FORADIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for FORADIL (FORADIL).
Formoterol is a long-acting beta2-adrenergic receptor agonist (LABA) that relaxes bronchial smooth muscle by increasing intracellular cyclic AMP.
| Metabolism | Metabolized primarily by hepatic glucuronidation and to a lesser extent by CYP2D6, CYP2C19, and CYP2C9. |
| Excretion | Renal (60% as unchanged drug and metabolites) and fecal (40% as metabolites). |
| Half-life | Terminal half-life: 7-10 hours. Steady-state achieved within 3-5 days; clinical context: allows twice-daily dosing for bronchodilation. |
| Protein binding | 61% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 6.0 L/kg (extensive tissue distribution, indicating high penetration into lungs and peripheral tissues). |
| Bioavailability | Inhalation: ~30% (systemic absorption from lungs; oral bioavailability negligible due to first-pass metabolism). |
| Onset of Action | Inhalation: 5-15 minutes (peak effect at 1-3 hours). |
| Duration of Action | 12 hours (bronchodilation sustained for 12 hours with twice-daily dosing). |
| Molecular Weight | 392.9 Da |
Inhalation: 12 mcg twice daily (every 12 hours) via Foradil Aerolizer.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific dose adjustment recommended; use caution in severe hepatic impairment. |
| Pediatric use | Children 5 years and older: 12 mcg inhalation twice daily. No dosing established for children under 5 years. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects due to potential comorbidities. |
| 1st trimester | Insufficient human data; animal studies show no teratogenicity. Use only if potential benefit justifies risk. |
| 2nd trimester | Limited human data; no known risk. May cause uterine relaxation delaying labor. |
| 3rd trimester | Avoid near term due to risk of uterine relaxation and potential for neonatal hypoglycemia. |
Clinical note
Comprehensive clinical and safety monograph for FORADIL (FORADIL).
| Placental transfer | Crosses placenta; extent not quantified but likely due to low molecular weight. |
| Breastfeeding | Excreted into breast milk in small amounts; unlikely to cause adverse effects in infant. Use with caution. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category C. In animal studies, formoterol fumarate (active ingredient of FORADIL) showed adverse effects on fetal development at high doses, including increased fetal loss, decreased fetal weight, and skeletal variations. There are no adequate and well-controlled studies in pregnant women. During first trimester, risk cannot be ruled out. Second and third trimesters: potential risk of maternal beta-agonist effects causing uterine relaxation and delayed labor. Use only if potential benefit justifies potential risk to fetus. |
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and serum potassium levels due to potential hypokalemia. Assess for signs of preterm labor or uterine relaxation. In fetus, monitor heart rate and growth if used long-term. Periodic assessment of asthma control and lung function. |
| Fertility Effects | No human studies on fertility. In animal studies, formoterol fumarate had no effect on fertility in rats at oral doses up to 10 mg/kg/day (approximately 2000 times the maximum recommended daily inhalation dose on a mg/m² basis). However, at very high doses, decreased fertility in males was observed. |
■ FDA Black Box Warning
LABAs increase the risk of asthma-related death; Foradil should only be used in patients with asthma not adequately controlled on asthma controller medications or whose disease severity warrants initiation of both an inhaled corticosteroid and a LABA.
| Serious Effects |
Hypersensitivity to formoterol or any componentStatus asthmaticusAcute episodes of asthma requiring intensive care
| Precautions | Increased risk of asthma-related death, Deterioration of disease and acute episodes may occur and should be treated with a short-acting beta2-agonist, Cardiovascular effects (increased heart rate, blood pressure, ECG changes), Hypokalemia and hyperglycemia may occur, Paradoxical bronchospasm may occur and require immediate discontinuation, Do not use with other LABAs |
| Food/Dietary | No specific food interactions. Grapefruit/grapefruit juice may increase systemic exposure via CYP3A4 inhibition; avoid concurrent use. |
| Clinical Pearls | FORADIL (formoterol fumarate) is a long-acting beta2-agonist (LABA) indicated for maintenance treatment of asthma and COPD, but must not be used as monotherapy for asthma without concomitant inhaled corticosteroid. Onset of bronchodilation occurs within 5-10 minutes, peaking at 1-3 hours, with duration up to 12 hours. Not for acute bronchospasm. Risk of paradoxical bronchospasm; discontinue if occurs. Monitor for increased heart rate, blood pressure, and QTc prolongation. Caution in patients with cardiovascular disorders, seizure disorders, thyrotoxicosis, or diabetes. |
| Patient Advice | Use FORADIL exactly as prescribed; do not use to relieve sudden breathing problems. · Always have a fast-acting rescue inhaler (e.g., albuterol) for acute symptoms. · Do not use more than 2 inhalations every 12 hours; maximum daily dose is 48 mcg. · Rinse mouth with water after each use to reduce risk of thrush (if using with ICS). · Seek medical help immediately if breathing worsens, chest tightness, or hives develop. · Inform your doctor if you have heart disease, high blood pressure, seizures, thyroid problems, or diabetes. · Store capsules in blister pack, use only with provided Aerolizer inhaler; do not swallow capsules. |
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