Glycopyrronium (Glycopyrrolate)
Indications
Glycopyrronium (Glycopyrrolate) is used for:
In Anesthesia:
- As a pre-operative antimuscarinic agent to reduce salivary, tracheobronchial and pharyngeal secretions; and to reduce the volume and free acidity of gastric secretions.
- As a pre-operative or intra-operative antimuscarinic to attenuate or prevent intra-operative bradycardia with the use of suxamethonium or due to cardiac vagal reflexes.
- To protect against the peripheral muscarinic actions (e.g., bradycardia and excessive secretions) of anticholinesterases such as neostigmine and pyridostigmine given to reverse residual neuromuscular blockade produced by non-depolarising muscle relaxants.
In Peptic Ulcer:
For use in adults as adjunctive therapy for the treatment of peptic ulcer when rapid anticholinergic effect is desired or when oral medication is not tolerated.
Hyperhidrosis, Sialorrhea, Cerebral palsy
Adult Dose
Parenteral:
Reduction of secretions
Preoperative: By IM injection, 4 µg/kg admin 30-60 minutes before procedure.
Intraoperative: By IV injection, 0.1 mg; may repeat at 2-3-minute intervals when needed. Max: 400 µg/dose.
NOTE: Larger doses may result in profound and prolonged antisialogogue effect which may be unpleasant for the patient
Reversal of neuromuscular blockade
By IV injection, 200 µg for each 1 mg of Neostigmine or 5 mg of Pyridostigmine. Alternatively, 5-15 µg/kg with 50 µg/kg Neostigmine (25-70 µg/kg of Neostigmine) or 0.1-0.3 mg/kg of Pyridostigmine.
NOTE: Glycopyrronium bromide may be administered simultaneously from the same syringe with the anticholinesterase; greater cardiovascular stability results from this method of administration
Peptic ulcer
By IM/IV injection, 0.1-0.2 mg 3-4 times daily
Child Dose
Child (<1 month): Glycopyrronium injection should not be used in neonates due to its benzyl alcohol content.
Glycopyrronium injection is not recommended for the treatment of peptic ulcer in pediatric patients
Reduction of secretions
Preoperative: By IM injection, Child (1 month to <2 years): 4-9 µg/kg; >2 years, 4 µg/kg. Dose to be given 30-60 minutes before procedure.
Intraoperative: By IV injection, 4 µg/kg (Max: 0.1 mg); repeat at 2-3-minute intervals as needed.
Max dosage: Child (>1 month): 200 µg/dose.
NOTE: Larger doses may result in profound and prolonged antisialogogue effect which may be unpleasant for the patient
Reversal of neuromuscular blockade
By IV injection, Child (1 month to 12 years): 10 µg/kg with 50 µg/kg Neostigmine.
NOTE: Glycopyrronium bromide may be administered simultaneously from the same syringe with the anticholinesterase; greater cardiovascular stability results from this method of administration
Renal Dose
Patients with Renal Impairment
Glycopyrronium can be used in patients with mild to moderate renal impairment. In patients with severe renal impairment or end-stage renal disease requiring dialysis this medication should be used only if the expected benefit outweighs the potential risk.
Patients with Hepatic Impairment
Glycopyrronium can be used in patients with mild and moderate hepatic impairment. No data are available for subjects with severe hepatic impairment
Administration
For intramuscular or intravenous administration
Contra Indications
Hypersensitivity to glycopyrronium or any of its inactive ingredients.
Angle-closure glaucoma;
Myasthenia gravis (large doses of quaternary ammonium compounds have been shown to block end plate nicotinic receptors);
Paralytic ileus;
Pyloric stenosis;
Prostatic enlargement;
Anticholinesterase-antimuscarinic combinations such as neostigmine plus glycopyrronium should be avoided in patients with a prolonged QT interval
Precautions
Antimuscarinics should be used with caution (due to increased risk of side effects) in Down’s syndrome, in children and in the elderly.
They should also be used with caution in gastro-esophageal reflux disease, diarrhea, ulcerative colitis, acute myocardial infarction, hypertension, conditions characterized by tachycardia (including hyperthyroidism, cardiac insufficiency, cardiac surgery) because of the increase in heart rate produced by their administration, coronary artery disease and cardiac arrhythmias, pyrexia (due to inhibition of sweating).
Because of prolongation of renal elimination, repeated or large doses of glycopyrronium bromide should be avoided in patients with uremia.
Large doses of quaternary anticholinergic compounds have been shown to block end plate nicotinic receptors. This should be considered before using glycopyrrolate in patients with myasthenia gravis.
It is known that the administration of anticholinergic agents during inhalation anesthesia can result in ventricular arrhythmias.
Pregnancy and lactation
Pregnancy:
There are no data from the use of Glycopyrronium Bromide Injection in pregnant women. Animal studies for glycopyrronium bromide are insufficient with respect to reproductive toxicity. Use of Glycopyrronium Bromide Injection is not recommended during pregnancy.
Breastfeeding:
It is unknown whether glycopyrronium is excreted in human milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from Glycopyrronium Bromide Injection therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman
Pregnancy-Lactation
Recommendations on the use of Glycopyrronium (Glycopyrrolate) in Pregnancy & Lactation:
There are insufficient data to recommend the use of Glycopyrronium during pregnancy or lactation. There is no evidence that drugs in the same class cause developmental toxicity. Use only when the benefit outweighs the potential risk (Briggs & Freeman, 2015; Schaefer et al., 2015).
References:
1. Briggs, G. G., & Freeman, R. K. (2015). Drugs in pregnancy and lactation: A reference guide to fetal and neonatal risk (Tenth edition). Wolters Kluwer/Lippincott Williams & Wilkins Health.
2. Schaefer, C., Peters, P., & Miller, R. K. (2015). Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment (Third Edition). Academic Press
Interactions
Decreases levodopa effects.
Effects may be enhanced by using drugs with antimuscarinic properties or MAOIs concurrently.
May antagonise the GI effects of cisapride, metoclopramide and domperidone.
Potentially Fatal: IV admin in the presence of cyclopropane anesthetic can result in ventricular arrhythmias
Adverse Effects
Side effects of Glycopyrronium (Glycopyrrolate) :
Since glycopyrronium reduces the body's sweating ability, it can cause hyperthermia and heat stroke in hot environments.
Dry mouth, difficulty urinating, headaches, diarrhoea and constipation are also observed side effects of the medication.
The medication also induces drowsiness or blurred vision, an effect exacerbated by the consumption of alcohol