Glycopyrronium

Registered South African indications:

• Chronic obstructive pulmonary disease

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe renal impairment CrCl <30ml/min

Cautions

• Pregnancy
• Breastfeeding
• Renal Impairment
• Hepatic impairment 
• Acute bronchospasm
• Narrow angle glaucoma
• Urinary retention
• Unstable ischaemic heart disease
• Left ventricular failure
• Myocardial infarction
• Arrhythmia 
• Prolonged QT syndrome
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: inc

Chronic obstructive pulmonary disease - Maintenance

• Inhaled (inc): 50μg, dly; Max: 50μg/24hrs

The capsules must only be administered using the inhaler

Only remove capsule from packaging prior to use

DO NOT swallow capsules

Not established for use in children below 18 years

Pregnancy

• Caution
• There are no data from the use of glycopyrronium in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity
• Glycopyrronium should only be used during pregnancy if the expected benefit to the patient justifies the potential risk to the foetus

Breastfeeding

• Caution
• It is unknown whether glycopyrronium is excreted in human milk. However, glycopyrronium (including its metabolites) was excreted in the milk of lactating rats. The use of glycopyrronium by breastfeeding women should only be considered if the expected benefit to the woman is greater than any possible risk to the infant

Renal Impairment

• Caution; no dose adjustment recommended
• Severe: Contraindicated 

Hepatic Impairment

• Caution; no dose adjustment recommended

Elderly

• No dose adjustment recommended 

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Headache
• Hypoaesthesia
• Fatigue

Cardiovascular Disorders

• Atrial fibrillation
• Palpitations

Respiratory Disorders

• Nasopharyngitis
• Rhinitis
• Sinus congestion
• Productive cough
• Throat irritation
• Epistaxis
• Paradoxical bronchospasm
• Dysphonia

Gastrointestinal Disorders

• Dry mouth
• Gastroenteritis
• Dyspepsia
• Dental caries

Genitourinary Disorders

• Cystitis
• Urinary retention
• Dysuria

Endocrine and Metabolic Disorders

• Hyperglycaemia

Musculoskeletal Disorders

• Pain in extremity
• Musculoskeletal chest pain

Skin and Subcutaneous Tissue Disorders

• Rash
• Pruritis

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
• Angioedema

• Anticholinergics

None routine

Glycopyrronium is an inhaled long-acting muscarinic receptor antagonist (anticholinergic) for once-daily maintenance bronchodilator treatment of COPD. Parasympathetic nerves are the major bronchoconstrictive neural pathway in airways, and cholinergic tone is the key reversible component of airflow obstruction in COPD. Glycopyrronium works by blocking the bronchoconstrictor action of acetylcholine on airway smooth muscle cells, thereby dilating the airways. Glycopyrronium bromide is a high affinity muscarinic receptor antagonist. A greater than 4-fold selectivity for the human M3 receptors over the human M2 receptor has been demonstrated using radioligand binding studies. It has a rapid onset of action as evidenced by observed receptor association/dissociation kinetic parameters and the onset of action after inhalation in clinical studies.

Inhalation capsule 50μg

• Seebri Breezhaler  (Novartis)