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Pronunciation: AR-for-MOE-ter-ol TAR-trate
Class: Bronchodilator, Sympathomimetic
- Solution for inhalation 7.5 mcg/mL
Relaxes bronchial smooth muscles.
C max is 4.3 pg/mL and occurs approximately 0.5 h after administration.
In vitro plasma protein binding is 52% to 65%.
Metabolized primarily by direct conjugation (glucuronidation) and secondarily by O-demethylation (CYP2D6 and, to a lesser degree, CYP2C19).
After 14 days, 67% is recovered in urine (1% as unchanged arformoterol) and 22% in feces. Mean terminal half-life is 26 h.
Special PopulationsRenal Function Impairment
Systemic exposure (AUC and C max ) to arformoterol was similar in patients with renal impairment compared with healthy control subjects.Hepatic Function Impairment
The systemic exposure (C max and AUC) to arformoterol increased 1.3- to 2.4-fold in subjects with hepatic impairment.Elderly
No significant differences in systemic exposure (AUC and C max ) were observed between elderly and younger subjects.Children
Pharmacokinetics of arformoterol have not been studied.Gender
No effect of gender on the pharmacokinetics of arformoterol has been observed.Race
There was no clinically significant impact of race on the pharmacokinetics of arformoterol.
Indications and Usage
Long-term maintenance treatment of bronchoconstriction in COPD, including chronic bronchitis and emphysema.
History of hypersensitivity to arformoterol, racemic formoterol, or any component of the product; patients with asthma without the use of a long-term asthma control medicine.
Dosage and AdministrationAdults
Inhalation 15 mcg twice daily (morning and evening) by nebulization (max, 30 mcg/day).
- For use by nebulization only. Arformoterol should not be swallowed. Administer by the inhaled route via a standard jet nebulizer connected to an air compressor. The safety and efficacy of arformoterol have been established in clinical trials when administered using the Pari LC Plus nebulizers and Pari Dura-Neb 3000 compressors.
- Dilution is not required.
- Discard any vial if solution is not colorless.
- Do not use more often or in higher doses than recommended, or with other long-acting beta agonists.
- Instruct patients to discontinue use of inhaled, short-acting beta-2 agonists on a regular basis (eg, 4 times a day) and use them only for symptomatic relief of acute respiratory symptoms.
- The drug compatibility (physical and chemical), efficacy, and safety of arformoterol when mixed with other drugs in a nebulizer have not been established.
Store in the protective foil pouch between 36° and 46°F. Protect from light and excessive heat. Once foil pouch is opened, use contents of vial immediately and return unused vials to the pouch. Unopened foil pouch also may be stored between 68° and 77°F for up to 6 wk.
Drug InteractionsAdrenergic drugs (eg, salmeterol)
Arformoterol sympathomimetic effects may be potentiated. Avoid concurrent use.Beta-blockers (eg, propranolol)
Effects of both agents may be inhibited. Do not normally treat patients with COPD with beta-blockers. However, under certain circumstances (eg, prophylaxis after MI), there may be no acceptable alternatives. In this instance, cardioselective beta-blockers could be considered; administer them with caution.MAOIs (eg, phenelzine), drugs known to prolong the QTc interval (eg, pimozide), tricyclic antidepressants (eg, amitriptyline)
Arformoterol may potentiate these agents, increasing the risk of cardiac arrhythmias. Use with extreme caution.Methylxanthines (eg, aminophylline, theophylline), steroids (eg, prednisone)
May potentiate the hypokalemic effect of arformoterol. Monitor the clinical response and adjust treatment as needed.Nonpotassium-sparing diuretics (eg, loop [eg, furosemide] or thiazide [eg, chlorothiazide] diuretics)
ECG changes and/or hypokalemia may be worsened by arformoterol. Use with caution and closely monitor the clinical response.
Arteriosclerosis, atrial flutter, AV block, CHF, heart block, inverted T-wave, MI, QT interval prolongation, supraventricular tachycardia (less than 2%).
Agitation, cerebral infarct, circumoral paresthesia, hypokinesia, paralysis, somnolence, tremor (less than 2%).
Rash (4%); dry skin, herpes simplex, herpes zoster, skin discoloration, skin hypertrophy (less than 2%).
Abnormal vision, glaucoma, voice alteration (less than 2%).
Diarrhea (6%); constipation, gastritis, melena, oral moniliasis, periodontal abscess, rectal hemorrhage (less than 2%).
Breast neoplasm, calcium crystalluria, cystitis, glycosuria, hematuria, increased prostate-specific antigen, kidney calculus, nocturia, pelvic pain, pyuria, urinary tract disorder, urine abnormality (less than 2%).
Decreased glucose tolerance, dehydration, edema, gout, hyperglycemia, hyperlipemia, hypoglycemia, hypokalemia (less than 2%).
Back pain (6%); leg cramps (4%); arthralgia, arthritis, bone disorder, neck rigidity, rheumatoid arthritis, tendinous contracture (less than 2%).
Sinusitis (5%); dyspnea (4%); lung disorder, primarily pulmonary or chest congestion (2%); lung carcinoma, respiratory disorder (less than 2%).
Pain (8%); chest pain (7%); flu syndrome, peripheral edema (3%); abscess, allergic reaction, digitalis intoxication, fever, hernia, neoplasm, retroperitoneal hemorrhage (less than 2%).
Long-acting beta-2 adrenergic agonists may increase the risk of asthma-related death. The safety and efficacy of arformoterol in patients with asthma have not been established. All long-acting beta-2 agonists, including arformoterol, are contraindicated in patients with asthma without use of a long-term asthma control medication.
Monitor patients with hepatic impairment closely. Assess serum potassium and serum glucose during therapy.
Category C .
Safety and efficacy not established.
Immediate hypersensitivity reactions may occur.
Special Risk Patients
Use with caution in patients with convulsive disorders or thyrotoxicosis, and in patients who are unusually responsive to sympathomimetic amines.
Acute respiratory events
Arformoterol is not indicated for the treatment of acute episodes of bronchospasm (ie, rescue therapy). Arformoterol has not been studied in the relief of acute symptoms; do not use extra doses for that purpose. When prescribing arformoterol, also provide the patient with an inhaled, short-acting beta-2 agonist for treatment of COPD symptoms that occur acutely, despite regular twice-daily (morning and evening) use of arformoterol.
Can cause clinically important CV effects; therefore, use with caution in patients with CV disorders, especially coronary insufficiency, cardiac arrhythmia, and hypertension.
Increasing inhaled beta-2 agonist use is a signal of deteriorating disease for which prompt medical attention is indicated. Do not initiate arformoterol in patients with acutely deteriorating COPD, which may be a life-threatening condition. The use of arformoterol in this setting is inappropriate.
Clinically significant changes in blood glucose were infrequent during clinical studies with long-term administration of arformoterol at the recommended dose.
May produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse CV effects. The decrease in serum potassium is usually transient and does not require supplementation.
If paradoxical bronchospasm occurs, discontinue arformoterol and institute alternative therapy.
Angina, arrhythmias, cardiac arrest, death, dizziness, dry mouth, fatigue, headache, hyperglycemia, hypertension, hypokalemia, hypotension, insomnia, malaise, metabolic acidosis, muscle cramp, nausea, nervousness, palpitation, tachycardia, tremor.
- Advise patient to read the Medication Guide before using product the first time and with each refill.
- Inform patient that arformoterol 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 the medication to stop using it and inform health care provider immediately.
- Inform patients that arformoterol may increase the risk of asthma-related death.
- Inform patient that arformoterol is not indicated to relieve acute respiratory symptoms and not to use extra doses for this purpose. Treat acute symptoms with an inhaled, short-acting beta-2 agonist.
- Instruct patients who have used a short-acting beta-2 agonist on a regular basis when treatment with arformoterol was started to discontinue the regular use of the short-acting agent and use it only for symptomatic relief of acute respiratory symptoms.
- Instruct patient not to use this product more often, at higher than recommended doses, or with other long-acting beta-2 agonists.
- Inform patient that treatment may lead to adverse reactions, such as chest pain, nervousness, palpitations, rapid heart rate, or tremor.
- Instruct patient to use this product by nebulizer only and not to inject or swallow this solution.
- Instruct patients to protect arformoterol vials from light and excessive heat. Store the protective foil pouches under refrigeration between 36° and 46°F. Instruct patients to use the contents of the vial immediately once the foil pouch is opened.
Copyright © 2009 Wolters Kluwer Health.