Inhalation/Respiratory Maintenance therapy in chronic obstructive pulmonary disease
Adult: 50 mcg once daily via inhaler device.
Intravenous Reversal of neuromuscular blockade
Adult: Concurrent use with neostigmine: 200 mcg as a single dose. Alternatively, 10-15 mcg/kg. Child: 10 mcg/kg as a single dose.
Intravenous Reversal of bradycardia, Reversal of vagal reflexes
Adult: 100 mcg as a single dose given intraoperatively. Dose may be repeated as needed at 2-3 minutes intervals. Child: 4 mcg/kg at 2-3 minutes intervals.
Oral Adjunct in peptic ulcer
Adult: 1-2 mg tid. Max: 8 mg daily. Dose may be adjusted as needed according to response and tolerability.
Oral Excessive salivation
Child: ≥3 years Initially, 20 mcg/kg tid. Titrate dose in increments of 20 mcg/kg every 5-7 days according to response. Max: 100 mcg/kg tid not to exceed 1,500-3,000 mcg/dose.
Parenteral Reduction of secretions
Adult: 200-400 mcg or 4-5 mcg/kg up to Max 400 mcg via IM or IV inj given before induction of anaesthesia. Similar dose may be given intraoperatively and may be repeated if necessary. Child: 4-8 mcg/kg up to Max 200 mcg given via IM or IV inj before induction of anaesthesia. Similar dose may be given intraoperatively and may be repeated if necessary.
Topical/Cutaneous Hyperhidrosis
Adult: As a 0.05% solution in distilled water: Apply to the affected area before iontophoretic treatment. Treat 1 site at a time, and only 2 sites in any 24 hours. Treatment should not be repeated within 7 days.
Contraindications
Severe ulcerative colitis, obstructive disease of the gastrointestinal tract (e.g. achalasia, pyloroduodenal stenosis), paralytic ileus, intestinal atony in elderly or debilitated patients, toxic megacolon complicating ulcerative colitis, unstable cardiovascular status in acute haemorrhage, glaucoma, obstructive uropathy (e.g. bladder neck obstruction due to prostatic hypertrophy), myasthenia gravis. Acute deterioration of COPD. Concomitant use with solid oral KCl.
Special Precautions
Patient with CV disease (e.g. coronary artery disease, ischemic heart disease, ventricular failure, MI, long QT syndrome, tachyarrhythmia, heart failure, hypertension and tachycardia); autonomic neuropathy, hyperthyroidism, hiatal hernia with reflux esophagitis, ulcerative colitis and severe hypersensitivity to milk proteins. Renal and hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Drowsiness, blurred vision, constipation, intestinal pseudo-obstruction, heat prostration, diarrhoea, incomplete intestinal obstruction, urinary retention, bronchospasm, hypersensitivity reactions. Blood and lymphatic system disorders: Hypokalaemia, hypernatraemia. Cardiac disorders: Arrhythmia, palpitation, tachycardia. Gastrointestinal disorders: Abdominal pain, dry mouth, nausea, vomiting. General disorders and administration site conditions: Pyrexia. Infections and infestations: Upper respiratory tract infection, otitis media, UTI, influenza, pharyngitis streptococcal, pneumonia, sinusitis, gastroenteritis viral, nasopharyngitis, ear infection, cellulitis, oral herpes. Metabolism and nutrition disorders: Dehydration, dysgeusia. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Behavioural changes, agitation, irritability, restlessness, insomnia. Renal and urinary disorders: Dysuria. Respiratory, thoracic and mediastinal disorders: Nasal congestion, reduced bronchial secretion, epistaxis. Skin and subcutaneous tissue disorders: Flushing, rash.
This drug may cause drowsiness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor heart rate, anticholinergic effects, pulmonary function (e.g. FEV1, peak flow) of patients on inhalation.
Overdosage
Symptoms: Mydriasis, dry mouth, hypotension, respiratory depression. Management: Symptomatic and supportive treatment. Perform gastric lavage. Administer cathartics and/or enemas immediately following large dose ingestion.
Drug Interactions
May enhance ulcerogenic effect of solid oral KCl. May increase antimuscarinic side effects with amantadine, antiarrhythmics (e.g. disopyramide), anticholinergics, TCA, MAOIs, antipsychotics (e.g. phenothiazine, clozapine, haloperidol), antiparkinsonian drugs, antispasmodics (e.g. domperidone, metoclopramide), and antihistamines. Reduced absorption of ketoconazole. May increase risk of severe constipation with opioid analgesics.
Action
Description: Glycopyrronium bromide is a synthetic quaternary ammonium antimuscarinic. It competitively and reversibly blocks the action of acetylcholine at muscarinic receptors in the bronchial smooth muscle, secretory glands and the CNS.
Synonym: glycopyrrolate Onset: 15-30 minutes (IM); approx 1 minute (IV). Duration: Vagal effect: 2-3 hours (parenteral). Inhibition of salivation: up to 7 hours (parenteral). Anticholinergic effect: 8-12 hours (oral). Pharmacokinetics: Absorption: Poorly absorbed from the gastrointestinal tract. Bioavailability: Approx 3% (oral); approx 40% (inhalation). Time to peak plasma concentration: 3.1 hours (oral); approx 30-45 minutes (IV/IM); 5 minutes (inhalation); 1-1.5 hours (topical). Distribution: Poorly crosses blood-brain barrier and placenta. Volume of distribution: 0.42 ± 0.22 L/kg (adult). Plasma protein binding: 38-41 % (inhalation). Metabolism: Inhalation: Metabolised in the liver (minimal). Excretion: Mainly via urine [as unchanged drug; >80% (IM), 85% (IV)]; bile (<5% as unchanged drug). Elimination half-life: 0.55-1.25 hours (IM); 0.83 ± 0.27 hour (IV); 3 hours (oral); 33-53 hours (inhalation).
Chemical Structure
Glycopyrronium Source: National Center for Biotechnology Information. PubChem Database. Glycopyrronium, CID=3494, https://pubchem.ncbi.nlm.nih.gov/compound/Glycopyrronium (accessed on Jan. 21, 2020)
R03BB06 - glycopyrronium bromide ; Belongs to the class of other inhalants used in the treatment of obstructive airway diseases, anticholinergics. A03AB02 - glycopyrronium bromide ; Belongs to the class of synthetic anticholinergics, quaternary ammonium compounds. Used in the treatment of functional bowel disorders.
References
Anon. Glycopyrrolate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/01/2021.Anon. Glycopyrronium Bromide [Glycopyrrolate] (Oral Inhalation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/01/2021.Anon. Glycopyrronium Bromide [Glycopyrrolate] (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/01/2021.Anon. Glycopyrronium Bromide [Glycopyrrolate] (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/01/2021.Buckingham R (ed). Glycopyrronium Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/01/2021.Glycopyrronium Bromide 1 mg Tablets (Kinedexe UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 05/01/2021.Glycopyrronium Bromide 1 mg/5 mL Solution (Colonis Pharma Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/01/2021.Glycopyrronium Bromide 2 mg Tablets (Dawa Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/01/2021.Glycopyrronium Bromide 200 mcg/mL Injection (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 05/01/2021.Joint Formulary Committee. Glycopyrronium Bromide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/01/2021.
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