BROVANA
Clinical safety rating
cautionComprehensive clinical and safety monograph for BROVANA (BROVANA).
BROVANA (arformoterol tartrate) is a long-acting beta2-adrenergic agonist (LABA). It stimulates intracellular adenyl cyclase, increasing cyclic AMP levels, leading to relaxation of bronchial smooth muscle and inhibition of mast cell mediator release.
| Metabolism | Primarily metabolized via glucuronidation (UGT1A1, UGT1A3, UGT1A9) and to a lesser extent by O-demethylation via CYP2D6 and CYP2E1. |
| Excretion | Primarily renal (60% unchanged drug); remainder via biliary/fecal (approximately 20%) and metabolic transformation. |
| Half-life | Terminal elimination half-life: approximately 26 hours (range 22–30 hours) in healthy adults; prolonged in hepatic impairment (up to 50% increase). |
| Protein binding | Approximately 75% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 1.9 L/kg (indicating extensive extravascular distribution). |
| Bioavailability | Inhalation: approximately 9–15% (due to lung deposition and local metabolism; oral bioavailability <2% due to first-pass effect). |
| Onset of Action | Inhalation: within 1–3 minutes; peak effect at 30–60 minutes. |
| Duration of Action | 12 hours (bronchodilation maintained for 12 hours with twice-daily dosing; may extend to 24 hours in some patients). |
| Molecular Weight | 467.6 |
15 mcg (2 mL) by nebulization twice daily, not to exceed 30 mcg/day.
| Dosage form | SOLUTION |
| Renal impairment | No adjustment required for GFR ≥30 mL/min; insufficient data for GFR <30 mL/min; use with caution. |
| Liver impairment | No specific Child-Pugh based adjustments; use with caution in severe hepatic impairment. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established for patients <18 years. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects; start at low end of dosing range if renal or hepatic impairment present. |
| 1st trimester | Insufficient human data; animal studies show no evidence of teratogenicity at clinically relevant doses. Use only if potential benefit justifies risk. |
| 2nd trimester | No known risk in second trimester; beta-agonists may inhibit uterine contractions. Use with caution. |
| 3rd trimester | Risk of neonatal hypoglycemia, tachycardia, and tremor if used near term; may delay labor. Use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for BROVANA (BROVANA).
| Placental transfer | Limited data; arformoterol is a beta-agonist and likely crosses the placenta given its molecular weight and lipophilicity. Animal studies indicate placental transfer. |
| Breastfeeding | Arformoterol is excreted into breast milk in low amounts; however, the potential for beta-agonist effects in the infant (e.g., tachycardia, tremor) should be considered. Use with caution, especially in preterm infants or those with cardiovascular conditions. |
| Lactation Rating | L3 (Moderately Safe; potential for adverse effects in the infant has not been well established) |
| Teratogenic Risk | Pregnancy Category C. No adequate well-controlled studies in pregnant women. In animal studies, arformoterol (the active enantiomer of formoterol) caused fetal malformations (including omphalocele and skeletal abnormalities) at doses approximately 2.4 times the maximum recommended human daily inhalation dose (MRHDID) in rats, and delayed ossification at doses approximately 0.24 times MRHDID in rabbits. Use only if potential benefit justifies potential risk to fetus. First trimester: limited human data; second and third trimesters: may cause preterm labor due to beta-adrenergic receptor stimulation; monitor for uterine contractions. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, serum potassium (beta-agonists can cause hypokalemia), and signs of bronchospasm. Fetal monitoring: assess fetal heart rate and uterine activity; risk of preterm labor and fetal tachycardia. |
| Fertility Effects | No human fertility studies. In rats, arformoterol did not impair fertility at exposures up to approximately 2.4 times MRHDID. |
■ FDA Black Box Warning
LABAs increase the risk of asthma-related death. BROVANA is not indicated for the treatment of asthma.
| Serious Effects |
Hypersensitivity to arformoterol or any component of the formulationHypersensitivity to other beta-agonists (e.g., formoterol, salmeterol)
| Precautions | Paradoxical bronchospasm, cardiovascular effects (tachycardia, hypertension, QT prolongation), hypokalemia, hyperglycemia, immediate hypersensitivity reactions, and use with other beta-agonists. |
| Food/Dietary | No specific food interactions. Avoid caffeine or other stimulants as they may increase sympathetic side effects (e.g., tremor, tachycardia). |
| Clinical Pearls | Arformoterol (BROVANA) is a long-acting beta-2 agonist (LABA) indicated for maintenance treatment of COPD, not for acute exacerbations. It should not be used with other LABAs. Monitor for paradoxical bronchospasm and cardiovascular effects. Twice-daily dosing, not once-daily like some LABAs. |
| Patient Advice | Use BROVANA exactly as prescribed, twice daily (morning and evening), not for sudden breathing problems. · Do not use more than the prescribed dose; overuse can increase risk of side effects. · Rinse mouth with water after each dose to reduce risk of thrush (if using via nebulizer with a mouthpiece). · Contact your healthcare provider if symptoms worsen or you need your rescue inhaler more often. · Common side effects include headache, chest pain, back pain, diarrhea, and sinusitis. |
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