Glyriva

Glycopyrronium Bromide is a long-acting muscarinic antagonist (LAMA) primarily used in respiratory conditions.

Approved Indications:

• Maintenance treatment of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema, to improve lung function and reduce exacerbations.
• Prevention of exercise-induced bronchoconstriction in selected patients with COPD.
• Adjunct therapy in severe asthma patients not adequately controlled by inhaled corticosteroids plus a long-acting β2-agonist (LABA).

Clinically Accepted Off-Label Uses:

• Symptomatic management of bronchospasm in chronic bronchitis or emphysema.
• Relief of airway obstruction in overlap COPD-asthma syndrome (ACO).
• Preoperative reduction of airway secretions in selected surgical patients (less common).

Adults (≥18 years):

• Dose: 50 µg once daily via inhalation using a dry powder inhaler.
• Maximum daily dose: 50 µg.

Elderly:

• Same as adult dose; monitor for anticholinergic side effects (dry mouth, urinary retention).

Pediatrics (<18 years):

• Safety and efficacy not established; not routinely recommended.

Special Populations:

• Renal Impairment: No dose adjustment required; caution in severe renal failure.
• Hepatic Impairment: Use with caution in severe hepatic impairment; dose adjustment generally not required.

Administration Notes:

• Administer at the same time each day for consistent effect.
• Rinse mouth after inhalation if co-administered with inhaled corticosteroids.
• Not intended for relief of acute bronchospasm; use short-acting rescue inhaler as needed.

Glycopyrronium Bromide is a long-acting muscarinic antagonist (LAMA) that selectively blocks M3 acetylcholine receptors in bronchial smooth muscle. By inhibiting the action of acetylcholine, it prevents parasympathetic-mediated bronchoconstriction and reduces mucus secretion, leading to bronchodilation and improved airflow. This prolonged receptor blockade provides sustained symptomatic relief in COPD and other airway obstructive conditions.

• Absorption: Rapidly absorbed after inhalation; systemic bioavailability ~10–15%.
• Distribution: Low plasma protein binding; volume of distribution ~20–30 L.
• Metabolism: Minimal hepatic metabolism; mostly unchanged in circulation.
• Excretion: Eliminated via urine (~50%) and feces.
• Half-life: ~33–57 hours for sustained bronchodilatory effect.
• Onset of Action: Symptomatic bronchodilation begins within 5 minutes; peak effect at 1–2 hours.

• Pregnancy: Category C — animal studies show no teratogenic effects, but human data are limited. Use only if clearly needed.
• Lactation: Excreted in small amounts in breast milk; caution advised. Monitor infant for anticholinergic effects.
• Note: Avoid high-dose or prolonged therapy during pregnancy and lactation.

• Primary Class: Bronchodilator
• Subclass: Long-acting muscarinic antagonist (LAMA)

• Known hypersensitivity to glycopyrronium or any excipients.
• Acute bronchospasm requiring immediate rescue therapy.
• Severe hypersensitivity to other anticholinergic drugs.
• Narrow-angle glaucoma or urinary retention unless benefits outweigh risks.

• High-risk patients:
• Elderly — increased susceptibility to anticholinergic side effects (dry mouth, urinary retention, constipation).
• Patients with glaucoma, prostatic hypertrophy, or bladder obstruction.
• Serious potential risks:
• Paradoxical bronchospasm (rare).
• Monitoring:
• Pulmonary function periodically to assess efficacy.
• Observe for early signs of severe adverse events such as chest pain, palpitations, or worsening respiratory symptoms.

Common:

• Dry mouth
• Throat irritation
• Constipation
• Mild urinary retention

Serious/Rare:

• Paradoxical bronchospasm
• Glaucoma exacerbation
• Severe urinary retention requiring medical intervention
• Cardiac arrhythmias (rare)

Dose Dependence: CNS and anticholinergic effects are dose-related, though typically mild at recommended doses.

• Drug-Drug:
• Other anticholinergic drugs — additive anticholinergic effects.
• Certain β2-agonists — monitor cardiovascular status.
• Drug-Food: No significant interactions noted.
• Drug-Alcohol: No significant interaction; caution advised with CNS depressants.
• Enzyme Systems: Minimal metabolism; no major CYP450 interactions expected.

• Recommended as first-line LAMA therapy in maintenance treatment of moderate-to-severe COPD.
• Emphasis on once-daily inhalation for improved adherence and sustained bronchodilation.
• Not intended for acute symptom relief; short-acting bronchodilators remain necessary for rescue.
• GOLD 2025 guidelines highlight LAMA monotherapy for patients with frequent symptoms and low exacerbation risk.

• Store at 20°C–25°C (room temperature).
• Protect from moisture, heat, and light.
• Keep inhaler tightly closed when not in use.
• Do not freeze.
• Keep out of reach of children.