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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SEEBRI NEOHALER (SEEBRI NEOHALER).
| Breastfeeding | Not known if excreted in human milk; caution advised. M/P ratio not available. |
| 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. |
■ FDA Black Box Warning
Not applicable (no boxed warning).
| Serious Effects |
["History of hypersensitivity to glycopyrrolate or any ingredient in the formulation"]
| Precautions | ["Paradoxical bronchospasm","Worsening of narrow-angle glaucoma","Worsening of urinary retention","Immediate hypersensitivity reactions","Not for acute bronchospasm or acute episodes of COPD"] |
Loading safety data…
| Fertility Effects | No adverse effects on fertility observed in animal studies. |