We regularly hear about the benefits and uses of Hyoscine . Here we tell you all the details.

Hyoscine – what is it

Hyoscine, also known as scopolamine, is a drug used to treat motion sickness and postoperative nausea and vomiting. It is also sometimes used before surgery to decrease saliva. When used by injection, the effects begin after about 20 minutes and last up to 8 hours. It can also be used orally and as a skin patch.

Hyoscine – side effects

Common side effects include drowsiness, blurred vision, dilated pupils, and a dry mouth. It is not recommended in people with glaucoma or intestinal obstruction. It is not clear if use during pregnancy is safe; however, it appears to be safe while breastfeeding. Hyoscine belongs to the family of antimuscarinic medications and works by blocking some of the effects of acetylcholine on the nervous system.

Hyoscine – Discovery

Hyoscine was first written in 1881 and entered into medical use in 1947. It is on the WHO Model List of Essential Medicines, the most effective and safest medicines needed in a healthcare system. It is produced from plants of the Solanaceae family. The name “scopolamine” is derived from a type of nightshade known as Scopolia, while “hyoscine” is another type known as Hyoscyamus niger.

One of the oldest alkaloids isolated from plant sources, hyoscine has been used in its purified forms (as various salts, including hydrochloride, hydrobromide, hydroiodide, and sulfate), since its isolation by the German scientist Albert Ladenburg in 1880, and as various preparations from its vegetable form since ancient times and perhaps prehistoric times. Following Ladenburg’s description of the structure and activity of hyoscine, the search for synthetic analogs and methods for the total synthesis of hyoscine and / or atropine in the 1930s and 1940s resulted in the discovery of diphenhydramine, an early antihistamine and the prototype of its chemical subclass of these drugs, and pethidine, the first fully synthetic opioid pain reliever,

Hyoscine was used in conjunction with morphine, oxycodone, or other opioids from before 1900 to the 1960s to put laboring mothers into a kind of “twilight sleep.”

Hyoscine mixed with oxycodone (Eukodal) and ephedrine was marketed by Merck as SEE (from the German initials for ingredients) and Scophedal starting in 1928, and the mixture is sometimes mixed on site rarely in the area of ​​its greatest historical use. namely Germany and Central Europe.

Hyoscine was also one of the active ingredients in Asthmador, an over-the-counter (OTC) smoking preparation marketed in the 1950s and 1960s that claimed to fight asthma and bronchitis.

Hyoscine – what is it for

Medical use

Hyoscine has several uses in medicine, where it is used to treat the following:

  • Postoperative nausea and vomiting and sea sickness, leading to use by divers
  • Motion sickness (where it is often applied as a transdermal patch behind the ear)
  • Gastrointestinal spasms
  • Kidney or biliary spasms
  • Assists in gastrointestinal radiology and endoscopy
  • Irritable bowel syndrome
  • Clozapine-induced hypersalivation (drooling)
  • Intestinal colic
  • Eye inflammation
  • It is sometimes used as a premedication to surgery, usually by injection.

Hyoscine – Use in pregnancy

Hyoscine crosses the placenta and is a pregnancy category C in the United States and a category B1 medication in Australia, which means that a risk to the fetus cannot be ruled out. There are not enough studies in women and animals to rule out harm, but existing studies have not shown an increased risk. Medications should be given only if the potential benefits justify the potential risk to the fetus. May cause respiratory depression and / or neonatal bleeding when used during pregnancy. Transdermal hyoscine has been used as an adjunct to epidural anesthesia for caesarean section. Except when used before a cesarean section, it should only be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus.

Breast-feeding

Hyoscine enters breast milk through secretion. Although there are no human studies to document the safety of hyoscine during breastfeeding, the manufacturer recommends that caution be exercised if hyoscine is administered to a breastfeeding woman.

Hyoscine – Risk in the elderly

The likelihood of experiencing adverse effects from hyoscine is increased in the elderly compared to the young. This phenomenon is especially true for older people who also take other medications. It is recommended to avoid the use of hyoscine in this age group due to these potent anticholinergic adverse effects.

Hyoscine – Contraindications

Uncommon adverse effects (incidence 0.1-1%) include:

  • Dry mouth
  • Dyshidrosis (reduced ability to sweat to cool off)
  • Tachycardia (usually occurs in higher doses and is followed by bradycardia)
  • Bradicardia
  • Urticaria (urticaria)
  • Pruritus (itching)

Rare adverse effects (<0.1% incidence) include:

  • Constipation
  • Urinary retention
  • Hallucinations
  • Agitation
  • Confusion
  • Restlessness
  • Seizures

Side effects of unknown frequency include:

  • Anaphylactic shock
  • Anaphylactic reactions
  • Dyspnea (shortness of breath)
  • Eruption
  • Erythema

Other hypersensitivity reactions:

  • Blurry vision
  • Mydriasis (dilated pupils)
  • Drowsiness
  • Dizziness
  • Drowsiness

Hyoscine – Overdose

Physostigmine is a cholinergic drug that readily crosses the blood-brain barrier and has been used as an antidote to treat the central nervous system depression symptoms of a hyoscine overdose. Apart from this supportive treatment and induced emesis (vomiting) are generally recommended as treatments for oral overdoses.

  • Tachycardia
  • Arrhythmia
  • Blurry vision
  • Photophobia
  • Urinary retention
  • Drowsiness or paradoxical reaction that may present with hallucinations
  • Cheyne-Stokes respiration
  • Dry mouth
  • Redness of the skin
  • Inhibition of gastrointestinal motility

Hyoscine – Interactions

Due to interactions with the metabolism of other drugs, hyoscine can cause significant unwanted side effects when taken with other medications. Specific attention should be paid to other drugs in the same drug class as hyoscine, also known as anticholinergics. The following medications could interact: pain relievers / pain relievers, ethanol, zolpidem, thiazide diuretics, buprenorphine, anticholinergic drugs such as tiotropium.

Hyoscine – administration

Hyoscine can be taken orally, subcutaneously, ophthalmic, and intravenously, as well as through a transdermal patch. The transdermal patch (eg, Transderm Scōp) for preventing nausea and motion sickness uses hyoscine base and is effective for up to three days. Oral, ophthalmic, and intravenous forms have shorter half-lives and are generally found in the form of hyoscine hydrobromide (for example, in Scopace, 0.4 mg soluble tablets, or Donnatal).

NASA is currently developing a nasal delivery method. With accurate dosing, NASA’s aerosol formulation has been shown to work faster and more reliably than the oral form.

Hyoscine – Mechanism of action

Although it is generally referred to as a nonspecific antimuscarinic, there is indirect evidence for the specificity of the m1 receptor subtype.

Biosynthesis in plants

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

A putrescine oxidase that specifically recognizes methylated putrescine catalyzes the deamination of this compound to 4-methylaminobutanal, which then undergoes spontaneous ring formation to the N-methyl-pyrrolinium cation.

Samantha Robson
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Dr. Samantha Robson ( CRN: 0510146-5) is a nutritionist and website content reviewer related to her area of ​​expertise. With a postgraduate degree in Nutrition from The University of Arizona, she is a specialist in Sports Nutrition from Oxford University and is also a member of the International Society of Sports Nutrition.

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