Glycopyrronium

ATC CodeD11AA01
CAS number596-51-0
PUB number11693
Drugbank IDDB00986
Empirical formulaC19H28NO3
Molar mass (g·mol−1)318,4305
Physical statesolid
Melting point (°C)193-194,5
PKS value11,53
Solubility0.000944 mg/mL

Basics

Glycopyrronium is an active ingredient used to dilate the bronchi, i.e. the airways in the lungs, and is therefore used to treat chronic obstructive pulmonary disease (COPD) and bronchial asthma. It is also used to treat excessive sweating (hyperhidrosis) and is used in anesthetic medicine (anesthesia) during operations to reduce salivation and secretion in the throat (pharynx). Glycopyrronium belongs to the group of parasympatholytics.

Graphic structural formula of the active ingredient glycopyrronium

Effect

Glycopyrronium binds to the muscarinic receptors as a competitive antagonist. It thus blocks the receptors to which acetylcholine, a messenger substance (neurotransmitter), otherwise binds. This prevents or at least weakens the effect of acetylcholine. Glycopyrronium is therefore an antagonist of acetylcholine and weakens its effect. The muscarinic receptors of type M1 and M3 experience the strongest attenuation, which cause a constriction of the bronchi and a reduction in sweating. The muscle tension of the bronchi is released and they widen, allowing more air to flow through. The strong sweat-reducing effect was originally regarded as a side effect, but has been approved as an active ingredient for external (topical) use, i.e. as an ointment, cream, gel, etc., since 2022. As the muscarinic receptors M1 and M3 are also present in the cardiovascular system, side effects are more likely to occur there. The advantages of glycopyrronium are that it acts very quickly and for a very long time.

Glycopyrronium is broken down by the liver (mainly via CYP2D6) and 85% is excreted via the kidneys. The plasma half-life, i.e. the time it takes the body to excrete half of the active ingredient, is around 55 minutes. It is 38-44% bound to plasma proteins.

Dosage

Always take Glycopyrronium exactly as described in the package leaflet or as advised by your doctor.

Glycopyrronium is available as an inhaler or tablet for the treatment of asthma and COPD, and as a cream or tablet for the treatment of excessive sweating. It is also used in operating theaters as a solution for injection and given to children as an oral solution ("juice") to treat excessive salivation. Due to the many different forms of use (application methods), it is not possible to speak of a common dose.

Side effects

The following side effects may occur:

Very common:

  • Dry mouth
  • Suppressed milk secretion
  • constipation
  • diarrhea
  • Nausea and vomiting
  • feeling of heat
  • blocked nose
  • Bladder emptying disorders (urinary retention)
  • Irritability

Frequent:

Occasionally:

  • Bad breath
  • Fungal infection in the mouth and throat
  • Movement disorders of the gastrointestinal tract
  • Dilated pupils (mydriasis)
  • Involuntary eye movements (nystagmus)
  • Headaches
  • Dehydration
  • Thirst

Frequency unknown:

Interactions

Interactions may occur if the following medicines are taken at the same time:

  • Potassium chloride
  • anticholinergics
  • spasmolytics
  • Topiramate for the treatment of epilepsy
  • Antihistamines for the treatment of allergies
  • Clozapine
  • Haloperidol
  • phenotiazine
  • Botulinum toxin (e.g. Botox)
  • Antidepressants
  • Opioids for severe pain
  • Corticosteroids for the treatment of inflammatory diseases
  • ß-sympathomimetics - it can increase the heart rate-increasing effect
  • When taken at the same time as cimetidine, there may be less excretion via the kidneys, which means that more active substance remains in the body

Contraindications

Glycopyrronium must not be taken in the following cases

  • if you are allergic to glycopyrronium
  • glaucoma
  • in case of urination disorders (urinary retention)
  • severe kidney disease
  • in case of obstruction of the stomach outlet (pyloric stenosis)
  • for diarrhea
  • ulcerative colitis
  • Stomach pain and swelling
  • myasthenia gravis (muscle weakness)
  • in Sjörgen syndrome

Age restriction

The use for children under 3 years of age is not permitted.

Pregnancy & breastfeeding

Glycopyrronium should not be used during pregnancy, as no experience reports are available.

Glycopyrronium should not be used during breastfeeding because it is not known whether it passes into breast milk and because glycopyrronium is known to inhibit milk secretion (lactation).


Thomas Hofko

Thomas Hofko

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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