FORADIL CERTIHALER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FORADIL CERTIHALER (FORADIL CERTIHALER).
Formoterol is a long-acting beta2-adrenergic receptor agonist that stimulates intracellular adenyl cyclase, increasing cyclic AMP production and causing bronchodilation.
| Metabolism | Formoterol is extensively metabolized by direct glucuronidation via UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT2B7, and UGT2B15, and O-demethylation via CYP2D6 and CYP2C19. |
| Excretion | After oral inhalation, the majority of a dose is excreted in feces (up to 70%) as unchanged drug and metabolites via biliary elimination. Renal excretion accounts for approximately 13-25% of the dose, primarily as metabolites. Unabsorbed drug accounts for the remainder. |
| Half-life | The terminal elimination half-life of formoterol (active component) ranges from 5 to 10 hours following inhalation. This supports twice-daily dosing, though clinical effect may persist longer due to prolonged receptor binding. |
| Protein binding | Formoterol is approximately 60-70% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | The volume of distribution (Vd) of formoterol is approximately 3.4 L/kg, indicating extensive distribution into tissues beyond plasma. |
| Bioavailability | Inhaled bioavailability is highly variable, approximately 20-30% of the inhaled dose reaches the lungs. Oral bioavailability is low (<10%) due to first-pass metabolism. The swallowed portion contributes minimally to systemic levels. |
| Onset of Action | Bronchodilation begins within 1-3 minutes after inhalation, with significant improvement in FEV1 observed within 5-10 minutes. Peak effect occurs at 1-3 hours. |
| Duration of Action | Bronchodilator effect lasts up to 12 hours, supporting twice-daily administration. However, duration may be shorter in some patients; regular dosing (not rescue) is recommended. |
One inhalation (12 mcg) twice daily via oral inhalation.
| Dosage form | POWDER |
| Renal impairment | No dosage adjustment required for renal impairment. Use with caution in severe impairment. |
| Liver impairment | No dosage adjustment recommended; pharmacokinetics unaffected by mild to moderate hepatic impairment. |
| Pediatric use | For children 5 years and older: one inhalation (12 mcg) twice daily. Safety and efficacy in children under 5 not established. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects due to potential age-related comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FORADIL CERTIHALER (FORADIL CERTIHALER).
| Breastfeeding | It is unknown if formoterol is excreted in human breast milk. No M/P ratio available. In lactating rats, formoterol was detected in milk. Because many drugs are excreted in human milk, caution is advised. Decision to discontinue nursing or drug should consider importance of drug to mother. Consider alternative therapies with more breastfeeding safety data. |
| Teratogenic Risk | Formoterol fumarate (FORADIL CERTIHALER) is classified as FDA Pregnancy Category C. In animal studies, formoterol caused fetal malformations (e.g., omphalocele, skeletal abnormalities) at high systemic exposures. There are no adequate well-controlled studies in pregnant women. Risk to fetus cannot be ruled out; use only if potential benefit justifies potential risk. First trimester: limited data, theoretical risk based on animal findings. Second and third trimesters: may cause uterine relaxation and delay labor; avoid use near term unless clearly needed. |
■ FDA Black Box Warning
Long-acting beta2-adrenergic agonists increase the risk of asthma-related death; Foradil should only be used as add-on therapy for patients not adequately controlled on other asthma controllers or whose disease severity warrants initiation of a LABA.
| Serious Effects |
["Treatment of status asthmaticus or other acute episodes of asthma","Hypersensitivity to formoterol fumarate or any inactive ingredients"]
| Precautions | ["Asthma-related death","Deterioration of disease","Use of anti-inflammatory agents","Paradoxical bronchospasm","Cardiovascular effects","Hypokalemia","Hyperglycemia","Immediate hypersensitivity reactions"] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and serum potassium levels due to potential hypokalemia. Assess fetal heart rate and uterine activity if used near term. Monitor for signs of maternal tachycardia or arrhythmia. Assess asthma control with peak expiratory flow (PEF) and symptom diaries. |
| Fertility Effects | No human studies on fertility effects. In animal studies, formoterol did not impair fertility at systemic exposures up to 15 times the maximum recommended human daily inhalation dose. Theoretical potential for beta-2 agonist to affect uterine contractility or ovulation, but clinical significance unknown. |