides, hydrobromides, hydroiodides and sulfates), since isolation by German scientist Albert Ladenburg in 1880, and various preparations of the plant-based form past and possibly prehistoric times. Following the description of structure and hyoscine activity by Ladenburg, the search for synthetic analogs and methods for total synthesis of hyoscine and/or atropine in the 1930s and 1940s resulted in the discovery of diphenhydramine, the early antihistamines and prototype subclass chemistry of these drugs, and pethidine, analgesics the first fully synthetic opioid, known as Dolatin and Demerol among many other trade names.

Hyosin is used in conjunction with morphine, oxycodone, or other opioids from before 1900 to 1960s to get working mothers into a kind of "twilight sleep". The analgesia of a strong hyoscine plus opioid is deep enough to allow higher doses to be used as an anesthetic form.

Hyoscine mixed with oxycodone (Eukodal) and ephedrine was marketed by Merck as SEE (from the German initials of the ingredients) and Scophedal began in 1928, and the mixture was sometimes mixed on site on rare occasions in its largest historical use area, Germany and Central Europe.

Hyoscine is also one of the active ingredients in Asthmador, an over-the-counter (OTC) smoking preparation marketed in the 1950s and 1960s claiming to combat asthma and bronchitis. In November 1990, the US Food and Drug Administration forced OTC products with hyoscines and several hundred other ingredients that were not suspected to be effective in the market. Hyoscine shares a small segment of the OTC sleeping pills market with diphenhydramine, phenyltoloxamine, pyrilamine, doxylamine, and other first-generation antihistamines, many of which are still used for this purpose in drugs such as Sominex, Tylenol PM, NyQuil.

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Society and culture

Name

Hyoscine hydrobromide is an international nonproprietary name, and scopolamine hydrobromide is the United States Adopted Name. Other names include levo-duboisine, demonic breath and burundanga.

Use of recreation

Although sometimes used recreatively for its hallucinogenic properties, the experience is often unpleasant, mentally and physically. It's also physically dangerous, so repeated use is rare.

In June 2008, more than 20 people were hospitalized with psychosis in Norway after ingesting a false Rohypnol tablet containing hyoscine.

In January 2018, 9 people were hospitalized in Perth, Western Australia, after being reportedly swallowed in hygiene.

Interrogation

The effects of hiosin were studied for use as a truth serum in interrogation in the early 20th century, but due to adverse effects, investigations were dropped. In 2009, it was evident that the secret police of the Cekoslovak countries had used hiosin at least three times to gain recognition from people suspected of anti-dissidents.

Crime

In 1910, hyoscine was detected in the remains believed to belong to Cora Crippen, Dr. Hawley Harvey Crippen, and was accepted at the time as the cause of his death, as her husband is known to have bought some at the beginning of this year.

This drug is known to result in memory loss after exposure and drowsiness, similar to the effects of benzodiazepines or alcohol poisoning, which affects a person's ability to withstand criminal aggression. Travel advice published by the US Department of State in 2012 states:

One common and very dangerous method used by criminals to rob victims is through the use of drugs. The most common [in Colombia] is hiosin. Unofficial estimates say the number of annual hyosin incidents in Colombia is around 50,000. Hyoscine can make the victim unconscious for 24 hours or more. In large doses, may cause respiratory failure and death. It is most often given in liquid or powder form in foods and beverages. The majority of these incidents occur in nightclubs and bars, and usually men, considered wealthy, targeted by attractive young women. To avoid becoming a victim of hiosin, one should not accept food or drink offered by strangers or new acquaintances or leave unattended food or drink. The victims of hiosin or other drugs should seek immediate medical attention.

In addition to the robbery was also allegedly involved in abduction and sexual assault. The ClÃÆ'nic Hospital in Barcelona introduced a special protocol in 2008 to help medical workers identify cases, while Madrid hospital adopted the same work document in February 2015. However, the ClÃÆ'nic Hospital i> have found little scientific evidence to support this use and rely on the victim's story to reach any conclusion. Although poisoning by hyoscine quite often appears in the media as an aid to rape, kidnapping, killing or robbery, the effects of this drug and the way it is applied by criminals (added to drinks, transdermal injections, on playing cards and paper etc.) are often exaggerated , especially the use of transdermal, because the doses that can be absorbed by the skin are too low to have any effect (transdermal hyosin spots should be used for hours to days).

The name "burundanga" comes from plant extract brugmansia .

About one in five emergency rooms receiving poisoning in BogotÃÆ'¡, Colombia, has been linked to hiosin. Most commonly, victims have been poisoned by robbers who give victims of a scopolamine-bound drink, in the hope that the victim will become unconscious or unable to effectively fight the robbery.

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Research

Hyoscine has been used as a research tool to study the involvement of acetylcholine in cognition. The results in primates indicate that acetylcholine is involved in encoding new information into long-term memory. Hyoscine has also been studied as a rapid antidepressant with a number of small studies finding positive results.

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See also

  • Hyoscine butylbromide (scopolamine butylbromide)

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References




External links

  • Media related to hyoscines on Wikimedia Commons

Source of the article : Wikipedia

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