FORADIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FORADIL (FORADIL).

How it works

Formoterol is a long-acting beta2-adrenergic receptor agonist (LABA) that relaxes bronchial smooth muscle by increasing intracellular cyclic AMP.

What the body does with it

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).

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FORADIL (FORADIL).

Breastfeeding

Formoterol is excreted in human milk in small amounts. M/P ratio not established. Caution should be exercised when administered to nursing women. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for FORADIL and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition.

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.

Warnings & precautions

■ 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.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to formoterol or any ingredient in the formulation","Use as monotherapy in asthma without concomitant inhaled corticosteroid","Treatment of acute asthma symptoms or exacerbations"]

Clinical Precautions

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"]

Clinical Tips & Counseling

Drug interactions

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FORADIL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FORADIL (FORADIL).

How it works

Formoterol is a long-acting beta2-adrenergic receptor agonist (LABA) that relaxes bronchial smooth muscle by increasing intracellular cyclic AMP.

What the body does with it

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).

Classification & Brands

Dosing & administration

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.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FORADIL (FORADIL).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to formoterol or any ingredient in the formulation","Use as monotherapy in asthma without concomitant inhaled corticosteroid","Treatment of acute asthma symptoms or exacerbations"]