XOPENEX HFA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XOPENEX HFA (XOPENEX HFA).
Selective beta-2 adrenergic receptor agonist; relaxes bronchial smooth muscle by increasing intracellular cyclic AMP via activation of adenylyl cyclase.
| Metabolism | Primarily hepatic via glucuronidation and sulfate conjugation; minor contribution from CYP450 enzymes (CYP3A4, CYP2D6). |
| Excretion | Renal: 80-100% as unchanged drug and metabolites; fecal: minimal (<5%) |
| Half-life | Terminal elimination half-life: 3-4 hours; clinical context: dosing every 4-6 hours for bronchodilation |
| Protein binding | 52-57% bound to albumin |
| Volume of Distribution | Vd: 2.5-4.5 L/kg; indicates extensive extravascular distribution |
| Bioavailability | Inhalation: 15-30% (lung deposition); oral: <1% due to extensive first-pass metabolism |
| Onset of Action | Inhalation: 5-15 minutes |
| Duration of Action | 4-6 hours; clinical note: effects may diminish with regular use due to tolerance |
2 inhalations (90 mcg each) every 4-6 hours as needed via oral inhalation. Maximum 12 inhalations per 24 hours.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dose adjustment required for renal impairment. Data not sufficient for specific recommendations. |
| 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). |
| Pediatric use | Children 4-11 years: 1 inhalation (45 mcg) every 4-6 hours as needed; maximum 4 inhalations per 24 hours. Children ≥12 years: same as adult dosing. |
| Geriatric use | No specific dose adjustment recommended. Use with caution due to potential for increased sensitivity to beta-agonists; consider lower starting doses if clinically appropriate. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XOPENEX HFA (XOPENEX HFA).
| Breastfeeding | Excretion in human milk unknown. Low systemic bioavailability after inhalation suggests minimal transfer. M/P ratio not available. Use caution; monitor infant for beta-adrenergic effects (tachycardia, tremor). |
| Teratogenic Risk | Animal studies: No evidence of teratogenicity in rats and rabbits at doses up to 2.5 and 50 times the maximum daily human inhalation dose, respectively. Human data: Insufficient. Beta-agonists may cause fetal tachycardia and hyperglycemia; risk of oligohydramnios with high systemic exposure. First trimester: No known teratogenic risk. Second/third trimester: May inhibit uterine contractions; use only if benefit outweighs risk. Consider reduced placental perfusion. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to levalbuterol or any component of the formulation."]
| Precautions | ["Paradoxical bronchospasm may occur with repeated use; discontinue immediately if occurs.","May cause cardiovascular effects (increased heart rate, blood pressure, ECG changes); use with caution in patients with cardiovascular disorders.","Hypokalemia may occur; monitor serum potassium levels.","Immediate hypersensitivity reactions possible.","Do not exceed recommended dose or frequency."] |
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| Fetal Monitoring | Maternal: Heart rate, blood pressure, blood glucose, serum potassium (hypokalemia). Fetal: Heart rate monitoring, ultrasound for growth if prolonged use; assess for uterine contractions. |
| Fertility Effects | No human data on fertility. Animal studies: No impairment of fertility in rats at doses up to 50 times the human dose. Use not expected to affect fertility. |