PERFOROMIST
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 844.9 |
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 | There are no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | Same as first trimester. |
| 3rd trimester | Same as first trimester. May inhibit uterine contractions and affect neonatal respiratory adaptation due to beta2-agonist effects. |
Clinical note
Comprehensive clinical and safety monograph for PERFOROMIST (PERFOROMIST).
| Placental transfer | Likely crosses placenta due to low molecular weight; beta2-agonists are known to cross placenta. Specific data for formoterol fumarate limited. |
| Breastfeeding | Excretion into breast milk is unknown. Use with caution in nursing mothers, considering importance of drug to mother and potential risk to infant (e.g., tachycardia, agitation). |
| Lactation Rating | L3 (Moderately Safe) - No studies in breastfeeding women; potential for adverse effects in infant. |
| 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. |
| 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. |
■ 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 componentNeed for acute bronchodilation in status asthmaticusUse in monotherapy for asthma without concomitant inhaled corticosteroid
| 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 |
| Food/Dietary | No specific food interactions are established for formoterol. However, excessive caffeine intake (coffee, tea, energy drinks) may theoretically increase sympathetic stimulation, potentially exacerbating adverse effects such as tachycardia and tremor. Patients should maintain adequate hydration and avoid abrupt changes in potassium intake, as formoterol can cause hypokalemia. Grapefruit has no known effect on formoterol metabolism. |
| Clinical Pearls | PERFOROMIST (formoterol fumarate) is a long-acting beta2-agonist (LABA) indicated for maintenance treatment of asthma and COPD. It should not be used for acute bronchospasm. Monitor for paradoxical bronchospasm, cardiovascular effects (tachycardia, hypertension), and hypokalemia. In asthma, always use with an inhaled corticosteroid; LABA monotherapy increases risk of asthma-related death. Teach patients to rinse mouth after inhalation to prevent oropharyngeal candidiasis with concomitant ICS. Use with caution in patients with thyrotoxicosis, diabetes, or QTc prolongation. The inhaler device (Aerolizer) requires loading a capsule immediately before use; do not store capsules in the device. |
| Patient Advice | Do not use PERFOROMIST for sudden breathing problems; have a rescue inhaler (e.g., albuterol) available. · Take twice daily, every 12 hours, even if you have no symptoms. Do not take more than prescribed. · Always use PERFOROMIST with an inhaled corticosteroid if you have asthma. · Rinse your mouth with water after each dose to prevent oral thrush (if using with ICS). · Load the capsule into the Aerolizer device just before use; do not store capsules in the device. · Seek emergency medical attention if you experience chest pain, fast heart rate, tremors, or worsening breathing. · Tell your doctor about all medications, especially beta-blockers, diuretics, and MAOIs. · Avoid caffeine and grapefruit juice? (No known significant interactions with formoterol; but advise limiting caffeine due to additive stimulant effects.) · Store capsules at room temperature, away from moisture and heat. |
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