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Formoterol Fumarate

Pronunciation

Pronunciation: for-MOE-ter-ol FUE-ma-rate
Class: Sympathomimetic

Trade Names

Foradil Aerolizer
- Inhalation powder in capsules 12 mcg

Perforomist
- Inhalation solution 10 mcg/mL

Oxeze Turbuhaler (Canada)

Pharmacology

Relaxes bronchial smooth muscles.

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Pharmacokinetics

Absorption

Inhalation powder

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

Inhalation solution

C max is 72 pg/mL and T max is 12 min.

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

Inhalation powder

Eliminated in the urine (59% to 62%) and feces (32% to 34%). About 10% is excreted unchanged in the urine, and about 15% to 18% is excreted in the urine as conjugates. Mean half-life is 10 h.

Inhalation solution

1.1% to 1.7% excreted unchanged in the urine. The half-life is 7 h.

Duration

12 h.

Special Populations

Children

The pharmacokinetics of formoterol inhalation solution have not been studied in children.

Gender

Pharmacokinetics did not differ between men and women.

Elderly/Hepatic and renal function impairment

Pharmacokinetic studies have not been done in elderly patients or in subjects with hepatic or renal function impairment.

Indications and Usage

Inhalation powder

Treatment of asthma; prevention of bronchospasm; prevention of exercise-induced bronchospasm.

Inhalation powder, inhalation solution

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

Contraindications

For the treatment of asthma without concomitant use of a long-term asthma control medication, such as an inhaled corticosteroid; hypersensitivity to formoterol or any component of the product.

Dosage and Administration

Treatment of Asthma/Bronchospasm
Adults and Children 5 y of age and older Inhalation powder

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

Prevention of Exercise-Induced Bronchospasm
Adults and Children 5 y of age and older Inhalation powder

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

Maintenance Treatment of COPD
Adults Inhalation powder

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

Inhalation solution

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

General Advice

  • More frequent administration or administration of a larger number of inhalations of formoterol is not recommended.
  • Do not use in combination with other inhaled, long-acting beta-2 agonists or with other medications containing long-acting beta-2 agonists.
  • Use of a short-acting beta-2 agonist on a regular basis should be discontinued and the short-acting beta-2 agonist should only be used for symptomatic relief of acute asthma symptoms when treatment with formoterol begins.
  • Inhalation powder
  • 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.
  • Inhalation solution
  • Administer by orally inhaled route via a standard jet nebulizer connected to an air compressor.
  • Store in foil pouch and remove immediately before use. Dilution of the solution is not required prior to administration. Discard any partially used container.

Storage/Stability

Prior to dispensing, store in refrigerator between 36° and 46°F. Protect from heat and moisture. After dispensing, inhalation powder should be stored between 68° and 77°F and inhalation solution should be stored between 36° and 77°F.

Drug Interactions

Adrenergic agents

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.

Beta-blockers

Beta-blockers block the therapeutic effects of beta-2 agonists and may produce bronchospasm in patients with asthma and COPD. Effects of both agents may be inhibited. In these patients, a cardioselective beta-blocker should be considered; although, they should be administered with caution.

Drugs known to prolong the QTc interval, MAOIs, tricyclic antidepressants

Formoterol may potentiate the CV effects of these agents, increasing the risk of cardiac arrhythmia. Use with extreme caution.

Linezolid

Coadministration of linezolid and formoterol may result in adverse CV effects characterized by hypertension. Caution should be used with or within 2 wk of coadministration of linezolid and formoterol. Monitor BP.

Methylxanthines (eg, aminophylline, theophylline)

Concomitant treatment with methylxanthines may potentiate the hypokalemic effects of formoterol. In addition, concurrent use of theophyllines and formoterol may augment the bronchodilating response. Measure theophylline concentrations and adjust the theophylline dose as needed. Monitor serum potassium.

Nonpotassium-sparing diuretics (eg, loop [eg, furosemide] or thiazide [eg, chlorothiazide] diuretics)

ECG changes and/or hypokalemia may be worsened by formoterol, especially when the recommended dose of formoterol is exceeded. Use with caution. Monitor the ECG and serum potassium concentrations.

Steroids

Concomitant treatment with steroids may potentiate the hypokalemic and hyperglycemic effects of formoterol. Use with caution. Additional clinical and blood chemistry monitoring may be needed.

Adverse Reactions

Cardiovascular

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

CNS

Anxiety, dizziness, insomnia, tremor (2%); fatigue; headache; malaise; nervousness.

Dermatologic

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

EENT

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

GI

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

Miscellaneous

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

Precautions

Warnings

Long-acting beta-2 adrenergic agonists increase the risk of asthma-related death. Use of formoterol for the treatment of asthma without a concomitant long-term asthma control medication, such as an inhaled corticosteroid, is contraindicated. Use formoterol only as additional therapy for patients with asthma who are currently taking but are inadequately controlled on a long-term asthma control medication. Once asthma control is achieved or maintained, assess the patient at regular intervals and step down therapy (eg, discontinue formoterol) if possible without loss of asthma control, and maintain patient on a long-term asthma control medication. Do not use formoterol for patients whose asthma is adequately controlled on low or medium dose inhaled corticosteroids.

Data from controlled clinical trials suggest that long-acting beta-2 adrenergic agonists increase the risk of asthma-related hospitalization in children and adolescents. Consider a fixed-dose combination product containing both an inhaled corticosteroid and a long-acting beta-2 agonist to ensure adherence with both drugs in children and adolescents who asthma who require the addition of a long-acting beta-2 agonist to an inhaled corticosteroid. In cases in which the use of a separate long-term asthma control medication and a long-acting beta-agonist is clinically indicated, appropriate steps must be taken to ensure adherence with both components.


Monitor

Consider monitoring of pulse rate and BP, glucose levels, and potassium levels periodically during therapy.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Inhalation powder

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

Inhalation solution

Safety and efficacy not established.

Elderly

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

Hypersensitivity

Hypersensitivity reactions, including anaphylaxis, angioedema, bronchospasm, rash, and urticaria, have been observed immediately after administration of formoterol. Formoterol inhalation powder contains trace levels of milk protein, which may produce allergic reaction in patients with severe milk protein allergy.

Special Risk Patients

Use with caution in patients with convulsive disorders or thyrotoxicosis, and in patients unusually responsive to sympathomimetic amines.

Acute worsening of or deteriorating asthma or chronic obstructive pulmonary disease

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.

Excessive use

Fatalities and clinically significant CV effects have been reported in association with excessive use of inhaled sympathomimetic drugs in patients with asthma. Use of higher than recommended doses is also associated with an increased risk of serious asthma exacerbations.

Metabolic effects

Significant hypokalemia may be produced, which has the potential to produce CV adverse reactions. Transient hyperglycemia and/or aggravation of preexisting diabetes mellitus and ketoacidosis may also occur.

Paradoxical bronchospasm

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

Use of anti-inflammatory agents

Formoterol is not a substitute for inhaled or oral corticosteroids. Do not stop or reduce corticosteroids at the time formoterol is initiated.

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.
  • Inform patient that long-acting beta-2 agonists may increase the risk of asthma-related death and may increase the risk of asthma-related hospitalizations in children and adolescents. Currently available data are inadequate to determine whether concurrent use of inhaled corticosteroids or other long-term asthma control drugs mitigate the increased risk of asthma-related death from long-acting beta-2 agonists.
  • Inform patient that formoterol should not be used as the only therapy for the treatment of asthma and must only be used as additional therapy when a long-term asthma control medication does not adequately control asthma symptoms.
  • 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.
  • Remind patient not to use this medicine more frequently than twice daily (morning and evening) for maintenance treatment of asthma or COPD.
  • 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.
  • Inform patient that treatment with beta-2 agonists may lead to adverse reactions that include chest pain, dizziness, dry mouth, fatigue, headache, high blood sugar, increased or decreased blood pressure, low blood potassium, malaise, muscle cramps, nausea, nervousness, palpitations, rapid heart rate, tremor, or trouble sleeping.
  • Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
  • Inform patient never to use this medication with a spacer and never to exhale into the device.
  • Inform patient that the inhalation powder contains lactose, which contains trace amounts of milk protein.
  • Remind patient that the solution is to be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor.
  • Advise patient that the solution is not to be swallowed or injected. It is for inhalation use only.

Copyright © 2009 Wolters Kluwer Health.

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