DrugindexOnline^{2nd edition}

Pronouncation: (ar-for-MOE-ter-ole TAR-trate)
Class: Sympathomimetic

Trade Names:
Brovana
- Solution for inhalation 15 mcg

Mechanism of Action

Pharmacology

Relaxes bronchial smooth muscles.

Pharmacokinetics

Absorption

C _max is 4.3 pg/mL and occurs approximately 0.5 h after administration.

Distribution

In vitro plasma protein binding is 52% to 65%.

Metabolism

Metabolized primarily by direct conjugation (glucuronidation) and secondarily by demethylation (CYP2D6 and, to a lesser degree, CYP2C19).

Elimination

After 14 days, 67% is recovered in urine and 22% in feces.

Indications and Usage

Long-term maintenance treatment of bronchoconstriction in COPD, including bronchitis and emphysema.

Contraindications

History of hypersensitivity to arformoterol, racemic formoterol, or any component of the product.

Dosage and Administration

Adults

Inhalation 15 mcg twice daily (morning and evening) by nebulization (max, 30 mcg/day).

Storage/Stability

Store in the protective foil pouch under refrigeration at 36° to 46°F. Protect from light and excessive heat. Once foil pouch is opened, use contents of vial immediately. Discard any vial if solution is not colorless. Unopened foil pouch also may be stored at room temperature (68° to 77°F) for up to 6 wk.

Drug Interactions

Adrenergic drugs

Arformoterol sympathomimetic effects may be potentiated.

Beta-blockers

Effects of both agents may be inhibited.

Diuretics, methylxanthines (eg, aminophylline, theophylline), steroids

May potentiate the hypokalemic effect of arformoterol.

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

Arformoterol may potentiate these agents, increasing the risk of cardiac arrhythmias.

Non-potassium-sparing diuretics (eg, loop or thiazide diuretics)

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

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Arteriosclerosis, atrial flutter, AV block, CHF, heart block, inverted T-wave, MI, QT interval prolongation, supraventricular tachycardia (less than 2%).

CNS

Agitation, cerebral infarct, circumoral paresthesia, hypokinesia, paralysis, somnolence, tremor (less than 2%).

Dermatologic

Rash (4%); dry skin, herpes simplex, herpes zoster, skin discoloration, skin hypertrophy (less than 2%).

EENT

Abnormal vision, glaucoma (less than 2%).

GI

Diarrhea (6%); constipation, gastritis, melena, oral moniliasis, periodontal abscess, rectal hemorrhage (less than 2%).

Genitourinary

Breast neoplasm, calcium crystalluria, cystitis, glycosuria, hematuria, increased prostate-specific antigen, kidney calculus, nocturia, pyuria, urinary tract disorder, urine abnormality (less than 2%).

Metabolic-Nutritional

Decreased glucose tolerance, dehydration, edema, gout, hyperglycemia, hyperlipemia, hypoglycemia, hypokalemia (less than 2%).

Musculoskeletal

Back pain (6%); leg cramps (4%); arthralgia, arthritis, bone disorder, neck rigidity, pelvic pain, rheumatoid arthritis, tendinous contracture (less than 2%).

Respiratory

Sinusitis (5%); dyspnea (4%); lung disorder, primarily pulmonary or chest congestion (2%); lung carcinoma, respiratory disorder, voice alteration (less than 2%).

Miscellaneous

Pain (8%); chest pain (7%); flu syndrome, peripheral edema (3%); abscess, allergic reaction, digitalis intoxication, fever, hernia, neoplasm, retroperitoneal hemorrhage (less than 2%).

Precautions

Warnings Long-acting beta 2 -adrenergic agonists may increase the risk of asthma-related death.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Acute worsening or deteriorating asthma

Use of arformoterol in these conditions is inappropriate.

COPD

Arformoterol is not indicated for treating acute symptoms of COPD.

CV effects

Can cause clinically important CV effects; therefore, use with caution in patients with CV disorders, especially coronary insufficiency, cardiac arrhythmia, and hypertension.

Paradoxical bronchospasm

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

Hypersensitivity reactions

Immediate hypersensitivity reactions may occur.

Overdosage

Symptoms

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.

Patient Information

• 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.