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 |
| Molecular Weight | 239.31 |
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 | Limited human data; animal studies show no teratogenicity at high doses. Generally avoided unless benefit justifies risk. |
| 2nd trimester | Use only if clearly needed; may inhibit uterine contractions. No known teratogenicity. |
| 3rd trimester | Use near term may inhibit labor; monitor for tachycardia/hypoglycemia in neonate. Avoid for tocolysis. |
Clinical note
Comprehensive clinical and safety monograph for XOPENEX HFA (XOPENEX HFA).
| Placental transfer | Levalbuterol crosses placenta; extent similar to racemic albuterol. Fetal levels approximately 10-20% of maternal. |
| Breastfeeding | Excreted into breast milk in small amounts; minimal risk to infant. Use lowest effective dose; monitor infant for irritability or tachycardia. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
History of hypersensitivity to levalbuterol or albuterolSevere hypersensitivity to 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. |
| Food/Dietary | No clinically significant food interactions have been reported. Avoid caffeine-containing foods and beverages if they worsen anxiety or palpitations. |
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| 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. |
| 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. |
| Clinical Pearls | XOPENEX HFA (levalbuterol tartrate) is the R-isomer of albuterol and may cause less beta-1-mediated tachycardia than racemic albuterol. It is dosed by inhalation; one canister provides 200 inhalations. Priming is required before first use and after not using for more than 3 days (4 test sprays into the air). |
| Patient Advice | Use exactly as prescribed; do not increase dose or frequency without consulting your healthcare provider. · Rinse your mouth with water after each use to reduce the risk of oral thrush. · If you experience chest pain, rapid heart rate, or worsening breathing, seek medical attention immediately. · Clean the inhaler mouthpiece weekly by wiping with a dry cloth; do not wash or put in water. · Carry a rescue inhaler at all times if prescribed for acute asthma or COPD exacerbations. |