PERFOROMIST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PERFOROMIST (PERFOROMIST).
PERFOROMIST (formoterol fumarate) is a long-acting beta2-adrenergic agonist (LABA) that stimulates intracellular adenyl cyclase, increasing cyclic AMP levels, leading to relaxation of bronchial smooth muscle.
| Metabolism | Formoterol is primarily metabolized via direct glucuronidation and O-demethylation, with involvement of CYP2D6 and CYP2C19 enzymes. |
| Excretion | Renal: 60% as unchanged drug; biliary/fecal: 30% as metabolites and unchanged; 10% metabolized via CYP450. |
| Half-life | Terminal elimination half-life is approximately 8-10 hours in adults, allowing twice-daily dosing for sustained bronchodilation. |
| Protein binding | Approximately 85-90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd: 2-4 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Inhalation: approximately 25-30% due to pulmonary absorption; oral: <1% due to first-pass metabolism. |
| Onset of Action | Inhalation: within 5-10 minutes for bronchodilation. |
| Duration of Action | 12 hours post-inhalation; clinical bronchodilation persists for the full dosing interval. |
20 mcg (2 mL) via nebulization twice daily; not to exceed 40 mcg/day.
| Dosage form | SOLUTION |
| Renal impairment | No specific dose adjustment for renal impairment; use caution in severe impairment (eGFR <30 mL/min). |
| Liver impairment | No specific dose adjustment for Child-Pugh A or B; Child-Pugh C: use with caution, monitor for adverse effects. |
| Pediatric use | Approved for ages ≥6 years: 20 mcg nebulized twice daily; weight-based dosing not established. |
| Geriatric use | No specific dose adjustment; monitor for increased systemic effects due to reduced renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PERFOROMIST (PERFOROMIST).
| Breastfeeding | Formoterol is excreted in human breast milk; M/P ratio unknown. Due to potential for beta-agonist effects in the infant (e.g., tachycardia, tremor), caution is advised. The manufacturer recommends weighing risk vs. benefit. Consider alternative therapies or monitor infant for signs of beta-agonist stimulation. |
| Teratogenic Risk | Perforomist (formoterol fumarate) is a long-acting beta2-adrenergic agonist. Human data are limited; animal studies show no teratogenic effects at clinically relevant doses. Beta-agonists may cause uterine relaxation and delay labor. Risk cannot be excluded; use only if clearly needed. First trimester: limited data, no confirmed malformation risk. Second/third trimester: potential for fetal tachycardia, hypoglycemia, and hypokalemia if used near term. |
■ FDA Black Box Warning
LABAs increase the risk of asthma-related death. PERFOROMIST should not be used for the treatment of asthma without concomitant use of a long-term asthma control medication such as an inhaled corticosteroid.
| Serious Effects |
["Hypersensitivity to formoterol fumarate or any component","Use as monotherapy without an inhaled corticosteroid in asthma (due to black box warning)"]
| Precautions | ["Increased risk of asthma-related death (black box warning)","Not for acute bronchospasm or deterioration","Cardiovascular effects: increased heart rate, blood pressure, or arrhythmias","Paradoxical bronchospasm","Hypokalemia and hyperglycemia","Immediate hypersensitivity reactions"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and serum potassium (risk of hypokalemia). Monitor fetal heart rate and uterine activity if used during labor. In pregnancy, assess maternal respiratory status and fetal growth via ultrasound if prolonged use. Watch for signs of preterm labor (tocolysis due to beta-agonists). |
| Fertility Effects | No human studies on fertility. In animal studies, formoterol had no adverse effects on male or female fertility at doses up to 18 times the maximum recommended human daily inhalation dose. No known impact on human reproductive function. |