SEEBRI NEOHALER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SEEBRI NEOHALER (SEEBRI NEOHALER).
Long-acting muscarinic antagonist (LAMA) that inhibits acetylcholine at M3 receptors in bronchial smooth muscle, causing bronchodilation.
| Metabolism | Primarily hydrolyzed via esterases to an alcohol metabolite (M29) and glycolic acid; CYP2D6 and CYP3A4 contribute minimally to metabolism. |
| Excretion | After oral inhalation, the absorbed fraction is predominantly eliminated via hepatic metabolism and biliary excretion into feces. Renal elimination accounts for <20% of the total clearance, with about 14% of an IV dose recovered in urine as unchanged drug and metabolites; fecal excretion accounts for >70% of the administered dose. |
| Half-life | Terminal elimination half-life is 5.5–7.8 days (mean ~6.7 days) after multiple dosing, reflecting slow dissociation from the M3 receptor and enterohepatic recycling; this supports once-daily dosing. |
| Protein binding | Approximately 85–90% bound to human plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 800 L (9–11 L/kg based on 70 kg body weight), indicating extensive tissue distribution, particularly into the lungs and peripheral tissues. |
| Bioavailability | Absolute bioavailability after oral inhalation is approximately 30–40% of the nominal dose due to partial lung deposition and swallowed fraction undergoing first-pass metabolism. The oral bioavailability of swallowed drug is low (<5%) due to extensive hepatic metabolism. |
| Onset of Action | Following oral inhalation, bronchodilation is detectable within 5 minutes, with clinically meaningful improvement (≥12% increase in FEV1) observed by 30 minutes. |
| Duration of Action | Bronchodilator effect persists for at least 24 hours with once-daily dosing; trough FEV1 remains significantly above placebo after 24 hours, supporting sustained COPD symptom control. |
| Molecular Weight | 440.54 |
Inhalation: 1 capsule (50 mcg glycopyrrolate) twice daily via Neohaler device.
| Dosage form | POWDER |
| Renal impairment | Contraindicated if estimated GFR < 30 mL/min/1.73 m². For GFR 30-59 mL/min/1.73 m², use with caution; no dose adjustment required. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C); use with caution. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline. Caution in patients with severe renal impairment (GFR < 30 mL/min/1.73 m²); contraindicated. |
| 1st trimester | Insufficient human data; animal studies show no teratogenicity. Risk cannot be excluded. |
| 2nd trimester | Limited human data; animal studies show no adverse effects. Use only if benefit outweighs risk. |
| 3rd trimester | Use caution near term due to potential beta-agonist effect on uterine contractility. |
Clinical note
Comprehensive clinical and safety monograph for SEEBRI NEOHALER (SEEBRI NEOHALER).
| Placental transfer | Limited human data; animal studies indicate minimal placental transfer. Molecular properties suggest low transfer. |
| Breastfeeding | Excreted in breast milk in small amounts; unlikely to affect infant. Caution in preterm infants or those with impaired renal function. |
| Lactation Rating |
■ FDA Black Box Warning
Not applicable (no boxed warning).
| Serious Effects |
Hypersensitivity to glycopyrrolate or any ingredientHistory of hypersensitivity to glycopyrrolate
| Precautions | Paradoxical bronchospasm, Worsening of narrow-angle glaucoma, Worsening of urinary retention, Immediate hypersensitivity reactions, Not for acute bronchospasm or acute episodes of COPD |
| Food/Dietary | No specific food restrictions are required. Grapefruit and its juice have no known interaction with glycopyrrolate. Alcohol may worsen COPD symptoms or interact with other medications; avoid excessive intake. |
| Clinical Pearls |
Loading safety data…
| L3 - Moderately safe |
| Teratogenic Risk | Limited human data; animal studies show no teratogenicity at clinically relevant doses. Avoid use in first trimester unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal pulmonary function and fetal growth if used during pregnancy. |
| Fertility Effects | No adverse effects on fertility observed in animal studies. |
| SEEBRI NEOHALER (glycopyrrolate) is a long-acting muscarinic antagonist (LAMA) indicated for maintenance treatment of COPD. It should not be used for acute bronchospasm. The device is breath-activated; ensure patients do not exhale into it. Common adverse effects include dry mouth, urinary tract infection, and cough. Monitor for paradoxical bronchospasm and worsening of narrow-angle glaucoma or urinary retention. |
| Patient Advice | Do not use SEEBRI NEOHALER for sudden breathing problems; always have a rescue inhaler available. · Inhale one capsule once daily using the Neohaler device; do not swallow the capsules. · Store capsules in the blister pack and only remove one immediately before use. · Rinse your mouth with water after each dose to reduce the risk of dry mouth and oral thrush. · Avoid getting the powder in your eyes; if contact occurs, rinse with water and seek medical advice if symptoms develop. · Tell your healthcare provider if you have glaucoma, trouble urinating, or an enlarged prostate. |