Formoterol Fumarate

Trade Names:
Foradil Aerolizer
- Inhalation powder in capsules 12 mcg

Trade Names:
Perforomist
- Inhalation solution 20 mcg per 2 mL

Pharmacology

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Relaxes bronchial smooth muscles.

Pharmacokinetics

Absorption

C _max is 92 pg/mL and T _max is 5 min.

Undetectable or very low plasma concentrations measured.

Distribution

Protein binding is 61% to 64%.

Metabolism

Formoterol is primarily metabolized by direct glucuronidation and O-demethylation by CYP-450 2D6, 2C19, 2C9, and 2A6 isozymes.

Elimination

About 10% is excreted unchanged in the urine, and about 15% to 18% is excreted in the urine as conjugates. Mean t _½ is 10 h.

1.1% to 1.7% excreted unchanged in the urine. The t _½ is 7 h.

Duration

12 h.

Special Populations

Pharmacokinetics did not differ between men and women.

Pharmacokinetic studies have not been done in elderly patients or in subjects with hepatic or renal function impairment. Limited data are available in children.

Indications and Usage

Long-term maintenance treatment of asthma; prevention of bronchospasm; prevention of exercise-induced bronchospasm.

Long-term administration in the maintenance of bronchoconstriction in COPD, including chronic bronchitis and emphysema.

Contraindications

Standard considerations.

Dosage and Administration

Inhalation 12 mcg every 12 h (max, 24 mcg per 24 h).

Inhalation 12 mcg 15 min prior to exercise given on an occasional, as-needed basis.

Inhalation 12 mcg every 12 h (max, 24 mcg per 24 h).

Inhalation 20 mcg twice daily (morning and evening) by nebulization (max, 40 mcg/day).

General Advice

• For inhalation only. Do not swallow or take capsules by mouth. Administer only with supplied inhaler.
• Do not use a spacer with the inhalation powder. Keep inhaler dry and never wash. Store medication-filled capsules in their blisters and only remove immediately before use.

• Administer by orally inhaled route via a standard jet nebulizer connected to an air compressor.
• Store in foil pouch and remove immediately before use. Discard any partially used container.

Storage/Stability

Prior to dispensing, store in refrigerator at 36° to 46°F. Protect from heat and moisture.

Drug Interactions

Other adrenergic agents may potentiate the sympathetic effects. Long-acting beta-2 agonists should not be coadministered. Short-acting beta-2 agonists should not be taken on a regular basis and should only be used for symptomatic relief of acute asthma symptoms.

Effects of both agents may be inhibited.

May potentiate the hypokalemic effect of formoterol.

Formoterol may potentiate the CV effects of these agents, increasing the risk of cardiac arrhythmia.

ECG changes and/or hypokalemia may be worsened by formoterol.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Angina, arrhythmias, hypertension, hypotension, palpitations, tachycardia.

CNS

Anxiety, dizziness, insomnia, tremor (2%).

Dermatologic

Pruritus (2%); rash (1%).

EENT

Pharyngitis (4%); nasopharyngitis (3%); tonsillitis (1%).

GI

Diarrhea, nausea (5%); dry mouth (3%); increased sputum, vomiting (2%).

Hypersensitivity

Anaphylactic reactions, including severe hypotension and angioedema (postmarketing).

Metabolic

Hyperglycemia, hypokalemia, metabolic acidosis.

Musculoskeletal

Back pain (4%); leg cramps, muscle cramps (2%).

Respiratory

Upper respiratory tract infection (7%); bronchitis (5%); chest infection, sinusitis (3%); dyspnea (2%).

Miscellaneous

Viral infection (17%); chest pain (3%); fever (2%); dysphonia (1%); serious exacerbation of asthma (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 5 yr of age.

Safety and efficacy not established.

Elderly

No overall differences in safety and efficacy were observed between patients 65 yr of age and older compared with younger individuals.

Special Risk Patients

Use with caution in patients with CV disorders (especially coronary insufficiency, cardiac arrhythmias, and hypertension), convulsive disorders, or thyrotoxicosis, and in patients unusually responsive to sympathomimetic amines.

Acute worsening of or deteriorating asthma

Use of formoterol in these conditions is not appropriate.

CV effects

Because formoterol can produce clinically important CV effects, use with caution in patients with CV disorders, especially cardiac arrhythmia, coronary insufficiency, and hypertension.

Paradoxical bronchospasm

If paradoxical bronchospasm occurs, discontinue formoterol and institute alternative therapy.

Metabolic effects

Significant hypokalemia may be produced, which has the potential to produce CV adverse reactions.

Overdosage

Symptoms

Angina, arrhythmias, cardiac arrest, death, dizziness, dry mouth, fatigue, headache, hyperglycemia, hypertension, hypokalemia, hypotension, insomnia, malaise, metabolic acidosis, muscle cramps, nausea, nervousness, palpitation, seizures, tachycardia, tremor.

Patient Information

• Advise patient to read the Medication Guide before using product the first time and to reread with each refill.
• Instruct patient on the proper storage and use of the dry powder inhaler.
• Remind patient that capsules should only be used with the Aerolizer inhaler and should not be taken by mouth.
• Inform patient to never wash the Aerolizer inhaler and to have dry hands when handling the capsules containing the medication.
• Advise patient using more than 1 inhaled medication to use short-acting bronchodilator medication first, if needed, and then to use this medicine. Tell patient to take inhaled corticosteroids or other inhaled controller medications last.
• Remind patient not to use this medicine more frequently than twice daily (morning and evening) for maintenance treatment of asthma.
• Remind patient that if using this medicine to prevent exercise-induced bronchospasm, to use at least 15 min before exercise and not to take additional doses for at least 12 h.
• Remind patient that this medication is not a “rescue medication” and is not to be used for the treatment of acute or deteriorating asthma.
• Advise patient that if asthma symptoms worsen immediately after using this medication to stop using it and inform health care provider immediately.
• Advise patient that formoterol is not a substitute for inhaled or oral corticosteroids and not to stop taking or reduce the dose of their corticosteroid medication.
• Advise patient to contact health care provider if medication no longer seems to control asthma symptoms or if increasing doses of the short-acting bronchodilator (“rescue medicine”) are needed. This may indicate worsening of asthma.
• Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
• Inform patients never to use this medication with a spacer and never to exhale into the device.
• Inform patients that the product contains lactose, which contains trace amounts of milk protein.
• Remind patients that the solution is to be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor.
• Advise patients that the solution is not to be swallowed or injected. It is for inhalation use only.

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