Mechanism of effect
The pharmacologic effects of β2-adrenoceptor agonist drugs, including arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of proinflammatory mediators from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung.
Pharmacodynamic
While it is recognized that β2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and β1-receptors are the predominant receptors in the heart, data indicate that there are also β2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective β2-agonists may have cardiac effects.
Arformoterol seems to have little or no effect on β1-adrenergic receptors.
Pharmacokinetics
Excretion: Urine (67%); feces (22%)
Onset: 7-20 min
Half-life: 26hr
Peak plasma time: 0.5-3hr
Peak Plasma: 4.3 pg/mL
AUC: 34.5 pg.hr/mL
Protein Bound: 52-65%
Metabolism: uridine diphosphoglucuronosyltransferases (glucuronidation), CYP2D6, CYP2C19 (O-demethylation)
Renal Clearance: 8.9 L/hr
Drug indications
Chronic obstructive pulmonary diseaseDosage
Adult
Chronic Obstructive Pulmonary Disease
15 mcg inhaled via nebulization twice daily (AM & PM)
Not to exceed 30 mcg/day
Pediatric
Saftety and efficacy not established
Drug contraindications
Hypersensitivity to this drug , Concurrency with other long-acting beta2-agonists , Treatment of asthma without a concomitant long-term asthma control medication, such as an inhaled corticosteroidSide effects
Sinusitis , Pain , Diarrhea , chest pain , Dyspnea , Peripheral edema , Rash , Lung disorderInteractions
Drospirenone , Carteolol , Amitriptyline , Ondansetron , Imipramine , Propranolol , Trazodone , Tranylcypromine , glasdegib , Fluticasone and Vilanterol , lofepramine , Panobinostat , Ribociclib , Inotuzumab , Penbutolol , Nadolol , ivosidenib , Levobunolol , Amoxapine , isocarboxazid , protriptyline , cocaine , Pindolol , Maprotiline , Nortriptyline , Carvedilol , Clomipramine , Linezolid , Phenelzine , Trimipramine , Timolol , Desipramine , Doxepin , Sotalol , Labetalol , GemtuzumabAlerts
May cause paradoxical bronchospasm
Safety and efficacy in patients with asthma not established; not indicated for asthma
Long-acting beta2-agonists may increase risk of asthma-related death
Use caution in cardiovascular disorder (arrhythmias, HTN, CAD), hepatic impairment, hypokalemia, thyrotoxicosis, seizure disorders
Risk of hypokalemia (usu transient not requiring supplementation)
Combined with asthma controller medication (e.g., inhaled corticosteroid)
Use only if not adequately controlled by asthma controller medications
Use only for shortest duration of time
Beta2-agonists may increase serum glucose (use with caution in patients with diabetes)
Black Box Warnings
Long-acting beta2-adrenergic agonists (LABAs), such as arformoterol, may increase the risk of asthma-related deaths; therefore, when treating patients with asthma, this drug should only be used as additional therapy for patients not adequately controlled on other asthma controller medications (eg, low-to-medium dose inhaled corticosteroids) or whose disease severity clearly warrants initiation of treatment with 2 maintenance therapies, including LABAs
Because of this risk, use of LABAs for the treatment of asthma without a concomitant long-term asthma control medication, such as an inhaled corticosteroid, is contraindicated
Once asthma control is achieved and maintained, assess the patient at regular intervals and step down therapy (eg, discontinue LABA) if possible without loss of asthma control, and maintain the patient on a long-term asthma control medication, such as an inhaled corticosteroid
Do not use LABAs if asthma is adequately controlled on low or medium dose inhaled corticosteroids
Available data from controlled clinical trials suggest that LABA increase the risk of asthma-related hospitalization in pediatric and adolescent patients; for pediatric and adolescent patients with asthma who require addition of a LABA to an inhaled corticosteroid, a fixed-dose combination product containing both an inhaled corticosteroid and LABA should ordinarily be considered to ensure adherence with both drugs
Safety and efficacy of arformoterol in patients with asthma not established
Points of recommendation
- Tell all of your health care providers that you take arformoterol. This includes your doctors, nurses, pharmacists, and dentists.
- If you have high blood sugar (diabetes), arformoterol may sometimes raise blood sugar. Talk with your doctor about how to keep your blood sugar under control.
- Call your doctor right away if your breathing problems get worse, if your rescue inhaler does not work as well, or if you need to use your rescue inhaler more often.
- Do not take more of arformoterol or use it more often than you have been told. Deaths have happened when too much of this type of drug has been taken. Talk with your doctor.
- Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using arformoterol while you are pregnant.
- Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.
- To gain the most benefit, do not miss doses.
- Keep using arformoterol as you have been told by your doctor or other health care provider, even if you feel well.
- Do not swallow arformoterol.
- Do not inject arformoterol.
- Only use the type of nebulizer that you have been told to use. If you are not sure what type of nebulizer to use, talk with the doctor.
- Each container is for one use only. Use right after opening. Throw away any part of the opened container after you have used your dose.
- Take doses about 12 hours apart.
- Do not mix other drugs in nebulizer.
- Do not use if the solution is cloudy, leaking, or has particles.
- Do not use if solution changes color.
What do I do if I miss a dose?
- Skip the missed dose and go back to your normal time.
- Do not take 2 doses at the same time or extra doses.
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